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62 条记录 (耗时 0.018 秒)

    STEREOSELECTIVE PROCESS FOR PREPARING (CYCLO)ALKYL PHENYLGLYCOLIC ACIDS
    6.
    发明申请
    STEREOSELECTIVE PROCESS FOR PREPARING (CYCLO)ALKYL PHENYLGLYCOLIC ACIDS 审中-公开
    制备（CYCLO）烷基苯乙醇酸的立体选择性方法

    公开(公告)号：WO00027786A1

    公开(公告)日：2000-05-18

    申请号：PCT/US1999/025587

    申请日：1999-10-29

    IPC分类号： C07B53/00 ,  C07B61/00 ,  C07C51/09 ,  C07C51/353 ,  C07C51/36 ,  C07C59/54 ,  C07D317/34

    CPC分类号： C07D317/34 ,  C07C51/353 ,  C07C59/54

    摘要： A process for preparing an alkyl phenylglycolic acid is disclosed. It follows the sequence of condensing a substituted acetaldehyde with mandelic acid to provide a 5-phenyl-1,3-dioxolan-4-one, which is condensed with an alkyl ketone or aldehyde to provide a 5-(1-hydroxyalkyl)-5-phenyl-1,3-dioxolan-4-one, which is dehydrated to a 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one. The 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one may be hydrolyzed and reduced to an alpha -alkylphenylglycolic acid or the hydrolysis and reduction steps may be reversed. The process enables the production of single enantiomers of cyclohexylphenylglycolic acid (CHPGA). An analogous process for racemic CHPGA is disclosed employing racemic mandelic acid and acetone. Novel intermediates in the process are also disclosed.

    摘要翻译： 公开了一种制备烷基苯基乙醇酸的方法。 它遵循将取代的乙醛与扁桃酸缩合的顺序，得到5-烷基酮或醛缩合的5-苯基-1,3-二氧戊环-4-酮，得到5-（1-羟基烷基）-5 - 苯基-1,3-二氧戊环-4-酮，将其脱水至5-（1-烯基）-5-苯基-1,3-二氧戊环-4-酮。 可以将5-（1-烯基）-5-苯基-1,3-二氧戊环-4-酮水解并还原成α-烷基苯基乙醇酸，或者可以逆转水解和还原步骤。 该方法能够生产环己基苯基乙醇酸（CHPGA）的单一对映异构体。 公开了外消旋CHPGA的类似方法，其使用外消旋扁桃酸和丙酮。 还公开了该方法中的新型中间体。

    LEUKOTRIENE B4 DERIVATIVES, METHODS OF PREPARING THEM AND THEIR USE AS DRUGS
    7.
    发明申请
    LEUKOTRIENE B4 DERIVATIVES, METHODS OF PREPARING THEM AND THEIR USE AS DRUGS 审中-公开
    新白三烯B4衍生物，用于生产及其作为药物

    公开(公告)号：WO1995020562A1

    公开(公告)日：1995-08-03

    申请号：PCT/EP1994000214

    申请日：1994-01-27

    申请人： SCHERING AKTIENGESELLSCHAFT ,  SKUBALLA, Werner ,  BUCHMANN, Bernd ,  HEINDL, Josef ,  FRÖHLICH, Wolfgang ,  EKERDT, Roland ,  GIESEN, Claudia

    发明人： SCHERING AKTIENGESELLSCHAFT

    IPC分类号： C07C59/46

    CPC分类号： C07F9/4018 ,  C07C59/46 ,  C07C59/54 ,  C07C69/007 ,  C07C69/732 ,  C07C235/30 ,  C07C405/0066 ,  C07C2601/04 ,  C07C2601/14 ,  C07D309/30 ,  C07F9/4015

