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1. 发明申请

WO2018053036A1 METHOD OF REDUCING THYROID-ASSOCIATED SIDE EFFECTS 审中-公开
标题翻译：减少甲状腺相关副作用的方法
公开(公告)号：WO2018053036A1
公开(公告)日：2018-03-22
申请号：PCT/US2017/051410
申请日：2017-09-13
申请人： VIKING THERAPEUTICS, INC. , METABASIS THERAPEUTICS, INC.
发明人： LIAN, Brian , MASAMUNE, Hiroko , ERION, Mark , ITO, Bruce
IPC分类号： A61K31/662 , A61K31/665 , A61P5/14 , A61P3/06 , A61P3/04 , A61P1/16
摘要： The present disclosure is directed to methods of administration of thyroid hormone receptor agonists. The disclosure provides methods wherein the activity of the given thyroid receptor agonists in ameliorating or curing obesity, hyperlipidemia, hypercholesterolemia, diabetes, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, atherosclerosis, cardiovascular disease, hypothyroidism, and related disorders is maintained, while thyroid- related and thyroid axis-related side effects are reduced or eliminated.
摘要翻译：本公开涉及甲状腺激素受体激动剂的施用方法。本公开内容提供了方法，其中给定的甲状腺受体激动剂在改善或治疗肥胖症，高脂血症，高胆固醇血症，糖尿病，非酒精性脂肪肝病，非酒精性脂肪性肝炎，动脉粥样硬化，心血管疾病，甲状腺机能减退症和相关病症中的活性得以维持，而甲状腺相关的和甲状腺轴相关的副作用减少或消除。

2. 发明申请

WO2011038207A1 PHOSPHORUS-CONTAINING THYROID HORMONE RECEPTOR AGONISTS AND METHODS OF USE 审中-公开
标题翻译：含磷酸的甲状腺激素受体激动剂及其使用方法
公开(公告)号：WO2011038207A1
公开(公告)日：2011-03-31
申请号：PCT/US2010/050169
申请日：2010-09-24
申请人： METABASIS THERAPEUTICS, INC. , BOYER, Serge H. , ERION, Mark D. , ITO, Bruce , JACINTHO, Jason
发明人： BOYER, Serge H. , ERION, Mark D. , ITO, Bruce , JACINTHO, Jason
IPC分类号： A61K31/662 , C07F9/30 , A61P5/14
CPC分类号： C07F9/306 , A61K31/662 , C07F9/4006 , C07F9/4056 , C07F9/4075
摘要： The present invention relates to sulfonic acid containing compounds that bind to thyroid receptors in the liver. Activation of these receptors results in modulation of gene expression of genes regulated by thyroid hormones. The compounds can be used to treat diseases and disorders including metabolic diseases such as NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, and metabolic syndrome X.
摘要翻译：本发明涉及与肝中的甲状腺受体结合的含磺酸化合物。这些受体的活化导致调节由甲状腺激素调节的基因的基因表达。该化合物可用于治疗疾病和病症，包括诸如NASH，高胆固醇血症和高脂血症的代谢疾病，以及相关病症如动脉粥样硬化，冠心病，糖耐量异常和代谢综合征X.

3. 发明申请

WO2010047982A1 NOVEL CYCLIC BENZIMIDAZOLE DERIVATIVES USEFUL ANTI-DIABETIC AGENTS 审中-公开
标题翻译：新型循环苯并咪唑衍生物有用的抗糖尿病药
公开(公告)号：WO2010047982A1
公开(公告)日：2010-04-29
申请号：PCT/US2009/060304
申请日：2009-10-12
申请人： MERCK SHARP & DOHME CORP. , METABASIS THERAPEUTICS, INC. , BOOKSER, Brett, C. , DANG, Qun , GIBSON, Tony, S. , JIANG, Hongjian , CHUNG, De Michael , BAO, Jianming , JIANG, Jinlong , KASSICK, Andy , KEKEC, Ahmet , LAN, Ping , LU, Huagang , MAKARA, Gergely, M. , ROMERO, F., Anthony , SEBHAT, Iyassu , WILSON, David , WODKA, Dariusz
发明人： BOOKSER, Brett, C. , DANG, Qun , GIBSON, Tony, S. , JIANG, Hongjian , CHUNG, De Michael , BAO, Jianming , JIANG, Jinlong , KASSICK, Andy , KEKEC, Ahmet , LAN, Ping , LU, Huagang , MAKARA, Gergely, M. , ROMERO, F., Anthony , SEBHAT, Iyassu , WILSON, David , WODKA, Dariusz
IPC分类号： A01N43/50 , A61K31/415 , C07D243/08
CPC分类号： C07F9/65068 , C07F9/65583 , C07F9/657181
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, Metabolic Syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译：结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制AMPK活化蛋白激酶介导的疾病。本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖，高胆固醇血症和高血压。

