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1. 发明申请

US20080214572A1 Selected Tetracyclic Tetrahydrofuran Derivatives Containing a Cyclic Amine Side Chain 审中-公开
标题翻译：含有环胺侧链的四环四氢呋喃衍生物
公开(公告)号：US20080214572A1
公开(公告)日：2008-09-04
申请号：US11914169
申请日：2006-05-17
申请人： Francisco Javier Fernandez-Gadea , Jose Ignacio Andres-Gil , Andres Avelino Trabanco-Suarez , Jose Maria Cid-Nunez , Antonius Adrianus Hendrikus Petrus Megens
发明人： Francisco Javier Fernandez-Gadea , Jose Ignacio Andres-Gil , Andres Avelino Trabanco-Suarez , Jose Maria Cid-Nunez , Antonius Adrianus Hendrikus Petrus Megens
IPC分类号： A61K31/495 , C07D241/04 , C07D211/14 , A61K31/4453 , A61P25/00 , A61P25/18 , A61P25/06
CPC分类号： C07D405/06 , C07D307/93 , C07D493/04 , C07D495/04
摘要： This invention concerns novel tetracyclic tetrahydrofuran derivatives containing a cyclic amine side chain with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production.The compounds according to the invention can be represented by general Formula (I) and comprises also a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof, and a quaternary ammonium salt thereof, wherein all substituents are defined as in claim 1.
摘要翻译：本发明涉及含有对五羟色胺受体，特别是5-HT 2A和5-HT 2C受体具有结合亲合力的环胺侧链的新型四环四氢呋喃衍生物，以及针对多巴胺受体，特别是多巴胺D 2受体，包含本发明化合物的药物组合物，其作为药物的用途，特别是用于预防和/或治疗一系列精神和神经障碍，特别是某些精神病，心血管和胃肠功能障碍及其生产过程。根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式及其季铵盐，其中所有取代基如权利要求1中所定义。

2. 发明申请

US20090023721A1 Novel Substituted Tetracyclic Tetrahydrofuran, Pyrrolidine and Tetrahydrothiophene Derivatives and Their Use as a Medicament 审中-公开
标题翻译：新型取代四环四氢呋喃，吡咯烷和四氢噻吩衍生物及其作为药物的用途
公开(公告)号：US20090023721A1
公开(公告)日：2009-01-22
申请号：US11915202
申请日：2006-05-24
申请人： Antonius Adrianus Hendrikus Petrus Megens , Andres Avelino Trabanco-Suarez , Jose Maria Cid-Nunez , Hua Mao , Sushil Chandra Jha , Francisco Javier Fernandez-Gadea , Mohamed Koukni , Georges Joseph Cornelius Hoornaert , Frans Josef Cornelius Compernolle , Tomasz Kozlecki
发明人： Antonius Adrianus Hendrikus Petrus Megens , Andres Avelino Trabanco-Suarez , Jose Maria Cid-Nunez , Hua Mao , Sushil Chandra Jha , Francisco Javier Fernandez-Gadea , Mohamed Koukni , Georges Joseph Cornelius Hoornaert , Frans Josef Cornelius Compernolle , Tomasz Kozlecki
IPC分类号： A61K31/4184 , C07D235/02 , C07D241/36 , C07D333/50 , A61K31/498 , A61K31/35 , A61K31/5377 , A61P25/00 , A61K31/403 , A61K31/381 , C07D311/02 , C07D209/56 , C07D413/12
CPC分类号： C07D209/94 , C07D221/18 , C07D307/93 , C07D311/94 , C07D333/80 , C07D487/04 , C07D491/04
摘要： This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production.The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
摘要翻译：本发明涉及对5-羟色胺受体，特别是5-HT2A和5-HT2C受体以及对多巴胺受体，特别是多巴胺D2受体和去甲肾上腺素再摄取抑制性质具有结合亲和力的新型取代四环四氢呋喃，吡咯烷和四氢噻吩衍生物，包含根据本发明的化合物，其用作药物，特别是用于预防和/或治疗一系列精神和神经障碍，特别是某些精神病性，心血管和胃肠功能障碍及其生产方法。根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式及其前药，其中所有取代基定义为在权利要求1中。

