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1. 发明申请

WO2004093806A2 COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS 审中-公开
标题翻译：用于治疗代谢性疾病的化合物
公开(公告)号：WO2004093806A2
公开(公告)日：2004-11-04
申请号：PCT/US2004/012142
申请日：2004-04-20
申请人： WELLSTAT THERAPEUTICS CORPORATION , HODGE, Kirvin, L. , KAUFMAN, Robert, J. , LEE, Albert , SHARMA, Shalini , VON BORSTEL, Reid, W.
发明人： HODGE, Kirvin, L. , KAUFMAN, Robert, J. , LEE, Albert , SHARMA, Shalini , VON BORSTEL, Reid, W.
IPC分类号： A61K
CPC分类号： C07C69/734 , A61K31/235
摘要： Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Formula (I) wherein n is 1 or 2; m is 2 or 3; q is 0 or 1; t is 0 or 1; R 2 is alkyl having from 1 to 3 carbon atoms; R 3 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula I by a ring carbon; and R 1 is hydrogen or alkyl having 1 or 2 carbon atoms. Alternatively, when R 1 is hydrogen, the biologically active agent can be a pharmaceutically acceptable salt of the compound of Formula (I).
摘要翻译：公开了用于治疗各种代谢疾病如胰岛素抵抗综合征，糖尿病，高脂血症，脂肪肝疾病，恶病质，肥胖症，动脉粥样硬化和动脉硬化的药剂。式（I）其中n为1或2; m为2或3; q为0或1; t为0或1; R 2是具有1至3个碳原子的烷基; R 3是氢，卤素，具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基; A是未取代的或被1或2个选自：卤素，具有1或2个碳原子的烷基，全氟甲基，具有1或2个碳原子的烷氧基和全氟甲氧基取代的苯基; 或具有3至6个环碳原子的环烷基，其中环烷基是未取代的或一个或两个环碳独立地被甲基或乙基单取代; 或具有1或2个选自N，S和O的环杂原子的5或6元杂芳环，杂芳环通过环碳与式I化合物的其余部分共价结合; 和R 1是氢或具有1或2个碳原子的烷基。或者，当R 1是氢时，生物活性剂可以是式（I）化合物的药学上可接受的盐。

2. 发明申请

WO2004073611A2 COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS 审中-公开
标题翻译：用于治疗代谢性疾病的化合物
公开(公告)号：WO2004073611A2
公开(公告)日：2004-09-02
申请号：PCT/US2004/003718
申请日：2004-02-09
申请人： WELLSTAT THERAPEUTICS CORPORATION , HODGE, Kirvin, L. , LEE, Albert , SHARMA, Shalini , VON BORSTEL, Reid, W.
发明人： HODGE, Kirvin, L. , LEE, Albert , SHARMA, Shalini , VON BORSTEL, Reid, W.
IPC分类号： A61K
CPC分类号： C07C69/734 , A61K31/192 , A61K31/24 , C07C59/68 , C07C65/24 , C07C69/76 , C07C69/92
摘要： Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, artherosclerosis and arteriosclerosis are disclosed. Formula (I) wherein n is 1 or 2; m is 0, 1, 2, 4 or 5; q is 0 or 1; t is 0 or 1; R 2 is alkyl from 1 to 3 carbon atoms; R 3 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; A is phenyl, unsubstituted or substituted by or 1 or 2 groups selected from: halo, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloaldyl having from 3 to 6 ring carbon atoms wherein the cycloaldyl is unsubstitited or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compounds of formula (I) by a ring carbon; and R 1 is hydrogen or alkyl having 1 or 2 carbon atoms. Alternatively, when R 1 is hydrogen, the biologically active agent can be a pharmaceutically acceptable salt of the compound of Formula (I).
摘要翻译：公开了用于治疗各种代谢疾病如胰岛素抵抗综合征，糖尿病，高脂血症，脂肪肝疾病，恶病质，肥胖症，动脉粥样硬化和动脉硬化的药剂。式（I）其中n为1或2; m为0,1,2,4或5; q为0或1; t为0或1; R 2是1至3个碳原子的烷基; R 3是氢，卤素，具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基; A是未取代或被1或2个选自以下的基团取代的苯基：卤素，具有1或2个碳原子的烷基，全氟甲基，具有1或2个碳原子的烷氧基和全氟甲氧基; 或具有3至6个环碳原子的环戊烯基，其中所述环烯基未被取代或一个或两个环碳独立地被甲基或乙基单取代; 或具有1或2个选自N，S和O的环杂原子的5或6元杂芳环，杂芳环通过环碳与其余的式（I）化合物共价结合; 和R 1是氢或具有1或2个碳原子的烷基。或者，当R 1是氢时，生物活性剂可以是式（I）化合物的药学上可接受的盐。