4. 发明申请

WO2007081755A3 INDOLE-BENZIMIDAZOLE AND INDAZOLE INHIBITORS OF TYROSINE PHOSPHATASES 审中-公开
标题翻译：吡啶并吡唑并吲哚啉酮抑制剂
公开(公告)号：WO2007081755A3
公开(公告)日：2007-11-01
申请号：PCT/US2007000198
申请日：2007-01-08
申请人： METABASIS THERAPEUTICS INC , RIDEOUT DARRYL , YALAMOORI VENKATACHALAPATHI V , TSAI CHUNG Y , CHERUVALLATH ZACHARIA S , RAJAPPAN VASANTHAKUMAR , SEMPLE JOSEPH E
发明人： RIDEOUT DARRYL , YALAMOORI VENKATACHALAPATHI V , TSAI CHUNG Y , CHERUVALLATH ZACHARIA S , RAJAPPAN VASANTHAKUMAR , SEMPLE JOSEPH E
IPC分类号： C07F9/38 , A61K31/66 , A61P3/10 , C07F9/40 , C07F9/572 , C07F9/576 , C07F9/6503 , C07F9/6506
CPC分类号： C07F9/5728 , C07F9/65038 , C07F9/65068 , C07F9/65583 , C07F9/65586 , C07F9/6561 , C07F9/657181
摘要： Compounds and compositions are provided for; modulating the activityj of protein tyrosine phosphatases. In one embodiment, the compounds and compositions inhibit the activity of protein tyrosine phosphatase IB.
摘要翻译：提供化合物和组合物; 调节蛋白酪氨酸磷酸酶的活性。在一个实施方案中，化合物和组合物抑制蛋白酪氨酸磷酸酶IB的活性。

5. 发明申请

WO2006128055A3 NOVEL PHOSPHORUS-CONTAINING THYROMIMETICS 审中-公开
标题翻译：新型含磷的THYROMIMETICS
公开(公告)号：WO2006128055A3
公开(公告)日：2007-05-24
申请号：PCT/US2006020607
申请日：2006-05-26
申请人： METABASIS THERAPEUTICS INC , ERION MARK D , JIANG HONGJIAN , BOYER SERGE H
发明人： ERION MARK D , JIANG HONGJIAN , BOYER SERGE H
IPC分类号： C07F9/02 , C07F9/30 , C07F9/38 , C07F9/40 , C07F9/44 , C07F9/572 , C07F9/58 , C07F9/6571
CPC分类号： C07F9/65517 , C07F9/3211 , C07F9/36 , C07F9/3808 , C07F9/3882 , C07F9/4006 , C07F9/4056 , C07F9/4075 , C07F9/4407 , C07F9/4426 , C07F9/4465 , C07F9/657181
摘要： The present invention relates to compounds of phosphonic acid-containing T3 mimetics and monoesters thereof, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome x and diabetes.
摘要翻译：本发明涉及含膦酸的T3模拟物及其单酯的化合物，其立体异构体，药学上可接受的盐，共晶体和前体药物以及前体药学上可接受的盐和共晶体，以及它们的制备和用途预防和/或治疗诸如肥胖，NASH，高胆固醇血症和高脂血症等代谢疾病，以及相关病症如动脉粥样硬化，冠心病，葡萄糖耐量异常，代谢综合症x和糖尿病。

6. 发明申请

WO2007022073A2 NOVEL 2'-C-METHYL AND 4'-C-METHYL NUCLEOSIDE DERIVATIVES 审中-公开
标题翻译：新的2'-C-甲基和4'-C-甲基核苷衍生物
公开(公告)号：WO2007022073A2
公开(公告)日：2007-02-22
申请号：PCT/US2006/031614
申请日：2006-08-14
申请人： MERCK & CO., INC. , METABASIS THERAPEUTICS, INC. , ERION, Mark, D. , REDDY, K., Raja , MACCOSS, Malcolm , OLSEN, David, B.
发明人： ERION, Mark, D. , REDDY, K., Raja , MACCOSS, Malcolm , OLSEN, David, B.
IPC分类号： A61K31/7072
CPC分类号： C07H19/10
摘要： Novel 2'-C-methyl nucleoside 5 '-monophosphate and 4'-C-methyl nucleoside 5'- monophosphate derivatives, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of hepatitis C viral infection are described.
摘要翻译：新型2'-C-甲基核苷5'-单磷酸酯和4'-C-甲基核苷5'-单磷酸衍生物，立体异构体及其药学上可接受的盐或前药，其制备及其用于治疗丙型肝炎病毒感染的用途被描述。

