首页> 外国专利> COSMETIC AND PHARMACEUTICAL COMPOSITIONS CONTAINING 2-7-(1- ADAMANTYL) NAPHTHYL ARYL DERIVATIVES FOR TREATMENT OF AILMENTS INVOLVING RETINOID ACID RECEPTORS AND HYPERVITAMINOSIS A AND SOME NEW SUCH COMPOUNDS

COSMETIC AND PHARMACEUTICAL COMPOSITIONS CONTAINING 2-7-(1- ADAMANTYL) NAPHTHYL ARYL DERIVATIVES FOR TREATMENT OF AILMENTS INVOLVING RETINOID ACID RECEPTORS AND HYPERVITAMINOSIS A AND SOME NEW SUCH COMPOUNDS

机译:含有2- [7-(1-金刚烷基)萘基]芳基衍生物的化妆品和药物成分,用于治疗涉及类视黄酸受体和高维生素A和某些新化合物的疾病

摘要

A cosmetic or pharmaceutical composition for the treatment of disorders or aliments related to an overregulation of RARs and/or to hypervitaminosis A, comprising as an active agent a pharmaceutically effective amount of at least one compound of retinoid type of general formula 2134 כ" ה באלול התשס" א - September 13, 2001 in which -R1 represents (i) the -CH3 radical, (ii) the -CH2OH radical, (iii) the -O-R3 radical, (iv) the -CO-R4 radical, R3 and R4 having the meanings given below, Ar is a radical of formula: R5 having the meaning given below, R2 represents: (a) an -(X)n-(CH2)p-R6 radical, (b) an - (X)n-(CH2)q-R7 radical, (c) a -CH=CH-(CH2)s-R6 radical, (d) a -CH=CH-(CH2)t-R7 radical, R6, R7, X, n p , q, s and t having the meanings given below, it being understood that: R3 represents a hydrogen atom, a lower alkyl radical or a -(CH2)m-(CO)n-R8 radical, R8, m and n having the meanings given below, R4 represents: (a) a hydrogen atom, (b) a lower alkyl radical, (c) a radical of formula: (d) an -OR9 radical, R(, R) and R9 having the meanings given below, R5 represents a hydrogen or halogen atom, a linear or branched alkyl radical having from 1 to 20 carbon atoms, a hydroxyl 2135 כ" ה באלול התשס" א - September 13, 2001 radical or an -OR10 or O , -O-C-R10 radical, R10 having the meaning given below, R6 represents a hydrogen atom, a linear or branched alkyl radical having from 1 to 20 carbon atoms, an alkenyl radical or an alkynyl radical, R7 represents an aryl radical, a mono- or polyhydroxyalkyl radical in which the hydroxyls are optionally protected in the methoxy or acetoxy or acetonide form, an aminoalkyl radical in which the amine functional group is optionally substituted by one or two lower alkyl groups, a polyether radical, a -COR4 radical, a saturated or unsaturated heterocycycle radical or alternatively an aminoaryl radical, R8 represents a lower alkyl radical or a saturated heterocycle, R9 represents a hydrogen atom, a linear or branched alkyl radical having from 1 to 20 carbon atoms, an alkenyl radical, a mono- or polyhydroxyalkyl radical, an optionally substituted aryl or aralkyl radical or a sugar residue or an amino acid or peptide residue, R10 represents a lower alkyl radical, X represents an oxygen atom or an -S(O)r radical, R( and R), which are identical or different, represent a hydrogen atom, a lower alkyl radical, a mono- or polyhydroxyalkyl radical, an optionally substituted aryl radical or an amino acid, peptide or sugar residue or alternatively, taken together, form a saturated heterocycle, m is an integer between 1 and 3 inclusive, n is an integer between 0 and 1 inclusive, p is an integer between 5 and 12 inclusive, q is an integer between 0 and 12 inclusive, r is an integer between 0 and 2 inclusive, s is an integer between 3 and 10 inclusive, t is an integer between 0 and 10 inclusive, as well as their salts and their chiral analogues. Claimed as new are compounds, characterized in that they have the formula (I), as defined above in which R7 is a polyether radical having a carbon in the position a to the carbon which is in the 6-position of the naphthyl radical.
机译:一种用于治疗与RARs过度调节和/或维生素A过多相关的疾病或饮食的化妆品或药物组合物,其包含药学有效量的至少一种通式2134的类维生素A类化合物作为活性剂。 2001年9月13日,其中-R1代表(i)-CH3自由基,(ii)-CH2OH自由基,(iii)-O-R3自由基,(iv)-CO-R4自由基,R3 R 4具有以下含义。R 5具有以下含义,R 2表示:(a)-(X)n-(CH 2)p -R 6基团,(b)-(X )n-(CH2)q-R7基团,(c)-CH = CH-(CH2)s-R6基团,(d)-CH = CH-(CH2)t-R7基团,R6,R7,X ,np,q,s和t具有以下给出的含义,应理解:R3代表氢原子,低级烷基或-(CH2)m-(CO)n-R8基团,R8,m和n具有以下含义,R 4表示:(a)氢原子,(b)低级烷基基团,(c)具有下式的基团:(d)-OR9基团,R(,R)和R9具有以下给出的含义,R5代表氢或卤素原子,具有1至20的直链或支链烷基碳原子,一个羟基2135-2001年9月13日基团或-OR10或O--OC-R10基团,R10具有以下含义,R6代表氢原子,为直链或支链烷基具有7至20个碳原子的基团,烯基基团或炔基基团,R 7表示芳基基团,其中羟基任选地以甲氧基或乙酰氧基或丙酮化物形式被保护的单-或多羟基烷基基团,其中的氨基烷基基团。胺官能团任选被一个或两个低级烷基,聚醚基,-COR4基,饱和或不饱和杂环基或氨基芳基取代,R8代表低级烷基或饱和杂环,R9代表液压原子,具有1至20个碳原子的直链或支链烷基,烯基,单或多羟烷基,任选取代的芳基或芳烷基或糖残基或氨基酸或肽残基,R 10表示低级烷基,X表示氧原子或-S(O)r基,R(和R)相同或不同,表示氢原子,低级烷基,单或多羟基烷基,任选取代的芳基或氨基酸,肽或糖残基,或一起形成饱和杂环,m为1至3之间的整数,n为0至1之间的整数,p为5至3的整数。 12是一个整数,q是0到12包括一个整数,r是0到2包括一个整数,s是3到10包括一个整数,t是0到10包括一个整数,以及它们的盐和它们的手性类似物。要求保护的是新化合物,其特征在于它们具有如上所定义的式(I),其中R 7是在碳原子上萘基的6-位上的a位具有碳的聚醚基。

