341 articles for thisTarget

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PMID	Data	Article Title	Organization
28197309	40	Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors.	Global Blood Therapeutics
27994741	48	Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.	Bristol-Myers Squibb R & D
27663548	7	Design, synthesis, and structure-activity relationship of novel and effective apixaban derivatives as FXa inhibitors containing 1,2,4-triazole/pyrrole derivatives as P2 binding element.	Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)
27612545	37	Synthesis and P1' SAR exploration of potent macrocyclic tissue factor-factor VIIa inhibitors.	Bristol-Myers Squibb Research & Development
27455395	66	Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.	Bristol-Myers Squibb R & D
27015008	51	Atropisomer Control in Macrocyclic Factor VIIa Inhibitors.	Bristol-Myers Squibb Research & Development
26985294	114	Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation.	Southern Research
27073051	71	Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.	Bristol-Myers Squibb
26871940	7	Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure-Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program.	Merck Research Laboratories
26704266	80	Novel phenylalanine derived diamides as Factor XIa inhibitors.	Bristol-Myers Squibb
26421993	44	Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.	Aurigene Discovery Technologies
26318999	70	Development of a novel tricyclic class of potent and selective FIXa inhibitors.	Merck Research Laboratories
25978966	65	Development of a novel class of potent and selective FIXa inhibitors.	Merck Research Laboratories
26114810	8	Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.	Southeast University
25592713	37	Pyridine and pyridinone-based factor XIa inhibitors.	Bristol-Myers Squibb
26151189	56	Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors.	TBA
26005539	23	Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.	Bristol-Myers Squibb
25990761	66	Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin.	Institute For Infection Research
25937013	40	Rapid development of two factor IXa inhibitors from hit to lead.	Merck Research Laboratories
25911624	121	Design, synthesis and structure-activity relationship of oxazolidinone derivatives containing novel S4 ligand as FXa inhibitors.	Shenyang Pharmaceutical University
25839438	19	Identification of anthranilamide derivatives as potential factor Xa inhibitors: drug design, synthesis and biological evaluation.	China Pharmaceutical University
25881820	62	Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors.	Bristol-Myers Squibb R & D
25728130	79	Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.	Bristol-Myers Squibb
25559742	6	Design, synthesis and evaluation of isoxazolo[5,4-d]pyrimidin-4(5H)-one derivatives as antithrombotic agents.	Southeast University
24951330	25	Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.	Bristol-Myers Squibb
25523211	18	Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system.	Astellas Pharma
25453807	13	A simple, general approach of allosteric coagulation enzyme inhibition through monosulfated hydrophobic scaffolds.	Virginia Commonwealth University
25438755	9	Novel strategy to boost oral anticoagulant activity of blood coagulation enzyme inhibitors based on biotransformation into hydrophilic conjugates.	Astellas Pharma
25405503	109	Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.	Bristol-Myers Squibb
25268757	16	How aß-D-glucoside side chain enhances binding affinity to thrombin of inhibitors bearing 2-chlorothiophene as P1 moiety: crystallography, fragment deconstruction study, and evaluation of antithrombotic properties.	Consiglio Nazionale Delle Ricerche
25179681	81	Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor.	Chinese Academy Of Sciences
15125936	61	Novel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand.	Aventis Pharma Deutschland
24405333	69	Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.	Bristol-Myers Squibb
24461292	14	Heterocyclic core analogs of a direct thrombin inhibitor.	Merck Research Laboratories
24418773	61	Design, synthesis, and SAR of a series of activated protein C (APC) inhibitors with selectivity against thrombin for the treatment of haemophilia.	Astrazeneca
24900796	42	Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.	Bristol-Myers Squibb R & D
24900621	48	Discovery of Pyridyl Bis(oxy)dibenzimidamide Derivatives as Selective Matriptase Inhibitors.	Aurigene Discovery Technologies
24175584	35	5-Chlorothiophene-2-carboxylic acid [(S)-2-[2-methyl-3-(2-oxopyrrolidin-1-yl)benzenesulfonylamino]-3-(4-methylpiperazin-1-yl)-3-oxopropyl]amide (SAR107375), a selective and potent orally active dual thrombin and factor Xa inhibitor.	Sanofi-Aventis R&D