7. 发明申请

WO2005123729A1 LEWIS ACID MEDIATED SYNTHESIS OF CYCLIC ESTERS 审中-公开
标题翻译： LEWIS酸介导的循环系统的合成
公开(公告)号：WO2005123729A1
公开(公告)日：2005-12-29
申请号：PCT/US2005/019440
申请日：2005-06-03
申请人： METABASIS THERAPEUTICS, INC. , MARTIN, Kevin
发明人： MARTIN, Kevin
IPC分类号： C07D471/02
CPC分类号： C07F9/657181
摘要： Methods for the synthesis of cyclic phosphonic acid diesters from 1,3-diols are described, whereby cyclic phosphonic acid diesters are produced by reacting a chiral 1,3-diol and an activated phosphonic acid in the presence of a Lewis acid.
摘要翻译：描述了从1,3-二醇合成环状膦酸二酯的方法，由此在路易斯酸存在下使手性1,3-二醇和活化的膦酸反应来制备环状膦酸二酯。

8. 发明申请

WO0203978A3 A COMBINATION OF FBPase INHIBITORS AND ANTIDIABETIC AGENTS USEFUL FOR THE TREATMENT OF DIABETES 审中-公开
标题翻译： FBPase抑制剂和用于治疗糖尿病的抗糖尿病药物的组合
公开(公告)号：WO0203978A3
公开(公告)日：2003-10-16
申请号：PCT/US0121557
申请日：2001-07-05
申请人： METABASIS THERAPEUTICS INC , SANKYO CO , VAN POELJE PAUL D , ERION MARK D , FUJIWARA TOSHIHIKO
发明人： VAN POELJE PAUL D , ERION MARK D , FUJIWARA TOSHIHIKO
IPC分类号： A61K31/426 , A61K31/64 , A61K31/675 , A61K45/06 , A61P3/04 , A61P3/10 , A61P5/00 , A61P5/50 , A61P43/00 , A61K31/52
CPC分类号： A61K31/426 , A61K45/06
摘要： A combination therapy of at least one FBPase inhibitor and at least one other antidiabetic agent is disclosed.
摘要翻译：公开了至少一种FBPase抑制剂和至少一种其它抗糖尿病药物的组合疗法。

