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1. 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。

2. 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。

3. 发明专利

ES2247325T3 INHIBIDORES DE 1-BIARIL-1,8-NAFTIRIDIN-4-ONA FOSFODIESTERASA-4. 未知
公开(公告)号：ES2247325T3
公开(公告)日：2006-03-01
申请号：ES02727127
申请日：2002-05-22
申请人： MERCK FROSST CANADA INC
发明人： GUAY DANIEL , GIRARD MARIO , HAMEL PIERRE , LALIBERTE SEBASTIEN , FRIESEN RICHARD , GIRARD YVES
IPC分类号： A61K31/4375 , A61K31/444 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K45/00 , A61P1/04 , A61P9/10 , A61P11/00 , A61P11/04 , A61P11/06 , A61P11/08 , A61P13/12 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D471/04 , A61K31/435 , A61K31/495
摘要： Un compuesto representado por la fórmula (I): o una sal farmacéuticamente aceptable del mismo, en la que Ar es fenilo, piridilo, pirimidilo, indolilo, quilnolinilo, tienilo, piridonilo, oxazolilo, oxadiazolilo, tiadiazolilo, o imidazolilo, u óxidos de los mismos cuando Ar es un heteroarilo; R es H o -alquiloC1-6; R1 es H, o un grupo -alquiloC1-6, -cicloalquiloC3~6, -alcoxiC1-6, -alqueniloC2-6, -alquinilo C3-6, heteroarilo, o heterociclo, opcionalmente sustituido con 1 - 3 sustituyentes independientes -alquilo C1-66, -alcoxiC1-6, OH, amino, (alquilCo_6)-SOn- (alquilC1-6), nitro, CN, =N-O-alquiloC1-6, -O-N=alquiloC1-6, o halógeno; R2 es H, halógeno, -alquiloC1-6, -cicloalquiloC3-6, -alquilC1-6 (cicloalquiIC3~6)(cicloalquiloC3~6), -alcoxiC1-66, fenilo, heteroarilo, heterociclo, amino, -C(O)-alquiloC1-6, -C(O)-O-alquiloC1-66, -alquilC1~6(=N-OH), -C(N=NOH)alquilo C1_6, -alquilC066(oxi)alquilC1~6-fenilo, -SOnNH(alquiloC066), o -(alquilC0_66)-SOn-(alquiloC1-6), en los que el fenilo, heteroarilo oheterociclo está opcionalmente sustituido con halógeno, -alquiloC1-66, -alcoxiC1-6, hidroxi, amino, o -C(O)-O-alquiloC1-6, y cualquier alquilo está opcionalmente sustituido 1 - 6 sustituyentes independientes halógeno u -OH; n es 0, 1, ó 2; R3 es H, OH, amina, halógeno o alquiloC1~6, en el que el alquilo está opcionalmente sustituido 1 - 6 ssustituyente independientes halógeno, OH, o amina; y R4, R5, R6, y R7 cada uno es independientemente H, halógeno, -alquiloC1-6, -alcoxiC1-6, o amina, y cualquier alquilo está opcionalmente sustituido con 1 - 6 sustituyentes independientes halógeno u -OH.

4. 发明专利

ECSP055809A INHIBIDORES 4-OXO-1-(3-FENIL SUSTITUIDO)-1,4-DIHIDRO-1,8-NAFTIRIDINA-3-CARBOXAMIDA DE LA FOSFODIESTERASA-4 未知
公开(公告)号：ECSP055809A
公开(公告)日：2005-08-11
申请号：ECSP055809
申请日：2005-05-20
申请人： MERCK FROSST CANADA INC
发明人： DUBE DANIEL , GALLANT MICHEL , LACOMBE PATRICK , ASPIOTIS RENEE , DUBE LAURENCE , GIRARD YVES , MACDONALD DWIGHT
IPC分类号： A61K31/4375 , A61K31/4745 , A61K31/506 , A61P25/00 , C07D221/00 , C07D471/02 , C07D471/04 , A61K31 , A61P25
摘要： Compuestos representados por la Fórmula (I): (I)o una sal farmacéuticamente aceptable de los mismos, son inhibidores de la fosfodiesterasa útiles en el tratamiento de asma e inflamación, y útiles para la intensificación de la cognición.

