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    ACETYLENES DISUBSTITUTED WITH HYDROXYARYL AND ARYL OR HETEROARYL GROUPS HAVING RETINOID-LIKE BIOLOGICAL ACTIVITY
    51.
    发明申请
    ACETYLENES DISUBSTITUTED WITH HYDROXYARYL AND ARYL OR HETEROARYL GROUPS HAVING RETINOID-LIKE BIOLOGICAL ACTIVITY 审中-公开
    用含有类似生物活性的羟基和芳基或杂环基取代的乙酰基

    公开(公告)号：WO1996020937A1

    公开(公告)日：1996-07-11

    申请号：PCT/US1995015804

    申请日：1995-12-07

    申请人： ALLERGAN

    发明人： ALLERGAN ,  SONG, Tae, K. ,  CHANDRARATNA, Roshantha, A.

    IPC分类号： C07D309/12

    CPC分类号： C07C65/19 ,  C07D213/55 ,  C07D309/12 ,  C07D405/12

    摘要： Compounds of formula (1), wherein R1-R3 and R5 independently are hydrogen, lower alkyl of 1 to 6 carbons, branched chain alkyl or cycloalkyl of 3 to 15 carbons, lower alkyl substituted cycloalkyl of 3 to 15 carbons; R4 is lower alkyl of 1 to 6 carbons, branched chain alkyl or cycloalkyl of 3 to 15 carbons or lower alkyl substituted cycloalkyl of 3 to 15 carbons; X is S or O; Y is a phenyl group, or heteroaryl selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, imidazolyl and oxazolyl, said groups being substituted with the R5 group defined above; A is (CH2)n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR8, CONR9R10, -CH2OH, CH2OR11, CH2OCOR11, CHO, CH(OR12)2, CHOR13O, -COR7, CR7(OR12)2, or CR7OR13O, where R7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R8 is phenyl or lower alkylphenyl, R9 and R10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R11 is lower alkyl, phenyl or lower alkylphenyl, R12 is lower alkyl, and R13 is divalent alkyl radical of 2-5 carbons, have retinoid-like biological activity.

    摘要翻译： 式（1）的化合物，其中R 1 -R 3和R 5独立地为氢，1至6个碳的低级烷基，3至15个碳的支链烷基或环烷基，3至15个碳的低级烷基取代的环烷基; R4是1至6个碳的低级烷基，3至15个碳的支链烷基或环烷基或3至15个碳的低级烷基取代的环烷基; X是S或O; Y是苯基或选自吡啶基，噻吩基，呋喃基，哒嗪基，嘧啶基，吡嗪基，噻唑基，咪唑基和恶唑基的杂芳基，所述基团被上述定义的R5基团取代; A是（CH 2）n，其中n是0-5，具有3-6个碳的低级支链烷基，具有3-6个碳的环烷基，具有2-6个碳的烯基和1或2个双键，具有2-6个碳原子的炔基和 1或2个三键; B是氢，COOH或其药学上可接受的盐，COOR8，CONR9R10，-CH2OH，CH2OR11，CH2OCOR11，CHO，CH（OR12）2，CHOR13O，-COR7，CR7（OR12）2或CR7OR13O，其中R7是烷基 ，碳原子数为1〜5的环烷基或链烯基，R8为碳原子数为1〜10的烷基或碳原子数为5〜10的环烷基，或R8为苯基或低级烷基苯基，R9和R10分别为氢，烷基 1〜10个碳原子的环烷基或5-10个碳原子的环烷基，或苯基或低级烷基苯基，R11为低级烷基，苯基或低级烷基苯基，R12为低级烷基，R13为2-5个碳原子的二价烷基，具有 类视黄醇样生物活性。

    SKIN LIGHTENING COMPOSITIONS
    52.
    发明申请
    SKIN LIGHTENING COMPOSITIONS 审中-公开
    皮肤发光组合物

    公开(公告)号：WO1995023780A2

    公开(公告)日：1995-09-08

    申请号：PCT/US1995002809

    申请日：1995-03-01

    申请人： THE PROCTER & GAMBLE COMPANY

    发明人： THE PROCTER & GAMBLE COMPANY ,  KVALNES, Kalla, Lynn ,  DELONG, Mitchell, Anthony ,  BRADBURY, Barton, James ,  MOTLEY, Curtis, Bobby ,  CARTER, John, David

    IPC分类号： C07C43/315

    CPC分类号： A61K8/498 ,  A61K8/347 ,  A61K8/368 ,  A61K8/37 ,  A61K8/375 ,  A61K8/41 ,  A61K8/42 ,  A61K8/44 ,  A61K8/46 ,  A61K8/466 ,  A61K8/49 ,  A61K8/4906 ,  A61K8/4973 ,  A61K8/4986 ,  A61K8/55 ,  A61Q17/04 ,  A61Q19/02 ,  C07C41/48 ,  C07C41/54 ,  C07C43/315 ,  C07D307/20 ,  C07D309/10 ,  C07D309/12 ,  C07D333/32 ,  C07D335/02 ,  Y02P20/582 ,  Y10S514/938 ,  C07C43/313

