公开(公告)号：US20100075986A1

公开(公告)日：2010-03-25

申请号：US12627536

申请日：2009-11-30

申请人： Philippe R. BOVY ,  Roberto CECCHI ,  Tiziano CROCI ,  Olivier VENIER

发明人： Philippe R. BOVY ,  Roberto CECCHI ,  Tiziano CROCI ,  Olivier VENIER

IPC分类号： A61K31/4965 ,  C07D211/06 ,  C07D241/04 ,  C07D401/04 ,  A61K31/438 ,  A61K31/4453 ,  A61P1/00 ,  A61P1/06

CPC分类号： C07D221/20 ,  C07D207/16 ,  C07D209/44 ,  C07D211/16 ,  C07D211/22 ,  C07D211/58 ,  C07D211/62 ,  C07D295/192

摘要： The invention relates to the compounds of general formula (I) where R1 represents H, a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl being optionally substituted, R2 represents H, a halogen atom, an —S(O)zR3, —NHSO2R3, —NHSO2-phenyl or —NHSO2—(C1-C4)alkylphenyl group where z is equal to 0, 1 or 2 and where R3 represents a (C1-C4)alkyl group, said phenyl being optionally substituted; A is chosen from where n is equal to 0, 1 or 2, R4 and R5 represent H, a (C1-C4)alkyl, hydroxyl, cyano, phenyl, benzyl, piperidyl, —CONH2, —CO-phenyl, —COOR3, —CH(phenyl) (OH) and —C(phenyl)2(OH) group, or R4 and R5 form together an optionally substituted 6-membered aromatic ring, R6 represents H, a (C1-C4)alkyl, phenyl or benzyl group, and B represents a 5- or 6-membered nitrogen-containing heterocycle or homocycle optionally fused with a phenyl group or optionally substituted; their addition salts; their method of preparation and their therapeutic application.

摘要翻译： 本发明涉及通式（I）的化合物，其中R1表示H，（C1-C4）烷基，-CO（C1-C4）烷基，（C1-C4）烷基苯基或-CO-苯基， 任选取代，R 2表示H，卤素原子，-S（O）z R 3，-NHSO 2 R 3，-NHSO 2 - 苯基或-NHSO 2 - （C 1 -C 4）烷基苯基，其中z等于0,1或2，其中R 3 表示（C1-C4）烷基，所述苯基任选被取代; A选自其中n等于0,1或2，R 4和R 5表示H，a（C 1 -C 4）烷基，羟基，氰基，苯基，苄基，哌啶基，-CONH 2，-CO-苯基，-COOR 3， -CH（苯基）（OH）和-C（苯基）2（OH）基团，或R 4和R 5一起形成任选取代的6元芳环，R 6表示H，（C 1 -C 4）烷基，苯基或苄基 并且B表示任选地与苯基稠合的5-或6-元含氮杂环或任选取代的杂环; 它们的加成盐; 其制备方法及其治疗应用。

公开(公告)号：US20070015745A1

公开(公告)日：2007-01-18

申请号：US11464537

申请日：2006-08-15

申请人： Philippe BOVY ,  Roberto CECCHI ,  Gilles COURTEMANCHE ,  Tiziano CROCI ,  Ambrogio OLIVA ,  Nunzia VIVIANI

发明人： Philippe BOVY ,  Roberto CECCHI ,  Gilles COURTEMANCHE ,  Tiziano CROCI ,  Ambrogio OLIVA ,  Nunzia VIVIANI

IPC分类号： A61K31/553 ,  A61K31/538 ,  A61K31/423 ,  A61K31/138 ,  C07D263/52

CPC分类号： C07C311/21 ,  C07C229/46 ,  C07C311/08 ,  C07C317/22 ,  C07C2601/14

摘要： The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —CO—phenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen atom, a (C1-C6)alkyl group, a (C1-C4)alkoxy group, a —COO(C1-C4)alkyl group, a —CO(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl groups, —NO2, —CN, —CONR4R5, —COOH, or a 4,5-dihydro-1,3-oxazol-2-yl or 4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl group; R4 and R5 represent, independently, a hydrogen atom, a phenyl, a (C1-C4)alkyl group or a phenyl-(C1-C4)alkyl group or R4 and R5 with the nitrogen atom to which they are attached, may form a ring of 5 to 7 atoms in total; and to the salts or solvates thereof, to the pharmaceutical compositions containing them, to a process for the preparation thereof and to intermediates in this process.