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21. 发明专利

NZ334966A Substituted arylalkylamines as neurokinin antagonists 未知
公开(公告)号：NZ334966A
公开(公告)日：2000-10-27
申请号：NZ33496696
申请日：1996-10-28
申请人： SCHERING CORP
发明人： REICHARD GREGORY A , ASLANIAN ROBERT G
IPC分类号： A61K31/445 , A61K31/451 , A61P1/00 , A61P11/06 , A61P25/00 , A61P29/00 , A61P43/00 , C07D211/52
摘要： A compound represented by the structural formula I or a pharmaceutically acceptable salt thereof, wherein; A1 is OR6, N(R6)(R7), S(O)eR13 or (C(R6)(R7))1-6N(R6)(R7) and A2 is H, or A1 and A2 together are O, C(R6)(R7) or NOR6, Q is R5-phenyl, T is R4-aryl, b is 0, 1 or 2, b1 is 1 or 2, X is O, NR6, N(R6)C(O), OC(O)NR6 or N(R6)C(O)O, R4 and R5 are independently 1-3 substituents independently selected from the group consisting of H, halogeno, OR6, OC(O)R6, OC(O)N(R6)(R7), N(R6)(R7), C1-6 alkyl, CF3, C2F5, COR6, CO2R6, CON(R6)(R7), S(O)eR13, CN, OCF3, NR6CO2R16, NR6COR7, NR8CON(R6)(R7), R15-phenyl, R15-benzyl, NO2, N(R6)S(O)2R13 or S(O)2N(R6)(R7) or adjacent R4 substituents or adjacent R5 substituents can form a OCH2O group and R4 can also be R15-heteroaryl, R6, R7, R8, R8a, and R13 are independently selected from the group consisting of H, C1-6 alkyl, C2-C6 hydroxyalkyl, C1-C6 alkoxy-C1-C6 alkyl, R15-phenyl, and R15-benzyl or R6 and R7, together with the nitrogen to which they are attached, form a ring of 5 to 6 members, wherein 0, 1 or 2 ring members are selected from the group consisting of O, S and N(R19), R9 and R9a are independently selected from the group consisting of R6 and OR6, provided that when R9 is OH, X is N(R6)C(O), R10 is independently selected from the group consisting of H and C1-6 alkyl, R15 is 1 to 3 substituents independently selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, halogeno, CF3, C2F5, COR10, CO2R10, C(O)N(R10)2, S(O)eR10, CN, N(R10)COR10, N(R10)CON(R10)2 and NO2, R16 is C1-6 alkyl, R15-phenyl or R15-benzyl, R19 is H, C1-C6 alkyl, C(O)N(R10)2, CO2R10, (C(R8)(R9))fCO2R10 or (C(R8)(R9))uC(O)N(R10)2, f is 1-6, u is 0-6, Z is formula II or formula III, g is 1, j is 1 or 0, h is 2, k is 2 or 3, J is two hydrogen atoms or O, L is H, C1-C6 alkyl, C1-C6 alkenyl, CH2 cycloalkyl, R15-benzyl, R15-heteroaryl, C(O)R6, (CH2)mOR6, (CH2)mN(R6)(R7), (CH2)mC(O)OR6 or (CH2)mC(O)N(R6)(R7), L1 is H, R28 is H, OH, phenyl or H2NC(O) and R29 is H or R4-phenyl. The abovementioned compounds are useful in the treatment of asthma, cough, bronchospasm, central nervous system diseases, inflammatory diseases and gastrointestinal disorders.