    摘要： This invention relates to compositions, compounds and methods for lightening skin, using active compounds having the structure (I) or (II) wherein: (i) each X is, independently, selected from the group consisting of halo, alkyl, substituted alkyl, aryl, OR, OCOR, COR, CONRR, COOR, CN, SR, SOR, SO2R, SO3R and NRR, wherein X is other than hydroxy, amino and thio, if this X is attached ortho to the phenol hydroxy; (ii) m is an integer from 0 to 4; (iii) each R' and R'' is, independently, selected from the group consisting of hydrogen, halo, alkyl, substituted alkyl, aryl, OR, OCOR, OCRROR, COR, CR(OR)OR, CONRR, COOR, CRROR, CN, SR, and NRR; wherein halo, when it appears, is other than geminal to a hydroxy, NH2, or SH; (iv) R''' is alkyl or substituted alkyl; wherein when R''' is present, and R' is also hydrogen, R'' is other than hydrogen, hydroxy, halo, thio, cyano and amino; (v) each R is, independently, selected from the group consisting of hydrogen, alkyl, substituted alkyl and aryl; (vi) n is an integer from 1 to about 5, wherein at least one carbon in (C)n has other than alkyl or hydroxy as a substituent and (C)n adjacent to Z has other than amino, SH, CN or hydroxy as R'; (vii) Z is selected from the group consisting of O, NR, S, SO, SO2, PO2R and POR; (viii) wherein any carbon, when disubstituted, having one substituent selected from the group consisting of hydroxy, amino, cyano and thiol, has the other substituent selected from the group consisting of hydrogen, alkyl, and aryl, whether this substituent is R' or R''; and to pharmaceutically acceptable salts of these compounds, stereoisomers and enantiomers thereof free from or mixed with other enantiomers or stereoisomers; and such compounds in compositions with a pharmaceutically-acceptable carrier thereof comprising a safe and effective amount of a subject skin lightening active.

    摘要翻译： 本发明涉及使用具有结构（I）或（II）的活性化合物来减轻皮肤的组合物，化合物和方法，其中：（i）每个X独立地选自卤素，烷基，取代的烷基， 芳基，OR，OCOR，COR，CONRR，COOR，CN，SR，SOR，SO2R，SO3R和NRR，其中X不是羟基，氨基和硫基，如果该X连接到酚羟基的邻位; （ii）m为0〜4的整数， （iii）每个R'和R“独立地选自氢，卤素，烷基，取代的烷基，芳基，OR，OCOR，OCRROR，COR，CR（OR）OR，CONRR，COOR，CRROR ，CN，SR和NRR; 其中当出现卤素时，除羟基，NH 2或SH之外的其它卤素除外; （iv）R“是烷基或取代的烷基; 其中当R''存在时，R'也是氢，R“不是氢，羟基，卤素，硫代，氰基和氨基; （v）每个R独立地选自氢，烷基，取代的烷基和芳基; （vi）n为1〜5的整数，（C）n中的至少一个碳不是烷基或羟基作为取代基，（C）与Z相邻的n不同于氨基，SH，CN或羟基 作为R' （vii）Z选自O，NR，S，SO，SO 2，PO 2 R和POR; （viii）其中当二取代时，具有选自羟基，氨基，氰基和硫醇的一个取代基的任何碳具有选自氢，烷基和芳基的其它取代基，该取代基是否为R' 或R“ 和这些化合物的药学上可接受的盐，它们的立体异构体和对映异构体与其它对映异构体或立体异构体没有或混合; 并且具有其药学上可接受的载体的组合物中的这种化合物包含安全有效量的受试者皮肤增亮活性物质。

    (4-ALKOXYPYRAN-4-YL) SUBSTITUTED ARYLALKYLARYL-, ARYLALKENYLARYL-, AND ARYLALKYNYLARYLUREA INHIBITORS OF 5-LIPOXYGENASE
    53.
    发明申请
    (4-ALKOXYPYRAN-4-YL) SUBSTITUTED ARYLALKYLARYL-, ARYLALKENYLARYL-, AND ARYLALKYNYLARYLUREA INHIBITORS OF 5-LIPOXYGENASE 审中-公开
    （4-ALKOXYPYRAN-4-YL）取代的芳基乙烯基-L-亚苄基胆碱酯酶和5-氯吡咯烷酮的芳基烯丙基胺抑制剂

