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2. 发明申请

WO2004106295A3 SUBSTITUTED PIPERODINES AND PYRROLIDINES AS CALCIUM SENSING RECEPTOR MODULATORS AND METHOD 审中-公开
标题翻译：作为钙感测受体调节剂和方法的取代的哌嗪和吡咯烷
公开(公告)号：WO2004106295A3
公开(公告)日：2005-12-29
申请号：PCT/US2004016712
申请日：2004-05-27
申请人： SQUIBB BRISTOL MYERS CO , DICKSON JOHN K , LAWRENCE R MICHAEL , ROBERGE JACQUES Y , ROTELLA DAVID P , YANG WU
发明人： DICKSON JOHN K , LAWRENCE R MICHAEL , ROBERGE JACQUES Y , ROTELLA DAVID P , YANG WU
IPC分类号： A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/454 , A61K31/55 , C07D20060101 , C07D207/04 , C07D409/06
CPC分类号： C07D207/06 , C07D207/08 , C07D207/10 , C07D211/18 , C07D211/22 , C07D333/28
摘要： Compounds are provided which are antagonists of the calcium sensing receptor, and have the general formula (I) wherein m is 0, 1, 2, 3 or 4; each X is independently selected from the group consisting of hydrogen, halo, cyano, nitro, OCF3, hydroxy, amino, carboxyl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, haloalkyl, alkoxy, alkoxycarbonylalkyl, hydroxycarbonylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkylalkyl, R O, R R N, R OCO, R CO, R R NCO, R R NCONR , R OCONR , R CONR , R S, R SO, R SO2, R R NSO2, R R NSO2NR , and R SO2NR ; R is alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; R and R are the same or different and are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; n is 1, 2, or 3; W is O or H,R ; R is hydrogen or hydroxyl; Ar is a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group; Q is hydrogen, F, or hydroxyl. In addition, a method for using these compounds to treat diseases associated with abnormal or mineral homeostasis is also provided.
摘要翻译：提供化合物，其是钙感应受体的拮抗剂，并具有通式（I），其中m为0,1,2,3或4; 每个X独立地选自氢，卤素，氰基，硝基，OCF 3，羟基，氨基，羧基，烷基，烯基，炔基，环烷基，环杂烷基，卤代烷基，烷氧基，烷氧基羰基烷基，羟基羰基烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基烷基，R 1 O，R 1 R 2 N，R 1 OCO，R 1 CO，R 1 R 2 NCO，R 1 R 2， NCONR 2a，R 1 OCONR 2a，R 1 CONR 2a，R 1 S，R 1 SO，R 1 SO 2，R 1 R 2 NSO 2 R 1 R 2 NSO 2 NR 2a和R 1 SO 2 NR 2a; R 1是烷基，烯基，炔基，环烷基，环杂烷基，芳基，杂芳基，芳基烷基或杂芳基烷基; R 2和R 2a相同或不同并且独立地选自氢，烷基，烯基，炔基，环烷基，环杂烷基，芳基，杂芳基，芳基烷基或杂芳基烷基; n为1,2或3; W是O或H，R 3; R 3是氢或羟基; Ar是取代或未取代的芳基或取代或未取代的杂芳基; Q是氢，F或羟基。此外，还提供了使用这些化合物治疗与异常或矿物质内稳态相关疾病的方法。

3. 发明申请

WO2002102314A2 PURINE INHIBITORS OF PHOSPHODIESTERASE (PDE) 7 审中-公开
标题翻译：磷脂酰胆碱酯酶抑制剂（PDE）7
公开(公告)号：WO2002102314A2
公开(公告)日：2002-12-27
申请号：PCT/US2002/019126
申请日：2002-06-17
申请人： BRISTOL-MYERS SQUIBB COMPANY , VACCARO, Wayne , ROBERGE, Jacques, Y. , LEFTHERIS, Katerina , PITTS, William, J. , BARBOSA, Joseph
发明人： VACCARO, Wayne , ROBERGE, Jacques, Y. , LEFTHERIS, Katerina , PITTS, William, J. , BARBOSA, Joseph
IPC分类号： A61K
CPC分类号： C07D403/12 , A61K31/00 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/522 , C07D401/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/00 , C07D473/16 , C07D487/04 , C07D491/10
摘要： Purine phosphodiesterase 7 (PDE 7) inhibitors of the following formulas(Ia, Ib), wherein R 1 , R 2 , Z, Y and J are described herein, and analogs thereof are provided which are useful in treating T-cell mediated diseases.
摘要翻译：本文描述了其中R 1，R 2，Z，Y和J的下式（Ia，Ib）的嘌呤磷酸二酯酶7（PDE 7）抑制剂，其类似物可用于治疗T- 细胞介导的疾病。

