公开(公告)号：EP1934203A2

公开(公告)日：2008-06-25

申请号：EP06802156.7

申请日：2006-08-23

申请人： Schering Corporation ,  PHARMACOPEIA, INC.

发明人： MCCORMICK, Kevin, D. ,  BOYCE, Christopher, W. ,  SHIH, Neng-Yang ,  ASLANIAN, Robert, G. ,  MANGIARACINA, Pietro ,  DE LERA RUIZ, Manuel ,  YU, Younong ,  BIJU, Purakkattle, J. ,  HUANG, Chia-Yu ,  LIANG, Bo ,  LIU, Ruiyan ,  LIU, Rong-Qiang ,  GUISE-ZAWACKI, Lisa

IPC分类号： C07D403/06 ,  C07D413/06 ,  C07D417/06 ,  A61K31/435 ,  A61K31/41 ,  A61P29/00

CPC分类号： C07D413/06 ,  C07D403/06 ,  C07D413/04 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as a2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the a2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.

公开(公告)号：EP2125784A2

公开(公告)日：2009-12-02

申请号：EP08714239.4

申请日：2008-02-11

申请人： Schering Corporation ,  Pharmacopeia, LLC

发明人： MCCORMICK, Kevin, D. ,  BOYCE, Christopher, W. ,  SHIH, Neng-yang ,  ASLANIAN, Robert, G. ,  CHAO, Jianhua ,  FEVRIER, Salem ,  MANGIARACINA, Pietro ,  YU, Younong ,  HUANG, Chia-yu ,  LIANG, Bo ,  LU, Huagang ,  LIU, Rong-qiang

IPC分类号： C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/403 ,  A61P31/10 ,  A61P29/00 ,  A61P9/00 ,  A61P25/22

CPC分类号： C07D403/02 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： In its many embodiments, the present invention provides a novel class of indolines as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.

摘要翻译： 在其许多实施方案中，本发明提供了一类新的作为α2C肾上腺素能受体激动剂抑制剂的吲哚啉，制备此类化合物的方法，含有一种或多种这类化合物的药物组合物，制备包含一种或多种这类化合物的药物制剂的方法， 使用这样的化合物或药物组合物治疗，预防，抑制或改善与α2C肾上腺素能受体相关的一种或多种病症的方法。

公开(公告)号：EP2125749A2

公开(公告)日：2009-12-02

申请号：EP08714238.6

申请日：2008-02-11

申请人： Schering Corporation ,  Pharmacopeia, LLC

发明人： DE LERA RUIZ, Manuel ,  MCCORMICK, Kevin, D. ,  BOYCE, Christopher, W. ,  ASLANIAN, Robert, G. ,  YU, Younong ,  MANGIARACINA, Pietro ,  ZHENG, Junying ,  BERLIN, Michael, Y. ,  CIESLA, Stephanie, L. ,  HUANG, Chia-yu ,  LIANG, Bo

IPC分类号： C07D233/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  A61K31/4035 ,  A61P31/10 ,  A61P29/00 ,  A61P9/00 ,  A61P25/22

CPC分类号： C07D403/14 ,  C07D233/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14

摘要： In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of ÿ2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ÿ2C adrenergic receptors using such compounds or pharmaceutical compositions.

公开(公告)号：EP1539742B1

公开(公告)日：2006-11-08

申请号：EP03761216.5

申请日：2003-06-20

申请人： SCHERING CORPORATION

发明人： ASLANIAN, Robert, G. ,  BERLIN, Michael, Y. ,  MANGIARACINA, Pietro ,  MC CORMICK, Kevin, D. ,  MUTAHI, Mwangi, W. ,  ROSENBLUM, Stuart, B.

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K31/445 ,  A61P25/06 ,  A61P25/18 ,  A61P25/28 ,  A61P25/20 ,  A61P27/14

CPC分类号： C07D405/14 ,  C07D401/14 ,  C07D409/14 ,  C07D471/04

摘要： Disclosed are novel compounds of the formula I wherein M1 is CH or N and M2 is C(R3) or N; R1 is optionally substituted indolyl or an aza derivative thereof; R2 is optionally substituted aryl or heteroaryl; and the remaining variables are as defined in the specification. 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.

公开(公告)号：EP1494671A1

公开(公告)日：2005-01-12

申请号：EP03719770.4

申请日：2003-04-16

申请人： SCHERING CORPORATION

发明人： TING, Pauline, C. ,  ASLANIAN, Robert, G. ,  BERLIN, Michael, Y. ,  BOYCE, Christopher, W. ,  CAO, Jianhua ,  MANGIARACINA, Pietro ,  MC CORMICK, Kevin, D. ,  MUTAHI, Mwangi, W. ,  ROSENBLUM, Stuart, B. ,  SHIH, Neng-Yang ,  SOLOMON, Daniel, M. ,  TOM, Wing, C. ,  ZENG, Qingbei

IPC分类号： A61K31/4545 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  A61K31/4184 ,  A61P37/08

CPC分类号： C07D471/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

摘要： Disclosed are histamine H3 antagonists of the formula (I) wherein R is benzimidazolone derivative, M and M are optionally substituted carbon or nitrogen, R includes optionally substituted aryl or heteroaryl, and the remaining variables are as defined in the specification. 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.