24102612	105	Synthesis and biological evaluation of direct thrombin inhibitors bearing 4-(piperidin-1-yl)pyridine at the P1 position with potent anticoagulant activity.	University Of Bari &Quot;Aldo Moro&Quot
23845220	53	Nonbenzamidine acylsulfonamide tissue factor-factor VIIa inhibitors.	Bristol-Myers Squibb R & D
23927973	41	Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold.	Bristol-Myers Squibb Research & Development
23899618	9	Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug.	Lg Life Sciences
23478148	10	Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor.	Bristol-Myers Squibb Pharmaceutical Research Institute
23644213	57	Low molecular weight dual inhibitors of factor Xa and fibrinogen binding to GPIIb/IIIa with highly overlapped pharmacophores.	University Of Ljubljana
23602442	28	Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.	Bristol-Myers Squibb
23416003	52	Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.	Bristol-Myers Squibb R & D
23376251	32	Towards dual antithrombotic compounds - balancing thrombin inhibitory and fibrinogen GPIIb/IIIa binding inhibitory activities of 2,3-dihydro-1,4-benzodioxine derivatives through regio- and stereoisomerism.	University Of Ljubljana
23379567	2	Torsion angle preferences in druglike chemical space: a comprehensive guide.	University Of Hamburg
23294255	114	Development of new cyclic plasmin inhibitors with excellent potency and selectivity.	Philipps University Marburg
21443196	38	Local structural changes, global data views: graphical substructure-activity relationship trailing.	Rheinische Friedrich-Wilhelms-Universita£T
16644215	52	Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.	Celera Genomics
12565961	177	Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors.	Berlex Biosciences
21413808	170	Synopsis of some recent tactical application of bioisosteres in drug design.	Bristol-Myers Squibb Pharmaceutical Research And Development
22788964	2	Designing allosteric regulators of thrombin. Monosulfated benzofuran dimers selectively interact with Arg173 of exosite 2 to induce inhibition.	Virginia Commonwealth University
21732671	4	Polysulfated xanthones: multipathway development of a new generation of dual anticoagulant/antiplatelet agents.	Universidade Do Porto (Cequimed-Up)
23124211	22	Synthesis and structure-activity relationship of potent, selective and orally active anthranilamide-based factor Xa inhibitors: application of weakly basic sulfoximine group as novel S4 binding element.	Zydus Research Centre
22770607	54	Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.	Virginia Commonwealth University
22276953	63	A new strategy for the development of highly potent and selective plasmin inhibitors.	Philipps University Marburg
20503967	138	Factor Xa inhibitors: next-generation antithrombotic agents.	Bristol-Myers Squibb
20121198	63	Studies of benzothiophene template as potent factor IXa (FIXa) inhibitors in thrombosis.	Trigen
19861238	14	Synthesis and biological evaluation of the metabolites of 2-(1-{3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl}piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one.	Takeda Pharmaceutical
19715320	87	Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.	University Of Florida
18424044	32	Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.	Bristol-Myers Squibb Research And Development
18164204	24	Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.	Takeda Pharmaceutical
18329876	53	Sulfonamidolactam inhibitors of coagulation factor Xa.	Bristol-Myers Squibb
18053726	364	Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.	Johnson & Johnson Pharmaceutical Research & Development
18053714	20	Structure and property based design of factor Xa inhibitors: biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs.	Glaxosmithkline
18039572	22	Design, synthesis, and biological activity of piperidine diamine derivatives as factor Xa inhibitor.	Daiichi Sankyo
18077174	31	Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors.	Takeda Pharmaceutical
18054227	45	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.	Bristol-Myers Squibb Research And Development
18052026	97	Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.	University Of Antwerp
17588746	103	SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.	Bristol-Myers Squibb
16876411	17	Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa.	Daiichi Asubio Medical Research Laboratories
16517159	45	Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.	Abbott
15887966	58	Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.	Central Pharmaceutical Research Institute
