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1. 发明申请

WO2006071954A2 METHOD OF TREATING CANCER 审中-公开
标题翻译：治疗癌症的方法
公开(公告)号：WO2006071954A2
公开(公告)日：2006-07-06
申请号：PCT/US2005/047313
申请日：2005-12-27
申请人： MYRIAD GENETICS, INC. , ROTH, Bruce , BAICHWAL, Vijay , PLEIMAN, Chris
发明人： ROTH, Bruce , BAICHWAL, Vijay , PLEIMAN, Chris
IPC分类号： A61K9/127
CPC分类号： A61K31/167
摘要： The present invention provides therapeutic compounds and methods for the treatment of refractory and multidrug resistant cancers in patients in need of such treatment.
摘要翻译：本发明提供治疗化合物和治疗需要这种治疗的患者耐受性和多药耐药性癌症的方法。

2. 发明申请

WO2005014539A3 PYRROLE-BASED HMG-COA REDUCTASE INHIBITORS 审中-公开
标题翻译：基于PYRROLE的HMG-COA还原抑制剂
公开(公告)号：WO2005014539A3
公开(公告)日：2005-05-12
申请号：PCT/IB2004002540
申请日：2004-07-30
申请人： WARNER LAMBERT CO , KENNEDY ROBERT MICHAEL , PARK WILLIAM KEUN-CHAN , ROTH BRUCE DAVID , SONG YUNTAO , TRIVEDI BHARAT KALIDAS
发明人： KENNEDY ROBERT MICHAEL , PARK WILLIAM KEUN-CHAN , ROTH BRUCE DAVID , SONG YUNTAO , TRIVEDI BHARAT KALIDAS
IPC分类号： C07C303/40 , C07C311/13 , C07D207/32 , C07D207/33 , C07D207/34 , C07D207/36 , C07D319/06 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , A61K31/40 , A61K31/4025 , A61P3/06 , C07C311/11
CPC分类号： C04B35/632 , C07C303/40 , C07C311/13 , C07D207/33 , C07D207/34 , C07D207/36 , C07D319/06 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14
摘要： HMGCo-A reductase inhibitor compounds of formula (I) useful as hypocholesterolemic and hypolipidemic compounds are provided. Also provided are pharmaceutical compositions of the compounds. Methods of making and methods of using the compounds are also provided.
摘要翻译：提供了可用作低胆固醇血症和降血脂化合物的式（I）的HMGCo-A还原酶抑制剂化合物。还提供了化合物的药物组合物。还提供了制备方法和使用该化合物的方法。

3. 发明申请

WO1998009940A1 BIPHENYL BUTYRIC ACIDS AND THEIR DERIVATIVES AS INHIBITORS OF MATRIX METALLOPROTEINASES 审中-公开
标题翻译：二苯基丁酸及其作为基质金属蛋白酶抑制剂的衍生物
公开(公告)号：WO1998009940A1
公开(公告)日：1998-03-12
申请号：PCT/US1997014852
申请日：1997-08-22
申请人： WARNER-LAMBERT COMPANY , PURCHASE, Claude, Forsey, Jr. , ROTH, Bruce, David , WHITE, Andrew, David , SCHIELKE, Gerald, Paul , WALKER, Lary, Craswell
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07C251/48
CPC分类号： C07C323/63 , C07C59/56 , C07C59/84 , C07C59/88 , C07C59/90 , C07C69/738 , C07C251/48 , C07C251/86 , C07C255/64
摘要： Biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.
摘要翻译：描述了联苯丁酸化合物和衍生物以及用于制备的酸法和其药物组合物，其可用作基质金属蛋白酶抑制剂，特别是明胶酶A（72kD明胶酶）和基质溶素-1和用于治疗多发性硬化症，动脉粥样硬化斑块破裂，主动脉瘤，心力衰竭，再狭窄，牙周病，角膜溃疡，烧伤治疗，褥疮性溃疡，伤口愈合，癌症，炎症，疼痛，关节炎或依赖于白细胞组织侵袭的其他自身免疫性或炎性病症，其他活化的迁移细胞，急性和慢性神经变性疾病，包括中风，头部创伤，脊髓损伤，阿尔茨海默病，肌萎缩性侧索硬化，脑淀粉样血管病，艾滋病，帕金森病，亨廷顿病，朊病毒疾病，重症肌无力和杜氏肌营养不良症。

