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1. 发明申请

WO2004004665A3 SUBSTITUTED HETEROCYCLIC DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 审中-公开
公开(公告)号：WO2004004665A3
公开(公告)日：2004-01-15
申请号：PCT/US2003/022149
申请日：2003-07-02
申请人： BRISTOL-MYERS SQUIBB COMPANY , CHENG, Peter, T., W. , CHEN, Sean , DEVASTHALE, Pratik , DING, Charles, Z. , HERPIN, Timothy, F. , WU, Shung , ZHANG, Hao , WANG, Wei , YE, Xiang-Yang
发明人： CHENG, Peter, T., W. , CHEN, Sean , DEVASTHALE, Pratik , DING, Charles, Z. , HERPIN, Timothy, F. , WU, Shung , ZHANG, Hao , WANG, Wei , YE, Xiang-Yang
IPC分类号： C07D403/06
摘要： Formula, wherein Z 1 is (CH 2 ) q or C=O; Z 2 is (CH 2 ) p or C=O; D is -CH= or C=O or (CH 2 ) m where m is 0, 1, 2 or 3; n = 0, 1 or 2; p = 1 or 2; q = 0, 1 or 2; Q is C or N; A is (CH 2 ) x where x is 1 to 5, or A is (CH 2 ) x 1 , where x 1 is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is -(CH 2 ) x 2 -O-(CH 2 ) x 3 - where x 2 is 0 to 5 and x 3 is 0 to 5, provided that at least one of x 2 and x 3 is other than 0; B is a bond or is (CH 2 ) x 4 where x 4 is 1 to 5; X is CH or N; X 2 is C, N, O or S; X 3 is C, N, O or S; X 4 is C, N, O or S; X 5 is C, N, O or S; X 6 is C, N, O or S; provided that at least one of X 2 , X 3 , X 4 X 5 and X 6 is N; and at least one of X 2 , X 3 , X 4 X 5 and X 6 is C. R 1 is H or alkyl; R 2 is H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; R 2a , R 2b and R 2c may be the same or different and are selected from H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; and R 3 , E, Z and Y are as defined herein.

2. 发明申请

WO2004093799A2 THYROID RECEPTOR LIGANDS 审中-公开
标题翻译：甲状腺受体配体
公开(公告)号：WO2004093799A2
公开(公告)日：2004-11-04
申请号：PCT/US2004011883
申请日：2004-04-16
申请人： SQUIBB BRISTOL MYERS CO , RYONO DENNIS E , HANGELAND JON J , FRIENDS TODD J , DEJNEKA TAMARA , DEVASTHALE PRATIK , CARINGAL YOLANDA V , ZHANG MINSHENG , DOWEYKO ARTHUR M P , MALM JOHAN , SANIN ANDREI
发明人： RYONO DENNIS E , HANGELAND JON J , FRIENDS TODD J , DEJNEKA TAMARA , DEVASTHALE PRATIK , CARINGAL YOLANDA V , ZHANG MINSHENG , DOWEYKO ARTHUR M P , MALM JOHAN , SANIN ANDREI
IPC分类号： A61K20060101 , A61K31/16 , A61K31/165 , A61K31/19 , A61K31/277 , A61K31/421 , A61K31/44 , A61K47/00 , C07C205/00 , C07C235/20 , C07C255/49 , C07C381/00 , A61K
CPC分类号： C07C311/46 , A61K31/4439 , A61K31/662 , A61K45/06 , C07C43/29 , C07C43/295 , C07C59/68 , C07C59/72 , C07C65/24 , C07C65/26 , C07C69/16 , C07C69/736 , C07C69/94 , C07C205/38 , C07C217/58 , C07C233/29 , C07C235/34 , C07C235/42 , C07C235/46 , C07C235/52 , C07C235/60 , C07C235/62 , C07C235/64 , C07C311/37 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07D213/30 , C07D239/26 , C07D257/04 , C07D263/14 , C07D263/32 , C07D277/24 , C07D285/06 , C07D307/42 , C07D307/52 , C07D307/87 , C07D317/58 , C07D317/60 , C07D333/32 , C07F9/306 , C07F9/3241 , C07F9/4056 , A61K2300/00
摘要： Thyroid receptor ligands are provided which have the general formula (I), wherein: R1 is formula (II); R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, provided that at least one of R2 and R3 is other than hydrogen; R4 is formula (III); R5 and R6 are the same or different and are selected from hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, aralkyl or heteroaralkyl. R7 is aryl, heteroaryl, alkyl, aralkyl, or heteroaralkyl; R8 is aryl, heteroaryl, or cycloalkyl; R9 is R7 or hydrogen; R10 is hydrogen, halogen, cyano or alkyl; R11 and R12 are each independently selected from the group consisting of hydrogen, halogen, alkoxy, hydroxy (-OH) cyano, and alkyl; R13 is carboxylic acid (COOH) or esters thereof, phosphonic and phosphinic acid or esters thereof, sulfonic acid, tetrazole, hydroxamic acid, thiazolidinedione, acylsulfonamide, or other carboxylic acid surrogates known in the art; R14 and R15 may be the same or different and are selected from hydrogen and alkyl, or R14 and R15 may be joined together forming a chain of 2 to 5 methylene groups [-(CH2)m-, m = 2, 3, 4 or 5], thus forming 3- to 6-membered cycloalkyl rings; R16 is hydrogen or alkyl of 1 to 4 carbons; R17 and R18 are the same or different and selected from hydrogen, halogen and alkyl; n is 0 or an integer from 1 to 4; X is oxygen (-O-), sulfur (-S-), sulfonyl (-SO2-), sulfenyl (-SO-) selenium (-Se-), carbonyl (-CO-), amino (-NH-) or methylene (-CH2-); wherein the substituents are as described herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
摘要翻译：提供具有通式（I）的甲状腺受体配体，其中：R1是式（II）; R2和R3相同或不同，为氢，卤素，1至4个碳原子的烷基或3至5个碳原子的环烷基，条件是R 2和R 3中的至少一个不是氢; R4是式（III）; R5和R6相同或不同，并且选自氢，芳基，杂芳基，烷基，环烷基，芳烷基或杂芳烷基。 R7是芳基，杂芳基，烷基，芳烷基或杂芳烷基; R8是芳基，杂芳基或环烷基; R9为R7或氢; R 10是氢，卤素，氰基或烷基; R 11和R 12各自独立地选自氢，卤素，烷氧基，羟基（-OH）氰基和烷基; R13是羧酸（COOH）或其酯，膦酸和次膦酸或其酯，磺酸，四唑，异羟肟酸，噻唑烷二酮，酰基磺酰胺或本领域已知的其它羧酸替代物; R 14和R 15可以相同或不同，并且选自氢和烷基，或者R 14和R 15可以连接在一起形成2至5个亚甲基 - [ - （CH 2）m - ，m = 2,3,4或 5]，从而形成3-至6-元环烷基环; R16是氢或1至4个碳的烷基; R 17和R 18相同或不同，选自氢，卤素和烷基; n为0或1至4的整数; X是氧（-O-），硫（-S-），磺酰基（-SO 2 - ），亚磺酰基（-SO-）硒（-Se-），羰基（-CO-），氨基（-NH-）或亚甲基（-CH 2 - ）其中取代基如本文所述。此外，提供了一种用于预防，抑制或治疗与代谢功能障碍相关或依赖于T3调节基因的表达的疾病或病症的方法，其中如上所述的化合物以治疗有效量施用。

