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31. 发明申请

WO2009091732A1 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：WO2009091732A1
公开(公告)日：2009-07-23
申请号：PCT/US2009/030845
申请日：2009-01-13
申请人： WELLSTAT THERAPEUTICS CORPORATION , SHARMA, Shalini , VON BORSTEL, Reid, W.
发明人： SHARMA, Shalini , VON BORSTEL, Reid, W.
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04
CPC分类号： C07C69/76 , C07C67/343
摘要： Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. The agent is a compound of Formula (I): wherein m is 0, 1, 2, 3, 4, 5, 6, 7 or 8; R 1 is hydrogen or alkyl having from 1 to 3 carbon atoms; and R 2 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, hydroxy, 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; Alternatively, the 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，多囊卵巢综合征，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。该试剂是式（I）的化合物：其中m是0,1,2,3,4,5,6,7或8; R1是氢或具有1至3个碳原子的烷基; 且R 2为氢，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，羟基，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; 或者，试剂可以是式（I）化合物的药学上可接受的盐。

32. 发明申请

WO2007095462A2 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：WO2007095462A2
公开(公告)日：2007-08-23
申请号：PCT/US2007/061908
申请日：2007-02-09
申请人： WELLSTAT THERAPEUTICS CORPORATION , SHARMA, Shalini , VON BORSTEL, Reid, W.
发明人： SHARMA, Shalini , VON BORSTEL, Reid, W.
CPC分类号： C07C43/23
摘要： Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Formula (I) wherein n is 1 or 2; q is 0 or 1; t is 0 or 1; R 1 is alkyl having from 1 to 3 carbon atoms; R 2 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, hydroxy, 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. Alternatively, the 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，多囊卵巢综合征，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; q为0或1; t为0或1; R 1是具有1至3个碳原子的烷基; R 2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，羟基，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。或者，该试剂可以是式I化合物的药学上可接受的盐。

33. 发明申请

WO2007092729A3 COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS 审中-公开
公开(公告)号：WO2007092729A3
公开(公告)日：2007-08-16
申请号：PCT/US2007/061441
申请日：2007-02-01
申请人： WELLSTAT THERAPEUTICS CORPORATION , SHARMA, Shalini , VON BORSTEL, Reid, W.
发明人： SHARMA, Shalini , VON BORSTEL, Reid, W.
IPC分类号： A61K31/075 , A01N31/14
摘要： Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Formula (I) wherein n is 1 or 2; m is 0, 1, 2, 3, or 4; q is 0 or 1; tis 0 or 1; R 1 is alkyl having from 1 to 3 carbon atoms; R 2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; one of R 3 and R 4 is hydrogen or hydroxy and the other is hydrogen; or R 3 and R 4 together are =O; R 5 is hydrogen or alkyl having one, two, three, four or five carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, 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. Alternatively, the agent can be a pharmaceutically acceptable salt of the compound of Formula (I).

34. 发明申请

WO2007092729A2 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：WO2007092729A2
公开(公告)日：2007-08-16
申请号：PCT/US2007061441
申请日：2007-02-01
申请人： WELLSTAT THERAPEUTICS CORP , SHARMA SHALINI , VON BORSTEL REID W
发明人： SHARMA SHALINI , VON BORSTEL REID W
CPC分类号： A61K31/185 , C07C327/12
摘要： Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Formula (I) wherein n is 1 or 2; m is 0, 1, 2, 3, or 4; q is 0 or 1; tis 0 or 1; R 1 is alkyl having from 1 to 3 carbon atoms; R 2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; one of R 3 and R 4 is hydrogen or hydroxy and the other is hydrogen; or R 3 and R 4 together are =O; R 5 is hydrogen or alkyl having one, two, three, four or five carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, 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. Alternatively, the 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，多囊卵巢综合征，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物。式（I）其中n是1或2; m是0,1,2,3或4; q是0或1; 0或1; R 1是具有1至3个碳原子的烷基; R 2为氢，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; R 3和R 4中的一个是氢或羟基，另一个是氢; 或R 3和R 4一起是= O; R 5是氢或具有1,2,3,4或5个碳原子的烷基; A是未取代的或被1或2个选自以下的基团取代的苯基：卤素，羟基，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个环碳原子的环烷基，其中所述环烷基未被取代或者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元杂芳族环，并且杂芳族环通过环碳与式（I）化合物的其余部分共价结合。或者，所述药剂可以是式（I）化合物的药学上可接受的盐。

