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1. 发明申请

WO0068198A2 HETEROSUBSTITUTED PYRIDINE DERIVATIVES AS PDE 4 INHIBITORS 审中-公开
标题翻译：作为PDE 4抑制剂的异源化吡啶衍生物
公开(公告)号：WO0068198A2
公开(公告)日：2000-11-16
申请号：PCT/CA0000500
申请日：2000-05-03
申请人： MERCK FROSST CANADA INC , COTE BERNARD , FRIESEN RICHARD , FRENETTE RICHARD , GIRARD MARIO , GIRARD YVES , GODBOUT CEDRICKX , GUAY DANIEL , HAMEL PIERRE , BLOUIN MARC , DUCHARME YVES , PRESCOTT SYLVIE
发明人： COTE BERNARD , FRIESEN RICHARD , FRENETTE RICHARD , GIRARD MARIO , GIRARD YVES , GODBOUT CEDRICKX , GUAY DANIEL , HAMEL PIERRE , BLOUIN MARC , DUCHARME YVES , PRESCOTT SYLVIE
IPC分类号： A61K31/444 , A61K31/4725 , A61P1/04 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/02 , A61P25/24 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D213/74 , C07D213/76 , C07D213/79 , C07D213/89 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , A61K31/4427
CPC分类号： C07D213/74 , C07D213/76 , C07D213/79 , C07D213/89 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The invention encompasses the novel compound of Formula (I) useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE 4) or a pharmaceutically acceptable salt or hydrate thereof. The invention also encompasses pharmaceutical compositions and methods for treatment.
摘要翻译：本发明包括通过通过抑制磷酸二酯酶IV（PDE 4）或通过增加环腺苷-3'，5'-单磷酸（cAMP）的水平而可用于治疗疾病，包括哮喘的式（I）的新化合物或其药学上可接受的盐或水合物。本发明还包括用于治疗的药物组合物和方法。

2. 发明申请

WO0170738A3 TRI-ARYL-SUBSTITUTED-ETHANE PDE4 INHIBITORS 审中-公开
标题翻译：三苯乙烯替代 - 乙烷PDE4抑制剂
公开(公告)号：WO0170738A3
公开(公告)日：2002-08-01
申请号：PCT/CA0100365
申请日：2001-03-19
申请人： MERCK FROSST CANADA INC , FRIESEN RICHARD , DUCHARME YVES , COTE BERNARD , BLOUIN MARC , MARTINS EVELYN , GUAY DANIEL , HAMEL PIERRE , GIRARD MARIO , FRENETTE RICHARD , LALIBERTE SEBASTIEN
发明人： FRIESEN RICHARD , DUCHARME YVES , COTE BERNARD , BLOUIN MARC , MARTINS EVELYN , GUAY DANIEL , HAMEL PIERRE , GIRARD MARIO , FRENETTE RICHARD , LALIBERTE SEBASTIEN
IPC分类号： C07D417/04 , A61K31/4439 , A61K31/444 , A61K45/00 , A61P1/00 , A61P1/04 , A61P3/10 , A61P3/12 , A61P7/00 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P11/08 , A61P11/14 , A61P13/02 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/04 , A61P25/24 , A61P25/28 , A61P27/14 , A61P29/00 , A61P29/02 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/08 , A61P39/02 , A61P43/00 , C07D417/06 , C07D417/14 , C07D417/08 , A61K31/427
CPC分类号： C07D417/06
摘要： Novel ethanes substituted with i) a phenyl, ii) a thiazole, and iii) a pyridyl moiety are PDE4 inhibitors.
摘要翻译：用I）苯基取代的新型乙烷，ii）噻唑，和iii）吡啶基部分是PDE4抑制剂。

3. 发明申请

WO0064874A3 HETEROSUBSTITUTED PYRIDINE DERIVATIVES AS PDE 4 INHIBITORS 审中-公开
标题翻译：作为PDE 4抑制剂的异源化吡啶衍生物
公开(公告)号：WO0064874A3
公开(公告)日：2001-02-15
申请号：PCT/CA0000427
申请日：2000-04-19
申请人： MERCK FROSST CANADA INC , FRENETTE RICHARD , FRIESEN RICHARD , GIRARD MARIO , GIRARD YVES , GODBOUT CEDRICKX , GUAY DANIEL , HAMEL PIERRE , PERRIER HELENE
发明人： FRENETTE RICHARD , FRIESEN RICHARD , GIRARD MARIO , GIRARD YVES , GODBOUT CEDRICKX , GUAY DANIEL , HAMEL PIERRE , PERRIER HELENE
IPC分类号： A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D213/64 , C07D213/76 , C07D213/79 , C07D213/89 , C07D405/14 , C07D409/14 , C07D417/14 , A61K31/4427
CPC分类号： C07D213/64 , C07D213/76 , C07D213/79 , C07D213/89 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The invention encompasses the novel compound of Formula (I) useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE 4). The invention also encompasses pharmaceutical compositions and methods for treatment.
摘要翻译：本发明包括通过抑制磷酸二酯酶IV（PDE4）提高环腺苷-3'，5'-单磷酸（cAMP）的水平，可用于治疗包括哮喘在内的疾病的式（I）化合物。本发明还包括用于治疗的药物组合物和方法。

