公开(公告)号：EP1765829B1

公开(公告)日：2010-07-07

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

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.

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.

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.

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.

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.

公开(公告)号：EP1200087A1

公开(公告)日：2002-05-02

申请号：EP00904560.0

申请日：2000-01-26

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： A61K31/445 ,  A61K31/46 ,  A61K45/06 ,  A61P11/14

CPC分类号： A61K45/06 ,  A61K31/00 ,  A61K31/438 ,  A61K31/439 ,  A61K31/451 ,  A61K31/4535 ,  A61K31/454

摘要： The present invention relates to the use of ORL-1 receptor agonists for the treatment of cough, alone or in combination with one or more agents for the treatment of cough, allergy or asthma symptoms, in particular to the use of ORL-1 agonists of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents and 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.

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.

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.

公开(公告)号：EP1966220A2

公开(公告)日：2008-09-10

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.

公开(公告)号：EP1453835A2

公开(公告)日：2004-09-08

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.