METHOD FOR PRODUCING OPTICALLY ACTIVE 1-AMINO-4-(HYDROXYMETHYL)-CYCLOPENT-2-ENE DERIVATIVES
    6.
    发明申请
    METHOD FOR PRODUCING OPTICALLY ACTIVE 1-AMINO-4-(HYDROXYMETHYL)-CYCLOPENT-2-ENE DERIVATIVES 审中-公开
    用于生产光学活性的1-氨基-4-(羟甲基) - 环戊-2- EN衍生物

    公开(公告)号:WO00039324A2

    公开(公告)日:2000-07-06

    申请号:PCT/EP1999/010382

    申请日:1999-12-23

    CPC分类号: C12P41/004 C12P13/02

    摘要: The invention relates to a new method for producing enantiomer-enriched 1-amino-4-(hydroxymethyl)-cyclopent-2-ene derivatives of the general formulae (I) and (II) in which R is hydrogen or a possibly substituted C1-8 alkyl rest, aryl rest or cycloalkyl rest and R is a possibly substituted acyl. According to said method a racemic 1-amino-4-(hydroxymethyl)-cyclopent-2-ene derivative of general formula (III), in which R has the meaning given above, is converted using a hydrolase and in the presence of an acylation agent.

    摘要翻译: 描述了一种用于制备对映体富集的1-氨基-4-(羟甲基)的通式-cyclopent- -2-烯衍生物(I),(II),其中R <1>是氢或任选取代的C 1-8的新工艺 - 烷基,芳基或环烷基并且R <2>的任选取代的酰基,该方法包括外消旋1-氨基-4-(羟甲基)反应-cyclopent-通式-2-烯衍生物(III)其中R <1 具有在酰化剂存在下借助水解酶给出的含义。

    NITRIC ACID ESTERS OF CYCLOHEXANOL DERIVATIVES
    7.
    发明申请
    NITRIC ACID ESTERS OF CYCLOHEXANOL DERIVATIVES 审中-公开
    环己烷衍生物的硝酸酯

    公开(公告)号:WO1991012230A1

    公开(公告)日:1991-08-22

    申请号:PCT/EP1991000290

    申请日:1991-02-14

    IPC分类号: C07C233/23

    摘要: The present invention relates to novel nitric acid esters of cyclohexanol derivatives of formula (I) in which A is a valency line or a C1-C6 alkylene chain and B is the group -NR1-CO-Z, -NR1-SO2-Z or -CO-NR2-Z, where R1 is hydrogen or a C¿1?-C6-alkyl group, R?2¿ is hydrogen, a hydroxy, hydroxy-C¿1?-C6-alkyl, C1-C6-alkoxy, C1-C6-alkyl, C2-C6-alkenyl or C2C6-alkinyl group and Z is hydrogen, a C1-C6-alkyl, C2-C6-alkenyl or C2C6-alkinyl group, which may be substituted once or several times by a hydroxy, C1-C6-alkylcarbonyloxy, C1-C6-alkoxy, halogen, cyano, carboxy, C1-C6-alkoxycarbonyl, -CO-NR?3R4¿, mercapto, C¿1?-C6-alkylcarbonyl mercapto group, or Z is a C3-C6-cycloalkyl group or a pyridine, N-oxypyridine, tetrazolyl or pyrrolidinone ring, or Z together with R?2¿ and the nitrogen atom to which Z and R2 are bonded, form a heterocyclic ring which may additionally contain an oxygen, sulphur or nitrogen atom, whereby the heterocyclic ring with an additional nitrogen atom may be acylated, possibly on the nitrogen atom, by a C¿1?-C6-alkylcarbonyl group, and if B is a -NR?1¿-CO-Z- group, Z may also be a C¿1?-C6-alkoxy group, or if Z is a C1-C6-alkyl or C2-C6-alkenyl group substituted by a mercapto, C1-C6-alkylmercapto or C1-C6-alkylcarbonyl mercapto, the C1-C6-alkyl or C2-C6-alkenyl group may be additionally substituted by the NR?4/R5¿ or a C¿1?-C4-alkylcarbonyl group and R?3 and R4¿ may be the same or different and mutually independently hydrogen, a C¿1?-C6-alkyl group or R?3 and R4¿ together with the nitrogen atom to which they are bonded form a heterocyclic ring, their optically active forms and physiological permissible salts, and medicaments containing these compounds. The invention also concerns processes for producing compounds of formula (I) and novel intermediate products.

