公开(公告)号：US20050054641A1

公开(公告)日：2005-03-10

申请号：US10497379

申请日：2002-12-02

Applicant: Laura Barzaghi ,  Roberto Cecchi ,  Nunzia Viviani

Inventor： Laura Barzaghi ,  Roberto Cecchi ,  Nunzia Viviani

IPC: C07D319/22 ,  A61K31/138 ,  A61K31/18 ,  A61K31/357 ,  A61P1/00 ,  A61P1/04 ,  A61P1/14 ,  A61P3/04 ,  A61P3/10 ,  A61P15/00 ,  A61P15/06 ,  A61P25/18 ,  A61P25/24 ,  A61P27/06 ,  C07B53/00 ,  C07C217/74 ,  C07C311/08 ,  C07D265/36 ,  A61K31/428 ,  A61K31/538 ,  C07C229/34 ,  C07D263/52

CPC classification number: C07C311/08 ,  C07C2602/10

Abstract: The invention concerns compounds of formula (1), wherein A is a group of formula (a) or (b), wherein: R represents a hydrogen or halogen atom, a —S(O)z(C1-C4)Alk wherein z is 0, 1 or 2, a —NHSO2(C1-C4)Alk, —SO2NH(C1-C4)Alk, —NHSO2—(C1-C4)Alk-phenyl or —NHSO2-phenyl group, said phenyl capable of bearing a halogen atom, a (C1-C4)Alk group or a (C1-C6)alkoxy group; R1 represents a hydrogen atom or a —(C1-C4)Alk, —CO(C1-C4)Alk, —(C1-C4)Alk-phenyl or —CO-phenyl group, said phenyl capable of bearing a halogen atom or a —(C1-C4)Alk or (C1-C6)alkoxy group; R2 is a hydrogen atom, a —SO2(C1-C4)Alk, —SO2—(C1-C4)Alk-phenyl, —SO2-phenyl group, or a —(C1-C4)Alk group; X completes a saturated or unsaturated cycle of 5 to 8 atoms, capable of bearing one or two —(C1-C4)Alk groups and/or two carbonyl groups; R3 and R′3 represent each independently a hydrogen or halogen atom, a —(C1-C6)Alk, hydroxy, —CN, —(C1-C6)alkoxy, —COR4 or Y—CR8R9—COR4 group; Y represents O or CH2; R4 represents a hydroxy, (C1-C6)alkoxy or —NR5R6 group; R5 and R6 independently represent a hydrogen atom, a —(C1-C4)Alk, group, aryl or heteroaryl optionally substituted by a R7 group, aralkyl or heteroaralkyl optionally substituted by a R7 group; or R5 and R6, with the nitrogen atom which bears them, form a saturated or unsaturated cycle of 5 to 7 atoms optionally substituted by a R7 group; and R7 represents a hydrogen or halogen atom, a hydroxy, —(C1-C4)Alk, —(C1-C6)alkoxy, —NH(C1-C4)Alk, —N(C1-C4)Alk2, —COO(C1-C4)Alk, aralkyl or heteroaryl group; R8 and R9 independently represent a hydrogen atom or a —(C1-C4)Alk group; their salts or solvates, the pharmaceutical compositions containing them, a method for preparing them and synthesis intermediates.

Abstract translation: 本发明涉及式（1）的化合物，其中A是式（a）或（b）的基团，其中：R表示氢或卤素原子，-S（O）z（C1-C4） 是0,1或2，-NHSO 2（C 1 -C 4）Alk，-SO 2 NH（C 1 -C 4）Alk，-NHSO 2 - （C 1 -C 4）烷基 - 苯基或-NHSO 2 - 苯基， 卤素原子，（C1-C4）Alk基或（C1-C6）烷氧基; R1表示氢原子或 - （C1-C4）Alk，-CO（C1-C4）Alk， - （C1-C4）Alk-苯基或-CO-苯基，所述能够带有卤素原子或 - （C1-C4）Alk或（C1-C6）烷氧基; R2是氢原子，-SO2（C1-C4）Alk，-SO2-（C1-C4）烷基 - 苯基，-SO2-苯基或 - （C1-C4） X完成5至8个原子的饱和或不饱和的循环，能承载一个或两个 - （C 1 -C 4）Alk基团和/或两个羰基基团; R 3和R'3各自独立地表示氢或卤素原子，α-（C1-C6）Alk，羟基，-CN， - （C1-C6）烷氧基，-COR4或Y-CR8R9-COR4基团; Y表示O或CH 2; R4表示羟基，（C1-C6）烷氧基或-NR5R6基团; R 5和R 6独立地表示氢原子，任选被R 7取代的 - （C 1 -C 4）Alk，基团，芳基或杂芳基