5. 发明申请

WO2011153953A1 CRYSTALLINE FORM OF BENZYLBENZENE SGLT2 INHIBITOR 审中-公开
标题翻译：苯乙烯SGLT2抑制剂的结晶形式
公开(公告)号：WO2011153953A1
公开(公告)日：2011-12-15
申请号：PCT/CN2011/075554
申请日：2011-06-10
申请人： THERACOS, INC. , CAI, Mengzhuang , LIU, Qian , XU, Ge , LV, Binhua , SEED, Brian , ROBERGE, Jacques Y.
发明人： CAI, Mengzhuang , LIU, Qian , XU, Ge , LV, Binhua , SEED, Brian , ROBERGE, Jacques Y.
IPC分类号： C07H7/04 , A61K31/70 , A61P3/00
CPC分类号： C07H1/06 , C07D309/10 , C07H7/04
摘要： Crystalline forms of a compound having an inhibitory effect on sodium-dependent glucose cotransporter SGLT2 are disclosed. Pharmaceutical compositions, methods for preparing the crystalline compound, and methods of using the crystalline compound, independently or in combination with other therapeutic agents for treating diseases and conditions which are affected by SGLT or SGLT2 inhibition are also disclosed.
摘要翻译：公开了对钠依赖性葡萄糖协同转运体SGLT2具有抑制作用的化合物的结晶形式。还公开了药物组合物，制备结晶化合物的方法以及使用结晶化合物独立地或与其它治疗剂组合用于治疗受SGLT或SGLT2抑制影响的疾病和病症的方法。

6. 发明申请

WO2004069793A3 NOVEL 2-SUBSTITUTED CYCLIC AMINES AS CALCIUM SENSING RECEPTOR MODULATORS 审中-公开
标题翻译：新型2-取代的循环胺作为钙感测受体调节剂
公开(公告)号：WO2004069793A3
公开(公告)日：2005-01-20
申请号：PCT/US2004002296
申请日：2004-01-27
申请人： SQUIBB BRISTOL MYERS CO , GAVAI ASHVINIKUMAR V , VAZ ROY J , DICKSON JOHN K JR , ROBERGE JACQUES Y , YANG WU , GUNGOR TIMUR , CORTE JAMES R , ROTELLA DAVID P , WANG YUFENG
发明人： GAVAI ASHVINIKUMAR V , VAZ ROY J , DICKSON JOHN K JR , ROBERGE JACQUES Y , YANG WU , GUNGOR TIMUR , CORTE JAMES R , ROTELLA DAVID P , WANG YUFENG
IPC分类号： A61K31/517 , C07D20060101 , C07D205/04 , C07D207/09 , C07D207/34 , C07D207/48 , C07D211/26 , C07D215/20 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D417/06 , C07D417/14
CPC分类号： C07D409/06 , C07D205/04 , C07D207/09 , C07D207/34 , C07D207/48 , C07D211/26 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/06 , C07D417/14
摘要： The present invention relates to modulators of the calcium sensing receptor having the formula I (I) wherein Ar , X, n, R , R , R , and Q are as defined herein.
摘要翻译：本发明涉及具有式I（I）的钙感应受体的调节剂，其中Ar 1，X，n，R 1，R 2，R 3和Q如本文所定义。

7. 发明申请

WO2002102314A3 PURINE INHIBITORS OF PHOSPHODIESTERASE (PDE) 7 审中-公开
公开(公告)号：WO2002102314A3
公开(公告)日：2002-12-27
申请号：PCT/US2002/019126
申请日：2002-06-17
申请人： BRISTOL-MYERS SQUIBB COMPANY , VACCARO, Wayne , ROBERGE, Jacques, Y. , LEFTHERIS, Katerina , PITTS, William, J. , BARBOSA, Joseph
发明人： VACCARO, Wayne , ROBERGE, Jacques, Y. , LEFTHERIS, Katerina , PITTS, William, J. , BARBOSA, Joseph
IPC分类号： C07D473/16
摘要： Purine phosphodiesterase 7 (PDE 7) inhibitors of the following formulas(Ia, Ib), wherein R 1 , R 2 , Z, Y and J are described herein, and analogs thereof are provided which are useful in treating T-cell mediated diseases.

