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1. 发明申请

WO2016065226A1 INDOLE CARBOXAMIDES COMPOUNDS USEFUL AS KINASE INHOBITORS 审中-公开
标题翻译：吲哚类化合物可用作激酶抑制剂
公开(公告)号：WO2016065226A1
公开(公告)日：2016-04-28
申请号：PCT/US2015/057055
申请日：2015-10-23
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： AHMAD, Saleem , TINO, Joseph A. , MACOR, John E. , TEBBEN, Andrew J. , GONG, Hua , LIU, Qingjie , BATT, Douglas G. , NGU, Khehyong , WATTERSON, Scott Hunter , GUO, Weiwei , BEAUDOIN BERTRAND, Myra
IPC分类号： C07D403/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/10 , C07D209/18 , A61K31/4045 , A61P29/00 , A61P37/00
CPC分类号： C07D401/10 , C07D209/08 , C07D209/18 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/10
摘要： Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR 4 or N; R 1 , R 2 , R 3 , R 4 , and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译：公开了式（I）的化合物或其盐，其中：X是CR 4或N; R1，R2，R3，R4和A在本文中定义。还公开了使用这种化合物作为Bruton酪氨酸激酶（Btk）的抑制剂的方法和包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫疾病和血管疾病）中的疾病或病症的进展。

2. 发明申请

WO2016064957A1 BICYCLIC HETEROARYL AMINE COMPOUNDS AS PI3K INHIBITORS 审中-公开
标题翻译：双酚A异构化合物作为PI3K抑制剂
公开(公告)号：WO2016064957A1
公开(公告)日：2016-04-28
申请号：PCT/US2015/056576
申请日：2015-10-21
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BHIDE, Rajeev S. , BATT, Douglas G. , CHERNEY, Robert J. , CORNELIUS, Lyndon A.M. , LIU, Qingjie , MARCOUX, David , NEELS, James , POSS, Michael A. , QIN, Lan-ying , RUAN, Zheming , SHI, Qing , SRIVASTAVA, Anurag S. , TINO, Joseph A. , WATTERSON, Scott Hunter
IPC分类号： C07D487/04 , C07D491/08 , A61K31/4985 , A61K31/53 , A61K31/5377 , A61K31/541 , A61P29/00
CPC分类号： C07D491/08 , C07D487/04
摘要： Disclosed are compounds of Formula (I) or a salt thereof; wherein: X is N or CH; Q 1 is: (i) C1, Br, I, -CN, -CH 3 , or -CF 3 ; (ii) a 5-membered heteroaryl selected from pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, and thiadiazolyl; (iii) a 6?membered heteroaryl selected from pyridinyl, pyridazinyl, and pyrimidinyl; or (iv) a bicyclic heteroaryl selected from indolyl, pyrrolopyridinyl, pyrazolopyridinyl and benzo[d]oxazolyl; wherein each of said 5-membered, 6-membered, and bicyclic heteroaryl is substituted with zero to 1 R a and zero to 1 R b ; and R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R a , and R b are defined herein. Also disclosed are methods of using such compounds as modulators of PI3K, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.
摘要翻译：公开了式（I）的化合物或其盐; 其中：X为N或CH; Q1是：（i）C1，Br，I，-CN，-CH3或-CF3; （ii）选自吡咯基，吡唑基，咪唑基，恶唑基，噻唑基，三唑基，恶二唑基和噻二唑基的5元杂芳基。（iii）选自吡啶基，哒嗪基和嘧啶基的6元杂芳基; 或（iv）选自吲哚基，吡咯并吡啶基，吡唑并吡啶基和苯并[d]恶唑基的双环杂芳基; 其中所述5元，6元和双环杂芳基中的每一个被0至1个Ra和0至1个Rb取代; 并且R 1，R 2，R 3，R 4，R 5，R 6，R a和R b在本文中定义。还公开了使用这种化合物作为PI3K的调节剂的方法和包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓炎症和自身免疫性疾病。

3. 发明申请

WO2023034732A1 COMPOUND USEFUL FOR PET-IMAGING OF BRUTON'S TYROSINE KINASE 审中-公开
公开(公告)号：WO2023034732A1
公开(公告)日：2023-03-09
申请号：PCT/US2022/075556
申请日：2022-08-29
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： DONNELLY, David J. , ALLENTOFF, Alban J. , WALLACE, Michael Arthur , BONACORSI, Samuel J. , WATTERSON, Scott Hunter , TINO, Joseph A.
IPC分类号： A61K51/04 , A61K101/00
摘要： Disclosed is a compound of Formula (Ib): The compound of Formula (Ib) is useful for positron emission tomography (PET) imaging of Bruton's Tyrosine Kinase (BTK) in mammals. Also disclosed are methods of using the compound as a labeling and diagnostic imaging agent of Bruton's Tyrosine Kinase (BTK), and methods of preparing Compound (Ib).