著录项

  • 公开/公告号IL118076B

    专利类型

  • 公开/公告日2001-09-13

    原文格式PDF

  • 申请/专利号IL118076

  • 发明设计人

    申请日1996-04-29

  • 分类号C07H13/02;A61K7/48;A61K31/015;A61K31/03;A61K31/045;A61K31/075;A61K31/10;A61K31/11;A61K31/12;A61K31/135;A61K31/165;A61K31/17;A61K31/19;A61K31/215;A61K31/33;A61K31/7024;A61K38/02;A61P9/00;A61P17/00;A61P19/00;A61P27/02;A61P29/00;A61P31/12;A61P35/00;A61P37/00;C07C13/615;C07C25/22;C07C25/24;C07C33/34;C07C33/36;C07C33/38;C07C33/50;C07C39/17;C07C39/23;C07C39/42;C07C43/20;C07C43/257;C07C47/52;C07C49/20;C07C49/76;C07C63/49;C07C63/66;C07C63/68;C07C65/01;C07C65/21;C07C69/003;C07C69/007;C07C69/017;C07C211/26;C07C215/28;C07C215/48;C07C217/20;C07C217/74;C07C219/28;C07C223/02;C07C225/18;C07C229/38;C07C233/64;C07C235/42;C07C237/28;C07C275/24;C07C275/28;C07C317/14;C07C317/22;C07C317/24;C07C317/32;C07C317/44;C07C321/28;C07D213/24;C07D213/65;C07D213/78;C07D295/182;C07D307/38;C07D307/58;C07D307/68;C07D317/14;C07D319/06;C07D321/06;C07D333/06;C07D333/32;C07D333/38;C07D401/06;C07D401/12;C07D405/06;C07D405/12;C07D407/06;C07D407/12;C07D409/06;C07D409/12;C07D413/06;C07D413/12;C07D417/12;C07D521/00;C07K2/00;C07C25/27;C07D416/06;

  • 国家 IL

  • 入库时间 2022-08-22 01:25:05

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