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1. 发明申请

WO2003043624A1 DUAL INHIBITORS OF ADIPOCYTE FATTY ACID BINDING PROTEIN AND KERATINOCYTE FATTY ACID BINDING PROTEIN 审中-公开
标题翻译： ADIPOCYTE脂肪酸结合蛋白和KERATINOCYTE脂肪酸结合蛋白的双重抑制剂
公开(公告)号：WO2003043624A1
公开(公告)日：2003-05-30
申请号：PCT/US2002/036580
申请日：2002-11-15
申请人： BRISTOL-MYERS SQUIBB COMPANY , MAGNIN, David, R. , SULSKY, Richard, B. , ROBL, Jeffrey, A. , CAULFIELD, Thomas, J. , PARKER, Rex, A.
发明人： MAGNIN, David, R. , SULSKY, Richard, B. , ROBL, Jeffrey, A. , CAULFIELD, Thomas, J. , PARKER, Rex, A.
IPC分类号： A61K31/19
CPC分类号： C07C323/56 , A61K31/155 , A61K31/19 , A61K31/195 , A61K31/41 , A61K31/427 , A61K31/64 , A61K38/28 , A61K45/06 , C07C45/41 , C07C45/59 , C07C45/71 , C07C47/575 , C07C51/487 , C07C59/68 , C07C65/24 , C07C205/35 , C07C205/59 , C07C229/36 , C07C233/47 , C07C233/81 , C07C233/87 , C07C235/12 , C07C251/48 , C07C255/54 , C07C311/21 , C07C317/18 , C40B40/00 , A61K2300/00 , C07C47/565
摘要： Compounds that are dual aP2/k-FABP inhibitors are provided having the formula (I), wherein A, B, X, Y, R 1 , R 2 and R 3 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing dual aP2/k-FABP inhibitors alone or in combination with at least one other antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.
摘要翻译：提供具有式（I）的双重aP2 / k-FABP抑制剂的化合物，其中A，B，X，Y，R 1，R 2和R 3如本文所述。还提供了一种用于治疗糖尿病和相关疾病，特别是II型糖尿病的方法，其单独使用双重aP2 / k-FABP抑制剂或与至少一种其它抗糖尿病药如二甲双胍，格列本脲，曲格列酮和/或胰岛素组合。

2. 发明申请

WO2002083128A1 2,1-OXAZOLINE AND 1,2-PYRAZOLINE-BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND METHOD 审中-公开
标题翻译： 2,1-氧杂环丁烷和基于1,2-吡唑啉酮的DIPIPTIDYP肽酶IV和方法的抑制剂
公开(公告)号：WO2002083128A1
公开(公告)日：2002-10-24
申请号：PCT/US2002/010936
申请日：2002-04-05
申请人： BRISTOL-MYERS SQUIBB COMPANY , SULSKY, Richard, B. , ROBL, Jeffrey, A.
发明人： SULSKY, Richard, B. , ROBL, Jeffrey, A.
IPC分类号： A61K31/415
CPC分类号： C07D231/06 , A61K31/415 , A61K31/42 , C07D231/04 , C07D261/02 , A61K2300/00
摘要： Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula where n is 0 or 1; X is H or CN; Y is N, NH or O; Z is CH 2 when Y is O or N-H, with Y-Z forming a single bond, and Z is CH when Y is N, with Y-Z forming a double bond; and wherein R 1 , R 2 , R 3 and R 4 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.
摘要翻译：提供二肽基肽酶IV（DP 4）抑制化合物，其具有下式其中n为0或1; X是H或CN; Y是N，NH或O; 当Y为O或N-H时，Z为CH 2，Y-Z为单键，Y为N时Z为CH，Y-Z为双键; 并且其中R 1，R 2，R 3和R 4如本文所述。还提供了一种用于治疗糖尿病和相关疾病，特别是II型糖尿病和本文所列的其它疾病的方法，其使用这种DP 4抑制剂或这种DP 4抑制剂与一种或多种其它抗糖尿病药如二甲双胍，格列本脲，曲格列酮，吡格列酮，罗格列酮和/或胰岛素和/或降血脂药和/或抗肥胖剂和/或其它治疗剂中的一种或多种。

