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1. 发明授权

US6113527A Diaza-spiro[3,5] nonane derivatives 失效
标题翻译： Diaza-spiro [3,5]壬烷衍生物
公开(公告)号：US6113527A
公开(公告)日：2000-09-05
申请号：US330851
申请日：1999-06-11
申请人： Geo Adam , Andrea Cesura , Fran.cedilla.ois Jenck , Sabine Kolczewski , Stephan Rover , Jurgen Wichmann
发明人： Geo Adam , Andrea Cesura , Fran.cedilla.ois Jenck , Sabine Kolczewski , Stephan Rover , Jurgen Wichmann
IPC分类号： C07D401/00 , A61K31/00 , A61K31/438 , A61P3/04 , A61P9/10 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , C07D471/10 , A61K31/44 , C07D221/20
CPC分类号： C07D471/10
摘要： The invention relates to compounds of the general formula ##STR1## wherein R.sup.1 is C.sub.6-12 -cycloalkyl, optionally substituted by lower alkyl or C(O)O lower alkyl, indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; acenaphthen-1-yl; bicyclo[3.3.1]non-9-yl, octahydro-inden-2-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl, decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; decahydro-naphthalen-1-yl, decahydro-naphthalen-2-yl; tetrahydro-naphthalen-1-yl, tetrahydro-naphthalen-2-yl or 2-oxo-1,2-diphenyl-ethyl;R.sup.2 is .dbd.O or hydrogen,R.sup.3 is hydrogen, isoindolyl-1,3-dione, lower alkoxy, lower alkyl, amino, benzyloxy, --CH.sub.2 OR.sup.5 or --CH.sub.2 N(R.sup.5).sub.2 ;R.sup.4 is hydrogen or --CH.sub.2 OR.sup.5 ;R.sup.5 is hydrogen or lower alkyl; ##STR2## is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; to racemic mixtures and their corresponding enantiomers and or pharmaceutically acceptable acid addition salts thereof.The compounds of the present invention are agonists of the orphamin FQ (OFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.
摘要翻译：本发明涉及以下通式的化合物：其中R 1为C 6-12 - 环烷基，任选被低级烷基或C（O）O低级烷基，茚满-1-基或茚满-2-基取代，任选被低级烷基取代; 苊-1-基; 双环[3.3.1]壬-9-基，八氢 - 茚-2-基; 2,3-二氢-1H-苯并芬-1-基; 2,3,3a，4,5,6-六氢-1H-吩酚-1-基，十氢 - 薁-2-基; 双环[6.2.0]癸-9-基; 十氢萘-1-基，十氢萘-2-基; 四氢 - 萘-1-基，四氢 - 萘-2-基或2-氧代-1,2-二苯基 - 乙基; R2是= O或氢，R3是氢，异吲哚基-1,3-二酮，低级烷氧基，低级烷基，氨基，苄氧基，-CH 2 OR 5或-CH 2 N（R 5）2; R4是氢或-CH2OR5; R5是氢或低级烷基; 是环己基或苯基，任选被低级烷基，卤素或烷氧基取代; 外消旋混合物及其相应的对映异构体和/或其药学上可接受的酸加成盐。本发明的化合物是衍生物FQ（OFQ）受体的激动剂，因此可用于治疗与该受体有关的疾病。

2. 发明授权

US6043366A 1,3,8,-triaza spiro (4,5)decan-4-on derivatives 失效
标题翻译： 1,3,5， - 三氮螺（4,5）癸-4-酮衍生物
公开(公告)号：US6043366A
公开(公告)日：2000-03-28
申请号：US204184
申请日：1998-12-03
申请人： Geo Adam , Andrea Cesura , Caido Galley , Fran.cedilla.ois Jenck , Stephan Rover , Jurgen Wichmann
发明人： Geo Adam , Andrea Cesura , Caido Galley , Fran.cedilla.ois Jenck , Stephan Rover , Jurgen Wichmann
IPC分类号： C07D235/02 , A61K31/00 , A61K31/41 , A61K31/435 , A61K31/438 , A61P3/00 , A61P3/04 , A61P9/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D207/04 , C07D233/30 , C07D471/10 , C07D215/20 , C07D211/56 , C07D211/68
CPC分类号： C07D471/10
摘要： The present invention relates to compounds of formula I and pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明涉及式I化合物及其药学上可接受的酸加成盐。

