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1. 发明申请

WO2014047117A1 PROCESS FOR PREPARING PHOSPHORAMIDATE DERIVATIVES OF NUCLEOSIDE COMPOUNDS FOR TREATMENT OF VIRAL INFECTIONS 审中-公开
标题翻译：制备用于治疗病毒感染的核苷酸化合物的磷酸酯衍生物的方法
公开(公告)号：WO2014047117A1
公开(公告)日：2014-03-27
申请号：PCT/US2013/060306
申请日：2013-09-18
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： SCHMIDT, Michael , SILVERMAN, Steven , EASTGATE, Martin D.
IPC分类号： C07H1/02 , C07H19/06 , C07H19/16
CPC分类号： C07H1/02 , C07H19/06 , C07H19/16
摘要： Processes for the production of nucleoside phosphoramidate compounds having the following Formula I are provided.
摘要翻译：提供了制备具有下列通式I的核苷氨基磷酸酯化合物的方法。

2. 发明申请

WO2012078593A3 LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS AND THEIR USE IN THE TREATMENT FIBROSIS 审中-公开
公开(公告)号：WO2012078593A3
公开(公告)日：2012-06-14
申请号：PCT/US2011/063465
申请日：2011-12-06
申请人： AMIRA PHARMACEUTICALS, INC. , SEIDERS, Thomas, Jon , WANG, Bowei , HUTCHINSON, John, Howard , STOCK, Nicholas, Simon , VOLKOTS, Deborah
发明人： SEIDERS, Thomas, Jon , WANG, Bowei , HUTCHINSON, John, Howard , STOCK, Nicholas, Simon , VOLKOTS, Deborah
IPC分类号： A61K31/192 , A61K31/27 , A61K31/381 , A61K31/415 , A61K31/421 , A61K31/44 , A61K31/47 , C07C53/134 , C07C271/28 , C07D213/75 , C07D217/16 , C07D231/36 , C07D263/48 , C07D333/16 , A61P19/04
摘要： Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.

3. 发明申请

WO2005116028A2 BICYCLIC HETEROCYCLES AS KINASE INHIBITORS 审中-公开
标题翻译：双相异构体作为激酶抑制剂
公开(公告)号：WO2005116028A2
公开(公告)日：2005-12-08
申请号：PCT/US2005/014164
申请日：2005-04-26
申请人： BRISTOL-MYERS SQUIBB COMPANY , BORZILLERI, Robert M. , KIM, Kyoung , CAI, Zhen-wei
发明人： BORZILLERI, Robert M. , KIM, Kyoung , CAI, Zhen-wei
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The compounds of the instant invention can be used as anticancer agents. More specifically, the invention comprises a compound having Formula (I) or (II),
摘要翻译：本发明的化合物可以用作抗癌剂。更具体地，本发明包括具有式（I）或（II）的化合物，

4. 发明申请

WO2002087335A1 METHOD FOR TREATING TUMORS BY THE ADMINISTRATION OF TEGAFUR, URACIL, FOLINIC ACID, AND CYCLOPHOSPHAMIDE 审中-公开
标题翻译：通过管理TEGAFUR，URACIL，FOLINIC ACID和CYPOPHOSPHAMIDE治疗肿瘤的方法
公开(公告)号：WO2002087335A1
公开(公告)日：2002-11-07
申请号：PCT/US2002/012769
申请日：2002-04-22
申请人： BRISTOL-MYERS SQUIBB COMPANY , WINER, Eric , BUNNELL, Craig , RESSLER-TATRO, Jody , DUGAN, Terry
发明人： WINER, Eric , BUNNELL, Craig , RESSLER-TATRO, Jody , DUGAN, Terry
IPC分类号： A01N43/04
CPC分类号： A61K31/675 , A61K31/505 , A61K31/513 , A61K31/70 , A61K31/7072 , A61K45/06 , A61K2300/00
摘要： This invention provides a method of treating a tumor in a warm-blooded animal, including humans, by administering, in combination, an anti-tumor effective amount of tegafur, uracil, folinic acid or pharmaceutically acceptable salt thereof and cyclophosphamide.
摘要翻译：本发明提供了一种通过组合施用抗肿瘤有效量的替加氟，尿嘧啶，亚叶酸或其药学上可接受的盐和环磷酰胺来治疗包括人在内的温血动物的肿瘤的方法。