    公开(公告)号：WO1994026264A1

    公开(公告)日：1994-11-24

    申请号：PCT/US1994005341

    申请日：1994-05-12

    申请人： ABBOTT LABORATORIES

    发明人： ABBOTT LABORATORIES ,  DELLARIA, Joseph, F. ,  BASHA, Anwer ,  BLACK, Lawrence, A. ,  CHERNESKY, Linda, J. ,  LEE, Wendy

    IPC分类号： A61K31/335

    CPC分类号： C07D405/12 ,  C07D309/12

    摘要： Compounds of structure (I), wherein W is selected from (a), and (b), where Q is oxygen or sulfur, R and R are hydrogen or alkyl, or R and R , together with the nitrogen atoms to which they are attached, define a radical of formula (II) or (III), R is selected from hydrogen, alkyl, haloalkyl, optionally substituted phenyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, (alkoxycarbonyl)alkyl, and (alkylaminocarbonyl)alkyl; Z is -CH2-, oxygen, sulfur, or -NR where R is hydrogen or alkyl, L and L are selected from a valence bond, alkylene, propenylene, and propynylene, R , R , R , and R are independently selected from alkyl, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl, Y is selected from oxygen, -NR , where R is hydrogen or alkyl, and (c), where n = 0, 1, or 2, and R is alkyl, inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

    摘要翻译： 其中W选自（a）和（b）中的结构（I）的化合物，其中Q是氧或硫，R 6和R 7是氢或烷基，或R 6和R 6， （II）或（III）的基团，其中R 8与它们所连接的氮原子一起定义为式（II）或（III）的基团，R 8选自氢，烷基，卤代烷基，任选取代的苯基，羟基烷基，氨基烷基，羧基烷基， （烷氧基羰基）烷基和（烷基氨基羰基）烷基; Z是-CH 2 - ，氧，硫或-NR 9，其中R 9是氢或烷基，L 1和L 2选自价键，亚烷基，亚丙烯基和亚丙炔基，R R 1，R 2，R 3和R 4独立地选自烷基，卤代烷基，卤素，氰基，氨基，烷氧基羰基和二烷基氨基羰基，Y选自氧，-NR 10， 其中R 10是氢或烷基，和（c）其中n = 0,1或2，R 5是烷基，抑制白细胞三烯的生物合成。 这些化合物可用于治疗或改善过敏性和炎性疾病状态。

    PREPARATION OF CHIRAL HYDROXYKETONES
    55.
    发明申请
    PREPARATION OF CHIRAL HYDROXYKETONES 审中-公开
    精制羟基酮的制备

    公开(公告)号：WO1992017433A1

    公开(公告)日：1992-10-15

    申请号：PCT/US1992002231

    申请日：1992-03-25

    申请人： SCHERING CORPORATION ,  GALA, Dinesh

    发明人： SCHERING CORPORATION

    IPC分类号： C07C45/64

    CPC分类号： C07D309/12 ,  C07C45/46 ,  C07C45/64 ,  C07C49/807 ,  C07C49/82

    摘要： A process for preparing an hydroxyketone of formula (X); wherein Ar represents substituted phenyl, aromatic heterocyclic, or substituted aromatic heterocyclic; R and R independently represents hydrogen, C-1 to C-16 alkyl, aromatic, substituted aromatic, aromatic heterocyclic, substituted aromatic heterocyclic or C-1 to C-5 alkyl covalently bonded to Ar, with the provision that R and R are different. The process comprises contacting a compound of formula (V) with a solvent, a base and a chiral hydroxylating agent at a temperature of about -85 DEG C or less. Compounds of formulae (I) and (II) also are disclosed.

    摘要翻译： 制备式（X）的羟基酮的方法; 其中Ar表示取代的苯基，芳族杂环或取代的芳族杂环; R 1和R 2独立地表示氢，C 1至C 16烷基，芳族，取代的芳族，芳族杂环，取代的芳族杂环或与Ar共价结合的C-1至C-5烷基， R 1和R 2不同。 该方法包括在约-85℃或更低的温度下使式（V）化合物与溶剂，碱和手性羟基化试剂接触。 还公开了式（I）和（II）的化合物。

    ASYMMETRIC CHEMICAL SYNTHESIS AND INTERMEDIATES FOR MAKING ANTIFUNGAL COMPOUNDS
    56.
    发明申请
    ASYMMETRIC CHEMICAL SYNTHESIS AND INTERMEDIATES FOR MAKING ANTIFUNGAL COMPOUNDS 审中-公开
    不对称化学合成和制备抗真菌化合物的中间体

    公开(公告)号：WO1991003451A1

    公开(公告)日：1991-03-21

    申请号：PCT/US1990004843

    申请日：1990-08-30

    申请人： SCHERING CORPORATION ,  GIRIJAVALLABHAN, Viyyoor, M. ,  GANGULY, Ashit, K. ,  PINTO, Patrick ,  SARRE, Olga, Z.