22. 发明专利

PE134599A1 OXIMAS SUSTITUIDAS COMO ANTAGONISTAS EN NEUROQUININA 未知
公开(公告)号：PE134599A1
公开(公告)日：2000-01-07
申请号：PE00112298
申请日：1998-11-18
申请人： SCHERING CORP
发明人： SHIH NENG-YANG , REICHARD GREGORY A , ALAIMO CHERYL A , CARRUTHERS NICHOLAS I , LAVEY BRIAN J , TING PAULINE C
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61K31/45 , A61K31/451 , A61K31/452 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/5375 , A61K31/5377 , A61K31/541 , A61P1/00 , A61P1/08 , A61P11/00 , A61P11/06 , A61P11/14 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/28 , A61P27/02 , A61P29/00 , A61P43/00 , C07D211/24 , C07D211/26 , C07D211/34 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/76 , C07D211/94 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/12 , C07D409/14 , C07D417/14
摘要： SE REFIERE A OXIMAS SUSTITUIDAS DE FORMULA I; DONDE T ES FENILO, R2-FENILO o R3-PIRIDILO; R1 ES H, METILO, ETILO, -CH2CN, -CH2C(O)NH2, -(CH2)3SO3H, -CH2C(O)NHCH3, -CH2C(O)NHOCH3, -CH2C(O)NHCH2CN, -CH2F, -CH2C(O)NHCH2SO3H, ENTRE OTROS; R2 ES CLORO, METILO, METOXI; R3 ES CLORO, METILO; R4 ES METILO O ETILO; Z ES PIPERIDINILO SUSTITUIDO, DE PREFERENCIA UN GRUPO DE FORMULA a, b. TAMBIEN SE REFIERE A UN COMPUESTO PREFERIDO DE FORMULA Ia. EL COMPUESTO I ES UN INHIBIDOR DE RECEPTORES DE TAQUIQUININA, EN PARTICULAR ANTAGONISTAS DE LOS NEUROPEPTIDOS RECEPTOR DE NEUROQUININA-1 , NEUROQUININA-2 o NEUROQUININA-3; QUE SE ENCUENTRAN EN EL SNC, EN EL SISTEMA CIRCULATORIO Y EN LOS TEJIDOS PERIFERICOS DE LOS MAMIFEROS; POR LO QUE PUEDEN SER UTILES EN EL TRATAMIENTO O PREVENCION DE ASMA, TOS, ENFERMEDADES PULMONARES OBSTRUCTIVAS CRONICAS, BRONCOESPASMO, EMESIS, ENFERMEDADES NEURODEGENERATIVAS, ENFERMEDADES OCULARES, ENFERMEDADES INFLAMATORIAS TAL COMO ARTRITIS; CONDICIONES DEL SNC COMO MIGRANA, EPILEPSIA, NOCICEPCION, PSICOSIS, ENFERMEDAD DE CROHN

23. 发明专利

CZ342497A3 SUBSTITUTED OXIMES, HYDRAZONES AND OLEFINS AS NEUROKININ ANTAGONISTS 未知
公开(公告)号：CZ342497A3
公开(公告)日：1998-07-15
申请号：CZ342497
申请日：1996-05-01
申请人： SCHERING CORP
发明人： REICHARD GREGORY A , ASLANIAN ROBERT G , ALAIMO CHERYL L , KIRKUP MICHAEL P , LUPO ANDREW , MANGIARACINA PIETRO , MCCORMICK KEVIN D , PIWINSKI JOHN J , SHANKAR BANDARPALLE , SHIH NENG YANG , SPITLER JAMES M , TING PAULINE C , GANGULY ASHIT , CARRUTHERS NICHOLAS I
IPC分类号： C07D295/12 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/4178 , A61K31/439 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61K31/45 , A61K31/451 , A61K31/452 , A61K31/4523 , A61K31/4525 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P1/00 , A61P11/00 , A61P25/00 , A61P29/00 , A61P43/00 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/14 , C07D211/52 , C07D211/58 , C07D211/76 , C07D295/13 , C07D295/185 , C07D333/22 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/12 , C07D409/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D451/04 , C07D295/18
摘要： Compound represented by the structural formula I or a pharmaceutically acceptable salt thereof, wherein: a is 0, 1, 2 or 3; b, d and e are independently 0, 1 or 2; R is H, C1-6 alkyl, -OH or C2-C6 hydroxyalkyl; A is an optionally substituted oxime, hydrazone or olefin; X is a bond, -C(O)-, -O-, -NR6-, -S(O)e-, -N(R6)C(O)-, -C(O)N(R6)-OC(O)NR6-, -OC(=S)NR6-, -N(R6)C(=S)O-, -C(=NOR1)-, -S(O)2N(R6)-, -N(R6)S(O)2-,-N(R6)C(O)O- or -OC(O)-; T is H, phthalimidyl, aryl, heterocycloalkyl, heteroaryl, cycloalkyl or bridged cycloalkyl; Q is -SR6, -N(R6)(R7), -OR6, phenyl, naphthyl or heteroaryl; R6a, R7a, R8a, R9a, R6 and R7 are H, C1-6 alkyl, C2-C6 hydroxyalkyl, C1-C6 alkoxy-C1-C6 alkyl, phenyl or benzyl; or R6 and R7, together with the nitrogen to which they are attached, form a ring; R9a is R6 or -OR6; Z is morpholinyl, optionally N-substituted piperazinyl, optionally substituted or substituted g is 0-3 and h is 1-4, provided the sum of h and g is 1-7; wherein aryl, heterocycloalkyl, heteroaryl, cycloalkyl and bridged cycloalkyl groups are optionally substituted; methods of treating asthma, cough, bronchospasm, imflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.

