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1. 发明申请

WO2004067482A2 SUBSTITUTED ANILIDE LIGANDS FOR THE THYROID RECEPTOR 审中-公开
标题翻译：用于甲状腺受体的替代辅助配体
公开(公告)号：WO2004067482A2
公开(公告)日：2004-08-12
申请号：PCT/US2004/001985
申请日：2004-01-23
申请人： BRISTOL-MYERS SQUIBB COMPANY , KARO BIO AB , WASHBURN, William, N. , MENG, Wei , RYONO, Denis, E. , ELLSWORTH, Bruce, A. , ERICSSON, Thomas , RAHIMI- GHADIM, Mahmoud , GARG, Neeraj , MALM, Johan
发明人： WASHBURN, William, N. , MENG, Wei , RYONO, Denis, E. , ELLSWORTH, Bruce, A. , ERICSSON, Thomas , RAHIMI- GHADIM, Mahmoud , GARG, Neeraj , MALM, Johan
IPC分类号： C07C
CPC分类号： A61K45/06 , A61K31/195 , A61K31/277 , A61K31/44 , C07C233/25 , A61K2300/00
摘要： Novel thyroid receptor ligands are provided having the general formula I wherein X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 . and R 13 are as defined herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolic dysfunction or which are dependent upon the expression of a T 3 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的新型甲状腺受体配体，其中X，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11，R 12。和R 13如本文所定义。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。

2. 发明公开

EP1601641A2 SUBSTITUTED ANILIDE LIGANDS FOR THE THYROID RECEPTOR 审中-公开
标题翻译：替补ANILIDBINDER甲状腺
公开(公告)号：EP1601641A2
公开(公告)日：2005-12-07
申请号：EP04704944.0
申请日：2004-01-23
申请人： Bristol-Myers Squibb Company , KARO BIO AB
发明人： WASHBURN, William, N. , MENG, Wei , RYONO, Denis, E. , ELLSWORTH, Bruce, A. , ERICSSON, Thomas , RAHIMI- GHADIM, Mahmoud , GARG, Neeraj , MALM, Johan
IPC分类号： C07C229/08 , C07C229/22 , A61K31/24 , A61K31/195
CPC分类号： A61K45/06 , A61K31/195 , A61K31/277 , A61K31/44 , C07C233/25 , A61K2300/00
摘要： Novel thyroid receptor ligands are provided having the general formula I wherein X, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12. and R13 are as defined herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolic 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.

