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1. 发明申请

WO2009018065A2 NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME 审中-公开
标题翻译：新型葡糖激酶激活剂及其使用方法
公开(公告)号：WO2009018065A2
公开(公告)日：2009-02-05
申请号：PCT/US2008070962
申请日：2008-07-24
申请人： SQUIBB BRISTOL MYERS CO , 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 , A61K31/4164 , A61K31/4196 , A61K31/426 , A61P3/00 , C07C237/22 , C07D231/14 , C07D233/90 , C07D241/24 , C07D249/10 , C07D277/56 , C07D277/68 , C07D471/04 , C07D513/04
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.
摘要翻译：提供了作为酶葡糖激酶活化剂的化合物，因此可用于治疗糖尿病和相关疾病，所述化合物具有结构式：（I）; 其中Q是式（II）; 或式（III）; 且R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如本文所定义或其药学上可接受的盐。还提供了使用上述化合物治疗糖尿病和相关疾病的方法。

2. 发明申请

WO0194293A2 BENZAMIDE LIGANDS FOR THE THYROID RECEPTOR 审中-公开
标题翻译：苄基受体的苯扎林配体
公开(公告)号：WO0194293A2
公开(公告)日：2001-12-13
申请号：PCT/US0117742
申请日：2001-06-01
申请人： SQUIBB BRISTOL MYERS CO , RYONO DENIS E
发明人： RYONO DENIS E
IPC分类号： A61K45/00 , A61K31/07 , A61K31/166 , A61K31/195 , A61K31/22 , A61K31/351 , A61K31/40 , A61K31/404 , A61K31/4418 , A61K31/455 , A61K31/592 , A61K38/28 , A61P3/00 , A61P3/04 , A61P3/06 , A61P5/14 , A61P5/16 , A61P9/04 , A61P9/06 , A61P9/10 , A61P17/00 , A61P17/02 , A61P17/10 , A61P17/16 , A61P19/10 , A61P25/24 , A61P27/06 , A61P35/00 , C07C235/52 , C07C235/00
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）的新甲状腺受体配体，其中：X是-O - ， - S - ， - CH 2 - ， - CO-或-NH-; R1是卤素，三氟甲基或1-6个碳的烷基或3-7个碳的环烷基; R2和R3相同或不同，为氢，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。此外，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，其中以治疗有效量施用如上所述的化合物。与代谢功能障碍相关或依赖于T3调节基因的表达的这种疾病的实例包括肥胖症，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，甲状腺癌，青光眼，充血性心力衰竭和皮肤病。

3. 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.

4. 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。

5. 发明申请

WO2004007430A2 BENZAMIDE OR PHENYLACETAMIDE DERIVATIVES USEFUL AS THYROID RECEPTOR LIGANDS 审中-公开
标题翻译：苯甲酰胺或苯甲酰胺衍生物作为甲状腺受体配体有用
公开(公告)号：WO2004007430A2
公开(公告)日：2004-01-22
申请号：PCT/EP0307333
申请日：2003-07-08
申请人： KAROBIO AB , SQUIBB BRISTOL MYERS CO , GARG NEERAJ , GADIM MAHMOUD RAHIMI , ERICSSON THOMAS ANDERS WILSON , MALM LARS JOHAN , RYONO DENIS EVAN
发明人： GARG NEERAJ , GADIM MAHMOUD RAHIMI , ERICSSON THOMAS ANDERS WILSON , MALM LARS JOHAN , RYONO DENIS EVAN
IPC分类号： A61K31/427 , A61K31/155 , A61K31/18 , A61K31/195 , A61K31/198 , A61K31/7034 , A61P3/04 , A61P3/06 , A61P5/14 , A61P5/16 , A61P9/00 , A61P9/10 , A61P17/00 , A61P19/10 , A61P25/24 , A61P35/00 , A61P43/00 , C07C235/34 , C07C235/52
CPC分类号： C07C235/52 , C07C235/34
摘要： This invention relates to novel compounds, which are thyroid receptor ligands, and to methods of preparing such compounds. 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 herein is administered in a therapeutically effective amount.
摘要翻译：本发明涉及作为甲状腺受体配体的新化合物及其制备方法。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与T3调节基因的表达相关的疾病或病症的方法，其中本文所述的化合物以治疗有效量施用。

6. 发明申请

WO2004067482A3 SUBSTITUTED ANILIDE LIGANDS FOR THE THYROID RECEPTOR 审中-公开
标题翻译：用于甲状腺受体的取代的苯胺配体
公开(公告)号：WO2004067482A3
公开(公告)日：2004-10-21
申请号：PCT/US2004001985
申请日：2004-01-23
申请人： SQUIBB BRISTOL MYERS CO , KAROBIO 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： A61K31/195 , A61K31/24 , A61K31/277 , A61K31/44 , C07C20060101 , C07C229/08 , C07C229/22 , C07C233/25 , C07D213/57
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.
摘要翻译：提供具有通式I的新的甲状腺受体配体，其中X，R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，R12。和R13如本文所定义。此外，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病症或依赖于T3调节基因表达的方法，其中如上所述的化合物以治疗有效量施用。

