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CAS号638-02-8 2,5-二甲基噻吩 | CAS号29874-05-3 2,5-dimethylthi...2,5-二甲基噻吩置于磺酰氯,N,N-二甲基甲酰胺体系中,化学反应 1.0H,以66%的收率获得产物2,5-二甲基-3-硫代噻吩磺酰氯
参考文献:The Use Ofn,N-Dimethylformamide-sulfonyl Chloride Complex For The Preparation Of Thiophenesulfonyl Chlorides
标题:The Use Ofn,N-Dimethylformamide-sulfonyl Chloride Complex For The Preparation Of Thiophenesulfonyl Chlorides
摘要:发现1:1的n,N-二甲基甲酰胺-so2Cl2复合物是一种有效的试剂,可用于一步法合成噻吩磺酰氯.
DOI:10.1246/bcsj.58.1063
专利信息
专利号:US-6150403-A
优先权日:1997-10-14
标 题 :Topical compositions for regulating the oily/shiny appearance of skin
发明人:BIEDERMANN KIMBERLY A; SCHUBERT HARRY L; PARRAN JR JOHN J
权利人:PROCTER & GAMBLE
摘要:The present invention relates to methods for inhibiting sebaceous gland activity in mammalian skin comprising administration of a topical composition comprising dehydroacetic acid or pharmaceutically acceptable salts thereof, and a dermatologically-acceptable carrier. The present invention also relates to methods and topical compositions further comprising agents which regulate the oily and/or shiny appearance of skin, and agents which treat acne and related skin disorders in mammalian skin and scalp. Methods of reducing sebum synthesis with the use of dehydroacetic acid, methods of regulating the oily and/or shiny appearance of skin, and methods of treating acne and other skin disorders are also encompassed by the present invention.
专利号:US-7615634-B2
优先权日:2003-02-10
标题:4-aminopyrimidine-5-one derivatives
发明人:BARTKOVITZ DAVID JOSEPH; CHU XIN-JIE; DING QINGJIE; JIANG NAN; LOVEY ALLEN JOHN; MOLITERNI JOHN ANTHONY; MULLIN JR JOHN GUILFOYLE; VU BINH THANH; WOVKULICH PETER MICHAEL
权利人:HOFFMANN LA ROCHE
摘要:Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors.
专利号:CA-2640585-A1
优先权日:2003-02-05
标题 :Synthesis of 2-butyl-3-(2'-(1-trityl-1h-tetrazol-5-yl)biphenyl-4-yl)-1,3-diazaspirol{4,4}-non-ene-4-one
专利号:US-2008194629-A1
优先权日:2005-05-03
标题 :3-Mono-and 3,5-Disubstituted Piperidine Derivatives as Renin Inhibitors
发明人:BAESCHLIN DANIEL KASPAR; BREITENSTEIN WERNER; EHRHARDT CLAUS; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; ZIMMERMANN JUERG; RUDISSER SIMON; VANGREVELINGHE ERIC; IRIE OSAMU; UMEMURA ICHIRO; SUZUKI MASAKI; MOGI MUNETO; KANAZAWA TAKANORI; YOKOKAWA FUMIAKI; NIHONYANAGI ATSUKO
权利人:BAESCHLIN DANIEL KASPAR; BREITENSTEIN WERNER; EHRHARDT CLAUS; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; ZIMMERMANN JUERG; RUDISSER SIMON; VANGREVELINGHE ERIC; IRIE OSAMU; UMEMURA ICHIRO; SUZUKI MASAKI; MOGI MUNETO; KANAZAWA TAKANORI; YOKOKAWA FUMIAKI; NIHONYANAGI ATSUKO
摘要:The invention relates to 3,5-piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-piperidine compound, and/or a method of treatment comprising administering a 3,5-piperidine compound, a method for the manufacture of a 3,5-piperidine compound, and novel intermediates and partial steps for their synthesis. Especially, the 3,5-piperidine compounds have the formula I, wherein the symbols have the meanings described in the specification.
专利号:EP-2746253-A1
优先权日:2012-12-21
标 题 :Novel compounds with skin lightening properties
发明人:BAXENDALE IAN RICHARD; GINGER REBECCA SUSAN; GLEN ROBERT CHARLES; GREEN MARTIN RICHARD; RIVA ELENA; SCHNETKAMP PAUL PETRUS MARIUS; SZERENCSEI ROBERT TIMOTHY; ZMUIDINAVICIUS DONATAS
权利人:UNILEVER PLC
摘要:This invention relates to novel compounds with skin lightening properties based on an aromatic hydrazine carboxyimidoamide structure, topical skin lightening compositions comprising the same and a method of skin lightening using the said compositions. In particular, the skin lightening benefit is selected from any one of the group consisting of treating melasma, treating post-inflammatory hyperpigmentation, treating age spots, treating dark spots and treating uneven skin tone. n Desired skin colour is a major unmet consumer need around the world and especially in Asia. Consumers particularly desire even skin colour, absence of age spots (solar lentigines), absence of hyperpigmentation and lighter overall skin tone. One solution is to use biological actives that reduce the activity of melanocyte cells in skin. These cells, present in the basal layer of the epidermis, make the dark coloured pigment melanin and export it, in small export vesicles called melanosomes, to the neighbouring keratinocytes. It is well described in the literature that compounds which reduce melanin synthesis when topically applied to the skin will reduce skin darkness over time and can generate a more even skin tone. n Tyrosinase is a very popular target for the regulation of melanocyte pigment production. However effective inhibitors of tyrosinase are bedevilled by safety issues causing, for example, melanocyte cell death, permanent depigmentation, irritation and allergic reactions. Often effective inhibitors kill melanocytes (for example hydroquinone) or cause sensitisation reactions. There is therefore a great need for safe and effective inhibitors of skin pigment production that work through an alternative safe mechanism. n The inventors have observed that selected compounds of the same generic structure inhibit the production of soluble melanin by B16 mouse melanoma cells without cell toxicity.
专利号:US-2016243015-A1
优先权日:2013-10-25
标题 :Skin lightening composition
发明人:GREEN MARTIN RICHARD; GINGER REBECCA SUSAN; GLEN ROBERT CHARLES
权利人:CONOPCO INC DBA UNILEVER
摘要:Desired skin colour is a major unmet consumer need around the world and especially in Asia. Consumers particularly desire even skin colour, absence of age spots (solar lentigines), absence of hyperpigmentation and lighter overall skin tone. One solution is to use biological actives that reduce the activity of melanocyte cells in skin. These cells, present in the basal layer of the epidermis, make the dark coloured pigment melanin and export it, in small export vesicles called melanosomes, to the neighbouring keratinocytes. It is well described in the literature that compounds which reduce melanin synthesis when topically applied to the skin will reduce skin darkness over time and can generate a more even skin tone. Tyrosinase is a very popular target for the regulation of melanocyte pigment production. However effective inhibitors of tyrosinase are bedevilled by safety issues causing, for example, melanocyte cell death, permanent depigmentation, irritation and allergic reactions. Often effective inhibitors kill melanocytes (for example hydroquinone) or cause sensitisation reactions. There is therefore a great need for safe and effective inhibitors of skin pigment production that work through an alternative safe mechanism. The inventors have observed that selected compounds of the same generic structure: or a salt thereof; wherein R 1 , R 2 , R 3 , R 4 and R 5 may be independently selected from the group consisting of —H, -halide, and methyl, ethyl, propyl, iso-propyl, butyl, and t-butyl moieties, inhibit melanin production in Melanodermsâ„¢.