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    N-(4-ARYLOXYPIPERIDIN-1-YLALKYL) CINNAMIC AMIDES AS CCR3-3 RECEPTOR ANTAGONISTS
    1.
    发明公开
    N-(4-ARYLOXYPIPERIDIN-1-YLALKYL) CINNAMIC AMIDES AS CCR3-3 RECEPTOR ANTAGONISTS 有权
    N-（4- ARYLOXYPIPERIDIN -1-基烷基）cinnamamides AS CCR3受体拮抗剂

    公开(公告)号：EP1330436A1

    公开(公告)日：2003-07-30

    申请号：EP01976285.5

    申请日：2001-10-08

    申请人： Novartis AG ,  Novartis Pharma GmbH

    发明人： BHALAY, Gurdip ,  HOWE, Trevor, John ,  LE GRAND, Darren, Mark

    IPC分类号： C07D211/46 ,  C07D401/06 ,  A61K31/495 ,  A61P29/00

    CPC分类号： C07D211/46

    摘要： Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more substituents selected from halogen, cyano, nitro, and C¿1?-C8-alkyl optionally substituted by cyano or halogen, Ar?2¿ is phenyl optionally which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C¿1?-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-alkoxycarbonyl, R?1 is C¿1-C8-alkyl substituted by hydroxy, C1-C8-alkoxy, acyloxy, -N(R2)R3, halogen, carboxy, C¿1?-C8-alkoxycarbonyl, phenyl- C1-C8-alkoxycarbonyl, -CON(R?4)R5¿ or by a monovalent cyclic organic group, R?2 and R3 ¿ are each independently hydrogen or C¿1?-C8-alkyl, or R?2¿ is hydrogen and R3 is acyl or SO¿2?R?6, or R2 and R3¿ together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, R?4 and R5¿ are each independently hydrogen, C¿1?-C8-alkyl optionally substituted by hydroxy or phenyl, or phenyl optionally substituted by C1-C8-alkyl, halogen, cyano or C1-C8-alkoxy, or R?4 and R5¿ together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, R6 is C1-C8-alkyl, C1-C8-haloalkyl, or phenyl optionally substituted by C1-C8-alkyl, and n is 1, 2, 3 or 4. The compounds are useful as pharmaceuticals.

    8-QUINOLINXANTHINE AND 8-ISOQUINOLINXANTHINE DERIVATIVES AS PDE 5 INHIBITORS
    3.
    发明授权
    8-QUINOLINXANTHINE AND 8-ISOQUINOLINXANTHINE DERIVATIVES AS PDE 5 INHIBITORS 有权
    8-QUINOLINXANTHINE和8-异喹啉黄嘌呤衍生物作为PDE 5抑制剂

    公开(公告)号：EP1268480B1

    公开(公告)日：2003-11-05

    申请号：EP01940294.0

    申请日：2001-04-05

    申请人： Novartis AG ,  Novartis Pharma GmbH

    发明人： BHALAY, Gurdip ,  COLLINGWOOD, Stephen Paul ,  FAIRHURST, Robin Alec ,  GOMEZ, Sylvie, Felicite ,  NAEF, Reto ,  SANDHAM, David, Andrew

    IPC分类号： C07D473/06 ,  C07D239/54 ,  A61K31/52 ,  A61P15/00

    CPC分类号： C07D239/545 ,  C07D473/06

    摘要： A compound of formula (I) in free or salt form, where R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula -N(R6)R7, aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and R?6 and R7¿ are each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of R?6 and R7¿ is hydrogen and the other is acyl, or R?6 and R7¿ together with the nitrogen atom to which they are attached denote a 5- or 6- membered heterocyclyl group.

    摘要翻译： 其中R 1为氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 2为氢，烷基，羟基烷基，烷基羰基氧基烷基，烷氧基烷基，烷基硫代烷基，烯基，环烷基烷基，杂环基烷基，芳烷基 其中其芳环任选与5-元杂环基稠合或任选被一个或多个选自烷氧基，氨基，烷基氨基，二烷基氨基，酰基氨基，卤素，羟基，氨基磺酰基，烷基氨基磺酰基，二烷基氨基磺酰基，烷基磺酰基氨基或二烷基氨基磺酰基氨基 R 3为氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 4为氢或烷基，R 5为任选稠合至5元杂环基且任选被一个或多个选自以下的取代基取代的喹啉基，异喹啉基或氧代二氢异喹啉基： 卤素，氰基，羟基，烷基，羟基烷基，烷氧基烷基，烷硫基烷基，烷氧基，烷硫基， 烷基羰基，炔基，羧基，酰基，式-N（R 6）R 7的基团，任选被一个或多个选自卤素或烷氧基的取代基取代的芳基，或通过环碳原子连接的具有5或6个环原子的杂芳基 所指出的碳原子和R16和R7各自独立地为氢或被羟基或烷氧基任意取代的烷基或R6或R7中的一个为氢而另一个为酰基或R6和R7与 它们所连接的氮原子表示5或6元杂环基。

