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公开(公告)号:US08222246B2
公开(公告)日:2012-07-17
申请号:US12748524
申请日:2010-03-29
申请人: Bernd Buettelmann , Stephen Deems Gabriel , Steven Paul Hanlon , Roland Jakob-Roetne , Matthew C. Lucas , Paul Spurr , Andrew Thomas , Pius Waldmeier
发明人: Bernd Buettelmann , Stephen Deems Gabriel , Steven Paul Hanlon , Roland Jakob-Roetne , Matthew C. Lucas , Paul Spurr , Andrew Thomas , Pius Waldmeier
IPC分类号: C07D413/02 , A61K31/44
CPC分类号: C07D413/12 , C07D413/14
摘要: The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula I wherein R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A α5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.
摘要翻译: 本发明涉及式I的新型羟基 - 甲基异恶唑衍生物,其中R 1,R 2和R 3如本文所述,以及其药学上可接受的盐和酯。 本发明的活性化合物对GABA Aα5受体具有亲和性和选择性。 此外,本发明涉及制备式I的活性化合物,含有它们的药物组合物及其作为药物的用途。
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公开(公告)号:US20080139544A1
公开(公告)日:2008-06-12
申请号:US12008452
申请日:2008-01-11
IPC分类号: A61K31/537 , C07D401/04 , C07D265/04 , A61K31/4747
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 Ia and Ib 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.
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公开(公告)号:US20120040949A1
公开(公告)日:2012-02-16
申请号:US13207481
申请日:2011-08-11
申请人: Steven Joseph Berthel , Roland Joseph Billedeau , Christine E. Brotherton-Pleiss , Fariborz Firooznia , Stephen Deems Gabriel , Xiaochun Han , Ramona Hilgenkamp , Saul Jaime-Figueroa , Buelent Kocer , Francisco Javier Lopez-Tapia , Yan Lou , Lucja Orzechowski , Timothy D. Owens , Jenny Tan , Peter Michael Wovkulich
发明人: Steven Joseph Berthel , Roland Joseph Billedeau , Christine E. Brotherton-Pleiss , Fariborz Firooznia , Stephen Deems Gabriel , Xiaochun Han , Ramona Hilgenkamp , Saul Jaime-Figueroa , Buelent Kocer , Francisco Javier Lopez-Tapia , Yan Lou , Lucja Orzechowski , Timothy D. Owens , Jenny Tan , Peter Michael Wovkulich
IPC分类号: A61K31/502 , C07D413/14 , C07D403/14 , C07D487/10 , A61P37/00 , C07D491/107 , A61K31/5377 , A61K31/541 , A61K31/501 , A61P29/00 , C07D401/14 , C07D417/14
CPC分类号: C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/107
摘要: This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y4, are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
摘要翻译: 本申请公开了根据通式I的6-(2-羟基甲基 - 苯基)-2-甲基-2H-哒嗪-3-酮衍生物:其中,变量X,R和Y4如本文所述定义,其抑制Btk 。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎性和自身免疫疾病,例如类风湿性关节炎。 还公开了含有式I化合物和至少一种载体,稀释剂或赋形剂的组合物。
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公开(公告)号:US08697696B2
公开(公告)日:2014-04-15
申请号:US13287152
申请日:2011-11-02
IPC分类号: C07D403/12 , C07D405/14 , C07D413/14 , C07D417/06 , C07D417/14
CPC分类号: C07D413/14 , C07D403/12 , C07D405/14 , C07D417/06 , C07D417/14
摘要: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The compounds of present invention have affinity and selectivity for the GABA A α5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
摘要翻译: 本发明涉及式(I)的新三唑化合物,其中A,X,Y,u,v,R 1,R 2和R 3如本文所述,以及其药学上可接受的盐。 本发明的化合物对GABA Aα5受体具有亲和性和选择性。 此外,本发明涉及制备式(I)化合物,包含它们的药物组合物及其作为药物的用途。
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公开(公告)号:US08481540B2
公开(公告)日:2013-07-09
申请号:US13207481
申请日:2011-08-11
申请人: Steven Joseph Berthel , Roland Joseph Billedeau , Christine E. Brotherton-Pleiss , Fariborz Firooznia , Stephen Deems Gabriel , Xiaochun Han , Ramona Hilgenkamp , Saul Jaime-Figueroa , Buelent Kocer , Francisco Javier Lopez-Tapia , Yan Lou , Lucja Orzechowski , Timothy D. Owens , Jenny Tan , Peter Michael Wovkulich
发明人: Steven Joseph Berthel , Roland Joseph Billedeau , Christine E. Brotherton-Pleiss , Fariborz Firooznia , Stephen Deems Gabriel , Xiaochun Han , Ramona Hilgenkamp , Saul Jaime-Figueroa , Buelent Kocer , Francisco Javier Lopez-Tapia , Yan Lou , Lucja Orzechowski , Timothy D. Owens , Jenny Tan , Peter Michael Wovkulich
IPC分类号: A01N43/58 , A61K31/50 , C07D237/00
