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1. 发明授权

EP1283839B1 ADENOSINE A2A RECEPTOR ANTAGONISTS 有权
标题翻译：腺苷A2A受体拮抗剂
公开(公告)号：EP1283839B1
公开(公告)日：2005-04-20
申请号：EP01945991.6
申请日：2001-05-24
申请人： SCHERING CORPORATION
发明人： NEUSTADT, Bernard, R. , LINDO, Neil, A. , GREENLEE, William, J. , TULSHIAN, Deen , SILVERMAN, Lisa, S. , XIA, Yan , BOYLE, Craig, D. , CHACKALAMANNIL, Samuel
IPC分类号： C07D487/14 , A61K31/505 , A61P25/28
CPC分类号： C07D487/14
摘要： Compounds having the structural formula (I) or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or -C(O)CH2-;Y is -N(R2)CH2CH2N(R3)-, -OCH¿2?CH2N(R?2¿)-, -O-, -S-, -CH¿2?S-, -(CH2)2-NH-, or optionally substituted,(Ia), m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R?6¿-C(O)-, R6-SO2-, R6-OC(O)-, R7-N(R8)-C(O)-, R7-N(R8)-C(S)-, phenyl-CH(OH)-, or phenyl-C(=NOR2)-; or when Q is CH, (Ib),phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R?2, R3, R6, R7, and R8¿ are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formula (I).

2. 发明授权

EP0538332B1 POLYCYCLIC GUANINE DERIVATIVES 失效
标题翻译：多环芳烃GUANINDERIVATE
公开(公告)号：EP0538332B1
公开(公告)日：1997-07-23
申请号：EP91912779.5
申请日：1991-06-20
申请人： SCHERING CORPORATION
发明人： NEUSTADT, Bernard, R. , LINDO, Neil, A. , MCKITTRICK, Brian, A.
IPC分类号： C07D487/14
CPC分类号： C07D487/14
摘要： Novel polycyclic guanine derivatives of formula (I) and (I'), wherein J is oxygen or sulfur, R1 is hydrogen, alkyl or alkyl substituted with aryl or hydroxy; R2 is hydrogen, aryl, heteroaryl, cycloalkyl, alkyl or alkyl substituted with aryl, heteroaryl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino, or -(CH¿2?)mTCOR?20¿ wherein m is an integer from 1 to 6, T is oxygen or -NH- and R20 is hydrogen, aryl, heteroaryl, alkyl or alkyl substituted with aryl or heteroaryl; R3 is hydrogen, halo, trifluoromethyl, alkoxy, alkylthio, alkyl, cycloalkyl, aryl, aminosulfonyl, amino, monoalkylamino, dialkylamino, hydroxyalkylamino, aminoalkylamino, carboxy, alkoxycarbonyl or aminocarbonyl or alkyl substituted with aryl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino; R?a, Rb, Rc and Rd¿ independently represent hydrogen, alkyl, cycloalkyl or aryl; or (R?a and Rb) or (Rc and Rd) or (Rb and Rc¿) can complete a saturated ring of 5- to 7- carbon atoms, or (R?a and Rb¿) taken together and (R?b and Rc¿) taken together, each complete a saturated ring of 5- to 7- carbon atoms, wherein each ring optionally can contain a sulfur or oxygen atom and whose carbon atoms may be optionally substituted with one or more of the following: alkenyl, alkynyl, hydroxy, carboxy, alkoxycarbonyl, alkyl or alkyl substituted with hydroxy, carboxy or alkoxycarbonyl; or such saturated ring can have two adjacent carbon atoms which are shared with an adjoining aryl ring; and n is zero or one. The compounds of formulas (I) and (I') are useful as antihypertensive, muscle relaxant and bronchodilating agents.

3. 发明公开

EP0156889A1 PHENYLGUANIDINES 失效
标题翻译：苯基胍。
公开(公告)号：EP0156889A1
公开(公告)日：1985-10-09
申请号：EP84903630.0
申请日：1984-09-21
申请人： SCHERING CORPORATION
发明人： VASHI, Dhiru, B. , CLARK, Jeffrey, N. , LINDO, Neil, A.
IPC分类号： C07C317 , C07C323
CPC分类号： C07C323/44 , C07C317/42
摘要： L'invention concerne des composés de phénylguanidine ainsi que des procédés de préparation de ces composés, des compositions les contenant et des procédés d'utilisation de ces composés en tant qu'anthelmintiques.

