发明名称 Sulphonylaminopyrrolidinone derivatives, their preparation and their therapeutic application
摘要 The invention relates to new sulphonylaminopyrrolidinone compounds having antithrombotic activity which, in particular, inhibit blood clotting factor IXa and/or factor Xa, to processes for their preparation and to use thereof as drugs.
申请公布号 US9150544(B2) 申请公布日期 2015.10.06
申请号 US201214366402 申请日期 2012.12.19
申请人 Sanofi 发明人 Alet Nathalie;Altenburger Jean-Michel;Herault Jean-Pascal;Kirsch Reinhard;Lassalle Gilbert;Mallart Sergio;Philippo-Orts Marie-Claire
分类号 C07D401/14;C07D417/14;A61K31/4709 主分类号 C07D401/14
代理机构 McDonnell Boehnen Hulbert & Berghoff 代理人 McDonnell Boehnen Hulbert & Berghoff
主权项 1. A compound of formula (I)wherein R1 is hydrogen,(C1-C6)alkyl,(C3-C7)cycloalkyl,(C3-C7)cycloalkyl-(C1-C6)alkyl-,Rb—O—Ra— where Rb is (C1-C6)alkyl or (C3-C7)cycloalkyl and Ra is (C1-C6)alkyl,Rd-O—C(O)—O-Rc- where Rd is (C1-C6)alkyl or (C3-C7)cycloalkyl, and Rc is (C1-C6)alkyl, orRf—C(O)—O—Re— where Re is (C1-C6)alkyl and Rf is (C1-C6)alkyl; R2 is halogen,—OH,—CN,(C1-C6)alkyl or —O—(C1-C6)alkyl in which each (C1-C6)alkyl is non-substituted or substituted by one or more halogen identical to or different from one another, orRg-O—Rh—O—, in which Rg is (C1-C6)alkyl and Rh is (C1-C6)alkyl; R2′ is hydrogen or (C1-C6)alkyl; R3 is wherein R4 and R5 are, independently of one another, (C1-C6) alkyl or (C3-C7)cycloalkyl, or R4 and R5, when taken together with the nitrogen atom to which they are attached, form a 3 to 7 membered heterocycloalkyl comprising from 1 to 2 heteroatoms chosen from nitrogen, oxygen and sulphur, said heterocycloalkyl being non-substituted or substituted by one or more groups independently selected from halogen, (C1-C6)alkyl, (C1-C6)alkoxy, —CF3 and —OCF3; and R6 is halogen, hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy or —CN; or an enantiomer, diastereoisomer or mixture thereof, or pharmaceutically acceptable salt thereof.
地址 Paris FR