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1. 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。

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

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。

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

US6054588A Heterocyclic vinyl ethers 失效
标题翻译：杂环乙烯基醚
公开(公告)号：US6054588A
公开(公告)日：2000-04-25
申请号：US304624
申请日：1999-05-04
申请人： Geo Adam , Sabine Kolczewski , Vincent Mutel , Heinz Stadler , Jurgen Wichmann , Thomas Johannes Woltering
发明人： Geo Adam , Sabine Kolczewski , Vincent Mutel , Heinz Stadler , Jurgen Wichmann , Thomas Johannes Woltering
IPC分类号： A61K31/41 , A61K31/4164 , A61K31/4174 , A61K31/4196 , A61P1/08 , A61P13/02 , A61P21/02 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/34 , A61P25/36 , A61P27/02 , A61P29/00 , C07D233/60 , C07D249/08 , C07D257/04 , C07D521/00
CPC分类号： C07D257/04 , A61K31/41 , A61K31/4174 , A61K31/4196 , C07D231/12 , C07D233/56 , C07D249/08
摘要： The compounds of the formula ##STR1## wherein R signifies halogen or lower alkyl;n signifies 0-3;R.sup.1 signifies lower alkyl; cycloalkyl; benzyl optionally substituted by hydroxy, halogen, lower alkoxy or lower alkyl; benzoyl optionally substituted by amino, lower alkyl-amino or di-lower alkylamino; acetyl or cycloalkyl-carbonyl; and ##STR2## signifies an aromatic 5-membered residue which is bonded via a N-atom and which contains further 1-3 N atoms in addition to the linking N atom,as well as their pharmaceutically acceptable salts as therapeutically active substances, especially for the control or prevention of acute and/or chronic neurological disorders.
摘要翻译：下式的化合物其中R表示卤素或低级烷基; n表示0-3; R1表示低级烷基; 环烷基任选被羟基，卤素，低级烷氧基或低级烷基取代的苄基; 任选被氨基，低级烷基 - 氨基或二 - 低级烷基氨基取代的苯甲酰基; 乙酰基或环烷基 - 羰基; 并且表示通过N-原子键合并且除了连接的N原子之外还含有1-3个N原子的芳族5元残基以及它们的药学上可接受的盐作为治疗活性物质，特别是用于对照或预防急性和/或慢性神经障碍。

7. 发明授权

US6020525A (2S,2'R,3'R)-2-(2,3-dicarboxyl-cyclopropyl)-glycine (DCG-1/4) and .sup.3 H-DCG-1/4 and to process for the preparation thereof 失效
标题翻译：（2S，2'R，3'R）-2-（2,3-二羧基 - 环丙基） - 甘氨酸（DCG-1/4）和3H-DCG-1/4并进行制备
公开(公告)号：US6020525A
公开(公告)日：2000-02-01
申请号：US256047
申请日：1999-02-23
申请人： Geo Adam , Philippe Nicolas Huguenin-Virchaux , Jurgen Wichmann
发明人： Geo Adam , Philippe Nicolas Huguenin-Virchaux , Jurgen Wichmann
IPC分类号： C07C51/09 , C07C51/363 , C07C61/06 , C07C67/02 , C07C67/31 , C07C67/317 , C07C69/757 , C07C227/16 , C07C229/46 , C07C253/08 , C07C255/31 , C07D307/93 , C07C61/04
CPC分类号： C07C253/00 , C07C229/46 , C07C51/09 , C07C51/363 , C07C67/31 , C07C67/317 , C07D307/93 , C07B2200/05 , C07B2200/07 , C07C2101/02
摘要： This invention relates to (2S,2'R,3'R)-2-(2,3-dicarboxyl-cyclopropyl)-glycine of formula ##STR1## wherein R.sub.2 is hydrogen or tritium and to a process for the preparation thereof. The described compounds can be used as a pharmacological tool to study the function of group II mGluR (metabotropic glutamate receptor).
摘要翻译：本发明涉及式（2S，2'R，3'R）-2-（2,3-二羧基 - 环丙基） - 甘氨酸，其中R2是氢或氚，以及其制备方法。所述化合物可用作研究II组mGluR（代谢型谷氨酸受体）的功能的药理学工具。

8. 发明授权

US5958931A Phenyl-substituted 5H-thiazolo�3,2-A!pyrimidine derivative glutamate receptor antagonists 失效
标题翻译：苯基取代的5H-噻唑并[3,2-A]嘧啶衍生物谷氨酸受体拮抗剂
公开(公告)号：US5958931A
公开(公告)日：1999-09-28
申请号：US115191
申请日：1998-07-14
申请人： Geo Adam , Sabine Kolczewski , Vincent Mutel , Jurgen Wichmann , Thomas Johannes Woltering
发明人： Geo Adam , Sabine Kolczewski , Vincent Mutel , Jurgen Wichmann , Thomas Johannes Woltering
IPC分类号： C07D239/22 , A61K31/00 , A61K31/505 , A61K31/519 , A61P1/08 , A61P9/00 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P27/02 , A61P43/00 , C07D239/00 , C07D239/40 , C07D277/00 , C07D513/04
CPC分类号： C07D513/04 , C07D239/40
摘要： The invention is concerned with compounds of the general formula ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, phenyl or benzyl,R.sup.2 is lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n N(R.sup.13)(R.sup.14), --(CH.sub.2).sub.n N(R.sup.13)(R.sup.14) or --N(R.sup.15)(CH.sub.2).sub.n N(R.sup.13)(R.sup.14),R.sup.3 -R.sup.12 are hydrogen, halogen, trifluoromethyl, lower alkyl, cycloalkyl, lower alkoxy, hydroxy, nitro, cyano, --N(R.sup.13).sub.2, phenyl, phenyloxy, benzyl or benzyloxy, orR.sup.6 and R.sup.7 together are a benzene ring,R.sup.13 -R.sup.15 are hydrogen, lower alkyl or cycloalkyl andn is 1-5,as well as their pharmaceutically acceptable salts.
摘要翻译：本发明涉及下列通式的化合物：其中R1是氢，低级烷基，苯基或苄基，R2是低级烷基，低级烷氧基，-O（CH2）nN（R13）（R14）， - （CH2）nN（R13））（R14）或-N（R15）（CH2）nN（R13）（R14），R3-R12是氢，卤素，三氟甲基，低级烷基，环烷基，低级烷氧基，羟基，硝基，氰基，-N（R13） 2，苯基，苯氧基，苄基或苄氧基，或R6和R7一起是苯环，R13-R15是氢，低级烷基或环烷基，n是1-5，以及它们的药学上可接受的盐。

