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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：JP2001199954A
公开(公告)日：2001-07-24
申请号：JP2000366579
申请日：2000-12-01
Applicant: MERCK FROSST CANADA INC
Inventor： BELLEY MICHEL , GAUTHIER JACQUES Y , ERICH GRIMM , LEBLANC YVES , CHUNG-SING LI , THERIEN MICHEL , BLACK CAMERON , CHEUK-KUN LAU , PETPIBOON PRASIT , ROY PATRICK
IPC: C07D333/06 , A61K31/12 , A61K31/122 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/404 , A61K31/4184 , A61K31/4196 , A61K31/425 , A61K31/429 , A61K31/433 , A61K31/435 , A61K31/4355 , A61K31/437 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/4709 , A61K31/505 , A61K31/506 , A61K31/54 , A61P25/04 , A61P29/00 , A61P43/00 , C07C317/24 , C07D213/64 , C07D307/58 , C07D307/60 , C07D307/62 , C07D307/64 , C07D307/66 , C07D307/68 , C07D307/83 , C07D307/94 , C07D333/26 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04
Abstract: PROBLEM TO BE SOLVED: To provide a new compound useful for treating cyclooxygenase-2- mediated diseases. SOLUTION: The compound represented by formula (I), and the medicinal composition for treating cyclooxygenase-2-mediated diseases, such as inflammatory diseases. Concretely, the compound of formula (II) is exemplified.
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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：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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公开(公告)号：EP1482924A4
公开(公告)日：2006-03-08
申请号：EP03716238
申请日：2003-02-28
Applicant: MERCK FROSST CANADA INC , AXYS PHARM INC
Inventor： BAYLY CHRISTOPHER I , BLACK CAMERON , LEGER SERGE , LI CHUN SING , MCKAY DAN , MELLON CHRISTOPHE , GAUTHIER JACQUES YVES , LAU CHEUK , THERIEN MICHEL , TRUONG VOUY-LINH , GREEN MICHAEL J , HIRSCHBEIN BERNARD L , JANC JAMES W , PALMER JAMES T , BASKARAN CHITRA
IPC: A61K31/275 , C07D295/12 , A61K31/381 , A61K31/404 , A61K31/417 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/4465 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/5375 , A61K45/00 , A61P1/02 , A61P3/14 , A61P19/00 , A61P19/02 , A61P19/08 , A61P19/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07C255/25 , C07C255/29 , C07C255/46 , C07C255/58 , C07C255/60 , C07C259/10 , C07C311/37 , C07C317/32 , C07C317/36 , C07D209/08 , C07D211/26 , C07D211/38 , C07D213/36 , C07D213/38 , C07D213/57 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/89 , C07D215/12 , C07D231/12 , C07D233/54 , C07D233/64 , C07D239/06 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D295/135 , C07D295/22 , C07D307/52 , C07D333/20 , C07D401/04 , C07D417/04
CPC classification number: C07C237/20 , A61K31/165 , A61K31/18 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4418 , A61K31/495 , C07C255/25 , C07C255/29 , C07C255/46 , C07C255/58 , C07C259/10 , C07C311/37 , C07C317/32 , C07C2601/02 , C07C2601/14 , C07D209/08 , C07D213/38 , C07D213/57 , C07D213/64 , C07D213/70 , C07D213/89 , C07D215/12 , C07D231/12 , C07D233/64 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D277/30 , C07D295/135 , C07D295/155 , C07D307/52 , C07D333/20 , C07D401/04 , C07D417/04
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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Patent Agency Ranking
公开(公告)号：CZ295764B6
公开(公告)日：2005-10-12
申请号：CZ110198
申请日：1996-10-09
Applicant: MERCK FROSST CANADA INC
Inventor： BELLEY MICHEL , GAUTHIER JACQUES Y , GRIMM ERICH , LEBLANC YVES , LI CHUNG-SING , THERIEN MICHEL , BLACK CAMERON , LAU CHEUK-KUN , PRASIT PETPIBOON , ROY PATRICK
IPC: C07D333/06 , A61K31/12 , A61K31/122 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/404 , A61K31/4184 , A61K31/4196 , A61K31/425 , A61K31/429 , A61K31/433 , A61K31/435 , A61K31/4355 , A61K31/437 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/4709 , A61K31/505 , A61K31/506 , A61K31/54 , A61P25/04 , A61P29/00 , A61P43/00 , C07C317/24 , C07D213/64 , C07D307/58 , C07D307/60 , C07D307/62 , C07D307/64 , C07D307/66 , C07D307/68 , C07D307/83 , C07D307/94 , C07D333/26 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04 , A61K31/365 , A61K31/58
Abstract: The present invention relates to (Methylsulfonyl)phenyl-2-(5h)-furanone derivatives of the general formula I, in which the individual general symbols are as specified in the main Claim, wherein these derivatives are effective inhibitors of cyclooxygenase, exhibit antiphlogistic activity and therefore they can be used for the preparation of a pharmaceutical composition forming a part of the present invention, too and having the above-indicated effect.