3. 发明申请

US20080287450A1 Novel Substituted Tetracyclic Tetahydrofuran, Pyrrolidine And Tetrahydrothiophene Derivatives 有权
标题翻译：新型四取代四氢呋喃，吡咯烷和四氢噻吩衍生物
公开(公告)号：US20080287450A1
公开(公告)日：2008-11-20
申请号：US11815726
申请日：2005-12-06
申请人： Jose Maria Cid-Nunez , Antonius Adrianus Hendrikus Petrus Megens , Andres Avelino Trabanco-Suarez , Mohamed Koukni , Georges Joseph Cornelius Hoornaert , Frans Josef Cornelius Compernolle , Tomasz Kozlecki , Hua Mao , Sushil Chandra Jha , Francisco Javier Fernandez-Gadea
发明人： Jose Maria Cid-Nunez , Antonius Adrianus Hendrikus Petrus Megens , Andres Avelino Trabanco-Suarez , Mohamed Koukni , Georges Joseph Cornelius Hoornaert , Frans Josef Cornelius Compernolle , Tomasz Kozlecki , Hua Mao , Sushil Chandra Jha , Francisco Javier Fernandez-Gadea
IPC分类号： A61K31/403 , C07D487/04 , C07D209/56 , C07D491/044 , A61K31/4985 , A61K31/352 , A61P3/04 , A61P25/00 , A61K31/381 , A61K31/407 , C07D333/50 , C07D311/94
CPC分类号： C07D333/80 , C07D209/70 , C07D221/18 , C07D307/93 , C07D311/94 , C07D487/04 , C07D491/04
摘要： This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production.The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
摘要翻译：本发明涉及对5-羟色胺受体，特别是5-HT 2A和5-HT 2C受体具有结合亲和力的新型取代四环四氢呋喃，吡咯烷和四氢噻吩衍生物，并且涉及多巴胺受体，特别是多巴胺D2受体和去甲肾上腺素再摄取抑制性质，包含根据本发明的化合物的药物组合物，其作为药物的用途，特别是用于预防和/或治疗一系列精神和神经障碍，特别是某些精神病，心血管和胃肠功能障碍及其生产过程。根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式及其前药，其中所有取代基定义为在权利要求1中。