24. 发明专利

AU5086298A Substituted oximes, hydrazones and olefins as neurokinin antagonists 未知
公开(公告)号：AU5086298A
公开(公告)日：1998-05-29
申请号：AU5086298
申请日：1997-10-30
申请人： SCHERING CORP
发明人： SHIH NENG-YANG , REICHARD GREGORY A , ASLANIAN ROBERT G
IPC分类号： A61P25/04 , A61K31/438 , A61K31/547 , A61P1/04 , A61P11/06 , A61P11/08 , A61P11/14 , A61P19/02 , A61P25/08 , C07D233/61 , C07D249/08 , C07D471/10 , C07D513/10 , A61K31/435 , C07D213/63 , C07D221/20 , C07D239/48 , C07D257/04 , C07D295/12 , C07D473/18 , C07D495/10

25. 发明专利

AU7460796A Substituted arylalkylamines as neurokinin antagonists 未知
公开(公告)号：AU7460796A
公开(公告)日：1998-05-22
申请号：AU7460796
申请日：1996-10-28
申请人： SCHERING CORP
发明人： REICHARD GREGORY A , ASLANIAN ROBERT G
IPC分类号： A61K31/445 , A61K31/451 , A61P1/00 , A61P11/06 , A61P25/00 , A61P29/00 , A61P43/00 , C07D211/52
摘要： Aralkylamine derivatives of formula (I) and their salts are new: A1 = CH2R6, OR6, NR6R7, SOeR13, (CR6R7)qOR6, (CR6R7)qNR6R7 or (CR6R7)qSOeR13; q = 1-6; A2 = H; or A1+A2 = O, CR6R7, NOR6 or S; Q = R5-phenyl, R5-naphthyl, SR6, NR6R7, OR6 or R5-heteroaryl; T = H, R4-aryl, R4-heterocycloalkyl, R4-heteroaryl, R4-cycloalkyl or R10-bridged cycloalkyl; b = 0-2; b1 = 1-2; X = a bond, CO, O, NR6, SOe, NR6CO, CONR6, OC(O)NR6, OC(S)NR6, NR6C(S)O, C(=NOR6), SO2NR6, NR6SO2, NR6CO2 or OC(O); R4, R5 = 1-3 of H, halo, OR6, OC(O)R6, OC(O)NR6R7, NR6R7, 1-6C alkyl, CF3, C2F5, COR6, CO2R6, CONR6R7, SOeR13, CN, OCF3, NR6CO2R16, NR6COR7, NR8CONR6R7, R15-phenyl, R15-benzyl, NO2, NR6SO2R13 or SO2NR6R7; or adjacent R4 substituents or adjacent R5 substituents can form OCH2O; or R4 = R15-heteroaryl; R6, R7, R8, R8a, R13 = H, 1-6C alkyl, 2-6C hydroxyalkyl, 1-6C alkoxy-1-6C alkyl, R15-phenyl or R15-benzyl or NR6R7 = 5-6 membered ring containing 1-2 of O, S and/or NR19; R9, R9a = R6 or OR6; provided that when R9 = OH, then X = a bond, CO, NR6CO or C(=NOR6); R10 = H or 1-6C alkyl; R15 = 1-3 of H, 1-6C alkyl, 1-6C alkoxy, 1-6C alkylthio, halo, CF3, C2F5, COR10, CO2R10, CON(R10)2, SOeR10, CN, N(R10)COR10, N(R10)CON(R10)2 or NO2; R16 = 1-6C alkyl, R15-phenyl or R15-benzyl; R19 = H, 1-6C alkyl, CON(R10)2, CO2R10, (CR8R9)fCO2R10 or (CR8R9)uC(O)N(R10)2; f = 1-6; u = 0-6; Z = a group of formula (a)-(c): g, j = 0-3; h, k = 1-4, provided that h +g = 1-7; J = (H, H), O, S, NR9 or NOR9; L, L1 = H, 1-6C alkyl, 1-6C alkenyl, CH2-cycloalkyl, R15-benzyl, R15-heteroaryl, COR6, (CH2)mOR6, (CH2)mNR6R7, (CH2)mCO2R6 or (CH2)mCONR6R7; m = 0-4; provided that when j = 0 then m = 1-4; R25 = H, 1-6C alkyl, CN, R15-phenyl or R15-benzyl; R26, R27 = H, 1-6C alkyl, R4-aryl or R4-heteroaryl or R26 = H, 1-6C alkyl, R4-aryl or R4-heteroaryl and R27 = COR6, CONR6R7, COR4-aryl, COR4-heteroaryl, SO2R13 or SO2R4-aryl; R28 = H, (CR6R19)tG or (CR6R7)vG2; t, v = 0-3; provided that when j = 0 then t = 1-3; R29 = H, 1-6C alkyl, C(R10)2SOeR6, R4-phenyl or R4-heteroaryl; G = H, R4-aryl, R4-heterocycloalkyl, R4-heteroaryl, R4-cycloalkyl, OR6, NR7R6, COR6, CO2R6, CONR7R9, SOeR13, NR6CO2R16, NR6COR7, NR8CONR6R7, NR6SO2R13, SO2NR6R7, OC(O)R6, OC(O)NR6R7, C(=NOR8)NR6R7, C(=NR25)NR6R7, NR8C(=NR15)NR6R7, CN, C(O)NR6OR7 or C(O)N(R9)-(R4-heteroaryl), provided that when n = 1 and u = 0 or when R9 = OR6 then G is not OH or NR6R7 and G2 = R4-aryl, R4-heterocycloalkyl, R4-heteroaryl, R4-cycloalkyl, COR6, CO2R16, SO2NR6R7 or CONR6R7. 15 Compounds (I) are specifically claimed e.g: N-(2-(3,4-dichlorophenyl)-3-hydroxy-4-(4-hydroxy-4-phenyl-1-piperidinyl)butyl)-N-methyl benzamide.

