公开(公告)号：US07786149B2

公开(公告)日：2010-08-31

申请号：US11861870

申请日：2007-09-26

Applicant: Purakkattle J. Biju ,  Arthur G. Taveras ,  J. Robert Merritt ,  John J. Baldwin ,  Younong Yu ,  Junying Zheng ,  Jianhua Chao ,  Cynthia J. Aki

Inventor： Purakkattle J. Biju ,  Arthur G. Taveras ,  J. Robert Merritt ,  John J. Baldwin ,  Younong Yu ,  Junying Zheng ,  Jianhua Chao ,  Cynthia J. Aki

IPC: C07D285/06 ,  A01N43/82

CPC classification number: C07D285/10 ,  C07D285/06 ,  C07D417/12 ,  C07D417/14

Abstract: Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.

Abstract translation: 公开了下式的新化合物及其药学上可接受的盐和溶剂合物。 包含取代基A的基团的实例包括杂芳基，芳基，杂环烷基，环烷基，芳基，炔基，烯基，氨基烷基，烷基或氨基。 包含取代基B的基团的实例包括芳基和杂芳基。 还公开了治疗趋化因子介导的疾病，例如癌症，血管生成，血管生成性眼部疾病，肺部疾病，多发性硬化，类风湿性关节炎，骨关节炎，中风和缺血再灌注损伤，疼痛（例如急性疼痛，急性和慢性 炎性疼痛和神经性疼痛），使用式IA化合物。

公开(公告)号：US20100152138A1

公开(公告)日：2010-06-17

申请号：US12641952

申请日：2009-12-18

Applicant: Jared N. Cumming ,  Ulrich Iserloh ,  Andrew Stamford ,  Corey Strickland ,  Johannes H. Voigt ,  Yusheng Wu ,  Ying Huang ,  Yan Xia ,  Samuel Chackalamannil ,  Tao Guo ,  Douglas W. Hobbs ,  Thuy X.H. Le ,  Jeffrey F. Lowrie ,  Kurt W. Saionz ,  Suresh D. Babu

Inventor： Jared N. Cumming ,  Ulrich Iserloh ,  Andrew Stamford ,  Corey Strickland ,  Johannes H. Voigt ,  Yusheng Wu ,  Ying Huang ,  Yan Xia ,  Samuel Chackalamannil ,  Tao Guo ,  Douglas W. Hobbs ,  Thuy X.H. Le ,  Jeffrey F. Lowrie ,  Kurt W. Saionz ,  Suresh D. Babu

IPC: A61K31/4015 ,  C07D207/12 ,  C07D217/24 ,  C07D413/12 ,  C07D243/08 ,  A61K31/47 ,  A61K31/675 ,  A61K31/397 ,  A61K31/5377 ,  A61K31/551 ,  A61P25/28

CPC classification number: C07D243/08 ,  C07D205/04 ,  C07D207/08 ,  C07D207/09 ,  C07D207/12 ,  C07D207/26 ,  C07D209/52 ,  C07D211/26 ,  C07D211/46 ,  C07D217/18 ,  C07D233/32 ,  C07D241/04 ,  C07D241/08 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06

Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification.Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

Abstract translation: 公开了下式的化合物或其药学上可接受的盐或溶剂化物，其中R1是R是-C（O）-N（R27）（R28），或其余的变量如说明书中所定义。 还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。 还公开了治疗认知或神经变性疾病的药物组合物和方法，其包含式I化合物与除式I以外的分泌抑制剂抑制剂，HMG-CoA还原酶抑制剂，γ-分泌酶抑制剂，非 - 甾族抗炎药，N-甲基-D-天冬氨酸受体拮抗剂，胆碱酯酶抑制剂或抗淀粉样蛋白抗体。

公开(公告)号：US20100136620A1

公开(公告)日：2010-06-03

申请号：US12621241

申请日：2009-11-18

Applicant: Shahriar Shane Taremi ,  Gaolian Xie ,  Thomas Hesson ,  Jose S. Duca ,  Corey Strickland ,  William T. Windsor ,  Vincent S. Madison ,  Rumin Zhang ,  Paul Reichert ,  Yaolin Wang

Inventor： Shahriar Shane Taremi ,  Gaolian Xie ,  Thomas Hesson ,  Jose S. Duca ,  Corey Strickland ,  William T. Windsor ,  Vincent S. Madison ,  Rumin Zhang ,  Paul Reichert ,  Yaolin Wang