4. 发明授权

US5952510A 1,3-dihydro-1-(phenylalkenyl)-2H-imidazol-2-one derivatives having PDE IV and cytokine inhibiting activity 失效
标题翻译：具有PDE IV和细胞因子抑制活性的1,3-二氢-1-（苯基烯基）-2H-咪唑-2-酮衍生物
公开(公告)号：US5952510A
公开(公告)日：1999-09-14
申请号：US945849
申请日：1997-09-30
申请人： Eddy Jean Edgard Freyne , Gaston Stanislas Marcella Diels , Jose Ignacio Andres-Gil , Francisco Javier Fernandez-Gadea
发明人： Eddy Jean Edgard Freyne , Gaston Stanislas Marcella Diels , Jose Ignacio Andres-Gil , Francisco Javier Fernandez-Gadea
IPC分类号： A61K31/415 , A61K31/4166 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D233/32 , C07D233/38 , C07D233/70
CPC分类号： C07D233/32 , C07D233/70
摘要： The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; difluoromethyl; trifluoromethyl; C.sub.3-6 cycloalkyl; a saturated 5-, 6 or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo�2.2.1!-2-heptenyl; bicyclo�2.2.1!heptanyl; C.sub.1-6 alkylsulfonyl; arylsulfonyl; or substituted C.sub.1-10 alkyl; R.sup.3 is hydrogen, halo or C.sub.1-6 alkyloxy; R.sup.4 is hydrogen; cyano; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkyloxycarbonyl or aryl; R.sup.5 is hydrogen; cyano; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkyloxycarbonyl or aryl; Y is a direct bond or C.sub.1-3 alkanediyl; --A--B-- is a bivalent radical of formula --CR.sup.6 .dbd.CR.sup.7 -- or --CHR.sup.6 --CHR.sup.7 --; L is hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; C.sub.1-6 alkyloxycarbonyl; C.sub.1-6 alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl;, -furanyl or -thienyl; having PDE IV and cytokine inhibiting activity. Further, pharmaceutical compositions, preparations and use as a medicine are described.
摘要翻译： PCT No.PCT / EP96 / 01395 Sec。 371日期：1997年9月30日 102（e）1997年9月30日PCT PCT 1996年3月28日PCT公布。 WO96 / 31486 PCT公开号日期：1996年10月10日本发明涉及N-氧化物形式的化合物，其药学上可接受的酸或碱加成盐及其立体化学异构形式，其中R 1和R 2各自独立地为氢; C 1-6烷基; 二氟甲基三氟甲基 C 3-6环烷基; 含有一个或两个选自氧，硫或氮的杂原子的饱和的5-，6-或7-元杂环; 茚满基双环[2.2.1] -2-庚烯基; 双环[2.2.1]庚基; C 1-6烷基磺酰基; 芳基磺酰基; 或取代的C 1-10烷基; R3是氢，卤素或C1-6烷氧基; R4是氢; 氰基; 任选取代的C 1-6烷基; C 1-6烷氧基羰基或芳基; R5是氢; 氰基; 任选取代的C 1-6烷基; C 1-6烷氧基羰基或芳基; Y是直接键或C1-3烷二基; -A-B-是式-CR6 = CR7-或-CHR6-CHR7-的二价基团; L是氢; 任选取代的C 1-6烷基; C 1-6烷基羰基; C 1-6烷氧基羰基; C 1-6烷基磺酰基或芳基磺酰基; 芳基是任选取代的苯基; 哌嗪基，呋喃基或噻吩基;吗啉基或任选取代的哌啶基，哌嗪基，具有PDE IV和细胞因子抑制活性。此外，描述了作为药物的药物组合物，制剂和用途。

5. 发明授权

US5773433A Substituted tetracyclic oxazepine and thiazepine derivatives 失效
标题翻译：取代的四环氧氮杂和硫氮杂衍生物
公开(公告)号：US5773433A
公开(公告)日：1998-06-30
申请号：US817989
申请日：1997-04-25
申请人： Francisco Javier Fernandez-Gadea , Victor Karel Sipido , Jose Ignacio Andres-Gil , Theo Frans Meert
发明人： Francisco Javier Fernandez-Gadea , Victor Karel Sipido , Jose Ignacio Andres-Gil , Theo Frans Meert
IPC分类号： A61K31/535 , A61K31/55 , A61K31/553 , A61K31/554 , A61P9/00 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/26 , C07D261/20 , C07D267/16 , C07D498/04 , C07D513/04
CPC分类号： C07D513/04
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 to R.sup.10 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 alkyloxycarbonyl; R.sup.11 is hydrogen, C.sub.1-6 alkyl, or trifluoromethyl; R.sup.12 is hydrogen, C.sub.1-6 alkyl, cyano, or trifluoromethyl; n is zero to 6; and X is O, S, S(.dbd.O) or S(.dbd.O).sub.2. 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 / EP95 / 04197 Sec。 371日期1997年04月25日 102（e）日期1997年4月25日PCT提交1995年10月25日PCT公布。 WO96 / 14321 PCT出版物日期1996年5月17日本发明涉及式（I）化合物，其药学上可接受的盐和立体异构形式，以及其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至R10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（C1-6烷基）氨基，C1-6烷基羰基氨基，氨基磺酰基，单或二（C1-6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 11是氢，C 1-6烷基或三氟甲基; R 12是氢，C 1-6烷基，氰基或三氟甲基; n为0〜6; X为O，S，S（= O）或S（= O）2）。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