3. 发明申请

WO2008130951A1 FUSED HETEROCYCLIC 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS 审中-公开
标题翻译：熔融杂环11-羟基脱氢酶脱氢酶I型抑制剂
公开(公告)号：WO2008130951A1
公开(公告)日：2008-10-30
申请号：PCT/US2008/060395
申请日：2008-04-16
申请人： BRISTOL-MYERS SQUIBB COMPANY , LI, Jun , LI, James, J. , O'CONNOR, Stephen, P. , WANG, Haixia , KENNEDY, Lawrence, J. , ROBL, Jeffrey, A. , HAMANN, Lawrence, G.
发明人： LI, Jun , LI, James, J. , O'CONNOR, Stephen, P. , WANG, Haixia , KENNEDY, Lawrence, J. , ROBL, Jeffrey, A. , HAMANN, Lawrence, G.
IPC分类号： C07D487/04 , C07D495/14 , A61K31/5025 , A61K31/519 , A61K31/4985 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P9/12 , A61P27/06
CPC分类号： C07D487/04 , C07D513/14
摘要： Novel compounds are provided which are 1 1 -beta-hydroxysteroid dehydrogenase type I inhibitors. 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 1 1-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: W-L-Z or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, L are defined herein and Z is selected from the following bicyclic heteroaryl groups: (a), (b), (c), (d).
摘要翻译：提供了新的化合物，其为11β-羟基类固醇脱氢酶I型抑制剂。 11β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。这些新型化合物具有以下结构：WLZ或其立体异构体或前药或其药学上可接受的盐，其中W，L在本文中定义，Z选自以下双环杂芳基：（a），（b），（c），（d ）。

4. 发明申请

WO2007050726A2 NON-BASIC MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：非基础麦芽宁浓缩激素受体-1拮抗剂
公开(公告)号：WO2007050726A2
公开(公告)日：2007-05-03
申请号：PCT/US2006/041725
申请日：2006-10-26
申请人： BRISTOL-MYERS SQUIBB COMPANY , WASHBURN, William N. , HERNANDEZ, Andres S. , MANFREDI, Mark C. , ROBL, Jeffrey, A.
发明人： WASHBURN, William N. , HERNANDEZ, Andres S. , MANFREDI, Mark C. , ROBL, Jeffrey, A.
IPC分类号： C07D495/04 , A61K31/522 , A61P5/00 , A61P25/00
CPC分类号： C07D495/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
摘要翻译：本申请提供化合物，包括根据式I的所有立体异构体，溶剂合物，前药和药学上可接受的形式。另外，本申请提供含有至少一种根据式I的化合物和任选的至少一种另外的治疗剂的药物组合物。最后，本申请提供了通过施用治疗有效剂量的根据式I的化合物治疗患有MCHR-1调节的疾病或病症例如肥胖，糖尿病，抑郁或焦虑的患者的方法。

5. 发明申请

WO2003006023A1 PYRAZINONE INHIBITORS OF FATTY ACID BINDING PROTEIN AND METHOD 审中-公开
标题翻译：脂肪酸结合蛋白的吡嗪酮抑制剂和方法
公开(公告)号：WO2003006023A1
公开(公告)日：2003-01-23
申请号：PCT/US2002/022186
申请日：2002-07-12
申请人： BRISTOL-MYERS SQUIBB COMPANY , SULSKY, Richard , ROBL, Jeffrey, A.
发明人： SULSKY, Richard , ROBL, Jeffrey, A.
IPC分类号： A61K31/50
CPC分类号： C07D237/16 , B01D29/05 , B01D2201/305 , C07D237/14
摘要： aP2 inhibiting compounds are provided having the formula [I] wherein A, X, R and Z are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitors alone or in combination with other therapeutic agents, including other antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.
摘要翻译：提供具有式[I]的AP2抑制化合物，其中A，X，R和Z如本文所述。还提供了一种用于治疗糖尿病和相关疾病，特别是II型糖尿病的方法，其单独使用这种P 2抑制剂或与其它治疗剂，包括其它抗糖尿病药如二甲双胍，格列本脲，曲格列酮和/或胰岛素组合。

6. 发明申请

WO2009146365A1 HYDROXY SUBSTITUTED THIENO PYRIMIDINONES AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：羟基取代的三苯基嘧啶酮作为富含浓度的HORMONE受体-1拮抗剂的MELANIN
公开(公告)号：WO2009146365A1
公开(公告)日：2009-12-03
申请号：PCT/US2009/045452
申请日：2009-05-28
申请人： BRISTOL-MYERS SQUIBB COMPANY , WASHBURN, William, N. , AHMAD, Saleem , DEVASTHALE, Pratik , ROBL, Jeffrey, A. , GOSWAMI, Animesh , GUO, Zhiwei , PATEL, Ramesh, N.
发明人： WASHBURN, William, N. , AHMAD, Saleem , DEVASTHALE, Pratik , ROBL, Jeffrey, A. , GOSWAMI, Animesh , GUO, Zhiwei , PATEL, Ramesh, N.
IPC分类号： C07D495/04 , A61K31/522 , A61P5/00 , A61P25/00
CPC分类号： C07D495/04
摘要： The present invention provides compounds having the following Formula IA and IB, which are useful as MCHR1 antagonists, and includes prodrugs and pharmaceutically acceptable salts thereof.
摘要翻译：本发明提供具有以下式IA和IB的化合物，其可用作MCHR1拮抗剂，并且包括前药及其药学上可接受的盐。