6. 发明申请

WO9413293A3 (QUINOLIN-2-YLMETHOXY)INDOLES AS INHIBITORS OF THE BIOSYNTHESIS OF LEUKOTRIENES 审中-公开
标题翻译：（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
申请人： MERCK FROSST CANADA INC , PRASIT PETPIBOON , FORTIN REJEAN , HUTCHINSON JOHN H , BELLEY MICHEL L , LEGER SERGE , FRENETTE RICHARD , GILLARD JOHN
发明人： PRASIT PETPIBOON , FORTIN REJEAN , HUTCHINSON JOHN H , BELLEY MICHEL L , LEGER SERGE , FRENETTE RICHARD , GILLARD JOHN
IPC分类号： A61K31/475 , C07D215/14 , C07D401/12
CPC分类号： C07D401/12 , A61K31/475 , C07D215/14 , Y10S514/826 , Y10S514/914
摘要： 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.

7. 发明申请

WO2005009951A3 DIPHENYL SUBSTITUTED CYCLOALKANES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：二苯基取代的环状化合物，含有这些化合物的组合物和使用方法
公开(公告)号：WO2005009951A3
公开(公告)日：2005-12-08
申请号：PCT/US2004023334
申请日：2004-07-20
申请人： MERCK & CO INC , MERCK FROSST CANADA LTD , CHU LIN , GOULET MARK T , UJJAINWALLA FEROZE , FRENETTE RICHARD , GIRARD YVES , THERIEN MICHEL , MACDONALD DWIGHT , HUTCHINSON JOHN H , CHANG LINDA
发明人： CHU LIN , GOULET MARK T , UJJAINWALLA FEROZE , FRENETTE RICHARD , GIRARD YVES , THERIEN MICHEL , MACDONALD DWIGHT , HUTCHINSON JOHN H , CHANG LINDA
IPC分类号： A61K31/535 , C07D20060101 , C07D221/02 , C07D231/02 , C07D263/02
CPC分类号： C07D215/14 , C07D215/12 , C07D237/28 , C07D277/64 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/02
摘要： The instant invention provides compounds of formula: (I) which are 5-lipoxygenase activating protein inhibitors: formula (I). Compounds of formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
摘要翻译：本发明提供了式（I）化合物，它们是5-脂氧合酶活化蛋白抑制剂：式（I）。式（I）化合物可用作抗动脉粥样硬化剂，抗哮喘剂，抗过敏剂，抗炎剂和细胞保护剂。

8. 发明公开

EP0206741A2 Leukotriene antagonists. 失效
标题翻译： Leukotrienantagonisten。
公开(公告)号：EP0206741A2
公开(公告)日：1986-12-30
申请号：EP86304665
申请日：1986-06-17
申请人： MERCK FROSST CANADA INC
发明人： YOUNG ROBERT N , FRENETTE RICHARD , GAUTHIER JACQUES-YVES
IPC分类号： C07D333/34 , A61K31/11 , A61K31/12 , A61K31/135 , A61K31/165 , A61K31/17 , A61K31/19 , A61K31/195 , A61K31/255 , A61K31/275 , A61K38/00 , A61K45/06 , A61P1/16 , A61P3/00 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C47/52 , C07C49/84 , C07C59/64 , C07D207/456 , C07D209/10 , C07D213/89 , C07D215/16 , C07D215/22 , C07D257/04 , C07D275/06 , C07D285/08 , C07D285/10 , C07D307/78 , C07D311/08 , C07D311/24 , C07D521/00 , C07K5/06 , A61K31/35 , A61K31/41 , C07C149/273 , C07C149/40 , C07C149/42
CPC分类号： C07D257/04 , A61K38/00 , C07C323/00 , C07D311/24 , C07K5/0606
摘要： Compounds having the formula: are antagonists of leukotrienes of C4, D4 and E4, the slow reacting substance of anaphylaxis, and inhibitors of their biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory agents, anti-psoriatic agents, and cytoprotective agents, and can be made up into pharmaceutical compositions.
摘要翻译：具有下式的化合物：是C4，D4和E4的白细胞三烯的拮抗剂，过敏反应的缓慢反应物质及其生物合成的抑制剂。这些化合物可用作抗哮喘，抗过敏，抗炎药，抗牛皮癣药和细胞保护剂，并且可以制成药物组合物。

