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8 条记录 (耗时 0.025 秒)

    5-AROYLNAPHTHALENE DERIVATIVES
    1.
    发明授权
    5-AROYLNAPHTHALENE DERIVATIVES 失效
    5-AROYLPHPHALALIN DERIVATE

    公开(公告)号：EP0966437B1

    公开(公告)日：2002-06-12

    申请号：EP98905325.1

    申请日：1998-01-21

    申请人： F.HOFFMANN-LA ROCHE AG

    发明人： ROTSTEIN, David, Mark ,  SJOGREN, Eric, Brian

    IPC分类号： C07C311/29 ,  C07C317/24 ,  C07C317/22 ,  C07C311/51 ,  C07D295/12 ,  C07D213/42 ,  A61K31/18 ,  A61K31/10 ,  A61K31/275 ,  A61K31/235 ,  A61K31/435

    CPC分类号： C07D207/26 ,  C07C311/16 ,  C07C311/29 ,  C07C311/51 ,  C07C317/22 ,  C07C317/24 ,  C07C317/44 ,  C07C323/22 ,  C07C323/67 ,  C07C2601/04 ,  C07C2601/14 ,  C07D211/58 ,  C07D213/42 ,  C07D295/13 ,  C07D295/26 ,  C07D307/46 ,  C07D307/52 ,  C07D333/22 ,  C07D405/06

    摘要： The present invention relates to certain 5-aroylnaphthalene derivatives of formula (I), wherein A is a bond, -CH2-, -CH(OH)-, -C=NOR4-, -C(O)-, -NR5-, -O-, or -S(O)¿n?- where n is an integer from 0 to 2, R?4¿ is hydrogen or alkyl, and R5 is hydrogen, alkyl, or acyl; Z is a group represented by formula (B), (C), (D), or (E), where n1 is 0 to 3; X is O or S; R?6 and R7¿ are independently selected from hydrogen, alkyl, halogenalkyl, cycloalkyl, cycloalkylalkyl, acyl, alkylthio, cycloalkylthio, cycloalkylalkylthio, alkoxy, cycloalkyloxy, cycloalkylalkyloxy, halogenalkyloxy, alkenyl, halogen, cyano, nitro, hydroxy, or -NR9R10 where R?9 and R10¿ are independently hydrogen, alkyl, or acyl; or R?6 and R7¿ when they are adjacent to each other form methylenedioxy or ethylenedioxy; R8 is hydrogen, alkyl, halogenalkyl, alkoxy, cycloalkyloxy, halogenalkyloxy, alkylthio, cycloalkylthio, nitro, cyano, hydroxy, or halogen; R1 is hydrogen, alkyl, alkenyl, alkynyl, halogenalkyl, cycloalkyl, cycloalkylalkyl, alkoxy, alkenyloxy, cycloalkyloxy, cycloalkylalkyloxy, halogenalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, alkylthio, cycloalkylthio, cycloalkylalkylthio, hydroxy, halogen, cyano, carboxy, alkoxycarbonyl, acyl, -C=NOR?4, -NR9R10, -CONR9R10¿, -OCONR9R10, or -OSO¿2R?11 where R?4, R9, and R10¿ are as previously defined and R11 is alkyl, cycloalkyl, or halogenalkyl; R2 is hydrogen, alkyl, alkoxy, halogen, nitro, or -NR?9R10; and R3¿ is -SO¿2R?12 or -SO¿2?NR?13R14¿ where R12 is alkyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl, or alkoxycarbonylalkyl; R13 is hydrogen, alkyl, or acyl; and R14 is hydrogen, alkyl, halogenalkyl, cycloalkyl, cycloalkylalkyl, alkenyl, hydroxyalkyl, alkoxyalkyl, alkoxycarbonylalkyl, amino, aminoalkyl, aryl, aralkyl, heteroaralkyl, heterocyclo, heterocycloalkyl, acyl, hydroxy, or alkoxy; or R?13 and R14¿ together with the nitrogen atom to which they are attached optionally form a heterocycloamino group; that are inhibitors of prostaglandin G/H synthase, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

