专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2008064107A2 7,8-DIHYDRO-1,6-NAPHTHYRIDIN-5(6H)-ONES AND RELATED BICYCLIC COMPOUNDS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND METHODS 审中-公开
标题翻译： 7,8-二氢-1,6-萘啶-5（6H） - 酮及相关的双环化合物作为二磷酸肽酶IV的抑制剂和方法
公开(公告)号：WO2008064107A2
公开(公告)日：2008-05-29
申请号：PCT/US2007/084927
申请日：2007-11-16
申请人： BRISTOL-MYERS SQUIBB COMPANY , FEVIG, John M. , FENG, Jianxin
发明人： FEVIG, John M. , FENG, Jianxin
IPC分类号： C07D471/04 , A61K31/4375 , A61P3/06
CPC分类号： C07D471/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an DPP4 modulated disease or disorder such as, for example, diabetes, by administration of a therapeutically effective dose of a compound according to Formula I. wherein X, Z, A, R2, Y, R1, n, and b are as defined herein.
摘要翻译：本申请提供了包括根据式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的化合物。此外，本申请提供了药物组合物，其含有至少一种根据式I的化合物和任选地至少一种另外的治疗剂。最后，本申请提供了通过施用治疗有效剂量的根据式I的化合物治疗患有DPP4调节的疾病或病症例如糖尿病的患者的方法，其中X，Z，A，R2 ，Y，R1，n和b如本文所定义。

2. 发明申请

WO2008002824A1 CRYSTALLINE SOLVATES AND COMPLEXES OF (IS) -1, 5-ANHYDRO-L-C- (3- ( (PHENYL) METHYL) PHENYL) -D-GLUCITOL DERIVATIVES WITH AMINO ACIDS AS SGLT2 INHIBITORS FOR THE TREATMENT OF DIABETES 审中-公开
标题翻译：（IS）-1,5-二羟基-L-C-（3-（（苯基）甲基）苯基）-D-葡萄糖苷衍生物与氨基酸作为SGLT2抑制剂治疗糖尿病的晶体溶解剂和复合物
公开(公告)号：WO2008002824A1
公开(公告)日：2008-01-03
申请号：PCT/US2007/071749
申请日：2007-06-21
申请人： BRISTOL-MYERS SQUIBB COMPANY , GOUGOUTAS, Jack, Z. , LOBINGER, Hildegard , RAMAKRISHNAN, Srividya , DESHPANDE, Prashant, P. , BIEN, Jeffrey, T. , LAI, Chiajen , WANG, Chenchi , RIEBEL, Peter , GROSSO, John, Anthony , NIRSCHL, Alexandra, A. , SINGH, Janak , DIMARCO, John, D.
发明人： GOUGOUTAS, Jack, Z. , LOBINGER, Hildegard , RAMAKRISHNAN, Srividya , DESHPANDE, Prashant, P. , BIEN, Jeffrey, T. , LAI, Chiajen , WANG, Chenchi , RIEBEL, Peter , GROSSO, John, Anthony , NIRSCHL, Alexandra, A. , SINGH, Janak , DIMARCO, John, D.
IPC分类号： C07H7/04 , A61K31/70 , A61P3/10
CPC分类号： C07H15/207 , A61K31/7034 , A61K45/06 , A61P3/10 , C07H7/04
摘要： The present invention relates to physical crystal structures of a compound of the formula I: wherein R1, R2, R2a, R3 and R4 are as defined herein, especially pharmaceutical compositions containing structures of compound I or II, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译：本发明涉及式I化合物的物理结晶结构：其中R1，R2，R2a，R3和R4如本文所定义，特别是含有化合物I或II结构的药物组合物，其制备方法，制备方法以及使用这种结构治疗糖尿病等疾病的方法。

