专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20080261949A1 CYCLOHEXYL(ALKYL)PROPANOLAMINES, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 有权
公开(公告)号：US20080261949A1
公开(公告)日：2008-10-23
申请号：US12144843
申请日：2008-06-24
申请人： Philippe R. Bovy , Roberto Cecchi , Gilles Courtemanche , Tiziano Croci , Ambrogio Oliva , Nunzia Viviani
发明人： Philippe R. Bovy , Roberto Cecchi , Gilles Courtemanche , Tiziano Croci , Ambrogio Oliva , Nunzia Viviani
IPC分类号： A61K31/553 , C07C311/01 , A61K31/24 , A61K31/421 , C07D263/54 , C07D267/02
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 —COphenyl 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.

2. 发明授权

US07622460B2 Cyclohexyl(alkyl)propanolamines, preparation method and pharmaceutical compositions containing same 有权
公开(公告)号：US07622460B2
公开(公告)日：2009-11-24
申请号：US12144843
申请日：2008-06-24
申请人： Philippe R. Bovy , Roberto Cecchi , Gilles Courtemanche , Tiziano Croci , Ambrogio Oliva , Nunzia Viviani
发明人： Philippe R. Bovy , Roberto Cecchi , Gilles Courtemanche , Tiziano Croci , Ambrogio Oliva , Nunzia Viviani
IPC分类号： A61K31/553 , C07D263/54 , C07D267/02 , C07C311/01
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 —COphenyl 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.

3. 发明授权

US07419974B2 Cyclohexyl(alkyl)propanolamines, preparation method and pharmaceutical compositions containing same 有权
公开(公告)号：US07419974B2
公开(公告)日：2008-09-02
申请号：US11464537
申请日：2006-08-15
申请人： Philippe R. Bovy , Roberto Cecchi , Gilles Courtemanche , Tiziano Croci , Ambrogio Oliva , Nunzia Viviani
发明人： Philippe R. Bovy , Roberto Cecchi , Gilles Courtemanche , Tiziano Croci , Ambrogio Oliva , Nunzia Viviani
IPC分类号： A61K31/216 , A61K31/423 , A61K31/553 , A61K31/401
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 —COphenyl 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.

4. 发明授权

US07718646B2 Cyclohexyl(alkyl)propanolamines, preparation method and pharmaceutical compositions containing same 有权
公开(公告)号：US07718646B2
公开(公告)日：2010-05-18
申请号：US12144843
申请日：2008-06-24
申请人： Philippe R. Bovy , Roberto Cecchi , Gilles Courtemanche , Tiziano Croci , Ambrogio Oliva , Nunzia Viviani
发明人： Philippe R. Bovy , Roberto Cecchi , Gilles Courtemanche , Tiziano Croci , Ambrogio Oliva , Nunzia Viviani
IPC分类号： A61K31/553 , C07D263/54 , C07D267/02 , C07C311/01
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 —COphenyl 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.

5. 发明授权

US07388031B2 Cyclohexyl(alkyl)-propanolamines, preparation method and pharmaceutical compositions containing same 有权
公开(公告)号：US07388031B2
公开(公告)日：2008-06-17
申请号：US10432493
申请日：2001-11-30
申请人： Philippe R. Bovy , Roberto Cecchi , Gilles Courtemanche , Tiziano Croci , Ambrogio Oliva , Nunzia Viviani
发明人： Philippe R. Bovy , Roberto Cecchi , Gilles Courtemanche , Tiziano Croci , Ambrogio Oliva , Nunzia Viviani
IPC分类号： A61K31/18 , C07C311/08
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 —COphenyl 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.

6. 发明授权

US07453010B2 Phenylcyclohexylpropanolamine derivatives, preparation and therapeutic application thereof 失效
公开(公告)号：US07453010B2
公开(公告)日：2008-11-18
申请号：US10515145
申请日：2003-05-26
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： C07C311/00 , A61K31/18
CPC分类号： C07D317/58 , C07C311/08 , C07C311/21 , C07C317/22 , C07C2601/14 , C07C2603/18
摘要： The invention relates to compounds of general formula (I): where R1 represents H or a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl optionally being substituted; R2 represents H, a halogen atom, an —S(O)z(C1-C4)alkyl group, where z is equal to 0, 1 or 2, an —NHSO2(C1-C4)alkyl group, an —NHSO2-phenyl group or an —NHSO2—(C1-C4)alkylphenyl group, said phenyl optionally being substituted; R3 represents an —X—R4 group—in which X represents a bond, an oxygen atom or a —CH2— group and R4 represents H or a —CR5R6—COOR7 group, where R5, R6 and R7 independently represent H or a (C1-C4)alkyl group—a phenyl group optionally substituted or fused with a dioxolane group, a —CO—NR8R9 group—where R8 represents H, a (C1-C4)alkyl group or a (C1-C4)alkyl(C1-C4)alkoxy group and R9 represents a (C1-C4)alkyl(C1-C4)alkoxy group, a —(CH2)n-A group, where n is equal to 0, 1, 2, 3 or 4 and where A represents an indolyl group, a fluorenyl group or a phenyl group which is substituted, an optionally substituted —NH-phenyl group or a —CH(R10)—(CH2)n—COOR11 group, where n is 0, 1, 2 or 3 and where R11 represents H or a (C1-C4)alkyl group and R10 represents H, a (C1-C4)alkyl group or a —CH2-phenyl group, said phenyl optionally being substituted, or a —COOR12 group, where R12 represents H or a (C1-C4)alkyl group; their process of preparation and their therapeutic application.

