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1. 发明公开

EP1765829A1 TRICYCLIC COMPOUNDS AND THEIR USE AS MGLUR1 ANTAGONISTS 有权
标题翻译：三环化合物及其作为mGluR1拮抗剂的用途
公开(公告)号：EP1765829A1
公开(公告)日：2007-03-28
申请号：EP05761566.8
申请日：2005-06-14
申请人： SCHERING CORPORATION
发明人： MATASI, Julius, J. , TULSHIAN, Deen , BURNETT, Duane, A. , WU, Wen-Lian , KORAKAS, Peter , SILVERMAN, Lisa, S. , SASIKUMAR, Thavalakulamgara, K. , QIANG, Li , DOMALSKI, Martin, S.
IPC分类号： C07D495/14 , C07D491/14 , C07D495/04 , C07D471/14 , A61K31/519 , A61P25/00 , C07D333/00 , C07D239/00 , C07D221/00 , C07D307/00
CPC分类号： C07D471/14 , C07D491/14 , C07D495/04 , C07D495/14 , C09B57/00
摘要： In its many embodiments, the present invention provides tricyclic compounds of Formula (I) (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

2. 发明公开

EP1435960A1 IMIDAZO (4,3-E)-1,2,4-TRIAZOLO(1,5-C) PYRIMIDINES AS ADENOSINE A2A RECEPTOR ANTAGONISTS 有权
标题翻译：咪唑并[4,3-E] -1,2,4-三唑并[1,5-C]嘧啶，其腺苷A2A受体拮抗剂
公开(公告)号：EP1435960A1
公开(公告)日：2004-07-14
申请号：EP02778530.2
申请日：2002-10-11
申请人： SCHERING CORPORATION
发明人： TULSHIAN, Deen , SILVERMAN, Lisa, S. , MATASI, Julius, J. , KISELGOF, Eugenia, Y. , CALDWELL, John, P.
IPC分类号： A61K31/505 , A61P25/00 , C07D487/14
CPC分类号： C07D487/14 , A61K31/198 , A61K31/505 , A61K45/06 , Y02P20/582 , A61K2300/00
摘要： Compounds having the structural formula Ior a pharmaceutically acceptable salt thereof, whereinR is optionally substituted phenyl or heteroaryl, cycloalkenyl, -C(=CH2)CH3, -C=C-CH3, -CH=C(CH3)2,X is alkylene, -C(O)CH2- or -C(O)N(R )CH2-;Y is -N(R )CH2CH2N(R )-, -OCH2CH2N(R )-, -O-, -S-, -CH2S-, -(CH2)2-N(R )-, or optionally substituted divalent heteroaryl, piperidinyl or piperazinyl; andZ is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl or R -C(O)-;or when Y isZ is also R -SO2-, R -N(R )-C(O)-, R -N(R )-C(S)- or R OC(O)-;or when Y is 4-piperidinyl, Z can be phenylamino or pyridylamino; orZ and Y together are substituted piperidinyl, substituted pyrrolidinyl or substituted phenyl;R is H, halogen or optionally substituted alkyl; andQ, Q , m, n, R , R , R , R , R and R 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.

3. 发明授权

EP1453835B1 ADENOSINE A 2A RECEPTOR ANTAGONISTS 有权
标题翻译：腺苷A2A受体拮抗剂
公开(公告)号：EP1453835B1
公开(公告)日：2006-02-15
申请号：EP02784641.9
申请日：2002-11-26
申请人： SCHERING CORPORATION
发明人： MATASI, Julius, J. , CALDWELL, John, P. , TULSHIAN, Deen , SILVERMAN, Lisa, S. , NEUSTADT, Bernard, R.
IPC分类号： C07D487/04 , A61K31/505 , A61P25/16 , A61P25/28
CPC分类号： C07D487/04
摘要： This invention relates to compounds having the structural formula (I) or pharmaceutically acceptable salts or solvates thereof, wherein R, R?2 and R3¿ are as defined in the specification, pharmaceutical compositions thereof, and methods of treating stroke or central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment.

