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41. 发明专利

AU2003223627A1 (1-4-PIPERIDINYL) BENZIMIDAZOLE DERIVATIVES USEFUL AS HISTAMINE H3 ANTAGONISTS 未知
公开(公告)号：AU2003223627A1
公开(公告)日：2003-11-03
申请号：AU2003223627
申请日：2003-04-16
申请人： SCHERING CORP
发明人： CAO JIANHUA , KOZLOWSKI JOSEPH A , MANGIARACINA PIETRO , CORMICK KEVIN D MC , MUTAHI MWANGI W , ROSENBLUM STUART B , SHIH NENG-YANG , SOLOMON DANIEL M , TOM WING C , ZENG QINGBEI , ASLANIAN ROBERT G , BERLIN MICHAEL Y , BOYCE CHRISTOPHER W
IPC分类号： A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K45/00 , A61P1/00 , A61P3/04 , A61P9/00 , A61P11/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/28 , A61P37/08 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , A61K31/4184
摘要： Disclosed are histamine H3 antagonists of the formula (I) wherein R is optionally substituted benzimidazolyl or a derivative thereof; R is optionally substitutd aryl or heteroaryl; M1 and M are C(R ) or N; Q is -N(R )-, -S- or -O-; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating various diseases or conditions, such as allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I. Also disclosed are methods of treating said diseases or conditions using the compounds of formula I in combination with an H1 receptor antagonist.

42. 发明专利

NO20031744D0 未知
公开(公告)号：NO20031744D0
公开(公告)日：2003-04-15
申请号：NO20031744
申请日：2003-04-15
申请人： SCHERING CORP
发明人： ASLANIAN ROBERT G , SHIH NENG-YANG , TING PAULINE C , BERLIN MICHAEL Y , ROSENBLUM STUART B , MCCORMICK KEVIN D , TOM WING C , BOYCE CHRISTOPHER W , MANGIARACINA PIETRO , MUTAHI MWANGI WA , PIWINSKI JOHN J
IPC分类号： A61K31/445 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K45/00 , A61P1/00 , A61P3/04 , A61P5/00 , A61P9/00 , A61P11/02 , A61P11/04 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/28 , A61P37/08 , C07D213/73 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/04 , C07D
摘要： Disclosed are novel compounds of the Formula (I). Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I). Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula (I). Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g. nasal congestion) using the compounds of Formula (I) in combination with a H1 receptor antagonist.

43. 发明专利

GR3036676T3 SUBSTITUTED OXIMES, HYDRAZONES AND OLEFINS AS NEUROKININ ANTAGONISTS 未知
公开(公告)号：GR3036676T3
公开(公告)日：2001-12-31
申请号：GR20010401533
申请日：2001-09-20
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.

44. 发明专利

DK0823896T3 未知
公开(公告)号：DK0823896T3
公开(公告)日：2001-09-24
申请号：DK96915341
申请日：1996-05-01
申请人： SCHERING CORP
发明人： MANGIARACINA PIETRO , PIWINSKI JOHN J , REICHARD GREGORY A , ASLANIAN ROBERT G , ALAIMO CHERYL L , KIRKUP MICHAEL P , LUPO ANDREW , MCCORMICK KEVIN D , 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.

45. 发明专利

AU706526B2 Substituted oximes, hydrazones and olefins as neurokinin antagonists 未知
公开(公告)号：AU706526B2
公开(公告)日：1999-06-17
申请号：AU5714096
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.

46. 发明专利

BR9608269A 未知
公开(公告)号：BR9608269A
公开(公告)日：1999-02-17
申请号：BR9608269
申请日：1996-05-01
申请人： SCHERING CORP
发明人： ASLANIAN ROBERT G , ALAIMO CHERYL A , KIRKUP MICHAEL P , LUPO ANDREW JR , MANGIARACINA PIETRO , MCCORMICK KEVIN D , PIWINSKI JOHN J , REICHARD GREGORY A , SHANKAR BANDARPALLE , CARRUTHERS NICHOLAS I , SHIH NENG-YANG , SPITLER JAMES M , TING PAULINE C , GANGULY ASHIT
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.

47. 发明专利

PL323088A1 SUBSTITUTED OXIMES, HYDRAZONES AND OLEFINS AS NEUROKININ ANTAGONISTS 未知
公开(公告)号：PL323088A1
公开(公告)日：1998-03-02
申请号：PL32308896
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
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.