公开(公告)号：US07115780B2

公开(公告)日：2006-10-03

申请号：US10497379

申请日：2002-12-02

Applicant: Laura Barzaghi ,  Roberto Cecchi ,  Nunzia Viviani

Inventor： Laura Barzaghi ,  Roberto Cecchi ,  Nunzia Viviani

IPC: C07C211/19 ,  C07C213/02 ,  C07C307/02 ,  C07D263/52 ,  C07D265/36 ,  A61K31/18 ,  A61K31/42

CPC classification number: C07C311/08 ,  C07C2602/10

Abstract: The invention concerns compounds of formula (I), wherein A is a group of formula (a) or (b), wherein: R represents a hydrogen or halogen atom, a —S(O)z(C1–C4)Alk wherein z is 0, 1 or 2, a —NHSO2(C1–C4)Alk, —SO2NH(C1–C4)Alk, —NHSO2—(C1–C4)Alk-phenyl or —NHSO2-phenyl group, said phenyl capable of bearing a halogen atom, a (C1–C4)Alk group or a (C1–C6)alkoxy group; R1 represents a hydrogen atom or a —(C1–C4)Alk, —CO(C1–C4)Alk, —(C1–C4)Alk-phenyl or —CO-phenyl group, said phenyl capable of bearing a halogen atom or a —(C1–C4)Alk or (C1–C6)alkoxy group; R2 is a hydrogen atom, a —SO2(C1–C4)Alk, —SO2—(C1–C4)Alk-phenyl, —SO2-phenyl group, or a —(C1–C4)Alk group; X completes a saturated or unsaturated cycle of 5 to 8 atoms, capable of bearing one or two —(C1–C4)Alk groups and/or two carbonyl groups; R3 and R′3 represent each independently a hydrogen or halogen atom, a —(C1–C6)Alk, hydroxy, —CN, —(C1–C6)alkoxy, —COR4 or Y—CR8R9—COR4 group; Y represents O or CH2; R4 represents a hydroxy, (C1–C6)alkoxy or —NR5R6 group; R5 and R6 independently represent a hydrogen atom, a —(C1–C4)Alk, group, aryl or heteroaryl optionally substituted by a R7 group, aralkyl or heteroaralkyl optionally substituted by a R7 group; or R5 and R6, with the nitrogen atom which bears them, form a saturated or unsaturated cycle of 5 to 7 atoms optionally substituted by a R7 group; and R7 represents a hydrogen or halogen atom, a hydroxy, —(C1–C4)Alk, —(C1–C6)alkoxy, —NH(C1–C4)Alk, —N(C1–C4)Alk2, —COO(C1–C4)Alk, aralkyl or heteroaryl group; R8 and R9 independently represent a hydrogen atom or a —(C1–C4)Alk group; their salts or solvates, the pharmaceutical compositions containing them, a method for preparing them and synthesis intermediates

公开(公告)号：US07622460B2

公开(公告)日：2009-11-24

申请号：US12144843

申请日：2008-06-24

Applicant: Philippe R. Bovy ,  Roberto Cecchi ,  Gilles Courtemanche ,  Tiziano Croci ,  Ambrogio Oliva ,  Nunzia Viviani

Inventor： Philippe R. Bovy ,  Roberto Cecchi ,  Gilles Courtemanche ,  Tiziano Croci ,  Ambrogio Oliva ,  Nunzia Viviani

IPC: A61K31/553 ,  C07D263/54 ,  C07D267/02 ,  C07C311/01

Abstract: 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.

公开(公告)号：US20080261949A1

公开(公告)日：2008-10-23

申请号：US12144843

申请日：2008-06-24

Applicant: Philippe R. Bovy ,  Roberto Cecchi ,  Gilles Courtemanche ,  Tiziano Croci ,  Ambrogio Oliva ,  Nunzia Viviani

Inventor： Philippe R. Bovy ,  Roberto Cecchi ,  Gilles Courtemanche ,  Tiziano Croci ,  Ambrogio Oliva ,  Nunzia Viviani

IPC: A61K31/553 ,  C07C311/01 ,  A61K31/24 ,  A61K31/421 ,  C07D263/54 ,  C07D267/02

CPC classification number: C07C311/21 ,  C07C229/46 ,  C07C311/08 ,  C07C317/22 ,  C07C2601/14

Abstract: 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.

