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61. 发明专利

NO20010467D0 未知
公开(公告)号：NO20010467D0
公开(公告)日：2001-01-26
申请号：NO20010467
申请日：2001-01-26
申请人： SCHERING CORP
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： C07D491/107 , A61K31/00 , A61K31/438 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/46 , A61K31/496 , A61K31/5375 , A61K31/541 , A61K45/06 , A61P11/06 , A61P25/04 , A61P25/22 , A61P25/24 , A61P25/26 , A61P29/00 , C07D211/14 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/34 , C07D211/52 , C07D211/58 , C07D211/64 , C07D221/00 , C07D221/20 , C07D235/00 , C07D235/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D411/04 , C07D417/04 , C07D451/06 , C07D451/14 , C07D471/04 , C07D471/10 , C07D491/10 , C07D
摘要： A nociceptin receptor ORL-1 agonist is used in the manufacture of a pharmaceutical composition for the treatment of cough symptoms.

62. 发明专利

ZA200803718B 3-monosubstituted tropane derivatives as nociceptin receptor ligands 未知
公开(公告)号：ZA200803718B
公开(公告)日：2009-03-25
申请号：ZA200803718
申请日：2008-04-29
申请人： SCHERING CORP
发明人： HO GINNY D , SHU-WEI YANG , DEEN TULSHIAN
IPC分类号： A61K20090101 , A61P20090101 , C07D20090101
摘要： Compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R1 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R2 is H; or aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R3 is aryl, heteroaryl, cycloalkyl or heterocycloalkyl, all optionally substituted; X is a bond, —(CH2)m—N(R7)—(CH2)n—, —(CH2)m—O—(CH2)n—, —(CH2)m—S—(CH2)n—, —C(O)—, —CH(OH)—, —C(O)N(R7)—, —C(O)N(R7)-alkylene or —N(R7)C(O)—; R7 is H or alkyl; and m and n are each 0-6, provided that the sum of m and n is 0-6; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions thereof, and the use of said compounds in the treatment of cough, pain, anxiety, asthma, depression, alcohol abuse, urinary incontinence and overactive bladder are disclosed.

63. 发明专利

CA2465871C HETEROARYL DERIVATIVES AS SUPERIOR LIGANDS FOR NOCICEPTIN RECEPTOR ORL-1 未知
公开(公告)号：CA2465871C
公开(公告)日：2009-01-20
申请号：CA2465871
申请日：2002-11-06
申请人： SCHERING CORP
发明人： NG FAY W , HO GINNY D , TULSHIAN DEEN
IPC分类号： C07D451/06 , A61K31/46 , A61K31/506 , A61K45/00 , A61P11/06 , A61P11/14 , A61P25/04 , A61P25/22 , A61P25/24 , A61P25/32 , A61P29/00 , A61P37/08 , A61P43/00
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, pharmaceutic al compositions therefore, and the use of said compounds in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.

64. 发明专利

NO20082443L 未知
公开(公告)号：NO20082443L
公开(公告)日：2008-07-30
申请号：NO20082443
申请日：2008-05-30
申请人： SCHERING CORP
发明人： TULSHIAN DEEN , HO GINNY D , YANG SHU-WEI
IPC分类号： C07D451/04 , C07D451/02
摘要： Compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R1 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R2 is H; or aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R3 is aryl, heteroaryl, cycloalkyl or heterocycloalkyl, all optionally substituted; X is a bond, —(CH2)m—N(R7)—(CH2)n—, —(CH2)m—O—(CH2)n—, —(CH2)m—S—(CH2)n—, —C(O)—, —CH(OH)—, —C(O)N(R7)—, —C(O)N(R7)-alkylene or —N(R7)C(O)—; R7 is H or alkyl; and m and n are each 0-6, provided that the sum of m and n is 0-6; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions thereof, and the use of said compounds in the treatment of cough, pain, anxiety, asthma, depression, alcohol abuse, urinary incontinence and overactive bladder are disclosed.

