公开(公告)号：EP2285784B1

公开(公告)日：2012-07-04

申请号：EP09752080.3

申请日：2009-11-10

申请人： Wyeth LLC

发明人： HAYDAR, Simon N. ,  ANDRAE, Patrick M. ,  YUN, Heedong ,  ROBICHAUD, Albert J.

IPC分类号： C07D235/22 ,  A61K31/496 ,  A61P25/00

CPC分类号： C07D235/22 ,  C07D403/04 ,  C07D487/08

摘要： The invention relates to 1-(arylsulfonyl)-4-(piperazin-1-yl)-1H-benzimidazole compounds of the Formula I: or a tautomer, stereoisomer, or pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.

公开(公告)号：EP2415760A2

公开(公告)日：2012-02-08

申请号：EP11187558.9

申请日：2004-02-18

申请人： ENCYSIVE PHARMACEUTICALS, INC.

发明人： Wu, Chengde ,  Anderson, Eric, C ,  Bui, Huong ,  Gao, Daxin ,  Kassir, Jamal ,  Li, Wen ,  Wang, Junmei ,  Market, Robert, V.

IPC分类号： C07D207/30 ,  C07D213/04 ,  C07D307/34 ,  C07D333/04 ,  C07C15/00 ,  A61P43/00 ,  A61K31/34 ,  A61K31/381 ,  A61K31/40 ,  A61K31/435

CPC分类号： C07D333/38 ,  C07D207/16 ,  C07D209/08 ,  C07D209/44 ,  C07D213/74 ,  C07D237/08 ,  C07D239/26 ,  C07D241/42 ,  C07D295/135 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12

摘要： The present invention relates to CCR-9 antagonists, pharmaceutical compositions containing them and their use.

摘要翻译： 本发明涉及CCR-9拮抗剂，含有它们的药物组合物及其用途。

公开(公告)号：EP2300484B1

公开(公告)日：2011-12-14

申请号：EP09742523.5

申请日：2009-05-04

申请人： Pfizer Inc.

发明人： BRODNEY, Michael, Aaron ,  HELAL, Christopher, John ,  O'NEILL, Brian, Thomas

IPC分类号： C07D513/10 ,  A61K31/4436 ,  A61P25/28

CPC分类号： C07D513/10

摘要： Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：EP2125714B1

公开(公告)日：2011-06-08

申请号：EP08719316.5

申请日：2008-03-06

申请人： Pfizer Limited

发明人： GLOSSOP, Paul, Alan ,  JAMES, Kim

IPC分类号： C07D205/04 ,  A61K31/397 ,  A61P11/00

CPC分类号： C07D205/04

摘要： This invention relates to the hydrochloride salt of 5-[3-{3-hydroxyphenoxy)azetidin-1-yl]-5- methyl-2,2-diphenylhexanamide or derived form thereof and its use as a medicament.

公开(公告)号：EP2264036A1

公开(公告)日：2010-12-22

申请号：EP10173563.7

申请日：2006-01-09

申请人： Wyeth LLC (Formerly Known As Wyeth)

发明人： Malamas, Michael, Sotirios ,  Erdei, James, Joseph ,  Gunawan, Iwan, Suwandi ,  Nowak, Pawel ,  Harrison, Boyd, Lynn

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/28

CPC分类号： C07D487/04

摘要： The present invention provides an amino-imidazolone compound of formula (I):

Also provided are compositions and methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.

