公开(公告)号：US06649627B1

公开(公告)日：2003-11-18

申请号：US09719640

申请日：2001-03-26

申请人： Roberto Cecchi ,  Tiziano Croci ,  Umberto Guzzi ,  Eric Marsault

发明人： Roberto Cecchi ,  Tiziano Croci ,  Umberto Guzzi ,  Eric Marsault

IPC分类号： A61K31445

CPC分类号： C07D303/22 ,  C07D307/42 ,  C07D401/04 ,  C07D401/06 ,  C07D405/14

摘要： The invention concerns compounds of formula (Ia) wherein R1a represents hydrogen, an —S(O)z —(C1-C4)Alk group, a —CO(C1-C4)Alk group, an —NHSO2—(C1-C4)Alk group, an NCHl (C1-C4) Alk group, a 2-furyl group or a halogen; R2 represents hydrogen or a (C1-C4)Alk group, a (C1-C4) alkoxyl group, a halogen, —COOH, —COO(C1-C4)Alk, —CN, —CONR3R4, —NO2, —SO2NH2, —NHSO2(C1-C4)Alk; m and n are independently 0, 1 or 2; R3 and R4 independently represent hydrogen or a (C1-C4)Alk group; Z is 1 or 2 and their salts or solvates, the pharmaceutical compositions that contain them, the process for their preparation, and intermediate synthesis products.

摘要翻译： 本发明涉及式（Ia）化合物，其中R 1a表示氢，-S（O）z - （C 1 -C 4）Alk基，-CO（C 1 -C 4）Alk基，-NHSO 2 - （C 1 -C 4） 基团，NCH1（C1-C4）Alk基团，2-呋喃基或卤素; R2表示氢或（C1-C4）Alk基团，（C1-C4）烷氧基，卤素，-COOH， COO（C1-C4）Alk，-CN，-CONR3R4，-NO2，-SO2NH2，-NHSO2（C1-C4）Alk; m和n分别为0,1或2; R3和R4独立地表示氢或（C1 -C4）Alk基; Z为1或2及其盐或溶剂化物，含有它们的药物组合物，其制备方法和中间合成产物。

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.

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.

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。

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。

公开(公告)号：US5573949A

公开(公告)日：1996-11-12

申请号：US425743

申请日：1995-04-20

申请人： Roberto Cecchi ,  Laura Barzaghi ,  Umberto Guzzi

发明人： Roberto Cecchi ,  Laura Barzaghi ,  Umberto Guzzi

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

CPC分类号： C07C62/34 ,  C07C62/14 ,  C12P41/005 ,  C12P7/40

摘要： 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.

摘要翻译： 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

申请人： Umberto Guzzi ,  Roberto Cecchi ,  Luciano Manara

发明人： Umberto Guzzi ,  Roberto Cecchi ,  Luciano Manara

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

CPC分类号： A61K31/135 ,  A61K31/165 ,  A61K31/22 ,  C07C217/74 ,  C07C2102/10

摘要： 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.

摘要翻译： 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：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.

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。

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.