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    방향족 알데히드의 제조 방법
    84.
    发明公开
    방향족 알데히드의 제조 방법 失效
    生产芳族醛的方法

    公开(公告)号：KR1020060086352A

    公开(公告)日：2006-07-31

    申请号：KR1020067003054

    申请日：2003-08-27

    Applicant: 이하라케미칼 고교가부시키가이샤

    Inventor： 가와조에겐타로

    IPC: C07C45/30 ,  C07C45/00 ,  C07C47/54

    CPC classification number: C07C201/12 ,  C07C45/30 ,  C07C47/546 ,  C07C47/544 ,  C07C47/54 ,  C07C47/575 ,  C07C47/55 ,  C07C205/44

    Abstract: (3) (wherein R' and n are as defined below) is produced by a process characterized in that a benzyl compound of the general formula: (1) (wherein R represents a hydrogen atom, etc.; n is an integer of 1 to 6; and R's may be identical with or different from each other, and each represent a hydrogen atom, an alkyl group, a substituted or unsubstituted phenyl group, etc.) is reacted with a bromoxide of the general formula: MBrOm (2) (wherein M represents a hydrogen atom or a metal atom; and m is an integer of 1 to 3) in the presence of an acid catalyst. Aromatic aldehyde compounds can be produced with high selectivity by simple operation without the need to use expensive catalysts and transition metals.

    Abstract translation: （3）（其中R'和n如下所定义）通过以下方法制备：其特征在于通式为（1）的苄基化合物（其中R表示氢原子等; n为1的整数 至6; R可以彼此相同或不同，并且各自表示氢原子，烷基，取代或未取代的苯基等）与下列通式的溴化物反应：MBrOm（2） （其中M表示氢原子或金属原子，m为1〜3的整数）。 芳族醛化合物可以通过简单的操作以高选择性生产，而不需要使用昂贵的催化剂和过渡金属。

    인데논카르복실산 유도체 및 당뇨병 및 이상지혈증의 치료및 예방을 위한 이의 용도
    87.
    发明公开
    인데논카르복실산 유도체 및 당뇨병 및 이상지혈증의 치료및 예방을 위한 이의 용도 无效
    吲哚羧酸衍生物及其用于治疗和预防糖尿病和糖尿病的用途

    公开(公告)号：KR1020050091086A

    公开(公告)日：2005-09-14

    申请号：KR1020057012917

    申请日：2003-12-16

    Applicant: 메르크 파텐트 게엠베하

    Inventor： 애드제,나탈리 ,  브루네,미쉘 ,  로쉐,디디에 ,  제일러,장-자크 ,  이본,슈테판 ,  기야드-댕그레몽,발레 ,  콘타르드,프란시스 ,  게리에르,다니엘 ,  페랑,제라르 ,  본옴므,이브스

    IPC: C07C309/65 ,  C07C323/34 ,  A61P3/10 ,  A61P3/06

    CPC classification number: C07C323/56 ,  C07C45/46 ,  C07C45/673 ,  C07C45/68 ,  C07C49/747 ,  C07C49/755 ,  C07C59/72 ,  C07C59/90 ,  C07C65/40 ,  C07C67/30 ,  C07C67/31 ,  C07C69/712 ,  C07C69/736 ,  C07C69/76 ,  C07C205/45 ,  C07C211/60 ,  C07C229/18 ,  C07C233/33 ,  C07C251/44 ,  C07C255/40 ,  C07C309/65 ,  C07C317/44 ,  C07C323/22 ,  C07C323/52 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/42 ,  C07C47/575

    Abstract: The present invention relates to a compound of the formula ((I): in which: n is an integer chosen from 1, 2 and 3; Y represents O; N-OR9, in which R9represents H or a saturated hydrocarbon-based aliphatic group; CR10R 11, in which R10 and R11, which may be identical or different, represent H or a saturated hydrocarbon-based aliphatic group; R1 and R2, which may be identical or different, represent H or a saturated aliphatic hydrocarbon-based chain; or alternatively R1 and R2 together form an optionally substituted saturated aliphatic hydrocarbon-based chain; the radicals R3 and R4, which may be identical or different, take any of the is meanings given above for R1 and R2, or alternatively R1 and the group R4 borne by the carbon alpha to CR1R 2 represent nothing and a double bond links the CR1R 2 carbon to the alpha CR3R4 carbon; or alternatively one of the radicals R1 and R2 forms with one of the radicals R3 and R4 an optionally substituted saturated or unsaturated aliphatic hydrocarbon- based chain; one of the radicals R5 and R6 represents W, and the other represents Z which is chosen from a saturated or unsaturated aliphatic hydrocarbon-based radical; an optionally substituted, saturated, unsaturated and/or aromatic carbocyclic or heterocyclic radical; a radical -alk-Cy, in which alk represents an alkylene chain and Cy represents an optionally substituted saturated, unsaturated and/or aromatic heterocyclic or carbocyclic radical; W represents -XL-CO2R7;-X-L-Tet, in which X and L are as defined below and Tet represents optionally substituted tetrazole; in which L represents a saturated or unsaturated aliphatic hydrocarbon-based chain, which is optionally substituted and/or optionally interrupted by optionally substituted arylene; X represents O; NR8, in which R8 represents H; a saturated aliphatic hydrocarbon-based group; a group -CO-R' or -SO2-R', in which R' takes any of the meanings given below for R7 with the exception of H; or R8 represents an optionally substituted aromatic carbocyclic group; or X represent S(O)m, in which m is chosen from 0, 1 and 2; R7 represents H; a saturated or unsaturated aliphatic hydrocarbon-based group; an optionally substituted, saturated, unsaturated and/or aromatic carbocyclic group; an optionally substituted, saturated, unsaturated and/or aromatic heterocyclic group; and the pharmaceutically acceptable derivatives, salts, solvates and stereoisomers thereof, and also mixtures thereof in all proportions, which can be used in the treatment of dyslipidaemia, atherosclerosis and diabetes.

