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公开(公告)号:US07589199B2
公开(公告)日:2009-09-15
申请号:US11008774
申请日:2004-12-08
申请人: Andrew M. K. Pennell , James B. Aggen , J. J. Kim Wright , Subhabrata Sen , Brian E. McMaster , Daniel Joseph Dairaghi , Wei Chen , Penglie Zhang
发明人: Andrew M. K. Pennell , James B. Aggen , J. J. Kim Wright , Subhabrata Sen , Brian E. McMaster , Daniel Joseph Dairaghi , Wei Chen , Penglie Zhang
IPC分类号: A61K31/496 , C07D401/14 , C07D403/14
CPC分类号: C07D403/04 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K45/06 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D231/38 , C07D231/56 , C07D233/61 , C07D235/06 , C07D235/16 , C07D249/08 , C07D249/14 , C07D257/04 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/04 , C07D407/04 , C07D409/04 , C07D413/04 , C07D413/12 , C07D417/04 , C07D471/04 , C07D473/34 , A61K2300/00
摘要: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
摘要翻译: 提供了作为CCR1受体的有效拮抗剂并具有体内抗炎活性的化合物。 化合物通常为芳基哌嗪衍生物,并且可用于药物组合物,用于治疗CCR1介导的疾病的方法,以及用于鉴定竞争性CCR1拮抗剂的测定中的对照。
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公开(公告)号:US08324216B2
公开(公告)日:2012-12-04
申请号:US12555650
申请日:2009-09-08
申请人: Andrew M. K. Pennell , James B. Aggen , J. J. Kim Wright , Subhabrata Sen , Brian E. McMaster , Daniel Joseph Dairaghi , Wei Chen , Penglie Zhang
发明人: Andrew M. K. Pennell , James B. Aggen , J. J. Kim Wright , Subhabrata Sen , Brian E. McMaster , Daniel Joseph Dairaghi , Wei Chen , Penglie Zhang
IPC分类号: A61K31/496 , C07D233/61 , C07D249/14 , C07D257/04
CPC分类号: C07D403/04 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K45/06 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D231/38 , C07D231/56 , C07D233/61 , C07D235/06 , C07D235/16 , C07D249/08 , C07D249/14 , C07D257/04 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/04 , C07D407/04 , C07D409/04 , C07D413/04 , C07D413/12 , C07D417/04 , C07D471/04 , C07D473/34 , A61K2300/00
摘要: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
摘要翻译: 提供了作为CCR1受体的有效拮抗剂并具有体内抗炎活性的化合物。 化合物通常为芳基哌嗪衍生物,并且可用于药物组合物,用于治疗CCR1介导的疾病的方法,以及用于鉴定竞争性CCR1拮抗剂的测定中的对照。
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公开(公告)号:US07842693B2
公开(公告)日:2010-11-30
申请号:US10732897
申请日:2003-12-09
申请人: Andrew M. K. Pennell , James B. Aggen , J. J. Kim Wright , Subhabrata Sen , Brian E. McMaster , Daniel Joseph Dairaghi , Valeri V. Martichonok
发明人: Andrew M. K. Pennell , James B. Aggen , J. J. Kim Wright , Subhabrata Sen , Brian E. McMaster , Daniel Joseph Dairaghi , Valeri V. Martichonok
IPC分类号: A61K31/496 , A61K31/5377 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D401/14 , C07D409/14
CPC分类号: C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D231/38 , C07D231/56 , C07D233/56 , C07D235/06 , C07D249/12 , C07D257/04 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D409/04 , C07D473/34
摘要: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
摘要翻译: 提供了作为CCR1受体的有效拮抗剂的化合物,并且在用于CCR1的标志性疾病状态之一的炎症的动物试验中进一步证实了这些化合物。 化合物通常为芳基哌嗪衍生物,并且可用于药物组合物,用于治疗CCR1介导的疾病的方法,以及用于鉴定竞争性CCR1拮抗剂的测定中的对照。
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公开(公告)号:US20100240618A1
公开(公告)日:2010-09-23
申请号:US12555650
申请日:2009-09-08
申请人: Andrew M.K. Pennell , James B. Aggen , J.J. Kim Wright , Subhabrata Sen , Brian E. McMaster , Daniel Joseph Dairaghi , Wei Chen , Penglie Zhang
发明人: Andrew M.K. Pennell , James B. Aggen , J.J. Kim Wright , Subhabrata Sen , Brian E. McMaster , Daniel Joseph Dairaghi , Wei Chen , Penglie Zhang
IPC分类号: A61K31/655 , A61K31/551 , A61K31/5377 , A61K31/496 , A61K31/506 , A61K31/4709 , C07C245/04 , C07D413/14 , C07D473/00 , C07D403/14 , C07D401/14 , C07D403/12 , A61P37/06 , A61P29/00
