公开(公告)号：CA2079373C

公开(公告)日：2003-08-05

申请号：CA2079373

申请日：1992-09-29

Applicant: PRASIT PETPIBOON ,  HUTCHINSON JOHN H ,  THERIEN MICHEL ,  GILLARD JOHN W ,  FRENETTE RICHARD

Inventor： PRASIT PETPIBOON ,  HUTCHINSON JOHN H ,  THERIEN MICHEL ,  GILLARD JOHN W ,  FRENETTE RICHARD

IPC: A61K31/405 ,  A61K31/415 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: Compounds having the formula I: (see formula I) are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti- allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.

公开(公告)号：WO2011049979A2

公开(公告)日：2011-04-28

申请号：PCT/US2010/053245

申请日：2010-10-19

Applicant: AMIRA PHARMACEUTICALS, INC. ,  HUTCHINSON, John, Howard ,  PRASIT, Petpiboon, Peppi ,  DEARMOND, Isabelle, Marguerite

Inventor： HUTCHINSON, John, Howard ,  PRASIT, Petpiboon, Peppi ,  DEARMOND, Isabelle, Marguerite

IPC: A61K31/4709 ,  A61K31/44 ,  A61K31/404 ,  A61K31/40 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00

CPC classification number: A61K31/00 ,  A61K9/0019 ,  A61K31/40 ,  A61K31/404 ,  A61K31/44 ,  A61K31/4709 ,  A61K45/06 ,  A61K47/34 ,  A61K47/36 ,  A61K2300/00

Abstract: Described herein are injectable formulations for intra-articular or peri-articular administration, wherein the formulation is administered to treat joint pain. An injectable formulation for intra-articular or peri-articular administration disclosed herein comprises a therapeutically-effective amount of a leukotriene synthesis inhibitor compound formulated for intra-articular or peri-articular administration.

Abstract translation: 本文描述了用于关节内或关节周围给药的可注射制剂，其中施用该制剂以治疗关节疼痛。 本文公开的关节内或周围关节内给药的可注射制剂包含治疗有效量的配制用于关节内或关节周围给药的白细胞三烯合成抑制剂化合物。

公开(公告)号：WO2005054193A1

公开(公告)日：2005-06-16

申请号：PCT/GB2004/004985

申请日：2004-11-25

Applicant: MERCK & CO. INC. ,  MERCK SHARP & DOHME LIMITED ,  BEHER, Dirk ,  BETTATI, Michela ,  CHURCHER, Ian ,  MUNZO, Benito ,  PRASIT, Petpiboon ,  QUDDUS, Abdul ,  STOCK, Nicholas, S. ,  WRIGLEY, Jonathan, D. J.

Inventor： BEHER, Dirk ,  BETTATI, Michela ,  CHURCHER, Ian ,  MUNZO, Benito ,  PRASIT, Petpiboon ,  QUDDUS, Abdul ,  STOCK, Nicholas, S. ,  WRIGLEY, Jonathan, D. J.

IPC: C07D209/30

CPC classification number: C07D417/12 ,  A61K31/405 ,  C07D209/30 ,  C07D209/36 ,  C07D403/12

Abstract: Compounds of formula (I): modulate the activity of Υ -secretase, and hence find use in treatment or prevention of Alzheimer's disease and related conditions.

Abstract translation: 式（I）化合物：调节Upsilon分泌酶的活性，因此可用于治疗或预防阿尔茨海默病和相关病症。

公开(公告)号：WO2003051315A3

公开(公告)日：2003-06-26

申请号：PCT/US2002/041720

申请日：2002-12-13

Applicant: MERCK & CO., INC. ,  COSFORD, Nicholas, D., P. ,  TEHRANI, Lida, R. ,  ROPPE, Jeffrey, R. ,  SMITH, Nicholas, D. ,  PRASIT, Petpiboon

Inventor： COSFORD, Nicholas, D., P. ,  TEHRANI, Lida, R. ,  ROPPE, Jeffrey, R. ,  SMITH, Nicholas, D. ,  PRASIT, Petpiboon

IPC: C07D401/04

Abstract: Triazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl which are metabotropic glutamate receptor - subtype 5 ("mGluR5") modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal and other diseases.