3. 发明授权

US6166209A Piperidine derivatives 失效
标题翻译：哌啶衍生物
公开(公告)号：US6166209A
公开(公告)日：2000-12-26
申请号：US196992
申请日：1998-11-20
申请人： Geo Adam , Andrea Cesura , Guido Galley , Fran.cedilla.ois Jenck , Stephan Rover , Jurgen Wichmann
发明人： Geo Adam , Andrea Cesura , Guido Galley , Fran.cedilla.ois Jenck , Stephan Rover , Jurgen Wichmann
IPC分类号： A61K31/435 , A61K31/438 , A61K31/439 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , C07D221/20 , C07D451/04 , C07D471/10 , C07D491/10 , C07D491/107 , C07D491/20 , C07D498/10 , C07D498/20 , A61K31/40 , C07D405/04
CPC分类号： C07D471/10 , C07D221/20 , C07D491/10
摘要： The present invention relates to compounds of the formula ##STR1## wherein X is --O-- or --CH.sub.2 --;Y is --C(O)--, --(CH.sub.2).sub.n -- or --N(CH.sub.3)--;n is 1 or 2 orX and Y taken together are --CH.dbd.CH--Z is --NH--, --CH.sub.2 --, --O-- or .dbd.CH--;A.sup.1 is a group ##STR2## B is --(CH.sub.2).sub.m --; m is 0, 1 or 2;R.sup.1 and R.sup.2 are each independently hydrogen or lower alkyl;R.sup.3 is hydrogen or halogen;R.sup.4 is hydrogen or hydroxy andthe dotted line is (--CH.sub.2 --CH.sub.2 --).sub.n, and n' is 0 or 1 and to pharmaceutically acceptable acid addition salts thereof.The compounds of the present invention are antagonists of the OFQ receptor. Consequently they will be useful in the treatment of memory and attention deficits, psychiatric, neurological and physiological disorders, especially, but not limited to, amelioration of symptoms of anxiety and stress disorders, depression, memory loss due to Alzheimer's disease or other dementias, epilepsy and convulsions, acute and/or chronic pain conditions, symptoms of addictive drug withdrawal, control of water balance, Na.sup.+ excretion and arterial blood pressure disorders and metabolic disorders such as obesity.
摘要翻译：本发明涉及下式的化合物其中X是-O-或-CH 2 - ; Y是-C（O） - ， - （CH 2）n - 或-N（CH 3） - ; n为1或2或X和Y一起为-CH = CH-Z为-NH-，-CH 2 - ， - O-或= CH-; A1是基团B是 - （CH 2）m - ; m为0,1或2; R 1和R 2各自独立地为氢或低级烷基; R3是氢或卤素; R4是氢或羟基，虚线是（-CH2-CH2-）n，n'是0或1，并且其药学上可接受的酸加成盐。本发明的化合物是OFQ受体的拮抗剂。因此，它们将有助于治疗记忆和注意力缺陷，精神病学，神经和生理疾病，特别是但不限于改善焦虑和压力障碍症状，抑郁症，由阿尔茨海默病或其他痴呆症引起的记忆丧失，癫痫惊厥，急性和/或慢性疼痛病症，上瘾药物戒断症状，水分平衡控制，Na +排泄和动脉血压紊乱以及肥胖症等代谢性疾病。

