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1. 发明申请

WO2008002591A2 METHODS FOR TREATING ATHEROSCLEROSIS 审中-公开
标题翻译：治疗动脉粥样硬化的方法
公开(公告)号：WO2008002591A2
公开(公告)日：2008-01-03
申请号：PCT/US2007014873
申请日：2007-06-26
申请人： AMGEN INC , KAYSER FRANK , LABELLE MARC , SHAN BEI , ZHANG JIAN , ZHOU MINGYUE
发明人： KAYSER FRANK , LABELLE MARC , SHAN BEI , ZHANG JIAN , ZHOU MINGYUE
CPC分类号： C12N9/1029 , A61K31/497 , A61K38/45 , C07D403/12 , C07D417/12
摘要： The invention provides compounds, pharmaceutical compositions and methods for treating atherosclerosis, inflammation, thrombosis and other conditions and for decreasing or prevention of accumulation of cholesterol in a subject by modifying LCAT polypeptide.
摘要翻译：本发明提供了通过修饰LCAT多肽来治疗动脉粥样硬化，炎症，血栓形成和其他病症并降低或预防受试者中胆固醇积聚的化合物，药物组合物和方法。

2. 发明申请

WO2004047755A3 FUSED BICYCLIC NITROGEN-CONTAINING HETEROCYCLES 审中-公开
标题翻译：熔融双相含氮杂质
公开(公告)号：WO2004047755A3
公开(公告)日：2004-11-25
申请号：PCT/US0337574
申请日：2003-11-21
申请人： TULARIK INC , JAPAN TOBACCO INC , FOX BRIAN M , FURUKAWA NOBORU , HAO XIAOLIN , IIO KIYOSEI , INABA TAKASHI , JACKSON SIMON M , KAYSER FRANK , LABELLE MARC , LI KEXUE , MATSUI TAKUYA , MCMINN DUSTIN L , OGAWA NOBUYA , RUBENSTEIN STEVEN M , SAGAWA SHOICHI , SUGIMOTO KAZUYUKI , SUZUKI MASAHIRO , TANAKA MASAHIRO , YE GUOSEN , YOSHIDA ATSUHITO , ZHANG JIAN
发明人： FOX BRIAN M , FURUKAWA NOBORU , HAO XIAOLIN , IIO KIYOSEI , INABA TAKASHI , JACKSON SIMON M , KAYSER FRANK , LABELLE MARC , LI KEXUE , MATSUI TAKUYA , MCMINN DUSTIN L , OGAWA NOBUYA , RUBENSTEIN STEVEN M , SAGAWA SHOICHI , SUGIMOTO KAZUYUKI , SUZUKI MASAHIRO , TANAKA MASAHIRO , YE GUOSEN , YOSHIDA ATSUHITO , ZHANG JIAN
IPC分类号： A61K31/519 , A61K31/538 , A61K31/542 , C07D491/02 , C07D491/04 , C07D498/02 , C07D498/04 , C07D498/10 , C07D498/16 , C07D491/052 , A61K31/436 , A61K31/4365 , C07D513/04
CPC分类号： C07D491/04
摘要： Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the activity of proteins involved in lipid metabolism and cell proliferation.
摘要翻译：本文提供了可用于治疗或预防代谢和细胞增殖性疾病或病症的化合物，药物组合物和方法。特别地，本发明提供调节参与脂质代谢和细胞增殖的蛋白质的活性的化合物。