15837303	52	Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.	Berlex Biosciences
15261287	44	Structure-activity relationships of potent and selective factor Xa inhibitors: benzimidazole derivatives with the side chain oriented to the prime site of factor Xa.	Central Pharmaceutical Research Institute
15163182	47	Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.	Merck Research Laboratories
14640539	112	Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1).	Pharmaceutical Research Institute
12954057	113	Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors.	Pharmacia
12904065	30	Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide.	Lg Life Sciences
12036356	234	Design, synthesis, and activity of a novel series of factor Xa inhibitors: optimization of arylamidine groups.	Berlex Biosciences
11170646	106	Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa.	Dupont Pharmaceuticals
10669559	180	Protease inhibitors: current status and future prospects.	University Of Queensland
10956211	14	GRID/CPCA: a new computational tool to design selective ligands.	Boehringer Ingelheim Pharma
10479288	141	Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.	Rh£Ne-Poulenc Rorer
10464012	5	New 4-point pharmacophore method for molecular similarity and diversity applications: overview of the method and applications, including a novel approach to the design of combinatorial libraries containing privileged substructures.	Rh£Ne-Poulenc Rorer
10425086	83	Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1.	Dupont Pharmaceuticals
9836616	92	Tetrahydro-isoquinoline-based factor Xa inhibitors.	Boehringer Mannheim
9357536	47	Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.	Merck Research Laboratories
1527787	11	Synthesis and biological activity of ketomethylene pseudopeptide analogues as thrombin inhibitors.	Thrombosis Research Institute
15081015	91	Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.	The Bristol-Myers Squibb Pharmaceutical Research Institute
14980679	30	Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.	Maxim Pharmaceuticals
12639557	7	Exploring new non-sugar sulfated molecules as activators of antithrombin.	Virginia Commonwealth University
12824035	39	Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors.	Pharmacia
11909707	69	Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1.	Life Science R & D, Lgci
11858993	60	Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds.	Corvas International
10698459	41	The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.	Dupont Pharmaceuticals
10915051	43	The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position.	Novartis Horsham Research Centre
10340604	22	Solution-phase and solid-phase synthesis of novel transition state inhibitors of coagulation enzymes incorporating a piperidinyl moiety.	Research And Development
	43	S1 heterocyclic thrombin inhibitors	TBA
22365562	154	Fluorinated dual antithrombotic compounds based on 1,4-benzoxazine scaffold.	University Of Ljubljana
22192588	9	Structure-based library design and the discovery of a potent and selective mast cellß-tryptase inhibitor as an oral therapeutic agent.	Sanofi Pharmaceuticals
22047802	8	The arginine mimickingß-amino acidß³hPhe(3-H2N-CH2) as S1 ligand in cyclotheonamide-basedß-tryptase inhibitors.	Universit£T Bielefeld
22044620	36	Orally active zwitterionic factor Xa inhibitors with long duration of action.	Daiichi Sankyo
22041058	44	Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.	Bristol-Myers Squibb
21995444	32	Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor.	Astellas Pharma
21741839	83	Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT.	Philipps University Marburg
21641796	30	Design, synthesis and biological activity of novel peptidyl benzyl ketone FVIIa inhibitors.	Technical University Of Denmark
21345673	33	Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors.	Daiichi Sankyo
21349711	19	The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs.	Glaxosmithkline
21349710	21	Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs.	Glaxosmithkline
21316975	23	2-aminomethylphenylamine as a novel scaffold for factor Xa inhibitor.	Daiichi Sankyo
21168329	47	New furin inhibitors based on weakly basic amidinohydrazones.	Philipps University Marburg
20650636	118	Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate.	F. Hoffmann-La Roche
20355714	26	Discovery of a tetrahydropyrimidin-2(1H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor.	Takeda Pharmaceutical
20102150	35	Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.	Johnson & Johnson Pharmaceutical Research And Development
20121197	148	Structure based drug design: development of potent and selective factor IXa (FIXa) inhibitors.	Trigen