3. 发明申请

WO2004004665A2 SUBSTITUTED HETEROCYCLIC DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 审中-公开
标题翻译：用作抗糖尿病药和抗衰老药的取代的杂环衍生物和方法
公开(公告)号：WO2004004665A2
公开(公告)日：2004-01-15
申请号：PCT/US0322149
申请日：2003-07-02
申请人： SQUIBB BRISTOL MYERS CO , CHENG PETER T W , CHEN SEAN , DEVASTHALE PRATIK , DING CHARLES Z , HERPIN TIMOTHY F , WU SHUNG , ZHANG HAO , WANG WEI , YE XIANG-YANG
发明人： CHENG PETER T W , CHEN SEAN , DEVASTHALE PRATIK , DING CHARLES Z , HERPIN TIMOTHY F , WU SHUNG , ZHANG HAO , WANG WEI , YE XIANG-YANG
IPC分类号： A61K31/155 , A61K31/216 , A61K31/22 , A61K31/365 , A61K31/366 , A61K31/397 , A61K31/401 , A61K31/422 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/616 , A61K31/64 , A61K38/28 , A61K45/00 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/02 , A61P9/10 , A61P17/06 , A61P19/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/14 , C07D413/12 , C07D413/14 , A61K
CPC分类号： C07D413/12 , C07D413/14
摘要： Formula, wherein Z is (CH2)q or C=O; Z is (CH2)p or C=O; D is -CH= or C=O or (CH2)m where m is 0, 1, 2 or 3; n = 0, 1 or 2; p = 1 or 2; q = 0, 1 or 2; Q is C or N; A is (CH2)x where x is 1 to 5, or A is (CH2)x , where x is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is -(CH2)x -O-(CH2)x - where x is 0 to 5 and x is 0 to 5, provided that at least one of x and x is other than 0; B is a bond or is (CH2)x where x is 1 to 5; X is CH or N; X2 is C, N, O or S; X3 is C, N, O or S; X4 is C, N, O or S; X5 is C, N, O or S; X6 is C, N, O or S; provided that at least one of X2, X3, X4 X5 and X6 is N; and at least one of X2, X3, X4 X5 and X6 is C. R is H or alkyl; R is H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; R , R and R may be the same or different and are selected from H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; and R , E, Z and Y are as defined herein.
摘要翻译：式，其中Z 1是（CH 2）q或C = O; Z 2是（CH 2）p或C = O; D是-CH =或C = O或（CH 2）m，其中m是0,1,2或3; n = 0,1或2; p = 1或2; q = 0,1或2; Q是C或N; A是（CH 2）x，其中x是1至5，或A是（CH 2）x 1，其中x 1是1至5且链中任何位置嵌入烯基键或炔基键，或A是 - （CH 2）x 2 -O-（CH 2）x 3 - 其中x 2为0至5且x 3为0至5，条件是x 2和x中的至少一个 <3>不是0; B是键或是（CH 2）x 4，其中x 4是1至5; X是CH或N; X2是C，N，O或S; X3是C，N，O或S; X4是C，N，O或S; X5是C，N，O或S; X6是C，N，O或S; 条件是X2，X3，X4，X5和X6中的至少一个是N; 并且X 2，X 3，X 4，X 5和X 6中的至少一个是C.R 1是H或烷基; R 2是H，烷基，烷氧基，卤素，氨基，取代的氨基或氰基; R 2a，R 2b和R 2c可以相同或不同，并且选自H，烷基，烷氧基，卤素，氨基，取代的氨基或氰基; 并且R 3，E，Z和Y如本文所定义。

