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1. 发明授权

US06194405B1 Method of using substituted tetracyclic tetrahydrofuran derivatives 有权
标题翻译：使用取代四环四氢呋喃衍生物的方法
公开(公告)号：US06194405B1
公开(公告)日：2001-02-27
申请号：US09533625
申请日：2000-03-22
申请人： Pilar Gil-Lopetegui , Francisco Javier Fernández-Gadea , Theo Frans Meert
发明人： Pilar Gil-Lopetegui , Francisco Javier Fernández-Gadea , Theo Frans Meert
IPC分类号： A01N4346
CPC分类号： C07D493/04 , C07D307/93
摘要： This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or halomethyl; X is CR6R7, NR8, O, S, S(═O) or S(═O)2; aryl is optionally substituted phenyl; provided that the compound is other than (±)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3,4:6,7]-cyclohepta[1,2-b]-furan-2-methanamine oxalic acid. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体异构形式，其中n为0-6; p和q为零至4; r为0〜5; R1和R2各自独立地为氢; 任选取代的C 1-6烷基; C 1-6烷基羰基; 卤代甲基羰基; 或者R 1和R 2与它们所连接的氮原子一起可以形成吗啉基环或任选取代的杂环; 每个R 3和R 4独立地是卤素，氰基，羟基，卤代甲基，卤代甲氧基，羧基，硝基，氨基，单或二（C 1-6烷基）氨基，C 1-6烷基羰基氨基，氨基磺酰基，一或二（C 1-6烷基）氨基磺酰基， C 1-6烷基，C 1-6烷氧基，C 1-6烷基羰基，C 1-6烷氧基羰基; 每个R 5独立地是C 1-6烷基，氰基或卤代甲基; X是CR 6 R 7，NR 8，O，S，S（= O）或S（= O）2; 芳基是任选取代的苯基; 条件是该化合物不是（±）-3,3a，8,12b-四氢-N-甲基-2H-二苯并[3,4：6,7] - 环庚并[1,2-b] - 呋喃-2-基 - 草胺草酸。式（I）化合物可用作治疗或预防CNS障碍，心血管疾病或胃肠道疾病的治疗剂。

2. 发明授权

US06288058B1 Substituted tetracyclic tetrahydrofuran derivatives 失效
标题翻译：取代的四环四氢呋喃衍生物
公开(公告)号：US06288058B1
公开(公告)日：2001-09-11
申请号：US09745517
申请日：2000-12-21
申请人： Pilar Gil-Lopetegui , Francisco Javier Fernández-Gadea , Theo Frans Meert
发明人： Pilar Gil-Lopetegui , Francisco Javier Fernández-Gadea , Theo Frans Meert
IPC分类号： A61K63155
CPC分类号： C07D493/04 , C07D307/93
摘要： This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or halomethyl; X is CR6R7, NR8, O, S, S(═O) or S(═O)2; aryl is optionally substituted phenyl; provided that the compound is other than (±)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3,4:6,7]-cyclohepta[1,2-b]-furan-2-methanamine oxalic acid. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体异构形式，其中n为0-6; p和q为零至4; r为0〜5; R1和R2各自独立地为氢; 任选取代的C 1-6烷基; C 1-6烷基羰基; 卤代甲基羰基; 或者R 1和R 2与它们所连接的氮原子一起可以形成吗啉基环或任选取代的杂环; 每个R 3和R 4独立地是卤素，氰基，羟基，卤代甲基，卤代甲氧基，羧基，硝基，氨基，单或二（C 1-6烷基）氨基，C 1-6烷基羰基氨基，氨基磺酰基，一或二（C 1-6烷基）氨基磺酰基， C 1-6烷基，C 1-6烷氧基，C 1-6烷基羰基，C 1-6烷氧基羰基; 每个R 5独立地是C 1-6烷基，氰基或卤代甲基; X是CR 6 R 7，NR 8，O，S，S（= O）或S（= O）2; 芳基是任选取代的苯基; 条件是该化合物不是（±）-3,3a，8,12b-四氢-N-甲基-2H-二苯并[3,4：6,7] - 环庚并[1,2-b] - 呋喃-2-基 - 草胺草酸。式（I）化合物可用作治疗或预防CNS障碍，心血管疾病或胃肠道疾病的治疗剂。