4. 发明授权

EP1442036B1 HETEROARYL DERIVATIVES AS SUPERIOR LIGANDS FOR NOCICEPTIN RECEPTOR ORL-1 有权
标题翻译：杂芳基衍生物AS NOCICEPTINREZEPTORS ORL-1更好的配体
公开(公告)号：EP1442036B1
公开(公告)日：2006-01-11
申请号：EP02802860.3
申请日：2002-11-06
申请人： SCHERING CORPORATION
发明人： TULSHIAN, Deen , HO, Ginny, D. , NG, Fay, W.
IPC分类号： C07D451/06 , A61K31/46 , A61P43/00
CPC分类号： C07D451/06
摘要： Novel compounds of the formula (I), wherein R is optionally substituted heteroaryl or (a); R1 is H or C1-C6 alkyl; and R2 and R3 are -CH3, -OCH3 or halo; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions therefore, and the use of said compounds in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.

5. 发明授权

EP1100781B1 HIGH AFFINITY LIGANDS FOR NOCICEPTIN RECEPTOR ORL-1 有权
标题翻译：具有高亲和力的痛敏肽受体ORL-1配体
公开(公告)号：EP1100781B1
公开(公告)日：2004-09-22
申请号：EP99937174.3
申请日：1999-07-26
申请人： SCHERING CORPORATION
发明人： TULSHIAN, Deen , HO, Ginny, D. , SILVERMAN, Lisa, S. , MATASI, Julius, J. , McLEOD, Robbie, L. , HEY, John A. , CHAPMAN, Richard, W. , BERCOVICI, Ana , CUSS, Francis, M.
IPC分类号： C07D211/52 , C07D211/58 , C07D471/10 , C07D401/04 , A61K31/445
CPC分类号： C07D221/20 , A61K31/445 , A61K45/06 , C07D211/14 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/34 , C07D211/52 , C07D211/64 , C07D235/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D417/04 , C07D451/14 , C07D471/10 , C07D491/10 , A61K2300/00
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is -CHO, -CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X?1 and X2¿ together form an optionally benzofused spiro heterocyclyl group; R?1, R2, R3 and R4¿ are independently H and alkyl, or (R?1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4¿) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or -CO¿2?(alkyl or substituted amino) or CN; Z?2¿ is H or Z1; Z3 is H or alkyl; or Z?1, Z2 and Z3¿, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.

6. 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).

7. 发明公开

EP0686157A1 2-BENZYL-POLYCYCLIC GUANINE DERIVATIVES AND PROCESS FOR PREPARING THEM 失效
标题翻译： 2 BENZYLPOLYCYCLISCH鸟嘌呤及其制备方法
公开(公告)号：EP0686157A1
公开(公告)日：1995-12-13
申请号：EP94910124.0
申请日：1994-02-24
申请人： SCHERING CORPORATION
发明人： TULSHIAN, Deen , McKITTRICK, Brian, A. , XIA, Yan , CHACKALAMANNIL, Samuel , GALA, Dinesh , DIBENEDETTO, Donald, J. , KUGELMAN, Max
IPC分类号： C07D239 , C07D473 , C07D487
CPC分类号： C07D487/14 , C07D239/54 , C07D473/40
摘要： Antihypertensive and bronchodilating compounds of formula (I) or a pharmaceutically acceptable salt thereof, and a process for preparing them are disclosed, wherein: R1, R2 and R3 are hydrogen, lower alkyl, lower alkoxy, halogeno, hydroxy, (di-lower alkyl)amino, 4-morpholinyl, 1-pyrrolidinyl, 1-pyrrolyl, -CF3, -OCF3, phenyl or methoxyphenyl; or R1 and R2 together are methylenedioxy; or R1 and R2 together with the carbon atoms to which they are attached form a benzene ring; and Ra is hydrogen and R?b and Rc¿, together with the carbon atoms to which they are attached, form a saturated ring of 5 carbons; or Ra is lower alkyl, Rb is hydrogen or lower alkyl, and Rc is hydrogen; or Ra, Rb and the carbon atom to which they are attached form a saturated ring of 5-7 carbons, and Rc is hydrogen; or Ra is hydrogen, and Rb, Rc and the carbon atoms to which they are attached form a tetrahydrofuran ring; or R?a and Rb¿, together with the carbon atom to which they are attached, and R?b and Rc¿, together with the carbon atoms to which they are attached, each form a saturated ring of 5-7 carbons; pharmaceutical compositions containing said compounds: methods of treatment using said compounds; and a process for preparing polycyclic guanines comprising a) reducing a nitrosopyrimidine, and treating the reduced nitrosopyrimidine with an acylating reagent to give the amidopyrimidine; b) reacting the amidopyrimidine with a halogenating/cyclizing reagent to give a halopurine; c) reacting, in the presence of a base, the halopurine with an amine to give the substituted aminopurine; and d) closing the ring of the substituted aminopurine with a suitable dehydrating agent.