5. 发明申请

WO2016210414A1 IDO INHIBITORS 审中-公开
标题翻译： IDO抑制剂
公开(公告)号：WO2016210414A1
公开(公告)日：2016-12-29
申请号：PCT/US2016/039564
申请日：2016-06-27
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BALOG, James Aaron , CHERNEY, Emily Charlotte , MARKWALDER, Jay A. , SHAN, Weifang , WILLIAMS, David K.
IPC分类号： C07D239/42 , C07C275/42 , C07D261/14 , C07D285/12 , A61K31/17 , A61K31/136 , A61P35/00
CPC分类号： C07D239/42 , C07C233/44 , C07C275/40 , C07C275/42 , C07C311/49 , C07C311/51 , C07C2601/02 , C07C2601/14 , C07D261/14 , C07D285/12
摘要： There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
摘要翻译：公开了调节或抑制吲哚胺2,3-双加氧酶（IDO）的酶活性的化合物，含有所述化合物的药物组合物和使用所述化合物治疗增殖性疾病如癌症，病毒感染和/或炎症性疾病的方法发明。

6. 发明申请

WO2013070879A1 METHODS FOR TREATING SPINAL CORD INJURY WITH LPA RECEPTOR ANTAGONISTS 审中-公开
标题翻译：用LPA受体拮抗剂治疗脊髓损伤的方法
公开(公告)号：WO2013070879A1
公开(公告)日：2013-05-16
申请号：PCT/US2012/064098
申请日：2012-11-08
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： SANTOS NOGUEIRA, Eva , LOPEZ VALES, Ruben
IPC分类号： A61K31/42 , A61K39/00 , A61P25/00
CPC分类号： A61K31/42
摘要： The invention is directed to methods for treating spinal cord injury and other neurological conditions by administering an LPA1 receptor antagonist or an autotaxin inhibiting compound.
摘要翻译：本发明涉及通过施用LPA1受体拮抗剂或自体贴剂抑制化合物来治疗脊髓损伤和其它神经病症的方法。

