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1. 发明授权

US5488151A {(7S)-7-[(2R )-2-(3-chlorophenyl)-2-hydroxyethylamino)-2-hydroxyethylamino]5,} acetic acid and its pharmaceutically acceptable salts 失效
标题翻译： {（7S）-7 - [（2R）-2-（3-氯苯基）-2-羟乙基氨基）-2-羟乙基氨基] 5,6,7,8-四氢萘-2-基氧基}乙酸及其药学上可接受的盐
公开(公告)号：US5488151A
公开(公告)日：1996-01-30
申请号：US250830
申请日：1994-05-31
申请人： Marco Baroni , Roberto Cecchi , Tiziano Croci
发明人： Marco Baroni , Roberto Cecchi , Tiziano Croci
IPC分类号： A61K31/19 , A61P1/04 , A61P3/04 , A61P25/24 , A61P25/26 , A61P27/02 , C07C217/54 , C07C217/62 , C07C217/74 , C07C229/40
CPC分类号： C07C217/54 , C07C217/62 , C07C2102/10
摘要： The present invention relates to the novel compound {(7S)-7-[(2R)-2-(3-chlorophenyl)-2-hydroxyethylamino]-5,6,7,8-tetrahydronaphthalen-2-yloxy}acetic acid of formula (I): ##STR1## and its pharmaceutically acceptable salts, which act as .beta..sub.3 -adrenergic agonists, and to the pharmaceutical compositions and laboratory reagents in which it is present.
摘要翻译：本发明涉及新的化合物{（7S）-7 - [（2R）-2-（3-氯苯基）-2-羟乙基氨基] -5,6,7,8-四氢萘-2-基氧基}乙酸式（I）：其作为β3-肾上腺素能激动剂的药学上可接受的盐及其存在于其中的药物组合物和实验室试剂。

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.

4. 发明授权

US4707497A Phenylethanolaminotetralines, a process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：苯乙醇氨基四氢化萘，其制备方法和含有它们的药物组合物
公开(公告)号：US4707497A
公开(公告)日：1987-11-17
申请号：US883961
申请日：1986-07-10
申请人： Roberto Cecchi , Robert Boigegrain , Alberto Bianchetti , Elena Poggesi , Tiziano Croci
发明人： Roberto Cecchi , Robert Boigegrain , Alberto Bianchetti , Elena Poggesi , Tiziano Croci
IPC分类号： A61K31/135 , A61K31/19 , A61K31/22 , A61P3/04 , C07C67/00 , C07C213/00 , C07C215/64 , C07C217/74 , C07C219/26 , A61K31/215 , C07C101/30
CPC分类号： A61K31/135
摘要： A novel phenylethanolaminotetraline having lipolytic activity of formula ##STR1## wherin X represents hydrogen, halogen, a trifluoromethyl or a lower alkyl group and R represents hydrogen, a lower alkyl group not substituted or substituted by a cycloalkyl group containing 3 to 7 carbon atoms, a hydroxy group, a lower alkoxy, carboxy or lower carbalkoxy group; a cycloalkyl group containing 3 to 7 carbon atoms; or a lower alcanoyl group; or a pharmaceutically acceptable salt thereof; a process for its preparation; and pharmaceutical compositions containing it as active ingredient, useful for the treatment of obesity.
摘要翻译：具有式（I）的脂肪分解活性的新型苯基乙醇氨基三氯乙酸表示氢，卤素，三氟甲基或低级烷基，R表示氢，未被取代或被含有3〜7个碳原子的环烷基取代的低级烷基，羟基，低级烷氧基，羧基或低级烷氧羰基; 含有3〜7个碳原子的环烷基; 或低级烷酰基; 或其药学上可接受的盐; 其准备过程; 和含有它作为活性成分的药物组合物，其可用于治疗肥胖症。

5. 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.

6. 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。

7. 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.

8. 发明申请

US20060100283A1 Phenylcyclohexylpropanolamine derivatives, preparation and therapeutic application thereof 失效
公开(公告)号：US20060100283A1
公开(公告)日：2006-05-11
申请号：US10515145
申请日：2003-05-26
申请人： Phillippe Bovy , Roberto Cecchi , Tiziano Croci , Olivier Venier
发明人： Phillippe Bovy , Roberto Cecchi , Tiziano Croci , Olivier Venier
IPC分类号： A61K31/195 , A61K31/138
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.

9. 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。

10. 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.

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