公开(公告)号：WO2002069901A3

公开(公告)日：2002-09-12

申请号：PCT/US2002/006533

申请日：2002-03-01

Applicant: MERCK FROSST CANADA & CO. ,  AXYS PHARMACEUTICALS, INC. ,  PRASIT, Petpiboon ,  BAYLY, Christopher Ian ,  ROBICHAUD, Joel Stephane ,  BLACK, W. Cameron ,  SETTI, Eduardo, L. ,  RYDZEWSKI, Robert, M. ,  PALMER, James, T.

Inventor： PRASIT, Petpiboon ,  BAYLY, Christopher Ian ,  ROBICHAUD, Joel Stephane ,  BLACK, W. Cameron ,  SETTI, Eduardo, L. ,  RYDZEWSKI, Robert, M. ,  PALMER, James, T.

IPC: A61K31/496

Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

公开(公告)号：WO1997028121A1

公开(公告)日：1997-08-07

申请号：PCT/CA1997000058

申请日：1997-01-29

Applicant: MERCK FROSST CANADA INC. ,  BLACK, Cameron ,  GRIMM, Erich ,  HUGHES, Greg ,  LEGER, Serge ,  PRASIT, Petpiboon ,  WANG, Zhaoyin

Inventor： MERCK FROSST CANADA INC.

IPC: C07C317/46

CPC classification number: C07D405/12 ,  C07C317/22 ,  C07C317/24 ,  C07C317/44 ,  C07C317/46 ,  C07D307/58 ,  C07D307/60 ,  C07D307/64 ,  C07D307/66 ,  C07D307/94

Abstract: The invention encompasses the novel compound of formula (I) useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of formula (I).

Abstract translation: 本发明包括可用于治疗环氧合酶-2介导的疾病的新颖的式（I）化合物。 本发明还包括用于治疗包含式（I）化合物的环加氧酶-2介导的疾病的某些药物组合物。

公开(公告)号：WO1996019469A1

公开(公告)日：1996-06-27

申请号：PCT/CA1995000715

申请日：1995-12-18

Applicant: MERCK FROSST CANADA INC. ,  BLACK, Cameron ,  GRIMM, Erich ,  LEGER, Serge ,  PRASIT, Petpiboon ,  WANG, Zhaoyin

Inventor： MERCK FROSST CANADA INC.

IPC: C07D307/58

CPC classification number: C07D307/79 ,  C07C317/24 ,  C07D307/58 ,  C07D307/83 ,  C07D307/94 ,  C07D333/32 ,  C07D333/78 ,  C07D405/04 ,  C07D407/04 ,  C07D409/04 ,  C07D417/04 ,  C07D417/14 ,  C07D491/10 ,  C07D493/10 ,  C07D495/10 ,  C07F9/5325 ,  C07F9/65515

Abstract: The invention encompasses the novel compound of Formula (I) as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula (I). The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula (I).

Abstract translation: 本发明包括式（I）的新化合物以及治疗环加氧酶-2介导的疾病的方法，其包括向需要这种治疗无效治疗有效量的式（I）的化合物的患者施用。 本发明还包括用于治疗包含式（I）化合物的环氧合酶-2介导的疾病的某些药物组合物。

公开(公告)号：WO2007056220A2

公开(公告)日：2007-05-18

申请号：PCT/US2006/043095

申请日：2006-11-03

Applicant: AMIRA PHARMACEUTICALS, INC. ,  HUTCHINSON, John, H. ,  PRASIT, Petpiboon, Peppi ,  MORAN, Mark ,  EVANS, Jillian, F. ,  LI, Yiwei ,  ZUNIC, Jasmine, Eleanor ,  HADDACH, Mustapha ,  STOCK, Nicholas, Simon

Inventor： HUTCHINSON, John, H. ,  PRASIT, Petpiboon, Peppi ,  MORAN, Mark ,  EVANS, Jillian, F. ,  LI, Yiwei ,  ZUNIC, Jasmine, Eleanor ,  HADDACH, Mustapha ,  STOCK, Nicholas, Simon

IPC: A61K31/501 ,  A61K31/497 ,  A61K31/4439 ,  A61K31/427 ,  C07D417/02 ,  C07D403/02

CPC classification number: C07D401/10 ,  C07D401/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.