    摘要翻译： 本发明涉及式（I）的某些5-芳酰基萘衍生物：其为前列腺素G / H合成酶的抑制剂，含有它们的药物组合物，其使用方法和制备这些化合物的方法。

    CHEMOKINE CCR5 RECEPTOR MODULATORS
    2.
    发明公开
    CHEMOKINE CCR5 RECEPTOR MODULATORS 审中-公开
    趋化因子，CCR5受体调节剂

    公开(公告)号：EP1716156A2

    公开(公告)日：2006-11-02

    申请号：EP05707116.9

    申请日：2005-02-01

    申请人： F.HOFFMANN-LA ROCHE AG

    发明人： GABRIEL, Stephen, Deems ,  ROTSTEIN, David, Mark

    IPC分类号： C07D498/10 ,  A61K31/435 ,  A61K31/537 ,  A61P31/18

    CPC分类号： C07D498/10 ,  A61K31/435 ,  A61K31/4747 ,  A61K31/537 ,  A61K31/538 ,  A61K45/06 ,  A61K2300/00

    摘要： This invention relates to piperidine derivatives of formulae (I) with substituents as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 receptors is implicated. More particularly, the present invention relates to 1-oxa-3,8-diaza-spiro[4.5]decan-2-one and 1-oxa-3,9-diaza-spiro[5.5]undecan-2-one compounds and related derivatives, to compositions containing and to uses of such derivatives. Disorders that may be treated or prevented by the present derivatives include HIV and genetically related retroviral infections (and the resulting acquired immune deficiency syndrome, AIDS), diseases of the immune system and inflammatory diseases.

    OCTAHYDROPYRROLO[3,4-C]PYRROLE DERIVATIVES AN THEIR USE AS ANTIVIRAL AGENTS
    5.
    发明授权
    OCTAHYDROPYRROLO[3,4-C]PYRROLE DERIVATIVES AN THEIR USE AS ANTIVIRAL AGENTS 有权
    八氢 - 吡咯并[3,4-C]吡咯衍生物和它们作为抗病毒剂的应用

    公开(公告)号：EP1761542B1

    公开(公告)日：2008-01-02

    申请号：EP05754708.5

    申请日：2005-06-01

    申请人： F.HOFFMANN-LA ROCHE AG

    发明人： LEE, Eun, Kyung ,  MELVILLE, Chris, Richard ,  ROTSTEIN, David, Mark

    IPC分类号： C07D487/04 ,  A61K31/407

    CPC分类号： C07D487/04

    摘要： Chemokine receptor antagonists, in particular, 3,7-diazabicyclo [3.3.0] octane compounds according to formula (I) are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are allieviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula (I).

    HETEROCYCLIC ANTIVIRAL COMPOUNDS
    6.
    发明公开
    HETEROCYCLIC ANTIVIRAL COMPOUNDS 审中-公开
    杂环抗病毒化合物

    公开(公告)号：EP1987035A1

    公开(公告)日：2008-11-05

    申请号：EP07704347.9

    申请日：2007-02-05

    申请人： F.HOFFMANN-LA ROCHE AG

    发明人： LEMOINE, Remy ,  MELVILLE, Chris, Richard ,  PADILLA, Fernando ,  ROTSTEIN, David, Mark ,  WANNER, Jutta

    IPC分类号： C07D487/04 ,  A61K31/407 ,  A61P31/12 ,  A61P31/18

    CPC分类号： C07D487/04

    摘要： Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) wherein R1-R3 R6c and X1 are as defined herein are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula (I).