    发明人： SCHERING CORPORATION

    IPC分类号： C07C49/80

    CPC分类号： C07D231/12 ,  C07C33/46 ,  C07C49/80 ,  C07D233/56 ,  C07D249/08 ,  C07D303/08 ,  C07D309/12 ,  C07D407/12 ,  Y02P20/55

    摘要： Intermediates of structural formula (II), (III), (IV), (VIII), (XI), or (XII), wherein said compound has an asymmetric center(s) as indicated by the single asterisk (*) and the double asterisk (**) and wherein the compound is substantially free from compound (s) having the same chemical structure but having other absolute stereochemical configurations at the asterisked carbon centers, or a pharmaceutically acceptable salt thereof, wherein Ar represents phenyl, substituted phenyl, 3-thienyl, substituted 3-thienyl, 3-furanyl or substituted 3-furanyl; R represents alkyl or cycloalkyl; R1 represents H or alkyl; X represents chloro, bromo or iodo; X1 represents OH, chloro, bromo, iodo or P1 where P1 represents alkoxy-substituted phenyloxy, benzyloxy, substituted benzyloxy, acyloxy, phenylthio, substituted phenylthio or -NHP2 where P2 is an amino protecting group; and P represents H or a hydroxy protecting group and processes for making chemically pure, enantiomeric antifungal compounds.

    METHOD FOR THE PREPARATION OF INTERMEDIARY COMPOUNDS OF CARBACYCLIN
    58.
    发明申请
    METHOD FOR THE PREPARATION OF INTERMEDIARY COMPOUNDS OF CARBACYCLIN 审中-公开
    制备碳水化合物中间体化合物的方法

    公开(公告)号：WO1983001449A1

    公开(公告)日：1983-04-28

    申请号：PCT/DE1982000205

    申请日：1982-10-14

    申请人： SCHERING AKTIENGESELLSCHAFT ,  VORBRÜGGEN, Helmut

    发明人： SCHERING AKTIENGESELLSCHAFT

    IPC分类号： C07D309/12

    CPC分类号： C07D309/12 ,  C07F7/1804

    摘要： Method for the preparation of bicyclic ketones containing protected hydroxy groups having the general formula I wherein R1 represents the rest -CH2OR2 wherein R2 is benzyl, dimethyltert.-butyl-sylyl, diphenyl-tert.-butylsilyl, dimethylphenylsilyl, tribenzylsilyl or tetrahydropyranyl, wherein R2 has the same definition as hereabove, R4 is hydrogen or methyl and R5 a saturated or unsaturated alkyl rest with a straight or branched chain, substituted or not by fluorine, chlorine atomes, 1,2-methylene, 1,1-trimethylene or methoxy radicals or represents a rest CH2-X-aryl, wherein X is a rest CH2 or oxygen and aryl, a phenyl or heterocyclic rest which may substituted by methyl, methoxy radicals, atoms of fluorine, chlorine, bromine or a trifluoromethyl rest, or with R2, R4, R5 are defined as hereabove, and R3 has the signification given for R2 and is identical or different from R2 or forms with R2 the group wherein R6 and R7, identical or different, represent hydrogen, alkyl, cycloalkyl. It is characterized in that a ketonic acid containing protected hydroxy groups having the formula II is reacted with triphenyl-(phenyliminovinyliden)-phosphorane and then with alcohols. The carbacyclines thus obtained as intermediary products represent starting compounds for the preparation of prostacyclin having a pharmaceutical activity.

    摘要翻译： 制备含有通式I的保护羟基的双环酮的方法其中R1代表其余的-CH2OR2，其中R2是苄基，二甲基叔丁基 - 对苯基，二苯基叔丁基甲硅烷基，二甲基苯基甲硅烷基，三苄基甲硅烷基或四氢吡喃基 其中R 2具有与上述相同的定义，R 4是氢或甲基，R 5是饱和或不饱和的烷基，其具有直链或支链，被氟，氯原子，1,2-亚甲基， 1-三亚甲基或甲氧基，或代表其余的CH 2 -X-芳基，其中X是余下的CH 2或氧和芳基，可被甲基，甲氧基，氟，氯，溴或 三氟甲基保留基或R 2，R 4，R 5的定义如上，R3表示与R2相同或相同或相同或不同的基团，其中R6和R7相同或不同 ，代表h 炔，烷基，环烷基。 其特征在于含有具有式II的受保护羟基的酮酸与三苯基 - （苯基亚氨基亚乙烯基） - 磷烷然后与醇反应。 由此获得的作为中间产物的碳霉素代表用于制备具有药物活性的前列环素的起始化合物。