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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

US06642247B2 Di-or triaza-spiro [4,5] decane derivatives 失效
标题翻译：二 - 或三氮杂螺[4,5]癸烷衍生物
公开(公告)号：US06642247B2
公开(公告)日：2003-11-04
申请号：US09330724
申请日：1999-06-11
申请人： Geo Adam , Andrea Cesura , François Jenck , Sabine Kolczewski , Stephan Röver , Jürgen Wichmann
发明人： Geo Adam , Andrea Cesura , François Jenck , Sabine Kolczewski , Stephan Röver , Jürgen Wichmann
IPC分类号： A61K31438
CPC分类号： C07D471/10 , C07D513/10
摘要： The present invention relates to compounds of the general formula wherein R1 is C6-10-cycloalkyl, optionally substituted by lower alkyl or —C(O)O-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; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl or octahydro-inden-2-yl; R2 is hydrogen; lower alkyl; ═O or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; X is —CH(OH)—; —C(O)—; —CHR3—; —CR3═; —O—; —S—; —CH(COOR4)— or C(COOR4)═; Y is —CH2—; —CH═; —CH(COOR4)—, —C(COOR4)═; or —C(CN)—; R3 is hydrogen or lower alkoxy; R4 is lower alkyl, cycloalkyl, phenyl, or benzyl and either a or b is optionally an additional bond, and to pharmaceutically acceptable acid addition salts thereof. The compounds are agonists of the orphanin FQ (QFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.
摘要翻译：本发明涉及通式化合物R 1的化合物是任选被低级烷基或-C（O）O-低级烷基取代的C 6-10 - 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; 2,3-二氢-1H-苯并芬-1-基; 2,3,3a，4,5,6-六氢-1H-吩酚-1-基或八氢 - 茚-2-基; R 2是氢; 低级烷基任选被低级烷基，卤素或烷氧基取代的O或苯基;是任选被低级烷基，卤素或烷氧基取代的环己基或苯基; X是-CH（OH） - ; -C（O） - ; -CHR 3 - ; -CR 3 = -O-; -S-; -CH（COOR 4） - 或C（COOR 4）=; Y是-CH 2 - ; -CH =; -CH（COOR 4） - ， - C（COOR 4）=; 或-C（CN） - ; R 3是氢或低级烷氧基; R 4是低级烷基，环烷基，苯基或苄基，a或b任选是另外的键，以及其药学上可接受的酸加成盐该化合物是孤儿素FQ（QFQ）受体的激动剂，因此可用于治疗与该受体有关的疾病。

6. 发明授权

US06172075B2 Di-or triaza-spiro [4,5] decane derivatives 有权
公开(公告)号：US06172075B2
公开(公告)日：2001-01-09
申请号：US09330724
申请日：1999-06-11
申请人： Geo Adam , Andrea Cesura , François Jenck , Sabine Kolczewski , Stephan Röver , J{umlaut over (u)}rgen Wichmann
发明人： Geo Adam , Andrea Cesura , François Jenck , Sabine Kolczewski , Stephan Röver , J{umlaut over (u)}rgen Wichmann
IPC分类号： A61K31438
摘要： The present invention relates to compounds of the general formula wherein R1 is C6-10-cycloalkyl, optionally substituted by lower alkyl or —C(O)O-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; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl or octahydro-inden-2-yl; R2 is hydrogen; lower alkyl; ═O or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; {circumflex over (A)} is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; X is —CH(OH)—; —C(O)—; —CHR3—; —CR3═; —O—; —S—; —CH(COOR4)— or —C(COOR4)—; Y is —CH2—; —CH═; —CH(COOR4)—, —C(COOR4)═; or —C(CN)—; R3 is hydrogen or lower alkoxy; R4 is lower alkyl, cycloalkyl, phenyl, or benzyl and either a or b is optionally an additional bond, and to pharmaceutically acceptable acid addition salts thereof. The compounds are agonists of the orphanin FQ (QFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.

7. 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。

8. 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。

9. 发明授权

US06660736B2 Phthalimido derivatives and a process for their preparation 失效
标题翻译：邻苯二甲酰亚胺衍生物及其制备方法
公开(公告)号：US06660736B2
公开(公告)日：2003-12-09
申请号：US10387950
申请日：2003-03-13
申请人： Andrea Cesura , Rosa Maria Rodriguez Sarmiento , Andrew William Thomas , Rene Wyler
发明人： Andrea Cesura , Rosa Maria Rodriguez Sarmiento , Andrew William Thomas , Rene Wyler
IPC分类号： A61K31535
CPC分类号： C07D209/48 , C07D401/04 , C07D413/04 , C07D471/04
摘要： This invention relates to phthalimido derivatives of the formula wherein X is —N═ or —CH═, and R1 to R4 and m are as defined in the specification, as well as their pharmaceutically acceptable salts. The invention further relates to pharmaceutical compositions containing these compounds, a method of treating a disease by administering a therapeutically effective amount of at least one of these compounds, and a process for their preparation for the treatment or prevention of diseases in which MAO-B inhibitors might be beneficial.
摘要翻译：本发明涉及式Ⅳ的邻苯二甲酰亚氨基衍生物是-N =或-CH =，R 1至R 4和m如说明书中所定义，以及它们的药学上可接受的盐。本发明还涉及含有这些化合物的药物组合物，通过施用治疗有效量的这些化合物中的至少一种来治疗疾病的方法及其制备治疗或预防MAO-B抑制剂可能是有益的

10. 发明授权

US07642283B2 Mitochrondrial permeability transition pore affinity labels and modulators 失效
标题翻译：线粒体通透性转移孔亲和标记和调节剂
公开(公告)号：US07642283B2
公开(公告)日：2010-01-05
申请号：US11487119
申请日：2006-07-14
申请人： Andrea Cesura , Emmanuel Pinard
发明人： Andrea Cesura , Emmanuel Pinard
IPC分类号： A61K31/352 , C07D311/22 , C12Q1/00
CPC分类号： C07C255/47 , A61K31/12 , A61K31/35 , C07C49/665 , C07C49/683 , C07C2601/10 , C07C2603/32 , C07C2603/98 , C07D311/22
摘要： Methods of utilizing compounds of general formulas I and II as modulators and affinity labels of the MPTP complex are elucidated. Furthermore, methods for modulating the activity of the MPTP complex, methods for determining the presence of a component of the MPTP complex, and methods for identifying an active agent that modulates the activity of the MPTP complex, specifically methods for identifying an active agent that modulates the activity of the MPTP complex by interacting with the VDAC1 component are identified. Moreover, novel compounds of general formulas I and II are disclosed.
摘要翻译：阐述了将通式I和II的化合物用作MPTP复合物的调节剂和亲和标记物的方法。此外，用于调节MPTP复合物的活性的方法，用于确定MPTP复合物的组分的存在的方法，以及用于鉴定调节MPTP复合物的活性的活性剂的方法，特别是用于鉴定调节的活性剂的方法识别通过与VDAC1组分相互作用的MPTP复合物的活性。此外，公开了通式I和II的新化合物。

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