3. 发明申请

WO0220463A3 FXR MODULATORS 审中-公开
标题翻译： FXR调制器
公开(公告)号：WO0220463A3
公开(公告)日：2003-08-21
申请号：PCT/US0127239
申请日：2001-08-31
申请人： TULARIK INC , HOUZE JONATHAN , MCKENDRY SHARON , GERGELY JOSHUA P , XIA YI , SHAN BEI , KAYSER FRANK
发明人： HOUZE JONATHAN , MCKENDRY SHARON , GERGELY JOSHUA P , XIA YI , SHAN BEI , KAYSER FRANK
IPC分类号： A61P35/00 , C07C233/75 , C07C237/22 , C07C311/19 , C07C311/29 , C07D209/48 , C07D241/44 , C07D279/02 , A61K31/16 , C07C311/17 , C07K14/705
CPC分类号： C07D209/48 , C07C233/75 , C07C237/22 , C07C311/19 , C07C311/29 , C07C2601/14 , C07D241/44 , C07D279/02
摘要： The present invention provides compounds, pharmaceutical compositions and methods that are useful in modulating the farnesoid X receptor (FXR). As FXR is involved in negatively controlling the expression level of cholesterol 7 alpha -hydroxylase (cyp7a), the rate-limiting enzyme involved in the oxidative metabolism of cholesterol into bile acids, the compounds described herein find utility in treating diseases associated with abnormally high or low cholesterol levels. In certain aspects, the FXR modulators (e.g., antagonists) described herein block the negative feed-back downregulation of cyp7a expression produced by certain cholic acids, the endogenous ligands for FXR. Moreover, as FXR forms heterodimers with the retinoid X receptor (RXR) in some cell types, modulation of the level of FXR activity in cells has a wide range of effects on a variety of biological processes which are mediated by RXR or other RXR-interacting proteins such as PPAR gamma and PPAR alpha . Thus, compounds described herein are useful in treating other biological activities such as obesity, diabetes, lipid associated disorders, cancer, inflammatory disorders, disorders involving a disrupted or dysfunctional epidermal barrier, and various other metabolic disorders.
摘要翻译：本发明提供了可用于调节法呢酯X受体（FXR）的化合物，药物组合物和方法。由于FXR涉及负调控胆固醇7α-羟化酶（cyp7a）的表达水平，涉及胆固醇胆固醇氧化代谢的限速酶，本文所述的化合物可用于治疗与异常高相关的疾病或低胆固醇水平在某些方面，本文所述的FXR调节剂（例如拮抗剂）阻断某些胆酸（FXR的内源性配体）产生的cyp7a表达的负反馈下调。此外，由于FXR在一些细胞类型中与类视黄醇X受体（RXR）形成异源二聚体，因此细胞中FXR活性水平的调节对由RXR或其他RXR相互作用介导的各种生物过程具有广泛的影响蛋白质如PPARγ和PPARα。因此，本文所述的化合物可用于治疗其它生物活性，例如肥胖症，糖尿病，脂质相关疾病，癌症，炎性疾病，涉及破坏性或功能失调的表皮屏障的疾病以及各种其它代谢紊乱。

4. 发明申请

WO2006004658A2 FURANOPYRIMIDINES 审中-公开
公开(公告)号：WO2006004658A2
公开(公告)日：2006-01-12
申请号：PCT/US2005022727
申请日：2005-06-29
申请人： AMGEN INC , BUCHANAN JOHN L , BUCKNER WILLIAM H , BURKITT SIMON A , DIMAURO ERIN F , FARTHING CHRISTOPHER N , FRENKEL ALEXANDER DAVID , HARRISON MARTIN J , KAYSER FRANK , LIU JINQIAN , LIVELY SARAH E , MARSHALL TERESA L , MCGOWAN DAVID C , SHARMA RAJIV , SHUTTLEWORTH STEPHEN JOSEPH , ZHU XIAOTIAN
发明人： BUCHANAN JOHN L , BUCKNER WILLIAM H , BURKITT SIMON A , DIMAURO ERIN F , FARTHING CHRISTOPHER N , FRENKEL ALEXANDER DAVID , HARRISON MARTIN J , KAYSER FRANK , LIU JINQIAN , LIVELY SARAH E , MARSHALL TERESA L , MCGOWAN DAVID C , SHARMA RAJIV , SHUTTLEWORTH STEPHEN JOSEPH , ZHU XIAOTIAN
IPC分类号： C07D498/00
CPC分类号： C07D491/04 , C07D495/04
摘要： The present invention relates to furanopyrimidine compounds having the general Formula (I) and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula (I), methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula (I). The invention also relates to methods of manufacturing medicaments, which comprise one or more compounds of Formula (I).
摘要翻译：本发明涉及具有通式（I）的呋喃并嘧啶化合物及其立体异构体，互变异构体，溶剂化物，药学上可接受的盐和衍生物以及前药。本发明还包括包含式（I）化合物的药物组合物，治疗哺乳动物各种疾病和病症的方法，包括炎症，抑制T细胞活化，增殖，关节炎，器官移植，局部缺血或再灌注损伤，心肌梗塞，中风，多发性硬化症，炎性肠病，克罗恩病，狼疮，超敏反应，1型糖尿病，牛皮癣，皮炎，桥本氏甲状腺炎，干燥综合征，自身免疫性甲状腺机能亢进症，艾迪生病，自身免疫性疾病，肾小球肾炎，过敏性疾病，癌症，结肠癌和胸腺瘤，所述方法包括给所述哺乳动物施用治疗有效量的式（I）化合物。本发明还涉及制造包含一种或多种式（I）化合物的药物的方法。