3. 发明申请

WO2002100341A3 COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS 审中-公开
公开(公告)号：WO2002100341A3
公开(公告)日：2002-12-19
申请号：PCT/US2002/018388
申请日：2002-06-12
申请人： WELLSTAT THERAPEUTICS CORPORATION , SHARMA, Shalini , VON, Borstel, Reid, W. , HODGE, Kirvin, L. , BAMAT, Michael, K.
发明人： SHARMA, Shalini , VON, Borstel, Reid, W. , HODGE, Kirvin, L. , BAMAT, Michael, K.
IPC分类号： C07D249/12
摘要： Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

4. 发明申请

WO2004098496A2 COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS 审中-公开
标题翻译：用于治疗代谢性疾病的化合物
公开(公告)号：WO2004098496A2
公开(公告)日：2004-11-18
申请号：PCT/US2004/012141
申请日：2004-04-20
申请人： WELLSTAT THERAPEUTICS CORPORATION , HODGE, Kirvin, L. , SHARMA, Shalini , VON BORSTEL, Reid, W.
发明人： HODGE, Kirvin, L. , SHARMA, Shalini , VON BORSTEL, Reid, W.
IPC分类号： A61K
CPC分类号： A61K31/235 , A61K31/19 , A61K31/24
摘要： Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Formula (I) wherein n is 1 or 2; m is 0 to 4; q is 0 or 1; t is 0 or 1; R 2 is alkyl having from 1 to 3 carbon atoms; R 3 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula (I) by a ring carbon; and R 1 is hydrogen or alkyl having 1 or 2 carbon atoms. Alternatively, when R 1 is hydrogen, the biologically active agent can be a pharmaceutically acceptable salt of the compound of Formula (I).
摘要翻译：公开了用于治疗各种代谢疾病如胰岛素抵抗综合征，糖尿病，高脂血症，脂肪肝疾病，恶病质，肥胖症，动脉粥样硬化和动脉硬化的药剂。式（I）其中n为1或2; m为0〜4; q为0或1; t为0或1; R 2是具有1至3个碳原子的烷基; R 3是氢，卤素，具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基; A是未取代的或被1或2个选自：卤素，具有1或2个碳原子的烷基，全氟甲基，具有1或2个碳原子的烷氧基和全氟甲氧基取代的苯基; 或具有3至6个环碳原子的环烷基，其中环烷基是未取代的或一个或两个环碳独立地被甲基或乙基单取代; 或具有1或2个选自N，S和O的环杂原子的5或6元杂芳环，杂芳环通过环碳与式（I）化合物的其余部分共价结合; 和R 1是氢或具有1或2个碳原子的烷基。或者，当R 1是氢时，生物活性剂可以是式（I）化合物的药学上可接受的盐。