20100660	28	Phenyltriazolinones as potent factor Xa inhibitors.	Bristol-Myers Squibb
20006499	24	Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs.	Glaxosmithkline
20038105	50	Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.	Philipps University Marburg
19541481	57	Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.	Bristol-Myers Squibb
19200624	32	Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit.	F. Hoffmann-La Roche
19181521	69	Design, synthesis, and biological evaluation of 1,5-benzothiazepine-4-one derivatives targeting factor VIIa/tissue factor.	University Of Montpellier
19193009	25	Fluorinated benzyloxyphenyl piperidine-4-carboxamides with dual function against thrombosis: inhibitors of factor Xa and platelet aggregation.	University Of Bari
	15	Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2–P3 bicyclic lactam moiety	TBA
	37	Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitors	TBA
	32	Bisbenzamidine isoxazoline derivatives as factor Xa inhibitors	TBA
	27	Rational design and synthesis of a novel, selective class of thrombin inhibitors: P1-argininal derivatives incorporating P3---P4 quaternary lactam dipeptide surrogates	TBA
	25	Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogates	TBA
19297158	30	Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR.	Millennium Pharmaceuticals
19297154	88	Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.	Millennium Pharmaceuticals
19250826	100	Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors.	The Medicines Company (Leipzig)
19231206	20	Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action.	Pfizer
19128974	28	Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa.	Daiichi Sankyo
19046881	61	Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.	Bristol-Myers Squibb
19036586	128	Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors.	Curacyte Discovery
18729445	70	3,4-Dihydro-2H-1,4-benzoxazine derivatives combining thrombin inhibitory and glycoprotein IIb/IIIa receptor antagonistic activity as a novel class of antithrombotic compounds with dual function.	University Of Ljubljana
18675545	9	Stereoselective synthesis and biological evaluation of 3,4-diaminocyclohexanecarboxylic acid derivatives as factor Xa inhibitors.	Daiichi Sankyo
18674905	58	Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination.	Chugai Pharmaceutical
18667303	27	Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy.	Kissei Pharmaceutical
18644722	36	Synthesis and evaluation of acylguanidine FXa inhibitors.	Bristol-Myers Squibb Research And Development
18550370	33	Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.	Bristol-Myers Squibb
18507371	24	Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.	Takeda Pharmaceutical
18412326	16	Novel potent and selective thrombin inhibitors based on a central 1,4-benzoxazin-3(4H)-one scaffold.	University Of Ljubljana
9834152	29	Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade.	National University Of Singapore
18159923	24	7-fluoroindazoles as potent and selective inhibitors of factor Xa.	Johnson & Johnson Pharmaceutical Research And Development
18054228	23	Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs.	Glaxosmithkline
17933529	35	Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
17855089	25	Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
17643988	92	Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.	Bristol-Myers Squibb
17583500	31	Aminopyrrolidineamide inhibitors of site-1 protease.	Pfizer
17566736	60	Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa.	Pfizer
17555959	27	Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors.	Daiichi Pharmaceutical
17462889	110	From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3.	Curacyte Discovery
17420122	18	Selective and dual action orally active inhibitors of thrombin and factor Xa.	Glaxosmithkline
17416533	39	Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors.	Astellas Pharma
17064913	29	Design, synthesis and biological activity of selective and orally available TF/FVIIa complex inhibitors containing non-amidine P1 ligands.	Astellas Pharma
16793264	13	Potent 4-amino-5-azaindole factor VIIa inhibitors.	Celera Genomics
16714109	40	Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles.	Celera
16540315	23	Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors.	Mochida Pharmaceutical
16460935	39	A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.	Johnson & Johnson Pharmaceutical Research And Development
16257204	37	Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.	Celera
16213711	37	Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
16137886	88	Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.	Merck Research Laboratories
