公开(公告)号：EP1694659A1

公开(公告)日：2006-08-30

申请号：EP04814266.5

申请日：2004-12-16

申请人： SCHERING CORPORATION ,  Pharmacopeia Drug Discovery, Inc.

发明人： BIJU, Purakkattle, J. ,  TAVERAS, Arthur, G. ,  YU, Younong ,  ZHENG, Junying ,  CHAO, Jianhua ,  AKI, Cynthia, J. ,  FINE, Jay ,  LUNDELL, Daniel ,  PRIESTLEY, Tony ,  REGGIANI, Angelo ,  MERRITT, J., Robert ,  BALDWIN, John, J.

IPC分类号： C07D285/10 ,  C07D417/12 ,  C07D417/14 ,  A61K31/433 ,  A61K31/4436

CPC分类号： C07D285/10 ,  C07D285/06 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are novel compounds of Formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of Formula (IA).

公开(公告)号：EP1697354A1

公开(公告)日：2006-09-06

申请号：EP04814856.3

申请日：2004-12-20

申请人： SCHERING CORPORATION ,  Pharmacopeia Drug Discovery, Inc.

发明人： TAVERAS, Arthur, G. ,  ZHENG, Junying ,  BIJU, Purakkattle, J. ,  YU, Younong ,  CHAO, Jianhua ,  FINE, Jay ,  LUNDELL, Daniel ,  PRIESTLEY, Tony ,  REGGIANI, Angelo ,  MERRITT, J., Robert ,  BALDWIN, John, J. ,  LAI, Gaifa ,  WU, Minglang

IPC分类号： C07D417/12 ,  C07D275/02 ,  C07D417/14 ,  A61K31/427 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D275/03 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are novel compounds of the formula (IA): and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.

公开(公告)号：EP1694659B1

公开(公告)日：2008-08-27

申请号：EP04814266.5

申请日：2004-12-16

申请人： Schering Corporation ,  Pharmacopeia Drug Discovery, Inc.

发明人： BIJU, Purakkattle, J. ,  TAVERAS, Arthur, G. ,  YU, Younong ,  ZHENG, Junying ,  CHAO, Jianhua ,  AKI, Cynthia, J. ,  FINE, Jay ,  LUNDELL, Daniel ,  PRIESTLEY, Tony ,  REGGIANI, Angelo ,  MERRITT, J., Robert ,  BALDWIN, John, J.

IPC分类号： C07D285/10 ,  C07D417/12 ,  C07D417/14 ,  A61K31/433 ,  A61K31/4436

CPC分类号： C07D285/10 ,  C07D285/06 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are novel compounds of Formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of Formula (IA).

摘要翻译： 公开了式（IA）的新化合物及其药学上可接受的盐和溶剂化物。 包含取代基A的基团的实例包括杂芳基，芳基，杂环烷基，环烷基，芳基，炔基，烯基，氨基烷基，烷基或氨基。 包含取代基B的基团的例子包括芳基和杂芳基。 还公开了治疗趋化因子介导的疾病例如癌症，血管生成，血管生成性眼病，肺部疾病，多发性硬化症，类风湿性关节炎，骨关节炎，中风和局部缺血再灌注损伤，疼痛（例如急性疼痛，急性和慢性 炎症性疼痛和神经性疼痛）使用式（IA）的化合物。

公开(公告)号：EP2318391A1

公开(公告)日：2011-05-11

申请号：EP09790675.4

申请日：2009-07-21

申请人： Schering Corporation

发明人： DE LERA RUIZ, Manuel ,  BERLIN, Michael, Y. ,  ZHENG, Junying ,  ASLANIAN, Robert, G. ,  MCCORMICK, Kevin, D. ,  ZENG, Qingbei

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/14 ,  A61P11/02 ,  A61K31/445 ,  A61P37/08

CPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/14

摘要： The present invention relates to novel Tricyclic Heterocylce Derivatives, pharmaceutical compositions comprising the Tricyclic Heterocycle 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 disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. R1 is formula (Ia), (Ib) or (Ic); R
2 is alkvl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl. any of which can be optionally substituted with R
11 ; M
1 is -CH-. -C(halo)- or -N-; Y is -C(O)-, -S-. -S(O)-, -S(O)
2 -, -CH
2 - or -O-, such that Y is not -O- when an adjacent atom is N.

公开(公告)号：EP2318387A1

公开(公告)日：2011-05-11

申请号：EP09790676.2

申请日：2009-07-21

申请人： Schering Corporation

发明人： DE LERA RUIZ, Manuel ,  BERLIN, Michael, Y. ,  ZHENG, Junying ,  ASLANIAN, Robert, G. ,  MCCORMICK, Kevin, D.