7. 发明申请

WO2010104830A1 PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：吡咯烷酮类似物有效用于浓缩HORMONE受体-1拮抗剂的MELANIN
公开(公告)号：WO2010104830A1
公开(公告)日：2010-09-16
申请号：PCT/US2010/026626
申请日：2010-03-09
申请人： BRISTOL-MYERS SQUIBB COMPANY , AHMAD, Saleem , WASHBURN, William, N. , HERNANDEZ, Andres, S. , ROBL, Jeffrey, A. , NGU, Khehyong , WANG, Zhenghua
发明人： AHMAD, Saleem , WASHBURN, William, N. , HERNANDEZ, Andres, S. , ROBL, Jeffrey, A. , NGU, Khehyong , WANG, Zhenghua
IPC分类号： A61K31/4412 , A61P3/04 , C07D213/38 , C07D213/74 , C07D213/30 , C07D213/32 , C07D213/26 , C07D213/68 , C07D401/04 , A61K31/4409 , A61K31/4427
CPC分类号： C07D213/38 , A61K31/4412 , A61K31/4427 , C07D213/26 , C07D213/30 , C07D213/32 , C07D213/68 , C07D401/04
摘要： MCHR1 antagonists are provided having the following Formula I: wherein A 1 and A 2 are independently C or N; E is C or N; D 1 is a bond, -CR 8 R 9 X-, -XCR 8 R 9 -, -CHR 8 CHR 9 -, -CR 10 =CR 10' -, -C≡C-, or 1,2-cyclopropyl; X is O, S or -NR 11 ; R 1 , R 2 , and R 3 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, lower cycloalkoxy, -CF 3 , -OCF 3 , -OR 12 and -SR 12 ; G is O or S; D 2 is lower alkyl, lower cycloalkyl, lower alkylcycloalkyl, lower cycloalkylalkyl, lower cycloalkoxyalkyl or lower alkycycloalkoxy; Z 1 and Z 2 are independently hydrogen, halogen, lower alkyl, lower cycloalkyl, lower alkoxy, lower cycloalkoxy, halo, -CF 3 , -OCONR 14 R 14' , -CN, -CONR 14 R 14' , -SOR 12 , -SO 2 R 12 , -NR 14 COR 14' , -NR 14 CO 2 R 14' , -CO 2 R 12 , NR 14 SO 2 R 12 or -COR 12 provided that if Z 1 is -CH 3 and one of R 1 , R 2 , or R 3 is F, then Z 2 cannot be H;; R 5 , R 6 , and R 7 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, -CF 3 , -SR 12 , lower alkoxy, lower cycloalkoxy, -OCH 2 OMe, -CN, -CONR 14 R 14' , SOR 12 , SO 2 R 12 , NR 14 COR 14' , NR 14 CO 2 R 12 , CO 2 R 12 , NR 14 SO 2 R 12 and -COR 12 ; R 8 , R 9 , R 10 , R 10' , R 11 are independently hydrogen or lower alkyl; R 12 is lower alkyl or lower cycloalkyl; and R 14 and R 14' are independently H, lower alkyl, lower cycloalkyl or R 14 and R 14' together with the N to which they are attached form a ring having 4 to 7 atoms. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.
摘要翻译：提供具有下式I的MCHR1拮抗剂：其中A1和A2独立地为C或N; E为C或N; D1是键，-CR8R9X-，-XCR8R9-，-CHR8CHR9-，-CR10 = CR10'-，-C = C-或1,2-环丙基; X是O，S或-NR 11; R 1，R 2和R 3独立地选自氢，卤素，低级烷基，低级环烷基，低级环烷氧基，-CF 3，-OCF 3，-OR 12和-SR 12; G为O或S; D2是低级烷基，低级环烷基，低级烷基环烷基，低级环烷基烷基，低级环烷氧基烷基或低级烷基环烷氧基; Z1和Z2独立地是氢，卤素，低级烷基，低级环烷基，低级烷氧基，低级环烷氧基，卤素，-CF3，-OCONR14R14'，-CN，-CONR14R14'，-SOR12，-SO2R12，-NR14COR14'，-NR14CO2R14' ，-CO 2 R 12，NR 14 SO 2 R 12或-COR 12，条件是如果Z 1是-CH 3并且R 1，R 2或R 3中的一个是F，则Z 2不能是H。 R5，R6和R7独立地选自氢，卤素，低级烷基，低级环烷基，-CF3，-SR12，低级烷氧基，低级环烷氧基，-OCH2OMe，-CN，-CONR14R14'，SOR12，SO2R12， NR14COR14'，NR14CO2R12，CO2R12，NR14SO2R12和-COR12; R8，R9，R10，R10'，R11独立地为氢或低级烷基; R12是低级烷基或低级环烷基; 并且R 14和R 14'独立地为H，低级烷基，低级环烷基或R 14和R 14'与它们所连接的N一起形成具有4至7个原子的环。这些化合物可用于治疗MCHR1介导的疾病，例如肥胖症，糖尿病，IBD，抑郁症和焦虑症。