5. 发明申请

WO2005018628A1 COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS 审中-公开
标题翻译：用于治疗代谢性疾病的化合物
公开(公告)号：WO2005018628A1
公开(公告)日：2005-03-03
申请号：PCT/US2004/026561
申请日：2004-08-16
申请人： WELLSTAT THERAPEUTICS CORPORATION , SHARMA, Shalini , VON BORSTEL, Reid, W. , HODGE, Kirvin, L.
发明人： SHARMA, Shalini , VON BORSTEL, Reid, W. , HODGE, Kirvin, L.
IPC分类号： A61K31/19
CPC分类号： C07C323/62
摘要： Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Formula (I), wherein n is 1 or 2; m is 0 or 1; q is 0 or 1; t is 0 or 1; R 5 is alkyl having from 1 to 3 carbon atoms; R 9 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently monosubstituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and 0 and the heteroaromatic ring is covalently bound to the remainder of the compound of formula I by a ring carbon; and X is -CH 2 -, Q is -OR 1 and R 1 is methyl or ethyl; or X is -CH 2 CR 12 R 13 - or - CH 2 CH(NHAc)-wherein each of R 12 and R 13 is independently hydrogen or methyl, Q is OR 1 and R 1 is hydrogen or alkyl having from 1 to 7 carbon atoms; or X is -CH 2 CH 2 - and Q is NR 10 R 1 ' wherein one of R 10 and R 11 is hydrogen, alkyl having from 1 to 3 carbon atoms or hydroxy, and the other is hydrogen. Alternatively, when R 1 is hydrogen, the biologically active agent can be a pharmaceutically acceptable salt of the compound of Formula (I).
摘要翻译：公开了可用于治疗各种代谢紊乱，例如胰岛素抵抗综合征，糖尿病，高脂血症，脂肪肝疾病，恶病质，肥胖症，动脉粥样硬化和动脉硬化的药剂。式（I），其中n为1或2; m为0或1; q为0或1; t为0或1; R 5是具有1至3个碳原子的烷基; R 9是氢，卤素，具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基; A是未取代的或被1或2个选自：卤素，具有1或2个碳原子的烷基，全氟甲基，具有1或2个碳原子的烷氧基和全氟甲氧基取代的苯基; 或具有3至6个环碳原子的环烷基，其中所述环烷基是未取代的或一个或两个环碳原子被甲基或乙基独立地单取代; 或具有1或2个选自N，S和0的环杂原子的5或6元杂芳环，并且所述杂芳环通过环碳与式I化合物的其余部分共价结合; 且X为-CH 2 - ，Q为-OR 1且R 1为甲基或乙基; 或X是-CH 2 CR 12 R 13 - 或-CH 2 CH（NH-C） - 其中R 12和R 13各自独立地为氢或甲基，Q为OR 1且R 1为氢或具有1至7个碳原子的烷基; 或X为-CH 2 CH 2 - 且Q为NR 10 R 1'，其中R 10和R 11之一为氢，具有1至3个碳原子的烷基或羟基，另一个为氢。或者，当R 1是氢时，生物活性剂可以是式（I）化合物的药学上可接受的盐。

6. 发明申请

WO2002100341A2 COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS 审中-公开
标题翻译：用于治疗代谢性疾病的化合物
公开(公告)号：WO2002100341A2
公开(公告)日：2002-12-19
申请号：PCT/US2002/018388
申请日：2002-06-12
申请人： WELLSTAT THERAPEUTICS CORPORATION , SHARMA, Shalini , VON, Borstel, Reid, W. , HODGE, Kirvin, L.
发明人： SHARMA, Shalini , VON, Borstel, Reid, W. , HODGE, Kirvin, L.
IPC分类号： A61K
CPC分类号： C07B41/12 , A01N37/10 , A61K31/165 , A61K31/192 , A61K31/216 , A61K31/235 , A61K31/41 , A61K31/4196 , A61K31/44 , A61K31/445 , A61K31/535 , A61K31/54 , C07C59/68 , C07C59/90 , C07C67/47 , C07C69/738 , C07C209/68 , C07C217/22 , C07C233/31 , C07C233/47 , C07C235/78 , C07C235/84 , C07C259/06 , C07C323/52 , C07C323/59 , C07C2601/02 , C07C2601/04 , C07C2602/04 , C07D213/30 , C07D213/55 , C07D249/10 , C07D249/12 , C07D257/04 , C07D333/16 , C07D333/24 , Y10S514/866
摘要： Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
摘要翻译：公开了可用于治疗各种代谢紊乱（例如胰岛素抵抗综合征，糖尿病，高脂血症，脂肪肝疾病，恶病质，肥胖症，动脉粥样硬化和动脉硬化）的化合物。