3. 发明授权

US06699858B2 Halogen substituted tetracyclic tetrahydrofuran derivatives 失效
标题翻译：卤素取代四环四氢呋喃衍生物
公开(公告)号：US06699858B2
公开(公告)日：2004-03-02
申请号：US10292270
申请日：2002-11-12
申请人： José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Pilar Gil-Lopetegui
发明人： José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Pilar Gil-Lopetegui
IPC分类号： A61K31501
CPC分类号： C07D405/06 , C07D307/93 , C07D493/04
摘要： This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R1 and R2 each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 and R4 are both halogen; or R3 is halogen and R4 is hydrogen; or R3 is hydrogen and R4 is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中n为0,1,2,3,4,5或6; X是CH 2或O; R 1和R 2各自独立地为氢，C 1-6烷基，C 1-6烷基羰基，卤代甲基羰基或被羟基，C 1-6烷氧基，羧基，C 1-6烷基羰基氧基，C 1-6烷氧基羰基或芳基取代的C 1-6烷基。或R 1和R 2与它们所连接的氮原子一起可以形成吗啉基环或任选取代的杂环; R 3和R 4都是卤素; 或R 3是卤素，R 4是氢; 或R 3为氢，R 4为卤素; 并且芳基是苯基或被1,2或3个选自卤素，羟基，C 1-6烷基和卤代甲基的取代基取代的苯基。式（I）化合物可用作治疗剂。

4. 发明授权

US06511976B1 Halogen substituted tetracyclic tetrahydrofuran derivatives 失效
标题翻译：卤素取代四环四氢呋喃衍生物
公开(公告)号：US06511976B1
公开(公告)日：2003-01-28
申请号：US09529252
申请日：2000-04-06
申请人： José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Pilar Gil-Lopetegui , Adolfo Díaz-Martinez
发明人： José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Pilar Gil-Lopetegui , Adolfo Díaz-Martinez
IPC分类号： A61K31497
CPC分类号： C07D405/06 , C07D307/93 , C07D493/04
摘要： This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R1 and R2 each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 and R4 are both halogen; or R3 is halogen and R4 is hydrogen; or R3 is hydrogen and R4 is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中n为0,1,2,3,4,5或6; X是CH 2或O; R 1和R 2各自独立地为氢，C 1-6烷基，C 1-6烷基羰基，卤代甲基羰基或被羟基，C 1-6烷氧基，羧基，C 1-6烷基羰基氧基，C 1-6烷氧基羰基或芳基取代的C 1-6烷基。或者R 1和R 2与它们所连接的氮原子一起可以形成吗啉基环或任选取代的杂环; R3和R4都是卤素; 或R3是卤素，R4是氢; 或R3是氢，R4是卤素; 并且芳基是苯基或被1,2或3个选自卤素，羟基，C 1-6烷基和卤代甲基的取代基取代的苯基。式（I）化合物可用作治疗剂。

5. 发明授权

US6057441A Substituted tetracyclic tetrahydrofuran derivatives 有权
标题翻译：取代的四环四氢呋喃衍生物
公开(公告)号：US6057441A
公开(公告)日：2000-05-02
申请号：US155840
申请日：1998-10-06
申请人： Pilar Gil-Lopetegui , Francisco Javier Fernandez-Gadea , Theo Frans Meert
发明人： Pilar Gil-Lopetegui , Francisco Javier Fernandez-Gadea , Theo Frans Meert
IPC分类号： A61K31/00 , A61K31/34 , A61K31/343 , A61K31/4025 , A61K31/4035 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4525 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/55 , A61P1/00 , A61P1/14 , A61P9/00 , A61P9/02 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/30 , C07D307/93 , C07D405/02 , C07D405/06 , C07D491/048 , C07D493/04 , C07D493/10 , C07D495/04 , C07D223/14 , C07D211/08 , C07D313/00 , C07D337/12 , C07D405/00
CPC分类号： C07D493/04 , C07D307/93
摘要： This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; halomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or halomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.2 ; aryl is optionally substituted phenyl; provided that the compound is other than (.+-.)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3,4:6,7]-cyclohepta[1,2-b]-furan-2-methanamine oxalic acid. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.
摘要翻译： PCT No.PCT / EP97 / 01829 Sec。 371 1998年10月6日第 102（e）日期1998年10月6日PCT 1997年4月9日PCT公布。公开号WO97 / 38991 日期1997年10月23日本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐及其立体异构形式，其中n为0-6; p和q为零至4; r为0〜5; R1和R2各自独立地为氢; 任选取代的C 1-6烷基; C 1-6烷基羰基; 卤代甲基羰基; 或者R 1和R 2与它们所连接的氮原子一起可以形成吗啉基环或任选取代的杂环; 每个R 3和R 4独立地是卤素，氰基，羟基，卤代甲基，卤代甲氧基，羧基，硝基，氨基，单或二（C 1-6烷基）氨基，C 1-6烷基羰基氨基，氨基磺酰基，一或二（C 1-6烷基）氨基磺酰基， C 1-6烷基，C 1-6烷氧基，C 1-6烷基羰基，C 1-6烷氧基羰基; 每个R 5独立地是C 1-6烷基，氰基或卤代甲基; X是CR 6 R 7，NR 8，O，S，S（= O）或S（= O）2; 芳基是任选取代的苯基; 条件是该化合物不是（+/-） - 3,3a，8,12b-四氢-N-甲基-2H-二苯并[3,4：6,7] - 环庚并[1,2-b]呋喃 -2-甲胺草酸。式（I）化合物可用作治疗或预防CNS障碍，心血管疾病或胃肠道疾病的治疗剂。