3. 发明申请

WO2006028733A1 PROCESS FOR THE PREPARATION OF Z-5-CARBOXYMETHYLENE-1,3-DIOXOLAN-4-ONES 审中-公开
标题翻译：制备Z-5-羧甲基-1,3-二氧杂环己烷-4-酮的方法
公开(公告)号：WO2006028733A1
公开(公告)日：2006-03-16
申请号：PCT/US2005/030387
申请日：2005-08-25
申请人： BRISTOL-MYERS SQUIBB COMPANY , NUGENT, William A. , ZHU, Keming , SIMPSON, James H. , DELANEY, Edward J.
发明人： NUGENT, William A. , ZHU, Keming , SIMPSON, James H. , DELANEY, Edward J.
IPC分类号： C07D317/00
CPC分类号： C07D317/34
摘要： A process for preparing Z-5-carboxymethylene-1,3-dioxolan-4-ones is provided which includes the steps of reacting a bis-ketal or bis-acetal of tartaric acid with a potassium containing base to form the carboxymethylene-1,3-dioxolan-4-one. A process for preparing HIV integrase inhibitors employing the carboxymethylene-1,3-dioxolan-4-one inhibitor is also provided.
摘要翻译：提供一种制备Z-5-羧甲基-1,3-二氧戊环-4-酮的方法，其包括使酒石酸双缩酮或双缩醛与含钾碱反应以形成羧甲基-1， 1,3-二氧戊环-4-酮。还提供了使用羧亚甲基-1,3-二氧戊环-4-酮抑制剂制备HIV整合酶抑制剂的方法。

4. 发明申请

WO2005115339A3 COMPOSITION FOR ENHANCING ABSORPTION OF A DRUG AND METHOD 审中-公开
公开(公告)号：WO2005115339A3
公开(公告)日：2005-12-08
申请号：PCT/US2005/014165
申请日：2005-04-26
申请人： BRISTOL-MYERS SQUIBB COMPANY , MATHIAS, Neil, R. , LI, Lianli
发明人： MATHIAS, Neil, R. , LI, Lianli
IPC分类号： A61K9/14
摘要： A composition for enhancing absorption of a pharmaceutical which may have poor oral bioavailability, which composition has surprisingly little cytotoxicity, is provided which is in the form of a liquid or semi-solid or solid containing an admixture (1) a mucoadhesive polymer which is a polyacrylic acid polymer, preferably Carbopol 971P, and (2) an absorption or permeation enhancer which preferably is L-α-lyso-phosphatidylcholine (LPC), and which composition is free of polysaccharides. A method for improving bioavailability of a drug which has poor absorption properties is also provided wherein the above bioadhesive composition is administered with said pharmaceutical to the mucosal membrane of the GI tract, nose, oral cavity, sublingual, buccal, and vaginal mucosa. A method for reducing the cytotoxic effect of an absorption enhancer such as LPC is also provided wherein a mucoadhesive polymer as described above is administered with the LPC to a patient in need of treatment.

5. 发明申请

WO2008134480A1 NON-BASIC MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：非基础麦芽宁浓缩激素受体-1拮抗剂
公开(公告)号：WO2008134480A1
公开(公告)日：2008-11-06
申请号：PCT/US2008/061519
申请日：2008-04-25
申请人： BRISTOL-MYERS SQUIBB COMPANY , WASHBURN, William N. , AHMAD, Saleem , HERNANDEZ, Andres S.
发明人： WASHBURN, William N. , AHMAD, Saleem , HERNANDEZ, Andres S.
IPC分类号： C07D495/04 , A61K31/5025 , A61K31/53 , A61K31/381 , A61P25/24
CPC分类号： C07D495/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula (I) and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-I modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula (I) where R 1 , R 1a , R 1b , A, R 3 , R 4 , R 5 , R5 b and R 6 are as defined herein.
摘要翻译：本申请提供化合物，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。另外，本申请提供含有至少一种根据式（I）的化合物和任选的至少一种另外的治疗剂。最后，本申请提供了通过施用治疗有效剂量的根据式（I）的化合物治疗患有MCHR-1调节的疾病或病症例如肥胖，糖尿病，抑郁或焦虑的患者的方法，其中R 1，R 1a，R 1b，A，R 3，R 4， R 5，R 5，R 6和R 6如本文所定义。