    摘要： The invention concerns leukotriene B4 derivatives of the formula (I), in which R1 is CH2OH, CH3, CF3, COOR5, CONR6R7, or R1 together with R2 is a carbonyl group, R2 and R3, which may be the same or different, are H or an organic-acid group with 1 to 15 C-atomes, R4 is H, a C1-C14 alkyl group, optionally with one or more substituents, a C3-C10 cycloalkyl group, a C6-C10 aryl group optionally substituted, independently of each other, with one or more halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl oder hydroxy groups or R4 is a 5- or 6-membered aromatic heterocyclic ring with at least one hetero atom, R5 is H, C1-C10 alkyl, C3-C10 cycloalkyl, a C6-C10 aryl group optionally substituted with 1 to 3 halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy groups or R5 is CH2-CO-(C6-C10 aryl) or a 5- to 6-membered ring with at least one hetero atom, A is a trans, trans-CH=CH-CH=CH, a -CH2CH2-CH=CH- or a tetramethylene group, B is a straight-chain or branched-chain C1-C10 alkylene group, which may be substituted with fluorine, or the group (a), D is a direct bond, oxygen, sulphur, -C=C-, -CH=CR8, or together with B, may also form a direct bond, R6 and R7, which may be the same or different, are H or C1-C4 alkyl, or R is H and R is C1-C15 alkanoyl or C1-C10 alkane sulphonyl, optionally substituted with OH, R8 is H, C1-C5 alkyl, chlorine, bromine and n is 2 to 5 plus, when R5 is hydrogen, salts of these compounds with physiologically tolerated bases, as well as their cyclodextrin clathrates.

    摘要翻译： 本发明涉及其中R 1 CH 2 OH，CH 3，CF 3，COOR 5，CONR 6 R 7，或R 1与R 2一起表示羰基，R 2和R 3是相同或不同的H或有机残基与1-15的式（I）的白三烯B4衍生物 表示碳原子，R 4是H，任选地单取代或多取代的C1-C14烷基，C3-C10环烷基，任选独立地被取代地被卤素，苯基，C1-C4烷基，C1-C4烷氧基，氟甲基一次或多次 氯甲基，三氟甲基，羧基或羟基取代的C 6 -C 10芳基或具有至少1个杂原子象征着的5-6元芳族杂环，R 5是氢，C1-C10烷基，C3-C10环烷基，任选被1-3个卤素取代的，苯基， 指C1-C4烷基，C1-C4烷氧基，氟甲基，氯甲基，三氟甲基，羧基或羟基取代的C 6 -C 10 - 芳基，CH 2 -CO-（C6-C10）芳基或具有至少1个杂原子的5-6元环 中，是反式，反式CH = CH-CH = CH，一-C H2CH2-CH = CH-或四亚甲基，B是直链或支链C，其可任选被氟取代的1〜10的亚烷基，或（a）象征团，D是一个直接键，氧，硫，-C = C- ，-CH = CR 8，或连同B也可以表示直接键合，R 6和R 7相同或不同并且是H或C1-C4烷基，或者R <7>为H，R <6> C1-C15烷酰基或C1 C10链烷磺酰基代表任选被OH取代，R8是H，C1-C5烷基，氯，溴，n是2-5和，当R 5是氢，其与生理学上可接受的碱及其环糊精笼形物的盐。

    CRYSTALLINE FORMS OF BIMATOPROST ACID, METHODS FOR PREPARATION, AND METHODS FOR USE THEREOF
    10.
    发明申请
    CRYSTALLINE FORMS OF BIMATOPROST ACID, METHODS FOR PREPARATION, AND METHODS FOR USE THEREOF 审中-公开
    二羧酸的结晶形式，制备方法及其使用方法

    公开(公告)号：WO2014106194A1

    公开(公告)日：2014-07-03

    申请号：PCT/US2013/078334

    申请日：2013-12-30

    申请人： ALLERGAN, INC.

    发明人： WU, Ke ,  FENG, Shaoxin ,  KARAMI, Thomas K. ,  SMITH, Scott W.

    IPC分类号： C07C59/54 ,  A61P27/06 ,  A61K31/192

    CPC分类号： A61K31/192 ,  A61K9/0051 ,  C07B2200/13 ,  C07C59/54

    摘要： The invention provides new crystalline forms of 7-[3,5-Dihydroxy-2-(3-hydroxy-5-phenyl-pent-1-enyl)-cyclopentyl]-hept-5-enoic acid. This compound is commonly referred to as "bimatoprost acid." The novel crystalline forms are designated forms I, II, and III. The invention crystalline forms are useful for solid ocular implant formulations, utilized in the treatment of various ocular conditions, such as, for example, ocular hypertension. In addition, invention crystalline forms are useful for solid or semisolid dosage formulations used to treat ocular hypertension.

    摘要翻译： 本发明提供7- [3,5-二羟基-2-（3-羟基-5-苯基 - 戊-1-烯基） - 环戊基] - 庚-5-烯酸的新结晶形式。 该化合物通常称为“比马前列素酸”。 新型结晶形式指定为I，II和III型。 本发明的结晶形式可用于固体眼部植入制剂，用于治疗各种眼部病症，例如高眼压症。 此外，本发明的结晶形式可用于治疗眼高血压的固体或半固体剂型。