US5994376A 1,3-dihydro-1-(phenylalkyl)-2H-imidazol-2-one compounds and their use for treating allergic, atopic or inflammatory diseases 失效
标题翻译： 1,3-二氢-1-（苯基烷基）-2H-咪唑-2-酮化合物及其用于治疗过敏性，特应性或炎性疾病的用途
公开(公告)号：US5994376A
公开(公告)日：1999-11-30
申请号：US930296
申请日：1997-09-29
申请人： Eddy Jean Edgard Freyne , Gaston Stanislas Marcella Diels , Jose Ignacio Andres-Gil , Francisco Javier Fernandez-Gadea
发明人： Eddy Jean Edgard Freyne , Gaston Stanislas Marcella Diels , Jose Ignacio Andres-Gil , Francisco Javier Fernandez-Gadea
IPC分类号： C07D233/32 , A61K31/415 , A61K31/4166 , A61K31/44 , A61K31/4427 , A61K31/443 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D233/36 , C07D233/38 , C07D233/70 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12
CPC分类号： C07D401/06 , C07D233/36 , C07D233/38 , C07D233/70
摘要： The present invention describes 1,3-dihydro-1-(phenylalkyl)-2H-imidazol-2-one compounds and their use for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases.
摘要翻译： PCT No.PCT / EP96 / 01394 Sec。 371日期：1997年9月29日 102（e）1997年9月29日PCT PCT 1996年3月28日PCT公布。出版物WO96 / 31485 日期：1996年10月10日本发明描述了1,3-二氢-1-（苯基烷基）-2H-咪唑-2-酮化合物及其用于治疗与异常酶促或催化活性有关的疾病状态的温血动物磷酸二酯酶IV（PDE IV）和/或与细胞因子的生理有害过量相关的疾病状态，特别是过敏性，特应性和炎性疾病。

7. 发明授权

US5869515A 1,3-dihydro-2H-imidazol-2-one compounds 失效
标题翻译： 1,3-二氢-2H-咪唑-2-酮化合物
公开(公告)号：US5869515A
公开(公告)日：1999-02-09
申请号：US930478
申请日：1997-09-29
申请人： Eddy Jean Edgard Freyne , Gaston Stanislas Marcella Diels , Jose Ignacio Andres-Gil , Francisco Javier Fernandez-Gadea
发明人： Eddy Jean Edgard Freyne , Gaston Stanislas Marcella Diels , Jose Ignacio Andres-Gil , Francisco Javier Fernandez-Gadea
IPC分类号： A61K31/415 , A61K31/4166 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D233/32 , C07D233/38 , C07D233/70 , C07D405/04 , C07D405/06
CPC分类号： C07D405/04 , C07D233/32 , C07D233/70
摘要： The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; difluoromethyl; trifluoromethyl; C.sub.3-6 cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo�2.2.1!-2-heptenyl; bicyclo�2.2.1!heptanyl; C.sub.1-6 alkylsulfonyl; arylsulfonyl; or substituted C.sub.1-10 alkyl; R3 is hydrogen, halo or C.sub.1-6 alkyloxy ##STR2## is a bivalent radical of formula ##STR3## Alk is C1-4alkanediyl; --A--B-- is a bivalent radical of formula: --CR.sup.6 .dbd.CR.sup.7 -- or --CHR.sup.6 --CHR.sup.7 --; L is hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; C.sub.1-6 alkyloxycarbonyl; optionally substituted C.sub.3-6 alkenyl; optionally substituted piperidinyl; C.sub.1-6 alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het.sup.1 is morpholinyl or optionally substituted pyridinyl, -furanyl, -thienyl, -hydroxypyridinyl, -imidazolyl, -thiazolyl, -oxazolyl, -isoquinolinyl, -quinolinonyl, -piperidinyl, -piperazinyl; and Het.sup.2 is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl, -furanyl or -thienyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I) and pharmaceutical compositions thereof.
摘要翻译： PCT No.PCT / EP96 / 01393 Sec。 371日期：1997年9月29日 102（e）1997年9月29日PCT PCT 1996年3月28日PCT公布。公开号WO96 / 31487 日期：1996年10月10日本发明涉及式（I）的化合物：（I）N-氧化物形式，其药学上可接受的酸或碱加成盐及其立体化学异构形式，其中R1和R2各自独立地为氢; C 1-6烷基; 二氟甲基三氟甲基 C 3-6环烷基; 含有一个或两个选自氧，硫或氮的杂原子的饱和的5-，6-或7-元杂环; 茚满基双环[2.2.1] -2-庚烯基; 双环[2.2.1]庚基; C 1-6烷基磺酰基; 芳基磺酰基; 或取代的C 1-10烷基; R 3是氢，卤素或C 1-6烷氧基，是下式的二价基团：其中A k是C 1-4烷二基; -A-B-是下式的二价基团：-CR 6 = CR 7 - 或-CHR 6 -CHR 7 - ; L是氢; 任选取代的C 1-6烷基; C 1-6烷基羰基; C 1-6烷氧基羰基; 任选取代的C 3-6烯基; 任选取代的哌啶基; C 1-6烷基磺酰基或芳基磺酰基; 芳基是任选取代的苯基; - Het1是吗啉基或任意取代的吡啶基， - 呋喃基， - 噻吩基， - 羟基吡啶基， - 咪唑基， - 噻唑基， - 恶唑基， - 异喹啉基， - 喹啉酮基， - 哌啶基，和Het2是吗啉基或任选取代的哌啶基，哌嗪基， - 吡啶基， - 呋喃基或 - 噻吩基; 具有PDE IV和细胞因子抑制活性。本发明还涉及制备式（I）化合物及其药物组合物的方法。

