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公开(公告)号:US06603014B1
公开(公告)日:2003-08-05
申请号:US10053323
申请日:2002-01-23
IPC分类号: C07D27764
CPC分类号: A61K8/4946 , A61K8/49 , A61K8/494 , A61K2800/52 , A61Q1/04 , A61Q17/04
摘要: The use of compounds of the formula I in which R1 and R2 are identical or different, electron-withdrawing radicals chosen from the group consisting of cyano, alkyl- or arylcarbonyl, alkyloxy- or aryloxycarbonyl and optionally substituted aminocarbonyl, R3 is a hydrogen atom, a C1-C20-alkyl radical or a C3-C20-cycloalkyl radical or a radical of the formula —CH2—CH2—SO3—M+, where M+ is a cation, X is the divalent radical of oxygen, sulfur or the radical where R3 is as defined above, is the divalent radical of the formula II or III, which forms a fused system with the radical of the formula I where R4 can be bonded one or more times to the benzylidene ring I or naphthylidene ring II, and is hydrogen, alkyl, cycloalkyl, alkyloxy, cycloalkyloxy, alkoxycarbonyl, mono- or dialkylaminocarbonyl, alkylamino, dialkylamino, each having up to 20 carbon atoms, and also cyano, amino and SO3—M+, where M+ is a cation, as photostable UV filters in cosmetic and pharmaceutical preparations to protect human skin and human hair against solar rays, alone or together with compounds which absorb in the UV region and are known per se for cosmetic and pharmaceutical preparations.
摘要翻译: 使用其中R 1和R 2相同或不同的式Iin化合物,选自氰基,烷基 - 或芳基羰基,烷氧基 - 或芳氧基羰基和任选取代的氨基羰基的吸电子基,R 3是氢原子,C 1 -C 20 - 烷基或C 3 -C 20环烷基或式-CH 2 -CH 2 -SO 3 -M +的基团,其中M +是阳离子,X是氧,硫或基团的二价基团,其中R3如所定义 是式II或III的二价基团,其与式I的基团形成稠合体系,其中R 4可以与亚苄基环I或亚萘基环II键合一次或多次,并且是氢,烷基,环烷基 ,烷氧基,环烷氧基,烷氧基羰基,单或二烷基氨基羰基,烷基氨基,二烷基氨基,各自具有至多20个碳原子,以及氰基,氨基和SO3-M +,其中M +是阳离子,作为化妆品和药物制剂中的光稳定性UV过滤剂 保护人体皮肤a 将人类头发抵抗太阳光线,单独或与在UV区域吸收的化合物一起,并且本身已知用于化妆品和药物制剂。
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公开(公告)号:US06395897B1
公开(公告)日:2002-05-28
申请号:US09434106
申请日:1999-11-05
申请人: Charles L. Cywin , Michel J. Emmanuel , Leah L. Frye , Denice M. Spero , David S. Thomson , Yancey D. Ward
发明人: Charles L. Cywin , Michel J. Emmanuel , Leah L. Frye , Denice M. Spero , David S. Thomson , Yancey D. Ward
IPC分类号: C07D27764
CPC分类号: C07D295/215 , C07C311/42 , C07D263/32 , C07D277/64 , C07D413/04
摘要: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.
摘要翻译: 公开的是本文定义的式(I),(Ia)和(II),(IIa)的组织蛋白酶S可逆抑制化合物。 该化合物可用于治疗自身免疫性疾病。 还公开了制备这些新化合物的方法。
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公开(公告)号:US06576765B2
公开(公告)日:2003-06-10
申请号:US09980103
申请日:2002-03-18
申请人: Keisuke Isozumi
发明人: Keisuke Isozumi
IPC分类号: C07D27764
CPC分类号: C07C269/04 , C07D277/64
摘要: The present invention provides a process for producing an amic acid ester represented by the following general formula (7) (wherein A is substituted or unsubstituted lower alkylene or the like; R1 is substituted or unsubstituted lower alkyl or the like; and R3 is hydrogen or lower alkyl), which process comprises reacting, in the presence of water, an amino acid represented by formula (1) with a halogenated carbonic acid ester represented by formula (2) (wherein X is halogen) to form an amide compound represented by formula (3), then reacting the amide compound with a halogenated carbonic acid ester represented by formula (4) (wherein R2 is substituted or unsubstituted lower alkyl or the like; and X is halogen) to form, in the system, a mixed acid anhydride represented by formula (5), and reacting the mixed acid anhydride with an amine compound represented by formula (6) (wherein Het is substituted or unsubstituted heterocyclic).
摘要翻译: 本发明提供由以下通式(7)表示的酰胺酸酯的制造方法(其中A为取代或未取代的低级亚烷基等; R 1为取代或未取代的低级烷基等; R 3为氢或 低级烷基),该方法包括在水存在下使由式(1)表示的氨基酸与由式(2)表示的卤代碳酸酯(其中X为卤素)反应以形成式 (3),然后使酰胺化合物与由式(4)表示的卤代碳酸酯(其中R 2是取代或未取代的低级烷基等,X是卤素)反应,在体系中形成混合酸酐 由式(5)表示,并使混合的酸酐与由式(6)表示的胺化合物(其中Het是取代或未取代的杂环)反应。
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公开(公告)号:US06197969B1
公开(公告)日:2001-03-06
申请号:US09509783
申请日:2000-04-03
申请人: Kazuto Umezu , Shuji Taniguchi , Mahito Ogawa , Hidetaka Hiyoshi
发明人: Kazuto Umezu , Shuji Taniguchi , Mahito Ogawa , Hidetaka Hiyoshi
IPC分类号: C07D27764
CPC分类号: C07D277/64
摘要: The present invention provides a process for producing a substituted alkylamine represented by formula (3): or a salt thereof, which process comprises reacting a 2-aminothiophenol derivative metal salt represented by formula (1): with an amino acid-N-carboxy anhydride represented by formula (2): and then subjecting the reaction product to cyclization under an acidic condition. A substituted alkylamine typified by 1-(2-benzothioazolyl)akylamine, or a salt thereof can be produced from a 2-aminothiophenol derivative industrially at a high handleability and a high yield, and even when the intended substituted alkylamine is an optically active compound, the intended product can be produced without reducing the optical purity of the optically active raw material.
摘要翻译: 本发明提供一种制备由式(3)表示的取代烷基胺或其盐,该方法包括使由式(1)表示的2-氨基苯硫酚衍生金属盐与氨基酸-N-羧酸酐反应 由式(2)表示:然后使反应产物在酸性条件下环化。 以1-(2-苯并噻唑基)烷基胺或其盐为代表的取代烷基胺可以在工业上以高处理性和高产率由2-氨基苯硫酚衍生物制备,即使目标取代的烷基胺是光学活性化合物, 可以在不降低光学活性原料的光学纯度的情况下制造目标产品。
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