4. 发明申请

WO2016065236A1 CARBAZOLE DERIVATIVES 审中-公开
标题翻译：卡博唑衍生物
公开(公告)号：WO2016065236A1
公开(公告)日：2016-04-28
申请号：PCT/US2015/057077
申请日：2015-10-23
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： AHMAD, Saleem , BATT, Douglas G. , LIU, Qingjie , MACOR, John E. , TINO, Joseph A. , WATTERSON, Scott Hunter , NAIR, Satheesh Kesavan , MAISHAL, Tarun Kumar
IPC分类号： C07D401/04 , C07D403/04 , C07D471/04 , C07D209/88 , A61K31/403 , A61P29/00 , A61P37/00
CPC分类号： C07D209/88 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D471/04 , C07D471/10 , C07D487/04 , C07D495/04
摘要： Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein Q, R 1a , R 1b , R 2a , R 2b , R 3 , R 4 , R 5a , R 5b , R 6a , R 6c , R 7a , R 7b , R 7c , and R 7d are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译：公开了式（I）：（I）的化合物或其盐，其中Q，R1a，R1b，R2a，R2b，R3，R4，R5a，R5b，R6a，R6c，R7a，R7b，R7c和R7d定义于此。还公开了使用这种化合物作为Bruton酪氨酸激酶（Btk）的抑制剂的方法和包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫疾病和血管疾病）中的疾病或病症的进展。

5. 发明申请

WO2016064958A1 HETEROARYL SUBSTITUTED PYRROLOTRIAZINE AMINE COMPOUNDS AS PI3K INHIBITORS 审中-公开
标题翻译：作为PI3K抑制剂的异氟醚取代的吡咯烷胺化合物
公开(公告)号：WO2016064958A1
公开(公告)日：2016-04-28
申请号：PCT/US2015/056577
申请日：2015-10-21
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BHIDE, Rajeev S. , RUAN, Zheming , CHERNEY, Robert J. , CORNELIUS, Lyndon A.M. , DHAR, T.G. Murali , GONG, Hua , MARCOUX, David , POSS, Michael A. , QIN, Lan-ying , SHI, Qing , TINO, Joseph A.
IPC分类号： C07D487/04 , A61K31/53 , A61K31/5377 , A61K31/541 , A61P29/00
CPC分类号： C07D487/04
摘要： Disclosed are compounds of Formula (I); or a salt thereof; wherein Qi is (i) C1, Br, I, -CN, -CH 3 , or -CF 3 ; or (ii) pyrazole, triazole, or pyridinyl, each substituted with R 1 ; Q 2 is pyridinyl, indazolyl, isoquinolinyl, or benzo[d]imidazolyl substituted with R 2 and R 3 ; and R 1 , R 2 , and R 3 are defined herein. Also disclosed are methods of using such compounds as modulators of PI3K, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.
摘要翻译：公开了式（I）的化合物; 或其盐; 其中Qi是（i）C1，Br，I，-CN，-CH3或-CF3; 或（ii）各自被R 1取代的吡唑，三唑或吡啶基; Q2是被R2和R3取代的吡啶基，吲唑基，异喹啉基或苯并[d]咪唑基; 并且R1，R2和R3在本文中定义。还公开了使用这种化合物作为PI3K的调节剂的方法和包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓炎症和自身免疫性疾病。

