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1. 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。

2. 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。

3. 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。

4. 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。

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