6. 发明授权

US5552399A Substituted tetracyclic azepine derivatives 失效
标题翻译：取代四环吖庚因衍生物
公开(公告)号：US5552399A
公开(公告)日：1996-09-03
申请号：US457968
申请日：1995-05-31
申请人： Victor K. Sipido , Francisco J. Fern andez-Gadea , Jos e I. Andr es-Gil , Theo F. Meert , Pilar Gil-Lopetegui
发明人： Victor K. Sipido , Francisco J. Fern andez-Gadea , Jos e I. Andr es-Gil , Theo F. Meert , Pilar Gil-Lopetegui
IPC分类号： A61K31/535 , A61K31/55 , A61P9/00 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/26 , C07D223/20 , C07D223/30 , C07D261/00 , C07D498/04 , C07D498/10
CPC分类号： C07D223/20
摘要： This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. ##STR1## wherein: R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; C.sub.1-6 alkyl substituted with hydroxy, C.sub.1-6 alkyloxy, carboxyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkyloxycarbonyl or aryl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9, R.sup.10, R.sup.11 or R.sup.12 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)-amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)-aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxy-carbonyl; R.sup.7 and R.sup.8 are each independently hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or R.sup.7 and R.sup.8 taken together may form mono- or di(cyano)methylene, or together with the carbon atom to which they are attached form a carbonyl or a spiro substituent; or R.sup.7 and R.sup.8 taken together may form methylene; R.sup.13 is hydrogen, C.sub.1-6 alkyl, or trifluoromethyl; R.sup.14 is hydrogen, C.sub.1-6 alkyl, cyano, or trifluoromethyl; n is zero to 6. These compounds were tested as mCPP-antagonists in rats. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.
摘要翻译：本发明涉及式（I）的化合物，其药学上可接受的盐和立体异构形式，以及它们的N-氧化物形式。（I）其中：R1和R2各自独立地为氢; C 1-6烷基; C 1-6烷基羰基; 三卤代甲基羰基被羟基，C 1-6烷氧基，羧基，C 1-6烷基羰基氧基，C 1-6烷氧基羰基或芳基取代的C 1-6烷基; 或者R 1和R 2与它们所连接的氮原子一起可以形成吗啉基环或任选取代的杂环; R3，R4，R5，R6，R9，R10，R11或R12各自独立地为氢，卤素，氰基，羟基，三氟甲基，三氟甲氧基，羧基，硝基，氨基，单或二（C 1-6烷基） - 氨基，一烷基或二（C 1-6烷基） - 氨基磺酰基，C 1-6烷基，C 1-6烷氧基，C 1-6烷基羰基，C 1-6烷氧基 - 羰基; R 7和R 8各自独立地为氢，羟基，C 1-6烷基，C 1-6烷氧基或R 7和R 8一起可以形成一或二（氰基）亚甲基，或与它们所连接的碳原子一起形成羰基或螺环取代基; 或者R 7和R 8一起形成亚甲基; R 13是氢，C 1-6烷基或三氟甲基; R 14是氢，C 1-6烷基，氰基或三氟甲基; n为0至6.这些化合物在大鼠中作为mCPP拮抗剂测试。式（I）化合物可用作治疗或预防CNS障碍，心血管疾病或胃肠道疾病的治疗剂。

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