35. 发明申请

WO2007087505A2 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：WO2007087505A2
公开(公告)日：2007-08-02
申请号：PCT/US2007060832
申请日：2007-01-22
申请人： WELLSTAT THERAPEUTICS CORP , SHARMA SHALINI , VON BORSTEL REID W
发明人： SHARMA SHALINI , VON BORSTEL REID W
IPC分类号： A61K31/138
CPC分类号： C07C49/84 , A61K31/138 , C07C43/23
摘要： Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, 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 1 is alkyl having from 1 to 3 carbon atoms; R 2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; one of R 3 and R 4 is hydrogen or hydroxy and the other is hydrogen; or R 3 and R 4 together are =O; R 5 is hydrogen or alkyl having one, two, three, four or five carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, 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. Alternatively, the. 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，多囊卵巢综合征，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物。其中n是1或2; m是0,1,2,3或4; q是0或1; t是0或1; R 1是具有1至3个碳原子的烷基; R 2为氢，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; R 3和R 4中的一个是氢或羟基，另一个是氢; 或R 3和R 4一起是= O; R 5是氢或具有1,2,3,4或5个碳原子的烷基; A是未取代的或被1或2个选自以下的基团取代的苯基：卤素，羟基，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个环碳原子的环烷基，其中所述环烷基未被取代或者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元杂芳族环，并且所述杂芳族环通过环碳与式I化合物的其余部分共价结合。或者，药剂可以是式I化合物的药学上可接受的盐。

36. 发明申请

WO2007087504A2 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：WO2007087504A2
公开(公告)日：2007-08-02
申请号：PCT/US2007/060830
申请日：2007-01-22
申请人： WELLSTAT THERAPEUTICS CORPORATION , SHARMA, Shalini , VON BORSTEL, Reid, W.
发明人： SHARMA, Shalini , VON BORSTEL, Reid, W.
IPC分类号： A61K31/366
CPC分类号： C07D307/33
摘要： Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, 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 1 is alkyl having from 1 to3 carbon atoms; R 2 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, hydroxy, 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. Alternatively, the 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，多囊卵巢综合征，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 1是具有1至3个碳原子的烷基; R 2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，羟基，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。或者，试剂可以是式（I）化合物的药学上可接受的盐。

37. 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.

38. 发明申请

WO2009151695A1 COMPOUNDS AND METHOD FOR REDUCING URIC ACID 审中-公开
标题翻译：化合物和减少尿酸的方法
公开(公告)号：WO2009151695A1
公开(公告)日：2009-12-17
申请号：PCT/US2009/037128
申请日：2009-03-13
申请人： WELLSTAT THERAPEUTICS CORPORATION , O'NEIL, James, Dennen , BAMAT, Michael, K. , VON BORSTEL, Reid, W. , SHARMA, Shalini , ARUDCHANDRAN, Ramachandran
发明人： O'NEIL, James, Dennen , BAMAT, Michael, K. , VON BORSTEL, Reid, W. , SHARMA, Shalini , ARUDCHANDRAN, Ramachandran
IPC分类号： A01N43/08
CPC分类号： C07C59/68 , A23G3/36 , A23G3/38 , A23G3/42 , A23G3/48 , A23G3/563 , A61K8/498 , A61K9/0056 , A61K31/192 , A61K31/216 , A61K31/352 , A61K31/704 , A61K45/06 , A61Q11/00 , C07C59/66 , C07C59/84 , C07C59/88 , C07C59/90 , C07C61/39 , C07C69/716 , C07C69/734 , C07C69/738 , C07C2601/02
摘要： Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula (I) or a pharmaceutically acceptable salt thereof. In Formula (I) m is 0, 1, 2, 3 or 4; n is 0 or 1; m + n is not more than 4; t is 0 or 1; q is 0 or 1; and r is 0, 1 or 2. R 6 is hydrogen, methyl or ethyl and R 12 is hydrogen or methyl, or R 6 is hydroxy and R 12 is hydrogen, or R 6 is O and R 12 is absent, or R 6 and R 12 together are -CH 2 CH 2 -. R 7 is hydrogen or alkyl having from 1 to 3 carbon atoms. One of R 8 and R 9 is alkyl having from 1 to 3 carbon atoms, and the other is hydrogen or alkyl having from 1 to 3 carbon atoms. R 10 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms or alkoxy having from 1 to 3 carbon atoms. X is C(O) and r is 0 and t is 0; or X is NH(R 11 ) wherein R 11 is hydrogen or alkyl having from 1 to 3 carbon atoms. A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from halo, hydroxy, methyl, ethyl, perfluoromethyl, methoxy, ethoxy, and perfluoromethoxy; 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; 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. The uric acid-lowering effects of the Compounds of Formula (I) are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, and cognitive impairment.
摘要翻译：通过施用式（I）的化合物或其药学上可接受的盐，减少哺乳动物受试者的尿酸并增加尿酸的排泄。式（I）中，m为0,1,2,3或4; n为0或1; m + n不大于4; t为0或1; q为0或1; R6是氢，甲基或乙基，R12是氢或甲基，或R6是羟基，R12是氢，或R6是O，R12不存在，或者R6和R12一起是-CH 2 CH 2 - 。 R7是氢或具有1至3个碳原子的烷基。 R8和R9中的一个是具有1至3个碳原子的烷基，另一个是氢或具有1至3个碳原子的烷基。 R 10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。 X为C（O），r为0且t为0; 或X是NH（R 11），其中R 11是氢或具有1至3个碳原子的烷基。 A是未取代或被1或2个选自卤素，羟基，甲基，乙基，全氟甲基，甲氧基，乙氧基和全氟甲氧基的基团取代的苯基; 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; 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原子被甲基或乙基独立地单取代。式（I）化合物的尿酸降低作用用于治疗或预防各种病症，包括痛风，高尿酸血症，升高的尿酸水平，不符合常规诊断为高尿酸血症，肾功能不全的水平，肾结石，心血管疾病，发生心血管疾病的风险，肿瘤溶解综合征和认知障碍。

