111 articles for thisTarget

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The following articles (labelled with PubMed ID or TBD) are for your review

PMID	Data	Article Title	Organization
28085275	53	Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.	Bristol-Myers Squibb
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
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
27073051	71	Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.	Bristol-Myers Squibb
26704266	80	Novel phenylalanine derived diamides as Factor XIa inhibitors.	Bristol-Myers Squibb
25592713	37	Pyridine and pyridinone-based factor XIa inhibitors.	Bristol-Myers Squibb
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
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
24405333	69	Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.	Bristol-Myers Squibb
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
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
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
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
22366654	33	2-Amidino analogs of glycine-amiloride conjugates: inhibitors of urokinase-type plasminogen activator.	University Of Louisville
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
18164204	24	Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.	Takeda Pharmaceutical
18053726	364	Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.	Johnson & Johnson Pharmaceutical Research & Development
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
16517159	45	Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.	Abbott
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
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
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
10479288	141	Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.	Rh£Ne-Poulenc Rorer
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
9301673	234	Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine.	Klinikum Der Friedrich-Schiller-Universit£T Jena
2231595	96	Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses.	Abbott Laboratories
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
	24	L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitor	TBA
22285569	107	Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA).	University Of Antwerp
22041058	44	Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.	Bristol-Myers Squibb
20405925	5	Multiple toxin production in the cyanobacterium microcystis: isolation of the toxic protease inhibitor cyanopeptolin 1020.	University Of Basel
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
19908842	84	Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.	National Human Genome Research Institute
19703768	63	Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA).	Berlex Biosciences
19541481	57	Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.	Bristol-Myers Squibb
	25	Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogates	TBA
	61	(N-acyl-N-alkyl)glycyl borolysine analogs: A new class of potent thrombin inhibitors	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
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
18507371	24	Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.	Takeda Pharmaceutical
17905583	2	Geometry of GPPE binding to picrate and to the urokinase type plasminogen activator.	Pedagogical University
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
17420122	18	Selective and dual action orally active inhibitors of thrombin and factor Xa.	Glaxosmithkline
16970403	74	Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position.	University Of Antwerp
16460935	39	A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.	Johnson & Johnson Pharmaceutical Research And Development
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
15801822	28	9-hydroxyazafluorenes and their use in thrombin inhibitors.	Merck Research Laboratories
15582418	103	Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.	Abbott Laboratories
15177456	17	Design and synthesis of oxadiazolidinediones as inhibitors of plasminogen activator inhibitor-1.	Wyeth Research
15149680	58	Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.	Pfizer
15149645	92	Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.	Abbott Laboratories
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
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
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
12639567	135	Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.	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
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
12039584	59	Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors.	Millennium Pharmaceuticals
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
11755350	31	Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 2: (3-Substituted-5-halo-2-pyridinyl)guanidines.	Pfizer
11755349	24	Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines.	Pfizer
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
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
11378359	57	Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.	3-Dimensional Pharmaceuticals
10937736	35	Nonbenzamidine compounds as selective factor Xa inhibitors.	Aventis Pharmaceuticals
10853674	32	Synthesis and biological activity of peptidyl aldehyde urokinase inhibitors.	Corvas International
10698439	68	Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.	Rhone-Poulenc Rorer
10509929	116	Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.	RhôNe-Poulenc Rorer
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
9876114	111	Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase.	Institut FüR Biochemie
9873692	54	Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.	Dupont Pharmaceuticals
9871573	15	Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.	Biotech Research Institute
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
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
7473571	90	Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.	Eli Lilly
1447734	29	Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases.	University Of Illinois
28460818	29	Neutral macrocyclic factor VIIa inhibitors.	Bristol-Myers Squibb Research And Development
	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
27264434	13	3-aminopyrazolopyrazine derivatives as spleen tyrosine kinase inhibitors.	Jilin University
10691684	20	Chiral nonsteroidal affinity ligands for the androgen receptor. 1. Bicalutamide analogues bearing electrophilic groups in the B aromatic ring.	University Of Tennessee At Memphis