4. 发明申请

WO1989007598A2 IMPROVED PROCESS FOR TRANS-6-[2-(SUBSTITUTED-PYRROL-1-YL)ALKYL]PYRAN-2-ONE INHIBITORS OF CHOLESTEROL SYNTHESIS 审中-公开
标题翻译：改进方法TRANS-6- [2-（取代的吡咯-1-基）烷基]吡喃-2-酮抑制剂胆固醇的合成
公开(公告)号：WO1989007598A2
公开(公告)日：1989-08-24
申请号：PCT/US1989000719
申请日：1989-02-22
申请人： WARNER-LAMBERT COMPANY , BUTLER, Donald, Eugene , DEERING, Carl, Francis , MILLAR, Alan , NANNINGA, Thomas, Norman , ROTH, Bruce, David
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D405/06
CPC分类号： C07D319/08 , C07C235/80 , C07D207/34 , C07D319/06 , C07D405/06
摘要： An improved process for the preparation of trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where 1,6-heptadien-4-ol is converted in eight operations to the desired products, as well as an improved process for the preparation of (2R-trans) and trans-(U)-5-(4-fluoro-phenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide by a novel synthesis where 4-methyl-3-oxo-N-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-alpha-[2-methyl-1-oxopropyl]-gamma-oxo-N,beta-diphenylbenzenebutaneamide is converted in one step to the desired product, and additionally, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide from (R)-4-cyano-3-[[(1,1-dimethylethyl)dimethylsilyl]oxy]butanoic acid, as well as other valuable intermediates used in the processes.
摘要翻译：它已经开发了一种改进的方法，用于反式-6-的制备[2-（取代的吡咯-1-基）烷基]吡喃-2-酮由一个新的合成装置，用于将1,6-heptadiène- 在所需产品中进行8次操作。制备（2R-反式）和反式 - （U）-5-（4-氟 - 苯基）-2-（1-甲基乙基）-N，4-二苯基-1的改进方法也被开发出来。 [2-（四氢-4-羟基-6-氧代-2H-吡喃-2-基）乙基]使用新的合成用于将4-甲基-3-氧代-1H-吡咯-3-甲酰胺 -N苯基戊酰胺在八个操作中，期望的产物或在另一个实施方案中变换4-氟-α-[2-甲基-1-氧代丙基〕-gamma氧代-N，β-diphénylbenzènebutaneamide在一个步骤中在期望的产品中。已经进一步开发出一种方法，用于制备式（2R-反式）-5-（4-flurophényle）-2-（1-甲基乙基）-N，4-二苯基-1- [2-（四氢 4-羟基-6-氧代-2H-吡喃-2-基）乙基]从（R）-4-氰基-3- -1H-吡咯-3-甲酰胺 - [[（1,1-二甲乙基）二甲基甲硅烷 ]氧]丁酸，以及在该方法中使用的其他有价值的中间体。

5. 发明申请

WO2006071954A3 METHOD OF TREATING CANCER 审中-公开
标题翻译：治疗癌症的方法
公开(公告)号：WO2006071954A3
公开(公告)日：2007-09-13
申请号：PCT/US2005047313
申请日：2005-12-27
申请人： MYRIAD GENETICS INC , ROTH BRUCE , BAICHWAL VIJAY , PLEIMAN CHRIS
发明人： ROTH BRUCE , BAICHWAL VIJAY , PLEIMAN CHRIS
IPC分类号： A01N29/00
CPC分类号： A61K31/167
摘要： The present invention provides therapeutic compounds and methods for the treatment of refractory and multidrug resistant cancers in patients in need of such treatment.
摘要翻译：本发明提供治疗化合物和治疗需要这种治疗的患者耐受性和多药耐药性癌症的方法。

