195 articles for thisTarget

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PMID	Data	Article Title	Organization
27287367	36	Evaluation of bisbenzamidines as inhibitors for matriptase-2.	University of Bonn
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
26732532	69	Active site-directed plasmin inhibitors: Extension on the P2 residue.	Kobe Gakuin University
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
26367391	6	Phenylalanine and Phenylglycine Analogues as Arginine Mimetics in Dengue Protease Inhibitors.	Heidelberg University
26393374	34	Improving the Selectivity of Engineered Protease Inhibitors: Optimizing the P2 Prime Residue Using a Versatile Cyclic Peptide Library.	Queensland University of Technology
26114810	8	Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.	Southeast University
26122211	3	Discovery of non-competitive thrombin inhibitor derived from competitive tryptase inhibitor skeleton: Shift in molecular recognition resulted from skeletal conversion of carboxylate into phosphonate.	Tokyo University of Pharmacy and Life Sciences
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
25782055	9	Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.	Rempex Pharmaceuticals
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
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
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
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
23586812	38	Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy.	Ecole Polytechnique F�D�Rale De Lausanne Epfl
23294255	114	Development of new cyclic plasmin inhibitors with excellent potency and selectivity.	Philipps University Marburg
10602702	22	Simple linear QSAR models based on quantum similarity measures.	Czech Academy of Sciences
22726924	14	Discovery of benzothiazole guanidines as novel inhibitors of thrombin and trypsin IV.	Astrazeneca
16250649	10	Selective inhibitors of the serine protease plasmin: probing the S3 and S3' subsites using a combinatorial library.	Brown University
15887966	58	Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.	Central Pharmaceutical Research Institute
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
12930148	41	Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone.	Johnson & Johnson Pharmaceutical Research & Development
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
12190311	37	Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151).	Gsk
12036356	234	Design, synthesis, and activity of a novel series of factor Xa inhibitors: optimization of arylamidine groups.	Berlex Biosciences
12036355	36	Simple, intuitive calculations of free energy of binding for protein-ligand complexes. 1. Models without explicit constrained water.	University of Parma
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
10794696	233	Protease inhibitors: synthesis and QSAR study of novel classes of nonbasic thrombin inhibitors incorporating sulfonylguanidine and O-methylsulfonylisourea moieties at P1.	Universit£
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
10425086	83	Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1.	Dupont Pharmaceuticals
9464370	28	Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.	Merck Research Laboratories
9836616	92	Tetrahydro-isoquinoline-based factor Xa inhibitors.	Boehringer Mannheim
9083470	9	Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site.	Merck Research Laboratories
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
2319567	29	Analogues of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) in the treatment of experimental Pneumocystis carinii pneumonia.	University of North Carolina
15081015	91	Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.	The Bristol-Myers Squibb Pharmaceutical Research Institute
12873514	56	Design and synthesis of potent and selective macrocyclic thrombin inhibitors.	Merck Research Laboratories
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
10201829	9	1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors.	Nv Organon
10522702	26	Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors.	Nv Organon
10498204	25	Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.	Rh£Ne-Poulenc Rorer
9873373	20	Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases).	Institute For Drug Research
	24	L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitor	TBA
	43	S1 heterocyclic thrombin inhibitors	TBA
19841155	29	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.	Merck Research Laboratories
	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
	44	Biaryl substituted alkylboronate esters as thrombin inhibitors	TBA
	3	An efficient preparation of the potent and selective pseudopeptide thrombin inhibitor, inogatran	TBA
	25	Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogates	TBA
	15	RATIONAL DESIGN, SYNTHESIS, AND SERINE PROTEASE INHIBITORY ACTIVITY OF NOVEL P1-ARGININOYL HETEROCYCLES	TBA
	78	Synthesis and evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease inhibitors	TBA
	61	(N-acyl-N-alkyl)glycyl borolysine analogs: A new class of potent thrombin inhibitors	TBA
16759084	12	Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors.	Peking University
16137886	88	Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.	Merck Research Laboratories
15801822	28	9-hydroxyazafluorenes and their use in thrombin inhibitors.	Merck Research Laboratories
15501047	75	Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.	Merck
15341970	59	P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.	Eli Lilly
15203158	84	Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.	Merck
15149645	92	Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.	Abbott Laboratories
15149641	44	A novel series of potent and selective small molecule inhibitors of the complement component C1s.	3-Dimensional Pharmaceuticals
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
14761180	31	Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G.	Johnson & Johnson Pharmaceutical Research & Development
14711304	117	Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.	Abbott Laboratories
14698147	60	Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.	The Bristol-Myers Squibb Pharmaceutical Research Institute
14505652	45	Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.	Merck Research Laboratories
12824026	14	Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.	Pharmacia
12824020	31	Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.	Boehringer Ingelheim Pharma
12668020	29	Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.	3-Dimensional Pharmaceuticals