6. 发明申请

WO2008057855A3 HETEROCYCLIC COMPOUNDS AS MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-I, AND /OR NP-KAPPA-B ACTIVITY 审中-公开
公开(公告)号：WO2008057855A3
公开(公告)日：2008-05-15
申请号：PCT/US2007/083083
申请日：2007-10-31
申请人： BRISTOL-MYERS SQUIBB COMPANY , DHAR, T.g. Murali , XIAO, Hai-yun , SHEPPECK, James E.
发明人： DHAR, T.g. Murali , XIAO, Hai-yun , SHEPPECK, James E.
IPC分类号： C07D471/04 , A61K31/437 , A61P3/00 , A61P29/00 , A61P37/00
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1 and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I):, its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein the group X is O or (R x )(R y ); is heterocyclo or heteroaryl; E is -N-, -NR 1 -, -O-, -C(=O), -S-, -SO 2 -, or -CR 2 -; F is -N-, -NR 1a , -O-, -C(=O), -S-, -SO 2 -, or -CR 2a -; G is independently N, -NR 1b -, -O-, -C(=O), -S-, -SO 2 - or -CR 2b - provided that the heterocyclic ring formed does not contain a S-S or S-O bond and at least one of E, F and G is a hetero atom; and Ma, R x , R y , R 1 , R 1a , R 1b , R 2 , R 2a , R 2b , R 4 , R 5a , R 6 , R 7 , X, Z a and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases employing said compounds.

7. 发明申请

WO2007027454A1 HETEROCYCLIC DIHYDROPYRIMIDINE COMPOUNDS 审中-公开
标题翻译：杂环二氢嘧啶化合物
公开(公告)号：WO2007027454A1
公开(公告)日：2007-03-08
申请号：PCT/US2006/032382
申请日：2006-08-18
申请人： BRISTOL-MYERS SQUIBB COMPANY , HAN, Wei , HU, Zilun
发明人： HAN, Wei , HU, Zilun
IPC分类号： C07D487/04 , A61K31/505 , A61P9/06
CPC分类号： C07D487/04
摘要： Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra rapidly activating delayed rectifier, which have the structure: (Formula I); stereoisomers including enantiomers thereof and diastereomers thereof, or a pharmaceutically acceptable salt thereof, wherein Q is alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl or: (Formula II) which is aryl, substituted aryl, heteroaryl or substituted heteroaryl; R 3 is a) (Formula III), b) (Formula IV), or c) (Formula V); wherein R 1 , R 2 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are defined herein. Methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds are also provided.
摘要翻译：可用作钾通道功能抑制剂的新型杂环二氢嘧啶化合物（特别是电压门控K +通道的Kv1亚家族抑制剂，特别是与超快速活化延迟整流剂连接的抑制剂Kv1.5，其结构如下：（式I）其中Q为烷基，取代的烷基，环烷基，取代的环烷基，环杂烷基，取代的环杂烷基或：（式II），其为芳基，取代的芳基，杂芳基或取代的杂芳基 ; R 3是a）（式III），b）（式IV）或c）（式V）; 其中R 1，R 2，R 4，R 5，R 6， R 7，R 8，R 9和R 10在本文中定义。还提供了使用这些化合物预防和治疗心律失常和IKur相关病症的方法，以及含有这些化合物的药物组合物。