7. 发明申请

WO2004007430A3 BENZAMIDE OR PHENYLACETAMIDE DERIVATIVES USEFUL AS THYROID RECEPTOR LIGANDS 审中-公开
公开(公告)号：WO2004007430A3
公开(公告)日：2004-01-22
申请号：PCT/EP2003/007333
申请日：2003-07-08
申请人： KARO BIO AB , BRISTOL-MYERS SQUIBB COMPANY , GARG, Neeraj , GADIM, Mahmoud, Rahimi , ERICSSON, Thomas, Anders, Wilson , MALM, Lars, Johan , RYONO, Denis, Evan
发明人： GARG, Neeraj , GADIM, Mahmoud, Rahimi , ERICSSON, Thomas, Anders, Wilson , MALM, Lars, Johan , RYONO, Denis, Evan
IPC分类号： C07C235/52
摘要： This invention relates to novel compounds, which are thyroid receptor ligands, and to methods of preparing such compounds. 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 T 3 regulated gene, wherein a compound as described herein is administered in a therapeutically effective amount.

8. 发明申请

WO0039077A3 THYROID RECEPTOR LIGANDS 审中-公开
标题翻译：甲状腺受体配体
公开(公告)号：WO0039077A3
公开(公告)日：2000-09-21
申请号：PCT/IB9902084
申请日：1999-12-23
申请人： KAROBIO AB , HANGELAND JON , ZHANG MINSHENG , CARINGAL YOLANDA , RYONO DENIS , LI YI LIN , MALM JOHAN , LIU YE , GARG NEERAJ , LITTEN CHRIS , GARCIA COLLAZO ANA MARIA , KOEHLER KONRAD
发明人： HANGELAND JON , ZHANG MINSHENG , CARINGAL YOLANDA , RYONO DENIS , LI YI-LIN , MALM JOHAN , LIU YE , GARG NEERAJ , LITTEN CHRIS , GARCIA COLLAZO ANA MARIA , KOEHLER KONRAD
IPC分类号： C07D233/88 , A61K31/381 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/4168 , A61K31/433 , A61K31/44 , A61K31/4409 , A61K31/495 , A61K31/55 , A61K45/00 , A61P3/04 , A61P3/06 , A61P5/14 , A61P9/06 , A61P9/10 , A61P17/00 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/10 , A61P25/24 , A61P27/06 , A61P35/00 , C07C235/32 , C07C235/34 , C07C235/52 , C07C307/06 , C07C311/00 , C07C311/51 , C07C323/41 , C07C323/59 , C07C323/60 , C07D207/09 , C07D207/26 , C07D207/27 , C07D211/24 , C07D211/34 , C07D211/58 , C07D211/60 , C07D211/96 , C07D213/38 , C07D213/40 , C07D213/74 , C07D223/12 , C07D231/38 , C07D233/54 , C07D241/04 , C07D257/04 , C07D285/06 , C07D285/12 , C07D285/125 , C07D285/135 , C07D295/13 , C07D295/185 , C07D333/20 , C07D333/34 , A61K31/195 , C07C237/06 , C07C279/14 , C07D207/16 , C07D209/20
CPC分类号： C07D207/27 , C07C235/32 , C07C235/52 , C07C307/06 , C07C311/51 , C07C323/41 , C07C323/60 , C07D207/09 , C07D211/24 , C07D211/34 , C07D211/58 , C07D211/96 , C07D213/40 , C07D223/12 , C07D231/38 , C07D233/64 , C07D257/04 , C07D285/06 , C07D285/135 , C07D295/13 , C07D295/185 , C07D333/20
摘要： New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; 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 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR'R'') or an acylsulphonamide (CONHSO2R') derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, R4 may be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR'R''). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5=H). 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）的新甲状腺受体配体，其中：n为0至4的整数; R1是卤素，三氟甲基或1-6个碳的烷基或3-7个碳的环烷基; R2和R3相同或不同，为氢，卤素，1至4个碳的烷基或3至5个碳的环烷基，R2和R3中的至少一个不是氢; R4是羧酸酰胺（CONR'R“）或酰基磺酰胺（CONHSO 2 R'）衍生物或其药学上可接受的盐及其所有立体异构体; 或当n等于或大于1时，R 4可以是可被取代或未取代的杂芳族部分，或胺（NR'R“）。 R5是氢或酰基（如乙酰基或苯甲酰基）或能够生物转化以产生游离酚结构的其他基团（其中R5 = H）。此外，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，其中以治疗有效量施用如上所述的化合物。与代谢功能障碍相关或依赖于T3调节基因的表达的这种疾病的实例包括肥胖症，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，甲状腺癌，青光眼，充血性心力衰竭和皮肤病。

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