12668008	34	3-amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors.	Merck Research Laboratories
12643903	81	Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors.	Bristol-Myers Squibb
12639567	135	Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.	Millennium Pharmaceuticals
12617893	28	Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors.	Merck Research Laboratories
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
12570369	60	Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.	Merck Research Laboratories
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
12482415	30	Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.	Merck Research Laboratories
12113838	36	Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification.	Millennium Pharmaceuticals
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
12036353	38	Design of selective thrombin inhibitors based on the (R)-Phe-Pro-Arg sequence.	Pfizer
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
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
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
11425524	62	Dibasic inhibitors of human mast cell tryptase. Part 3: identification of a series of potent and selective inhibitors containing the benzamidine functionality.	Axys Pharmaceuticals
11378359	57	Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.	3-Dimensional 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
11212109	14	The identification of alpha-ketoamides as potent inhibitors of hepatitis C virus NS3-4A proteinase.	Roche Discover Welwyn
11212093	21	Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors.	Biochem Pharma
11087565	86	Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.	Dupont Pharmaceuticals
11078188	20	1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.	Shionogi
11063603	53	Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors.	Pfizer
11055356	236	Dibasic inhibitors of human mast cell tryptase. Part 2: structure-activity relationships and requirements for potent activity.	Axys Pharmaceuticals
11055355	72	Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors.	Axys Pharmaceuticals
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
10915052	20	The design and synthesis of thrombin inhibitors: the introduction of in vivo efficacy and oral bioavailability into benzthiazolylalanine inhibitors.	Novartis Horsham Research Centre
10866385	13	Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin.	The Oxford Centre For Molecular Sciences
10853668	52	Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.	Berlex Biosciences
10843219	20	Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors.	Merck Research Laboratories
10782677	73	Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa.	Corvas International
10698439	68	Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.	Rhone-Poulenc Rorer
10669563	7	Structural basis of the thrombin selectivity of a ligand that contains the constrained arginine mimic (2S)-2-amino-(3S)-3-(1-carbamimidoyl- piperidin-3-yl)-propanoic acid at P1.	Warner-Lambert
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
10498211	42	Novel benzo-fused lactam scaffolds as factor Xa inhibitors.	Corvas International
10498197	58	The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 2.	Warner-Lambert
10498196	42	The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1.	Warner-Lambert
10425106	12	4-Heterocyclohexanone-based inhibitors of the serine protease plasmin.	Brown University
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
10328312	27	Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa.	Dupont Pharmaceuticals
10328293	23	The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore.	Novartis Horsham Research Centre
10230612	22	Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.	Dupont Pharmaceuticals
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
10206546	27	Potent and selective bicyclic lactam inhibitors of thrombin: Part 3: P1' modifications.	Warner-Lambert
10206542	50	Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease.	Warner-Lambert
10091694	90	Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors.	Nippon Steel
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
9873743	13	Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications.	Warner-Lambert
9873692	54	Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.	Dupont Pharmaceuticals
9873654	37	5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.	Glaxo Wellcome Research and Development
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
9873535	13	Highly efficient and versatile synthesis of libraries of constrained beta-strand mimetics.	Molecumetics
9873422	16	C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.	Merck Research Laboratories
9873418	16	Identification and SAR for a selective, nonpeptidyl thrombin inhibitor.	Merck Research Laboratories
9871573	15	Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.	Biotech Research Institute
9871547	15	L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.	Merck Research Laboratories
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
9804686	16	Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.	Merck Research Laboratories
9703466	35	Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.	Merck Research Laboratories
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
9379436	46	Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase.	Zeneca Pharmaceuticals
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
8426361	111	Highly selective tripeptide thrombin inhibitors.	Eli Lilly
8035417	23	Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.	Bristol-Myers Squibb Pharmaceutical Research Institute
7629790	32	New orally active serine protease inhibitors.	Minase Research Institute
7562936	10	Synthesis of tight binding inhibitors and their action on the proprotein-processing enzyme furin.	Friedrich Miescher-Institut
7562931	41	Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.	Zeneca Pharmaceuticals
2136920	39	New leupeptin analogues: synthesis and inhibition data.	University of Arkansas
14744476	35	Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity.	Emory University
24058293	12	Modulation of global low-frequency motions underlies allosteric regulation: demonstration in CRP/FNR family transcription factors.	Durham University
10715152	151	5,6-Dihydropyran-2-ones possessing various sulfonyl functionalities: potent nonpeptidic inhibitors of HIV protease.	Parke-Davis Pharmaceutical Research