7. 发明申请

WO2010042682A1 AZOLOTRIAZINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：阿莫洛芬酮麦拉宁浓缩HORMONE受体-1拮抗剂
公开(公告)号：WO2010042682A1
公开(公告)日：2010-04-15
申请号：PCT/US2009/059941
申请日：2009-10-08
申请人： BRISTOL-MYERS SQUIBB COMPANY , DEVASTHALE, Pratik , WASHBURN, William N. , RENDUCHINTALA, Kishore V. , SRIDHAR, Radhakrishnan
发明人： DEVASTHALE, Pratik , WASHBURN, William N. , RENDUCHINTALA, Kishore V. , SRIDHAR, Radhakrishnan
IPC分类号： C07D487/04 , A61K31/53 , A61P3/04
CPC分类号： C07D487/04 , A61K31/53 , A61K31/541
摘要： The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I, wherein R 1 , is selected from the group consisting of monocyclic aryl or monocyclic heteroaryl; W is selected from the group consisting of a direct bond, -O-, and -N(R 6 )-; provided that if W is a direct bond, D is a cyclic amine that is attached to A via the nitrogen atom of the cyclic amine; D is selected from the group consisting of a direct bond, substituted or unsubstituted C 1 to C 4 alkyl, substituted or unsubstituted C 3 to C 7 cycloalkyl, cycloalkylalkyl, and 4- to 6-membered cyclic amines, provided that if D is a direct bond, R 2a , R 2b , and R 2c must be selected from H, alkyl, or cycloalkyl; E and G are independently N or CH provided that both are not N; R 1 is substituted or unsubstituted phenyl or substituted or unsubstituted monocyclic heteroaryl; R 2a , R 2b , and R 2c are independently selected from the group consisting of hydrogen, halo, cyano, hydroxyl, -NR 5 R 5a , -SO 2 R 34 , -CO 2 R 35 -NR 5 CO 2 R 21 , -NR 5 COR 21 , substituted or unsubstituted C 1 to C 4 alkyl, substituted or unsubstituted C 3 to C 7 cycloalkyl, substituted or unsubstituted 4- to 6-membered cyclic amines wherein said cyclic amine is optionally substituted with -OH, carbonylamino, alkoxycarbonylamino, or at least one of R 2a , R 2b , and R 2c is a prodrug moiety selected from amino acid esters or phosphoric acid esters wherein said amino acid ester has the formula -OC(O)CH(NH 2 )R 31 , wherein R 31 is H or C 1 to C 4 alkyl; or any two of R 2a , R b , or R 2c , may be taken together to form a ring; R 3 and R 3a are each independently selected from the group consisting of hydrogen, hydroxyl, lower alkoxy, halo, CN, substituted or unsubstituted C 1 to C 4 alkyl, perfluoroalkyl, substituted or unsubstituted C 3 to C 7 cycloalkyl, cycloalkoxy, amino, alkylamino, dialkylamino, and aminoalkyl, wherein R 3 or R 3a and D may optionally be taken together with the atoms to which they are attached to form a 5- to 7-membered ring; R 5 and R 5a are the same or different and are independently selected from the group consisting of hydrogen, substituted or unsubstituted lower alkyl, hydroxyalkyl, hydroxyalkylcycloalkyl, substituted or unsubstituted heterocycloalkyl, acyl, alkoxycarbonyl, carboxyalkyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted cycloalkylalkyl, wherein the R 5 and R 5a groups and the N atom to which they are attached may form a ring; R 21 and R 31 are each H or C 1 to C 4 alkyl; R 34 is alkyl; R 35 is H or alkyl; and R 6 is selected from the group consisting of H, C 1 to C 4 alkyl and C 3 to C 7 cycloalkyl.
摘要翻译：本申请提供了可用作MCHR1拮抗剂的化合物，特别是用于治疗肥胖症，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，其中R 1选自单环芳基或单环杂; W选自直接键，-O-和-N（R6） - ; 条件是如果W是直接键合，D是通过环胺的氮原子连接到A的环胺; D选自直链，取代或未取代的C1至C4烷基，取代或未取代的C3至C7环烷基，环烷基烷基和4-至6-元环胺，条件是如果D为直接键，则R2a R2b和R2c必须选自H，烷基或环烷基; E和G独立地为N或CH，条件是两者不是N; R1是取代或未取代的苯基或取代或未取代的单环杂芳基; R2a，R2b和R2c独立地选自氢，卤素，氰基，羟基，-NR5R5a，-SO2R34，-CO2R35 -NR5CO2R21，-NR5COR21，取代或未取代的C1至C4烷基，取代或未取代的C3至C7 环烷基，取代或未取代的4-至6-元环胺，其中所述环胺任选被-OH，羰基氨基，烷氧基羰基氨基或R 2a，R 2b和R 2c中的至少一个取代为选自氨基酸酯或磷酸酯酸酯，其中所述氨基酸酯具有式-OC（O）CH（NH 2）R 31，其中R 31是H或C 1至C 4烷基; 或R 2a，R b或R 2c中的任何两个可以一起形成环; R3和R3a各自独立地选自氢，羟基，低级烷氧基，卤素，CN，取代或未取代的C1至C4烷基，全氟烷基，取代或未取代的C3至C7环烷基，环烷氧基，氨基，烷基氨基，二烷基氨基和氨基烷基，其中R3或R3a和D可以任选地与它们所连接的原子一起形成5-至7-元环; R5和R5a相同或不同，并且独立地选自氢，取代或未取代的低级烷基，羟基烷基，羟基烷基环烷基，取代或未取代的杂环烷基，酰基，烷氧基羰基，羧基烷基，取代或未取代的环烷基和取代或未取代的环烷基烷基其中R5和R5a基团和它们所连接的N原子可以形成环; R 21和R 31各自为H或C 1至C 4烷基; R34是烷基; R35是H或烷基; 并且R 6选自H，C 1至C 4烷基和C 3至C 7环烷基。

8. 发明申请

WO2004030620A3 NOVEL TYROSINE KINASE INHIBITORS 审中-公开
公开(公告)号：WO2004030620A3
公开(公告)日：2004-04-15
申请号：PCT/US2003/030669
申请日：2003-09-29
申请人： BRISTOL-MYERS SQUIBB COMPANY , VELAPARTHI, Upender , WITTMAN, Mark, D.
发明人： VELAPARTHI, Upender , WITTMAN, Mark, D.
IPC分类号： A61K31/496
摘要： The present invention provides compounds of Formula (I) or (II) that are useful as anti-cancer agents and other diseases that can be treated by inhibiting tyrosine kinase enzymes.

