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公开(公告)号：JP2000038375A
公开(公告)日：2000-02-08
申请号：JP17467899
申请日：1999-06-21
Applicant: MERCK FROSST CANADA INC
Inventor： DUCHARME YVES , GAUTHIER JACQUES Y , PRASIT PETPIBOON , LEBLANC YVES , WANG ZHAOYIN , LEGER SERGE , THERIEN MICHEL
IPC: A61K31/00 , A61K31/10 , A61K31/12 , A61K31/122 , A61K31/341 , A61K31/351 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/4015 , A61K31/426 , A61P1/00 , A61P1/02 , A61P1/04 , A61P7/04 , A61P11/06 , A61P15/00 , A61P17/02 , A61P19/00 , A61P19/02 , A61P21/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/16 , A61P35/00 , A61P43/00 , C07C311/29 , C07C311/46 , C07C311/49 , C07C317/24 , C07D207/26 , C07D207/444 , C07D275/02 , C07D277/02 , C07D277/26 , C07D307/33 , C07D307/38 , C07D307/58 , C07D309/32 , C07D333/18 , C07D333/38 , C07D333/40 , C07D405/04
Abstract: PROBLEM TO BE SOLVED: To obtain a new compound useful in pharmaceutical compositions for treating inflammatory diseases sensitive to the therapies using nonsteroidal anti-inflammatory agents. SOLUTION: This new compound is shown by formula I [X-Y-Z is such as to be CH2CH2CH2, C(O)CH2CH2, S-N=CH, or the like when side (b) is a double bond and side (a) and side (c) are each a single bond, =N-S-CH=, =N-O-CH=, =N-S-N=, or the like when side (a) and side (c) are each a double bond and side (b) is a single bond; R1 is S(O)2CH3, S(O)2NHC(O)CF3, P(O)(CH3)OH, or the like; R2 is a 1-6C alkyl, 3-7C cycloalkyl, trisubstituted phenyl or the like], e.g. 3-[4-(aminosulfonyl)phenyl]-2-(4-fluorophenyl)-5-(2- hydroxy-2-propyl)thiophene. The compound of formula I is obtained, for example, by using a ketone of formula II (Ra is SMe or the like) as starting material to form a compound of formula III (R4 is H or the like).
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公开(公告)号：JP2002069054A
公开(公告)日：2002-03-08
申请号：JP2001123291
申请日：2001-04-20
Applicant: MERCK FROSST CANADA INC
Inventor： DUCHARME YVES , GAUTHIER JACQUES Y , PRASIT PETPIBOON , LEBLANC YVES , WANG ZHAOYIN , LEGER SERGE , THERIEN MICHEL
IPC: A61K31/00 , A61K31/10 , A61K31/12 , A61K31/122 , A61K31/341 , A61K31/351 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/4015 , A61K31/426 , A61P1/00 , A61P1/02 , A61P1/04 , A61P7/04 , A61P11/06 , A61P15/00 , A61P17/02 , A61P19/00 , A61P19/02 , A61P21/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/16 , A61P35/00 , A61P43/00 , C07C311/29 , C07C311/46 , C07C311/49 , C07C317/24 , C07D207/26 , C07D207/444 , C07D275/02 , C07D277/02 , C07D277/26 , C07D307/33 , C07D307/38 , C07D307/58 , C07D309/32 , C07D333/18 , C07D333/38 , C07D333/40 , C07D405/04
Abstract: PROBLEM TO BE SOLVED: To obtain new compounds effective for treating diseases mediated by cyclooxygenase 2, to provide a method for producing the same and to obtain pharmaceutical compositions comprising the compounds. SOLUTION: The new compounds are represented by formulas (1), (2) and (3) The methods for producing the compounds are provided. The pharmaceutical compositions comprise the compounds.
