229343-30-0

Upstream product

• 19798-80-2 2-Amino-4-chloropyridine 
• 4743-17-3 5-Chloroisatoic anhydride 
• 1072-98-6 5-chloro-2-pyridylamine 
• 41994-44-9 5-chloro-2-nitrobenzoyl chloride 
• 280771-82-6 N-(5-chloropyridin-2-yl)-5-chloro-2-nitrobenzamide 

Downstream Products

• 280771-91-7 N-(5-Chloropyridin-2-yl)-2-[(1-Boc-piperidin-3-ene-4-ylcarbonyl)amino]-5-chlorobenzamide 
• 280771-94-0 N-(5-chloropyridin-2-yl)-2-[(1-Boc-piperidin-4-ylcarbonyl)amino]-5-chlorobenzamide 
• 280769-65-5 2-(4-Acetylaminobenzyl)amino-5-chloro-N-(5-chloropyridin-2-yl)benzamide 
• 358660-00-1 5-Chloro-N-(5-chloro-pyridin-2-yl)-2-(4-pyrrolidin-1-ylmethyl-benzoylamino)-benzamide 
• 330940-57-3 N-{4-chloro-2-[N-(5-chloro(2-pyridyl))carbamoyl]phenyl}[4-(1-methyl(2-imidazolin-2-yl))phenyl]carboxamide 
• 330940-94-8 N-(5-chloro(2-pyridyl))(5-chloro-2-{[4-(2-sulfamoylphenyl)-phenyl]carbonylamino}phenyl)-carboxamide 
• 358658-28-3 C₂₂H₁₈Cl₂FN₅O₂ 
• 1147095-62-2 5-chloro-2-(4-(N-(2-chloroacetyl)-S-methylsulfonimidoyl)benzamido)-N-(5-chloropyridin-2-yl)benzamide 
• 1147095-85-9 5-chloro-N-(5-chloropyridin-2-yl)-2-(4-(N-(diethylglycyl)-S-methylsulfonimidoyl)benzamido)benzamide 
• 358661-80-0 5-Chloro-2-(4-chloromethyl-benzoylamino)-N-(5-chloro-pyridin-2-yl)-benzamide 
• 503613-37-4 5-chloro-N-(5-chloropyridin-2-yl)-2-({4-[(2-oxopiperidine)-1-yl]benzoyl}amino)benzamide 
• 1147096-25-0 S-[4-(N-{2-[N-(5-chloro(2-pyridyl))carbamoyl]-4-chlorophenyl}carbamoyl)phenyl]-S-methyl-N-(2-diethylamino-acetyl)sulfoximide hydrochloride 
• 1147096-17-0 S-[4-(N-{2-[N-(5-chloro(2-pyridyl))carbamoyl]-4-chlorophenyl}carbamoyl)phenyl]-S-methyl-N-(2-(pyrrolidin-1-yl)ethyl)sulfoximide 
• 1147096-16-9 S-[4-(N-{2-[N-(5-chloro(2-pyridyl))carbamoyl]-4-chlorophenyl}carbamoyl)phenyl]-S-methyl-N-(2-(diethylamino)ethyl)sulfoximide 

Relevant academic research and scientific papers

LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS

The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Benzamides and related inhibitors of factor Xa

Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

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

A novel series of potent and efficacious factor Xa inhibitors which possesses sulfoximine moiety as novel S4 binding element in anthranilamide chemotype has been identified. Lead optimization at this novel P4 group led to many potent factor Xa inhibitors with excellent anticoagulant activity in human plasma. Selected compounds were dosed orally in rats and checked for their ex vivo prothrombin time prolonging activity, which resulted in identification of compound 5-chloro-N-(5-chloropyridin-2-yl)-2-(4-(N-(2-(diethylamino)acetyl)-S- methylsulfonimidoyl)benzamido)benzamide (18f). The detailed pharmacokinetic evaluation and subsequent metabolism study of 18f suggested the presence of an active metabolite. The compound 18f and its active metabolite 18b demonstrated excellent in vivo efficacy in both arterial and venous thrombosis model in rats and were found to be highly selective against related serine proteases. Based on this promising profile, compound 18f was selected for further evaluation.

URETHANES, UREAS, AMIDINES AND RELATED INHIBITORS OF FACTOR XA

The invention relates to a new class of compounds, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions that are effective as selective inhibitors of factor Xa, both in the isolated state and in a complex with other proteins. The compounds of the invention can be used for treating and preventing diseases, such as acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, thromboses caused by post-thrombolytic therapy or coronary angioplasty, acute ischemia mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, and other diseases in humans and other mammals associated with blood coagulation problems.

SULFOXIMINE DERIVATIVES AS FACTOR XA INHIBITORS

The present invention relates to novel substituted sulfoximine derivatives of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their pre

Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors

There remains a high unmet medical need for a safe oral therapy for thrombotic disorders. The serine protease factor Xa (fXa), with its central role in the coagulation cascade, is among the more promising targets for anticoagulant therapy and has been the

Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity

Compound 2 containing an aminomethylbenzoyl moiety as the S4 binding motif was synthesized in order to modulate hydrophlicity of anthranilamide-based factor Xa inhibitors with substituted biphenyl P4 groups. Structure-activity relationship studies around 2 have led to a series of potent factor Xa inhibitors which are highly active in the human plasma-based thrombin generation assay with 2XTG values less than 1 μM. Compound 55 shows strong antithrombotic activity in our rabbit deep vein thrombosis model, and also exhibits good oral bioavailability and a long half life in rats.

Lactam-containing compounds and derivatives thereof as factor Xa inhibitors

The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

1,1-DISUBSTITUTED CYCLOALKYL DERIVATIVES AS FACTOR XA INHIBITORS

The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.

Glycinamides as factor Xa inhibitors

The present application describes glycinamidic compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.