39. 发明申请

WO2008022267A3 COMBINATION TREATMENT FOR METABOLIC DISORDERS 审中-公开
公开(公告)号：WO2008022267A3
公开(公告)日：2008-02-21
申请号：PCT/US2007/076116
申请日：2007-08-16
申请人： WELLSTAT THERAPEUTICS CORPORATION , WOLPE, Stephen, D. , ARUDCHANDRAN, Ramachandran , VON BORSTEL, Reid, W.
发明人： WOLPE, Stephen, D. , ARUDCHANDRAN, Ramachandran , VON BORSTEL, Reid, W.
IPC分类号： A01N37/10 , A61K31/19
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 compound selected from an incretin mimetic and a dipeptidyl peptidase IV inhibitor in combination with a Compound of Formula,I or a pharmaceutically acceptable salt thereof, Formula (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, perfluoromethyl, 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.

40. 发明申请

WO2008022267A2 COMBINATION TREATMENT FOR METABOLIC DISORDERS 审中-公开
标题翻译：代谢病的组合治疗
公开(公告)号：WO2008022267A2
公开(公告)日：2008-02-21
申请号：PCT/US2007076116
申请日：2007-08-16
申请人： WELLSTAT THERAPEUTICS CORP , WOLPE STEPHEN D , ARUDCHANDRAN RAMACHANDRAN , VON BORSTEL REID W
发明人： WOLPE STEPHEN D , ARUDCHANDRAN RAMACHANDRAN , VON BORSTEL REID W
IPC分类号： A61K31/5377
CPC分类号： A61K38/22 , A61K31/192 , A61K31/5377
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 compound selected from an incretin mimetic and a dipeptidyl peptidase IV inhibitor in combination with a Compound of Formula,I or a pharmaceutically acceptable salt thereof, Formula (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, perfluoromethyl, 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.
摘要翻译：诸如胰岛素抵抗综合征，糖尿病，多囊卵巢综合征，高脂血症，脂肪肝病，恶病质，肥胖症，动脉粥样硬化和动脉硬化的各种代谢病症可用选自肠降血糖素模拟物和二肽基肽酶IV抑制剂的化合物与式I化合物或其药学上可接受的盐，式（I）R 1，R 2，R 3，R 3，R 3，其中R 4和R 5是氢并且其余部分独立地选自氢，卤素，羟基，甲基，乙基，全氟甲基，甲氧基，乙氧基和全氟甲氧基; 并且m是0,2或4. R6是氢，O或羟基，并且X是-OR7，其中R7是氢或具有1至3个碳原子的烷基; 或R 6是氢，并且X是-NR 8 R 9，其中R 8是氢或羟基并且R 9是氢，甲基或乙基。当X为-NR 8 R 9，羟基时，R 1，R 2，R 3，R 4， 3，R 4和R 5是羟基。

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