4. 发明授权

US6071925A 1,3,8-triazaspiro[4,5]decan-4-one derivatives 失效
标题翻译： 1,3,8-三氮杂螺[4,5]癸-4-酮衍生物
公开(公告)号：US6071925A
公开(公告)日：2000-06-06
申请号：US9457
申请日：1998-01-20
申请人： Geo Adam , Andrea Cesura , Guido Galley , Fran.cedilla.ois Jenck , Frederick Monsma, Jr. , Stephan Rover , Jurgen Wichmann
发明人： Geo Adam , Andrea Cesura , Guido Galley , Fran.cedilla.ois Jenck , Frederick Monsma, Jr. , Stephan Rover , Jurgen Wichmann
IPC分类号： C07D233/04 , A61K31/00 , A61K31/41 , A61K31/435 , A61K31/438 , A61K31/445 , A61K31/55 , A61K51/02 , A61P3/04 , A61P3/12 , A61P9/00 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D215/58 , C07D305/14 , C07D471/00 , C07D471/10 , C07D498/00 , C07D211/98
CPC分类号： C07D471/10
摘要： The present invention relates to compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each independently hydrogen, lower alkyl, lower alkoxy or halogen;R.sup.3 is phenyl, which is unsubstituted or substituted by lower alkyl, CF.sub.3, lower alkoxy or halogen;R.sup.4 is hydrogen, lower alkyl, lower alkenyl, --C(O)-lower alkyl, --C(O)-phenyl, lower alkyl-C(O)-phenyl, lower alkylene-C(O)O-lower alkyl, lower alkantriyl-di-C(O)O-lower alkyl, hydroxy-lower alkyl, lower alkyl-O-lower alkyl, lower alkyl-CH(OH)CF.sub.3, phenyl or benzyl,R.sup.5 and R.sup.6 are each independently hydrogen, phenyl, lower alkyl or di-lower alkyl or R.sup.5 and R.sup.6 together with the carbon atoms to which they are bound form a phenyl ring, orR.sup.5 and one of R.sup.1 or R.sup.2 together with the carbon atoms to which they are bound form a saturated or unsaturated 6 membered ring,A is a 4-7 membered saturated ring, their racemates and the enantiomers thereof, and thepharmaceutically acceptable acid addition salts thereof which are agonists and/or antagonists of the OFQ receptor.
摘要翻译：本发明涉及下式的化合物，其中R 1和R 2各自独立地为氢，低级烷基，低级烷氧基或卤素; R3是未取代的或被低级烷基，CF 3，低级烷氧基或卤素取代的苯基; R4是氢，低级烷基，低级烯基，-C（O） - 低级烷基，-C（O） - 苯基，低级烷基-C（O） - 苯基，低级亚烷基-C（O）O-低级烷基，低级烷基 - 二-C（O）O-低级烷基，羟基 - 低级烷基，低级烷基-O-低级烷基，低级烷基-CH（OH）CF 3，苯基或苄基，R 5和R 6各自独立地为氢，苯基，低级烷基或二低级烷基或R 5和R 6与它们所连接的碳原子一起形成苯环，或R 5和R 1或R 2中的一个与它们所连接的碳原子一起形成饱和或不饱和的6元环，A是4-7元饱和环，它们的外消旋体及其对映异构体及其药学上可接受的酸加成盐，它们是OFQ受体的激动剂和/或拮抗剂。