8. 发明授权

US5990123A Vasoconstrictive substituted 2,3-dihydro-1,4-dioxinopyridines 失效
标题翻译：血管收缩性取代2,3-二氢-1,4-二恶英吡啶
公开(公告)号：US5990123A
公开(公告)日：1999-11-23
申请号：US875835
申请日：1997-08-06
申请人： Guy Rosalia Eugene Van Lommen , Jose Ignacio Andres-Gil , Francisco Javier Fernandez-Gadea , Maria Encarnacion Matesanz-Ballesteros
发明人： Guy Rosalia Eugene Van Lommen , Jose Ignacio Andres-Gil , Francisco Javier Fernandez-Gadea , Maria Encarnacion Matesanz-Ballesteros
IPC分类号： A61K31/435 , A61P9/08 , A61P25/04 , A61P25/06 , C07D491/04 , C07D491/056
CPC分类号： C07D491/04
摘要： The present invention is concerned with compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein .dbd.a.sub.1 --a.sub.2 .dbd.a.sub.3 --a.sub.4 .dbd. is a bivalent radical of formula .dbd.N--CH.dbd.CH--CH.dbd. (a), .dbd.CH--N.dbd.CH--CH.dbd. (b), .dbd.CH--CH.dbd.N--CH.dbd. (c), .dbd.CH--CH.dbd.CH--N.dbd. (d), wherein one or two hydrogen atoms can be substituted by halo, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is C.sub.1-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a five- or six-membered heterocyclic ring containing at least one nitrogen atom or a radical of formula --C(NR.sup.5 R.sup.6).dbd.C--R.sup.4 wherein R.sup.4 is hydrogen, cyano, aminocarbonyl or C.sub.1-6 alkyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.6 is hydrogen or C.sub.1-6 alkyl; or R.sup.5 and R.sup.6 taken together may form a bivalent radical of formula --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --.Pharmaceutical compositions, preparations and use as a medicine are described.
摘要翻译： PCT No.PCT / EP96 / 00396 Sec。 371日期：1997年8月6日 102（e）日期1997年8月6日PCT 1996年1月30日PCT PCT。公开号WO96 / 24596 日期：1996年8月15日本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐及其立体化学异构形式，其中= a1-a2 = a3-a4 =是式= N-CH = CH-CH =（a），= CH-N = CH-CH =（b），= CH-CH = N-CH =（c），= CH-CH = CH-N =（d）其中一个或两个氢原子可以被卤素，羟基，C 1-6烷基或C 1-6烷氧基取代; R1是氢或C1-6烷基; R2是氢或C1-6烷基; R3是氢或C1-6烷基; Alk1是C1-5烷二基; Alk2是C2-15烷二基; Q是含有至少一个氮原子或式-C（NR 5 R 6）= C-R 4的基团的五元或六元杂环，其中R 4是氢，氰基，氨基羰基或C 1-6烷基; R5是氢，C1-6烷基，C3-6烯基或C3-6炔基; R6是氢或C1-6烷基; 或R 5和R 6一起形成式 - （CH 2）4 - 或 - （CH 2）5 - 的二价基团。描述了作为药物的药物组合物，制剂和用途。

