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    Aromatic heterocyclic derivatives and their therapeutic and cosmetic use
    13.
    发明授权
    Aromatic heterocyclic derivatives and their therapeutic and cosmetic use 失效
    芳香杂环衍生物及其治疗和美容用途

    公开(公告)号：US5288744A

    公开(公告)日：1994-02-22

    申请号：US900479

    申请日：1992-06-18

    申请人： Braham Shroot ,  Jacques Eustache ,  Jean-Michel Bernardon

    发明人： Braham Shroot ,  Jacques Eustache ,  Jean-Michel Bernardon

    IPC分类号： A61C9/00 ,  C07C59/64 ,  C07D209/10 ,  C07D235/18 ,  C07D263/56 ,  C07D263/57 ,  C07D277/66 ,  C07D307/79 ,  C07D333/54 ,  C07D405/04 ,  C07D417/01 ,  A61K31/425

    CPC分类号： C07D263/57 ,  A61C9/00 ,  C07C59/64 ,  C07D209/10 ,  C07D235/18 ,  C07D277/66 ,  C07D307/79 ,  C07D333/54 ,  C07D405/04

    摘要： Aromatic heterocyclic derivatives have the formula ##STR1## wherein R.sub.1 represents (i)--CH.sub.3, (ii)--CH.sub.2 OH or (iii) ##STR2## wherein R.sub.3 represents hydrogen, --OR.sub.4 wherein R.sub.4 represents hydrogen, alkyl having 1-20 carbon atoms or mono- or polyhydroxyalkyl or R.sub.3 represents ##STR3## wherein r' and r" represent hydrogen, lower alkyl or together form a heterocycle, R.sub.2 represents hydrogen or --CH.sub.3 and Ar represents ##STR4## wherein Z is O or S, ##STR5## wherein R.sub.5 is lower alkyl or ##STR6## wherein R.sub.6 is hydrogen or alkyl having 1-10 carbon atoms and R.sub.7 represents alkyl having 4-12 carbon atoms or cycloalkyl, Y is CH or a nitrogen atom and X represents oxygen, sulfur or --N--R.sub.8 when R.sub.8 represents hydrogen, lower alkyl or lower alkoxycarbonyl, with the proviso that (i) when Y is CH and X is oxygen or sulfur Ar is other than C and (ii) when Y is nitrogen and X is oxygen, Ar is other than (C) or (D) in which R.sub.6 is alkyl having 1-4 carbon atoms and R.sub.7 is branched alkyl having 4-12 atoms.

    摘要翻译： 芳族杂环衍生物具有下式（其中R 1表示（i）-CH 3，（ii）-CH 2 OH或（iii）其中R 3表示氢，-OR 4，其中R 4表示氢，具有1-20个碳原子的烷基或 单或多羟基烷基或R 3表示其中r'和r“表示氢，低级烷基或一起形成杂环，R 2表示氢或-CH 3，Ar表示（A）其中 Z是O或S，其中R 5是低级烷基或（D），其中R 6是氢或具有1-10个碳原子的烷基，R 7表示具有4-12个碳原子的烷基或环烷基，Y 当R 8表示氢，低级烷基或低级烷氧基羰基时，X表示氧，硫或-N-R8，条件是（ⅰ）当Y为CH且X为氧或硫时，Ar不为C 和（ii）当Y是氮且X是氧时，Ar不是（C）或（D），其中R6是具有1-4个碳原子的烷基，R7是具有4-12个原子的支链烷基 s。

    Benzonaphtahalene derivatives, a process for their preparation and their use in therapeutic and cosmetic compositions
    14.
    发明授权
    Benzonaphtahalene derivatives, a process for their preparation and their use in therapeutic and cosmetic compositions 失效
    苯并萘林衍生物，其制备方法及其在治疗和美容组合物中的用途

    公开(公告)号：US5183889A

    公开(公告)日：1993-02-02

    申请号：US803965

    申请日：1991-12-09

    申请人： Braham Shroot ,  Jacques Eustache ,  Jean-Michel Bernardon

    发明人： Braham Shroot ,  Jacques Eustache ,  Jean-Michel Bernardon

    IPC分类号： A61K8/368 ,  A61K31/165 ,  A61K31/19 ,  A61K31/235 ,  A61Q5/00 ,  A61Q19/00 ,  C07C15/20 ,  C07C39/42 ,  C07C63/36 ,  C07C65/11 ,  C07C65/24 ,  C07C65/26 ,  C07C233/64 ,  C07D295/185

    CPC分类号： C07D295/185 ,  A61K31/165 ,  A61K31/235 ,  A61K8/368 ,  A61Q19/00 ,  A61Q5/00 ,  C07C39/42 ,  C07C63/36 ,  C07C65/11 ,  C07C65/24 ,  C07C65/26 ,  A61K2800/75

    摘要： A benzonphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjuctive tissues. The compound also possesses anti-tumor activity.