16125385	55	The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex.	Pfizer
15501047	75	Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.	Merck
15456260	21	Synthesis and conformational analysis of a non-amidine factor Xa inhibitor that incorporates 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine as S4 binding element.	Daiichi Pharmaceutical
15203158	84	Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.	Merck
15203149	72	Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition.	Aventis Pharma Deutschland
15149685	55	Novel thrombin inhibitors incorporating weakly basic heterobicyclic P1-arginine mimetics: optimization via modification of P1 and P3 moieties.	University Of Ljubljana
15149641	44	A novel series of potent and selective small molecule inhibitors of the complement component C1s.	3-Dimensional Pharmaceuticals
15125963	20	Orally active factor Xa inhibitors: 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine derivatives.	Daiichi Pharmaceutical
15115382	16	Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.	University Of Antwerp
15081014	35	Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase.	The Bristol-Myers Squibb Pharmaceutical Research Institute
15080981	72	N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors.	Millennium Pharmaceuticals
15013007	319	Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.	Millennium Pharmaceuticals
15013006	69	Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs.	Millennium Pharmaceuticals
15006404	56	Thrombin inhibitors built on an azaphenylalanine scaffold.	University Of Ljubljana
14980671	78	1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.	Millennium Pharmaceuticals
14980670	107	1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs.	Millennium Pharmaceuticals
14698147	60	Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.	The Bristol-Myers Squibb Pharmaceutical Research Institute
14667222	74	Analyses of activity for factor Xa inhibitors based on Monte Carlo simulations.	Yale University
14552766	12	Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex.	Pharmacia
14552764	5	A general synthesis of 1-aryl carbamoyl-2-alkyl-4-aryl substituted semicarbazides as nonbasic factor Xa inhibitors.	Merck
12951087	23	Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics.	University Of Ljubljana
12824026	14	Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.	Pharmacia
12824021	39	Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents.	Boehringer Ingelheim Pharma
12824020	31	Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.	Boehringer Ingelheim Pharma
12729667	47	Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library.	Bristol-Myers Squibb
12723948	30	Rational design, synthesis, and structure-activity relationships of novel factor Xa inhibitors: (2-substituted-4-amidinophenyl)pyruvic and -propionic acids.	Ajinomoto
12668020	29	Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.	3-Dimensional Pharmaceuticals
12668013	42	Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors.	Aventis Pharma Deutschland
12643903	81	Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors.	Bristol-Myers Squibb
12639568	52	Design, synthesis, and structure-activity relationships of substituted piperazinone-based transition state factor Xa inhibitors.	Millennium Pharmaceuticals
12639567	135	Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.	Millennium Pharmaceuticals
12617892	43	Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics.	University Of Ljubljana
12593666	30	Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.	Senju Pharmaceutical
12593648	53	Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.	Aventis Pharmaceuticals
12565972	69	Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors.	Millennium Pharmaceuticals
12565931	37	Nonbenzamidine tetrazole derivatives as factor Xa inhibitors.	Bristol-Myers Squibb
12482444	38	Design and synthesis of factor Xa inhibitors and their prodrugs.	Millennium Pharmaceuticals
12372529	21	Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.	Bristol-Myers Squibb Pharmaceutical Research Institute
12113838	36	Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification.	Millennium Pharmaceuticals
12113833	183	4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.	Celera
12113832	120	2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.	Celera
12039587	39	Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.	Aventis Pharmaceuticals
12039586	42	Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency.	Aventis Pharmaceuticals
12039584	59	Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors.	Millennium Pharmaceuticals
12039583	140	Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides.	Millennium Pharmaceuticals