IPC: C12P21/00 ,  C07H21/04 ,  C12N15/63 ,  C12N1/21

CPC classification number: C07H21/04 ,  C07D209/20 ,  C07K14/47 ,  C07K2299/00

Abstract: The present invention discloses modified Hdm2 proteins that are soluble. In addition, the present invention discloses nucleic acids that encode the modified Hdm2 proteins of the present invention. The invention also provides crystals of modified Hdm2 proteins that are suitable for X-ray crystallization analysis. The present invention also discloses methods of using the modified Hdm2 proteins and crystals thereof to identify, select and/or design compounds that may be used as anticancer agents. The present invention further discloses compounds that bind to modified Hdm2 proteins in protein-ligand complexes.

Abstract translation: 本发明公开了可溶性的修饰的Hdm2蛋白。 此外，本发明公开了编码本发明的修饰的Hdm2蛋白质的核酸。 本发明还提供了适用于X射线结晶分析的修饰的Hdm2蛋白晶体。 本发明还公开了使用修饰的Hdm2蛋白及其晶体鉴定，选择和/或设计可用作抗癌剂的化合物的方法。 本发明还公开了与蛋白质 - 配体复合物中的修饰的Hdm2蛋白结合的化合物。

公开(公告)号：US07192944B2

公开(公告)日：2007-03-20

申请号：US10791979

申请日：2004-03-03

Applicant: Duane A. Burnett ,  John W. Clader

Inventor： Duane A. Burnett ,  John W. Clader

IPC: C07D205/08 ,  A61K31/397 ,  A61K31/7052 ,  A61P3/06 ,  C07H7/02

CPC classification number: C07D405/12 ,  Y10S930/28

Abstract: The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as specified herein, formulations including the above compounds, processes for preparing the same and methods for treating vascular conditions, such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols.

公开(公告)号：US5601815A

公开(公告)日：1997-02-11

申请号：US531994

申请日：1995-09-21

Applicant: Fiona Powrie ,  Robert Coffman

Inventor： Fiona Powrie ,  Robert Coffman

IPC: A61K38/00 ,  A61K38/20 ,  C07K16/24 ,  A61K45/05

CPC classification number: C07K16/247 ,  A61K38/2026 ,  A61K38/2066

Abstract: The invention provides in vivo methods for potentiating IL-10 mediated inhibition of cytokine production by T cells in a mammal. The method comprises co-administering to the mammal an effective amount of IL-4 and IL-10, preferably intravascularly.

Abstract translation: 本发明提供用于增强IL-10介导的抑制哺乳动物中T细胞产生细胞因子的体内方法。 该方法包括向哺乳动物施用有效量的IL-4和IL-10，优选血管内给药。

公开(公告)号：US5283359A

公开(公告)日：1994-02-01

申请号：US030185

申请日：1993-03-01

Applicant: Chou-Hong Tann ,  T. K. Thiruvengadam ,  John Chiu ,  Michael Green ,  Timothy L. McAllister ,  Cesar Colon ,  Junning Lee

Inventor： Chou-Hong Tann ,  T. K. Thiruvengadam ,  John Chiu ,  Michael Green ,  Timothy L. McAllister ,  Cesar Colon ,  Junning Lee

IPC: C07D317/30 ,  C07C20060101 ,  C07C45/64 ,  C07C49/82 ,  C07C49/84 ,  C07C59/64 ,  C07C65/32 ,  C07C65/40 ,  C07C69/76 ,  C07C69/84 ,  C07C69/88 ,  C07C69/92 ,  C07C213/02 ,  C07C215/60 ,  C07C235/84 ,  C07D317/26 ,  C07D319/06 ,  C07F5/02 ,  C07F5/04

CPC classification number: C07C215/60 ,  C07C235/84 ,  C07C69/88 ,  C07F5/022 ,  C07F5/04

Abstract: The preparation of arylethanolamines, and in particular albuterol (salbutamol), together with their novel boron, acetal and hemi-acetal intermediates is described.