    摘要翻译： 苯并萘化合物具有式（I）其中R 1表示（ⅰ）或（ⅱ）-CH 2 OH; R6表示<或者>其中R7表示氢，具有1-20个碳原子的烷基，一羟基烷基或多羟基烷基，r'或r“表示氢，低级烷基，单或多羟基烷基，芳基或氨基酸或 糖，或一起形成杂环; R 2表示氢，具有1-15个碳原子的烷基，具有1-4个碳原子的烷氧基或脂环族基; R3表示氢，羟基，具有1-4个碳原子的烷基，具有1-10个碳原子的烷氧基，脂环族基团，硫代环脂族基团或-O-Si（CH3）2-R8，其中R8表示低级烷基; 并且R 4和R 5表示氢，低级烷基，羟基或低级酰氧基。 该化合物可用于局部和全身治疗皮肤病和治疗结缔组织的变性。 该化合物还具有抗肿瘤活性。

    Aromatic esters and thioesters, a process for their preparation and their use in human or veterinary medicine and in cosmetic compositions
    15.
    发明授权
    Aromatic esters and thioesters, a process for their preparation and their use in human or veterinary medicine and in cosmetic compositions 失效
    芳族酯和硫酯，它们的制备方法及其在人或兽医学和化妆品组合物中的应用

    公开(公告)号：US5173289A

    公开(公告)日：1992-12-22

    申请号：US480486

    申请日：1990-02-16

    申请人： Braham Shroot ,  Jacques Eustache ,  Jean-Michel Bernardon

    发明人： Braham Shroot ,  Jacques Eustache ,  Jean-Michel Bernardon

    IPC分类号： C07C69/00 ,  C07C69/773

    CPC分类号： C07C69/00 ,  C07C2103/00 ,  C07C2103/74 ,  Y10S514/88

    摘要： Aromatic esters and thioesters of the formula ##STR1## are useful in human and veterinary medicine and in cosmetic formulations. In the formula, X represents oxygen or sulfur, r' and 4" represent hydrogen, lower alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl or benzyl optionally substituted, the residue of an amino acid or aminated sugar, or taken together form a heterocycle, R.sub.2 represents .alpha., .alpha.'- dissubstituted alkyl having 4-12 carbon atoms or mono- or polycyclic cycloalkyl having 5-12 carbon atoms whose carbon linking carbon is trisubstituted and R.sub.3 and R.sub.4 represent hydrogen or lower alkyl.

    摘要翻译： 具有式（I）的芳族酯和硫酯可用于人和兽医学和化妆品制剂。 在该式中，X表示氧或硫，r'和4“表示氢，低级烷基，单羟基烷基，多羟基烷基，芳基或任选取代的苄基，氨基酸或胺化糖的残基或一起形成杂环R2 表示具有4-12个碳原子的α，α'-取代的烷基或具有5-12个碳原子的单环或多环环烷基，其碳连接碳是三取代的，R3和R4代表氢或低级烷基。

    Benzonaphthalene derivatives, a process for their preparation and their use in therapeutic and cosmetic compositions
    18.
    发明授权
    Benzonaphthalene derivatives, a process for their preparation and their use in therapeutic and cosmetic compositions 失效
    苯并萘衍生物，其制备方法及其在治疗和美容组合物中的用途

    公开(公告)号：US5212303A

    公开(公告)日：1993-05-18

    申请号：US952341

    申请日：1992-09-28

    申请人： Braham Shroot ,  Jacques Eustache ,  Jean-Michel Bernardon

    发明人： Braham Shroot ,  Jacques Eustache ,  Jean-Michel Bernardon

    IPC分类号： A61K8/368 ,  A61K8/37 ,  A61Q5/00 ,  A61Q19/00 ,  C07C15/24 ,  C07C39/42 ,  C07C63/36 ,  C07C65/11 ,  C07C65/24 ,  C07C65/26 ,  C07D295/185

    CPC分类号： C07D295/185 ,  A61K8/368 ,  A61K8/37 ,  A61K8/42 ,  A61Q19/00 ,  A61Q5/00 ,  C07C39/42 ,  C07C63/36 ,  C07C65/11 ,  C07C65/24 ,  C07C65/26

    摘要： A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents (i) ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --0--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjuctive tissues. The compound also possesses anti-tumor acitivity.

    摘要翻译： 苯并萘化合物具有下式（I）其中R 1表示（i）图像或（ii）-CH 2 OH; R6表示<或者>其中R7表示氢，具有1-20个碳原子的烷基，一羟基烷基或多羟基烷基，r'或r“表示氢，低级烷基，单或多羟基烷基，芳基或氨基酸或 糖，或一起形成杂环; R 2表示氢，具有1-15个碳原子的烷基，具有1-4个碳原子的烷氧基或脂环族基; R3表示氢，羟基，具有1-4个碳原子的烷基，具有1-10个碳原子的烷氧基，脂环族基团，硫代环脂族基团或-O-Si（CH3）2-R8，其中R8表示低级烷基; 并且R 4和R 5表示氢，低级烷基，羟基或低级酰氧基。 该化合物可用于局部和全身治疗皮肤病和治疗结缔组织的变性。 该化合物还具有抗肿瘤活性。