26. 发明专利

CA2269858A1 SUBSTITUTED OXIMES, HYDRAZONES AND OLEFINS AS NEUROKININ ANTAGONISTS 未知
公开(公告)号：CA2269858A1
公开(公告)日：1998-05-14
申请号：CA2269858
申请日：1997-10-30
申请人： SCHERING CORP
发明人： SHIH NENG-YANG , REICHARD GREGORY A , ASLANIAN ROBERT G
IPC分类号： A61P25/04 , A61K31/438 , A61K31/547 , A61P1/04 , A61P11/06 , A61P11/08 , A61P11/14 , A61P19/02 , A61P25/08 , C07D233/61 , C07D249/08 , C07D471/10 , C07D513/10 , A61K31/435 , C07D213/63 , C07D221/20 , C07D239/48 , C07D257/04 , C07D295/12 , C07D473/18 , C07D495/10
摘要： Compound represented by structural formula (I) or a pharmaceutically acceptable salt thereof, wherein: a is 0, 1, 2 or 3; b, d and e are independently 0, 1 or 2; R is H, C1-6 alkyl, -OH or C2-C6 hydroxyalkyl; A is an optionally substituted oxime, hydrazone or olefin; X is a bond, -C(O)-, -O-, -NR6-, -S(O)e-, -N(R6)C(O)-, -C(O)N(R6)-, -OC(O)NR6-, -OC(=S)NR6-, N(R6)C(=S)O-, -C(=NOR1)-, -S(O)2N(R6)-, -N(R6)S(O)2-, -N(R6)C(O)O- or -OC(O)-; T is H, phthalimidyl, aryl, heterocycloalkyl, heteroaryl, cycloalkyl or bridged cycloalkyl; Q is -SR6, -N(R6)(R7), -OR6, phenyl, naphthyl or heteroaryl; R6a, R7a, R8a, R9a, R6 and R7 are H, C1-6 alkyl, C2-C6 hydroxyalkyl, C1-C6 alkoxy-C1-C6 alkyl, phenyl or benzyl; or R6 and R7, together with the nitrogen to which they are attached, form a ring; R9a is R6 or -OR6; and Z is spiro-substituted piperidinyl or substituted piperazinyl wherein aryl, heterocycloalkyl, heteroaryl, cycloalkyl and bridged cycloalkyl groups are optionally substituted; methods of treating asthma, cough, bronchospasm, inflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.