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公开(公告)号：WO9500501A3
公开(公告)日：1995-04-13
申请号：PCT/CA9400318
申请日：1994-06-09
Applicant: MERCK FROSST CANADA INC , DUCHARME YVES , GAUTHIER JACQUES YVES , PRASIT PETPIBOON , LEBLANC YVES , WANG ZHAOYIN , LEGER SERGE , THERIEN MICHEL
Inventor： DUCHARME YVES , GAUTHIER JACQUES YVES , PRASIT PETPIBOON , LEBLANC YVES , WANG ZHAOYIN , LEGER SERGE , THERIEN MICHEL
IPC: C07D333/06 , A61K31/00 , A61K31/10 , A61K31/12 , A61K31/122 , A61K31/18 , A61K31/19 , A61K31/255 , A61K31/34 , A61K31/341 , A61K31/35 , A61K31/351 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/425 , A61K31/426 , A61K31/66 , A61P1/00 , A61P1/02 , A61P1/04 , A61P7/04 , A61P11/06 , A61P15/00 , A61P17/02 , A61P19/00 , A61P19/02 , A61P21/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/16 , A61P35/00 , A61P43/00 , C07C20060101 , C07C13/08 , C07C13/10 , C07C305/18 , C07C307/02 , C07C311/15 , C07C311/16 , C07C311/29 , C07C311/37 , C07C311/46 , C07C311/49 , C07C311/51 , C07C317/10 , C07C317/24 , C07C323/29 , C07D207/26 , C07D207/333 , C07D207/38 , C07D207/444 , C07D207/448 , C07D275/02 , C07D277/02 , C07D277/22 , C07D277/24 , C07D277/26 , C07D307/33 , C07D307/38 , C07D307/58 , C07D309/32 , C07D333/04 , C07D333/12 , C07D333/16 , C07D333/18 , C07D333/24 , C07D333/38 , C07D333/40 , C07D405/04 , C07D407/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D503/04 , C07F9/40 , C07F9/547 , C07F9/572 , C07F9/6506 , C07F9/653 , C07F9/6539 , C07F9/655 , C07D307/02
CPC classification number: C07D275/02 , C07C311/29 , C07C311/46 , C07C311/49 , C07C317/24 , C07C2601/08 , C07D277/26 , C07D307/38 , C07D307/58 , C07D333/18 , C07D333/38 , C07D405/04
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。
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4.发明申请(QUINOLIN-2-YLMETHOXY)INDOLES AS INHIBITORS OF THE BIOSYNTHESIS OF LEUKOTRIENES 审中-公开（QUINOLIN-2-YLMETHOXY）作为紫杉醇生物合成的抑制剂
公开(公告)号：WO9413293A3
公开(公告)日：1994-08-18
申请号：PCT/CA9300527
申请日：1993-12-10
Applicant: MERCK FROSST CANADA INC , PRASIT PETPIBOON , FORTIN REJEAN , HUTCHINSON JOHN H , BELLEY MICHEL L , LEGER SERGE , FRENETTE RICHARD , GILLARD JOHN
Inventor： PRASIT PETPIBOON , FORTIN REJEAN , HUTCHINSON JOHN H , BELLEY MICHEL L , LEGER SERGE , FRENETTE RICHARD , GILLARD JOHN
IPC: A61K31/475 , C07D215/14 , C07D401/12
CPC classification number: C07D401/12 , A61K31/475 , C07D215/14 , Y10S514/826 , Y10S514/914
Abstract: Compounds having 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.
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公开(公告)号：WO0149288A9
公开(公告)日：2001-10-25
申请号：PCT/US0100341
申请日：2001-01-05
Applicant: MERCK FROSST CANADA INC , AXYS PHARM INC , OBALLA RENATA MARCELLA , PRASIT PETPIBOON , ROBICHAUD JOEL STEPHANE , ISABEL ELISE , MENDONCA ROHAN V , VENKATRAMAN SHANKAR , SETTI EDUARDO , WANG DAN XIONG
Inventor： OBALLA RENATA MARCELLA , PRASIT PETPIBOON , ROBICHAUD JOEL STEPHANE , ISABEL ELISE , MENDONCA ROHAN V , VENKATRAMAN SHANKAR , SETTI EDUARDO , WANG DAN-XIONG
IPC: C07D295/08 , A61K31/192 , A61K31/197 , A61K31/275 , A61K31/357 , A61K31/381 , A61K31/40 , A61K31/401 , A61K31/404 , A61K31/415 , A61K31/4172 , A61K31/42 , A61K31/426 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4465 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/505 , A61K31/5375 , A61P1/02 , A61P13/12 , A61P19/02 , A61P19/10 , A61P21/04 , A61P29/00 , A61P33/06 , A61P35/00 , A61P43/00 , C07C255/25 , C07C255/29 , C07C255/41 , C07D207/08 , C07D207/14 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/30 , C07D209/42 , C07D211/34 , C07D213/38 , C07D213/56 , C07D213/61 , C07D213/74 , C07D215/12 , C07D217/12 , C07D231/12 , C07D233/64 , C07D239/26 , C07D239/42 , C07D261/08 , C07D263/22 , C07D265/30 , C07D277/20 , C07D277/30 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/46 , C07D277/48 , C07D277/58 , C07D277/68 , C07D295/14 , C07D295/155 , C07D295/22 , C07D319/16 , C07D319/18 , C07D333/24 , C07D333/34 , C07D417/04 , C07D471/04 , A61K31/405 , A61K31/50 , C07D209/04 , C07D215/00 , C07D217/00 , C07D235/04 , C07D401/00 , C07D405/00 , C07D413/00
CPC classification number: C07D207/08 , C07C255/25 , C07C255/41 , C07C2601/04 , C07C2601/14 , C07C2602/02 , C07D207/14 , C07D209/16 , C07D209/30 , C07D211/34 , C07D213/56 , C07D213/61 , C07D215/12 , C07D239/42 , C07D263/22 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/48 , C07D277/58 , C07D277/68 , C07D295/155 , C07D319/18 , C07D333/34 , C07D417/04 , C07D471/04
Abstract: The present invention relates to novel cysteine protease inhibitors of Formula (I), the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them.
