CAS: 110703-94-1; 2-(4-Oxo-3-((5-(Trifluoromethyl)Benzo[d]Thiazol-2-yl)Methyl)-3,4-Dihydrophthalazin-1-yl)Acetic Acid

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Ethyl 3,4-Dihydro-4-Oxo-3-<<5-(Trifluoromethyl)-2-Benzothiazolyl>Methyl>-1-Phthalazineacetate 110722-28-6

📜Ethyl 3,4-Dihydro-4-Oxo-3-<<5-(Trifluoromethyl)-2-Benzothiazolyl>Methyl>-1-Phthalazineacetate 反应生成唑泊司他
参考文献:Heterocyclic Oxophthalazinyl Acetic Acids
标题:Heterocyclic Oxophthalazinyl Acetic Acids
摘要:一种具有醛还酶抑制活性的杂环氧酞嗪基乙酸,其化学式为##str1##其中x为氧或硫;Z为共价键,O,S,Nh或ch.Sub.2或chr.Sub.5,Z为乙烯基;R.Sub.1为羟基,或前药基;R.Sub.2为杂环基,R.Sub.3和r.Sub.4为氢或相同或不同的取代基,R.Sub.5为氢,甲基或三氟甲基.其中r.Sub.1为二(c.Sub.1-C.Sub.4)烷基氨基或(c.Sub.1-C.Sub.4)烷氧基被n-吗啡基或二(c.Sub.1-C.Sub.4)烷基氨基取代的上述化合物的药学上可接受的酸盐,以及其中r.Sub.1为羟基的上述化合物的药学活性碱盐也是醛还酶抑制剂.

专利信息

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-9315483-B2
优先权日:2007-09-13
标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
发明人：JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
权利人:CONCERT PHARMACEUTICALS INC
摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

专利号:US-2005004225-A1
优先权日:2003-04-16
标题:Oxidoreductase inhibitors and methods of screening and using thereof
发明人：BALENDIRAN GANESARATNAM K
摘要:The present invention relates to 1) the design and synthesis of analogs to glutathione conjugates which bind to or interact with aldose reductase (AR) through unique conformations that are distinctly different from the substrates and inhibitors of AR which are members of sugar metabolism; 2) the screening of the analogs to identify those that interact with or inhibit or enhance the activity of AR; and 3) the use of AR ligands, AR inhibitors (AR antagonsits) or AR enhancer (AR agonists) in the detection of AR activity, the modulation of AR activity, and the treatment of conditions in a subject in need of modulating AR activity. Such conditions include but not limited to cardiovascular disease, diabetes, artheriosclerosis, cancer, neoplasm, obesity, cataract, retinopathy, keratopathy, nephropathy, neurosis, thrombosis, faulty union of corneal injury and neuropathy. Examples of the treatment include the use of fibrates as AR inhibitors to treat these conditions.

专利号:US-2018370905-A1
优先权日:2013-04-05
标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same

专利号:EP-1551403-B1
优先权日:2002-10-10
标 题 :5-substituted 2h-pyrazone-3-carboxylic acid derivatives as antilipolytic agents for the treatment of metabolic-related disorders such as dyslipidemia
发明人：SEMPLE GRAEME; AVERBUJ CLAUDIA; SKINNER PHILIP; GHARBAOUI TAWFIK; SHIN YOUNG-JUN
权利人:ARENA PHARM INC
摘要:The present invention relates to certain pyrazole carboxylic acid derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, as antilipolytic agents and against for the receptor RUP25, wherein: R₂ is H, halogen, C_1-12 alkyl or C_1-12 haloalkyl; and R₃ is C_3-6 cycloalkyl, C_1-12 alkyl, C_1-12 haloalkyl, C_3-6 cycloalkyl-C_1-4-alkylene, aryl-C_1-4-alkylene or heteroaryl-C_1-4-alkylene, wherein said aryl-C_1-4-alkylene and heteroaryl-C_1-4-alkylene can be optionally substituted 1 to 5 substituents selected from the substituents listed in the claims. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for pharmaceutical compositions in combination with other active agents, for example, those agents belonging to the class of alpha-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, thiazolidinedione and the like.

专利号:US-2006122240-A1
优先权日:2002-11-05
标题 :Benzotriazoles and methods of prophylaxis or treatment of metabolic-related disorders thereof
发明人：SEMPLE GRAEME; SKINNER PHILIP J; CHERRIER MARTIN C; WEBB PETER; TAMURA SUSAN Y
权利人:ARENA PHARM INC
摘要:The present invention relates to certain benzotriazole carboxylic acid or ester derivatives of Formula (I), pharmaceutically acceptable salts and solvates thereof, which exhibit useful pharmaceutical properties, for example, as agonists for the GPCR referred to as hRUP38. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the prophylaxis or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of -glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.