3. 发明申请

WO1997037646A1 CATECHOLAMINE SURROGATES USEFUL AS 'beta'3 AGONISTS 审中-公开
标题翻译： CATECHOLAMINE SURROGATES有用作β3激动剂
公开(公告)号：WO1997037646A1
公开(公告)日：1997-10-16
申请号：PCT/US1997005324
申请日：1997-04-01
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BRISTOL-MYERS SQUIBB COMPANY , CHENG, Peter, T., W. , BISACCHI, Gregory, S. , GAVAI, Ashvinikumar, V. , POSS, Kathleen, M. , RYONO, Denis, E. , SHER, Philip, M. , SUN, Chong-Qing , WASHBURN, William, N.
IPC分类号： A61K31/18
CPC分类号： C07C311/46 , C07C311/08 , C07C311/39 , C07D263/32 , C07D277/28 , C07F9/4056
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof. As used in formula (I), and throughout the specification, the symbols have the following meanings: R is lower alkyl, aryl or arylalkyl; R is hydrogen, hydroxyl, hydroxymethyl or halogen; R is hydrogen or alkyl; R and R are independently hydrogen, alkoxy, alkoxymethyl, hydroxyl, -CN, -CON(R )R 2 , -N(R )R , -NR COR , -NR SO2R ; or R and R may together with the carbon atoms to which they are bonded form a heterocycle; R , R and R are independently A or B, wherein A is hydrogen, alkyl, cylcoalkyl, halogen, hydroxyl, aryl, alkoxy, cyano, -SR , -SOR , -SO2R , -N(R )R , -NR COR , -OCH2CON(R )R , -OCH2CO2R , CON(R )R , -CO2R ; and B is -(CH2)nN(R )R , -(CH2)mPO(OR )OR , -(CH2)nNR COR , -O-aryl, -OCH2CH2N(R )R , -COR , -SO2N(R )R , -NR CO2R , -NR CO(N(R )R ), heterocycle or -R and R may together with the carbon atoms to which they are bonded form a heterocycle, provided that at least one of R , R and R is B; R and R are independently hydrogen or lower alkyl; R is lower alkyl; R is hydrogen, lower alkyl, aryl or arylalkyl; m is an integer of 0 to 6; and n is an integer of 1 to 6. These compounds are beta three adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.
摘要翻译：式（I）化合物及其药学上可接受的盐。在式（I）中使用，并且在整个说明书中，符号具有以下含义：R 1是低级烷基，芳基或芳基烷基; R 2是氢，羟基，羟甲基或卤素; R 3是氢或烷基; R 4和R 4独立地是氢，烷氧基，烷氧基甲基，羟基，-CN，-CON（R 6）R 6'，-CO 2，R 6， R 6）R 6，-NR 6 COR 8，-NR 6 SO 2 R 1; 或R 4和R 4'可以与它们所键合的碳原子一起形成杂环; R 5，R 5和R 5独立地是A或B，其中A是氢，烷基，环烷基，卤素，羟基，芳基，烷氧基，氰基，-SR 7，-SOR -SO 2 R 7，-N（R 6）R 6'，-NR 6 COR 8，-OCH 2 CON（R 6）R 6，-OCH 2 CO 2 R CON（R 6）R 6，-CO 2 R 6; 并且B是 - （CH 2）n N（R 6）R 6'， - （CH 2）m PO（OR 6）OR 6， - （CH 2）n NR 6 COR 8， -O-芳基，-OCH 2 CH 2 N（R 6）R 6'，-COR 7，-SO 2 N（R 6）R 6'，-NR 6 CO 2 R 7， NR 6 CO（N（R 6）R 6'），杂环或-R 5和R 5可以与它们所键合的碳原子一起形成杂环，条件是 R 5，R 5'和R 5“中的至少一个是B; R 6和R 6独立地是氢或低级烷基; R 7是低级烷基; R 8是氢，低级烷基，芳基或芳基烷基; m为0〜6的整数。并且n是1至6的整数。这些化合物是β三肾上腺素能受体激动剂，因此可用于例如糖尿病，肥胖症和胃肠道疾病的治疗。

4. 发明申请

WO2009018065A3 NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME 审中-公开
公开(公告)号：WO2009018065A3
公开(公告)日：2009-02-05
申请号：PCT/US2008/070962
申请日：2008-07-24
申请人： BRISTOL-MYERS SQUIBB COMPANY , SHI, Yan , CHENG, Peter, T., W. , WANG, Ying , RYONO, Denis, E.
发明人： SHI, Yan , CHENG, Peter, T., W. , WANG, Ying , RYONO, Denis, E.
IPC分类号： C07D213/81 , C07D231/14 , C07D233/90 , C07D241/24 , C07D249/10 , C07D277/56 , C07D277/68 , C07D471/04 , C07D513/04 , C07C237/22 , A61K31/426 , A61K31/4196 , A61K31/4164 , A61P3/00
摘要： Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure Formula: (I); where Q is Formula: (II); or Formula: (III); and R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 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.

5. 发明公开

EP2173717A2 NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME 失效
标题翻译：新型葡萄糖激酶激活和使用方法
公开(公告)号：EP2173717A2
公开(公告)日：2010-04-14
申请号：EP08782284.7
申请日：2008-07-24
申请人： Bristol-Myers Squibb Company
发明人： SHI, Yan , CHENG, Peter, T., W. , WANG, Ying , RYONO, Denis, E.
IPC分类号： C07D213/81 , C07D231/14 , C07D233/90 , C07D241/24 , C07D249/10 , C07D277/56 , C07D277/68 , C07D471/04 , C07D513/04 , C07C237/22 , A61K31/426 , A61K31/4196 , A61K31/4164 , A61P3/00
CPC分类号： C07D277/56 , C07C317/22 , C07D213/81 , C07D231/14 , C07D233/90 , C07D241/24 , C07D249/10 , C07D277/68 , C07D471/04 , C07D513/04
摘要： Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure Formula: (I); where Q is Formula: (II); or Formula: (III); and R1, R2, R3, R4, R5, R6, R7 and R8 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.