Abstract translation: 本发明涉及式（I）的新型半胱氨酸蛋白酶抑制剂，其药学上可接受的盐和N-氧化物衍生物，它们作为治疗剂的用途及其制备方法。
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Patent Agency Ranking
公开(公告)号：EP1372655A4
公开(公告)日：2005-10-12
申请号：EP02723314
申请日：2002-03-01
Applicant: MERCK FROSST CANADA INC , AXYS PHARM INC
Inventor： PRASIT PETPIBOON , BAYLY CHRISTOPHER IAN , ROBICHAUD JOEL STEPHANE , BLACK W CAMERON , SETTI EDUARDO L , RYDZEWSKI ROBERT M , PALMER JAMES T
IPC: A61K31/275 , A61K31/341 , A61K31/381 , A61K31/401 , A61K31/41 , A61K31/4196 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/506 , A61K45/00 , A61P1/02 , A61P19/02 , A61P19/08 , A61P19/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07C255/29 , C07C323/60 , C07C323/61 , C07C323/62 , C07D207/16 , C07D209/18 , C07D209/42 , C07D211/20 , C07D211/58 , C07D211/60 , C07D215/12 , C07D231/12 , C07D231/18 , C07D231/38 , C07D231/40 , C07D233/54 , C07D239/42 , C07D249/12 , C07D257/04 , C07D257/06 , C07D261/14 , C07D271/08 , C07D275/02 , C07D275/03 , C07D285/06 , C07D295/08 , C07D295/096 , C07D295/12 , C07D295/135 , C07D295/155 , C07D295/205 , C07D307/22 , C07D307/66 , C07D333/28 , C07D333/36 , C07D333/54 , C07D401/04 , C07D409/10 , C07D417/04 , C07D417/10 , C07D487/08 , C07D241/04
CPC classification number: C07D231/12 , C07C255/29 , C07C323/60 , C07C323/61 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/16 , C07D209/42 , C07D211/20 , C07D211/58 , C07D211/60 , C07D215/12 , C07D231/18 , C07D231/38 , C07D233/64 , C07D239/42 , C07D249/12 , C07D257/06 , C07D261/14 , C07D271/08 , C07D275/03 , C07D285/06 , C07D295/096 , C07D295/135 , C07D295/155 , C07D295/205 , C07D307/66 , C07D333/28 , C07D333/36 , C07D333/54 , C07D401/04 , C07D409/10 , C07D417/04 , C07D417/10 , C07D487/08
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公开(公告)号：EP1248612A4
公开(公告)日：2005-09-07
申请号：EP01900903
申请日：2001-01-05
Applicant: MERCK FROSST CANADA INC , AXYS PHARM INC
Inventor： OBALLA RENATA MARCELLA , PRASIT PETPIBOON , ROBICHAUD JOEL STEPHANE , ISABEL ELISE , MENDONCA ROHAN V , VENKATRAMAN SHANKAR , SETTI EDUARDO , WANG DAN-XIONG
IPC: C07D295/08 , A61K31/192 , A61K31/197 , A61K31/275 , A61K31/357 , A61K31/381 , A61K31/40 , A61K31/401 , A61K31/404 , A61K31/415 , A61K31/4172 , A61K31/42 , A61K31/426 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4465 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/505 , A61K31/5375 , A61P1/02 , A61P13/12 , A61P19/02 , A61P19/10 , A61P21/04 , A61P29/00 , A61P33/06 , A61P35/00 , A61P43/00 , C07C255/25 , C07C255/29 , C07C255/41 , C07D207/08 , C07D207/14 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/30 , C07D209/42 , C07D211/34 , C07D213/38 , C07D213/56 , C07D213/61 , C07D213/74 , C07D215/12 , C07D217/12 , C07D231/12 , C07D233/64 , C07D239/26 , C07D239/42 , C07D261/08 , C07D263/22 , C07D265/30 , C07D277/20 , C07D277/30 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/46 , C07D277/48 , C07D277/58 , C07D277/68 , C07D295/14 , C07D295/155 , C07D295/22 , C07D319/16 , C07D319/18 , C07D333/24 , C07D333/34 , C07D417/04 , C07D471/04 , A61K31/405 , A61K31/50 , C07D209/04 , C07D215/00 , C07D217/00 , C07D235/04 , C07D401/00 , C07D405/00 , C07D413/00
