CAS: 78613-35-1; (2S,6R)-2,6-Dimethyl-4-(2-Methyl-3-(4-(Tert-Pentyl)Phenyl)Propyl)Morpholine

该化合物是一种红外线衍生的抗冻剂,主要用于治疗皮肤和酵母感染,特别是宫颈菌病(幼虫感染),其行动机制包括抑制雌激素生物合成,针对酶+14-呼吸酶和7-8异构体酶,破坏真菌细胞膜的完整性;Amorolfine展示了针对皮肤和酵母的广谱活动,其真菌和真菌效应取决于浓度.一个关键优势是其长期保留在指甲板上,允许每两周一次或两次局部应用.其脂质性能会增强对氯酸盐组织的渗透,而低系统吸收会最大限度地减少有害影响.Amorolfine被设计成有针对性地交付的指甲花,为局部真菌感染提供方便和有效的治疗选择.

结构式图片

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CAS号75-85-4 叔戊醇 | CAS号922734-43-8 bepromoline hyd... | CAS号594-36-5 2-氯代-2-甲基丁烷

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    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    专利号:US-2009131660-A1
    优先权日:2006-04-03
    标 题 :SYNTHESIS OF 3-[4-(1,1-DIMETHYL-PROPYL)-PHENYL]-2-METHYL-PROPIONALDEHYDE AND cis-4--2,6-DIMETHYL-MORPHOLINE (AMOROLFINE)
    发明人:BOITEAU JEAN-GUY; MUSICKI BRANISLAV
    权利人:GALDERMA SA
    摘要:3-[4-(1,1-Dimethyl-propyl)-phenyl]-2-methyl-propionaldehyde and cis-4-{3-[4-(1,1-dimethyl-propyl)-phenyl]-2-methyl-propyl}-2,6-dimethyl-morpholine (Amorolfine) are synthesized, first by Heck reacting a compound of general formula (VI): n n n n n n n n n n with 2-methyl-prop-2-en-1-ol of formula (VII): n n n n n n n n n n in the presence of a palladium catalyst and a base, in a solvent selected from among N,N-dimethylformamide, polar protic and non-polar organic solvents, and at a temperature ranging from 60° C. to 150° C., and then conducting an amino reduction by reacting the 3-[4-(1,1-dimethyl-propyl)-phenyl]-2-methyl-propionaldehyde of formula (II) with cis-2,6-dimethyl morpholine of formula (IV): n n n n n n n n n n in the presence of a reducing agent and in a solvent.

    专利号:US-9382288-B2
    优先权日:2010-10-06
    标题 :Derivatives of steroid benzylamines, having an antiparasitic antibacterial, antimycotic and/or antiviral action
    发明人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO
    权利人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO; UNIV GIESSEN JUSTUS LIEBIG
    摘要:The present invention relates to compounds derived from steroids of the general formula (I) n nwherein L represents a linker and R # represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).

    专利号:WO-2009056955-A1
    优先权日:2007-10-30
    标题 :Amine-bearing phospholipids (abps), their synthesis and use
    发明人:ZUMBUEHL ANDREAS
    权利人:UNIV BASEL; ZUMBUEHL ANDREAS
    摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.

    专利号:AU-2007308022-A2
    优先权日:2006-10-05
    标题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

    专利号:AU-2007308022-A1
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
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    主要参考文献


    1: Tabara K, Szewczyk AE, Bienias W, Wojciechowska A, Pastuszka M, Oszukowska M, Kaszuba A. Amorolfine vs. ciclopirox - lacquers for the treatment of onychomycosis. Postepy Dermatol Alergol. 2015 Feb;32(1):40-5. doi: 10.5114/pdia.2014.40968. Epub 2015 Feb 3. Review.
    2: Auvinen T, Tiihonen R, Soini M, Wangel M, Sipponen A, Jokinen JJ. Efficacy of topical resin lacquer, amorolfine and oral terbinafine for treating toenail onychomycosis: a prospective, randomized, controlled, investigator-blinded, parallel-group clinical trial. Br J Dermatol. 2015 Oct;173(4):940-8. doi: 10.1111/bjd.13934. Epub 2015 Oct 1. doi: 10.3109/09546634.2015.1109029. Epub 2015 Nov 11. doi: 10.1111/myc.12473. Epub 2016 Feb 11. doi: 10.1111/myc.12369. Epub 2015 Sep 3. doi: 10.1159/000441569. Epub 2015 Nov 7. Erratum in: Skin Appendage Disord. 2016 May;1(4):168.
    7: Monti D, Tampucci S, Chetoni P, Burgalassi S, Mailland F. Ciclopirox vs amorolfine: in vitro penetration into and permeation through human healthy nails of commercial nail lacquers. J Drugs Dermatol. 2014 Feb;13(2):143-7. doi: 10.1111/jpc.12740. doi: 10.1007/s10103-016-1990-z. Epub 2016 Jun 23. doi: 10.1111/bjd.13982. doi: 10.1007/s13555-016-0093-x. Epub 2016 Feb 1. Erratum in: Dermatol Ther (Heidelb). 2016 Sep;6(3):451.

    合成参考文献


    摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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