8. 发明申请

WO2005030758A1 PYRIMIDINE AND PYRIDINE DERIVATIVES USEFUL AS HMG-COA REDUCTASE INHIBITORS AND METHOD OF PREPARATION THEREOF 审中-公开
标题翻译：用作HMG-COA还原酶抑制剂的吡嗪和吡啶衍生物及其制备方法
公开(公告)号：WO2005030758A1
公开(公告)日：2005-04-07
申请号：PCT/US2004/031212
申请日：2004-09-22
申请人： BRISTOL-MYERS SQUIBB COMPANY , AHMAD, Saleem , ROBL, Jeffrey, A. , NGU, Khehyong
发明人： AHMAD, Saleem , ROBL, Jeffrey, A. , NGU, Khehyong
IPC分类号： C07D403/12
CPC分类号： C07D213/74 , C04B35/632 , C07D239/42 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： Compounds are provided having the following structure which are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia, dyslipidemia, hormone replacement therapy, hypercholsterolemia, hypertriglyceridemia and atherosclerosis as well as Alzheimer's disease and osteoporosis identified in Formula (I) wherein X is N or CR 5 ; and pharmaceutically acceptable salts thereof, Z is identified in Formula (II) or in Formula (III) ; wherein R 1 to R 7 are as defined herein. A method for treating the above diseases employing the above compounds is also provided.
摘要翻译：提供具有以下结构的化合物，其为HMG CoA还原酶抑制剂，因此具有抑制胆固醇生物合成，调节血清脂质，例如降低LDL胆固醇和/或增加HDL胆固醇，以及治疗高脂血症，血脂异常，激素替代疗法，高胆固醇血症，高甘油三酯血症和动脉粥样硬化以及式（I）中鉴定的阿尔茨海默病和骨质疏松症，其中X是N或CR5; Z在式（II）或式（III）中鉴定; 其中R 1至R 7如本文所定义。还提供了使用上述化合物治疗上述疾病的方法。

9. 发明申请

WO2003011824A1 BICYCLIC MODULATORS OF ANDROGEN RECEPTOR FUNCTION 审中-公开
标题翻译：雄激素受体功能的双相调制剂
公开(公告)号：WO2003011824A1
公开(公告)日：2003-02-13
申请号：PCT/US2002/024185
申请日：2002-07-31
申请人： BRISTOL-MYERS SQUIBB COMPANY , SUN, Chongqing , ROBL, Jeffrey, A. , SALVATI, Mark, E. , WANG, Tammy , HAMANN, Lawrence , AUGERI, David
发明人： SUN, Chongqing , ROBL, Jeffrey, A. , SALVATI, Mark, E. , WANG, Tammy , HAMANN, Lawrence , AUGERI, David
IPC分类号： C07D207/09
CPC分类号： C07D207/16 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The invention provides compounds of the formula I [INSERT CHEMICAL STRUCTURE HERE]wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia, and also provided are pharmaceutical compositions containing such compounds.
摘要翻译：本发明提供了式I化合物[其中化学结构如此），其中取代基如本文所述。还提供了使用这些化合物治疗核激素受体相关病症（如与年龄相关的疾病，例如肌肉减少症）的方法，并且还提供含有这些化合物的药物组合物。

10. 发明申请

WO1997043257A1 INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND METHOD 审中-公开
标题翻译： MICROSOMAL TRIGLYCERIDE转移蛋白的抑制剂和方法
公开(公告)号：WO1997043257A1
公开(公告)日：1997-11-20
申请号：PCT/US1997007603
申请日：1997-05-06
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BRISTOL-MYERS SQUIBB COMPANY , DICKSON, John, K., Jr. , ROBL, Jeffrey, A. , BILLER, Scott, A.
IPC分类号： C07D207/12
CPC分类号： C07D207/273 , C07D207/14 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D473/00
摘要： Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have structure (1) or (2) wherein R to R , Q, W and X are as defined herein.
摘要翻译：提供抑制微粒体甘油三酯转运蛋白的化合物，因此可用于降低血清脂质和治疗动脉粥样硬化及相关疾病。化合物具有结构（1）或（2），其中R 1至R 6，Q，W和X如本文所定义。

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