公开(公告)号：WO2006055404A2

公开(公告)日：2006-05-26

申请号：PCT/US2005040851

申请日：2005-11-10

Applicant: MERCK & CO INC ,  MUNOZ BENITO ,  PAYNE JOSEPH E ,  PRASIT PETPIBOON ,  REGER THOMAS S ,  SMITH NICHOLAS D ,  STOCK NICHOLAS S ,  MCGUIRE ANGELA R

Inventor： MUNOZ BENITO ,  PAYNE JOSEPH E ,  PRASIT PETPIBOON ,  REGER THOMAS S ,  SMITH NICHOLAS D ,  STOCK NICHOLAS S ,  MCGUIRE ANGELA R

IPC: A61K31/4745

CPC classification number: C07C69/24 ,  C07C53/128 ,  C07C257/14 ,  C07C317/46 ,  C07D217/02 ,  C07D311/80

Abstract: Disclosed are compounds for treating stroke, and pharmaceutical compositions comprising them, which may be effective in modulating multiple events in the biochemical cascade of stroke. Also disclosed are methods of treating patients who have had a stroke, or are at risk of stroke, by administering the compounds or compositions of the invention.

Abstract translation: 公开了用于治疗中风的化合物和包含它们的药物组合物，其可以有效调节中风的生物化学级联中的多个事件。 还公开了通过施用本发明的化合物或组合物来治疗患有中风或有中风风险的患者的方法。

公开(公告)号：WO2004064771A2

公开(公告)日：2004-08-05

申请号：PCT/US2004/000424

申请日：2004-01-09

Applicant: MERCK & CO., INC. ,  MUNOZ, Benito ,  PRASIT, Petpiboon ,  STOCK, Nicholas Simon

Inventor： MUNOZ, Benito ,  PRASIT, Petpiboon ,  STOCK, Nicholas Simon

IPC: A61K

CPC classification number: C07D257/04 ,  C07C57/30 ,  C07C57/58 ,  C07C59/68 ,  C07D207/20 ,  C07D209/26 ,  C07D209/28 ,  C07D209/46 ,  C07D209/48 ,  C07D209/86 ,  C07D209/88 ,  C07D263/57 ,  C07D333/22 ,  C07D333/24 ,  C07D337/14

Abstract: The present invention encompasses compounds of Formula I (I) or pharmaceutically acceptable salts thereof, wherein A is the base molecule of a propionic acid or acetic acid NSAID, or a derivative thereof, X is -CO 2 H, 1 H -tetrazol-5-yl or 2 H -tetrazol-5-yl and R 1 and R 2 are each independently selected from the group consisting of: C 1 - 6 alkyl and C 3 - 6 cycloalkyl, as well as pharmaceutical composition comprising said compounds and methods of using said compounds. The compounds of the present invention lower the level of Aß 42 and are therefore useful for preventing, delaying or reversing the progression of Alzheimer s Disease.

Abstract translation: 本发明包括式I（I）的化合物或其药学上可接受的盐，其中A是丙酸或乙酸NSAID或其衍生物的基础分子，X是-CO 2 H，1H-四唑-5-基或 2H-四唑-5-基和R 1和R 2各自独立地选自：C 1-6烷基和C 3-6环烷基，以及包含所述化合物的药物组合物和使用所述化合物的方法。 本发明的化合物降低Aβ42的水平，因此可用于预防，延缓或逆转阿尔茨海默病的进展。