CPC分类号: C07D403/04 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K45/06 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D231/38 , C07D231/56 , C07D233/61 , C07D235/06 , C07D235/16 , C07D249/08 , C07D249/14 , C07D257/04 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/04 , C07D407/04 , C07D409/04 , C07D413/04 , C07D413/12 , C07D417/04 , C07D471/04 , C07D473/34 , A61K2300/00
摘要: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
摘要翻译: 提供了作为CCR1受体的有效拮抗剂并具有体内抗炎活性的化合物。 化合物通常为芳基哌嗪衍生物,并且可用于药物组合物,用于治疗CCR1介导的疾病的方法,以及用于鉴定竞争性CCR1拮抗剂的测定中的对照。
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公开(公告)号:US07157464B2
公开(公告)日:2007-01-02
申请号:US10460752
申请日:2003-06-11
申请人: Andrew M. K. Pennell , James B. Aggen , J.J. Kim Wright , Subrabrata Sen , Brian E. McMaster , Daniel Joseph Dairaghi
发明人: Andrew M. K. Pennell , James B. Aggen , J.J. Kim Wright , Subrabrata Sen , Brian E. McMaster , Daniel Joseph Dairaghi
IPC分类号: C07D403/06 , C07D409/14 , A61K31/496
CPC分类号: C07D473/34 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D231/38 , C07D231/56 , C07D233/56 , C07D235/06 , C07D249/12 , C07D257/04 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D409/04
摘要: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
摘要翻译: 提供了作为CCR1受体的有效拮抗剂的化合物,并且在用于CCR1的标志性疾病状态之一的炎症的动物试验中进一步证实了这些化合物。 化合物通常为芳基哌嗪衍生物,并且可用于药物组合物,用于治疗CCR1介导的疾病的方法,以及用于鉴定竞争性CCR1拮抗剂的测定中的对照。
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公开(公告)号:US07449576B1
公开(公告)日:2008-11-11
申请号:US11491540
申请日:2006-07-21
申请人: Andrew M.K. Pennell , James B. Aggen , J.J. Kim Wright , Subrabrata Sen , Brian E. McMaster , Daniel Joseph Dairaghi
发明人: Andrew M.K. Pennell , James B. Aggen , J.J. Kim Wright , Subrabrata Sen , Brian E. McMaster , Daniel Joseph Dairaghi
IPC分类号: C07D401/12 , C07D403/12
CPC分类号: C07D473/34 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D231/38 , C07D231/56 , C07D233/56 , C07D235/06 , C07D249/12 , C07D257/04 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D409/04
摘要: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
摘要翻译: 提供了作为CCR1受体的有效拮抗剂的化合物,并且在用于CCR1的标志性疾病状态之一的炎症的动物试验中进一步证实了这些化合物。 化合物通常为芳基哌嗪衍生物,并且可用于药物组合物,用于治疗CCR1介导的疾病的方法,以及用于鉴定竞争性CCR1拮抗剂的测定中的对照。
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公开(公告)号:US20080261987A1
公开(公告)日:2008-10-23
申请号:US11491540
申请日:2006-07-21
申请人: Andrew M.K. Pennell , James B. Aggen , J.J. Kim Wright , Subrabrata Sen , Brian E. McMaster , Daniel Joseph Dairaghi
发明人: Andrew M.K. Pennell , James B. Aggen , J.J. Kim Wright , Subrabrata Sen , Brian E. McMaster , Daniel Joseph Dairaghi
IPC分类号: A61K31/53 , A61K31/506 , A61K31/501 , A61K31/496 , A61K31/495 , C07D403/02
CPC分类号: C07D473/34 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D231/38 , C07D231/56 , C07D233/56 , C07D235/06 , C07D249/12 , C07D257/04 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D409/04
摘要: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
摘要翻译: 提供了作为CCR1受体的有效拮抗剂的化合物,并且在用于CCR1的标志性疾病状态之一的炎症的动物试验中进一步证实了这些化合物。 化合物通常为芳基哌嗪衍生物,并且可用于药物组合物,用于治疗CCR1介导的疾病的方法,以及用于鉴定竞争性CCR1拮抗剂的测定中的对照。
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公开(公告)号:US07649011B2
公开(公告)日:2010-01-19
申请号:US10743281
申请日:2003-12-22
IPC分类号: A61K31/541 , A61K31/496 , C07D417/02
CPC分类号: C07D241/04 , C07C235/48 , C07C235/50 , C07D207/06 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/14 , C07D211/42 , C07D211/56 , C07D241/42 , C07D295/13 , C07D401/04 , C07D401/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14
摘要: Pharmaceutical compositions containing organic compounds or salts thereof that serve as modulators for the SDF-1 or I-TAC chemokines are disclosed. The compounds and compositions are useful in the treatment of cancer, especially in the inhibition of cancer proliferation, growth, and metastasis. Methods of interfering with SDF-1 and/or I-TAC binding to the CCXCKR2 receptor and treating cancer using the compounds and pharmaceutical compositions of the present invention are also disclosed.
