229343-30-0

Basic information

• Product Name: Benzamide, 2-amino-5-chloro-N-(5-chloro-2-pyridinyl)-
• CAS NO: 229343-30-0
• Molecular Formula: C12H9Cl2N3O
• Molecular Weight: 282.129
• Mol File: 229343-30-0.mol
• Article Data: 11

Chemical Properties

• CAS DataBase Reference: Benzamide, 2-amino-5-chloro-N-(5-chloro-2-pyridinyl)-(CAS DataBase Reference)
• NIST Chemistry Reference: Benzamide, 2-amino-5-chloro-N-(5-chloro-2-pyridinyl)-(229343-30-0)
• EPA Substance Registry System: Benzamide, 2-amino-5-chloro-N-(5-chloro-2-pyridinyl)-(229343-30-0)

Safety Data

• Hazardous Substances Data: 229343-30-0(Hazardous Substances Data)

Upstream product

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

Downstream Products

• 358661-80-0 5-Chloro-2-(4-chloromethyl-benzoylamino)-N-(5-chloro-pyridin-2-yl)-benzamide 
• 229342-74-9 3-chloro-N-[4-chloro-2-[[(5-chloro-2-pyridinyl)amino]carbonyl]yphenyl]-4-chloromethyl-2-thiophenecarboxamide 
• 536759-09-8 5-chloro-N-(5-chloropyridin-2-yl)-2-({4-[methyl(pyrrolidin-1-ylacetyl)amino]benzyl}amino)benzamide 
• 536759-15-6 5-chloro-N-(5-chloropyridin-2-yl)-2-({4-[methyl(pyrrolidin-1-ylacetyl)amino]benzoyl}amino)benzamide 
• 280769-00-8 5-chloro-N-(5-chloropyridin-2-yl)-2-[[1-(4-pyridinyl)piperidin-4-ylcarbonyl]amino]benzamide hydrochloride 
• 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 
• 1217358-71-8 C₂₀H₁₁Cl₂FN₄O₂ 
• 406937-40-4 C₁₈H₁₀Cl₂N₄O₂S 
• 1217358-85-4 C₂₁H₁₄Cl₂N₄O₃ 
• 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 

Relevant articles and documents

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.

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.

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