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公开(公告)号：DE122005000010I1
公开(公告)日：2005-06-23
申请号：DE122005000010
申请日：1996-10-09
Applicant: MERCK FROSST CANADA INC
Inventor： BELLEY MICHEL , GAUTHIER JACQUES Y , GRIMM ERICH , LEBLANC YVES , LI CHUNG SING , THERIEN MICHEL , BLACK CAMERON , LAU CHEUK KUN , PRASIT PETPIBOON , ROY PATRICK
IPC: C07D333/06 , A61K31/12 , A61K31/122 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/404 , A61K31/4184 , A61K31/4196 , A61K31/425 , A61K31/429 , A61K31/433 , A61K31/435 , A61K31/4355 , A61K31/437 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/4709 , A61K31/505 , A61K31/506 , A61K31/54 , A61P25/04 , A61P29/00 , A61P43/00 , C07C317/24 , C07D213/64 , C07D307/58 , C07D307/60 , C07D307/62 , C07D307/64 , C07D307/66 , C07D307/68 , C07D307/83 , C07D307/94 , C07D333/26 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04
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).
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公开(公告)号：MA27295A1
公开(公告)日：2005-05-02
申请号：MA27826
申请日：2004-08-17
Applicant: MERCK FROSST CANADA INC , AXYS PHARM INC
Inventor： BASKARAN CHITRA , BLACK CAMERON , GREEN MICHAEL J , JANC JAMES W , LEGER SERGE , MCKAY DAN , PALMER JAMES T , TRUONG VOUY-LINH , BAYLY CHRISTOPHER I , GAUTHIER JACQUES YVES , HIRSCHBEIN BERNARD L , LAU CHEUK , LI CHUN SING , MELLON CHRISTOPHE , THERIEN MICHEL
IPC: C07D295/12 , A61K31/275 , A61K31/381 , A61K31/404 , A61K31/417 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/4465 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/5375 , A61K45/00 , A61P1/02 , A61P3/14 , A61P19/02 , A61P19/08 , A61P19/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07C255/25 , C07C255/29 , C07C255/46 , C07C255/58 , C07C255/60 , C07C259/10 , C07C311/37 , C07C317/32 , C07C317/36 , C07D209/08 , C07D211/26 , C07D211/38 , C07D213/36 , C07D213/38 , C07D213/57 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/89 , C07D215/12 , C07D231/12 , C07D233/54 , C07D233/64 , C07D239/06 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D295/135 , C07D295/22 , C07D307/52 , C07D333/20 , C07D401/04 , C07D417/04 , A61K
Abstract: Cette invention concerne une nouvelle classe de composés qui sont des inhibiteurs de cystéines protéases, y compris mais sans y être limités, des inhibiteurs des cathepsines K, L, S et B. Ces composés sont utiles pour traiter des maladies dans lesquelles l'inhibition de la résorption osseuse est indiquée, telles que l'ostéoporose.
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公开(公告)号：BR0308208A
公开(公告)日：2005-01-11
申请号：BR0308208
申请日：2003-02-28
Applicant: MERCK FROSST CANADA INC , AXYS PHARM INC
Inventor： BAYLY CHRISTOPHER I , BLACK CAMERON , LEGER SERGE , LI CHUN SING , MCKAY DAN , MELLON CHRISTOPHE , GAUTHIER JACQUES YVES , LAU CHEUK , THERIEN MICHEL , TRUONG VOUY-LINH , GREEN MICHAEL J , HIRSCHBEIN BERNARD L , JANC JAMES W , PALMER JAMES T , BASKARAN CHITRA
IPC: C07D295/12 , A61K31/275 , A61K31/381 , A61K31/404 , A61K31/417 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/4465 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/5375 , A61K45/00 , A61P1/02 , A61P3/14 , A61P19/02 , A61P19/08 , A61P19/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07C255/25 , C07C255/29 , C07C255/46 , C07C255/58 , C07C255/60 , C07C259/10 , C07C311/37 , C07C317/32 , C07C317/36 , C07D209/08 , C07D211/26 , C07D211/38 , C07D213/36 , C07D213/38 , C07D213/57 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/89 , C07D215/12 , C07D231/12 , C07D233/54 , C07D233/64 , C07D239/06 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D295/135 , C07D295/22 , C07D307/52 , C07D333/20 , C07D401/04 , C07D417/04
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：SK284114B6
公开(公告)日：2004-09-08
申请号：SK150295
申请日：1994-06-09
Applicant: MERCK FROSST CANADA INC
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
Abstract: In the present invention there are disclosed phenyl heterocyclic derivatives of the general formula (I), in which R1 represents the group SO2CH3 or the group SO2NH2, R2 represents a mono- or disubstituted phenyl and substituents are selected from a group comprising methyl, methoxy, a hydrogen, fluorine, chlorine or bromine atom. The derivatives are inhibitors of cyclooxygenase-2 and they are therefore suitable for treating diseases mediated by the action of this enzyme. The present invention also relates to pharmaceutical preparations containing these derivatives, use of such derivatives for preparing pharmaceutical preparations exhibiting non-steroidal antiphlogistic activity as well as processes for preparing the derivatives of the general formula (I).
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