65. 发明专利

PE11592007A1 DERIVADOS DE TROPANO 3-MONOSUSTITUIDO COMO LIGANDOS DE RECEPTORES DE NOCICEPTINA 未知
公开(公告)号：PE11592007A1
公开(公告)日：2007-11-30
申请号：PE0013052006
申请日：2006-10-26
申请人： SCHERING CORP
发明人： TULSHIAN DEEN , HO GINNY D , YANG SHU-WEI
IPC分类号： A61K31/46 , A61P11/14 , C07D451/02 , C07D451/04 , C07D451/06
CPC分类号： C07D451/02 , C07D451/04 , C07D451/06
摘要： SE REFIERE A DERIVADOS DE TROPANO 3-MONOSUSTITUIDOS DE FORMULA (I), EN DONDE R1 ES R4-ARILO; R4-ARILALQUILO, R4-HETEROARILO, ENTRE OTROS; R2 ES R5-ARILO, R5-ARILALQUILO, R5-HETEROARILO, ENTRE OTROS; R3 ES R6-ALQUILO, R6-ARILO; R4-ARILALQUILO, R4-HETEROARILO, ENTRE OTROS; X ES UN ENLACE ALQUILENO(C1-C3), -(CH2)m-N(R7)-(CH2)n-, -C(O)N(R7)-, ENTRE OTROS; n Y m SON DE 0 A 6; CADA R4 Y R5 SON INDEPENDIENTEMENTE H, HALO, ALQUILO, ENTRE OTROS. SON SELECCIONADOS: 8-[BIS(2-CLOROFENIL)METIL]-3-FENIL-8-AZABICICLO-[3,2,1]OCTANO, 8-[BIS(2-CLOROFENIL)METIL]-3-PIRIDINIL-8-AZABICICLO-[3,2,1]OCTANO, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICIONA FARMACEUTICA QUE ADEMAS PUEDE COMPRENDER AGENTES ADICIONALES. ESTOS COMPUESTOS SON AGONISTAS DEL RECEPTOR TIPO OPIOIDE NOP, POR LO QUE SON UTILES EN EL TRATAMIENTO DE DOLOR, ANSIEDAD, TOS, ASMA, ABUSO DE ALCOHOL, DEPRESION, INCONTINENCIA URINARIA O VEJIGA HIPERACTIVA

67. 发明专利

ES2259106T3 AZETIDINIL DIAMINAS UTILES COMO LIGANDOS DEL RECEPTOR DE NOCICEPTINA ORL-1. 未知
公开(公告)号：ES2259106T3
公开(公告)日：2006-09-16
申请号：ES02778840
申请日：2002-11-14
申请人： SCHERING CORP
发明人： BURNETT DUANE A , CAPLEN MARY ANN , CZARNIECKI MICHAEL F , DOMALSKI MARTIN S , HO GINNY D , TULSHIAN DEEN
IPC分类号： A61K31/397 , A61K31/4025 , A61K31/4178 , A61K31/4427 , A61K31/4523 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K45/06 , A61P11/06 , A61P11/14 , A61P25/04 , A61P25/22 , A61P25/24 , A61P25/32 , C07D205/04 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D417/06 , C07D521/00
摘要： la invención se refiere al uso de un compuesto de acuerdo con la invención en combinación con uno o más agentes adicionales para tratar tos, alergia o síntomas de asma, seleccionados del grupo que consiste en: antihistaminas, inhibidores de 5-lipooxigenasa, inhibidores de leucotrienos, inhibidores de los receptores H3 de histamina, agonistas de los receptores beta-adrenérgicos, derivados de xantina, agonistas de los receptores alfa-adrenérgicos, estabilizantes de mastocitos, antitusivos, expectorantes, antagonistas de los receptores de taquiquinina NK1, NK2 y NK3 y agonistas de GABAB para la fabricación de un medicamento para tratar la tos, el dolor, la ansiedad, el asma, el abuso de alcohol o la depresión.

68. 发明专利

NZ532088A Heteroaryl derivatives as superior ligands for nociceptin receptor ORL-1 to be used in compositions to treat pain, cough and asthma 未知
公开(公告)号：NZ532088A
公开(公告)日：2006-05-26
申请号：NZ53208802
申请日：2002-11-06
申请人： SCHERING CORP
发明人： TULSHIAN DEEN , HO GINNY D , NG FAY W
IPC分类号： A61K31/506 , A61K45/00 , A61P11/06 , A61P11/14 , A61P25/04 , A61P25/22 , A61P25/24 , A61P25/32 , A61P29/00 , A61P37/08 , A61P43/00 , C07D451/06 , A61K31/46
摘要： Disclosed is a compound of formula I wherein: R is R4- heteroaryl or pyrimidinyl; R1 is H or C1-C6 alkyl; R2and R3 are independently selected from the group consisting of -CH3, -OCH3, fluro, chloro, bromo and iodo; R4-R7 are as defined. These compounds are useful for the treatment of cough, pain, anxiety, asthma, depression and alcohol abuse.

