公开(公告)号：US20130005741A1

公开(公告)日：2013-01-03

申请号：US13610005

申请日：2012-09-11

Applicant: Keith John HARRIS ,  Joacy C. AGUIAR ,  Patrick Wai-Kwok SHUM ,  Zhicheng ZHAO ,  Gregory B. POLI ,  Gregory T. STOKLOSA ,  Yong-Mi CHOI-SLEDESKI ,  Stephan REILING

Inventor： Keith John HARRIS ,  Joacy C. AGUIAR ,  Patrick Wai-Kwok SHUM ,  Zhicheng ZHAO ,  Gregory B. POLI ,  Gregory T. STOKLOSA ,  Yong-Mi CHOI-SLEDESKI ,  Stephan REILING

IPC: C07D401/04 ,  A61P37/08 ,  A61P11/06 ,  A61P11/02 ,  A61P3/10 ,  A61P27/02 ,  A61P27/14 ,  A61P11/00 ,  A61P9/10 ,  A61P3/06 ,  A61K31/506 ,  A61P17/00

CPC classification number: C07D403/04

Abstract: The present invention is directed to a 2,6-substituted-4-monosubstitutedamino-pyrimidine compound of formula (I): or an enantiomer thereof, or an ester prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such a compound. The invention also includes a method of treatment of a patient by the administration of a pharmaceutically effective amount of such a compound.

Abstract translation: 本发明涉及式（I）的2,6-取代-4-单取代氨基嘧啶化合物或其对映异构体或其酯前药或其药学上可接受的盐，或包含这种化合物的药物组合物。 本发明还包括通过施用药学有效量的这种化合物来治疗患者的方法。

公开(公告)号：US20090176804A1

公开(公告)日：2009-07-09

申请号：US12357725

申请日：2009-01-22

Applicant: Zhaoxia YANG ,  Stephan REILING ,  Thaddeus NIEDUZAK ,  Rose M. MATHEW ,  Sharon JACKSON ,  Keith John HARRIS

Inventor： Zhaoxia YANG ,  Stephan REILING ,  Thaddeus NIEDUZAK ,  Rose M. MATHEW ,  Sharon JACKSON ,  Keith John HARRIS

IPC: A61K31/404 ,  C07D209/18 ,  C07D209/20 ,  C07D257/06 ,  A61K31/41 ,  A61P17/00 ,  A61P37/08 ,  A61K31/496 ,  A61K31/435

CPC classification number: C07D209/18

Abstract: The present invention is directed to 2-phenyl-indole compounds, their preparation, pharmaceutical compositions containing these compounds, and their pharmaceutical use in treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, eczema, urticaria diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which are generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like.

Abstract translation: 本发明涉及2-苯基 - 吲哚化合物，其制备方法，含有这些化合物的药物组合物及其在治疗患有PGD2介导的病症的患者中的药物用途，包括但不限于过敏性疾病（如过敏性疾病 鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），全身肥大细胞增多症，伴有系统性肥大细胞活化的疾病，过敏性休克，支气管收缩，支气管炎，湿疹，伴有瘙痒的荨麻疹（如特应性皮炎和荨麻疹） （如白内障，视网膜脱离，炎症，感染和睡眠障碍），其由于伴随瘙痒的行为（例如划伤和打浆），炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，慢性 类风湿性关节炎，胸膜炎，溃疡性结肠炎等。

公开(公告)号：US07516018B2

公开(公告)日：2009-04-07

申请号：US10206387

申请日：2002-07-25

Applicant: Stephan Reiling

Inventor： Stephan Reiling

IPC: G06F19/00 ,  C40B30/02

CPC classification number: G06F19/707

Abstract: A computer implemented method is disclosed for analyzing a large data set of chemical compounds for which there is a measured activity in the same assay for each compound to determine the structural units which are responsible for the observed activity of the compounds.

Abstract translation: 公开了一种计算机实现的方法，用于分析在每种化合物的相同测定中具有测量活性的大量数据化合物，以确定负责观察到的化合物的活性的结构单元。

公开(公告)号：US20130005728A1

公开(公告)日：2013-01-03

申请号：US13610027

申请日：2012-09-11

Applicant: Keith J. HARRIS ,  Joacy C. AGUIAR ,  Patrick Wai-Kwok SHUM ,  Zhicheng ZHAO ,  Gregory B. POLI ,  Gregory STOKLOSA ,  Yong-Mi CHOI-SLEDESKI ,  Stephan REILING ,  David STEFANY ,  Charles GARDNER

Inventor： Keith J. HARRIS ,  Joacy C. AGUIAR ,  Patrick Wai-Kwok SHUM ,  Zhicheng ZHAO ,  Gregory B. POLI ,  Gregory STOKLOSA ,  Yong-Mi CHOI-SLEDESKI ,  Stephan REILING ,  David STEFANY ,  Charles GARDNER

IPC: C07D403/04 ,  A61K31/5377 ,  A61K31/506 ,  C07D401/04 ,  A61P37/08 ,  A61P11/06 ,  A61P11/02 ,  A61P17/00 ,  A61P27/02 ,  A61P27/14 ,  A61P11/00 ,  A61P9/10 ,  A61P3/06 ,  A61P3/10 ,  C07D413/04

CPC classification number: C07D403/04

Abstract: The present invention is directed to a substituted pyrimidine compound of formula (I) or an enantiomer thereof, or a prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such a compound. The invention also includes a method of treatment of a patient by the administration of a pharmaceutically effective amount of such a compound.

Abstract translation: 本发明涉及式（I）的取代嘧啶化合物或其对映异构体或其前药或药学上可接受的盐，或包含该化合物的药物组合物。 本发明还包括通过施用药学有效量的这种化合物来治疗患者的方法。