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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：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：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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5.发明申请DIHYDROPYRROLO[1,2-A]INDOLE AND TETRAHYDROPYRIDO[1,2-A]-INDOLE DERIVATIVES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS 审中-公开作为PROSTAGLANDIN D2受体拮抗剂的二氢吲哚并[1,2-A]吲哚和四氢呋喃并[1,2-A] - 衍生物
公开(公告)号：WO02094830A8
公开(公告)日：2003-04-10
申请号：PCT/CA0200745
申请日：2002-05-22
Applicant: MERCK FROSST CANADA INC , WANG ZHAOYIN , BEAULIEU CHRISTIAN , DUFRESNE CLAUDE , GUAY DANIEL , LEBLANC YVES
Inventor： WANG ZHAOYIN , BEAULIEU CHRISTIAN , DUFRESNE CLAUDE , GUAY DANIEL , LEBLANC YVES
IPC: A61K31/407 , A61K31/41 , A61K31/4155 , A61K31/437 , A61K45/00 , A61P11/06 , A61P27/16 , A61P37/00 , A61P37/08 , A61P43/00 , C07D471/04 , C07D487/04 , C07D497/16
CPC classification number: C07D471/04 , C07D487/04
Abstract: Dihydropyrroloindoles and tetrahydropyridoindoles are prostaglandin receptor antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma.
Abstract translation: 二氢吡咯并吲哚和四氢吡啶并吲哚是用于治疗前列腺素介导的疾病如过敏性鼻炎，鼻塞和哮喘的前列腺素受体拮抗剂。
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Patent Agency Ranking6.发明申请DIHYDROPYRROLO[1,2-A]INDOLE AND TETRAHYDROPYRIDO[1,2-a]-INDOLE DERIVATIVES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS 审中-公开二氢吲哚并[1,2-A]吲哚和四氢呋喃并[1,2-a] - 衍生物作为PROSTAGLANDIN D2受体拮抗剂
公开(公告)号：WO02094830A3
公开(公告)日：2003-03-06
申请号：PCT/CA0200745
申请日：2002-05-22
Applicant: MERCK FROSST CANADA INC , WANG ZHAOYIN , BEAULIEU CHRISTIAN , DUFRESNE CLAUDE , GUAY DANIEL , LEBLANC YVES
Inventor： WANG ZHAOYIN , BEAULIEU CHRISTIAN , DUFRESNE CLAUDE , GUAY DANIEL , LEBLANC YVES
IPC: A61K31/407 , A61K31/41 , A61K31/4155 , A61K31/437 , A61K45/00 , A61P11/06 , A61P27/16 , A61P37/00 , A61P37/08 , A61P43/00 , C07D471/04 , C07D487/04 , C07D497/16
CPC classification number: C07D471/04 , C07D487/04
Abstract: Dihydropyrroloindoles and tetrahydropyridoindoles are prostaglandin receptor antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma.
Abstract translation: 二氢吡咯并吲哚和四氢吡啶并吲哚是用于治疗前列腺素介导的疾病如过敏性鼻炎，鼻塞和哮喘的前列腺素受体拮抗剂。
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公开(公告)号：CA2503767C
公开(公告)日：2009-09-22
申请号：CA2503767
申请日：2003-10-28
Applicant: MERCK FROSST CANADA INC
Inventor： LEBLANC YVES , ROY PATRICK , DUFRESNE CLAUDE
IPC: C07D471/14 , A61K31/4375 , A61K31/4745 , A61P11/00 , A61P29/00
Abstract: Pyridopyrrolizine and pyridoindolizine derivatives are prostaglandin recepto r antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma.
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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：BR0315681A
公开(公告)日：2005-09-06
申请号：BR0315681
申请日：2003-10-28
Applicant: MERCK FROSST CANADA INC
Inventor： LEBLANC YVES , DUFRESNE CLAUDE , ROY PATRICK
IPC: A61K31/4745 , A61P11/00 , A61P29/00 , C07D471/14 , A61K31/4375
Abstract: Pyridopyrrolizine and pyridoindolizine derivatives are prostaglandin receptor antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma.
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公开(公告)号：NO20052591A
公开(公告)日：2005-07-29
申请号：NO20052591
申请日：2005-05-27
Applicant: MERCK FROSST CANADA INC
Inventor： LEBLANC YVES , ROY PATRICK , DUFRESNE CLAUDE
IPC: A61K31/4745 , A61P11/00 , A61P29/00 , C07D471/14 , A61K31/4375
CPC classification number: C07D471/14
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