    PIPERIDINE COMPOUNDS FOR USE AS CCR-3 INHIBITORS
    4.
    发明授权
    PIPERIDINE COMPOUNDS FOR USE AS CCR-3 INHIBITORS 有权
    哌啶用作CCR-3抑制剂

    公开(公告)号：EP1303488B1

    公开(公告)日：2009-11-04

    申请号：EP01960488.3

    申请日：2001-07-10

    申请人： Novartis AG ,  Novartis Pharma GmbH

    发明人： HOWE, Trevor John ,  BHALAY, Gurdip ,  LE GRAND, Darren Mark ,  STORZ, Thomas

    IPC分类号： C07D211/32 ,  C07D401/06 ,  C07D405/06 ,  C07D417/06 ,  A61K31/4545 ,  A61P37/08 ,  A61P29/00

    CPC分类号： C07D401/06 ,  C07D211/32 ,  C07D405/06 ,  C07D417/06

    摘要： Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more halogen atoms, Ar¿2? is phenyl or naphthyl which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-alkoxycarbonyl, R?1¿ is hydrogen or C¿1?-C8-alkyl optionally substituted by hydroxy, C1-C8-alkoxy, acyloxy, N(R?2)R3¿, halogen, carboxy, C¿1?-C8-alkoxycarbonyl, -CON(R?4)R5¿ or by a monovalent cyclic organic group, R?2 and R3¿ are each independently hydrogen or C¿1?-C8-alkyl, or R?2¿ is hydrogen and R3 is acyl or -SO¿2?R?6, or R2 and R3¿ together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, R?4 and R5¿ are each independently hydrogen or C¿1?-C8-alkyl, or R?4 and R5¿ together with the nitrogen atom to which they are attached denote a 5- 6-membered heterocyclic group, R6 is C1-C8-alkyl, C1-C8-haloalkyl, or phenyl optionally substituted by C1-C8-alkyl, and n is 1, 2, 3, or 4, with the proviso that when Ar1 is p-chlorophenyl and R1 is hydrogen, Ar2 is not phenyl or p-nitrophenyl. The compounds are useful as pharmaceuticals.

    PIPERIDINE COMPOUNDS FOR USE AS CCR-3 INHIBITORS
    6.
    发明公开
    PIPERIDINE COMPOUNDS FOR USE AS CCR-3 INHIBITORS 有权
    哌啶用作CCR-3抑制剂

    公开(公告)号：EP1303488A1

    公开(公告)日：2003-04-23

    申请号：EP01960488.3

    申请日：2001-07-10

    申请人： Novartis AG ,  Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.

    发明人： HOWE, Trevor John ,  BHALAY, Gurdip ,  LE GRAND, Darren Mark ,  STORZ, Thomas

    IPC分类号： C07D211/32 ,  C07D401/06 ,  C07D405/06 ,  C07D417/06 ,  A61K31/4545 ,  A61P37/08 ,  A61P29/00

    CPC分类号： C07D401/06 ,  C07D211/32 ,  C07D405/06 ,  C07D417/06

    摘要： Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more halogen atoms, Ar¿2? is phenyl or naphthyl which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-alkoxycarbonyl, R?1¿ is hydrogen or C¿1?-C8-alkyl optionally substituted by hydroxy, C1-C8-alkoxy, acyloxy, N(R?2)R3¿, halogen, carboxy, C¿1?-C8-alkoxycarbonyl, -CON(R?4)R5¿ or by a monovalent cyclic organic group, R?2 and R3¿ are each independently hydrogen or C¿1?-C8-alkyl, or R?2¿ is hydrogen and R3 is acyl or -SO¿2?R?6, or R2 and R3¿ together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, R?4 and R5¿ are each independently hydrogen or C¿1?-C8-alkyl, or R?4 and R5¿ together with the nitrogen atom to which they are attached denote a 5- 6-membered heterocyclic group, R6 is C1-C8-alkyl, C1-C8-haloalkyl, or phenyl optionally substituted by C1-C8-alkyl, and n is 1, 2, 3, or 4, with the proviso that when Ar1 is p-chlorophenyl and R1 is hydrogen, Ar2 is not phenyl or p-nitrophenyl. The compounds are useful as pharmaceuticals.