5. 发明授权

US6075034A Spiro[piperidine-4,1'-pyrrolo [3,4-C] pyrrole]derivatives 失效
标题翻译：螺[哌啶-4,1'-吡咯并[3,4-C]吡咯]衍生物
公开(公告)号：US6075034A
公开(公告)日：2000-06-13
申请号：US330857
申请日：1999-06-11
申请人： Geo Adam , Frank Dautzenberg , Sabine Kolczewski , Stephan Rover , Jurgen Wichmann
发明人： Geo Adam , Frank Dautzenberg , Sabine Kolczewski , Stephan Rover , Jurgen Wichmann
IPC分类号： C07D401/14 , A01N43/42 , A61K31/00 , A61K31/395 , A61K31/435 , A61K31/438 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/535 , A61P3/04 , A61P3/12 , A61P9/12 , A61P25/04 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D20060101 , C07D209/00 , C07D221/00 , C07D471/10 , C07D471/20 , C07D487/20 , C07D498/10 , C07D513/10
CPC分类号： C07D471/20
摘要： The present invention relates to compounds of the general formula whereinR.sup.1 is C.sub.5-12 -cycloalkyl, optionally substituted by lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; acenaphthen-1-yl; bicyclo[3.3.1]non-9-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl; octahydro-inden-2-yl; 1,2,3,4-tetrahydro-naphthalen-1-yl; 1,2,3,4-tetrahydro-naphthalen-2-yl; naphthalen-lower alkyl-1-yl; naphthalen-lower alkyl-2-yl; acenaphthen-1-yl; and 5-isopropyl-2-methyl-bicyclo[3.1.0]hex-3-yl;R.sup.2, R.sup.3 are hydrogen; hydroxy; lower alkyl; .dbd.O; or phenyl, optionally substituted by lower allyl, halogen or alkoxy;R.sup.4 is hydrogen; lower alkyl; --(CH.sub.2).sub.n CH(OH)CF.sub.3 ; --(CH.sub.2).sub.n C.sub.3-6 -cycloalkyl; phenyl; benzyl; tetrahydrofuran-3-yl; --(CH.sub.2).sub.n OCH.sub.2 C.sub.6 H.sub.5 ; --(CH.sub.2).sub.n morpholinyl; 3-methyl-oxetan-3-yl-methyl; --(CH.sub.2).sub.n CH.sub.2 OH; --S(O).sub.2 -lower alkyl; --C(O)-lower alkyl; --C(O)CF.sub.3 ; --C(O)(CH.sub.2).sub.n OCH.sub.3 ; --(CH.sub.2).sub.n C(O)N(lower alkyl).sub.2 ; --S(O).sub.2 heteroaryl; --C(O)heteroaryl; --S(O).sub.2 -phenyl; --S(O).sub.2 --N(lower alkyl).sub.2 ; --C(O)--C.sub.3-6 -cycloalkyl; --C(O)O-phenyl; or --C(O)O-lower alkyl:R.sup.5 is hydrogen; halogen; lower alkyl; trifluoromethyl or lower alkoxy;n is 0-3;and to pharmaceutically acceptable acid addition salts thereofThe compounds of formula I and their salts are useful as in the treatment of psychiatric, neurological and physiological disorders.
摘要翻译：本发明涉及以下通式的化合物：其中R 1为任选被低级烷基取代的C 5-12 - 环烷基; 十氢萘-1-基; 十氢萘-2-基; 茚满-1-基或茚满-2-基，任选被低级烷基取代; 十氢 - 薁-2-基; 双环[6.2.0]癸-9-基; 苊-1-基; 双环[3.3.1]壬-9-基; 2,3-二氢-1H-苯并芬-1-基; 2,3,3a，4,5,6-六氢-1H-苯并芬-1-基; 八氢茚-2-基; 1,2,3,4-四氢 - 萘-1-基; 1,2,3,4-四氢 - 萘-2-基; 萘 - 低级烷基-1-基; 萘 - 低级烷基-2-基; 苊-1-基; 和5-异丙基-2-甲基 - 双环[3.1.0]己-3-基; R2，R3是氢; 羟基; 低级烷基 = O; 或苯基，任选被低级烯丙基，卤素或烷氧基取代; R4是氢; 低级烷基 - （CH 2）n CH（OH）CF 3; - （CH 2）n C 3-6 - 环烷基; 苯基; 苄基; 四氢呋喃-3-基; - （CH 2）n OCH 2 C 6 H 5; - （CH2）nmorpholinyl; 3-甲基 - 氧杂环丁烷-3-基 - 甲基; - （CH 2）n CH 2 OH; -S（O）2 - 低级烷基; -C（O） - 低级烷基; -C（O）CF 3; -C（O）（CH 2）n OCH 3; - （CH 2）n C（O）N（低级烷基）2; -S（O）2杂芳基; -C（O）杂芳基; -S（O）2 - 苯基; -S（O）2 -N（低级烷基）2; -C（O）-C 3-6 - 环烷基; -C（O）O-苯基; 或-C（O）O-低级烷基：R5是氢; 卤素; 低级烷基三氟甲基或低级烷氧基; n为0-3; 和其药学上可接受的酸加成盐。式I化合物及其盐可用于治疗精神病学，神经学和生理学疾病。