9. 发明申请

WO2016161279A1 INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：吲哚胺2,3-二氧化酶抑制剂治疗癌症
公开(公告)号：WO2016161279A1
公开(公告)日：2016-10-06
申请号：PCT/US2016/025544
申请日：2016-04-01
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BALOG, James Aaron , CHERNEY, Emily Charlotte , MARKWALDER, Jay A. , SEITZ, Steven P. , SHAN, Weifang , WILLIAMS, David K. , NARA, Susheel Jethanand , ROY, Saumya , THANGAVEL, Soodamani , SISTLA, Ramesh Kumar , CHERUKU, Srinivas , THANGATHIRUPATHY, Srinivasan , KANYABOINA, Yadagiri , PULICHARLA, Nagalakshmi , AUDRIS, Huang
IPC分类号： C07D309/14 , C07D405/12 , C07D487/04 , A61P35/00 , C07D413/12 , C07D487/08 , C07D265/30 , C07D211/08 , C07D295/155 , C07D407/12 , C07D207/08 , C07D307/22 , C07D335/02 , A61K31/35
CPC分类号： C07C275/40 , A61K31/17 , A61K31/196 , A61K31/277 , A61K31/351 , A61K31/382 , A61K31/397 , A61K31/428 , A61K31/437 , A61K31/445 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/5375 , A61K31/5377 , A61K31/538 , A61K39/3955 , A61K39/39558 , A61K45/06 , C07C229/42 , C07C233/81 , C07C235/38 , C07C235/56 , C07C255/57 , C07C255/58 , C07C275/30 , C07C275/42 , C07D205/04 , C07D207/08 , C07D207/12 , C07D211/08 , C07D211/14 , C07D239/34 , C07D239/47 , C07D265/30 , C07D265/36 , C07D277/64 , C07D295/155 , C07D307/22 , C07D309/04 , C07D309/14 , C07D317/46 , C07D335/02 , C07D401/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08
摘要： There are disclosed compounds of formula (I) that modulate or inhibit the enzymatic activity of indoleamine-2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
摘要翻译：公开了调节或抑制吲哚胺-2,3-双加氧酶（IDO）的酶活性的式（I）化合物，含有所述化合物的药物组合物和治疗增殖性疾病的方法，例如癌症，病毒感染和/或利用本发明化合物的炎性病症。

10. 发明申请

WO2010047956A1 AZOLOPYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：阿莫洛林粉红素浓缩激素受体-1拮抗剂
公开(公告)号：WO2010047956A1
公开(公告)日：2010-04-29
申请号：PCT/US2009/059924
申请日：2009-10-08
申请人： BRISTOL-MYERS SQUIBB COMPANY , DEVASTHALE, Pratik , WASHBURN, William, N. , WANG, Wei , HERNANDEZ, Andres , AHMAD, Saleem , ZHAO, Guohua
发明人： DEVASTHALE, Pratik , WASHBURN, William, N. , WANG, Wei , HERNANDEZ, Andres , AHMAD, Saleem , ZHAO, Guohua
IPC分类号： C07D487/04 , A61K31/4015 , A61P3/00
CPC分类号： C07D487/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula (I) including all pharmaceutically acceptable salts and stereoisomers thereof: wherein A is a monocyclic aryl or monocyclic heteroaryl; W is a direct bond, -0-, or -N(R 6 )-, provided that if W is a direct bond, D must be a cyclic amine that is attached to A via the nitrogen atom of said cyclic amine; D is a direct bond, substituted or unsubstituted C 1 to C 4 alkyl, substituted or unsubstituted C 3 to C 7 cycloalkyl, cycloalkylalkyl, or a 4 to 6 membered cyclic amine; B and E are independently N or CH provided that both are not CH;
摘要翻译：本申请提供了包括其所有药学上可接受的盐和立体异构体的根据式（I）的所有立体异构体，溶剂化物，前药和药学上可接受的形式的化合物：其中A是单环芳基或单环杂芳基; W是直接键，-O-或-N（R6） - ，条件是如果W是直接键，则D必须是通过所述环胺的氮原子连接到A的环胺; D是直接键，取代或未取代的C1至C4烷基，取代或未取代的C3至C7环烷基，环烷基烷基或4至6元环胺; B和E独立地为N或CH，条件是两者都不是CH;

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