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公开(公告)号：US20150239866A1
公开(公告)日：2015-08-27
申请号：US14431895
申请日：2013-09-24
申请人： Michelle R. MACHACEK , Eric T. ROMEO , Solomon D. KATTAR , Matthew CHRISTOPHER , Michael D. ALTMAN , Alan B. NORTHRUP , John Michael ELLIS , Brendan O BOYLE , Anthony DONOFRIO , Jonathan GRIMM , Michael H. REUTERSHAN , Kaleen Konrad CHILDERS , Ryan D. OTTE , Brandon CASH , Yves DUCHARME , Andrew M. HAIDLE , Kerrie SPENCER , Dilrukshi VITHARANA , Lingyun WU , Li ZHANG , Peng ZHANG , Christian BEAULIEU , Daniel GUAY
发明人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
IPC分类号： C07D401/14 , C07D471/04 , C07D405/14 , C07D413/14 , C07D498/04 , C07D409/14 , C07D417/14
CPC分类号： C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要： Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译： 提供式I的三唑衍生物，其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。 三唑衍生物可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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公开(公告)号：US09586931B2
公开(公告)日：2017-03-07
申请号：US14431895
申请日：2013-09-24
申请人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
发明人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
IPC分类号： A61K9/10 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D498/04 , C07D413/14 , C07D239/42 , A61K9/00 , A61K9/20 , A61K9/48 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04
CPC分类号： C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要： Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译： 提供式I的三唑衍生物，其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。 三唑衍生物可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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3.发明申请公开(公告)号：US20160326156A1
公开(公告)日：2016-11-10
申请号：US15105316
申请日：2014-12-18
申请人： Thomas A. MILLER , Alessia PETROCCHI , Eric T. ROMEO , Dilrukshi VITHARANA , Solomon D. KATTAR , Alan B. NORTHRUP , Michael D. ALTMAN , Neville J. ANTHONY , MERCK SHARP & DOHME CORP.
发明人： Thomas A. Miller , Alessia Petrocchi , Eric T. Romeo , Dilrukshi Vitharana , Solomon D. Kattar , Alan B. Northrup , Michael D. Altman , Neville J. Anthony
IPC分类号： C07D417/12 , C07D495/04 , A61K31/437 , C07D471/04 , A61K31/444 , C07D491/048 , A61K31/517 , A61K31/519
CPC分类号： C07D417/12 , A61K31/437 , A61K31/444 , A61K31/517 , A61K31/519 , C07D413/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04
摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring A, and the subscripts n1, n2, and r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
摘要翻译： 本发明提供了式（I）（I）的某些噻唑取代的氨基杂芳基化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，环A和下标n 1，n 2和r如上定义 这里。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）介导的疾病或病症的方法。
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公开(公告)号：US07138543B2
公开(公告)日：2006-11-21
申请号：US10819146
申请日：2004-04-07
IPC分类号： C07C321/06 , C07C323/04 , A61K31/19 , A61K31/185 , A61K31/195
CPC分类号： C07C323/62 , C07C323/56 , C07C323/58
摘要： The present invention relates to new thiolalkyl benzoic acids, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-β activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers, glaucoma, retinal disorders, and cancer.
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公开(公告)号：US08101604B2
公开(公告)日：2012-01-24
申请号：US12859312
申请日：2010-08-19
IPC分类号： A61K31/437
CPC分类号： C07D471/04
摘要： This invention provides alpha-carboline compounds of formula I: wherein R1, R2, R3, R4, R5, and x are as described in the specification. The compounds are useful for treating inflammatory diseases and cancer.
摘要翻译： 本发明提供了式I的α-咔啉化合物：其中R1，R2，R3，R4，R5和x如说明书中所述。 该化合物可用于治疗炎性疾病和癌症。
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公开(公告)号：US06740777B2
公开(公告)日：2004-05-25
申请号：US10156880
申请日：2002-05-30
IPC分类号： C02C32100
CPC分类号： C07C323/62 , C07C323/56 , C07C323/58
摘要： The present invention relates to new thiolalkyl benzoic acids, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers, glaucoma, retinal disorders, and cancer.
摘要翻译： 本发明涉及新的硫醇烷基苯甲酸，包含这些化合物的药物组合物和诊断试剂，以及使用这些化合物抑制NAALADase酶活性的方法，检测其中NAALADase水平被改变，影响神经元活性，影响TGF-β活性，抑制 血管生成和治疗谷氨酸异常，神经病，疼痛，强迫症，前列腺疾病，癌症，青光眼，视网膜疾病和癌症。
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公开(公告)号：US20100311715A1
公开(公告)日：2010-12-09
申请号：US12859312
申请日：2010-08-19
IPC分类号： A61K31/437 , C12N9/99 , A61K31/5377 , A61K31/506 , C07D413/06 , C07D471/04 , C07D401/04 , C07D403/06 , C07D209/34 , A61P35/00 , A61P35/04 , A61P29/00 , A61P37/00 , A61P11/06 , A61P17/06 , A61P1/00
CPC分类号： C07D471/04
摘要： This invention provides alpha-carboline compounds of formula I: wherein R1, R2, R3, R4, R5, and x are as described in the specification. The compounds are useful for treating inflammatory diseases and cancer.
摘要翻译： 本发明提供了式I的α-咔啉化合物：其中R1，R2，R3，R4，R5和x如说明书中所述。 该化合物可用于治疗炎性疾病和癌症。
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公开(公告)号：US07812018B2
公开(公告)日：2010-10-12
申请号：US11706760
申请日：2007-02-15
IPC分类号： A61K31/437 , C07D413/14 , C07D471/06
CPC分类号： C07D471/04
摘要： This invention provides alpha-carboline compounds of formula I: wherein R1, R2, R3, R4, R5, and x are as described in the specification. The compounds are useful for treating inflammatory diseases and cancer.
摘要翻译： 本发明提供了式I的α-咔啉化合物：其中R1，R2，R3，R4，R5和x如说明书中所述。 该化合物可用于治疗炎性疾病和癌症。
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公开(公告)号：US20070207997A1
公开(公告)日：2007-09-06
申请号：US11706760
申请日：2007-02-15
申请人： Michael Hepperle , Julie Liu , R. Rowland , Dilrukshi Vitharana
发明人： Michael Hepperle , Julie Liu , R. Rowland , Dilrukshi Vitharana
IPC分类号： A61K31/55 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： This invention provides alpha-carboline compounds of formula I: wherein R1, R2, R3, R4, R5, and x are as described in the specification. The compounds are useful for treating inflammatory diseases and cancer.
摘要翻译： 本发明提供了式I的α-咔啉化合物：其中R 1，R 2，R 3，R 4， >，R 5，和x如说明书中所述。 该化合物可用于治疗炎性疾病和癌症。
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