7. 发明授权

US07625929B2 Oxophenyl-cyclohexyl-propanolamine derivatives, production and use thereof in therapeutics 失效
标题翻译：氧基苯基 - 环己基 - 丙醇胺衍生物，其在治疗中的生产和应用
公开(公告)号：US07625929B2
公开(公告)日：2009-12-01
申请号：US10515093
申请日：2003-05-26
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： A61K31/445 , C07D211/06
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表示任选与苯基稠合的5-或6-元含氮杂环或任选被取代的杂环; 它们的加成盐; 其制备方法及其治疗应用。

8. 发明授权

US07030160B2 Propanolaminotetralines, preparation thereof and compositions containing same 失效
标题翻译：丙醇氨基四氢化萘，其制备方法和含有它们的组合物
公开(公告)号：US07030160B2
公开(公告)日：2006-04-18
申请号：US10297291
申请日：2001-05-29
申请人： Laura Barzaghi , Philippe R. Bovy , Roberto Cecchi , Tiziano Croci , Stefano Romagnano
发明人： Laura Barzaghi , Philippe R. Bovy , Roberto Cecchi , Tiziano Croci , Stefano Romagnano
IPC分类号： A61K31/216 , C07C311/08
CPC分类号： C07D295/185 , C07C271/24 , C07C311/08 , C07C2602/10
摘要： The invention relates to phenoxypropanolamines, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment of diseases that are improved by beta-3 agonist action.
摘要翻译：本发明涉及苯氧基丙胺胺，含有它们的药物组合物，其制备方法及其在治疗由β-3激动剂作用改善的疾病中的用途的方法。

9. 发明授权

US06852736B2 Phenoxypropanolamines, preparation and therapeutic use thereof 失效
标题翻译：苯氧基丙胺胺，其制备和治疗用途
公开(公告)号：US06852736B2
公开(公告)日：2005-02-08
申请号：US10149626
申请日：2000-12-15
申请人： Philippe R. Bovy , Roberto Cecchi , Olivier Venier
发明人： Philippe R. Bovy , Roberto Cecchi , Olivier Venier
IPC分类号： A61K31/4545 , A61K31/5377 , A61P1/00 , A61P3/04 , A61P3/10 , A61P15/00 , A61P17/02 , A61P25/00 , A61P25/18 , A61P25/24 , A61P27/06 , C07D401/04 , C07D401/14 , A61K31/445 , C07D211/06 , C07D401/06
CPC分类号： C07D401/04 , C07D401/14
摘要： The invention concerns phenoxypropanolamines of formula (I) in which R1 represents a hydrogen, a group —S(O)z—(C1-C4)alk-R′, (R′ being H, phenyl or (C1-C4)alkoxy), —NHSO2—(C1-C4)alk or NHCO(C1-C4)alk; m and n are each independently 0, 1 or 2; R2 and R3 independently represent a hydrogen, a (C5-C6)alkyl, (C3-C6)cycloalkyl, (C1-C4)alkoxy, hydrogen(C1-C4)alkoxy-(C1-C4)alkyl, mono- or di(C1-C4)alkamino(C1-C4)alkyl, pyrrolidino(C1-C4)alkyl, phenylamino or (C2-C4)alkenyl group, an aromatic or heteroaromatic group optionally substituted with a group R4, an aralkyl or heteroaralkyl group optionally substituted with a group R4, R2 and R3 can also together constitute a saturated or unsaturated ring of 3 to 8 atoms possibly bearing a (C1-C4)alkyl, amino (C1-C4)alkyl, carbamoyl or benzyl substituent; R4 represents a hydrogen or a halogen, or a group —CO(C1-C4)alk or a group —NHSO2—(C1-C4)alk; a group (C1-C4)alk, a group (C1-C4)alkoxy, a halogen, —COOH, —COO(C1-C4)alk, —CN, —CONR3R4, —NO2, —SO2NH2 or —NHSO2(C1-C4)alk; z is 1 or 2; and the salts or solvates thereof. The compounds have agonist activity toward β-3 adrenergic receptors.
摘要翻译：本发明涉及式（I）的苯氧基丙醇胺，其中R 1表示氢，-S（O）z - （C 1 -C 4）烷基-R'，（R'为H，苯基或（C 1 -C 4）烷氧基），-NHSO 2 - （C 1 -C 4）烷基或NHCO（C 1 -C 4）烷基; m和n各自独立地为0,1或2; R2和R3独立地表示氢，（C5-C6）烷基，（C3-C6）环烷基，（C1-C4）烷氧基，氢（C1-C4）烷氧基 - （C1-C4）烷基， C 1 -C 4烷基，吡咯烷子基（C 1 -C 4）烷基，苯基氨基或（C 2 -C 4）烯基，任选被基团R 4取代的芳族或杂芳族基团，任选被基团R4，R2和R3也可以一起构成3至8个可能带有（C 1 -C 4）烷基，氨基（C 1 -C 4）烷基，氨基甲酰基或苄基取代基的饱和或不饱和环; R4表示氢或卤素，或基团-CO（C1-C4）烷基或基团-NHSO2-（C1-C4）烷基; （C1-C4）烷基，（C1-C4）烷氧基，卤素，-COOH，-COO（C1-C4）烷基，-CN，-CONR3R4，-NO2，-SO2NH2或-NHSO2（C1- C4）烷基; z为1或2; 及其盐或溶剂合物。该化合物对β-3肾上腺素能受体具有激动作用。