6. 发明申请

WO1988004657A2 TRANS-6-[2-[2-(SUBSTITUTED-PHENYL)-3- (or 4-) HETEROARYL-5-SUBSTITUTED-1H-PYRROL-1-YL]-ETHYL]TETRAHYDRO-4-HYDROXY-2H-PYRAN-2-ONE INHIBITORS OF CHOLESTEROL BIOSYNTHESIS 审中-公开
标题翻译：反式-6- [2- [2-（取代的苯基）-3-（或4-）取代的5-取代的1H-吡咯-1-基] - 乙基]四氢-4-羟基-2H- 胆碱醇生物合成2-ONE抑制剂
公开(公告)号：WO1988004657A2
公开(公告)日：1988-06-30
申请号：PCT/US1987003047
申请日：1987-11-23
申请人： WARNER-LAMBERT COMPANY , ROTH, Bruce, David , SLISKOVIC, Drago, Robert
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D405/14
CPC分类号： C07D405/14
摘要： Certain trans-6-[2-[2-(substituted-phenyl)-3- (or 4-)heteroaryl-5-substituted-1H-pyrrol-1-yl]ethyl]tetrahydro-4-hydroxy-2H-pyran-2-ones and the corresponding lactone-ring-opened acids are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG CoA reductase) and are thus useful hypolipidemic or hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of inhibiting the biosynthesis of cholesterol employing such pharmaceutical compositions are also disclosed.

7. 发明申请

WO2005014539A2 NOVEL PYRROLE-BASED HMG-COA REDUCTASE INHIBITORS 审中-公开
标题翻译：基于PYRROLE的HMG-COA还原抑制剂
公开(公告)号：WO2005014539A2
公开(公告)日：2005-02-17
申请号：PCT/IB2004/002540
申请日：2004-07-30
申请人： WARNER-LAMBERT COMPANY LLC , KENNEDY, Robert, Michael , PARK, William, Keun-Chan , ROTH, Bruce, David , SONG, Yuntao , TRIVEDI, Bharat, Kalidas
发明人： KENNEDY, Robert, Michael , PARK, William, Keun-Chan , ROTH, Bruce, David , SONG, Yuntao , TRIVEDI, Bharat, Kalidas
IPC分类号： C07D207/00
CPC分类号： C04B35/632 , C07C303/40 , C07C311/13 , C07D207/33 , C07D207/34 , C07D207/36 , C07D319/06 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14
摘要： HMGCo-A reductase inhibitor compounds useful as hypocholesterolemic and hypolipidemic compounds are provided. Also provided are pharmaceutical compositions of the compounds. Method of making and methods of using the compounds are also provided.
摘要翻译：提供了可用作低胆固醇血症和降血脂化合物的HMGCo-A还原酶抑制剂化合物。还提供了化合物的药物组合物。还提供了制备方法和使用该化合物的方法。

8. 发明申请

WO1998016505A1 SULFONAMIDE INTERLEUKIN-1'beta' CONVERTING ENZYME INHIBITORS 审中-公开
标题翻译： SULFONAMIDE INTERLEUKIN-1 beta转化酶抑制剂
公开(公告)号：WO1998016505A1
公开(公告)日：1998-04-23
申请号：PCT/US1997018396
申请日：1997-10-09
申请人： WARNER-LAMBERT COMPANY , ALBRECHT, Hans, P. , ALLEN, Hamish, John , BRADY, Kenneth, Dale , HARTER, William, Glen , KOSTLAN, Catherine, Rose , ROTH, Bruce, David , WALKER, Nigel
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07C311/13
CPC分类号： C07K5/1024 , A61K38/00 , C07C311/06 , C07C311/19 , C07C2601/14 , C07C2602/08 , C07C2602/42 , C07C2603/18 , C07D217/24 , C07K5/06026 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06104 , C07K5/06139 , C07K5/0804 , C07K5/0812 , C07K5/0815 , C07K5/0819 , C07K5/0821 , C07K5/1005 , C07K5/1016 , C07K5/1019 , C07K5/1021
摘要： The present invention relates to compounds that are inhibitors of interleukin-1 beta converting enzyme that have the Formula (I). This invention also relates to a method of treatment of stroke, reperfusion injury, Alzheimer's disease, shigellosis, inflammatory diseases, and septic shock and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1 beta converting enzyme.
摘要翻译：本发明涉及具有式（I）的白细胞介素-1β转换酶抑制剂的化合物。本发明还涉及治疗中风，再灌注损伤，阿尔茨海默病，志贺氏菌病，炎性疾病和败血性休克的方法以及含有作为白细胞介素-1β转换酶抑制剂的化合物的药学上可接受的组合物。