6. 发明申请

WO2008005964A2 NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME 审中-公开
标题翻译：新型GLUCOKINASE激活剂及其使用方法
公开(公告)号：WO2008005964A2
公开(公告)日：2008-01-10
申请号：PCT/US2007/072708
申请日：2007-07-03
申请人： BRISTOL-MYERS SQUIBB COMPANY , RYONO, Dennis E. , CHENG, Peter T.W. , BOLTON, Scott A. , CHEN, Sean S. , SHI, Yan , MENG, Wei , TINO, Joseph A. , ZHANG, Hao , SULSKY, Richard B.
发明人： RYONO, Dennis E. , CHENG, Peter T.W. , BOLTON, Scott A. , CHEN, Sean S. , SHI, Yan , MENG, Wei , TINO, Joseph A. , ZHANG, Hao , SULSKY, Richard B.
IPC分类号： C07F9/32 , C07F9/40 , A61K31/675 , A61P3/00
CPC分类号： C07F9/6539 , C07F9/582 , C07F9/587 , C07F9/65032 , C07F9/650964 , C07F9/650982 , C07F9/65181
摘要： Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure of Formula (I), wherein Formula (II) is a heteroaryl ring; R 4 is -(CH 2 ) n -Z-(CH 2 ) m -PO(OR 7 )(OR 8 ), -(CH 2 ) n Z-(CH 2 ) m -PO(OR 7 )R 9 , -(CH 2 ) n -Z-(CH 2 ) m -OPO(OR 7 )R 9 , -(CH 2 ) n Z-(CH 2 ) m -OPO(R 9 )(R 10 ), or -(CH 2 ) n Z-(CH 2 ) m -PO(R 9 )(R 10 ); R 5 and R6 are independently selected from H, alkyl and halogen; Y is R 7 (CH 2 ) s or is absent; and X, n, Z, m, R 4 , R 5 , R 6 , R 7 , and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.
摘要翻译：提供了膦酸酯和次膦酸酯活化剂的化合物，因此可用于治疗糖尿病和相关疾病，并具有式（I）的结构，其中式（II）是杂芳基环; R 4是 - （CH 2 CH 2）n - （CH 2）n - （OR 7）（OR 8）， - （CH 2 CH 2）n - Z - （ CH 2 OR 2（OR 7）R 9， - （CH 2 CH 2） SUB>）_{名词 -Z-（CH _{2 ）_{米 -OPO（OR _{7 ）R _{9 - （CH 2）n - Z - （CH 2）2 - （O） - （CH 2）n - （R 10），或 - （CH 2）n - Z - （CH 2） 2 ）_{米 -PO（R _{9 ）（R _{10 ）; R 5和R 6独立地选自H，烷基和卤素; Y是R 7（CH 2）2，或不存在; 和X，n，Z，m，R 4，R 5，R 6，R 7，和 s如本文所定义; 或其药学上可接受的盐。还提供了使用上述化合物治疗糖尿病和相关疾病的方法。}}}}}}}}

7. 发明申请

WO2005027637A1 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：WO2005027637A1
公开(公告)日：2005-03-31
申请号：PCT/US2004/030547
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： A01N43/58
CPC分类号： C07D471/20 , A61K31/495 , A61K31/50
摘要： Compounds are provided which are useful in treating disorders of gastrointestinal motility and which have the structure [INSERT CHEMICAL STRUCTURE HERE] or a pharmaceutically acceptable salt thereof, a prodrug ester thereof, and all stereoisomers thereof, wherein R1 and R2 are the same or different and are independently selected from hydrogen, alkyl, aryl, cycloalkyl, alkenyl, alkynyl, arylalkyl, heteroaryl, heteroarylalkyl or heterocycloalkyl; Z is selected from -CON(R4)R4a, -CO2R4, -SO2N(R4)R4a, -SO2R4, CN, and [CHEMICAL STRUCTURE] , [CHEMICAL STRUCTURE] , [CHEMICAL STRUCTURE] , [CHEMICAL STRUCTURE] or [CHEMICAL STRUCTURE] ; R4 and R4a are the same or different and are independently selected from hydrogen, alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl or R4 and R4a can be joined together to form a heterocycle. R4b is selected from hydrogen, halogen, hydroxyl, CN, OCF3, CF3, CONH2, SONH2, SO2CH3, NHCOCH3 or NHCO2CH3; and Q is a substituted bicyclic heterocycle. A method for using such compounds for treating disorders of gastrointestinal motility is also provided.
摘要翻译：提供可用于治疗胃肠蠕动障碍的化合物，其具有[INSERT CHEMICAL STRUCTURE HERE]或其药学上可接受的盐，其前药酯及其所有立体异构体，其中R 1和R 2相同或不同，独立地选自氢，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; [化学结构]，[化学结构]，[化学结构]或[化学结构]（化学结构）中，Z选自-CON（R4）R4a，-CO2R4，-SO2N（R4）R4a，-SO2R4，CN， ]; R4和R4a相同或不同并且独立地选自氢，烷基，环烷基，芳基，芳基烷基，杂芳基或杂芳基烷基，或者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。还提供了使用这些化合物治疗胃肠蠕动障碍的方法。