8. 发明申请

WO2005108380A3 PROCESS EMPLOYING CONTROLLED CRYSTALLIZATION IN FORMING CRYSTALS OF A PHARMACEUTICAL 审中-公开
公开(公告)号：WO2005108380A3
公开(公告)日：2005-11-17
申请号：PCT/US2005/015338
申请日：2005-05-03
申请人： BRISTOL-MYERS SQUIBB COMPANY , KIM, Soojin , WEI, Chenkou , LINDRUD, Mark , CHUNG, Hyei-Jha
发明人： KIM, Soojin , WEI, Chenkou , LINDRUD, Mark , CHUNG, Hyei-Jha
IPC分类号： B01D9/00
摘要： A process is provided which employs reactive controlled crystallization to produce drug substance having desirable crystal properties which process involves providing reactants A and B in liquid or solution form and adding reactant B to reactant A using a cubic or incremental addition technique to control extent of reaction and thus crystallization kinetics, including supersaturation and nucleation, to produce crystals of drug substance which are generally larger, better quality and with few fines and narrow particle size distribution than normally obtainable employing prior art crystallization techniques. In addition, crystals of drug substance produced by the above process is also provided.

9. 发明申请

WO2010120963A1 TABLET FORMULATION FOR P38 INHIBITOR AND METHOD 审中-公开
标题翻译： P38抑制剂和方法的片剂配方
公开(公告)号：WO2010120963A1
公开(公告)日：2010-10-21
申请号：PCT/US2010/031138
申请日：2010-04-15
申请人： BRISTOL-MYERS SQUIBB COMPANY , DALI, Manisha M. , DAHLHEIM, Charles E. , NARINGREKAR, Vijay H. , MCGEORGE, Gary
发明人： DALI, Manisha M. , DAHLHEIM, Charles E. , NARINGREKAR, Vijay H. , MCGEORGE, Gary
IPC分类号： A61K9/16 , A61K9/20 , A61K31/53
CPC分类号： A61K31/53 , A61K9/1623 , A61K9/1652 , A61K9/2027 , A61K9/2077
摘要： A tablet formulation is provided which includes a medicament which is a pharmaceutically acceptable salt of a p38 inhibitor, such as the p38 HCl salt of the structure Formula (I) and which has good physical stability when stored at up to 25 C/60% RH in closed containers with desiccant. The tablet formulation will contain crospovidone as a tablet disintegrant, which, unlike croscarmellose sodium, will not cause disproportionation of the HCl salt to the free base of P38 inhibitor and thus will have acceptable dissolution properties even after storage at room temperature.
摘要翻译：提供了一种片剂制剂，其包括药物，其为p38抑制剂的药学上可接受的盐，例如结构式（I）的p38HCl盐，并且当以高达25℃/ 60％RH存储时具有良好的物理稳定性在带有干燥剂的密闭容器中。片剂制剂将含有交联聚维酮作为片剂崩解剂，其与交联羧甲纤维素钠不同，不会引起HCl盐对P38抑制剂的游离碱的歧化，因此即使在室温下储存后也具有可接受的溶解性能。

10. 发明申请

WO2010042674A1 PYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：吡咯酮梅兰宁浓缩HORMONE RECEPTOR-1 ANTAGONISTS
公开(公告)号：WO2010042674A1
公开(公告)日：2010-04-15
申请号：PCT/US2009/059918
申请日：2009-10-08
申请人： BRISTOL-MYERS SQUIBB COMPANY , ZHAO, Guohua , WASHBURN, William N. , MIGNONE, James
发明人： ZHAO, Guohua , WASHBURN, William N. , MIGNONE, James
IPC分类号： C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , A61K31/407 , A61P3/00
CPC分类号： C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R 1 , Formula Ia, R 4 , R 5 , Formula Ib, R 3 , R 3a , W, D, R 2a , R 2b and R 2c are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression, anxiety or intestinal inflammation, by administration of a therapeutically effective dose of a compound according to Formula I.
摘要翻译：本申请提供化合物，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R1，式Ia，R4，R5，式Ib，R3，R3a，W，D，R2a，R2b和R2c被定义于此。另外，本申请提供含有至少一种根据式I的化合物和任选的至少一种另外的治疗剂的药物组合物。最后，本申请提供了通过施用治疗有效剂量的化合物来治疗患有MCHR-1调节的疾病或病症例如肥胖症，糖尿病，抑郁症，焦虑或肠道炎症的患者的方法，一级方程式

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式