69. 发明专利

CA2338206C HIGH AFFINITY LIGANDS FOR NOCICEPTIN RECEPTOR ORL-1 未知
公开(公告)号：CA2338206C
公开(公告)日：2005-12-20
申请号：CA2338206
申请日：1999-07-26
申请人： SCHERING CORP
发明人： BERCOVICI ANA , MCLEOD ROBBIE L , CUSS FRANCIS M , SILVERMAN LISA S , MATASI JULIUS J , HO GINNY D , CHAPMAN RICHARD W , TULSHIAN DEEN , HEY JOHN A
IPC分类号： C07D491/107 , A61K31/00 , A61K31/438 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/46 , A61K31/496 , A61K31/5375 , A61K31/541 , A61K45/06 , A61P11/06 , A61P25/04 , A61P25/22 , A61P25/24 , A61P25/26 , A61P29/00 , C07D211/14 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/34 , C07D211/52 , C07D211/58 , C07D211/64 , C07D221/00 , C07D221/20 , C07D235/00 , C07D235/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D411/04 , C07D417/04 , C07D451/06 , C07D451/14 , C07D471/04 , C07D471/10 , C07D491/10 , C07D471/08
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, heteroary l or heterocycloalkyl; X2 is -CHO, -CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocycl yl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group; R1, R2, R3 and R4 are independently H a nd alkyl, or (R1 and R4) or (R2 and R3) or (R2 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-CO2(alkyl or substituted amino) or CN; Z2 is H or Z1; Z 3 is H or alkyl; or Z1, 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.

70. 发明专利

ES2229750T3 LIGANDOS DE ALTA AFINIDAD PARA EL RECEPTOR DE NOCICEPTINA ORL-1. 未知
公开(公告)号：ES2229750T3
公开(公告)日：2005-04-16
申请号：ES99937174
申请日：1999-07-26
申请人： SCHERING CORP
发明人： TULSHIAN DEEN , HO GINNY D , SILVERMAN LISA S , MATASI JULIUS J , MCLEOD ROBBIE L , HEY JOHN A
IPC分类号： C07D491/107 , A61K31/00 , A61K31/438 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/46 , A61K31/496 , A61K31/5375 , A61K31/541 , A61K45/06 , A61P11/06 , A61P25/04 , A61P25/22 , A61P25/24 , A61P25/26 , A61P29/00 , C07D211/14 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/34 , C07D211/52 , C07D211/58 , C07D211/64 , C07D221/00 , C07D221/20 , C07D235/00 , C07D235/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D411/04 , C07D417/04 , C07D451/06 , C07D451/14 , C07D471/04 , C07D471/10 , C07D491/10
摘要： Un compuesto representado por la **fórmula** o una de sus sales o uno de sus solvatos farmacéuticamente aceptables, donde: la línea de puntos representa un doble enlace opcional, X1 es R5-alquilo(C1-C12), R6-cicloalquilo(C3-C12), R7- arilo, R8-heteroarilo o R10-heterocicloalquilo(C3-C7); X2 es -CHO, -CN, -NHC(=NR26)NHR26, -CH(=NOR26), - NHOR26, R7-arilo, R7-aril-alquilo(C1-C6), R7-aril- alquenilo(C1-C6), R7-aril-alquinilo(C1-C6), -(CH2)vOR13, -(CH2)vCOOR27, -(CH2)vCONR14R15, - (CH2)vNR21NR22 o (CH2)vNHC(O)R21, en donde v es cero, 1, 2 ó 3; X1 y X2 conjuntamente forman un grupo espiro que tiene la **fórmula** m es 1 ó 2; n es 1, 2, ó 3, con la condición de que cuando n es 1, uno de R16 y R17 es -C(O)R28; p es 0 ó 1, Q es -CH2-, -O-, -S-, -SO-, -SO2- o -NR17-, R1, R2, R3 y R4 se seleccionan independientemente del grupo que consiste en hidrógeno y alquilo(C1-C6), ó (R1 y R4) ó (R2 y R3) ó (R1 y R3) ó (R2 y R4) conjuntamente pueden formar un puente de alquileno de 1 a 3 átomos de carbono; R5 es1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en H, R7-arilo, R6- cicloalquilo(C3-C12), R8-heteroarilo, R10- heterocicloalquilo(C3-C7), -NR19R20, -OR13 y -S(O)0-2R13; R6 es de 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en H, alquilo(C1-C6), R7-arilo, -NR19R20, -OR13 y -SR13; R7 es 1 a 3 sustituyentes seleccionados del grupo que consiste en hidrógeno, halo, alquilo(C1-C6), R25-arilo, cicloalquilo(C3-C12), -CN, -CF3, -OR19, -alquilo (C1-C6)- OR19, -OCF3, -NR19R20, -alquil(C1-C6)-NR19R20, -NHSO2R19, - SO2N(R26)2, -SO2R19, -SOR19, -SR19, -NO2, - CONR19R20, -NR20COR19, -COR19, -COCF3, -OCOR19, -OCO2R19, -COOR19, -alquil(C1-C6)-NHCOOC(CH3)3, -alquil(C1- C6)-NHCOCF3, alquil (C1-C6)-NHSO2-alquilo(C1-C6), alquil(C1- C6)-NHCONH-alquilo(C1-C6).

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