    摘要翻译： 趋化因子受体拮抗剂，特别是其中R 1 -R 3 R 6c和X 1如本文所定义的式（I）的3,7-二氮杂双环[3.3.0]辛烷化合物是趋化因子CCR5受体的拮抗剂，其可用于治疗或预防 人类免疫缺陷病毒（HIV）感染或治疗AIDS或ARC。 本发明进一步提供了用于治疗用CCR5拮抗剂减轻的疾病的方法。 本发明包括药物组合物和使用这些化合物治疗这些疾病的方法。 本发明进一步包括用于制备根据式（I）的化合物的方法。

    OCTAHYDROPYRROLO[3,4-C]PYRROLE DERIVATIVES AN THEIR USE AS ANTIVIRAL AGENTS
    7.
    发明公开
    OCTAHYDROPYRROLO[3,4-C]PYRROLE DERIVATIVES AN THEIR USE AS ANTIVIRAL AGENTS 有权
    八氢 - 吡咯并[3,4-C]吡咯衍生物和它们作为抗病毒剂的应用

    公开(公告)号：EP1761542A2

    公开(公告)日：2007-03-14

    申请号：EP05754708.5

    申请日：2005-06-01

    申请人： F.HOFFMANN-LA ROCHE AG

    发明人： LEE, Eun, Kyung ,  MELVILLE, Chris, Richard ,  ROTSTEIN, David, Mark

    IPC分类号： C07D487/04 ,  A61K31/407

    CPC分类号： C07D487/04

    摘要： Chemokine receptor antagonists, in particular, 3,7-diazabicyclo [3.3.0] octane compounds according to formula (I) are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are allieviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula (I).

    5-AROYLNAPHTHALENE DERIVATIVES
    8.
    发明公开
    5-AROYLNAPHTHALENE DERIVATIVES 失效
    5-芳酰基萘衍生物

    公开(公告)号：EP0966437A1

    公开(公告)日：1999-12-29

    申请号：EP98905325.0

    申请日：1998-01-21

    申请人： F.HOFFMANN-LA ROCHE AG

    发明人： ROTSTEIN, David, Mark ,  SJOGREN, Eric, Brian

    IPC分类号： C07D295 ,  A61K31 ,  A61P29 ,  A61P37 ,  A61P43 ,  C07C311 ,  C07C317 ,  C07C323 ,  C07D207 ,  C07D211 ,  C07D213 ,  C07D307 ,  C07D333 ,  C07D405

    CPC分类号： C07D207/26 ,  C07C311/16 ,  C07C311/29 ,  C07C311/51 ,  C07C317/22 ,  C07C317/24 ,  C07C317/44 ,  C07C323/22 ,  C07C323/67 ,  C07C2601/04 ,  C07C2601/14 ,  C07D211/58 ,  C07D213/42 ,  C07D295/13 ,  C07D295/26 ,  C07D307/46 ,  C07D307/52 ,  C07D333/22 ,  C07D405/06