    光学活性トランス-2-アミノシクロヘキサノールおよびその誘導体の製造方法
    9.
    发明申请
    光学活性トランス-2-アミノシクロヘキサノールおよびその誘導体の製造方法 审中-公开
    用于生产光学活性的转移-2-氨基环己醇及其衍生物的方法

    公开(公告)号:WO2007055180A1

    公开(公告)日:2007-05-18

    申请号:PCT/JP2006/322128

    申请日:2006-11-07

    摘要: 本発明は、一般式(1) 【化1】 (式中、R 1 は水素原子、ハロゲン原子、炭素数が1~6のアルキル基、アルコキシル基、ニトロ基から選択される基を示す。また、*はこの記号が付いている炭素原子が不斉中心であることを意味する。)で表される光学活性トランス-2-ベンジルアミノシクロヘキサノール誘導体またはそのプロトン酸塩を水素化分解することを特徴とする一般式(2) 【化2】 (*はこの記号が付いている炭素原子が不斉中心であることを意味する。)で示される光学活性トランス-2-アミノシクロヘキサノールまたはそのプロトン酸塩の製造方法である。この方法により光学活性トランス-2-アミノシクロヘキサノールおよびその誘導体を、工業的に有利で安価な原料から、簡便かつ高収率で製造する方法を提供する。

    摘要翻译: 公开了由下述通式(2)表示的光学活性的反式-2-氨基环己醇或其质子酸盐的制备方法。 该方法的特征在于将下述通式(1)表示的光学活性的反式-2-苄基氨基环己醇衍生物或其质子酸盐进行氢解。 该方法能够通过简单的方法以高产率从商业上有利的廉价原料制备光学活性的反式-2-氨基环己醇及其质子酸盐。 [化学式1](1)(式中,R 1表示选自氢原子,卤素原子,碳原子数1〜6的烷基,烷氧基和 硝基,符号*表示由其标记的碳原子是不对称中心。)[化学式2](2)(式中,符号*表示其标记的碳原子为不对称中心)

    DIHYDROCERAMIDE DESATURASE INHIBITORS.
    10.
    发明申请
    DIHYDROCERAMIDE DESATURASE INHIBITORS. 审中-公开
    DIHYDROCERAMIDE DESATURASE抑制剂。

    公开(公告)号:WO02050018A1

    公开(公告)日:2002-06-27

    申请号:PCT/ES2001/000486

    申请日:2001-12-14

    摘要: The invention relates to derivatives of cyclopropenylceramide used as desaturase inhibitors characterised by the general formula I, wherein R1 may be an alkyl, alkenyl, alkynyl, aryl or any heterocyclic group, n can have any value whatsoever, be branched or not and contain unsaturations, and R2 and R3 can have the same or different values, represent aryl, heteroaryl, alkyl or acyl groups with one or more unsaturations in the chain, which may be branched or not and substituted by OH groups. The members of this new class of compounds have demonstrated an extraordinary activity as inhibitors of dihydroceramide desaturase and of ceramide biosynthesis and are useful for the treatment of pathologies associated with increases in intracellular ceramide levels.

    摘要翻译: 本发明涉及用作去饱和酶抑制剂的环丙烯基神经酰胺的衍生物,其特征在于通式I,其中R 1可以是烷基,烯基,炔基,芳基或任何杂环基,n可以具有任何值,不分支或不含有不饱和基团, 并且R2和R3可以具有相同或不同的值,代表在链中具有一个或多个不饱和基团的芳基,杂芳基,烷基或酰基,其可以是支链的或不被OH基取代的。 这种新类化合物的成员已经表现出作为二氢神经酰胺去饱和酶抑制剂和神经酰胺生物合成的非凡活性,并且可用于治疗与细胞内神经酰胺水平升高相关的病理学。