9. 发明授权

US6156747A Isoxazolidine derivatives 有权
标题翻译：异恶唑烷衍生物
公开(公告)号：US6156747A
公开(公告)日：2000-12-05
申请号：US155839
申请日：1998-10-06
申请人： Jose Ignacio Andres-Gil , Pedro Martinez-Jimenez , Francisco Javier Fernandez-Gadea , Victor Karel Sipido
发明人： Jose Ignacio Andres-Gil , Pedro Martinez-Jimenez , Francisco Javier Fernandez-Gadea , Victor Karel Sipido
IPC分类号： A61K31/00 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/553 , A61P1/00 , A61P9/00 , A61P9/12 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D237/30 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D498/14 , C07D498/16 , C07D223/14 , C07D243/00 , C07D255/00 , C07D498/22
CPC分类号： C07D237/30 , C07D471/04 , C07D487/04
摘要： This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero to 6; p is zero to 3; q is zero to 3; r is zero to 3; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; 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, trihalomethyl, trihalomethoxy, 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 or C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or trihalomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.2 ; each ##STR2## independently represents a bivalent aromatic heterocycle wherein the heterocycle may be selected from the group consisting of pyrrole, pyrrazole, imidazole, triazole, furane, thiophene, isoxazole, oxazole, isothiazole, thiazole, pyridine, pyridazine, pyrimidine, pyrazine and triazine; or one of the two bivalent aromatic heterocycles in the compounds of formula (I) may be 1,2-benzenediyl; and aryl is optionally substituted phenyl; it further relates to compositions comprising thesae compounds, as well as their use 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 / 01830 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。 WO97 / 39001 PCT出版物日期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和立体化学异构体形式，其中n为0-6; p为0〜3; q为零至3; r为0〜3; 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; 三卤代甲基羰基或者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，三卤代甲基，三卤甲氧基，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，单或二（C 1-6烷基） - 氨基磺酰基，C 1-6烷基，C 1-6烷氧基，C 1-6烷基羰基或C 1-6烷氧基羰基; 每个R 5独立地是C 1-6烷基，氰基或三卤代甲基; X是CR 6 R 7，NR 8，O，S，S（= O）或S（= O）2; 各自独立地表示二价芳族杂环，其中杂环可以选自吡咯，吡唑，咪唑，三唑，呋喃，噻吩，异恶唑，恶唑，异噻唑，噻唑，吡啶，哒嗪，嘧啶，吡嗪和三嗪。或式（I）化合物中的两个二价芳族杂环中的一个可以是1,2-苯二基; 芳基是任选取代的苯基; 它还涉及包含该化合物的组合物，以及它们在治疗或预防CNS障碍，心血管疾病或胃肠道疾病中作为治疗剂的用途。

