📜2-(5-甲基-2-苯基-1,3-恶唑-4-基)-1-乙醇置于lithium Hydroxide,Sodium Tetrahydroborate,4 A Molecular Sieve,Magnesium Sulfate,Potassium Carbonate,三乙胺体系中,用 四氢呋喃,甲醇,二氯甲烷,乙腈 作为反应溶剂,化学反应 45.0H,反应生成 莫格列地 参考文献:Design And Synthesis Of N-[(4-Methoxyphenoxy)Carbonyl]-N-[[4-[2-(5-Methyl-2-Phenyl-4-Oxazolyl)Ethoxy]Phenyl]Methyl]Glycine [muraglitazar/bms-298585],A Novel Peroxisome Proliferator-Activated Receptor α/γ Dual Agonist With Efficacious Glucose And Lipid-Lowering Activities 标题:Design And Synthesis Of N-[(4-Methoxyphenoxy)Carbonyl]-N-[[4-[2-(5-Methyl-2-Phenyl-4-Oxazolyl)Ethoxy]Phenyl]Methyl]Glycine [muraglitazar/bms-298585],A Novel Peroxisome Proliferator-Activated Receptor α/γ Dual Agonist With Efficacious Glucose And Lipid-Lowering Activities 摘要:Muraglitazar/bms-298585 (2) Has Been Identified As A Non-Thiazolidinedione Ppar Alpha/gamma Dual Agonist That Shows Potent Activity In Vitro At Human Ppar Alpha (Ec50 = 320 Nm) And Ppar Gamma (Ec50 = 110 Nm). Compound 2 Shows Excellent Efficacy For Lowering Glucose,Insulin,Triglycerides,And Free Fatty Acids In Genetically Obese,Severely Diabetic Db/db Mice And Has A Favorable Adme Profile. Compound 2 Is Currently In Clinical Development For The Treatment Of Type 2 Diabetes And Dyslipidemia. DOI:10.1021/jm0496436
专利号:US-2009156465-A1 优先权日:2005-12-30 标题:Derivatives of beta-amino acid as dipeptidyl peptidase-iv inhibitors 发明人:SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND 权利人:SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND 摘要:The present invention relates to β-amino acid derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.
专利号:US-2008300251-A1 优先权日:2005-09-05 标 题 :Derivatives of 3-Azabicyclo[3.1.0] Hexane as Dipeptidyl Peptidase-IV Inhibitors 发明人:SATTIGERI JITENDRA A; ANDAPPAN MURUGAIAH M S; KISHORE KAUSHAL; SETHI SACHIN; KANDALKAR SACHIN RAMESH; PAL CHANCHAL KUMAR; MAHAJAN DIPAK C; AHMED SHAHADAT; PARKALE SANTHOSH SADASHIV; SRINIVASAN T; SHARMA LALIMA; BANSAL VINAY S; CHUGH ANITA; DAVIS JOSEPH ALEXANAND 权利人:SATTIGERI JITENDRA A; ANDAPPAN MURUGAIAH M S; KISHORE KAUSHAL; SETHI SACHIN; KANDALKAR SACHIN RAMESH; PAL CHANCHAL KUMAR; MAHAJAN DIPAK C; AHMED SHAHADAT; PARKALE SANTHOSH SADASHIV; SRINIVASAN T; SHARMA LALIMA; BANSAL VINAY S; CHUGH ANITA; DAVIS JOSEPH ALEXANAND 摘要:The present invention relates to novel 3-azabicyclo[3.1.0]hexane derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the said compounds. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.
专利号:US-2024400552-A1 优先权日:2016-11-11 标题 :Heterocyclic modulators of lipid synthesis 发明人:BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S 权利人:SAGIMET BIOSCIENCES INC 摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by dysregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).
专利号:US-11622968-B2 优先权日:2011-03-08 标 题:Heterocyclic modulators of lipid synthesis 发明人:BUCKLEY DOUGLAS; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S 权利人:SAGIMET BIOSCIENCES INC 摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).
专利号:US-2009118296-A1 优先权日:2005-07-20 标 题:Heteroaromatic Compounds As Inhibitors Of Stearoyl-Coenzyme A Delta-9 Desaturase 发明人:BLACK CAMERON; DESCHENES DENIS; GAGNON MARC; LACHANCE NICOLAS; LEBLANC YVES; LEGER SERGE; LI CHUN SING; OBALLA RENATA M 权利人:MERCK FROSST CANADA LTD 摘要:Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; lipid disorders; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and fatty liver disease.
专利号:US-2009318476-A1 优先权日:2006-08-09 标 题 :Azacycloalkane Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase 发明人:RAMTOHUL YEEMAM K 权利人:MERCK FROSST CANADA LTD 摘要:Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. Formula (I).
1: Coletta DK, Fernandez M, Cersosimo E, Gastaldelli A, Musi N, DeFronzo RA. The effect of muraglitazar on adiponectin signalling, mitochondrial function and fat oxidation genes in human skeletal muscle in vivo. Diabet Med. 2015 May;32(5):657-64. doi: 10.1111/dme.12664. Epub 2015 Jan 7. doi: 10.1186/ar4211. 3: Fernandez M, Gastaldelli A, Triplitt C, Hardies J, Casolaro A, Petz R, Tantiwong P, Musi N, Cersosimo E, Ferrannini E, DeFronzo RA. Metabolic effects of muraglitazar in type 2 diabetic subjects. Diabetes Obes Metab. 2011 Oct;13(10):893-902. doi: 10.1111/j.1463-1326.2011.01429.x.
合成参考文献
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