4. 发明公开

EP1283839A1 ADENOSINE A2A RECEPTOR ANTAGONISTS 有权
标题翻译：腺苷A2A受体拮抗剂
公开(公告)号：EP1283839A1
公开(公告)日：2003-02-19
申请号：EP01945991.6
申请日：2001-05-24
申请人： SCHERING CORPORATION
发明人： NEUSTADT, Bernard, R. , LINDO, Neil, A. , GREENLEE, William, J. , TULSHIAN, Deen , SILVERMAN, Lisa, S. , XIA, Yan , BOYLE, Craig, D. , CHACKALAMANNIL, Samuel
IPC分类号： C07D487/14 , A61K31/505 , A61P25/28
CPC分类号： C07D487/14
摘要： Compounds having the structural formula (I) or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or -C(O)CH2-;Y is -N(R2)CH2CH2N(R3)-, -OCH¿2?CH2N(R?2¿)-, -O-, -S-, -CH¿2?S-, -(CH2)2-NH-, or optionally substituted,(Ia), m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R?6¿-C(O)-, R6-SO2-, R6-OC(O)-, R7-N(R8)-C(O)-, R7-N(R8)-C(S)-, phenyl-CH(OH)-, or phenyl-C(=NOR2)-; or when Q is CH, (Ib),phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R?2, R3, R6, R7, and R8¿ are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formula (I).

5. 发明公开

EP0538332A1 POLYCYCLIC GUANINE DERIVATIVES 失效
标题翻译：多环芳烃GUANINDERIVATE。
公开(公告)号：EP0538332A1
公开(公告)日：1993-04-28
申请号：EP91912779.0
申请日：1991-06-20
申请人： SCHERING CORPORATION
发明人： NEUSTADT, Bernard, R. , LINDO, Neil, A. , MCKITTRICK, Brian, A.
IPC分类号： A61K31 , A61P9 , A61P11 , A61P25 , A61P43 , C07D473 , C07D487 , C12N9
CPC分类号： C07D487/14
摘要： Nouveaux dérivés polycycliques de guanine ayant les formules (I et I'), dans lesquelles J représente oxygène ou soufre, R1 représente hydrogène, alkyle ou alkyle remplacé par de l'aryle ou hydroxy; R2 représente hydrogène, aryle, hétéroaryle, cycloalkyle, alkyle ou alkyle remplacé par de l'aryle, hétéroaryle, hydroxy, alcoxy, amino, monoalkylamino ou dialkylamino, ou -(CH2)mTCOR20 où m représente un nombre entier compris entre 1 et 6, T représente oxygène ou -NH- et R20 représente hydrogène, aryle, hétéroaryle, alkyle ou alkyle remplacé par de l'aryle ou hétéroaryle; R3 représente hydrogène, halo, trifluorométhyle, alcoxy, alkylthio, alkyle, cycloalkyle, aryle, aminosulfonyle, amino, monoalkylamino, dialkylamino, hydroxyalkylamino, aminoalkylamino, carboxy, alcoxycarbonyle ou aminocarbonyle ou alkyle remplacé par de l'aryle, hydroxy, alcoxy, amino, monoalkylamino, ou dialkylamino; Ra, Rb, Rc et Rd représentent indépendamment hydrogène, alkyle, cycloalkyle ou alkyle; ou (Ra et Rb) ou (Rc et Rd) ou (Rb et R6) peuvent compléter un anneau saturé de 5 à 7 atomes de carbone, ou (Ra et Rb) pris ensemble et (Rb et Rc) pris ensemble complètent chacun un anneau saturé de 5 à 7 atomes de carbone, dans lesquels chaque atome peut facultativement contenir un atome de soufre ou d'oxygène et dont les atomes de carbone peuvent être facultativement remplacés par un ou plusieurs des éléments suivants: alcényle, alkynyle, hydroxy, carboxy, alcoxycarbonyle, alkyle ou alkyle remplacé par hydroxy, carboxy ou alcoxycarbonyle; ou ledit anneau saturé peut comporter deux atomes de carbone adjacent partagés avec un anneau aryle adjacent; et n représente 0 ou 1. Les composés des formules (I) et (I') sont utiles en tant qu'agents antihypertensifs, relaxant musculaire et bronchodilatateurs.

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