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1.发明申请公开(公告)号：US20080200454A1
公开(公告)日：2008-08-21
申请号：US12031010
申请日：2008-02-14
申请人： Michael K. Ameriks , Frank U. Axe , James P. Edwards , Cheryl A. Grice , Hui Cai , Elizabeth Ann Gleason , Steven P. Meduna , Kevin L. Tays , John J. M. Wiener , Alvah T. Wickboldt
发明人： Michael K. Ameriks , Frank U. Axe , James P. Edwards , Cheryl A. Grice , Hui Cai , Elizabeth Ann Gleason , Steven P. Meduna , Kevin L. Tays , John J. M. Wiener , Alvah T. Wickboldt
IPC分类号： A61K31/437 , A61P37/00 , A61P29/00 , A61P1/00 , A61P25/00 , A61P35/00 , A61K31/496 , A61K31/541 , A61K31/55 , A61P17/00 , A61P3/10 , A61P11/00 , C07D471/04 , A61K31/53
CPC分类号： C07D471/04 , C07D519/00
摘要： Carbon-linked tetrahydro-pyrazolo-pyridine compounds are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis.
摘要翻译： 描述了碳连接的四氢 - 吡唑并 - 吡啶化合物，其可用作组织蛋白酶S调节剂。 这些化合物可用于治疗由组织蛋白酶S活性介导的疾病状态，病症和病症的药物组合物和方法，例如银屑病，疼痛，多发性硬化，动脉粥样硬化和类风湿性关节炎。
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2.发明申请公开(公告)号：US20090111867A1
公开(公告)日：2009-04-30
申请号：US12336274
申请日：2008-12-16
IPC分类号： A61K31/4035 , C07D403/04 , A61P11/06 , A61P11/00
CPC分类号： C07D413/14 , C07D209/46 , C07D403/04 , C07D405/14 , C07D417/04 , C07D417/14
摘要： The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.
摘要翻译： 本发明涉及作为CRTH2受体拮抗剂的吲哚乙酸化合物。 本发明还涉及这些化合物用于抑制前列腺素D2及其代谢物或某些血栓烷代谢物与CRTH2受体的结合并治疗对这种抑制作用的病症的用途。
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3.发明授权Indole acetic acids exhibiting CRTH2 receptor antagonism and uses thereof 失效表现出CRTH2受体拮抗作用的吲哚乙酸及其应用公开(公告)号：US07981912B2
公开(公告)日：2011-07-19
申请号：US12566566
申请日：2009-09-24
IPC分类号： A61K31/425 , C07D275/06 , C07D417/04
CPC分类号： C07D413/14 , C07D209/46 , C07D403/04 , C07D405/14 , C07D417/04 , C07D417/14
摘要： The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.
摘要翻译： 本发明涉及作为CRTH2受体拮抗剂的吲哚乙酸化合物。 本发明还涉及这些化合物用于抑制前列腺素D2及其代谢物或某些血栓烷代谢物与CRTH2受体的结合并治疗对这种抑制作用的病症的用途。
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公开(公告)号：US20110092481A1
公开(公告)日：2011-04-21
申请号：US12988891
申请日：2009-04-21
申请人： Christopher John Love , Joseph Elisabeth Leenaerts , Ludwig Paul Cooymans , Donald Alec Labsack , Bryan James Branstetter , Jason Christopher Rech , Elizabeth Ann Gleason , Jennifer Diane Venable , Danielle Wiener , Deborah Margaret Smith , James Guy Breitenbucher
发明人： Christopher John Love , Joseph Elisabeth Leenaerts , Ludwig Paul Cooymans , Donald Alec Labsack , Bryan James Branstetter , Jason Christopher Rech , Elizabeth Ann Gleason , Jennifer Diane Venable , Danielle Wiener , Deborah Margaret Smith , James Guy Breitenbucher
IPC分类号： A61K31/4709 , C07D401/14 , C07D413/14 , A61K31/553 , A61K31/55 , A61K31/5377 , A61K31/506 , A61K31/496 , A61K31/4725 , A61P43/00
CPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/08
摘要： The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans. (I)
摘要翻译： 本发明涉及具有P2X7拮抗性质的新型式（I）化合物，包含这些化合物的药物组合物，用于制备这些化合物的化学方法及其用于治疗或预防与动物中P2X7受体活性有关的疾病的用途，特别是 人类。 （一世）
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5.发明授权Benzimidazole acetic acids exhibiting CRTH2 receptor antagonism and uses thereof 失效显示CRTH2受体拮抗作用的苯并咪唑乙酸及其应用公开(公告)号：US07732618B2
公开(公告)日：2010-06-08
申请号：US11230916
申请日：2005-09-21
IPC分类号： A61K31/4184 , C07D235/04
CPC分类号： C07D405/12 , C07D235/06 , C07D235/08 , C07D235/14 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12
摘要： The invention relates to benzimidazole acetic acid compounds which function as antagonists of the Chemoattractant Receptor-homologous molecule expressed on T-Helper type 2 cells (CRTH2) receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.