6. 发明授权

US5877193A Use of N-(4-aryl-thiazol-2-yl)-sulfonamides 失效
标题翻译：使用N-（4-芳基 - 噻唑-2-基） - 磺酰胺
公开(公告)号：US5877193A
公开(公告)日：1999-03-02
申请号：US874050
申请日：1997-06-12
申请人： Andrea Cesura , Stephan Rover
发明人： Andrea Cesura , Stephan Rover
IPC分类号： C07D277/20 , A61K31/00 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61P9/00 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/28 , A61P31/00 , A61P37/00 , A61P37/02 , A61P43/00 , C07D277/00 , C07D277/02 , C07D277/22 , C07D277/50 , C07D277/52 , C07D417/12
CPC分类号： A61K31/427 , A61K31/426
摘要： The invention is concerned with the use of sulfonamide derivatives of the general formula ##STR1## wherein R signifies lower-alkyl, phenyl, benzyl, naphthyl, pyridyl or thienyl, optionally substituted by one or more lower-alkyl, lower-alkoxy, lower-alkyl carbonyl-amino, halogen, cycloalkyl, nitro, amino, methylenedioxy, phenoxy or benzyloxy substituents, and the aromatic rings, can, in turn, be substituted by nitro, halogen or amino,R.sup.1 -R.sup.4 signify hydrogen, halogen, hydroxy, lower-alkyl, nitro, cyano, amino, lower-alkoxy, benzyloxy, trifluoromethyl or phenyl, optionally substituted by one or more lower-alkyl, trifluoromethyl, nitro, amino or hydroxy substituents, and wherein R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 together can form a benzene ring which optionally can be substituted by halogen, trifluoromethyl, nitro, lower-alkyl or lower alkoxy,and of their pharmaceutically acceptable salts as kynurenin-3-hydroxylase inhibitors in the control or prevention of neuro-degenerative disorders, neurological disorders resulting from an activation of the immune system, or psychiatric illnesses and, respectively, for the production of corresponding medicaments.
摘要翻译：本发明涉及使用通式为“IMAGE”I的磺酰胺衍生物，其中R表示低级烷基，苯基，苄基，萘基，吡啶基或噻吩基，任选地被一个或多个低级烷基，低级烷氧基，低级 - 烷基羰基 - 氨基，卤素，环烷基，硝基，氨基，亚甲二氧基，苯氧基或苄氧基取代基，芳环可以被硝基，卤素或氨基取代，R1-R4表示氢，卤素，羟基，低级烷基，硝基，氰基，氨基，低级烷氧基，苄氧基，三氟甲基或苯基，任选地被一个或多个低级烷基，三氟甲基，硝基，氨基或羟基取代基取代，并且其中R1和R2或R2和R3一起可以形成苯环，其任选地可以被卤素，三氟甲基，硝基，低级烷基或低级烷氧基取代，以及它们的药学上可接受的盐作为犬尿胆素-3-羟化酶抑制剂在控制或预防神经退行性疾病，神经病学由免疫系统的激活引起的疾病或精神疾病，以及分别用于生产相应的药物。

7. 发明授权

US5958910A Use of N-(4-aryl-thiazol-2-yl)-sulfonamides 失效
标题翻译：使用N-（4-芳基 - 噻唑-2-基） - 磺酰胺
公开(公告)号：US5958910A
公开(公告)日：1999-09-28
申请号：US197070
申请日：1998-11-20
申请人： Andrea Cesura , Stephan Rover
发明人： Andrea Cesura , Stephan Rover
IPC分类号： C07D277/20 , A61K31/00 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61P9/00 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/28 , A61P31/00 , A61P37/00 , A61P37/02 , A61P43/00 , C07D277/00 , C07D277/02 , C07D277/22 , C07D277/50 , C07D277/52 , C07D417/12
CPC分类号： A61K31/427 , A61K31/426
摘要： The invention is concerned with the use of sulfonamide derivatives of the general formula ##STR1## wherein R Signifies lower-alkyl, phenyl, benzyl, naphthyl, pyridyl or thienyl, optionally substituted by one or more lower-alkyl, lower-alkoxy, lower-alkyl carbonyl-amino, halogen, cycloalkyl, nitro, amino, methylenedioxy, phenoxy or benzyloxy substituents, and the aromatic rings, can, in turn, be substituted by nitro, halogen or amino,R.sup.1 -R.sup.4 signify hydrogen, halogen, hydroxy, lower-alkyl, nitro, cyano, amino, lower-alkoxy, benzyloxy, trifluoromethyl or phenyl, optionally substituted by one or more lower-alkyl, trifluoromethyl, nitro, amino or hydroxy substituents, and wherein R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 together can form a benzene ring which optionally can be substituted by halogen, trifluoromethyl, nitro, lower-alkyl or lower alkoxy,and of their pharmaceutically acceptable salts as kynurenin-3-hydroxylase inhibitors in the control or prevention of neuro-degenerative disorders, neurological disorders resulting from an activation of the immune system, or psychiatric illnesses and, respectively, for the production of corresponding medicaments.
摘要翻译：本发明涉及使用以下通式的磺酰胺衍生物，其中R表示低级烷基，苯基，苄基，萘基，吡啶基或噻吩基，任选地被一个或多个低级烷基，低级烷氧基，低级烷基羰基 - 氨基，卤素，环烷基，硝基，氨基，亚甲二氧基，苯氧基或苄氧基取代基，芳环可以被硝基，卤素或氨基取代，R 1 -R 4表示氢，卤素，羟基，低级烷基，硝基，氰基，氨基，低级烷氧基，苄氧基，三氟甲基或苯基，任选地被一个或多个低级烷基，三氟甲基，硝基，氨基或羟基取代基取代，并且其中R 1和R 2或R 2和R 3一起可以形成苯环其任选地可以被卤素，三氟甲基，硝基，低级烷基或低级烷氧基取代，以及它们的药学上可接受的盐作为犬尿胆素-3-羟化酶抑制剂在控制或预防神经退行性疾病，神经障碍是由于免疫系统的激活或精神疾病，以及分别用于生产相应的药物而产生的。