5. 发明申请

WO2005016277A2 ARYLSULFONAMIDOBENZYLIC COMPOUNDS 审中-公开
标题翻译： ARYLSULFONAMIDOBENZYLIC化合物
公开(公告)号：WO2005016277A2
公开(公告)日：2005-02-24
申请号：PCT/US2004026120
申请日：2004-08-11
申请人： AMGEN INC , HARRISON MARTIN J , JIAO XIAN YUN , JONES STUART D , KAYSER FRANK , KOPECKY DAVID J
发明人： HARRISON MARTIN J , JIAO XIAN YUN , JONES STUART D , KAYSER FRANK , KOPECKY DAVID J
IPC分类号： A61K20060101 , A61K31/695 , C07C271/20 , C07C271/30 , C07C311/40 , C07C311/42 , C07D231/10 , C07D241/36 , C07D307/02 , C07D309/06 , C07F7/10 , A61K
CPC分类号： C07C311/21 , C07C311/38 , C07C317/32 , C07C323/49 , C07C2601/02 , C07D231/12 , C07D239/26 , C07D307/14 , C07F7/0818
摘要： Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment or prevention of lipid disorders, metabolic disorders and cell-proliferative diseases. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in cholesterol metabolism. The subject compounds are particularly useful in the treatment of obesity, diabetes, hypercholesterolemia, atherosclerosis and hypolipoproteinemia.
摘要翻译：提供可用于治疗或预防脂质紊乱，代谢紊乱和细胞增殖性疾病的化合物，药物组合物和方法。特别地，本发明提供了调节涉及胆固醇代谢的蛋白质的表达和/或功能的化合物。主题化合物特别适用于治疗肥胖症，糖尿病，高胆固醇血症，动脉粥样硬化和低脂蛋白血症。

