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：US5312961A

公开(公告)日：1994-05-17

申请号：US905483

申请日：1992-06-29

Applicant: Umberto Guzzi ,  Roberto Cecchi ,  Luciano Manara

Inventor： Umberto Guzzi ,  Roberto Cecchi ,  Luciano Manara

IPC: A61K31/135 ,  A61K31/165 ,  A61K31/22 ,  C07C217/74 ,  C07C101/72

CPC classification number: A61K31/135 ,  A61K31/165 ,  A61K31/22 ,  C07C217/74 ,  C07C2102/10

Abstract: The invention relates to 2-amino-7-hydroxytetralin carboxyalkyl ethers of formula ##STR1## wherein Alk represents a straight or branched (C.sub.3 -C.sub.5)alkylene group, and R is hydrogen or (C.sub.1 -C.sub.4)alkyl, useful as starting materials in the synthesis of 7-substituted phenylethanolaminotetralins of formula (XII) ##STR2## wherein X represents hydrogen, halogen, (C.sub.1 -C.sub.4)alkyl, or trifluoromethyl which are useful as spasmolytics and anti-glaucoma agents.The new 7-substituted phenylethanolaminotetralins (XII) as well as the intermediates in the preparation of the compounds (I), the N-protected 2-amino-7-hydroxytetralin carboxyalkyl ethers, are also claimed.

Abstract translation: 本发明涉及式（I）的2-氨基-7-羟基四氢萘羧酸烷基醚，其中Alk表示直链或支链（C3-C5）亚烷基，R是氢或（C1-C4）烷基，可用作 合成式（XII）的7-取代苯乙醇氨基十氢化萘（XII）的原料，其中X代表氢，卤素，（C1-C4）烷基或三氟甲基，其可用作解聚物和抗青光眼剂。 还要求保护新的7-取代苯乙醇氨基十氢化萘（XII）以及化合物（I），N-保护的2-氨基-7-羟基四氢萘烷羧基烷基醚的制备中的中间体。

公开(公告)号：US5041606A

公开(公告)日：1991-08-20

申请号：US488137

申请日：1990-03-05

Applicant: Robert Boigegrain ,  Roberto Cecchi ,  Sergio Boveri

Inventor： Robert Boigegrain ,  Roberto Cecchi ,  Sergio Boveri

IPC: A61K31/215 ,  C07C20060101 ,  C07C67/00 ,  C07C213/00 ,  C07C213/06 ,  C07C215/60 ,  C07C217/54 ,  C07C217/60 ,  C07C217/74 ,  C07C229/40 ,  C07C229/42 ,  C07C239/00 ,  C07C271/16

CPC classification number: C07C213/06 ,  C07C217/74 ,  C07C271/16 ,  C07C271/24 ,  C07C2102/10

Abstract: A process for the preparation of a compound of formula ##STR1## wherein X represents hydrogen, halogen, trifluoromethyl or lower alkyl group; W represents methyl, Q represents hydrogen or W and Q, together, form an ethylene group and R' represents a lower alkyl group which comprises protecting the amino group of the phenol corresponding to the compound of formula I, submitting the compound thus obtained to an alkylation (with a compound of formula Hal--CH.sub.2 --COOR', wherein R' is as defined hereinabove for the formula I and Hal is chlorine, bromine or iodine) and then releasing the amino group of the product thus obtained.

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：US07625929B2

公开(公告)日：2009-12-01

申请号：US10515093

申请日：2003-05-26

Applicant: Philippe R. Bovy ,  Roberto Cecchi ,  Tiziano Croci ,  Olivier Venier

Inventor： Philippe R. Bovy ,  Roberto Cecchi ,  Tiziano Croci ,  Olivier Venier

IPC: A61K31/445 ,  C07D211/06

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

Abstract: 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.

Abstract translation: 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。

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：US20060100283A1

公开(公告)日：2006-05-11

申请号：US10515145

申请日：2003-05-26

Applicant: Phillippe Bovy ,  Roberto Cecchi ,  Tiziano Croci ,  Olivier Venier

Inventor： Phillippe Bovy ,  Roberto Cecchi ,  Tiziano Croci ,  Olivier Venier

IPC: A61K31/195 ,  A61K31/138

CPC classification number: C07D317/58 ,  C07C311/08 ,  C07C311/21 ,  C07C317/22 ,  C07C2601/14 ,  C07C2603/18

Abstract: 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.

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。

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：US06858629B1

公开(公告)日：2005-02-22

申请号：US10070453

申请日：2000-09-08

Applicant: Roberto Cecchi ,  Ambrogio Oliva

Inventor： Roberto Cecchi ,  Ambrogio Oliva

IPC: C07D401/12 ,  A61K31/454 ,  A61K31/4545 ,  A61P1/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/30 ,  A61P13/00 ,  A61P15/06 ,  A61P25/18 ,  A61P25/24 ,  A61P27/06 ,  A61P43/00 ,  C07D401/04 ,  C07D401/14 ,  A61K31/445 ,  C07D211/06 ,  C07D401/06

CPC classification number: C07D401/04 ,  C07D401/14

Abstract: Compounds of formula (I): where X is N or CH; A represents a group of formula (a) or (b) R1 represents hydrogen or an —NH2, —NR3R4, —NR3CO(C1-C4)Alk or —NR3SO2(C1-C4)Alk group; R2 represents hydrogen, a halogen or a (C1-C4)Alk, (C1-C4)alkoxy, —COOH, —COO(C1-C4)Alk, —CN, —CONR3R4, —NO2, —SO2NR3R4 or —NHSO2(C1-C4)Alk; m and n each represent 0, 1 or 2; R3 and R4 each represent hydrogen or a (C1-C4)Alk group; Y1 and Y2 each represent NH or O; and their salts or solvates, a process for their preparation and the pharmaceutical compositions comprising them.

Abstract translation: 式（I）化合物：其中X是N或CH; A代表式（a）或（b）的基团，R1代表氢或-NH2，-NR3R4，-NR3CO（C1-C4）Alk或-NR3SO2 C1-C4）Alk基; R2表示氢，卤素或（C1-C4）Alk，（C1-C4）烷氧基，-COOH，-COO（C1-C4）Alk，-CN，-CONR3R4，-NO2， -SO 2 NR 3 R 4或-NHSO 2（C 1 -C 4）Alk; m和n各自表示0,1或2; R 3和R 4各自表示氢或（C 1 -C 4）Alk基; Y 1和Y 2各自表示NH或O; 盐或溶剂合物，其制备方法和包含它们的药物组合物。