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  A61P11/02 ,  A61P37/08 ,  A61K31/445

CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

摘要： The present invention relates to novel bicyclic heterocycle derivatives, pharmaceutical compositions comprising the bicyclic heterocycle 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 disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. R
1 is: I, Ia, Ib ou Ic. R
2 is alkyl, alkenyl, aryl, cycloalkyl. heterocycloalkyl or heteroaryl, any of which can be optionally substituted with R
3 ; Y is -C(O)-, -S-, -S(O)-, -S(O)
2 -, -CH
2 - or -O-, such that if Y is -O- or -S-, then M is other than N and R
1 is (Ib);

公开(公告)号：EP2257546A2

公开(公告)日：2010-12-08

申请号：EP09713459.7

申请日：2009-02-19

申请人： Schering Corporation

发明人： ZHENG, Junying ,  CHAO, Jianhua ,  MCCORMICK, Kevin, D. ,  ASLANIAN, Robert, G. ,  MUTAHI, Mwangi, W. ,  BOYCE, Christopher, W. ,  WON, Walter, S.

IPC分类号： C07D403/06 ,  C07D403/08 ,  A61K31/47 ,  A61K31/403 ,  A61P29/00 ,  A61P25/00 ,  A61P3/10 ,  A61P9/00

CPC分类号： C07D403/06 ,  C07D403/08

摘要： In its many embodiments, the present invention provides a novel class of heterocyclic derivatives as a2C 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 a2C adrenergic receptors using such compounds or pharmaceutical compositions.

公开(公告)号：EP2356106A1

公开(公告)日：2011-08-17

申请号：EP09793312.1

申请日：2009-10-06

申请人： Schering Corporation

发明人： MCCORMICK, Kevin D. ,  DONG, Li ,  BOYCE, Christopher W ,  DE LERA RUIZ, Manuel ,  FEVRIER, Salem ,  WU, Jie ,  ZHENG, Junying ,  YU, Younong ,  CHAO, Jianhua ,  WON, Walter S. ,  RAO, Ashwin U. ,  KUANG, Rongze ,  TING, Pauline C. ,  HUANG, Xianhai ,  SHAO, Ning ,  PALANI, Anandan ,  BERLIN, Michael Y. ,  ASLANIAN, Robert G.

IPC分类号： C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10 ,  C07D235/02 ,  C07D263/52 ,  C07D498/10 ,  C07D519/00 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/424 ,  A61P11/02

CPC分类号： A61K31/5377 ,  A61K31/437 ,  A61K31/501 ,  A61K31/506 ,  A61K31/537 ,  C07D235/02 ,  C07D263/52 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/10 ,  C07D519/00

摘要： In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators 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二氨基螺氨基恶唑啉类似物作为α2C肾上腺素能受体激动剂的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种此类化合物 以及使用这些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：EP1902046B1

公开(公告)日：2009-12-02

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：EP2142538B1

公开(公告)日：2011-10-26

申请号：EP08714240.2

申请日：2008-02-11

申请人： Schering Corporation

发明人： ZHENG, Junying ,  MCCORMICK, Kevin, D. ,  CHAO, Jianhua ,  BOYCE, Christopher, W. ,  ASLANIAN, Robert, G. ,  YU, Younong

IPC分类号： C07D405/06 ,  C07D405/08 ,  C07D405/14 ,  C07D409/06 ,  C07D417/14 ,  C07D491/052 ,  A61K31/353 ,  A61P25/06

CPC分类号： C07D405/06 ,  C07D405/08 ,  C07D405/14 ,  C07D409/06 ,  C07D417/14 ,  C07D491/052

摘要： In its many embodiments, the present invention provides a novel class of chroman compounds of formula I as α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of prepaxing 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.

公开(公告)号：EP2205588A2

公开(公告)日：2010-07-14

申请号：EP08835011.1

申请日：2008-09-25

申请人： Schering Corporation

发明人： CHAO, Jianhua ,  ASLANIAN, Robert, G. ,  ZHENG, Junying

IPC分类号： C07D401/14 ,  C07D417/14 ,  A61K31/506 ,  A61K31/4523 ,  A61P1/00 ,  A61P25/00 ,  A61P3/04 ,  A61P3/10 ,  A61P37/08

CPC分类号： C07D417/14 ,  C07D401/14

摘要： The present invention relates to novel Oxypiperidine Derivatives, pharmaceutical compositions comprising the Oxypiperidine Derivatives and the use of the Oxypiperidine Derivatives for treating or preventing treating allergy, an allergy-induced airway response, congestion, hypotension, a cardiovascular disease, a gastrointestinal disorder, obesity, a sleep disorder, pain, diabetes, a diabetic complication, impaired glucose tolerance, impaired fasting glucose or a central nervous system (CNS) disorder.