摘要翻译： 本发明提供式（I）的氨基咪唑酮化合物：还提供了用于抑制β-分泌酶（BACE）和治疗β-淀粉样蛋白沉积物和神经原纤维缠结的组合物和方法。

公开(公告)号：EP2256107A1

公开(公告)日：2010-12-01

申请号：EP10172623.0

申请日：2006-09-22

申请人： Wyeth LLC

发明人： Malamas, Michael Sotirios ,  Erdei, James, Joseph ,  Fobare, William Floyd ,  Quagliato, Dominick, Anthony ,  Antane, Schuyler, Adam ,  Robichaud, Albert, Jean

IPC分类号： C07D233/88 ,  A61K31/4168 ,  A61P25/28

CPC分类号： C07D233/88 ,  C07D401/12 ,  C07D409/12

摘要： The present invention provides a 2-amino-5-[4-(difluoromethoxy)phenyl]-5-3,-dihydrophenylimidazol-4-one compound of formula (I):

The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neutrofibrillary tangles.

摘要翻译： 本发明提供式（I）的2-氨基-5- [4-（二氟甲氧基）苯基] -5-3-二氢苯基咪唑-4-酮化合物：本发明还提供了用于抑制² - 分泌酶（BACE）并治疗β-淀粉样沉积物和中性原纤维缠结。

公开(公告)号：EP2231630A1

公开(公告)日：2010-09-29

申请号：EP08858146.7

申请日：2008-12-04

申请人： Pfizer Inc.

发明人： WAGER, Travis, T. ,  BUTLER, Todd, William

IPC分类号： C07D295/073 ,  A61K31/40 ,  A61P1/00 ,  A61P11/00 ,  A61P25/00

CPC分类号： C07D295/073

摘要： The present invention is directed to the tosylate salt of trans-N-isobutyl- 3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)-phenyl]-cyclobutanecarboxamide Formula (1): to solvates (e.g., hydrates) thereof, to polymorphs thereof, to pharmaceutical compositions thereof and to a method of treating depression, mood disorders, schizophrenia, anxiety disorders, cognitive disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the Gl tract, hyper- and hypo-motility and acidic secretion of the gastro-intestinal tract comprising administering a therapeutically effective amount thereof.

公开(公告)号：EP2225256A2

公开(公告)日：2010-09-08

申请号：EP08854982.9

申请日：2008-11-17

申请人： Pfizer Limited

发明人： GLOSSOP, Paul Alan ,  MILLAN, David Simon ,  PRICE, David Anthony

IPC分类号： C07J71/00 ,  A61K31/58 ,  C07J7/00 ,  A61P11/06 ,  A61P5/46

CPC分类号： C07J71/0031 ,  A61K45/06 ,  C07J7/008 ,  A61K31/58 ,  A61K2300/00

摘要： This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.

公开(公告)号：EP2220065A2

公开(公告)日：2010-08-25

申请号：EP08794832.9

申请日：2008-07-28

申请人： ENCYSIVE PHARMACEUTICALS, INC.

发明人： ANDERSON, Eric, C. ,  BIEDIGER, Ronald, J. ,  CHEN, Jie ,  DUPRE, Brian ,  LORY, Pedro ,  MARKET, Robert, V. ,  MONK, Keith, A. ,  SAVAGE, Michael, M. ,  TENNYSON, Reginald ,  YOUNG, Brandon, M.

IPC分类号： C07D333/40 ,  C07D333/70 ,  C07D409/12 ,  C07D495/04 ,  A61K31/381

CPC分类号： C07D333/40 ,  C07D333/70 ,  C07D409/12 ,  C07D495/04

摘要： Provided are compounds that are modulators of CCR9 receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, provided are methods for treating or ameliorating diseases associated with modulation of CCR9 receptor activity.

公开(公告)号：EP2200998A1

公开(公告)日：2010-06-30

申请号：EP08830104.9

申请日：2008-09-11

申请人： Wyeth LLC

发明人： ZHOU, Dahui ,  GROSS, Jonathan Laird ,  ROBICHAUD, Albert Jean

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  A61K31/4025 ,  A61K31/435 ,  A61P25/00

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

摘要： The present invention provides a compound of formula (I) and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.

摘要翻译： 本发明提供式（I）化合物及其用于治疗与组胺-3受体相关或受其影响的中枢神经系统疾病的用途。