8. 发明授权

US5292732A Pyrrolopyrazine derivatives 失效
标题翻译：吡咯并吡嗪衍生物
公开(公告)号：US5292732A
公开(公告)日：1994-03-08
申请号：US905584
申请日：1992-06-26
申请人： Stephan Rover
发明人： Stephan Rover
IPC分类号： A61K31/495 , A61P25/00 , A61P25/28 , C07D207/30 , C07D207/32 , C07D207/325 , C07D207/33 , C07D207/333 , C07D209/60 , C07D241/04 , C07D307/46 , C07D405/04 , C07D487/04 , C07D233/61
CPC分类号： C07D207/325 , C07D207/33 , C07D207/333 , C07D209/60 , C07D307/46 , C07D405/04 , C07D487/04
摘要： The novel pyrrolopyrazines of the general formula ##STR1## wherein one of R.sup.1 and R.sup.2 signifies aryl and the other signifies hydrogen, lower alkyl or aryl or R.sup.1 and R.sup.2 together with the two carbon atoms denoted by .alpha. and .beta. signify the group A; ##STR2## R.sup.3 signifies hydrogen or lower alkyl and R.sup.4 signifies hydrogen orR.sup.3 and R.sup.4 together signify an additional C/N bond;R.sup.5 signifies hydrogen or lower alkyl;R.sup.6 signifies hydrogen or lower alkyl;R.sup.7 signifies hydrogen, halogen, lower alkyl, optionally substituted lower alkoxy, or C.sub.3-6 -cycloalkyl, C.sub.4-6 -cycloalkenyl, C.sub.3-6 -cycloalkyloxy, hydroxy, trifluoro- methanesulphonyloxy or optionally substituted benzyl- oxycarbonyloxy; and the dotted line signifies an optional additional C/C bond,and pharmaceutically acceptable acid addition salts of the compounds of formula I can be used in the control or prevention of illnesses or in the improvement of health, especially in the control or prevention of depressive states, cognitive disorders and neurodegenerative diseases such as Parkinson's disease and Alzheimer's disease.
摘要翻译：通式为“IMAGE”I的新型吡咯并吡嗪其中R 1和R 2中的一个表示芳基，另一个表示氢，低级烷基或芳基或R 1和R 2与由α和β表示的两个碳原子一起表示基团A; R 3表示氢或低级烷基，R 4表示氢或R 3和R 4一起表示另外的C / N键; R5表示氢或低级烷基; R6表示氢或低级烷基; R7表示氢，卤素，低级烷基，任选取代的低级烷氧基或C 3-6 - 环烷基，C 4-6 - 环烯基，C 3-6 - 环烷氧基，羟基，三氟 - 甲磺酰氧基或任选取代的苄氧基羰基氧基; 并且虚线表示任选的另外的C / C键，并且式I化合物的药学上可接受的酸加成盐可用于控制或预防疾病或改善健康，特别是在控制或预防抑郁症中状态，认知障碍和神经变性疾病如帕金森病和阿尔茨海默病。