12031331	48	Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.	Millennium Pharmaceuticals
11965378	78	Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity.	Berlex Biosciences
11965377	66	Design and synthesis of aminophenol-based factor Xa inhibitors.	Berlex Biosciences
11960487	30	Structure-based design of novel potent nonpeptide thrombin inhibitors.	Boehringer Ingelheim Pharma
11958994	31	Benzimidazoles and isosteric compounds as potent and selective factor Xa inhibitors.	Aventis Pharmaceuticals
11934589	57	Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates.	Corvas International
11934583	20	Novel bicyclic lactam inhibitors of thrombin: highly potent and selective inhibitors.	Shire Biochem
11881991	21	PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors.	Protherics Molecular Design
11844691	107	4-amidinobenzylamine-based inhibitors of urokinase.	Universitat Jena
11689072	49	Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.	Axys Pharmaceuticals
11677132	65	Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors.	Cor Therapeutics
11527714	66	Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors.	Cor Therapeutics
11527709	19	Optimization of a screening lead for factor VIIa/TF.	Axys Pharmaceuticals
11495587	198	Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa.	Axys Pharmaceuticals
11459634	94	Development of potent and selective factor Xa inhibitors.	Axys Pharmaceuticals
11266180	74	The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa.	Prosthetics Molecular Design
11266160	57	Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core.	Dupont Pharmaceuticals
11206465	13	Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors.	Aventis Pharma
11087565	86	Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.	Dupont Pharmaceuticals
11063603	53	Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors.	Pfizer
11055344	37	Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties.	Corvas International
10937736	35	Nonbenzamidine compounds as selective factor Xa inhibitors.	Aventis Pharmaceuticals
10866393	24	Synthesis and activity studies of conformationally restricted alpha-ketoamide factor Xa inhibitors.	Dupont Pharmaceuticals
10853669	102	Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.	Berlex Biosciences
10853668	52	Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.	Berlex Biosciences
10782677	73	Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa.	Corvas International
10782664	42	Isoxazolines and isoxazoles as factor Xa inhibitors.	Dupont Pharmaceuticals
10698439	68	Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.	Rhone-Poulenc Rorer
10639283	135	Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors.	Berlex Biosciences
10636250	20	Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines.	3-Dimensional Pharmaceuticals
10636232	58	Design, synthesis and structure-activity relationship of a series of arginine aldehyde factor Xa inhibitors. Part 1: structures based on the (D)-Arg-Gly-Arg tripeptide sequence.	Cor Therapeutics
10617091	73	Exploratory solid-phase synthesis of factor Xa inhibitors: discovery and application of p3-heterocyclic amides as novel types of non-basic arginine surrogates.	Corvas International
10509929	116	Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.	RhôNe-Poulenc Rorer
10508439	4	Conformations of trypsin-bound amidine inhibitors of blood coagulant factor Xa by double REDOR NMR and MD simulations.	Washington University
10498211	42	Novel benzo-fused lactam scaffolds as factor Xa inhibitors.	Corvas International
10425087	110	Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2.	Dupont Pharmaceuticals
10397495	49	Thrombin inhibitors based on [5,5] trans-fused indane lactams.	Glaxo Wellcome Research And Development
10346927	114	Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.	Berlex Biosciences
10328312	27	Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa.	Dupont Pharmaceuticals
10230630	36	Thrombin inhibitors based on a propargylglycine template.	Biotech Research Institute
10212122	35	Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.	Molecumetics
10206557	36	Investigation of the S3 site of thrombin: design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals.	Corvas International
9934495	26	Alkoxide-catalyzed ring-opening of a novel homosaccharin derivative: synthesis of potent, selective P3-lactam thrombin inhibitors containing P4-o-alkoxycarbonylbenzylsulfonamide residues.	Corvas International
9873607	21	The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies.	Dupont Pharmaceuticals
9873569	16	Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates.	Corvas International
9873520	27	Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.	Berlex Biosciences
