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1. 发明申请

WO2021163254A1 HETEROCYCLIC PAD4 INHIBITORS 审中-公开
公开(公告)号：WO2021163254A1
公开(公告)日：2021-08-19
申请号：PCT/US2021/017554
申请日：2021-02-11
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： SELVAKUMAR, Kumaravel , PAIDI, Venkatram Reddy , THANGATHIRUPATHY, Srinivasan , KUMAR CM, Vijaya , ALAJANGI, Tirupathi, Rao , SURA, Mallikarjun, Reddy , MAHADEVU, Krishna , SISTLA, Ramesh, Kumar , AGARWAL, Piyush , SUBBIAH KARUPPIAH, Arul, Mozhi , NAIR, Jalathi, S. , MORAMPUDI, Ooha , PANDA, Manoranjan , TINO, Joseph, A. , CHERNEY, Robert, J. , DUNCIA, John, V. , GARDNER, Daniel, S. , DHAR, T., G., Murali , ROSS, Audrey, Graham , GORMISKY, Paul, E. , ZHU, Xiao , SELETSKY, Boris, M. , ANTROPOW, Alyssa, H. , NIU, Deqiang , ZHU, Zhengdong , MIAO, Guobin , CUERVO, Julio, Hernán
IPC分类号： C07D401/14 , A61K31/41 , C07D403/14 , C07D413/14 , A61P35/00 , A61P19/00 , C07D407/14 , C07D409/14
摘要： The disclosure generally relates to substituted heterocyclic compounds of Formula (Ia), which are inhibitors of PAD4, method for preparing these compounds, pharmaceutical compositions comprising these compounds and use of these compounds in the treatment of a disease or a disorder associated with PAD4 enzyme activity.

2. 发明申请

WO2022241172A1 SUBSTITUTED HETEROCYCLIC COMPOUNDS 审中-公开
公开(公告)号：WO2022241172A1
公开(公告)日：2022-11-17
申请号：PCT/US2022/029105
申请日：2022-05-13
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： SPERGEL, Steven, H. , MOSLIN, Ryan, M. , MERTZMAN, Michael, Edward , POSY, Shoshana, L. , LAKKARAJU, Sirish, Kaushik , TINO, Joseph, A. , XIAO, Zili , LIU, Chunjian , LIN, James
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , A61P29/00 , A61P37/00 , A61K31/501
摘要： There are disclosed compounds of the following formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.

3. 发明申请

WO2005027908A1 COMPOUNDS USEFUL AS MOTILIN AGONISTS AND METHOD 审中-公开
标题翻译：化合物作为动力学和方法有用
公开(公告)号：WO2005027908A1
公开(公告)日：2005-03-31
申请号：PCT/US2004/030546
申请日：2004-09-16
申请人： BRISTOL-MYERS SQUIBB COMPANY , LI, James, J. , CHAO, Hannguang, J. , TINO, Joseph, A. , EWING, William, R.
发明人： LI, James, J. , CHAO, Hannguang, J. , TINO, Joseph, A. , EWING, William, R.
IPC分类号： A61K31/503
CPC分类号： C07D471/20 , A61K31/503
摘要： A method is provided for treating disorders of gastrointestinal motility which include the steps of administering to a patient in need of treatment of a compound having the structure or a pharmaceutically acceptable salt thereof, a prodrug ester thereof, and all stereoisomers thereof, wherein R1 is selected from alkyl, aryl, cycloalkyl, alkenyl, alkynyl, arylalkyl, heteroaryl, heteroarylalkyl or heterocycloalkyl; Z is selected from -CON(R 4 )R 4a , -SO 2 N(R 4 )R 4a , -CN, and R 4 and R 4a are the same or different and are independently selected from hydrogen, alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl or R 4 and R 4a can be joined together to form a heterocycle; R 4b is selected from hydrogen, halogen, hydroxyl, CN, OCF 3 , CF 3 , CONH 2 , SONH 2 , SO 2 CH 3 , NHCOCH 3 or NHCO 2 CH 3 ; and Q is a substituted bicyclic heterocycle. New compounds for use in treating disorders of gastrointestinal motility are also provided.
摘要翻译：提供了一种治疗胃肠蠕动障碍的方法，其包括对需要治疗具有其结构或其药学上可接受的盐的化合物，其前药酯及其所有立体异构体的患者给药的步骤，其中选择R1 烷基，芳基，环烷基，烯基，炔基，芳基烷基，杂芳基，杂芳基烷基或杂环烷基; Z选自-CON（R4）R4a，-SO2N（R4）R4a，-CN，R4和R4a相同或不同，独立地选自氢，烷基，环烷基，芳基，芳基烷基，杂芳基或杂芳基烷基或 R4和R4a可以连接在一起形成杂环; R4b选自氢，卤素，羟基，CN，OCF3，CF3，CONH2，SONH2，SO2CH3，NHCOCH3或NHCO2CH3; Q是取代的双环杂环。还提供了用于治疗胃肠蠕动障碍的新化合物。