CPC classification number: C07D207/08 , C07C255/25 , C07C255/41 , C07C2601/04 , C07C2601/14 , C07C2602/02 , C07D207/14 , C07D209/16 , C07D209/30 , C07D211/34 , C07D213/56 , C07D213/61 , C07D215/12 , C07D239/42 , C07D263/22 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/48 , C07D277/58 , C07D277/68 , C07D295/155 , C07D319/18 , C07D333/34 , C07D417/04 , C07D471/04
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公开(公告)号：EP1272467A4
公开(公告)日：2003-05-07
申请号：EP01930444
申请日：2001-04-04
Applicant: MERCK FROSST CANADA INC , AXYS PHARM INC , BANYU PHARMA CO LTD
Inventor： PRASIT PETPIBOON , FALGUEYRET JEAN-PIERRE , OBALLA RENATA , RYDZEWSKI ROBERT , OKAMOTO OSAMU
IPC: A61K31/397 , A61K31/40 , A61K31/401 , A61K31/4015 , A61K31/4035 , A61K31/4745 , A61P1/02 , A61P3/14 , A61P19/02 , A61P19/08 , A61P19/10 , A61P29/00 , A61P35/02 , A61P43/00 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/26 , C07D207/277 , C07D209/62 , C07D471/04 , A61K31/435 , C07D407/04
CPC classification number: C07D207/08 , C07D205/04 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/277 , C07D209/62 , C07D471/04
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公开(公告)号：CA2439415C
公开(公告)日：2011-09-20
申请号：CA2439415
申请日：2002-03-01
Applicant: MERCK FROSST CANADA INC , AXYS PHARM INC
Inventor： PRASIT PETPIBOON , BAYLY CHRISTOPHER IAN , ROBICHAUD JOEL STEPHANE , BLACK W CAMERON , SETTI EDUARDO L , RYDZEWSKI ROBERT M , PALMER JAMES T
IPC: C07D417/02 , A61K31/275 , A61K31/341 , A61K31/381 , A61K31/401 , A61K31/41 , A61K31/4196 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/506 , A61K38/55 , A61K45/00 , A61K45/06 , A61P1/02 , A61P19/02 , A61P19/08 , A61P19/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07C255/29 , C07C323/60 , C07C323/61 , C07C323/62 , C07D207/16 , C07D209/18 , C07D209/42 , C07D211/20 , C07D211/58 , C07D211/60 , C07D215/12 , C07D231/12 , C07D231/18 , C07D231/38 , C07D231/40 , C07D233/54 , C07D239/42 , C07D249/12 , C07D257/04 , C07D257/06 , C07D261/14 , C07D271/08 , C07D275/02 , C07D275/03 , C07D285/06 , C07D295/04 , C07D295/08 , C07D295/096 , C07D295/12 , C07D295/135 , C07D295/155 , C07D295/205 , C07D307/22 , C07D307/66 , C07D333/28 , C07D333/36 , C07D333/54 , C07D401/02 , C07D401/04 , C07D403/02 , C07D409/02 , C07D409/10 , C07D417/04 , C07D417/10 , C07D487/08
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.
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公开(公告)号：CA2244140C
公开(公告)日：2006-03-21
申请号：CA2244140
申请日：1997-01-29
Applicant: MERCK FROSST CANADA INC
Inventor： BLACK CAMERON , WANG ZHAOYIN , GRIMM ERICH , HUGHES GREGORY , PRASIT PETPIBOON , LEGER SERGE
IPC: C07C317/46 , A61K31/10 , A61K31/18 , A61K31/19 , A61K31/33 , A61K31/495 , C07C311/29 , C07C311/46 , C07C311/51 , C07C313/06 , C07C317/22 , C07C323/64 , C07D295/185 , C07D307/58
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).
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