9. 发明授权

US5955495A Method of treating diseases of the CNS 失效
标题翻译：治疗CNS疾病的方法
公开(公告)号：US5955495A
公开(公告)日：1999-09-21
申请号：US837140
申请日：1997-04-14
申请人： Michael Bos , Heinz Stadler , Jurgen Wichmann
发明人： Michael Bos , Heinz Stadler , Jurgen Wichmann
IPC分类号： A61K31/34 , A61K31/343 , A61P25/00 , A61P25/20 , A61P25/28 , C07D307/85 , C07D307/86
CPC分类号： C07D307/85 , A61K31/343 , C07D307/86
摘要： The invention is concerned with the use of compounds of the general formula ##STR1## wherein R.sup.1 -R.sup.4 signify hydrogen, halogen, lower-alkyl, lower-alkoxy, aryl, benzyloxy, lower-alkoxy-lower-alkyl, lower-alkyl-sulphanyl, lower-alkyl-sulphanyl-lower-alkyl or R.sup.1 and R.sup.2 together signify the group --O--(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.2 --O-- andR.sup.5 signifies hydrogen or hydroxy,as well as their pharmaceutically acceptable salts in the control or prevention of illnesses or disorders of the central nervous system such as migraine, schizophrenia, anxiety states, sleep disorders, anorexia, Alzheimer's disease, addictions (alcohol, nicotine, benzodiazepine, cocaine, etc.), as well as disorders which result from damage to the head/brain or to the spinal column/bone marrow and, respectively, for the production of corresponding medicaments.
摘要翻译：本发明涉及以下通式的化合物的用途：其中R 1 -R 4表示氢，卤素，低级烷基，低级烷氧基，芳基，苄氧基，低级烷氧基 - 低级烷基，低级烷基 - 硫基，烷基 - 硫基 - 低级 - 烷基或R 1和R 2一起表示基团-O-（CH 2）2 - 或 - （CH 2）2 -O-，并且R 5表示氢或羟基，以及它们在对照中的药学上可接受的盐，预防偏头痛，精神分裂症，焦虑症，睡眠障碍，厌食症，阿尔茨海默病，成瘾症（酒精，尼古丁，苯二氮卓，可卡因等）的中枢神经系统疾病或病症，以及由于损伤引起的疾病头/脑或脊柱/骨髓，分别用于生产相应的药物。

10. 发明授权

US5646173A Tricyclic pyrrole derivatives useful as 5-HT selective agents 失效
标题翻译：三环吡咯衍生物可用作5-HT选择剂
公开(公告)号：US5646173A
公开(公告)日：1997-07-08
申请号：US594533
申请日：1996-02-21
申请人： Michael Bos , Jurgen Wichmann , Ulrich Widmer
发明人： Michael Bos , Jurgen Wichmann , Ulrich Widmer
IPC分类号： C07D491/052 , A61K31/40 , A61K31/403 , A61P1/00 , A61P7/02 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , C07D209/56 , C07D209/58 , C07D209/60 , C07D209/70 , C07D209/96 , C07D491/04 , C07D495/04 , C07D513/04
CPC分类号： C07D209/96 , C07D209/60 , C07D209/70 , C07D491/04
摘要： The invention relates to tricyclic pyrrole derivatives useful as 5-HT selective agents of the formula ##STR1## wherein R.sup.1 to R.sup.4 are, independently, hydrogen, halogen, lower alkyl, phenyl, cycloalkyl or lower alkoxy and R.sup.2 additionally is lower alkoxycarbonyl, acyloxy or mesyloxy;R.sup.5 to R.sup.7 are, independently, hydrogen or lower alkyl;X is --CH.sub.2 CH(C.sub.6 H.sub.5)--, --CH.dbd.C(C.sub.6 H.sub.5)--, --YCH.sub.2 --, --CH.dbd.CH-- or --(CR.sup.11 R.sup.12).sub.n ;R.sup.11 and R.sup.12 are, independently, hydrogen, phenyl, lower alkyl or halogen;n is 1 to 3 andy is O or S,as well as pharmaceutically acceptable salts of basic compounds of formula I with pharmaceutically acceptable acids.
摘要翻译：本发明涉及三环吡咯衍生物，其可用作式I的5-HT选择剂，其中R 1至R 4独立地为氢，卤素，低级烷基，苯基，环烷基或低级烷氧基，并且R 2另外为低级烷氧基羰基，酰氧基或甲磺酰氧基; R5至R7独立地为氢或低级烷基; X是-CH 2 CH（C 6 H 5） - ， - CH = C（C 6 H 5） - ， - YCH 2 - ， - CH = CH-或 - （CR 11 R 12） R 11和R 12独立地是氢，苯基，低级烷基或卤素; n为1至3，y为O或S，以及式I的碱式化合物与药学上可接受的酸的药学上可接受的盐。

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