摘要翻译: 公开了含有作为SDF-1或I-TAC趋化因子调节剂的有机化合物或其盐的药物组合物。 化合物和组合物可用于治疗癌症,特别是抑制癌细胞增殖,生长和转移。 还公开了使用本发明的化合物和药物组合物干扰SDF-1和/或I-TAC与CCXCKR2受体结合并治疗癌症的方法。
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公开(公告)号:US06992084B2
公开(公告)日:2006-01-31
申请号:US10279353
申请日:2002-10-23
IPC分类号: C07D401/12 , C07D401/14 , A61K31/472 , A61K31/4725 , A61P11/06
CPC分类号: C07D239/91
摘要: The invention provides compounds and compositions of the formula: wherein, the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl, R1 is a member selected from the group consisting of substituted or unsubstituted (C5–C15)alkyl and (C8–C14)acyl group; R2 is a member selected from the group consisting of substituted or unsubstituted (C1–C8)alkyl; each R3 is independently a substituent Y is a member selected from the group consisting of substituted or unsubstituted (C2–C8)alkylene and substituted or unsubstituted (C2–C8)heteroalkylene; Z is —NR4R5 R4 and R5 are independently selected from the group consisting of hydrogen and (C1–C8)alkyl or taken together with the nitrogen atom to which each is attached to form a heterocyclyl or heteroaryl; These compounds and compositions bind to the CXCR3 chemokine receptor and are useful for treating diseases and conditions responsive to the modulation of CXCR3 activity, such as multiple sclerosis, rheumatoid arthritis, psoriasis, cancer, infectious disease, angiogenesis, and graft rejection.
摘要翻译: 本发明提供下式的化合物和组合物:其中,下标n为0-4的整数; Ar是选自取代或未取代的芳基和取代或未取代的杂芳基的成员,R 1是选自取代或未取代的(C 5 H 5) -C 15 -C 15烷基和(C 8 -C 14 -C 14)酰基; R 2是选自取代或未取代的(C 1 -C 8 -C 8)烷基的成员; 每个R 3独立地是取代基Y是选自取代或未取代的(C 1 -C 12 -C 8)亚烷基和 取代或未取代的(C 2 -C 8 -C 8)杂亚烷基; Z是-NR 4 R 5,R 4和R 5独立地选自氢和 (C 1 -C 8 -C 8烷基)或与各自连接的氮原子一起形成杂环基或杂芳基; 这些化合物和组合物结合CXCR3趋化因子受体,并且可用于治疗对调节CXCR3活性如多发性硬化,类风湿性关节炎,牛皮癣,癌症,感染性疾病,血管生成和移植物排斥反应的疾病和病症。
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10.
公开(公告)号:US07101894B2
公开(公告)日:2006-09-05
申请号:US10233326
申请日:2002-08-29
CPC分类号: C07D207/08 , A61K31/075 , A61K31/135 , A61K31/4709 , C07D207/27 , C07D211/14 , C07D211/26 , C07D231/12 , C07D241/04 , C07D295/088 , C07D295/096 , C07D295/135 , C07D295/155 , C07D453/04
摘要: Methods for treating CMV or a CMV-related disease are provided that use compounds having the formula: wherein Ar is a substituted or unsubstituted 5–14 membered heteroaryl group having from 1 to 5 heteroatoms as ring members; R1 is selected from the group consisting of substituted or unsubstituted aryl(C1–C4)alkyl, heteroaryl(C1–C4)alkyl, —C(O)R11, and —C(O)NR11R12, wherein each R11 and R12 independently is substituted or unsubstituted aryl, substituted or unsubstituted aryl(C1–C4)alkyl, substituted or unsubstituted (C4–C8)cycloalkyl(C1–C4)alkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroaryl(C1–C4)alkyl and substituted or unsubstituted hetero(C4–C8)cycloalkyl(C1–C4)alkyl; R2 is H or (C1–C8)alkyl; and ZN is a substituted or unsubstituted hetero(C6–C10)bicycloalkyl group.
摘要翻译: 提供了使用具有下式的化合物治疗CMV或CMV相关疾病的方法:其中Ar是具有1至5个杂原子作为环成员的取代或未取代的5-14元杂芳基; R 1选自取代或未取代的芳基(C 1 -C 4 -C 4)烷基,杂芳基(C 1 H 4) -C(O)R 11和-C(O)NR 11 R 12 > 12,其中每个R 11和R 12独立地是取代或未取代的芳基,取代或未取代的芳基(C 1〜 C 1 -C 4烷基,取代或未取代的(C 1 -C 4 -C 8)环烷基(C 1 -C 4 - 取代或未取代的杂芳基,取代或未取代的杂芳基(C 1 -C 4 -C 4)烷基和取代或未取代的杂原子(C
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