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    • 2. 发明申请
    • COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
    • 用于治疗代谢性疾病的化合物
    • WO2007137008A3
    • 2008-08-28
    • PCT/US2007068745
    • 2007-05-11
    • WELLSTAT THERAPEUTICS CORPSHARMA SHALINIVON BORSTEL REID W
    • SHARMA SHALINIVON BORSTEL REID W
    • A61K31/19A61K31/34C07C229/00
    • C07D317/32C07C59/68
    • 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, compound of the formula (I): wherein n is 1 or 2; m is 0, 1, 2, 3, 4, 5, 6, 7 or 8; 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; R 3 and R 4 together are alkyl having two or three carbon atoms; or R 3 and R 4 are the same as each other and each is methyl or ethyl; R 5 is hydrogen or alkyl having from one to six 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 A is 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 is 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).
    • 公开了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,其中n为1 或2; m为0,1,2,3,4,5,6,7或8; 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; R 3和R 4一起是具有两个或三个碳原子的烷基; 或R 3和R 4彼此相同,各自为甲基或乙基; R 5是氢或具有1至6个碳原子的烷基。 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A是具有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A是具有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。
    • 3. 发明申请
    • COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
    • 用于治疗代谢性疾病的化合物
    • WO2007095462A3
    • 2008-05-02
    • PCT/US2007061908
    • 2007-02-09
    • WELLSTAT THERAPEUTICS CORPSHARMA SHALINIVON BORSTEL REID W
    • SHARMA SHALINIVON BORSTEL REID W
    • A61K31/055C07C39/21C07C39/27C07C59/01
    • C07C43/23
    • 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).
    • 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,其中所述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。
    • 4. 发明申请
    • COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
    • 用于治疗代谢性疾病的化合物
    • WO2007101060A3
    • 2007-12-13
    • PCT/US2007062574
    • 2007-02-22
    • WELLSTAT THERAPEUTICS CORPSHARMA SHALINIVON BORSTEL REID W
    • SHARMA SHALINIVON BORSTEL REID W
    • A01N31/14A61K31/075
    • C07D263/14
    • 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 and R is hydrogen or hydroxy and the other is hydrogen; or R 3 and R 4 together are =0. 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).
    • 公开了用于治疗各种代谢疾病的药剂,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症,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和R之一是氢或羟基,另一个是氢; 或者R 3和R 4一起是= 0。 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,所述药剂可以是式(I)化合物的药学上可接受的盐。
    • 5. 发明申请
    • COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
    • 用于治疗代谢性疾病的化合物
    • WO2007087504A3
    • 2007-11-15
    • PCT/US2007060830
    • 2007-01-22
    • WELLSTAT THERAPEUTICS CORPSHARMA SHALINIVON BORSTEL REID W
    • SHARMA SHALINIVON BORSTEL REID W
    • A01N35/00A61K31/12
    • C07D307/33
    • 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).
    • 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; 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,该药剂可以是式(I)化合物的药学上可接受的盐。
    • 6. 发明申请
    • COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
    • 用于治疗代谢性疾病的化合物
    • WO2006127133A2
    • 2006-11-30
    • PCT/US2006/012050
    • 2006-03-31
    • WELLSTAT THERAPEUTICS CORPORATIONSHARMA, ShaliniVON BORSTEL, Reid, W.
    • SHARMA, ShaliniVON BORSTEL, Reid, W.
    • A61K31/165
    • C07C259/06C07C235/34
    • 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. wherein n is 1 or 2; m is 0, 1, 2, 3, 4 or 5; 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; R 3 is hydrogen or -(CH 2 ) g OH wherein g is 0, 1 or 2; R 4 is hydrogen, methyl or ethyl; 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; or a pharmaceutically acceptable salt of the compound.
    • 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。 其中n为1或2; m为0,1,2,3,4或5; 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; R 3是氢或 - (CH 2 CH 2)n OH其中g是0,1或2; R 4是氢,甲基或乙基; 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; 或该化合物的药学上可接受的盐。
    • 8. 发明申请
    • COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
    • 用于治疗代谢性疾病的化合物
    • WO2007137008A2
    • 2007-11-29
    • PCT/US2007/068745
    • 2007-05-11
    • WELLSTAT THERAPEUTICS CORPORATIONSHARMA, ShaliniVON BORSTEL, Reid, W.
    • SHARMA, ShaliniVON BORSTEL, Reid, W.
    • A61K31/195
    • C07D317/32C07C59/68
    • 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, compound of the formula (I): wherein n is 1 or 2; m is 0, 1, 2, 3, 4, 5, 6, 7 or 8; 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; R 3 and R 4 together are alkyl having two or three carbon atoms; or R 3 and R 4 are the same as each other and each is methyl or ethyl; R 5 is hydrogen or alkyl having from one to six 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 A is 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 is 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).
    • 公开了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,其中n为1 或2; m为0,1,2,3,4,5,6,7或8; 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; R 3和R 4一起是具有两个或三个碳原子的烷基; 或R 3和R 4彼此相同,各自为甲基或乙基; R 5是氢或具有1至6个碳原子的烷基。 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A是具有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A是具有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。
    • 10. 发明申请
    • COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
    • 用于治疗代谢性疾病的化合物
    • WO2007101060A2
    • 2007-09-07
    • PCT/US2007/062574
    • 2007-02-22
    • WELLSTAT THERAPEUTICS CORPORATIONSHARMA, ShaliniVON BORSTEL, Reid, W.
    • SHARMA, ShaliniVON BORSTEL, Reid, W.
    • C07D263/14
    • 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 and R is hydrogen or hydroxy and the other is hydrogen; or R 3 and R 4 together are =0. 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).
    • 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,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; R和R中的一个是氢或羟基,另一个是氢; 或R 3和R 4一起= 0。 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。