5. 发明专利

CA2239053C DIPHENYL PYRIDYL ETHANE DERIVATIVES AS PDE IV INHIBITORS 未知
公开(公告)号：CA2239053C
公开(公告)日：2005-04-26
申请号：CA2239053
申请日：1996-12-11
申请人： MERCK FROSST CANADA INC
发明人： GUAY DANIEL , DUCHARME YVES , GIRARD YVES
IPC分类号： C07D213/50 , A61K31/00 , A61K31/415 , A61K31/44 , A61K31/4409 , A61K31/4427 , A61K31/4439 , A61K31/495 , A61K31/496 , A61P11/00 , A61P11/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D213/30 , C07D213/44 , C07D213/53 , C07D213/60 , C07D213/89 , C07D233/54 , C07D401/10 , C07D403/10
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 IV). The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of formula (I).

6. 发明专利

AU778531B2 Substituted 8-arylquinoline phosphodiesterase-4 inhibitors 未知
公开(公告)号：AU778531B2
公开(公告)日：2004-12-09
申请号：AU2336201
申请日：2000-12-20
申请人： MERCK FROSST CANADA INC
发明人： DESCHENES DENIS , DUBE DANIEL , GALLANT MICHEL , GIRARD YVES , LACOMBE PATRICK , MACDONALD DWIGHT , MASTRACCHIO ANTHONY , PERRIER HELENE
IPC分类号： A61K31/47 , A61K31/4709 , A61K45/00 , A61P1/04 , A61P7/12 , A61P9/00 , A61P11/00 , A61P11/06 , A61P11/16 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/10 , A61P37/08 , C07D215/12 , C07D215/14 , C07D401/10 , C07D401/14 , C07D405/12 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/12 , C07D417/14
摘要： Novel substituted 8-arylquinolines represented by Formula (I), or a pharmaceutically acceptable salt thereof, wherein S1, S2 and S3 are independently H, -OH; halogen, -C1-C6alkyl, -NO2, -CN, or -C1-C6alkoxy, wherein the alkyl and alkoxy groups are optionally substituted with 1-5 substituents; wherein each substituent is independently a halogen or OH; R1 is a H, OH, halogen, carbonyl, or -C1-C6alkyl, -cycloC3-C6alkyl, -C1-C6alkenyl, -C1-C6alkoxy, aryl, heteroaryl, -CN, -heterocycloC3-C6alkyl, -amino, -C1-C6alkylamino, -(C1-C6alkyl)(C1-C6alkyl)amino, -C1-C6alkyl(oxy)C1-C6alkyl, -C(O)NH(aryl), -C(O)NH(heteroaryl), -SOnNH(aryl), -SOnNH(heteroaryl), -SOnNH(C1-C6alkyl), -C(O)N(C0-C6alkyl) (C0-C6alkyl), -NH-SOn-(C1-C6alkyl), -SOn-(C1-C6alkyl), -(C1-C6alkyl)-O-C(CN)-dialkylamino, or -(C1-C6alkyl)-SOn-(C1-C6alkal) group, wherein any of the groups is optionally substituted with 1-5 substituents; wherein each substituent is independently a halogen, -OH, -CN, -C1-C6alkyl, -cycloC3-C6alkyl, -C(O)(heterocycloC3-C6alkyl), -C(O)-O-(C0-C6alkyl), -C(O)-aryloxy, -C1-C6alkoxy, -(C0-C6alkyl)(C0-C6alkyl)amino, cycloalkyloxy, acyl, acyloxy, -cycloC3-C6alkyl, heterocycloC3-C6alkyl, aryl, heteroaryl, carbonyl, carbamoyl, or -SOn-(C1-C6alkyl); A is CH, C-ester, or C-R4; R2 and R3 independently is an aryl, heteroaryl, H, halogen, -CN, -C1-C6alkyl, heterocycloC3-6alkyl, -C1-C6alkoxy, carbonyl, carbamoyl, -C(O)OH, -C1-C6alkyl)-SOn-(C1-C6alkyl), -C(O)N(C0-C6alkyl)(C0-C6alkyl), or -C1-C6alkylacylamino group, wherein any of the groups is optionally substituted with 1-5 substituents, wherein each substituent is independently an aryl, heteroaryl, halogen, -NO2, -C(O)OH, carbonyl, -CN, -C1-C6alkyl, -SOn-(C1-C6alkyl), -SOn-(aryl), aryloxy, -heteroaryloxy, C1-C6alkoxy, N-oxide, -C(O)-heterocycloC3-C6alkyl, -NH-cycloC3-C6alkyl, amino, -OH, or -(C0-C6alkyl)(C0-C6alkyl)amino, -C(O)-N(C0-C6alkyl)(C0-C6alkyl) substituent group, wherein each substituent group independently is optionally substituted with -OH, C1-C6alkoxy, -C1-C6alkyl, -cycloC3-C6alkyl, aryloxy, -C(O)OH, -C(O)O(C1-C6alkyl), halogen, -NO2, -CN, -SOn-(C1-C6alkyl), or -C(O)-N(C0-C6alkyl)(C0-C6alkyl); one of R2 and R3 must be an aryl or heteroaryl, optionally substituted; when R2 and R3 are both an aryl or heteroaryl, then R2 and R3 may be optionally connected by a thio, oxy, or (C1-C4alkyl) bridge to form a fused three ring system; are PDE4 inhibitors.

