专利号:US-2021130409-A1 优先权日:2017-09-01 标 题 :Method for the Solid-Phase Synthesis of Cyclic Pentapeptides 发明人:ZHENGGUO JIANG; LUCIANO FORNI; ROBERTSON ALAN 权利人:Alsonex Pty Ltd 摘要:A method for the synthesis of a cyclic ornithine-proline-D-cyclohexylalanine-tryptophan-arginine pentapeptide of Formula A; n n n n n n n n n n n n wherein R 1 and R 2 are, independently, —H, or —C(O)R 3 where R 3 is —CH 2 Ph, —CH 2 CH 2 Ph, —CHâ•?CHPh, —C(NHAC)CH 2 Ph;n nthe method comprising the steps of;n nforming a linear proline-D-cyclohexylalanine-tryptophan-arginine-ornithine pentapeptide of Formula B, attached to a polymeric resin;n n n n n n n n n n n n n n n n n wherein R 1 is as for Formula A, RES indicates the polymeric resin, and P 1 and P 2 are protecting groups;n ncyclising the linear pentapeptide of Formula B to form a cyclic pentapeptide of Formula C, attached to the polymeric resin;n n n n n n n n n n n n n n n cleaving the cyclic peptide of Formula C from the resin providing a cleaved cyclic pentapeptide having a free amine group of an ornithine residue;n noptionally substituting the free amine group of the ornithine residue of the cleaved cyclic peptide;n nremoving the protecting groups P 1 and P 2 , to providethe cyclic peptide of Formula A.
专利号:US-9512096-B2 优先权日:2011-12-22 标题 :Synthesis of amine substituted 4,5,6,7-tetrahydrobenzothiazole compounds 发明人:CHEN WEIRONG; HUMORA MICHAEL; KWOK DAW-LONG ALBERT; KIESMAN WILLIAM F; IRDAM ERWIN AYANDRA 权利人:KNOPP BIOSCIENCES LLC; KNOPP BIOSCIENCES LLP 摘要:The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process.
专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-7598291-B2 优先权日:2004-09-02 标题 :Methods and compositions for enhancing collagen and proteoglycan synthesis in the skin 发明人:NIMNI MARCEL; HAN BO 权利人:NIMNI MARCEL; HAN BO 摘要:A composition for application to the skin can stimulate the in vivo synthesis of collagen and proteoglycans and improve the appearance of the skin, increasing its elasticity and fullness. In general, a composition according to the present invention comprises: (1) an antioxidant compound in a quantity sufficient to enhance collagen synthesis in the skin; (2) an organic penetrant in which the antioxidant compound is soluble in a sufficient quantity that a concentration of the antioxidant compound sufficient to enhance collagen synthesis can be applied topically and penetrate the skin; (3) a mixture of essential amino acids; (4) a supplemental source of sulfur; and (5) a topical pharmaceutically acceptable carrier. The antioxidant compound can be lipoic acid, a lipoic acid analogue or derivative, a bioflavonoid, a constituent of ginkgo, or an isoflavone. The organic penetrant is preferably benzyl alcohol. Other ingredients, such as esters of tocopherol and ascorbic acid, can be included.
专利号:US-2010160244-A1 优先权日:2004-09-02 标 题 :Methods and compositions for enhancing collagen, proteoglycan, and glutathione synthesis in the skin 发明人:NIMNI MARCEL; HAN BO 权利人:NIMNI MARCEL; HAN BO 摘要:A composition for application to the skin can stimulate the in vivo synthesis of collagen and proteoglycans and improve the appearance of the skin, increasing its elasticity and fullness. In general, a composition according to the present invention comprises: (1) an antioxidant compound in a quantity sufficient to enhance collagen synthesis in the skin; (2) an organic penetrant in which the antioxidant compound is soluble in a sufficient quantity that a concentration of the antioxidant compound sufficient to enhance collagen synthesis can be applied topically and penetrate the skin; (3) a mixture of essential amino acids or hydrolyzed whey protein; (4) a supplemental source of sulfur; and (5) a topical pharmaceutically acceptable carrier. The antioxidant compound can be lipoic acid or a lipoic acid analogue or derivative. The organic penetrant is preferably benzyl alcohol. Other ingredients, such as esters of tocopherol and ascorbic acid, can be included.
专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
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