Abstract translation: PCT No.PCT / US91 / 06248 Sec。 371日期1993年3月1日 102（e）1993年3月1日PCT PCT 1991年9月6日PCT公布。 出版物WO92 / 04314 日期：1992年3月19日。描述了芳基乙醇胺，特别是沙丁胺醇（沙丁胺醇）的制备及其新型的硼，缩醛和半缩醛中间体。

公开(公告)号：US3686406A

公开(公告)日：1972-08-22

申请号：US3686406D

申请日：1970-09-18

Applicant: SCHERING CORP

Inventor： SHERLOCK MARGARET H

IPC: C07D213/80 ,  A61K27/00

CPC classification number: C07D213/80

Abstract: This invention relates to 2-(2-methylanilino)-nicotinic acid, the non-toxic pharmaceutically acceptable salts thereof and to the methods for the preparation and use thereof. The tangible embodiments of this invention are prepared by condensing a 2-halonicotinic acid, or a functionally reactive equivalent thereof, with an o-toluidine, or a functionally reactive equivalent thereof, to produce either 2-(2methylanilino)-nicotinic acid or a derivative which is convertible thereinto.

Abstract translation: 本发明涉及2-（2-甲基苯胺基） - 烟酸，其无毒的药学上可接受的盐及其制备和使用方法。

公开(公告)号：US20120177658A1

公开(公告)日：2012-07-12

申请号：US13287456

申请日：2011-11-02

Applicant: Pedro A. Reche-Gallardo ,  Vassilli Soumelis ,  Yong-Jun Liu ,  Rene de Waal Malefyt ,  J. Fernando Bazan ,  Robert A. Kastelein

Inventor： Pedro A. Reche-Gallardo ,  Vassilli Soumelis ,  Yong-Jun Liu ,  Rene de Waal Malefyt ,  J. Fernando Bazan ,  Robert A. Kastelein

IPC: A61K39/395 ,  C12N5/02 ,  A61P35/00

CPC classification number: C07K16/244 ,  C07K14/54 ,  C07K14/7155 ,  G01N33/6863 ,  G01N33/6869 ,  G01N2333/54 ,  G01N2500/02

Abstract: Nucleic acids encoding mammalian cytokine receptor, e.g., for cytokine IL-B50, purified proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are described.

Abstract translation: 编码哺乳动物细胞因子受体的核酸，例如细胞因子IL-B50，纯化的蛋白质及其片段。 还提供了抗体，包括多克隆和单克隆抗体。 描述了用于诊断和治疗用途的组合物的方法。

公开(公告)号：US08075886B2

公开(公告)日：2011-12-13

申请号：US12493871

申请日：2009-06-29

Applicant: Pedro A. Reche-Gallardo ,  Vassili Soumelis ,  Yong-Jun Liu ,  Rene de Waal Malefyt ,  J. Fernando Bazan ,  Robert A. Kastelein

Inventor： Pedro A. Reche-Gallardo ,  Vassili Soumelis ,  Yong-Jun Liu ,  Rene de Waal Malefyt ,  J. Fernando Bazan ,  Robert A. Kastelein

IPC: A61K39/395

CPC classification number: C07K16/244 ,  C07K14/54 ,  C07K14/7155 ,  G01N33/6863 ,  G01N33/6869 ,  G01N2333/54 ,  G01N2500/02

Abstract: Nucleic acids encoding mammalian cytokine receptor, e.g., for cytokine IL-B50, purified proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are described.

Abstract translation: 编码哺乳动物细胞因子受体的核酸，例如细胞因子IL-B50，纯化的蛋白质及其片段。 还提供了抗体，包括多克隆和单克隆抗体。 描述了用于诊断和治疗用途的组合物的方法。

公开(公告)号：US08048663B2

公开(公告)日：2011-11-01

申请号：US12815817

申请日：2010-06-15

Applicant: Wenyan Wang ,  Shahriar Shane Taremi ,  Winifred Prosise ,  Paul Reichert ,  Charles A. Lesburg ,  Vincent S. Madison ,  Kuo-Chi Cheng

Inventor： Wenyan Wang ,  Shahriar Shane Taremi ,  Winifred Prosise ,  Paul Reichert ,  Charles A. Lesburg ,  Vincent S. Madison ,  Kuo-Chi Cheng

IPC: C12N9/12 ,  G01N23/20

CPC classification number: C07K14/70567 ,  C07K14/4705 ,  C07K2319/31

Abstract: The present invention relates to Pregnane X receptor (PXR) polypeptides and crystals that are useful, for example, for crystallization and in assays for identification of modulators of PXR.

Abstract translation: 本发明涉及可用于例如结晶和用于鉴定PXR调节剂的测定中的孕烷X受体（PXR）多肽和晶体。