8. 发明申请

WO2010009243A1 DEUTERATED BENZYLBENZENE DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译：去离子苯乙烯衍生物及其使用方法
公开(公告)号：WO2010009243A1
公开(公告)日：2010-01-21
申请号：PCT/US2009/050710
申请日：2009-07-15
申请人： THERACOS, INC. , SEED, Brian , LV, Binhua , ROBERGE, Jacques, Y. , CHEN, Yuanwei , PENG, Kun , DONG, Jiajia , XU, Baihua , DU, Jiyan , ZHANG, Lili , TANG, Xinxing , XU, Ge , FENG, Yan , XU, Min
发明人： SEED, Brian , LV, Binhua , ROBERGE, Jacques, Y. , CHEN, Yuanwei , PENG, Kun , DONG, Jiajia , XU, Baihua , DU, Jiyan , ZHANG, Lili , TANG, Xinxing , XU, Ge , FENG, Yan , XU, Min
IPC分类号： A01N43/04
CPC分类号： A61K45/06 , A61K31/35 , C07D309/10 , A61K2300/00
摘要： Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by SGLT inhibition.
摘要翻译：提供对钠依赖性葡萄糖转运蛋白SGLT具有抑制作用的化合物。本发明还提供药物组合物，制备化合物的方法，合成中间体，以及独立地或与其它治疗剂组合使用该化合物用于治疗受SGLT抑制影响的疾病和病症的方法。

9. 发明申请

WO2009026537A1 BENZYLBENZENE DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译：苯并噻吩衍生物及其使用方法
公开(公告)号：WO2009026537A1
公开(公告)日：2009-02-26
申请号：PCT/US2008/074058
申请日：2008-08-22
申请人： THERACOS, INC. , SONG, Yanli , CHEN, Yuanwei , CHENG, Huawei , LI, Shengbin , WU, Yuelin , FENG, Yan , LV, Binhua , XU, Baihua , SEED, Brian , HADD, Michael J. , DU, Jiyan , WANG, Congna , ROBERGE, Jacques Y.
发明人： SONG, Yanli , CHEN, Yuanwei , CHENG, Huawei , LI, Shengbin , WU, Yuelin , FENG, Yan , LV, Binhua , XU, Baihua , SEED, Brian , HADD, Michael J. , DU, Jiyan , WANG, Congna , ROBERGE, Jacques Y.
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： C07H7/04 , C07D309/10 , C07D407/12
摘要： Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.
摘要翻译：提供对钠依赖性葡萄糖转运蛋白SGLT具有抑制作用的化合物。本发明还提供药物组合物，制备化合物的方法，合成中间体，以及独立地或与其它治疗剂组合使用化合物治疗受SGLT抑制影响的疾病和病症的方法。

10. 发明申请

WO2005070920A1 AMINO-BENZAZOLES AS P2Y1 RECEPTOR INHIBITORS 审中-公开
标题翻译：氨基苯甲酸酯作为P2Y1受体抑制剂
公开(公告)号：WO2005070920A1
公开(公告)日：2005-08-04
申请号：PCT/US2005/001705
申请日：2005-01-20
申请人： BRISTOL-MYERS SQUIBB COMPANY , HERPIN, Timothy, F. , MORTON, George, C. , REHFUSS, Robert, P. , LAWRENCE, R., Michael , POSS, Michael, A. , ROBERGE, Jacques, Y. , GUNGOR, Timur
发明人： HERPIN, Timothy, F. , MORTON, George, C. , REHFUSS, Robert, P. , LAWRENCE, R., Michael , POSS, Michael, A. , ROBERGE, Jacques, Y. , GUNGOR, Timur
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D235/30 , C07D401/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D513/04
摘要： The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y 1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y 1 receptor activity.
摘要翻译：本发明提供了新的氨基 - 苯并唑类似物，它们是人P2Y1受体的选择性抑制剂。本发明还提供了相同的各种药物组合物以及治疗对P2Y1受体活性调节作用的疾病的方法。

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