28. 发明专利

AT435226T 未知
公开(公告)号：AT435226T
公开(公告)日：2009-07-15
申请号：AT05737542
申请日：2005-04-06
申请人： SCHERING CORP
发明人： XIAO DONG , PALANI ANANDAN , WANG CHENG , TSUI HON-CHUNG , SHIH NENG-YANG , REICHARD GREGORY A
IPC分类号： C07D471/04 , A61K31/4355 , A61K31/437 , A61K31/4375 , C07D498/04
摘要： A compound having the general structure shown in Formula 1: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.

29. 发明专利

DE60225067D1 未知
公开(公告)号：DE60225067D1
公开(公告)日：2008-03-27
申请号：DE60225067
申请日：2002-12-17
申请人： SCHERING CORP
发明人： PALIWAL SUNIL , REICHARD GREGORY A , WANG CHENG , XIAO DONG , TSUI HON-CHUNG , SHIH NENG-YANG , ARREDONDO JUAN D , WROBLESKI MICHELLE LACI , PALANI ANANDAN
IPC分类号： C07D211/60 , C07D491/107 , A61K31/357 , A61K31/40 , A61K31/401 , A61K31/4015 , A61K31/402 , A61K31/4025 , A61K31/4166 , A61K31/4178 , A61K31/4188 , A61K31/421 , A61K31/435 , A61K31/4355 , A61K31/437 , A61K31/438 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/499 , A61K31/505 , A61K31/537 , A61K31/5377 , A61K31/664 , A61K45/00 , A61P1/00 , A61P1/08 , A61P3/04 , A61P3/10 , A61P9/10 , A61P11/00 , A61P11/14 , A61P13/10 , A61P15/00 , A61P17/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/36 , A61P27/02 , A61P29/00 , A61P31/18 , C07D207/14 , C07D207/26 , C07D207/50 , C07D211/28 , C07D211/30 , C07D211/32 , C07D211/34 , C07D211/42 , C07D211/56 , C07D211/72 , C07D211/76 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D413/12 , C07D471/10 , C07D487/10 , C07D491/10 , C07D498/10 , C07D513/10
摘要： A NK 1 antagonist having the formula (I), wherein Ar 1 and Ar 2 are optionally substituted phenyl or heteroaryl, X 1 is an ether, thio or imino linkage, R 4 and R 5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.

30. 发明专利

ES2291538T3 ANTAGONISTAS DE NK1. 未知
公开(公告)号：ES2291538T3
公开(公告)日：2008-03-01
申请号：ES02803200
申请日：2002-11-12
申请人： SCHERING CORP
发明人： REICHARD GREGORY A , PALIWAL SUNIL , SHIH NENG-YANG , XIAO DONG , TSUI HON-CHUNG , SHAH SAPNA
IPC分类号： C07D207/273 , C07D211/76 , A61K31/4015 , A61K31/4025 , A61K31/44 , A61K31/4439 , A61K31/451 , A61K31/454 , A61K45/00 , A61P1/00 , A61P1/08 , A61P3/04 , A61P3/10 , A61P9/10 , A61P11/00 , A61P13/00 , A61P15/00 , A61P17/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P27/02 , A61P29/00 , C07D207/22 , C07D207/24 , C07D207/26 , C07D207/36 , C07D207/38 , C07D211/86 , C07D401/04 , C07D403/04
摘要： Un compuesto que tiene la fórmula (I) o una de sus sales farmacéuticamente aceptables, en donde: Ar1 y Ar2 se seleccionan cada uno independientemente del grupo que consiste en R17-heteroarilo- y X1 es -O-, -S-, -SO-, -SO2-, -NR18a-, -N(COR12)- o -N(SO2R15)-; X2 es C, S ó SO; cuando X2 es C, entonces Y es O, S ó NR11; cuando X2 es S ó SO, entonces Y es O, cuando X1 es -SO-, -SO2-, -N(COR12)- o -N(SO2R15)-, entonces; R1 y R2 se seleccionan cada uno independientemente del grupo que consiste en H, alquilo C1-C6, hidroxi (alquilo C1-C3)-, cicloalquilo C3-C8, cicloalquilalquilo C4-C8, -CH2F, -CHF2 y -CF3.

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