专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2009134995A2 TETRAZOLE COMPOUNDS FOR REDUCING URIC ACID 审中-公开
标题翻译：降低尿酸的四唑类化合物
公开(公告)号：WO2009134995A2
公开(公告)日：2009-11-05
申请号：PCT/US2009042298
申请日：2009-04-30
申请人： WELLSTAT THERAPEUTICS CORP , O'NEIL JAMES DENNEN , SHARMA SHALINI , ARUDCHANDRAN RAMACHANDRAN
发明人： O'NEIL JAMES DENNEN , SHARMA SHALINI , ARUDCHANDRAN RAMACHANDRAN
IPC分类号： A61K31/41
CPC分类号： C07D257/04 , A61K31/41 , A61K45/06
摘要： Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I. The uric acid-lowering effects of the compounds of this invention 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, cognitive impairment, early-onset essential hypertension, and Plasmodium falciparum-induced inflammation. In Formula 1, x is 1 or 2: y is O, 1, 2 or 3; and R1 is selected from the group consisting of hydrogen, alkyl having 1 or 2 carbon atoms, hydroxy, alkoxy having 1 or 2 carbon atoms, fluoro. chloro, bromo, and amino. A is phenyl unsubstituted or substituted by one, two or three groups selected from the group consisting of 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 atoms wherein the cycloalky! is unsubstituted or one one two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heleraromatic 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 by a ring carbon.
摘要翻译：通过施用式I化合物，哺乳动物受试者中的尿酸减少并且尿酸排泄增加。本发明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通常诊断为高尿酸血症，肾功能障碍，肾结石，心血管疾病，发展心血管疾病的风险，肿瘤溶解综合征，认知障碍，早发性原发性高血压和恶性疟原虫（Plasmodium falciparum- 诱导炎症。在式1中，x是1或2：y是0,1,2或3; 并且R 1选自氢，具有1或2个碳原子的烷基，羟基，具有1或2个碳原子的烷氧基，氟。氯，溴和氨基。 A是未被取代或被一个，两个或三个选自卤素，具有1或2个碳原子的烷基的基团取代的苯基。具有1或2个碳原子的全氟甲基烷氧基和全氟甲氧基; 或具有3至6个环原子的环烷基，其中环烷基是未取代的或者一个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，并且杂芳环通过环碳共价结合到化合物的其余部分。

2. 发明申请

WO2009151695A4 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：WO2009151695A4
公开(公告)日：2010-03-04
申请号：PCT/US2009037128
申请日：2009-03-13
申请人： WELLSTAT THERAPEUTICS CORP , 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. R6 is hydrogen, methyl or ethyl and R12 is hydrogen or methyl, or R6 is hydroxy and R12 is hydrogen, or R6 is O and R12 is absent, or R6 and R12 together are -CH2CH2-. R7 is hydrogen or alkyl having from 1 to 3 carbon atoms. One of R8 and R9 is alkyl having from 1 to 3 carbon atoms, and the other is hydrogen or alkyl having from 1 to 3 carbon atoms. R10 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(R11) wherein R11 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。

3. 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。

4. 发明申请

WO2009134995A3 TETRAZOLE COMPOUNDS FOR REDUCING URIC ACID 审中-公开
公开(公告)号：WO2009134995A3
公开(公告)日：2009-11-05
申请号：PCT/US2009/042298
申请日：2009-04-30
申请人： WELLSTAT THERAPEUTICS CORPORATION , O'NEIL, James, Dennen , SHARMA, Shalini , ARUDCHANDRAN, Ramachandran
发明人： O'NEIL, James, Dennen , SHARMA, Shalini , ARUDCHANDRAN, Ramachandran
IPC分类号： A61K31/41 , A01N43/64
摘要： Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I. The uric acid-lowering effects of the compounds of this invention 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, cognitive impairment, early-onset essential hypertension, and Plasmodium falciparum -induced inflammation. In Formula 1, x is 1 or 2: y is O, 1, 2 or 3; and R 1 is selected from the group consisting of hydrogen, alkyl having 1 or 2 carbon atoms, hydroxy, alkoxy having 1 or 2 carbon atoms, fluoro. chloro, bromo, and amino. A is phenyl unsubstituted or substituted by one, two or three groups selected from the group consisting of 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 atoms wherein the cycloalky! is unsubstituted or one one two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heleraromatic 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 by a ring carbon.

5. 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.

6. 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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式