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-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-2016107992-A1 优先权日:2013-06-20 标 题:Intermediates useful for the preparation of saxagliptin 发明人:CASTALDI GRAZIANO; PALLANZA GIUSEPPE; GABOARDI MAURO; CASTALDI MARTA 权利人:CHEMELECTIVA S R L 摘要:Intermediates useful for the synthesis of saxagliptin and their preparationare described.
专利号:WO-2014118612-A1 优先权日:2013-01-30 标 题:Process for the preparation of intermediates of synthesis of saxagliptin and novel compounds 发明人:BERTOLINI GIORGIO; SADA MARA; MAIORANA STEFANO; BIANCHI ALDO; TIMPANO GABRIELE 权利人:LABORATORIO CHIMICO INT SPA 摘要:The object of the present invention is the preparation of saxagliptin and novel intermediate compounds.
专利号:US-2012282255-A1 优先权日:2011-04-07 标题 :Methods and compositions for the treatment of alcoholism and alcohol dependence 发明人:PLUCINSKI GREG 权利人:PLUCINSKI GREG 摘要:The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated. Accordingly, the methods and compositions of the invention are useful for preventing, treating, diagnosing, or monitoring the progression various alcohol and drug dependency diseases disclosed herein.
1: Elmorsy EA, Youssef ME, Abdel-Hamed MR, Amer MM, Elghandour SR, Alkhamiss AS, Mohamed NB, Khodeir MM, Elsisi HA, Alsaeed TS, Kamal MM, Ellethy AT, Elesawy BH, Saber S. Activation of AMPK/SIRT1/FOXO3a signaling by BMS-477118 (saxagliptin) mitigates chronic colitis in rats: uncovering new anti-inflammatory and antifibrotic roles. Front Pharmacol. 2024 Sep 18;15:1456058. doi: 10.3389/fphar.2024.1456058. 2: Pham Nguyen TP, Leonard CE, Brensinger CM, Bilker WB, Chung SP, Horn JR, Bogar K, Miano TA, Hennessy S. Concomitant Use of Oral Anticoagulants with Oral Dipeptidyl Peptidase-4 Inhibitors and Serious Bleeding Events. Clin Pharmacol Ther. 2024 Sep 11. doi: 10.1002/cpt.3442. Epub ahead of print. 16(16):11994-12007. doi: 10.18632/aging.206074. Epub 2024 Aug 22. 4: Wang T, Tao T, Liu Y, Dong J, Ni S, Liu Y, Li Y, Xu N, Sun Z. Pharmacokinetic/Pharmacodynamic modelling of Saxagliptin and its active metabolite, 5-hydroxy Saxagliptin in rats with Type 2 Diabetes Mellitus. BMC Pharmacol Toxicol. 2024 Jun 26;25(1):35. doi: 10.1186/s40360-024-00757-3.
合成参考文献
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749