公开(公告)号：EP0823896A1

公开(公告)日：1998-02-18

申请号：EP96915341.0

申请日：1996-05-01

申请人： SCHERING CORPORATION

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 ,  A61K31 ,  A61P1 ,  A61P11 ,  A61P25 ,  A61P29 ,  A61P43 ,  C07D205 ,  C07D207 ,  C07D211 ,  C07D333 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409 ,  C07D413 ,  C07D417 ,  C07D451

CPC分类号： C07D295/185 ,  C07D211/52 ,  C07D211/58 ,  C07D211/76 ,  C07D295/13 ,  C07D333/22 ,  C07D401/04 ,  C07D401/06 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

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(R?6¿)C(O)-, -C(O)N(R6)-, -OC(O)NR6-, -OC(=S)NR?6-, -N(R6¿)C(=S)O-, -C(=NOR1)-, -S(O)¿2N(R?6)-, -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 -SR?6, -N(R6)(R7), -OR6¿, phenyl, naphthyl or heteroaryl; R?6a, R7a, R8a, R9a, R6 and R7¿ are H, C¿1-6? alkyl, C2-C6 hydroxyalkyl, C1-C6 alkoxy-C1-C6 alkyl, phenyl or benzyl; or R?6 and R7¿, together with the nitrogen to which they are attached, form a ring; R?9a is R6 or -OR6¿; Z is morpholinyl, optionally N-substituted piperazinyl, optionally substituted (a), or substituted (b); 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, inflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.

公开(公告)号：EP2318388A2

公开(公告)日：2011-05-11

申请号：EP09775391.7

申请日：2009-07-21

申请人： Schering Corporation

发明人： MCCORMICK, Kevin D. ,  ASLANIAN, Robert G. ,  MANGIARACINA, Pietro ,  BERLIN, Michael Y. ,  DE LERA RUIZ, Manuel ,  BOYCE, Christopher W ,  CHAO, Jianhua ,  TING, Pauline C. ,  ZHENG, Junying ,  ROSENBLUM, Stuart B.

IPC分类号： C07D401/06

CPC分类号： C07D471/10 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D491/107 ,  C07D491/20 ,  C07D495/20 ,  C07D498/10

摘要： The present invention relates to novel Tricyclic Spirocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Spirocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disoder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.

摘要翻译： 本发明涉及新的三环螺环衍生物，包含三环螺环衍生物的药物组合物以及这些化合物用于治疗或预防过敏症，过敏引起的气道反应，充血，心血管疾病，炎性疾病，胃肠道病症， 神经系统疾病，代谢疾病，肥胖或肥胖相关疾病，糖尿病，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。

公开(公告)号：EP2194986A1

公开(公告)日：2010-06-16

申请号：EP08714241.0

申请日：2008-02-11

申请人： Schering Corporation ,  Pharmacopeia, LLC

发明人： MCCORMICK, Kevin, D. ,  BOYCE, Christopher, W. ,  SHIH, Neng-yang ,  ASLANIAN, Robert, G. ,  FEVRIER, Salem ,  MANGIARACINA, Pietro ,  DE LERA RUIZ, Manuel ,  YU, Younong ,  ZHENG, Junying ,  HUANG, Chia-yu ,  LIANG, Bo ,  LIU, Rong-Qiang ,  LIU, Ruiyan ,  GUISE ZAWACKI, Lisa

IPC分类号： A61K31/4985 ,  A61K31/5383 ,  A61K31/42 ,  C07D403/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D498/04 ,  A61P11/02 ,  A61P29/00 ,  A61P25/24 ,  A61P27/06

CPC分类号： C07D413/14 ,  C07D241/36 ,  C07D279/06 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04

摘要： The present invention relates to a novel class of phenylmorpholine and phenyl thiomorpholine compounds useful as alpha2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition,- or amelioration of one or more diseases associated with the alpha2C adrenergic receptor agonists, such as allergic rhinitis, congestion, pain, diarrhea, glaucoma, congestive heart failure, cardiac ischemia, manic disorders, depression, anxiety and schizophrenia.

公开(公告)号：EP1902046A1

公开(公告)日：2008-03-26

申请号：EP06773528.2

申请日：2006-06-19

申请人： Schering Corporation

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 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  A61P3/04 ,  A61P29/00 ,  A61P37/00 ,  C07D409/14 ,  C07D471/04

CPC分类号： C07D295/185 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  Y02P20/582

摘要： Disclosed are novel compounds of the formula (I) 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 (II) 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.

公开(公告)号：EP1499316B1

公开(公告)日：2008-03-19

申请号：EP03719766.2

申请日：2003-04-16

申请人： Schering Corporation

发明人： ZENG, Qingbei ,  ASLANIAN, Robert, G. ,  BERLIN, Michael, Y. ,  BOYCE, Christopher, W. ,  CAO, Jianhua ,  KOZLOWSKI, Joseph, A. ,  MANGIARACINA, Pietro ,  MC CORMICK, Kevin, D. ,  MUTAHI, Mwangi, W. ,  ROSENBLUM, Stuart, B. ,  SHIH, Neng-Yang ,  SOLOMON, Daniel, M. ,  TOM, Wing, C.

IPC分类号： A61K31/4545 ,  C07D471/04 ,  C07D401/14 ,  A61K31/4184 ,  A61P37/08

CPC分类号： C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： Disclosed are histamine H3 antagonists of the formula (I) wherein R1 is optionally substituted benzimidazolyl or a derivative thereof; R2 is optionally substitutd aryl or heteroaryl; M1 and M2 are C(R3) or N; Q is -N(R8)-, -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.