CAS: 150399-21-6; Sodium (E)-5-((4-((2-Carboxylatoethyl)Carbamoyl)Phenyl)Diazenyl)-2-Hydroxybenzoate Dihydrate

该化合物是一种治疗甲胺(5-氨基硅酸)的药,主要用于治疗肺炎性脊髓炎等炎性肠道疾病,其化学结构包括与二钠盐和两个水分子相融合的巴萨拉齐德,增强稳定性和溶性,其设计目的是向结肠专门提供麦片胺,在结肠中,它产生局部的抗炎效应,而系统吸收的力度最小.这种有针对性的释放比传统配方减少胃肠侧效应.Balsalazide di di dydryd酸盐的特点是高度纯度,持续生物利用率和符合药用性标准,使它成为受控释放配方的一种可靠的有效药物成分.

结构式图片

合成工艺路线路线简述

    海关参考信息

    专利信息


    专利号:US-2013035307-A1
    优先权日:2010-01-26
    标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
    发明人:PRESTWICH GLENN D; KENNEDY THOMAS P
    权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
    摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

    专利号:US-11993606-B2
    优先权日:2015-10-16
    标题:Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
    发明人:MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; PANGAN AILEEN L; SONG IN-HO; KLÜNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S
    权利人:ABBVIE INC
    摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).

    专利号:WO-2023096715-A9
    优先权日:2021-10-22
    标 题:Immunomodulatory glycosphingolipids and methods of use thereof
    发明人:KASPER DENNIS; OH SUNGWHAN
    权利人:HARVARD COLLEGE
    摘要:Provided herein are a subset of alpha-galactosylceramide (alpha-GC) compounds having improved immunomodulatory activity, particularly with respect to NKT cell number and activity. Also provided herein are methods of use of such compounds, including in the modulation of NKT cells and/or activity in vivo. Further provided are combinatorial synthesis methods for generating alpha-GC compounds of specifically defined structure and thereby generating pure preparations thereof.

    专利号:US-11976077-B2
    优先权日:2015-10-16
    标 题 :Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms therof
    发明人:PANGAN AILEEN L; TEIXEIRA HENRIQUE D; MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; KLÜNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S
    权利人:ABBVIE INC
    摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and atopic dermatitis), kits, methods of synthesis, and products-by-process.

    专利号:US-11512092-B2
    优先权日:2015-10-16
    标题 :Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
    发明人:ALLIAN AYMAN; JAYANTH JAYANTHY; MOHAMED MOHAMED-ESLAM F; MULHERN MATHEW; NORDSTROM FREDRIK LARS; OTHMAN AHMED A; ROZEMA MICHAEL J; BHAGAVATULA LAKSHMI; MARROUM PATRICK J; MAYER PETER T; SHEIKH AHMAD Y; BORCHARDT THOMAS B; KLÜNDER BEN
    权利人:ABBVIE INC
    摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).

    专利号:US-11524964-B2
    优先权日:2015-10-16
    标题:Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
    发明人:MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; KLÜNDER BEN; PANGAN AILEEN L; SONG IN-HO
    权利人:ABBVIE INC
    摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).
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    1: Kim HY, Kim SL, Park YR, Liu YC, Seo SY, Kim SH, Kim IH, Lee SO, Lee ST, Kim SW. Balsalazide Potentiates Parthenolide-Mediated Inhibition of Nuclear Factor-κB Signaling in HCT116 Human Colorectal Cancer Cells. Intest Res. 2015 Jul;13(3):233-41. doi: 10.5217/ir.2015.13.3.233. Epub 2015 Jun 9.
    2: Sousa T, Yadav V, Zann V, Borde A, Abrahamsson B, Basit AW. On the colonic bacterial metabolism of azo-bonded prodrugsof 5-aminosalicylic acid. J Pharm Sci. 2014 Oct;103(10):3171-5. doi: 10.1002/jps.24103. Epub 2014 Aug 4. doi: 10.3748/wjg.v20.i13.3564. Review.
    4: Coman RM, Glover SC, Gjymishka A. Febrile pleuropericarditis, a potentially life-threatening adverse event of balsalazide--case report and literature review of the side effects of 5-aminosalicylates. Expert Rev Clin Immunol. 2014 May;10(5):667-75. doi: 10.1586/1744666X.2014.902313. Epub 2014 Apr 1. Review. doi: 10.1007/s00228-014-1660-7. Epub 2014 Mar 11.
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