CAS: 166518-60-1; 2,6-Diisopropylphenyl (2-(2,4,6-Triisopropylphenyl)Acetyl)Sulfamate

该化合物是一种合成有机化合物,主要以其作为胆固醇低温剂的作用而闻名,其功能是抑制胆固醇乙酰转移酶(ACAT),该酶是胆固醇酯酶的酶,对脂质新陈代谢至关重要;Avasimibe抑制胆固醇,导致胆固醇吸收减少,促进从血液中清除胆固醇;该化合物的特点是其特定的分子结构,包括有助于其生物活动的功能组别的特殊安排;Avasimibe在管理超利皮贫血和甲状腺素病方面的潜在治疗应用已经进行了研究;此外,还在各种临床前科和临床研究中对其进行了评估,以评估其功效和安全状况;然而,其发展面临挑战,临床实践尚未广泛采用.

结构式图片

上下游产品

CAS号52629-47-7 2-[2,4,6-tri(pr... | CAS号92050-02-7 2,6-DIISOPROPYL... | CAS号57199-00-5 2,4,6-三异丙基苯甲酰氯 | CAS号4276-88-4 (2,4,6-TRIISOPR... | CAS号4276-85-1 2,4,6-三异丙基苯乙酸 | CAS号4276-84-0 2,4,6-triisopro... | CAS号166519-14-8 2-(Bromomethyl)...

合成工艺路线路线简述

    📜2-(溴甲基)-1,3,5-三异丙基苯置于草酰氯,Tea,硫酸体系中,用 四氢呋喃,二甲基亚砜 用作溶剂,化学反应生成阿伐麦布
    参考文献:酰基辅酶a的抑制剂:胆固醇o-酰基转移酶(acat)作为降血脂药.Ci-1011:在补充了非胆固醇饮食的动物中具有独特的降低胆固醇活性的酰基氨基磺酸酯.
    标题:酰基辅酶a的抑制剂:胆固醇o-酰基转移酶(acat)作为降血脂药.Ci-1011:在补充了非胆固醇饮食的动物中具有独特的降低胆固醇活性的酰基氨基磺酸酯.
    摘要:
    Doi:10.1021/jm960674D

    海关参考信息

    专利信息


    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-7956214-B2
    优先权日:2001-11-02
    标题 :Process for the preparation of aniline-derived thyroid receptor ligands
    发明人:CHIDAMBARAM RAMAKRISHNAN; KANT JOYDEEP; WEAVER RAYMOND E; YU JURONG; GHOSH ARUN
    权利人:KAROBIO AB; BRISTOL MYERS SQUIBB CO
    摘要:Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.

    专利号:US-8598153-B2
    优先权日:2006-09-22
    标题 :Method of treatment using fatty acid synthesis inhibitors
    发明人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN
    权利人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN; MERCK SHARP & DOHME
    摘要:The present invention relates to natural products that possess fatty acid synthesis inhibitor activity and can be used to treat and prevent diseases such as obesity, cancer, diabetes, fungal infections, Mycobacterium tuberculosis infections, malarial infections and other apicomplexan protozoal diseases.

    专利号:US-2003134898-A1
    优先权日:2001-08-01
    标题 :Dual inhibitors of wax ester and cholesteryl ester synthesis for inhibiting sebum production
    发明人:HOMAN REYNOLD
    摘要:The present invention provides a method of inhibiting sebum production and treating sebaceous gland disorders comprising administering to a patient in need of said treatment an effective amount of a compound that inhibits both acyl-Coenzyme A:cholesteryl acyltransferase (ACAT), and acyl-Coenzyme A:fatty alcohol acyltransferase (AFAT), provided that the compound is not [(2,4,6-triisopropyl-phenyl)-acetyl]-sulfamic acid 2,6-diisopropyl-phenyl ester or a pharmaceutically acceptable salt or solvate thereof. The method of the invention is useful to treat sebaceous gland disorders caused or exacerbated by the overproduction of sebum, including oily skin, acne, seborrhea, perioral dermatitis, rosacea, and corticosteroid-induced acneiform lesions.

    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.

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    品牌试剂参考报价(招募中)

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Hasan MK, El Qaidi S, McDonald P, Roy A, Hardwidge PR. Repurposing Avasimibe to Inhibit Bacterial Glycosyltransferases. Pathogens. 2022 Mar 17;11(3):370. doi: 10.3390/pathogens11030370.
    2: Burnett JR, Huff MW. Avasimibe Pfizer. Curr Opin Investig Drugs. 2002 Sep;3(9):1328-33. 3(3):173-4. doi: 10.2165/00126839-200203030-00005.
    13:795934. doi: 10.3389/fphar.2022.795934.

    合成参考文献


    参考文献:10.1007/s11745-999-0403-7
    摘要:Borradaile NM, Carroll KK, Kurowska EM. Regulation of HepG2 cell apolipoprotein B metabolism by the citrus flavanones hesperetin and naringenin. Lipids. 1999 Jun;34(6):591–8. doi: 10.1007/s11745-999-0403-7.
    参考文献:10.1038/s41391-021-00431-3
    摘要:Eckhardt C, Sbiera I, Krebs M, Sbiera S, Spahn M, Kneitz B, Joniau S, Fassnacht M, Kübler H, Weigand I, Kroiss M. High expression of Sterol-O-Acyl transferase 1 (SOAT1), an enzyme involved in cholesterol metabolism, is associated with earlier biochemical recurrence in high risk prostate cancer. Prostate Cancer and Prostatic Diseases. 2021 Jul 29;25(3):484–90. doi: 10.1038/s41391-021-00431-3.
    参考文献:10.2165/00126839-199901060-00011
    摘要:Coleman SG, Brooke G. Lipid disorders. Summary and table. Drugs R D. 1999 Jun;1(6):471–5. doi: 10.2165/00126839-199901060-00011.
    参考文献:10.2165/00126839-199901060-00012
    摘要:Avasimibe. CI 1011. Drugs R D. 1999 Jun;1(6):477–8. doi: 10.2165/00126839-199901060-00012.
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