7. 发明专利

CA2238875C TRI-ARYL ETHANE DERIVATIVES AS PDE IV INHIBITORS 未知
公开(公告)号：CA2238875C
公开(公告)日：2003-09-16
申请号：CA2238875
申请日：1996-12-11
申请人： MERCK FROSST CANADA INC
发明人： HAMEL PIERRE , GIRARD YVES , BLOUIN MARC , DUCHARME YVES , GIRARD MARIO , GUAY DANIEL
IPC分类号： A61K31/00 , A61K31/44 , A61K31/4409 , A61P11/00 , A61P11/06 , A61P43/00 , C07D213/30 , C07D213/50 , C07D213/52 , C07D213/61 , C07D213/89 , C07D213/59 , A61K31/415 , A61K31/535 , A61K31/55 , C07D233/64 , C07D401/06
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 IV). The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of Formula (I).

8. 发明专利

AU764258B2 Heterosubstituted pyridine derivatives as PDE 4 inhibitors 未知
公开(公告)号：AU764258B2
公开(公告)日：2003-08-14
申请号：AU4282900
申请日：2000-05-03
申请人： MERCK FROSST CANADA INC
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
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.

10. 发明专利

CA2450686A1 SUBSTITUTED 8-ARYLQUINOLINE PDE4 INHIBITORS 未知
公开(公告)号：CA2450686A1
公开(公告)日：2003-01-09
申请号：CA2450686
申请日：2002-06-26
申请人： MERCK FROSST CANADA INC
发明人： LACOMBE PATRICK , DESCHENES DENIS , GIRARD YVES , MACDONALD DWIGHT , MASTRACCHIO ANTHONY , GALLANT MICHEL , DUBE DANIEL
IPC分类号： A61K31/47 , A61K31/4709 , A61K31/675 , A61K45/00 , A61P1/00 , A61P1/04 , A61P7/00 , A61P7/12 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P11/08 , A61P11/14 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/24 , A61P25/28 , A61P27/14 , A61P29/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P35/00 , A61P37/06 , A61P37/08 , A61P39/02 , A61P43/00 , C07D215/12 , C07D215/14 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/08 , C07D405/10 , C07D405/14 , C07D413/08 , C07D413/10 , C07D417/08 , C07D417/10 , C07D417/12 , C07F9/60 , C07F9/6571 , C07F9/6574 , C07D403/10
摘要： 8-arylquinolines of formula(I) wherein the aryl group at the 8-position contains a meta two atom bridge to an optionally substituted phenyl or pyrid yl group, are PDE4 inhibitors useful to treat asthma, chronic bronchitis, chron ic obstructive pulmonary disease, arthritis, respiratory distress syndrome, allergic rhinitis, neurogenic inflammation, pain, rheumatoid arthritis, and other diseases. R1-R7 and Ar are as in claim 1.

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