8. 发明公开

EP0658169A1 DIAMINO ACID DERIVATIVES AS ANTIHYPERTENSIVES 失效
标题翻译：抗生素DIAMINOSAÜREDERIVATE。
公开(公告)号：EP0658169A1
公开(公告)日：1995-06-21
申请号：EP93918488.0
申请日：1993-08-03
申请人： SCHERING CORPORATION
发明人： NEUSTADT, Bernard, R. , SMITH, Elizabeth, M. , TULSHIAN, Deen
IPC分类号： A61K38 , A61P9 , A61P13 , A61P15 , A61P43 , C07D209 , C07K1 , C07K5 , C07K14
CPC分类号： C07K5/022 , A61K38/00 , C07D209/20
摘要： Novel diamino acid derivative dual inhibitors of neutral endopeptidase and angiotensin converting enzyme of formula (I), wherein: Z is amino, lower alkylamino, di-(lower alkyl)amino R9C(O)NH- or an optionally substituted guanidino group; R1 is hydrogen or R?7R8N-; R2¿ is hydrogen, lower alkyl, cyclolower alkyl, aryllower alkyl or heteroaryl lower alkyl; and R3 is hydrogen, lower alkyl or cyclo lower alkyl; or R?2 and R3¿, together with the carbon to which they are attached, comprise a 3-7 membered carbocyclic ring; R4 is hydrogen, lower alkyl, aryl lower alkyl or heteroaryl lower alkyl; R?5 and R6¿ are independently hydroxy, lower alkoxy, amino, aryl lower alkoxy, lower alkylamino and di-(lower alkyl)amino; R7 is R9C(O)- or R10SO2-; and R8 is hydrogen, lower alkyl, aryl lower alkyl or aryl; or R?7 and R8¿, together with the nitrogen to which they are attached, comprise a 5-7 membered ring; R9 is lower alkyl, aryllower alkyl, aryl, heteroaryl lower alkyl, heteroaryl, lower alkoxy, aryl lower alkoxy, amino, alkylamino or dialkylamino; R10 is lower alkyl, aryl lower alkyl, aryl, heteroaryl lower alkyl, amino, lower alkylamino, di-(lower alkyl)amino or heteroaryl; n is 1, 2, 3, 4 or 5; and m is 1, 2, 3, 4 or 5; or a pharmaceutically acceptable addition salt thereof, useful in the treatment of cardiovascular disorders, are disclosed.

9. 发明授权

EP1966220B1 MGLUR1 ANATGONISTS AS THERAPEUTIC AGENTS 有权
标题翻译： MGluR1拮抗剂治疗物质
公开(公告)号：EP1966220B1
公开(公告)日：2011-01-26
申请号：EP06848624.0
申请日：2006-12-11
申请人： Schering Corporation
发明人： MATASI, Julius, J. , TULSHIAN, Deen , BURNETT, Duane, A. , WU, Wen-Lian , KORAKAS, Peter , SILVERMAN, Lisa, S. , THAVALAKULAMGARA, Sasikumar, K. , QIANG, Li , DOMALSKI, Martin, S.
IPC分类号： C07D495/14
CPC分类号： C07D495/14
摘要： In its many embodiments, the present invention provides tricyclic compounds of formula (I) (wherein J1 - J4, X, and R1- R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

10. 发明公开

EP2170896A2 POLYCYCLIC GUANINE DERIVATIVES AND USE THEREOF 审中-公开
标题翻译：多环鸟嘌呤衍生物及其应用
公开(公告)号：EP2170896A2
公开(公告)日：2010-04-07
申请号：EP08768585.5
申请日：2008-06-18
申请人： Schering Corporation
发明人： TULSHIAN, Deen , GEISS, William, B. , MARTIN, Gregory, S. , LE, Van-duc , HABER, James, C., Jr. , MATASI, Julius, J. , CZARNIECKI, Michael, F. , COOKE, Stephanie, Nicole
IPC分类号： C07D487/14 , A61K31/519 , A61P25/00
CPC分类号： C07D487/14
摘要： The present invention relates to Polycyclic Guanine Derivatives, compositions comprising the Polycyclic Guanine Derivatives and methods of using the Polycyclic Guanine Derivatives to treat pain or an inflammatory disease.

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