CPC分类号: C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/107
摘要: This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y4, are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
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公开(公告)号:US20120115868A1
公开(公告)日:2012-05-10
申请号:US13287152
申请日:2011-11-02
IPC分类号: A61K31/422 , C07D405/14 , A61K31/4155 , A61K31/5377 , C07D417/06 , A61K31/427 , C07D417/14 , A61K31/4439 , A61P25/00 , A61P25/28 , A61P25/18 , A61P25/22 , A61P25/30 , A61P25/14 , A61P25/16 , A61P25/24 , C07D413/14
CPC分类号: C07D413/14 , C07D403/12 , C07D405/14 , C07D417/06 , C07D417/14
摘要: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The compounds of present invention have affinity and selectivity for the GABA A α5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
摘要翻译: 本发明涉及式(I)的新三唑化合物,其中A,X,Y,u,v,R 1,R 2和R 3如本文所述,以及其药学上可接受的盐。 本发明的化合物对GABA Aα5受体具有亲和性和选择性。 此外,本发明涉及制备式(I)化合物,包含它们的药物组合物及其作为药物的用途。
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公开(公告)号:US20100256127A1
公开(公告)日:2010-10-07
申请号:US12748524
申请日:2010-03-29
申请人: Bernd Buettelmann , Stephen Deems Gabriel , Steven Paul Hanlon , Roland Jakob-Roetne , Matthew C. Lucas , Paul Spurr , Andrew Thomas , Pius Waldmeier
发明人: Bernd Buettelmann , Stephen Deems Gabriel , Steven Paul Hanlon , Roland Jakob-Roetne , Matthew C. Lucas , Paul Spurr , Andrew Thomas , Pius Waldmeier
IPC分类号: A61K31/465 , C07D413/12 , C07D417/14 , A61K31/541 , C07D413/14 , A61K31/5377 , A61P25/28
CPC分类号: C07D413/12 , C07D413/14
摘要: The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula I wherein R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A α5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.
摘要翻译: 本发明涉及式I的新型羟基 - 甲基异恶唑衍生物,其中R 1,R 2和R 3如本文所述,以及其药学上可接受的盐和酯。 本发明的活性化合物对GABA Aα5受体具有亲和性和选择性。 此外,本发明涉及制备式I的活性化合物,含有它们的药物组合物及其作为药物的用途。
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公开(公告)号:US20090028818A1
公开(公告)日:2009-01-29
申请号:US12220485
申请日:2008-07-24
IPC分类号: A61K38/20 , C07D401/14 , A61K39/395 , A61P31/18 , A61P11/06 , A61P19/02 , A61P37/02 , A61K31/445
CPC分类号: C07D401/14 , C07D407/14 , C07D413/14
摘要: This invention relates to piperidine derivatives of formula I wherein R1, R2, R3 and R4 are as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 receptors is implicated. 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), rheumatoid arthritis, solid organ transplant reject (graft vs. host disease), asthma and COPR.
摘要翻译: 本发明涉及式I的哌啶衍生物,其中R 1,R 2,R 3和R 4如本文所定义,可用于治疗各种疾病,包括涉及CCR5受体调节的疾病。 可以由本发明衍生物治疗或预防的疾病包括HIV和遗传相关的逆转录病毒感染(和所得的获得性免疫缺陷综合征,AIDS),类风湿性关节炎,实体器官移植排斥(移植物抗宿主病),哮喘和COPR。
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公开(公告)号:US07538122B2
公开(公告)日:2009-05-26
申请号:US12008452
申请日:2008-01-11
IPC分类号: A61K31/445 , C07D221/00
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 Ia and Ib 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.
摘要翻译: 本发明涉及式Ia和Ib的哌啶衍生物,其具有如本文定义的取代基,其可用于治疗各种疾病,包括涉及CCR5受体调节的各种疾病。 更具体地说,本发明涉及1-氧杂-3,8-二氮杂 - 螺[4.5]癸-2-酮和1-氧杂-3,9-二氮杂螺[5.5]十一烷-2-酮化合物及其相关 衍生物,含有和用于此类衍生物的组合物。 本衍生物可能治疗或预防的疾病包括艾滋病毒和基因相关的逆转录病毒感染(以及由此产生的获得性免疫缺陷综合征,艾滋病),免疫系统疾病和炎性疾病。
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公开(公告)号:US20090093501A1
公开(公告)日:2009-04-09
申请号:US12284039
申请日:2008-09-18
IPC分类号: A61K31/438 , C07D471/10 , A61P31/12 , A61P11/00 , A61P37/00 , A61K31/506 , A61K31/4545
CPC分类号: C07D471/10
摘要: This invention relates to piperidine derivatives of formula I wherein R1, R2, R3, R4 and Y are as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 receptors is implicated. 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), rheumatoid arthritis, solid organ transplant reject (graft vs. host disease), asthma and COPR.
摘要翻译: 本发明涉及式I的哌啶衍生物,其中R 1,R 2,R 3,R 4和Y如本文所定义,可用于治疗多种疾病,包括涉及CCR5受体调节的疾病。 可以由本发明衍生物治疗或预防的疾病包括HIV和遗传相关的逆转录病毒感染(和所得的获得性免疫缺陷综合征,AIDS),类风湿性关节炎,实体器官移植排斥(移植物抗宿主病),哮喘和COPR。
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