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    N-substituted N-(alpha-triazolyl-toluyl)pyrrole compounds and use for treatment of circulatory disorders
    24.
    发明授权
    N-substituted N-(alpha-triazolyl-toluyl)pyrrole compounds and use for treatment of circulatory disorders 失效
    N-取代的N-（ALPHA-TRIAZOLYL-TOLUYL）吡咯烷酮化合物和用于治疗循环障碍的用途

    公开(公告)号：US5175180A

    公开(公告)日：1992-12-29

    申请号：US630714

    申请日：1990-12-20

    申请人： Philippe R. Bovy ,  David B. Reitz ,  Robert E. Manning

    发明人： Philippe R. Bovy ,  David B. Reitz ,  Robert E. Manning

    IPC分类号： C07D403/10 ,  C07D403/14

    CPC分类号： C07D403/10 ,  C07D403/14

    摘要： A class of N-substituted N-(.alpha.-triazolyltoluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein R.sup.1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; 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, propylthio, butylthio, and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R.sup.5 and R.sup.8 must be selected from COOH, SH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, OH, ##STR2## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

    摘要翻译： 描述用于治疗循环系统疾病的一类N-取代的N-（α-三唑基甲苯磺酰基）吡咯化合物。 特别感兴趣的化合物是式IMAMA的血管紧张素II拮抗剂，其中m是1; 其中R1选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，4-甲基丁基，正戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，环己基乙基 ，环己酰基，1-氧代-2-环己基乙基，苯甲酰基，1-氧代-2-苯乙基，1-氧代丙基，1-氧代丁基，1-氧代戊基和2-羟基丁基; 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，丙硫基，丁硫基 ，和羟烷基; 其中R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10各自独立地选自氢，卤素，硝基，三氟甲基，羟基，烷氧基，氰基，羧基和甲氧基羰基; 条件是R 5和R 8中的至少一个必须选自COOH，SH，PO3H2，SO3H，CONHNH2，CONHNHSO2CF3，OH，其中R42和R43各自独立地选自氯，氰基，硝基，三氟甲基， 甲氧基羰基和三氟甲基磺酰基; 或其互变异构体或其药学上可接受的盐。 这些化合物特别可用于治疗或控制高血压和充血性心力衰竭。

    Cyclohexyl(alkyl)propanolamines, preparation method and pharmaceutical compositions containing same
    25.
    发明授权
    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.

    Oxophenyl-cyclohexyl-propanolamine derivatives, production and use thereof in therapeutics
    26.
    发明授权
    Oxophenyl-cyclohexyl-propanolamine derivatives, production and use thereof in therapeutics 失效
    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。

    Cyclohexyl(alkyl)-propanolamines, preparation method and pharmaceutical compositions containing same
    27.
    发明授权
    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.

    Phenoxypropanolamines, preparation and therapeutic use thereof
    29.
    发明授权
    Phenoxypropanolamines, preparation and therapeutic use thereof 失效
    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。

    2-arylquinoline derivatives, preparation and therapeutic use thereof
    30.
    发明授权
    2-arylquinoline derivatives, preparation and therapeutic use thereof 失效
    2-芳基喹啉衍生物，其制备和治疗用途

    公开(公告)号：US06617336B1

    公开(公告)日：2003-09-09

    申请号：US10130875

    申请日：2002-05-22

    申请人： Philippe R Bovy ,  Alain Braun ,  Christophe Philippo

    发明人： Philippe R Bovy ,  Alain Braun ,  Christophe Philippo

    IPC分类号： A61K314706

    CPC分类号： C07D401/04 ,  C07D215/12 ,  C07D215/14 ,  C07D409/04

    摘要： Compounds of general formula (I) in which: A represents a hydrogen atom, a hydroxyl, a C1-3 alkoxy group, a hydroxy(C1-6 alkyl) group, a (C1-3 alkoxy)(C1-3 alkyl) group, a thiol, (C1-6 alkyl)sulfanyl or a halogen; B and D represent, independently of one another, a hydrogen atom, a C1-6 alkyl group, a fluoro(C1-6 alkyl) group or a perfluoro(C1-2 alkyl) group or B and D together from an oxo; R1 represents a phenyl, a naphthyl or a heteroaryl comprising 4 or 5 carbon atoms; R2 and R3 represent, independently of one another, a hydrogen atom, a halogen or a C1-6 alkyl group, R4 represents a hydrogen atom, a hydroxyl or a halogen, and R5 and R6 represent, independently of one another, a hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C3-6 cycloalkyl group, a C3-6 cycloalkenyl group, a fluoro(C1-6 alkyl) group or a perfluoro(C1-2 alkyl) group or R5 and R6 together form a C2-6 alkylene chain or a C3-6 alkenylene chain, to give, with the nitrogen to which they are attached, a heterocycle, this heterocycle optionally being substituted by a C1-4 alkyl group; and their salts.

    摘要翻译： 通式（I）的化合物，其中：A表示氢原子，羟基，C 1-3烷氧基，羟基（C 1-6烷基），（C 1-3烷氧基）（C 1-3烷基） ，硫醇，（C 1-6烷基）硫烷基或卤素; B和D彼此独立地表示氢原子，C 1-6烷基，氟（C 1-6烷基）或全氟（C 1 -C 6烷基） -2烷基）基团或B和D一起来自氧代; R 1表示苯基，萘基或含有4或5个碳原子的杂芳基; R 2和R 3彼此独立地表示氢原子，卤素或C 1 -6-烷基，R 4表示氢原子，羟基或卤素，R 5和R 6彼此独立地表示氢原子，C 1-6烷基，C 2-6烯基，C 3-6环烷基 基团，C3-6环烯基，氟（C1-6烷基）基团或全氟（C1-2烷基）基团或R5和R6一起形成C 2-6亚烷基链或C 3-6亚烯基链，得到 与它们相连的氮，杂环，t 他的杂环任选被C 1-4烷基取代; 和它们的盐。