9. 发明授权

US06071929A Octahydro phenanthridine derivatives useful as NMDA-R receptor subtype blockers 失效
标题翻译：用作NMDA-R受体亚型阻断剂的八氢菲啶衍生物
公开(公告)号：US06071929A
公开(公告)日：2000-06-06
申请号：US320307
申请日：1999-05-26
申请人： Alexander Alanine , Anne Bourson , Bernd Buttelmann , Gunther Fischer , Marie-Paule Heitz Neidhart , Vincent Mutel , Emmanuel Pinard , Stephan Rover , Gerhard Trube , Rene Wyler
发明人： Alexander Alanine , Anne Bourson , Bernd Buttelmann , Gunther Fischer , Marie-Paule Heitz Neidhart , Vincent Mutel , Emmanuel Pinard , Stephan Rover , Gerhard Trube , Rene Wyler
IPC分类号： C07D217/16 , A61K31/47 , A61K31/472 , A61K31/473 , A61K31/4741 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D217/18 , C07D217/20 , C07D217/24 , C07D221/00 , C07D221/06 , C07D221/12 , C07D491/04 , C07D491/056
CPC分类号： C07D491/04 , C07D217/18 , C07D217/20 , C07D221/12
摘要： The present invention relates to the use of tetrahydroisoquinoline derivatives of the general formula: ##STR1## wherein: A is arylR.sup.1 is hydrogen, hydroxy, lower alkyl, lower alkoxy, R--CO-- or R--COO--, wherein R is lower alkyl;R.sup.2 is hydrogen, lower alkyl or cycloalkylR.sup.3 -R.sup.7 are independently hydrogen, lower alkyl, lower alkoxy, hydroxy orR.sup.3 and R.sup.4 taken together are --(CH.sub.2).sub.n -- orR.sup.6 and R.sup.7 taken together are --OCH.sub.2 O-- andn is 3 or 4,as well as pharmaceutically acceptable salts for the manufacture of medicaments for the control or treatment of diseases which represent therapeutic indications for NMDA receptor subtype specific blockers.
摘要翻译：本发明涉及以下通式的四氢异喹啉衍生物的用途：其中：A为芳基，R 1为氢，羟基，低级烷基，低级烷氧基，R-CO-或R-COO-，其中R为低级烷基; R 2是氢，低级烷基或环烷基R 3 -R 7独立地是氢，低级烷基，低级烷氧基，羟基或者R 3和R 4一起是 - （CH 2）n - 或R 6和R 7一起是-OCH 2 O-，n是3或 4，以及用于制备用于控制或治疗代表NMDA受体亚型特异性阻断剂的治疗适应症的疾病的药物的药学上可接受的盐。

10. 发明授权

US5952344A Tetrahydroisoquinoline derivatives 失效
标题翻译：四氢异喹啉衍生物
公开(公告)号：US5952344A
公开(公告)日：1999-09-14
申请号：US8724
申请日：1998-01-19
申请人： Alexander Alanine , Anne Bourson , Bernd Buttelmann , Gunther Fischer , Marie-Paule Heitz Neidhart , Vincent Mutel , Emmanuel Pinard , Stephan Rover , Gerhard Trube , Rene Wyler
发明人： Alexander Alanine , Anne Bourson , Bernd Buttelmann , Gunther Fischer , Marie-Paule Heitz Neidhart , Vincent Mutel , Emmanuel Pinard , Stephan Rover , Gerhard Trube , Rene Wyler
IPC分类号： C07D217/16 , A61K31/47 , A61K31/472 , A61K31/473 , A61K31/4741 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D217/18 , C07D217/20 , C07D217/24 , C07D221/00 , C07D221/06 , C07D221/12 , C07D491/04 , C07D491/056
CPC分类号： C07D491/04 , C07D217/18 , C07D217/20 , C07D221/12
摘要： The present invention relates to the use of tetrahydroisoquinoline derivatives of the general formula ##STR1## wherein A is arylR.sup.1 is hydrogen, hydroxy, lower alkyl, lower alkoxy, R--CO-- or R--COO--, wherein R is lower alkyl;R.sup.2 is hydrogen, lower alkyl or cycloalkylR.sup.3 -R.sup.7 are independently hydrogen, lower alkyl, lower alkoxy, hydroxy orR.sup.3 and R.sup.4 taken together are --(CH.sub.2).sub.n -- orR.sup.6 and R.sup.7 taken together are --OCH.sub.2 O-- andn is 3 or 4,as well as pharmaceutically acceptable salts for the manufacture of medicaments for the control or treatment of diseases which represent therapeutic indications for NMDA receptor subtype specific blockers.
摘要翻译：本发明涉及以下通式的四氢异喹啉衍生物的用途，其中A为芳基，R 1为氢，羟基，低级烷基，低级烷氧基，R-CO-或R-COO-，其中R为低级烷基; R 2是氢，低级烷基或环烷基R 3 -R 7独立地是氢，低级烷基，低级烷氧基，羟基或者R 3和R 4一起是 - （CH 2）n - 或R 6和R 7一起是-OCH 2 O-，n是3或 4，以及用于制备用于控制或治疗代表NMDA受体亚型特异性阻断剂的治疗适应症的疾病的药物的药学上可接受的盐。

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