4. 发明申请

WO2004021984A2 HETEROCYCLIC AROMATIC COMPOUNDS USEFUL AS GROWTH HORMONE SECRETAGOGUES 审中-公开
标题翻译：杂环芳香族化合物可用作生长激素分泌物
公开(公告)号：WO2004021984A2
公开(公告)日：2004-03-18
申请号：PCT/US2003/027513
申请日：2003-09-02
申请人： BRISTOL-MYERS SQUIBB COMPANY , YU, Guixue , LI, Jun , EWING, William, R. , SULSKY, Richard, B. , LI, James, J. , TINO, Joseph, A.
发明人： YU, Guixue , LI, Jun , EWING, William, R. , SULSKY, Richard, B. , LI, James, J. , TINO, Joseph, A.
IPC分类号： A61K
CPC分类号： C07D487/04 , C07D231/56 , C07D261/20 , C07D471/04 , C07D513/04
摘要： Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula (I) wherein R 1 , R 1 ', R 2 , R 3 , R 4 , Xa, Y, Z, and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
摘要翻译：提供可用于刺激内源性生长或生长激素释放的新型杂环芳族化合物，所述化合物具有式（I）的通式结构其中R 1，R 1，R 2，R 3，R 4，X a，Y，Z和n分别为在此描述。本文提供的化合物可用于治疗肥胖症，骨质疏松症（改善骨密度）和改善肌肉质量和肌肉力量。

5. 发明申请

WO2022241171A1 SUBSTITUTED HETEROCYCLIC COMPOUNDS 审中-公开
公开(公告)号：WO2022241171A1
公开(公告)日：2022-11-17
申请号：PCT/US2022/029102
申请日：2022-05-13
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： SPERGEL, Steven, H. , MOSLIN, Ryan, M. , MERTZMAN, Michael, Edward , TINO, Joseph, A. , POSY, Shoshana, L. , LAKKARAJU, Sirish Kaushik , XIAO, Zili , KEMPSON, James
IPC分类号： C07D401/14 , C07D403/12 , A61P29/00 , A61P37/00 , A61K31/501
摘要： There are disclosed compounds of the following formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.

6. 发明申请

WO2008006043A3 1,3-OXAZOLE DERIVATIVES USEFUL AS ANTI-ATHEROSCLEROTIC, ANTI-DYSLIPIDEMIC, ANTI-DIABETIC AND ANTI-OBESITY AGENTS 审中-公开
公开(公告)号：WO2008006043A3
公开(公告)日：2008-01-10
申请号：PCT/US2007/072891
申请日：2007-07-06
申请人： BRISTOL-MYERS SQUIBB COMPANY , TINO, Joseph, A. , CHENG, Peter, T.W. , SHI, Yan , LI, Jun , MUKHERJEE, Ranjan
发明人： TINO, Joseph, A. , CHENG, Peter, T.W. , SHI, Yan , LI, Jun , MUKHERJEE, Ranjan
IPC分类号： C07D263/32 , A61K31/421 , A61P3/00
摘要： Compounds are provided which have the structure of Formula (I): wherein R1 is halogen; and X is hydrogen or halogen, and salts thereof, which compounds are useful as anti-atherosclerotic, anti-dyslipidemic, anti-diabetic, and anti-obesity agents.

7. 发明申请

WO1998027979A1 HETEROCYCLIC INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND METHOD 审中-公开
标题翻译：微量TRIGLYCERIDE转移蛋白和方法的杂环抑制剂
公开(公告)号：WO1998027979A1
公开(公告)日：1998-07-02
申请号：PCT/US1997021950
申请日：1997-12-02
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BRISTOL-MYERS SQUIBB COMPANY , TINO, Joseph, A.
IPC分类号： A61K31/24
CPC分类号： C07D233/64 , C07D401/06 , C07D403/10 , C07D417/14
摘要： Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have structure (I), including pharmaceutically acceptable salts thereof, or prodrug esters thereof, A is (II) or (III) where Z is N or CH, or where Z is (IV) or CH2 when --- is a single bond; Q is (1) -O-; (2) -S-; or (3) (V); B is (VI) or (VII) or (VIII) or (IX) wherein a = 2, 3 or 4 or (X) or (XI) or (XII); and wherein L , R, R , R , R , R , R , R , R , R , R , X, (XIII), (XIV) and (XV) are as defined herein.
摘要翻译：提供作为MTP抑制剂的新型化合物，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，并且具有结构（I），包括其药学上可接受的盐或其前药酯，A是（II）或（III ）其中Z是N或CH，或当Z是（Ⅳ）或CH 2时，其中Z是单键; Q是（1）-O-; （2）-S-; 或（3）（V）; B是（VI）或（VII）或（VIII）或（IX）其中a = 2,3或4或（X）或（XI）或（XII）; 并且其中L 1，R 2，R 1，R 3，R 3，R 3a，R 3b，R 4，R 4，R 5，，R 5a，X，（XIII），（XIV）和（XV）如本文所定义。