10. 发明授权

US6008368A Pharmaceutical compositions for treatment of circulatory disorders using N-substituted (.alpha.-imidazolyl-toluyl) pyrrole aniotensin II antagonists 失效
标题翻译：使用N-取代的（α-咪唑基 - 甲苯酰基）吡咯类抗生素II拮抗剂治疗循环障碍的药物组合物
公开(公告)号：US6008368A
公开(公告)日：1999-12-28
申请号：US976757
申请日：1997-11-24
申请人： Philippe R. Bovy , Joe T. Collins , Robert E. Manning
发明人： Philippe R. Bovy , Joe T. Collins , Robert E. Manning
IPC分类号： C07D233/90 , C07D403/10 , A61K31/415 , A61K31/41 , C07D403/04 , C07D403/14
CPC分类号： C07D403/10
摘要： Pharmaceutical compositions comprising a compound selected from a class of N-substituted (.alpha.-imidazolyl-toluyl)pyrrole compounds are described for use in treatment of circulatory disorders. Compositions of particular interest comprise angiotensin II antagonist compounds of the formula ##STR1## wherein m is one; wherein R.sup.0 is selected from CH.sub.2 OH, CO.sub.2 H, CHO, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, CH.sub.2 OCH.sub.3, CH.sub.2 OCHOCH.sub.3 and CH.sub.2 --CO.sub.2 C.sub.2 H.sub.5 ; wherein R.sup.1 is selected from Cl, CF.sub.3, CHO, n-butyl, cyano, CO.sub.2 CH.sub.3 and CO.sub.2 CH.sub.2 CH.sub.3 ; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, propylthio, butylthio and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.9 and R.sup.10 is hydrido; wherein each of R.sup.5 and R.sup.8 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl, methoxycarbonyl with the proviso that at least one of R.sup.5 and R.sup.8 is an acidic group selected from C02H and tetrazolyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof. These compositions are particularly useful in treatment or control of hypertension and congestive heart failure.
摘要翻译：描述了包含选自一类N-取代的（α-咪唑基 - 甲苯酰基）吡咯化合物的化合物的药物组合物用于治疗循环障碍。特别感兴趣的组合物包括下式的血管紧张素II拮抗剂化合物其中m是1; 其中R 0选自CH 2 OH，CO 2 H，CHO，CO 2 CH 3，CO 2 C 2 H 5，CH 2 OCH 3，CH 2 OCHOCH 3和CH 2 -CO 2 C 2 H 5; 其中R 1选自Cl，CF 3，CHO，正丁基，氰基，CO 2 CH 3和CO 2 CH 2 CH 3; 其中R2选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，正戊基，异戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，环己基乙基，，丁硫基和羟烷基; 其中R3，R4，R6，R7，R9和R10各自为氢; 其中R 5和R 8各自独立地选自氢，卤素，硝基，三氟甲基，羟基，烷氧基，氰基，羧基，甲氧基羰基，条件是R 5和R 8中的至少一个是选自CO 2 H和四唑基的酸性基团; 或其互变异构体或其药学上可接受的盐。这些组合物特别可用于治疗或控制高血压和充血性心力衰竭。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式