9. 发明申请

WO8804657A3 TRANS-6-(2-(2-(SUBSTITUTED-PHENYL)-2-(OR-4-)HETEROARYL-5-SUBSTITUTED-1H-PYRROL-1-YL)-ETHYL)TETRAHYDRO-4-HYDROXY-2H-PYRAN-2-ONE INHIBITORS OF CHOLESTEROL BIOSYNTHESIS 审中-公开
标题翻译：反式-6-（2-（2-（取代的 - 苯基）-2-（OR-4-）杂芳基-5-取代-1H-吡咯-1-基） - 乙基）四氢-4-羟基-2H-吡喃 2-酮胆固醇生物合成抑制剂
公开(公告)号：WO8804657A3
公开(公告)日：1988-12-01
申请号：PCT/US8703047
申请日：1987-11-23
申请人： WARNER LAMBERT CO , ROTH BRUCE DAVID , SLISKOVIC DRAGO ROBERT
发明人： ROTH BRUCE DAVID , SLISKOVIC DRAGO ROBERT
IPC分类号： C07D405/14 , C07D409/14
CPC分类号： C07D405/14
摘要： Certain trans-6-[2-[2-(substituted-phenyl)-3- (or 4-)heteroaryl-5-substituted-1H-pyrrol-1-yl]ethyl]tetrahydro-4-hydroxy-2H-pyran-2-ones and the corresponding lactone-ring-opened acids are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG CoA reductase) and are thus useful hypolipidemic or hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of inhibiting the biosynthesis of cholesterol employing such pharmaceutical compositions are also disclosed.

10. 发明申请

WO2012031197A1 NOVEL COMPOUNDS AND COMPOSITIONS FOR THE INHIBITION OF NAMPT 审中-公开
标题翻译：新型化合物和组合物抑制NAMPT
公开(公告)号：WO2012031197A1
公开(公告)日：2012-03-08
申请号：PCT/US2011/050321
申请日：2011-09-02
申请人： FORMA THERAPEUTICS, INC. , GENENTECH, INC. , BAIR, Kenneth, W. , BAUMEISTER, Timm , BUCKMELTER, Alexandre, J. , CLODFELTER, Karl, H. , DRAGOVICH, Peter , GOSSELIN, Francis , HAN, Bingsong , LIN, Jian , REYNOLDS, Dominic J. , ROTH, Bruce , SMITH, Chase, C. , WANG, Zhongguo , YUEN, Po-Wai , ZHENG, Xiaozhang
发明人： BAIR, Kenneth, W. , BAUMEISTER, Timm , BUCKMELTER, Alexandre, J. , CLODFELTER, Karl, H. , DRAGOVICH, Peter , GOSSELIN, Francis , HAN, Bingsong , LIN, Jian , REYNOLDS, Dominic J. , ROTH, Bruce , SMITH, Chase, C. , WANG, Zhongguo , YUEN, Po-Wai , ZHENG, Xiaozhang
IPC分类号： C07D471/04 , C07D491/04 , C07D495/04 , A61K31/437 , A61P35/00
CPC分类号： A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/519 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04
摘要： The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below:
摘要翻译：本发明涉及抑制NAMPT，其合成，应用和解毒剂的化合物和组合物。本发明的说明性化合物如下所示：

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