48. 发明专利

NO975029L 未知
公开(公告)号：NO975029L
公开(公告)日：1997-12-30
申请号：NO975029
申请日：1997-10-31
申请人： SCHERING CORP
发明人： GANGULY ASHIT KUMAR , CARRUTHERS NICHOLAS I , 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
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
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.

49. 发明专利

ES2337727T3 DERIVADOS DE PIPERIDINA UTILES COMO ANTAGONISTAS DE HISTAMINA H3. 未知
公开(公告)号：ES2337727T3
公开(公告)日：2010-04-28
申请号：ES06773528
申请日：2006-06-19
申请人： SCHERING CORP
发明人： ASLANIAN ROBERT G , BERLIN MICHAEL Y , BOYCE CHRISTOPHER W , CHAO JIANHUA , DE LERA RUIZ MANUEL , MANGIARACINA PIETRO
IPC分类号： C07D401/12 , A61P3/04 , A61P29/00 , A61P37/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04
摘要： Un compuesto representado por la fórmula estructural **(Ver fórmula)** o una sal farmacéuticamente aceptable del mismo, donde: a es 0, 1 ó 2; b es 0, 1 ó 2; n es 2; P es 2; M1 es N; M2 es CH o CF; M3 es N; Y es -C(=O)-, -C(=S)-, -(CH2)q-, -C(=NOR7)- o -SO1-2-; q es 1, 2, 3, 4 ó 5, con la condición de que cuando M1 y M2 son los dos N, q es 2, 3, 4 ó 5; X es -N(R4)-, -N(R4)-CH(R19)-, -CH(R19)-N(R4)-, -CH(R19)CH(R19)N(R4)-, -(CH2),-C(O)-N(R4)-, -O-(CH2)2-C(O)-N(R4)-, -CH2-O-(CH2)3-C(O)-N(R4)-, -(CH2)t-N(R4)-C(O)-, -C(O)-N(R4)-CH2-, -(CH2)t-N(R18)C(O)N(R19)-, -N(R15)C(O)N(R19)-(CH2)t-, -(CH2)t-OC(O)N(R19)-, -N(R19)C(O)O-, -O-, -OCH2-, CH2O-, -OC(O)-, -C(O)O-, OCH(R19)-, -CH(R19)O- o -S-; r es 0, 1, 2 ó 3; t es 0 ó 1; Z es -CH2; R1 es H, R10-alquilo, R10-cicloalquilo, R10-arilo, R10-monoheteroarilo, R10-heterocicloalquilo, o un grupo de la fórmula: **(Ver fórmula)** donde el anillo A es un anillo monoheteroarilo, teniendo dicho anillo monoheteroarilo o monoheteroarilo de 1 a 4 heteroátomos seleccionados entre O, S y N, interrumpiendo dichos heteroátomos una estructura de anillo carbocíclico aromático que tiene de 1 a 6 átomos de carbono; R2 es R16-arilo, R16-heteroarilo, R16-cicloalquilo o R16-heterocicloalquilo; R3 es H. alquilo, R21-arilo, -R22-cicloalquilo, R22-heterocicloalquilo, R21-heteroarilo o-C(O)NH2; R4 es H, alquilo, haloalquilo, R18-arilo, R16-heteroarilo, R18-arilalquilo, -C(O)R12 o -SO2R13; cada uno de R5 y R6 se selecciona independientemente entre el grupo que consiste en halo alquilo, -OH, alcoxi, haloalquilo y -CN; o dos sustituyentes R5 en el mismo átomo de carbono o dos sustituyentes R6 en el mismo átomo de carbono forman =O; R7 es H, alquilo, haloalquilo, R10-arilo o R10-heteroarilo; cada R9 se selecciona independientemente entre el grupo que consiste en H y alquilo; R10 es 1, 2, 3 ó 4 sustituyentes seleccionados independientemente entre el grupo que consiste en H, halo, alquilo, R10''-cicloalquilo, -OH, alcoxi, R10''-arilo, R10''-arilalquilo, R10''-heteroarilo, R10''-hetercarilalquilo, R10-ariloxi, haloalquilo, haloalcoxi, -NO2, -C(O)-alquilo, -C(O)-heterocicloalquilo, -CO2R11, -N(R11)2,-CON(R11)2, -NHC(O)R11, -NHC(O)-alcoxialquil-, -NHC(O)-CH2-NHC(O)CH3, -NHSO2R11, -CH(=NOR19), -SO2N(R11)2, -SO2CF3 y -CN; cada R10'' es 1, 2, 3 ó 4 sustituyentes seleccionados independientemente entre el grupo que consiste en