9. 发明申请

WO9945016A9 NOVEL PRODRUGS FOR PHOSPHORUS-CONTAINING COMPOUNDS 审中-公开
标题翻译：含磷化合物的新产品
公开(公告)号：WO9945016A9
公开(公告)日：2000-03-02
申请号：PCT/US9904908
申请日：1999-03-05
申请人： METABASIS THERAPEUTICS INC
发明人： ERION MARK D , REDDY K RAJA , ROBINSON EDWARD D
IPC分类号： C07H19/213 , A61K31/665 , A61K31/675 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K49/00 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P31/12 , A61P33/00 , A61P35/00 , A61P43/00 , C07F9/6571 , C07F9/6574 , C07H19/10 , C07H19/11 , C07H19/20 , C07H19/207 , C07H19/00
CPC分类号： C07H19/10 , C07F9/657154 , C07F9/657181 , C07F9/65742 , C07F9/65744 , C07H19/20 , C07H19/207
摘要： Prodrugs of formula (I), their uses, their intermediates, and their method of manufacture are described, wherein V is selected from the group consisting of -H, aralkyl, alicyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, 1-alkenyl, 1-alkynyl, and -R ; or together V and Z are connected via 3-5 atoms to form a cyclic group, optionally containing 1 heteroatom, substituted with hydroxy, acyloxy, alkoxycarbonyloxy, or aryloxycarbonyloxy attached to a carbon atom that is three atoms from an oxygen attached to the phosphorus; or together V and Z are connected via 3-5 atoms to form a cyclic group, optionally containing 1 heteroatom, that is fused to an aryl group at the beta and gamma position to the oxygen attached to the phosphorus; or together V and W are connected via 3 carbon atoms to form an optionally substituted cyclic group containing 6 carbon atoms and substituted with one substituent selected from the group consisting of hydroxy, acyloxy, alkoxycarbonyloxy, alkylthiocarbonyloxy, and aryloxycarbonyloxy, attached to a carbon atom that is three atoms from an oxygen attached to the phosphorus; W and W' are independently selected from the group consisting of -H, alkyl, aralkyl, alicyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, 1-alkenyl, 1-alkynyl, and -R ; Z is selected from the group consisting of -CHR OH, -CHR OC(O)R , -CHR OC(S)R , -CHR OC(S)OR , -CHR OC(O)SR , -CHR OCO2R , -OR , -SR , -CHR N3, -CH2aryl, -CH(aryl)OH, -CH(CH=CR 2)OH, -CH(CCR )OH, -R , -NR 2, -OCOR , -OCO2R , -SCOR , -SCO2R , -NHCOR , -NHCO2R , -CH2NHaryl, -(CH2)p-OR , and -(CH2)p-SR ; R is an R or -H; R is selected from the group consisting of alkyl, aryl, aralkyl, and alicyclic; and R is selected from the group consisting of alkyl, aralkyl, and alicyclic; p is an integer from 2 to 3; with the provisos that a) V, Z, W, and W' are not all -H; and b) when z is -R , then at least one of V and W is not -H, or -R ; and M is selected from the group that attached to PO3 , P2O6 , or P3O9 is biologically active in vivo, and that is attached to the phosphorus in formula (I) via a carbon, oxygen, or nitrogen atom; and pharmaceutically acceptable prodrugs and salts thereof.
摘要翻译：描述了式（I）的前药，其用途，其中间体及其制备方法，其中V选自-H，芳烷基，脂环族，芳基，取代的芳基，杂芳基，取代的杂芳基，1-烯基，1-炔基和-R 9; 或一起V和Z通过3-5个原子连接形成环状基团，任选地含有1个被连接到磷上的氧原子连接到三个原子上的羟基，酰氧基，烷氧基羰基氧基或芳氧基羰基氧基的杂原子; 或一起V和Z通过3-5个原子连接以形成任选地含有1个杂原子的环状基团，其在β和γ位置处的芳基与连接到磷的氧融合; 或者一起V和W通过3个碳原子连接形成任选取代的含有6个碳原子的环状基团，并被一个选自羟基，酰氧基，烷氧基羰基氧基，烷硫基羰基氧基和芳氧基羰基氧基的一个取代基取代，是从附着于磷的氧的三个原子; W和W'独立地选自-H，烷基，芳烷基，脂环族，芳基，取代的芳基，杂芳基，取代的杂芳基，1-烯基，1-炔基和-R 9。 Z选自-CHR 2 OH，-CHR 2 OC（O）R 3，-CHR 2 OC（S）R 3，-CHR 2 OC（ S）OR 3，-CHR 2 OC（O）SR 3，-CHR 2 OCO 2 R 3，-OR 2，-SR 2，-CHR 2 N 3， -CH 2芳基，-CH（芳基）OH，-CH（CH = CR 2）OH，-CH（CCR 2）OH，-R 2，-NR 2，-OCOR 3 ，-OCO 2 R 3，-SCOR 3，-SCO 2 R 3，-NHCOR 2，-NHCO 2 R 3，-CH 2 NH芳基， - （CH 2）p -OR 2和 - （CH 2 ）对 - SR <2>; R 2是R 3或-H; R 3选自烷基，芳基，芳烷基和脂环族; 并且R 9选自烷基，芳烷基和脂环族; p是2至3的整数; 条件是a）V，Z，W和W'不全为-H; 和b）当z是-R 2时，V和W中的至少一个不是-H或-R 9; 并且M选自附着于PO 3 2-，P 2 O 6 3-或P3O 9 4-的基团在体内具有生物活性，并且通过碳与式（I）中的磷连接，氧或氮原子; 及其药学上可接受的前药及其盐。

10. 发明申请

WO2009073506A2 NUCLEOSIDE PRODRUGS AND USES THEREOF 审中-公开
标题翻译：核苷酸原料及其用途
公开(公告)号：WO2009073506A2
公开(公告)日：2009-06-11
申请号：PCT/US2008/084828
申请日：2008-11-26
申请人： METABASIS THERAPEUTICS INC. , HECKER, Scott J. , REDDY, K. Raja
发明人： HECKER, Scott J. , REDDY, K. Raja
CPC分类号： C07H19/10
摘要： This application provides compositions or compounds as disclosed herein that are suitable for treating hepatic viral diseases, such as hepatitis C (HCV).
摘要翻译：本申请提供了本文公开的适用于治疗肝病毒疾病如丙型肝炎（HCV）的组合物或化合物。

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