9. 发明公开

EP0206751A2 2-Substituted quinolines, their preparation and use. 失效
标题翻译： 2-Substituierte Chinoline，ihre Herstellung und Verwendung。
公开(公告)号：EP0206751A2
公开(公告)日：1986-12-30
申请号：EP86304686
申请日：1986-06-17
申请人： MERCK FROSST CANADA INC
发明人： YOUNG ROBERT N , LEGER SERGE , FRENETTE RICHARD , ZAMBONI ROBERT , WILLIAMS HAYDEN W R
IPC分类号： A61K31/47 , A61P9/00 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D215/12 , C07D215/14 , C07D215/16 , C07D215/18 , C07D215/36 , C07D401/12
CPC分类号： C07D401/12 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/36
摘要： Compounds having the formula: are selective antagonists of leukotrienes of D4. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents and may be made up into pharmaceutical compositions. In the formula R is H, halogen, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, -CF3, -OR , -SR , -NR R , -CHO, -COOR , -(C=0)R , -C(OH)R R , -CN, -NO2, substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, or substituted or unsubstituted phenethyl; R is H, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, -CF3, substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, or substituted or unsubstituted phenethyl; R is -(A)m-(CR =CR )p-(CR R )m-Q; R is H, halogen, -NO2, -CN, -OR , -SR , NR R , or C1-C8 alkyl; R is H or C1-C4 alkyl; R is A) a monocyclic or bicyclic heterocyclic radical containing from 3 to 12 nuclear carbon atoms and 1 or 2 nuclear heteroatoms selected from N and S with at least one being N, and with each ring in the heterocyclic radical being formed of 5 or 6 atoms, or B) the radical W-R ; R contains up to 21 carbon atoms and is (1) a hydrocarbon radical or (2) an acyl radical of an organic acyclic or monocyclic carboxylic acid containing not more than 1 heteroatom in the ring; R is -OR , -SR , or NR R ; R is H, C1-C6 alkyl, -(C=O)R , unsubstituted phenyl or unsubstituted benzyl; R is H, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, -CF3, or unsubstituted phenyl, benzyl, or phenethyl; m is 0-8; n is 1 or 2;
摘要翻译：具有下式的化合物：是D4的白三烯的选择性拮抗剂。这些化合物可用作抗哮喘，抗过敏，抗炎和细胞保护剂，并且可以制成药物组合物。在式中，R 1是H，卤素，C 1 -C 8烷基，C 2 -C 8烯基，C 2 -C 8炔基，-CF 3，-OR 2，-SR 2，-NR 2 R 2 >，-CHO，-COOR 2， - （C = O）R 2，-C（OH）R 2 R 2，-CN，-NO 2，取代或未取代的苯基，取代或未取代的苄基或取代或未取代的苯乙基; R 2是H，C 1 -C 8烷基，C 2 -C 8烯基，C 2 -C 8炔基，-CF 3，取代或未取代的苯基，取代或未取代的苄基或取代或未取代的苯乙基; R 3是 - （A）m - （CR 2 = CR 2）p - （CR 2 R 2）m -Q; R 4是H，卤素，-NO 2，-CN，-OR 2，-SR 2，NR 2 R 2或C 1 -C 8烷基; R 6是H或C 1 -C 4烷基; R 7是A）含有3至12个核碳原子和1或2个选自N和S的核杂原子，至少一个为N的单环或双环杂环基，杂环基中的每个环由 5或6个原子，或B）基团WR 8; R 8含有最多21个碳原子，并且（1）烃基或（2）环中含有不超过1个杂原子的有机无环或单环羧酸的酰基; R 9是-OR 1，O，R 1，R 2，R 11， R 1是H，C 1 -C 6烷基， - （C = O）R 1，未取代的苯基或未取代的苄基; R 1是H，C 1 -C 8烷基，C 2 -C 8烯基，C 2 -C 8炔基，-CF 3或未取代的苯基，苄基或苯乙基; m为0-8; n为1或2;

10. 发明专利

CA2250350A1 BISARYLCYCLOBUTENE DERIVATES AS CYCLOOXYGENASE INHIBITORS 未知
公开(公告)号：CA2250350A1
公开(公告)日：1997-10-09
申请号：CA2250350
申请日：1997-03-25
申请人： MERCK FROSST CANADA INC
发明人： PRESCOTT SYLVIE , FORTIN REJEAN , DUBE DANIEL , FRIESEN RICHARD , FRENETTE RICHARD , GUAY DANIEL
IPC分类号： C07D317/72 , A61K31/00 , A61K31/185 , A61K31/22 , A61K31/255 , A61K31/335 , A61K31/357 , A61K31/385 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61P29/00 , A61P31/00 , A61P31/12 , A61P35/00 , A61P43/00 , C07C311/15 , C07C311/16 , C07C317/14 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/44 , C07C321/28 , C07C323/22 , C07C323/62 , C07D213/30 , C07D333/22 , C07D339/06 , A61K31/10 , A61K31/12 , A61K31/15 , A61K31/18 , A61K31/27 , A61K31/33 , C07D213/53
摘要： 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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