9873451	19	Solid-phase synthesis of N-substituted amidinophenoxy pyridines as factor XA inhibitors.	Berlex Biosciences
9873397	37	In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.	3-Dimensional Pharmaceuticals
9871674	34	Rational design of boropeptide thrombin inhibitors: beta, beta-dialkyl-phenethylglycine P2 analogs of DuP 714 with greater selectivity over complement factor I and an improved safety profile.	Dupont Pharmaceuticals
9871573	15	Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.	Biotech Research Institute
9871540	100	Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.	Dupont Pharmaceuticals
9822554	14	1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.	Bristol-Myers Squibb Pharmaceutical Research Institute
9784099	84	Design of benzamidine-type inhibitors of factor Xa.	Institut FüR Biochemie
9733491	21	Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors.	Novartis Pharma
9733480	93	Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa.	Berlex Biosciences
9733479	18	(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa.	Berlex Biosciences
9484495	74	Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa.	Collegeville
9438022	55	Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors.	Dupont Pharmaceuticals
9371237	69	Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.	Merck Research Laboratories
9171866	12	Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy.	Merck Research Laboratories
8917639	50	Design, synthesis, and evolution of a novel, selective, and orally bioavailable class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 lactam sulfonamide moieties.	Corvas International
8917638	26	Potent and selective thrombin inhibitors incorporating the constrained arginine mimic l-3-piperidyl(N-guanidino)alanine at P1.	Corvas International
8426361	111	Highly selective tripeptide thrombin inhibitors.	Eli Lilly
8164262	38	Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors.	Daiichi Pharmaceutical
8035417	23	Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.	Bristol-Myers Squibb Pharmaceutical Research Institute
7739010	118	Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.	Thrombosis Research Institute
	18	Novel multi-targeted agents for Alzheimer's disease: Synthesis, biological evaluation, and molecular modeling of novel 2-[4-(4-substitutedpiperazin-1-yl)phenyl]benzimidazoles	Hacettepe University
12065740	8	8-Carboxamidocyclazocine: a long-acting, novel benzomorphan.	University Of Rochester
12065738	9	Characterization of the diarylether sulfonylester (-)-(R)-3-(2-hydroxymethylindanyl-4-oxy)phenyl-4,4,4-trifluoro-1-sulfonate (BAY 38-7271) as a potent cannabinoid receptor agonist with neuroprotective properties.	Bayer
11714875	18	Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.	Vrije Universiteit
9802391	31	The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4.	Uppsala University
19895505	11	Synthesis and pharmacological evaluation of analogs of indole-based cannabimimetic agents.	UniversitÀ
9383464	20	Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol.	University Of California San Diego
9195867	15	Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D.	University Of California Berkeley
18030989	56	Picomolar inhibitors as transition-state probes of 5'-methylthioadenosine nucleosidases.	Albert Einstein College Of Medicine
20383151	2	Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.	Dana-Farber Cancer Institute
19648931	16	Design, synthesis and selection of DNA-encoded small-molecule libraries.	Praecis Pharmaceuticals
19305397	22	Molecular docking and ligand specificity in fragment-based inhibitor discovery.	University Of California San Francisco
	28	A Thermodynamic Study of the Reactions of Cyclodextrins with Primary and Secondary Aliphatic Alcohols, with D- and L-Phenylalanine, and with L-Phenylalanine Amide	Nist
19645448	48	ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin: Design and Synthesis of Highly Potent and Selective Pyrazolopyrimidines	Wyeth Research
19884013	98	5-Vinyl-3-pyridinecarbonitrile inhibitors of PKCtheta: optimization of enzymatic and functional activity.	Wyeth Research
19162487	34	Biarylether amide quinolines as liver X receptor agonists.	Wyeth Research
19842661	140	Discovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM) kinases.	Abbott Laboratories
19699645	12	Design, synthesis, and biological evaluation of hydroquinone derivatives as novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase.	Northern Kentucky University
17184135	28	HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site.	Rutgers University
19572549	30	Identification of inhibitors of checkpoint kinase 1 through template screening.	The Institute Of Cancer Research