7. 发明申请

WO2004091486A2 COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS 审中-公开
标题翻译：用于治疗代谢性疾病的化合物
公开(公告)号：WO2004091486A2
公开(公告)日：2004-10-28
申请号：PCT/US2004/010799
申请日：2004-04-08
申请人： WELLSTAT THERAPEUTICS CORPORATION , HODGE, Kirvin, L. , SHARMA, Shalini , VON BORSTEL, Reid, W. , WOLPE, Stephen, D.
发明人： HODGE, Kirvin, L. , SHARMA, Shalini , VON BORSTEL, Reid, W. , WOLPE, Stephen, D.
IPC分类号： A61K
CPC分类号： A61K31/19 , A61K31/195 , A61K31/34 , A61K31/36 , A61K31/47
摘要： Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Wherein n is 1 or 2; m is 0, 1, 2, 3 or 4; q is 0 or 1; t is 0 or 1; R 2 is alkyl having from 1 to 3 carbon atoms; R 3 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and 0 and the heteroaromatic ring is covalently bound to the remainder of the compound of formula I by a ring carbon; and R 1 is hydrogen or alkyl having 1 or 2 carbon atoms, provided that when m is 0 or 1, R 1 is not hydrogen. Alternatively, when R 1 is hydrogen, the biologically active agent can be a pharmaceutically acceptable salt of the compound of Formula I.
摘要翻译：公开了用于治疗各种代谢疾病如胰岛素抵抗综合征，糖尿病，高脂血症，脂肪肝疾病，恶病质，肥胖症，动脉粥样硬化和动脉硬化的药剂。其中n为1或2; m为0,1,2,3或4; q为0或1; t为0或1; R 2是具有1至3个碳原子的烷基; R 3是氢，卤素，具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基; A是未取代的或被1或2个选自：卤素，具有1或2个碳原子的烷基，全氟甲基，具有1或2个碳原子的烷氧基和全氟甲氧基取代的苯基; 或具有3至6个环碳原子的环烷基，其中环烷基是未取代的或一个或两个环碳独立地被甲基或乙基单取代; 或具有1或2个选自N，S和0的环杂原子的5或6元杂芳环，并且所述杂芳环通过环碳与式I化合物的其余部分共价结合; 并且R 1是氢或具有1或2个碳原子的烷基，条件是当m是0或1时，R 1不是氢。或者，当R 1是氢时，生物活性剂可以是式I化合物的药学上可接受的盐。

8. 发明申请

WO2007117791A3 COMBINATION TREATMENT OF METABOLIC DISORDERS 审中-公开
公开(公告)号：WO2007117791A3
公开(公告)日：2007-10-18
申请号：PCT/US2007/063288
申请日：2007-03-05
申请人： WELLSTAT THERAPEUTICS CORPORATION , VON BORSTEL, Reid, W. , HODGE, Kirvin, L.
发明人： VON BORSTEL, Reid, W. , HODGE, Kirvin, L.
IPC分类号： A61K31/33 , A61K31/505 , A61K31/435 , A61K31/44 , A61K31/425 , A61K31/38
摘要： Various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis can be treated with a combination of a direct PPAR-gamma agonist and a Compound of Formula (I) or a pharmaceutically acceptable salt thereof (I) Three of R 1 , R 2 , R 3 , R 4 and R 5 are hydrogen and the remainder are independently selected from the group consisting of hydrogen, halo, hydroxy, methyl, ethyl, perfiuoromethyl, methoxy, ethoxy, and perfluoromethoxy; and m is 0, 2 or 4. R 6 is hydrogen, O or hydroxy, and X is -OR 7 , wherein R 7 is hydrogen or alkyl having from 1 to 3 carbon atoms; or R 6 is hydrogen, and X is -NR 8 R 9 , wherein R 8 is hydrogen or hydroxy and R 9 is hydrogen, methyl or ethyl. When X is -NR 8 R 9 , hydroxy none of R 1 , R 2 , R 3 , R 4 and R 5 is hydroxy.

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