公开(公告)号：US07879875B2

公开(公告)日：2011-02-01

申请号：US11990050

申请日：2006-08-08

申请人： Meng-Hsin Chen ,  James B. Doherty ,  Robert Tynebor ,  Swaminathan R. Natarajan ,  Zhen Li ,  Soumya P. Sahoo

发明人： Meng-Hsin Chen ,  James B. Doherty ,  Robert Tynebor ,  Swaminathan R. Natarajan ,  Zhen Li ,  Soumya P. Sahoo

IPC分类号： A61K31/4375 ,  C07D455/02

CPC分类号： C07D471/04

摘要： Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (I) are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.

摘要翻译： 由化学式（I）或其药学上可接受的盐描述的化合物：（I）是p38的抑制剂，可用于治疗炎症，例如治疗类风湿性关节炎，类风湿性脊椎炎，骨关节炎，痛风性关节炎和其他关节炎病症 ; 发炎关节，湿疹，牛皮癣或其他炎症皮肤病如晒伤; 炎症性眼病，包括结膜炎; 皮肤炎，疼痛等与炎症有关的病症。

公开(公告)号：US10336733B2

公开(公告)日：2019-07-02

申请号：US15767371

申请日：2016-11-28

申请人： Merck Sharp & Dohme Corp. ,  Yongxin Han ,  Jongwon Lim ,  Satyanarayana Tummanapalli ,  Phieng Siliphaivanh ,  Kerrie Spencer

发明人： Yongxin Han ,  Jongwon Lim ,  Satyanarayana Tummanapalli ,  Phieng Siliphaivanh ,  Kerrie Spencer

IPC分类号： C07D417/06 ,  C07D413/06 ,  C07D311/22 ,  C07D405/06 ,  A61K31/353 ,  A61K9/20

摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatoepatitis, metabolic syndrome, atherosclerosis, and cancer.

公开(公告)号：US08362005B2

公开(公告)日：2013-01-29

申请号：US13062540

申请日：2009-08-31

申请人： Ian M. Bell ,  Howard G. Selnick

发明人： Ian M. Bell ,  Howard G. Selnick

IPC分类号： C07D403/14 ,  C07D409/14 ,  C07D401/14 ,  A61K31/553 ,  A61K31/537 ,  A61P25/00 ,  A61P25/06

CPC分类号： C07D471/04 ,  C07D417/14 ,  C07D471/10

摘要： Compounds of formula (I): wherein variables B, m, n, J, R4, Ea, Eb, Ec, Re, Rf, RPG and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

摘要翻译： 式（I）化合物：其中变量B，m，n，J，R4，Ea，Eb，Ec，Re，Rf，RPb和Ec如本文所述，其是CGRP受体的拮抗剂，其可用于治疗 或预防CGRP涉及的疾病，如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。

公开(公告)号：US20140088937A1

公开(公告)日：2014-03-27

申请号：US14091459

申请日：2013-11-27

申请人： Duncan Brown ,  Julja Burchard ,  Eugen C. Buehler

发明人： Duncan Brown ,  Julja Burchard ,  Eugen C. Buehler

IPC分类号： G06F19/12

CPC分类号： G16B5/00 ,  G16B20/00

摘要： The present invention provides a method for determining the probability that an RNAi compound modulates the expression level of a gene using a linear regression model. The present invention also provides a method for determining the probabilities that an RNAi compound modulates the expression levels of each gene in a set of genes of interest using the linear regression model. The present invention provides a method for determining the seed-sequence-dependent signature size of an RNAi compound using the linear regression model. The invention provides a method for identifying genes having seed-sequence-dependent silencing effect by an siRNA using the linear regression model. The invention further provides a method for selecting from a plurality of siRNAs one or more siRNAs with higher silencing efficacy, specificity and diversity in silencing a target gene in an organism. The invention also provides a method for determining the coefficients of the above linear regression model.

摘要翻译： 本发明提供了使用线性回归模型确定RNAi化合物调节基因表达水平的可能性的方法。 本发明还提供了使用线性回归模型确定RNAi化合物调节一组感兴趣基因中的每个基因的表达水平的概率的方法。 本发明提供了使用线性回归模型确定RNAi化合物的种子序列依赖性特征大小的方法。 本发明提供一种使用线性回归模型鉴定siRNA的具有种子序列依赖性沉默效应的基因的方法。 本发明还提供了从多个siRNA中选择一种或多种沉默效力，特异性和沉默生物体中靶基因多样性的siRNA的方法。 本发明还提供了一种用于确定上述线性回归模型的系数的方法。

公开(公告)号：US08168649B2

公开(公告)日：2012-05-01

申请号：US11922629

申请日：2006-06-26

申请人： Subharekha Raghavan ,  Steven L. Colletti ,  Fa-Xiang Ding ,  Hong Shen ,  James R. Tata ,  Ashley Rouse Lins ,  Abigail Lee Smenton ,  Weichun Chen ,  Darby Rye Schmidt ,  George Scott Tria

发明人： Subharekha Raghavan ,  Steven L. Colletti ,  Fa-Xiang Ding ,  Hong Shen ,  James R. Tata ,  Ashley Rouse Lins ,  Abigail Lee Smenton ,  Weichun Chen ,  Darby Rye Schmidt ,  George Scott Tria

IPC分类号： A61K31/44 ,  A01N43/40 ,  A61K31/19 ,  A61K31/165

CPC分类号： C07D261/20 ,  C07C233/52 ,  C07C233/55 ,  C07C235/36 ,  C07C237/20 ,  C07C2601/10 ,  C07C2601/16 ,  C07D231/12 ,  C07D249/06 ,  C07D249/08 ,  C07D257/04 ,  C07D271/06 ,  C07D277/30 ,  C07D307/79 ,  C07D309/14 ,  C07D309/28 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04 ,  C07D513/04

摘要： The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.

摘要翻译： 本发明包括可用于治疗动脉粥样硬化，血脂异常等的式（I）化合物及其药学上可接受的盐和水合物。 还包括药物组合物和使用方法。