CAS: 207844-01-7; Calcium (S)-2-Benzyl-4-((3Ar,7As)-Octahydro-2H-Isoindol-2-yl)-4-Oxobutanoate Dihydrate

该化合物是一种主要用于管理2型糖尿病的口服低血糖剂,它是一种快速作用的胰岛素秘密室,刺激胰岛素在进餐后从胰岛素中释放出来,从而有助于控制脊髓外血糖水平;二氢酸钙的化学结构特征是一种独特的苯化酸衍生物,有助于其药理活动;作为钙盐,二氢化物形式表明每种钙离子中存在两种水分子,可影响其溶解性和稳定性;三氟化硫的特征是,其半衰期相对较短,需要每天多剂量来保持血糖控制;一般情况下,它具有良好的副作用,但可能包括低血糖和胃肠紊乱;该化合物的施用通常与饮食改变和锻炼以优化血糖管理相结合.与任何药物一样,它对于病人为个人治疗计划及任何不利反应的保健专业人员来说,对于任何有害治疗计划和监测至关重要.

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    专利信息


    专利号:US-6667406-B1
    优先权日:1999-03-10
    标题 :Methods for the synthesis of complex reduced isoindole, isooxyindole and isooxyquinoline libraries
    发明人:SUN SENGEN; MURRAY WILLIAM V
    权利人:ORTHO MCNEIL PHARM INC
    摘要:Disclosed are methods of synthesizing libraries of diverse complex hexahydroisoindole, hexahydroisooxyindole and octahydroisooxyquinoline compounds through the use of a facile intramolecular Diels Alder reaction. The invention is further directed to methods for synthesizing the libraries on solid supports. The invention is further directed to methods for identifying and isolating such hexahydroisoindole, hexahydroisooxyindole and octahydroisooxyquinoline compounds with useful and diverse activities from such libraries.

    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, C1-12 alkyl or C1-12 haloalkyl; and R3 is C3-6 cycloalkyl, C1-12 alkyl, C1-12 haloalkyl, C3-6 cycloalkyl-C1-4-alkylene, aryl-C1-4-alkylene or heteroaryl-C1-4-alkylene, wherein said aryl-C1-4-alkylene and heteroaryl-C1-4-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.
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    主要参考文献


    1: Son JW, Lee IK, Woo JT, Baik SH, Jang HC, Lee KW, Cha BS, Sung YA, Park TS, Yoo SJ, Yoon KH. A prospective, randomized, multicenter trial comparing the efficacy and safety of the concurrent use of long-acting insulin with mitiglinide or voglibose in patients with type 2 diabetes. Endocr J. 2015;62(12):1049-57. doi: 10.1507/endocrj.EJ15-0325. Epub 2015 Sep 25. doi: 10.1136/bmjdrc-2015-000122. eCollection 2015.
    3: Al Azzam KM, Muhammad E. Host-guest Inclusion Complexes between Mitiglinide and the Naturally Occurring Cyclodextrins α, β, and γ: A Theoretical Approach. Adv Pharm Bull. 2015 Jun;5(2):289-91. doi: 10.15171/apb.2015.040. Epub 2015 Jun 1.
    4: Tani S, Nagao K, Hirayama A. Differences between Mitiglinide/Voglibose Fixed-dose Combination and Glimepiride in Modifying Low-density Lipoprotein Heterogeneity in Japanese Type-2 Diabetic Patients: A Pilot Study. Drug Res (Stuttg). 2016 Feb;66(2):94-9. doi: 10.1055/s-0035-1549993. Epub 2015 May 26. doi: 10.1517/14656566.2015.1035646. Epub 2015 Apr 16. doi: 10.1620/tjem.235.255. doi: 10.1517/14656566.2014.970531. Epub 2014 Oct 20. doi: 10.1055/s-0034-1387719. Epub 2014 Sep 4. doi: 10.1517/14656566.2014.939070. Epub 2014 Jul 21. doi: 10.1517/14656566.2014.920323. Epub 2014 May 27. Erratum in: Expert Opin Pharmacother. 2014 Aug;15(11):1637. doi: 10.1016/j.bmc.2014.04.059. Epub 2014 May 6. doi: 10.1186/1758-5996-6-48. eCollection 2014.

    合成参考文献


    参考文献:10.1385/endo:29:2:309
    摘要:Mori Y, Ojima K, Fuujimori Y, Fujimori Y, Aoyagi I, Kusama H, Yamazaki Y, Kojima M, Kojima S, Shibata N, Itoh Y, Tajima N. Effects of mitiglinide on glucose-induced insulin release into the portal vein and fat-induced triglyceride elevation in prediabetic and diabetic OLETF rats. Endocrine. 2006 Apr;29(2):309–15. doi: 10.1385/endo:29:2:309.
    参考文献:10.1007/s12272-015-0621-8
    摘要:Tahara A, Takasu T, Yokono M, Imamura M, Kurosaki E. Effects of the combination of SGLT2 selective inhibitor ipragliflozin and various antidiabetic drugs in type 2 diabetic mice. Archives of Pharmacal Research. 2015 Oct 08;39(2):259–70. doi: 10.1007/s12272-015-0621-8.
    参考文献:10.1007/s40261-015-0348-9
    摘要:Scott LJ. Teneligliptin: a review in type 2 diabetes. Clin Drug Investig. 2015 Nov;35(11):765–72. doi: 10.1007/s40261-015-0348-9.
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