10. 发明授权

US6051718A PDE IV inhibiting 2-cyanoiminoimidazole derivatives 有权
标题翻译： PDE IV抑制2-氰基亚氨基咪唑衍生物
公开(公告)号：US6051718A
公开(公告)日：2000-04-18
申请号：US147925
申请日：1999-03-19
申请人： Eddy Jean Edgard Freyne , Francisco Javier Fernandez-Gadea , Jose Ignacio Andres-Gil
发明人： Eddy Jean Edgard Freyne , Francisco Javier Fernandez-Gadea , Jose Ignacio Andres-Gil
IPC分类号： C07D233/44 , A61K31/00 , A61K31/415 , A61K31/4164 , A61K31/4168 , A61P11/00 , A61P11/06 , A61P29/00 , A61P37/00 , A61P37/08 , C07D233/48 , C07D233/88 , C07D405/12 , C07D233/32 , C07D221/02 , C07D233/36 , C07D233/38 , C07D233/70 , A61R31/4168 , A61R31/438
CPC分类号： C07D405/12 , C07D233/48 , C07D233/88
摘要： The present invention concerns 2-cyanoiminoimidazole derivatives having the formula ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; difluoromethyl; trifluoromethyl; C.sub.3-6 cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; 6,7-dihydro-5H-cyclopentapyridinyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C.sub.1-6 alkylsulfonyl; arylsulfonyl; or substituted C.sub.1-10 alkyl; R.sup.3 is hydrogen, halo or C.sub.1-6 alkyloxy; R.sup.4 is hydrogen; halo; C.sub.1-6 alkyl; trifluoromethyl; C.sub.3-6 cycloalkyl; carboxyl; C.sub.1-4 alkyloxycarbonyl; C.sub.3-6 cycloalkylaminocarbonyl; aryl; Het.sup.1 ; or substituted C.sub.1-6 alkyl; or R.sup.4 is --O--R.sup.7 or --NH--R.sup.8 ; R.sup.5 is hydrogen, halo, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.6 is a hydrogen or C.sub.1-4 alkyl; or R.sup.4 and R.sup.6, or R.sup.4 and R.sup.5 taken together may form a bivalent radical; --A--B-- is --CR.sup.10 .dbd.CR.sup.11 -- or --CHR.sup.10 --CHR.sup.11 --; L is hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; C.sub.1-6 alkyloxycarbonyl; substituted C.sub.1-6 alkyl; C.sub.3-6 alkenyl; substituted C.sub.3-6 alkenyl; piperidinyl; substituted piperidinyl; C.sub.1-6 alkylsulfonyl or arylsulfonyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I) and pharmaceutical compositions thereof.
摘要翻译： PCT No.PCT / EP97 / 05322 Sec。 371日期1999年3月19日 102（e）1999年3月19日PCT PCT 1997年9月24日PCT公布。公开号WO98 / 14432 日期：1998年4月9日本发明涉及具有N-氧化物形式的2-氰基亚氨基咪唑衍生物，其药学上可接受的加成盐和立体化学异构形式，其中R 1和R 2各自独立地为氢; C 1-6烷基; 二氟甲基三氟甲基 C 3-6环烷基; 含有一个或两个选自氧，硫或氮的杂原子的饱和的5-，6-或7-元杂环; 茚满基 6,7-二氢-5H-环戊吡啶基; 双环[2.2.1] -2-庚烯基; 双环[2.2.1]庚基; C 1-6烷基磺酰基; 芳基磺酰基; 或取代的C 1-10烷基; R3是氢，卤素或C1-6烷氧基; R4是氢; 光环; C 1-6烷基; 三氟甲基 C 3-6环烷基; 羧基; C 1-4烷氧基羰基; C 3-6环烷基氨基羰基; 芳基; Het1; 或取代的C 1-6烷基; 或R 4为-O-R 7或-NH-R 8; R5是氢，卤素，羟基，C1-6烷基或C1-6烷氧基; R6是氢或C1-4烷基; 或R4和R6，或R4和R5一起可以形成二价基团; -A-B-是-CR10 = CR11-或-CHR10-CHR11-; L是氢; C 1-6烷基; C 1-6烷基羰基; C 1-6烷氧基羰基; 取代的C 1-6烷基; C 3-6烯基; 取代的C 3-6烯基; 哌啶基; 取代的哌啶基; C 1-6烷基磺酰基或芳基磺酰基; 具有PDE IV和细胞因子抑制活性。本发明还涉及制备式（I）化合物及其药物组合物的方法。

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