摘要翻译： 本发明涉及作为T-Helper 2型细胞（CRTH2）受体上表达的化学引诱物受体同源分子的拮抗剂的苯并咪唑乙酸化合物。 本发明还涉及这些化合物用于抑制前列腺素D2及其代谢物或某些血栓烷代谢物与CRTH2受体的结合并治疗对这种抑制作用的病症的用途。
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6.发明申请公开(公告)号：US20100016389A1
公开(公告)日：2010-01-21
申请号：US12566566
申请日：2009-09-24
IPC分类号： A61K31/427 , C07D417/04
CPC分类号： C07D413/14 , C07D209/46 , C07D403/04 , C07D405/14 , C07D417/04 , C07D417/14
摘要： The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.
摘要翻译： 本发明涉及作为CRTH2受体拮抗剂的吲哚乙酸化合物。 本发明还涉及这些化合物用于抑制前列腺素D2及其代谢物或某些血栓烷代谢物与CRTH2受体的结合并治疗对这种抑制作用的病症的用途。
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7.发明申请BENZIMIDAZOLE ACETIC ACIDS EXHIBITING CRTH2 RECEPTOR ANTAGONISM AND USES THEREOF 审中-公开苯并咪唑乙酸显示CRTH2受体拮抗剂及其用途公开(公告)号：US20110105573A1
公开(公告)日：2011-05-05
申请号：US12796050
申请日：2010-06-08
IPC分类号： A61K31/4184 , C12N5/071 , C07D235/08 , C07D235/16 , C07D417/12 , C07D405/12 , C07D413/12 , C07D409/12 , A61K31/427 , A61K31/422 , A61K31/428 , A61P11/06 , A61P11/00 , A61P11/08 , A61P11/02 , A61P11/14 , A61P17/00 , A61P17/06 , A61P17/02 , A61P1/00 , A61P37/08 , A61P25/28 , A61P25/00 , A61P25/06 , A61P9/10 , A61P31/18 , A61P37/02 , A61P3/10 , A61P31/08 , A61P1/16 , A61P13/12 , A61P37/06
CPC分类号： C07D405/12 , C07D235/06 , C07D235/08 , C07D235/14 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12
摘要： The invention relates to benzimidazole acetic acid compounds which function as antagonists of the Chemoattractant Receptor-homologous molecule expressed on T-Helper type 2 cells (CRTH2) receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.
摘要翻译： 本发明涉及作为T-Helper 2型细胞（CRTH2）受体上表达的化学引诱物受体同源分子的拮抗剂的苯并咪唑乙酸化合物。 本发明还涉及这些化合物用于抑制前列腺素D2及其代谢物或某些血栓烷代谢物与CRTH2受体的结合并治疗对这种抑制作用的病症的用途。
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8.发明授权Indole acetic acids exhibiting CRTH2 receptor antagonism and uses thereof 失效表现出CRTH2受体拮抗作用的吲哚乙酸及其应用公开(公告)号：US07405215B2
公开(公告)日：2008-07-29
申请号：US11230917
申请日：2005-09-21
IPC分类号： C07D417/04 , C07D413/04 , C07D403/04 , A61K31/501
CPC分类号： C07D413/14 , C07D209/46 , C07D403/04 , C07D405/14 , C07D417/04 , C07D417/14
摘要： The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.
摘要翻译： 本发明涉及作为CRTH2受体拮抗剂的吲哚乙酸化合物。 本发明还涉及这些化合物用于抑制前列腺素D 2和其代谢物或某些血栓烷代谢物与CRTH2受体的结合以及治疗对这种抑制作用的病症的结合的用途。
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公开(公告)号：US08431704B2
公开(公告)日：2013-04-30
申请号：US12988891
申请日：2009-04-21
申请人： Christopher John Love , Joseph Elisabeth Leenaerts , Ludwig Paul Cooymans , Donald Alec Lebsack , Bryan James Branstetter , Jason Christopher Rech , Elizabeth Ann Gleason , Jennifer Diane Venable , Danielle Wiener , Deborah Margaret Smith , James Guy Breitenbucher
发明人： Christopher John Love , Joseph Elisabeth Leenaerts , Ludwig Paul Cooymans , Donald Alec Lebsack , Bryan James Branstetter , Jason Christopher Rech , Elizabeth Ann Gleason , Jennifer Diane Venable , Danielle Wiener , Deborah Margaret Smith , James Guy Breitenbucher
IPC分类号： C07D215/38
CPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/08
摘要： The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans. (I).
摘要翻译： 本发明涉及具有P2X7拮抗性质的新型式（I）化合物，包含这些化合物的药物组合物，用于制备这些化合物的化学方法及其用于治疗或预防与动物中P2X7受体活性有关的疾病的用途，特别是 人类。 （一世）。
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10.发明授权Indole acetic acids exhibiting CRTH2 receptor antagonism and uses thereof 失效表现出CRTH2受体拮抗作用的吲哚乙酸及其应用公开(公告)号：US07601749B2
公开(公告)日：2009-10-13
申请号：US12336274
申请日：2008-12-16
IPC分类号： C07D417/04 , C07D413/04 , C07D403/04 , A61K31/501
CPC分类号： C07D413/14 , C07D209/46 , C07D403/04 , C07D405/14 , C07D417/04 , C07D417/14
摘要： The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.
摘要翻译： 本发明涉及作为CRTH2受体拮抗剂的吲哚乙酸化合物。 本发明还涉及这些化合物用于抑制前列腺素D2及其代谢物或某些血栓烷代谢物与CRTH2受体的结合并治疗对这种抑制作用的病症的用途。
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