6. 发明申请

WO2006130160A3 FURANOPYRIDINE DERIVATIVES AS ACK1 AND LCK MODULATORS 审中-公开
标题翻译：作为ACK1和LCK调节剂的呋喃亚胺衍生物
公开(公告)号：WO2006130160A3
公开(公告)日：2007-02-22
申请号：PCT/US2005025725
申请日：2005-07-19
申请人： AMGEN INC , NUNES JOSEPH J , MARTIN MATTHEW W , WHITE RYAN , MCGOWAN DAVID , BEMIS JEAN E , KAYSER FRANK , FU JIASHENG , LIU JINQIAN , JIAO XIANYUN
发明人： NUNES JOSEPH J , MARTIN MATTHEW W , WHITE RYAN , MCGOWAN DAVID , BEMIS JEAN E , KAYSER FRANK , FU JIASHENG , LIU JINQIAN , JIAO XIANYUN
IPC分类号： C07D491/04 , A61K31/4355 , C07D491/14
CPC分类号： C07D491/04 , C07D491/14
摘要： The present invention relates to furanopyridine compounds having the general Formula (I) and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of modulating Lck and ACK-1 enzymes and of treating various related diseases and conditions, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, comprising administering to the mammal a therapeutically effective amount a compound of Formula I, as described above, and methods of manufacturing medicaments comprising the compound of Formula (I).
摘要翻译：本发明涉及具有通式（I）的呋喃并吡啶化合物及其立体异构体，互变异构体，溶剂化物，药学上可接受的盐和衍生物及其前药。本发明还包括药物组合物，其包含式I化合物，调节Lck和ACK-1酶的方法以及治疗各种相关疾病和病症，包括炎症，T细胞活化抑制，增殖，关节炎，器官移植，缺血或再灌注损伤，心肌梗塞，中风，多发性硬化，炎性肠病，克罗恩病，狼疮，超敏反应，1型糖尿病，牛皮癣，皮炎，桥本氏甲状腺炎，干燥综合征，自身免疫性甲状腺功能亢进，艾迪生病，自身免疫性疾病，肾小球肾炎，过敏性疾病，哮喘，干草组织，湿疹，癌症，结肠癌，胸腺瘤，仅举几个例子，在哺乳动物中，包括向哺乳动物施用治疗有效量的如上所述的式I化合物和制备包含以下化合物的药物的方法：式（I）。

7. 发明申请

WO2006004703A3 PYRROLO[2,3-d]PYRIMIDINES THAT MODULATE ACK1 AND LCK ACTIVITY 审中-公开
标题翻译：吡咯并[2,3-d]嘧啶类化合物调节ACK1和LCK活性
公开(公告)号：WO2006004703A3
公开(公告)日：2006-03-09
申请号：PCT/US2005022836
申请日：2005-06-29
申请人： AMGEN INC , FARTHING CHRISTOPHER N , FAULDER PAUL , FRENKEL ALEXANDER DAVID , HARRISON MARTIN JAMES , JIAO XIANYUN , KAYSER FRANK , KOPECKY DAVID J , LIU JINQIAN , LIVELY SARAH E , SHARMA RAJIV , SHUTTLEWORTH STEPHEN JOSEPH
发明人： FARTHING CHRISTOPHER N , FAULDER PAUL , FRENKEL ALEXANDER DAVID , HARRISON MARTIN JAMES , JIAO XIANYUN , KAYSER FRANK , KOPECKY DAVID J , LIU JINQIAN , LIVELY SARAH E , SHARMA RAJIV , SHUTTLEWORTH STEPHEN JOSEPH
IPC分类号： C07D487/00 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： Compounds that modulate the action of ACK1 and LCK, and related compositions methods for treating ACK1- and LCK-mediated diseases are described. In one aspect, the compounds have the general structure: where the values of the substituents are provided herein.
摘要翻译：描述了调节ACK1和LCK作用的化合物，以及用于治疗ACK1-和LCK介导的疾病的相关组合物方法。在一个方面，化合物具有通式结构：其中取代基的值在本文中提供。

8. 发明申请

WO2005013907A3 PYRROLO[1,2-B]PYRIDAZINE DERIVATIVES 审中-公开
标题翻译：吡咯并[1,2-B]哒嗪衍生物
公开(公告)号：WO2005013907A3
公开(公告)日：2005-04-21
申请号：PCT/US2004025590
申请日：2004-08-06
申请人： TULARIK INC , JAPAN TOBACCO INC , FOX BRIAN M , IIO KIYOSEI , INABA TAKASHI , KAYSER FRANK , LI KEXUE , SAGAWA SHOICHI , TANAKA MASAHIRO , YOSHIDA ATSUHITO
发明人： FOX BRIAN M , IIO KIYOSEI , INABA TAKASHI , KAYSER FRANK , LI KEXUE , SAGAWA SHOICHI , TANAKA MASAHIRO , YOSHIDA ATSUHITO
IPC分类号： A01N43/58 , A01N43/60 , A61K20060101 , A61K31/495 , A61K31/50 , A61K31/503 , A61K31/535 , C07D237/26 , C07D237/28 , C07D413/00 , C07D487/00 , C07D487/04
CPC分类号： C07D487/04
摘要： Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the activity of proteins involved in lipid metabolism and cell proliferation.
摘要翻译：本文提供了可用于治疗或预防代谢和细胞增殖性疾病或病症的化合物，药物组合物和方法。具体而言，本发明提供了调节参与脂质代谢和细胞增殖的蛋白质的活性的化合物。