公开(公告)号：US07718646B2

公开(公告)日：2010-05-18

申请号：US12144843

申请日：2008-06-24

Applicant: Philippe R. Bovy ,  Roberto Cecchi ,  Gilles Courtemanche ,  Tiziano Croci ,  Ambrogio Oliva ,  Nunzia Viviani

Inventor： Philippe R. Bovy ,  Roberto Cecchi ,  Gilles Courtemanche ,  Tiziano Croci ,  Ambrogio Oliva ,  Nunzia Viviani

IPC: A61K31/553 ,  C07D263/54 ,  C07D267/02 ,  C07C311/01

CPC classification number: C07C311/21 ,  C07C229/46 ,  C07C311/08 ,  C07C317/22 ,  C07C2601/14

Abstract: 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.

公开(公告)号：US07388031B2

公开(公告)日：2008-06-17

申请号：US10432493

申请日：2001-11-30

Applicant: Philippe R. Bovy ,  Roberto Cecchi ,  Gilles Courtemanche ,  Tiziano Croci ,  Ambrogio Oliva ,  Nunzia Viviani

Inventor： Philippe R. Bovy ,  Roberto Cecchi ,  Gilles Courtemanche ,  Tiziano Croci ,  Ambrogio Oliva ,  Nunzia Viviani

IPC: A61K31/18 ,  C07C311/08

CPC classification number: C07C311/21 ,  C07C229/46 ,  C07C311/08 ,  C07C317/22 ,  C07C2601/14

Abstract: 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.

公开(公告)号：US07419974B2

公开(公告)日：2008-09-02

申请号：US11464537

申请日：2006-08-15

Applicant: Philippe R. Bovy ,  Roberto Cecchi ,  Gilles Courtemanche ,  Tiziano Croci ,  Ambrogio Oliva ,  Nunzia Viviani

Inventor： Philippe R. Bovy ,  Roberto Cecchi ,  Gilles Courtemanche ,  Tiziano Croci ,  Ambrogio Oliva ,  Nunzia Viviani

IPC: A61K31/216 ,  A61K31/423 ,  A61K31/553 ,  A61K31/401

CPC classification number: C07C311/21 ,  C07C229/46 ,  C07C311/08 ,  C07C317/22 ,  C07C2601/14

Abstract: 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.

公开(公告)号：US5573949A

公开(公告)日：1996-11-12

申请号：US425743

申请日：1995-04-20

Applicant: Roberto Cecchi ,  Laura Barzaghi ,  Umberto Guzzi

Inventor： Roberto Cecchi ,  Laura Barzaghi ,  Umberto Guzzi

IPC: C07C51/09 ,  C07C62/14 ,  C07C62/34 ,  C12P7/40 ,  C12P41/00

CPC classification number: C07C62/34 ,  C07C62/14 ,  C12P41/005 ,  C12P7/40

Abstract: The present invention relates to an enzymatic process for the preparation of optically active tetrahydro-2-naphthoic acids from the corresponding racemic esters by reaction with a lipase.

Abstract translation: 本发明涉及通过与脂肪酶反应从相应的外消旋酯制备光学活性的四氢-2-萘甲酸的酶法。

公开(公告)号：US5719308A

公开(公告)日：1998-02-17

申请号：US685488

申请日：1996-07-24

Applicant: Roberto Cecchi ,  Laura Barzaghi ,  Umberto Guzzi

Inventor： Roberto Cecchi ,  Laura Barzaghi ,  Umberto Guzzi

IPC: C07C51/09 ,  C07C62/14 ,  C07C62/34 ,  C12P7/40 ,  C12P41/00 ,  C07C69/76

CPC classification number: C07C62/34 ,  C07C62/14 ,  C12P41/005 ,  C12P7/40

Abstract: The present invention relates to an enzymatic process for the preparation of optically active tetrahydro-2-naphthoic acids from the corresponding racemic esters by reaction with a lipase.

Abstract translation: 本发明涉及通过与脂肪酶反应从相应的外消旋酯制备光学活性的四氢-2-萘甲酸的酶法。

公开(公告)号：US07030160B2

公开(公告)日：2006-04-18

申请号：US10297291

申请日：2001-05-29

Applicant: Laura Barzaghi ,  Philippe R. Bovy ,  Roberto Cecchi ,  Tiziano Croci ,  Stefano Romagnano

Inventor： Laura Barzaghi ,  Philippe R. Bovy ,  Roberto Cecchi ,  Tiziano Croci ,  Stefano Romagnano

IPC: A61K31/216 ,  C07C311/08

CPC classification number: C07D295/185 ,  C07C271/24 ,  C07C311/08 ,  C07C2602/10

Abstract: 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.

Abstract translation: 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。