4. 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。

5. 发明申请

WO2003040114A1 SUBSTITUTED ACID DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 审中-公开
标题翻译：替代的酸衍生物作为抗真菌剂和抗菌药物和方法有用
公开(公告)号：WO2003040114A1
公开(公告)日：2003-05-15
申请号：PCT/US2002/035704
申请日：2002-11-06
申请人： BRISTOL-MYERS SQUIBB COMPANY , DEVASTHALE, Pratik , JEON, Yoon, T.
发明人： DEVASTHALE, Pratik , JEON, Yoon, T.
IPC分类号： C07D263/56
CPC分类号： C07D413/06 , A61K31/421 , A61K45/06 , A61K2300/00
摘要： Compounds are provided which have the structure (I) wherein Q is C or N, X 1 is CH or N and, A, E, M, G, X 2 , X 3 , X 4 , R 1 , R 2 , R 2a , R 2b , R 2c , R 3 , Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
摘要翻译：提供具有结构（I）的化合物，其中Q是C或N，X 1是CH或N，且A，E，M，G，X 2，X 3，X 4，R 1，R 2， R 2a，R 2c，R 3，Y，x，m和n如本文所定义，该化合物可用作抗糖尿病，降血脂症和抗肥胖剂。

6. 发明申请

WO2010047956A9 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：WO2010047956A9
公开(公告)日：2011-10-06
申请号：PCT/US2009059924
申请日：2009-10-08
申请人： SQUIBB BRISTOL MYERS CO , 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(R6)-, 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 C1 to C4 alkyl, substituted or unsubstituted C3 to C7 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，溶剂合物，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;

7. 发明申请

WO2006127287A3 PYRROLOPYRIDINE-BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND METHODS 审中-公开
标题翻译：基于吡咯基吡啶的DIPEPTIDYL PEPTIDASE IV和方法的抑制剂
公开(公告)号：WO2006127287A3
公开(公告)日：2007-06-07
申请号：PCT/US2006018185
申请日：2006-05-11
申请人： SQUIBB BRISTOL MYERS CO , DEVASTHALE PRATIK , WANG WEI , HAMANN LAWRENCE G , O'CONNOR STEPHEN P , FEVIG JOHN M
发明人： DEVASTHALE PRATIK , WANG WEI , HAMANN LAWRENCE G , O'CONNOR STEPHEN P , FEVIG JOHN M
IPC分类号： C07D487/04 , A61K31/407
CPC分类号： C07D471/04
摘要： Compounds are provided having the formula (I): wherein R, X, Y, Z, A and n are as defined herein, which are inhibitors of dipeptidyl peptidase IV and thus are useful in treating diabetes and related diseases.
摘要翻译：提供具有式（I）的化合物：其中R，X，Y，Z，A和n如本文所定义，其是二肽基肽酶IV的抑制剂，因此可用于治疗糖尿病和相关疾病。

8. 发明申请

WO2006127287A2 PYRROLOPYRIDINE-BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND METHODS 审中-公开
标题翻译：基于吡咯基吡啶的DIPEPTIDYL PEPTIDASE IV和方法的抑制剂
公开(公告)号：WO2006127287A2
公开(公告)日：2006-11-30
申请号：PCT/US2006/018185
申请日：2006-05-11
申请人： BRISTOL-MYERS SQUIBB COMPANY , DEVASTHALE, Pratik , WANG, Wei , HAMANN, Lawrence G. , O'CONNOR, Stephen P. , FEVIG, John M.
发明人： DEVASTHALE, Pratik , WANG, Wei , HAMANN, Lawrence G. , O'CONNOR, Stephen P. , FEVIG, John M.
IPC分类号： C07D487/04 , A61K31/407
CPC分类号： C07D471/04
摘要： Compounds are provided having the formula (I): wherein R, X, Y, Z, A and n are as defined herein, which are inhibitors of dipeptidyl peptidase IV and thus are useful in treating diabetes and related diseases.
摘要翻译：提供具有式（I）的化合物：其中R，X，Y，Z，A和n如本文所定义，其是二肽基肽酶IV的抑制剂，因此可用于治疗糖尿病和相关疾病。

9. 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;

10. 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。

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