6. 发明授权

EP1292568B1 BENZAMIDE LIGANDS FOR THE THYROID RECEPTOR 有权
标题翻译：苯甲酰胺配体为甲状腺受体
公开(公告)号：EP1292568B1
公开(公告)日：2007-08-15
申请号：EP01946036.9
申请日：2001-06-01
申请人： Bristol-Myers Squibb Company
发明人： RYONO, Denis, E.
IPC分类号： C07C235/52 , A61K31/166
CPC分类号： A61K31/166 , C07C235/52 , C07C2601/02
摘要： New thyroid receptor ligands are provided which have the general formula (I) in which: X is -0-, -S-, -CH2-, -CO-, or -NH-; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 6 carbons, at least one of R2 and R3 being other than hydrogen; R4 is methyl, ethyl, n-propyl or trifluoromethyl; R5 is hydrogen or lower alkyl; R6 is carboxylic acid, or esters or prodrugs; R7 is hydrogen or an alkanoyl or an aroyl. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.
摘要翻译：提供了具有通式（I）的新的甲状腺受体配体，其中：X是-O - ， - S - ， - CH 2 - ， - CO-或-NH-; R1为卤素，三氟甲基或1-6个碳原子的烷基或3-7个碳原子的环烷基; R2和R3相同或不同，并且是氢，卤素，1至4个碳的烷基或3至6个碳的环烷基，R2和R3中的至少一个不是氢; R4是甲基，乙基，正丙基或三氟甲基; R5是氢或低级烷基; R6是羧酸，或酯或前药; R7是氢或烷酰基或芳酰基。另外，提供了用于预防，抑制或治疗与代谢功能障碍相关的疾病或依赖于T3调节基因的表达的方法，其中如上所述的化合物以治疗有效量施用。与代谢功能障碍相关或与T3调节基因的表达有关的这类疾病的例子包括肥胖症，高胆固醇血症，动脉粥样硬化，心律失常，抑郁症，骨质疏松症，甲状腺功能减退症，甲状腺肿，甲状腺癌以及青光眼，充血性心力衰竭和皮肤病。

7. 发明授权

EP2173717B9 NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME 失效
标题翻译：新型葡糖激酶激活剂及其使用方法
公开(公告)号：EP2173717B9
公开(公告)日：2013-06-26
申请号：EP08782284.7
申请日：2008-07-24
申请人： Bristol-Myers Squibb Company
发明人： SHI, Yan , CHENG, Peter, T., W. , WANG, Ying , RYONO, Denis, E.
IPC分类号： C07D213/81 , C07D231/14 , C07D233/90 , C07D241/24 , C07D249/10 , C07D277/56 , C07D277/68 , C07D471/04 , C07D513/04 , C07C237/22 , A61K31/426 , A61K31/4196 , A61K31/4164 , A61P3/00
CPC分类号： C07D277/56 , C07C317/22 , C07D213/81 , C07D231/14 , C07D233/90 , C07D241/24 , C07D249/10 , C07D277/68 , C07D471/04 , C07D513/04

8. 发明授权

EP2173717B1 NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME 失效
公开(公告)号：EP2173717B1
公开(公告)日：2013-03-27
申请号：EP08782284.7
申请日：2008-07-24
申请人： Bristol-Myers Squibb Company
发明人： SHI, Yan , CHENG, Peter, T., W. , WANG, Ying , RYONO, Denis, E.
IPC分类号： C07D213/81 , C07D231/14 , C07D233/90 , C07D241/24 , C07D249/10 , C07D277/56 , C07D277/68 , C07D471/04 , C07D513/04 , C07C237/22 , A61K31/426 , A61K31/4196 , A61K31/4164 , A61P3/00
CPC分类号： C07D277/56 , C07C317/22 , C07D213/81 , C07D231/14 , C07D233/90 , C07D241/24 , C07D249/10 , C07D277/68 , C07D471/04 , C07D513/04

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