8. 发明申请

WO2014210085A1 SUBSTITUTED TETRAHYDROCARBAZOLE AND CARBAZOLE CARBOXAMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：用作激酶抑制剂的替代四氯化碳和卡博唑酰胺化合物
公开(公告)号：WO2014210085A1
公开(公告)日：2014-12-31
申请号：PCT/US2014/043978
申请日：2014-06-25
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： TINO, Joseph A. , SRIVASTAVA, Anurag S. , KO, Soo Sung , GALELLA, Michael A. , LANGEVINE, Charles M. , DELUCCA, George V. , LIU, Qingjie , BATT, Douglas G. , WATTERSON, Scott Hunter , SHI, Qing , BERTRAND, Myra Beaudoin
IPC分类号： C07D403/10 , C07D471/04 , C07D513/04 , A61K31/429 , A61K31/513 , A61K31/517 , A61K31/522 , A61P37/00 , A61P29/00
CPC分类号： C07D513/04 , C07B2200/07 , C07B2200/13 , C07D209/88 , C07D239/70 , C07D403/10 , C07D471/04
摘要： Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: R 1 is F, Cl, CN, or CH 3 ; R 2 is Cl or CH 3 ; R 3 is C(CH 3 ) 2 OH or CH 2 CH 2 OH; R a is H or CH 3 ; each R 6 is independently F, Cl, CH 3 , and/or OCH 3 ; and n is zero, 1, or 2. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译：公开了式（I）的化合物，其中：两条虚线表示两个单键或双键; Q是：R1是F，Cl，CN或CH3; R2是Cl或CH3; R3是C（CH3）2OH或CH2CH2OH; Ra为H或CH3; 每个R 6独立地是F，Cl，CH 3和/或OCH 3; 并且n为0,1或2.还公开了使用这种化合物作为Bruton酪氨酸激酶（Btk）的抑制剂的方法和包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫疾病和血管疾病）中的疾病或病症的进展。

9. 发明申请

WO2005070884A3 HETEROCYCLIC COMPOUNDS USEFUL AS GROWTH HORMONE SECRETAGOGUES 审中-公开
公开(公告)号：WO2005070884A3
公开(公告)日：2005-08-04
申请号：PCT/US2005/001013
申请日：2005-01-12
申请人： BRISTOL-MYERS SQUIBB COMPANY , ZHAI, Weixu , GERRITZ, Samuel , ANDRES, Charles J., Jr. , TINO, Joseph A.
发明人： ZHAI, Weixu , GERRITZ, Samuel , ANDRES, Charles J., Jr. , TINO, Joseph A.
IPC分类号： C07D207/09 , A61K31/40
摘要： The present invention relates to novel heterocyclic compounds, according to Formula I, that stimulate endogenous production and/or release of growth hormone, wherein R1, R2, R3, R4 and X are defined herein. Further, the present invention relates to methods for using such compounds and to pharmaceutical compositions containing such compounds.

10. 发明公开

EP3209665A1 HETEROARYL SUBSTITUTED PYRROLOTRIAZINE AMINE COMPOUNDS AS PI3K INHIBITORS 有权
标题翻译：杂芳基取代的吡咯并三嗪胺类化合物作为PI3K抑制剂
公开(公告)号：EP3209665A1
公开(公告)日：2017-08-30
申请号：EP15787838.0
申请日：2015-10-21
申请人： Bristol-Myers Squibb Company
发明人： BHIDE, Rajeev S. , RUAN, Zheming , CHERNEY, Robert J. , CORNELIUS, Lyndon A.M. , DHAR, T.G. Murali , GONG, Hua , MARCOUX, David , POSS, Michael A. , QIN, Lan-ying , SHI, Qing , TINO, Joseph A.
IPC分类号： C07D487/04 , A61K31/53 , A61K31/5377 , A61K31/541 , A61P29/00
CPC分类号： C07D487/04
摘要： Disclosed are compounds of Formula (I); or a salt thereof; wherein Qi is (i) C1, Br, I, -CN, -CH3, or -CF3; or (ii) pyrazole, triazole, or pyridinyl, each substituted with R1; Q2 is pyridinyl, indazolyl, isoquinolinyl, or benzo[d]imidazolyl substituted with R2 and R3; and R1, R2, and R3 are defined herein. Also disclosed are methods of using such compounds as modulators of PI3K, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.
摘要翻译：公开了式（I）的化合物; 或其盐; 其中Q 1是（i）Cl，Br，I，-CN，-CH 3或-CF 3; 或（ii）各自被R 1取代的吡唑，三唑或吡啶基; Q2是被R2和R3取代的吡啶基，吲唑基，异喹啉基或苯并[d]咪唑基; 并且R1，R2和R3在本文中定义。还公开了使用这种化合物作为PI3K调节剂的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓炎症和自身免疫性疾病。

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