9. 发明申请

WO03024395A8 LINKED BIARYL COMPOUNDS 审中-公开
标题翻译：链接的二元化合物
公开(公告)号：WO03024395A8
公开(公告)日：2004-01-22
申请号：PCT/US0229232
申请日：2002-09-13
申请人： TULARIK INC , JAPAN TOBACCO INC , ABE HIROYUKI , HOUZE JONATHAN , KAWASAKI HISASHI , KAYSER FRANK , SHARMA RAJIV , SPERRY SAMUEL
发明人： ABE HIROYUKI , HOUZE JONATHAN , KAWASAKI HISASHI , KAYSER FRANK , SHARMA RAJIV , SPERRY SAMUEL
IPC分类号： C07D215/20 , A61K31/192 , A61K31/216 , A61K31/4184 , A61K31/421 , A61K31/426 , A61K31/4406 , A61K31/47 , A61P1/00 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/08 , A61P13/12 , A61P15/00 , A61P19/02 , A61P25/00 , A61P25/06 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , C07C317/22 , C07C321/30 , C07C323/20 , C07C323/21 , C07D213/65 , C07D215/22 , C07D235/26 , C07D263/40 , C07D277/20 , C07D277/34 , A61K31/415 , A61K31/24 , A61K31/40 , A61K31/42 , A61K31/425 , C07D207/00 , C07D209/02 , C07D215/00 , C07D233/00 , C07D239/02
CPC分类号： C07C317/22 , C07C323/20 , C07C323/21 , C07C2602/10
摘要： Compounds, compositions and methods that are useful for the treatment of metabolic disorders, inflammatory diseases and cancer are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in lipid metabolism, inflammation and cell proliferation. The subject compounds are linked biaryl compounds.
摘要翻译：本文提供了可用于治疗代谢紊乱，炎性疾病和癌症的化合物，组合物和方法。特别地，本发明提供调节参与脂质代谢，炎症和细胞增殖的蛋白质的表达和/或功能的化合物。主题化合物是联芳基化合物。

10. 发明申请

WO2004058702A3 4-[(4-(CARBOXYETHYL) PIPERIDINYL) METHYL] PYRROLIDINES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译： 4 - [（4-（羧甲基）哌啶基）甲基]吡咯烷作为趋化因子受体活性的调节剂
公开(公告)号：WO2004058702A3
公开(公告)日：2004-08-26
申请号：PCT/US0340785
申请日：2003-12-19
申请人： MERCK & CO INC , BERESIS RICHARD , BERGER RICHARD , COLLETTI STEVEN L , PARSONS WILLIAM H , RUPPRECHT KATHLEEN M , JOHANSON JILL N , KAYSER FRANK , KOVACS ERNEST W
发明人： BERESIS RICHARD , BERGER RICHARD , COLLETTI STEVEN L , PARSONS WILLIAM H , RUPPRECHT KATHLEEN M , JOHANSON JILL N , KAYSER FRANK , KOVACS ERNEST W
IPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D411/14
CPC分类号： C07D409/14 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： 3-Substituted pyrrolidines having a 4-carboxypiperidinylmethyl substituent on the 4-position of the ring are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
摘要翻译：在环的4-位具有4-羧基哌啶基甲基取代基的3-取代的吡咯烷可用作趋化因子受体活性的调节剂。特别地，这些化合物可用作趋化因子受体CCR-3和/或CCR-5的调节剂。

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