    摘要： The present invention relates to certain 5-aroylnaphthalene derivatives of formula (I), wherein A is a bond, -CH2-, -CH(OH)-, -C=NOR4-, -C(O)-, -NR5-, -O-, or -S(O)¿n?- where n is an integer from 0 to 2, R?4¿ is hydrogen or alkyl, and R5 is hydrogen, alkyl, or acyl; Z is a group represented by formula (B), (C), (D), or (E), where n1 is 0 to 3; X is O or S; R?6 and R7¿ are independently selected from hydrogen, alkyl, halogenalkyl, cycloalkyl, cycloalkylalkyl, acyl, alkylthio, cycloalkylthio, cycloalkylalkylthio, alkoxy, cycloalkyloxy, cycloalkylalkyloxy, halogenalkyloxy, alkenyl, halogen, cyano, nitro, hydroxy, or -NR9R10 where R?9 and R10¿ are independently hydrogen, alkyl, or acyl; or R?6 and R7¿ when they are adjacent to each other form methylenedioxy or ethylenedioxy; R8 is hydrogen, alkyl, halogenalkyl, alkoxy, cycloalkyloxy, halogenalkyloxy, alkylthio, cycloalkylthio, nitro, cyano, hydroxy, or halogen; R1 is hydrogen, alkyl, alkenyl, alkynyl, halogenalkyl, cycloalkyl, cycloalkylalkyl, alkoxy, alkenyloxy, cycloalkyloxy, cycloalkylalkyloxy, halogenalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, alkylthio, cycloalkylthio, cycloalkylalkylthio, hydroxy, halogen, cyano, carboxy, alkoxycarbonyl, acyl, -C=NOR?4, -NR9R10, -CONR9R10¿, -OCONR9R10, or -OSO¿2R?11 where R?4, R9, and R10¿ are as previously defined and R11 is alkyl, cycloalkyl, or halogenalkyl; R2 is hydrogen, alkyl, alkoxy, halogen, nitro, or -NR?9R10; and R3¿ is -SO¿2R?12 or -SO¿2?NR?13R14¿ where R12 is alkyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl, or alkoxycarbonylalkyl; R13 is hydrogen, alkyl, or acyl; and R14 is hydrogen, alkyl, halogenalkyl, cycloalkyl, cycloalkylalkyl, alkenyl, hydroxyalkyl, alkoxyalkyl, alkoxycarbonylalkyl, amino, aminoalkyl, aryl, aralkyl, heteroaralkyl, heterocyclo, heterocycloalkyl, acyl, hydroxy, or alkoxy; or R?13 and R14¿ together with the nitrogen atom to which they are attached optionally form a heterocycloamino group; that are inhibitors of prostaglandin G/H synthase, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

    摘要翻译： 本发明涉及式（I）的某些5-芳酰基萘衍生物，其中A为键，-CH 2 - ， - CH（OH） - ，-C = NOR 4 - ， - C（O） - ，-NR 5 - -O-或-S（O）n - - ，其中n是从0到2的整数，R 4是氢或烷基，并且R 5是氢，烷基或酰基; Z是由式（B），（C），（D）或（E）表示的基团，其中n1是0至3; X是O或S; 烷基，卤代烷基，环烷基，环烷基烷基，酰基，烷硫基，环烷硫基，环烷基烷硫基，烷氧基，环烷氧基，环烷基烷氧基，卤代烷氧基，链烯基，卤素，氰基，硝基，羟基或-NR9R10，其中R15和R17独立地选自氢， R9和R10独立地为氢，烷基或酰基; 或当R6和R7彼此相邻时形成亚甲二氧基或亚乙二氧基; R8是氢，烷基，卤代烷基，烷氧基，环烷氧基，卤代烷氧基，烷硫基，环烷硫基，硝基，氰基，羟基或卤素; 烷基，烯基，炔基，卤代烷基，环烷基，环烷基烷基，烷氧基，烯氧基，环烷氧基，环烷基烷氧基，卤代烷氧基，羟基烷氧基，烷氧基烷氧基，烷硫基，环烷硫基，环烷基烷硫基，羟基，卤素，氰基，羧基，烷氧基羰基，酰基，-C = NOR 4，-NR 9 R 10，-CONR 9 R 10，-OCONR 9 R 10或-OSO 2 R 11，其中R 14，R 9和R 10如先前所定义且R 11为烷基，环烷基或卤代烷基; R2是氢，烷基，烷氧基，卤素，硝基或-NR9R10; 其中R12是烷基，羟烷基，烷氧基烷基，羧基烷基或烷氧基羰基烷基;并且R3是-SO 2 R 12或-SO 2 NR 9 R 13 R 14，其中R 12是烷基， R13是氢，烷基或酰基; 烷基，卤代烷基，环烷基，环烷基烷基，烯基，羟基烷基，烷氧基烷基，烷氧基羰基烷基，氨基，氨基烷基，芳基，芳烷基，杂芳烷基，杂环基，杂环烷基，酰基，羟基或烷氧基; 或R 13和R 14与它们所连接的氮原子一起任选形成杂环氨基; 它们是前列腺素G / H合酶的抑制剂，含有它们的药物组合物，它们的使用方法以及制备这些化合物的方法。