H, halo, alquilo, cicloalquilo, -OH, alcoxi, arilo, arilalquilo, heteroarilo, heteroarilalquilo, ariloxi, haloalquilo, haloalcoxi, -NO2, -C(O)-alquilo, -C(O)-heterocicloalquilo, -CO2R11, -N(R11)2,-CON(R11)2, -NHC(O)R11, -NHC(O)-alcoxialquil-, NHC(O)-CH2-NHC(O)CH3, -NHSO2R11, -CH(=NOR19), -SO2N(R11)2, -SO2CF3 y - CN; cada R11 se selecciona independientemente entre el grupo que consiste en H, alquilo, haloalquilo, R18-arilo, R18-heteroarilo, R18-arilalquilo, R18-cicloalquilo y R18-heterocicloalquilo; R12 es alquilo, R18-cicloalquilo, R18-arilo, R18-heteroarilo o R18-heterocicloalquilo; R13 es alquilo, R18-arilo o alquilsulfonilalquilo; R16 es 1, 2 ó 3 sustituyentes seleccionados independientemente entre el grupo que consiste en H, halo, alquilo, R10-cicloalquilo, -OH, alcoxi, hidroxialquilo, R10-arilo, R10-heteroarilo, R10-heterocicloalquilo, R10-ariloxi, haloalquilo, haloalcoxi, -NO2, -CO2R17, -N(R17)2, -alquileno-N(R17)2, -CON(R17)2, -NHC(O)R17, -NHC(O)OR17, -NHSO2R17, -SO2N(R17)2 y -CN; cada R17 se selecciona independientemente entre el grupo que consiste en H, alquilo, haloalquilo, R18-arilo, R18-heteroarilo, R18-cicloalquilo y R18-heterocicloalquilo; R18 es 1, 2 ó 3 sustituyentes seleccionados independientemente entre el grupo que consiste en H, alquilo, halo, alcoxi, haloalquilo, -NO2, -CN y -alquileno-N(R17)2; cada R17 se selecciona independientemente entre el grupo que consiste en H, alquilo, haloalquilo arilo, heteroarilo, cicloalquilo y heterocicloalquilo; R19 se selecciona independientemente entre el grupo que consiste en H y alquilo; R21 es 1, 2, 3 ó 4 sustituyentes seleccionados independientemente entre el grupo que consiste en H, halo, alquilo, -OH, alcoxi, haloalquilo, haloalcoxi, -NO2, -CN, -C(O)N(R19)2 y - N(R19)2; y R22 es 1, 2 ó 3 sustituyentes seleccionados independientemente entre el grupo que consiste en halo, alquilo, -OH, alcoxi, haloalquilo, -NO2 y -CN-.

50. 发明专利

DE602006010870D1 未知
公开(公告)号：DE602006010870D1
公开(公告)日：2010-01-14
申请号：DE602006010870
申请日：2006-06-19
申请人： SCHERING CORP
发明人： ASLANIAN ROBERT G , BERLIN MICHAEL Y , BOYCE CHRISTOPHER W , CHAO JIANHUA , DE LERA RUIZ MANUEL , MANGIARACINA PIETRO , MCCORMICK KEVIN D , MUTAHI MWANGI W , ROSENBLUM STUART B , SHIH NENG-YANG , SOLOMON DANIEL M , TOM WING C , VACCARO HENRY A , ZHENG JUNYING , ZHU XIAOHONG
IPC分类号： C07D401/12 , A61P3/04 , A61P29/00 , A61P37/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04
摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(═O)—, —C(═S)—, —(CH2)q—, —C(═NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, or alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, all optionally substituted, or a group of the formula: where ring A is a heteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R3 is H, —C(O)NH2, or alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, all optionally substituted; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome, alcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma and cognition deficit disorders using said compounds, alone or in combination with other agents.

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