8. 发明申请

WO1997026240A1 CONFORMATIONALLY RESTRICTED AROMATIC INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND METHOD 审中-公开
标题翻译： MICROSOMAL TRIGLYCERIDE转移蛋白的连续限制性芳香抑制剂和方法
公开(公告)号：WO1997026240A1
公开(公告)日：1997-07-24
申请号：PCT/US1997000587
申请日：1997-01-13
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BRISTOL-MYERS SQUIBB COMPANY , BILLER, Scott, A. , DICKSON, John, K. , LAWRENCE, R., Michael , MAGNIN, David, R. , POSS, Michael, A. , ROBL, Jeffrey, A. , SLUSARCHYK, William, A. , SULSKY, Richard, B. , TINO, Joseph, A.
IPC分类号： C07C217/04
CPC分类号： C07D307/14 , A61K31/191 , A61K31/366 , A61K31/404 , A61K31/4468 , C07C17/093 , C07C47/453 , C07C49/563 , C07C49/567 , C07C49/573 , C07C69/00 , C07C205/11 , C07C205/43 , C07C205/55 , C07C233/58 , C07C233/59 , C07C233/60 , C07C233/62 , C07C233/63 , C07C233/78 , C07C235/40 , C07C235/56 , C07C237/22 , C07C237/24 , C07C255/41 , C07C259/08 , C07C271/22 , C07C291/04 , C07C311/19 , C07C311/21 , C07C311/37 , C07C311/42 , C07C311/46 , C07C317/12 , C07C321/22 , C07C323/60 , C07C2601/02 , C07C2601/14 , C07C2603/00 , C07C2603/18 , C07C2603/32 , C07C2603/74 , C07D207/335 , C07D207/38 , C07D209/08 , C07D209/16 , C07D209/34 , C07D209/38 , C07D209/46 , C07D209/48 , C07D211/60 , C07D211/62 , C07D213/40 , C07D213/64 , C07D213/74 , C07D213/75 , C07D213/80 , C07D213/89 , C07D221/16 , C07D231/56 , C07D233/24 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/06 , C07D235/08 , C07D235/16 , C07D235/24 , C07D235/26 , C07D235/28 , C07D235/30 , C07D239/38 , C07D239/42 , C07D239/47 , C07D249/12 , C07D249/14 , C07D249/18 , C07D253/07 , C07D263/38 , C07D263/46 , C07D263/58 , C07D271/07 , C07D277/36 , C07D277/56 , C07D277/74 , C07D285/08 , C07D285/125 , C07D295/108 , C07D295/155 , C07D295/185 , C07D311/84 , C07D317/30 , C07D317/58 , C07D319/06 , C07D327/06 , C07D333/20 , C07D335/14 , C07D401/12 , C07D403/04 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07F7/1804 , C07C25/22
摘要： Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure (I) or (IA) or (IB) including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0,1 or 2; R is H, alkyl, aryl or halogen; A is (1) a bond; (2) -O-; or (3) (i); B is: (ii) or (iii) or (iv) or (v) (wherein (a = 2, 3 or 4)) or (vi) or (vii) or (viii); and wherein L , L , R , R , R , R , R , R , R , R , R , X, (ix), (x) and (xi) are as defined herein.
摘要翻译：提供了作为MTP抑制剂的新型化合物，因此可用于降低血清脂质和治疗动脉粥样硬化和相关疾病，并且具有结构（I）或（IA）或（IB），包括其药学上可接受的盐或其前药酯，其中 q为0,1或2; R x是H，烷基，芳基或卤素; A是（1）债券; （2）-O- 或（3）（i）; B是：（ii）或（iii）或（iv）或（v）（其中（a = 2,3或4））或（vi）或（vii）或（viii）其中L 2，L 1，R 1，R 2，R 3，R 3，R 3a，R 3b，R 4， R 5，X，（ix），（x）和（xi）如本文所定义。

9. 发明申请

WO1996026205A1 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：WO1996026205A1
公开(公告)日：1996-08-29
申请号：PCT/US1996000824
申请日：1996-02-01
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BRISTOL-MYERS SQUIBB COMPANY , WETTERAU, John, R. II , SHARP, Daru, Young , GREGG, Richard, E. , BILLER, Scott, A. , DICKSON, John, A. , LAWRENCE, R., Michael , MAGNIN, David, R. , POSS, Michael, A. , ROBL, Jeffrey, A. , SULSKY, Richard, B. , TINO, Joseph, A. , LAWSON, John, E. , HOLAVA, Henry, M. , PARTYKA, Richard, A.
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D211/58 , C07D211/60 , C07D211/94 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12 , G01N2800/044
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 the structure (a, b, c or d) wherein R to R , Q, 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。化合物具有其中R 1至R 6，Q和X如本文所定义的结构（a，b，c或d）。

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