    Abstract translation: 本发明涉及式（（I）的化合物：其中：n是选自1,2和3的整数; Y表示O; N-OR 9，其中R9表示H或饱和烃基脂族基团 CR10R 11，其中R10和R11可以相同或不同，表示H或饱和烃基脂族基; R1和R2可以相同或不同，代表H或饱和脂族烃基链; 或者R 1和R 2一起形成任选取代的饱和脂族烃基链;基团R 3和R 4可以相同或不同，具有上面对R 1和R 2给出的任何含义，或者R 1和R 4 由CR1R 2的碳α承担，并且双键将CR1R2碳连接到αCR 3 R 4碳;或者基团R 1和R 2中的一个与基团R 3和R 4之一形成任选取代的饱和或不饱和脂族 地烃基 基于链的; 基团R5和R6之一表示W，另一个表示选自饱和或不饱和脂族烃基的基团的Z; 任选取代的饱和，不饱和和/或芳族碳环或杂环基; 一个自由基-alk-Cy，其中alk代表亚烷基链，Cy代表任选取代的饱和，不饱和和/或芳族杂环或碳环基团; W表示-XL-CO 2 R 7; -X-L-Tet，其中X和L如下所定义，Tet表示任选取代的四唑; 其中L表示饱和或不饱和的脂族烃基链，其任选被任选取代的和/或任选地被任选取代的亚芳基中断; X表示O; NR8，其中R8表示H; 饱和脂族烃基; 基团-CO-R'或-SO 2 -R'，其中R'取代以下对R 7的任何含义，除了H; 或R 8表示任选取代的芳族碳环基团; 或X表示S（O）m，其中m选自0,1和2; R7表示H; 饱和或不饱和脂族烃基; 任选取代的，饱和的，不饱和的和/或芳族的碳环基团; 任选取代的饱和，不饱和和/或芳族杂环基; 和其药学上可接受的衍生物，盐，溶剂合物和立体异构体，以及其各种比例的混合物，其可用于治疗血脂异常，动脉粥样硬化和糖尿病。

    선택적인 뉴로키닌 길항제
    89.
    发明公开
    선택적인 뉴로키닌 길항제 无效
    选择性神经营养因子拮抗剂

    公开(公告)号：KR1020020067548A

    公开(公告)日：2002-08-22

    申请号：KR1020027007620

    申请日：2000-12-14

    Applicant: 머크 샤프 앤드 돔 코포레이션

    Inventor： 쉬넹-양 ,  슈호-제인 ,  리챠드그레고리에이. ,  팔리왈수닐 ,  블리씬데이비드제이. ,  피윈스키죤제이. ,  샤오동 ,  첸샤오

    IPC: C07D413/10

    CPC classification number: C07D239/10 ,  C07C45/71 ,  C07C217/48 ,  C07D211/58 ,  C07D233/14 ,  C07D233/16 ,  C07D233/22 ,  C07D233/30 ,  C07D233/32 ,  C07D233/42 ,  C07D233/46 ,  C07D233/48 ,  C07D233/78 ,  C07D285/10 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D409/06 ,  C07D413/04 ,  C07D413/06 ,  C07D413/10 ,  C07F9/65061 ,  C07C47/575

    Abstract: 본원에는다음화학식 I의화합물또는이의약제학적으로허용되는염, 이러한화합물을사용하여뉴로키닌길항제로의치료에감수성인질병을치료하는방법, 및상기화합물을포함하는약제학적조성물이기재되어있다: 화학식 I 상기식에서, Ar및 Ar는임의로치환된헤테로아릴또는임의로치환된페닐이고; X은 -O-, -S-, -SO-, -SO-, -NR-, -NCOR- 또는 -NRSOR-이며; 은다음으로이루어진그룹중에서선택되며 X는 -O-, -S- 또는 -NR-이고; Y는 =O, =S 또는 =NR이며; Y은 H, C-C알킬, -NRR, -SCH, R-아릴(CH)-, R-헤테로아릴-(CH)-, -(CH)-헤테로사이클로알킬, -(C-C)알킬-NH-C(O)O(C-C)알킬또는 -NHC(O)R이고; R는 H 또는 -(CH)-G이며, n은 0 내지 5이고, G는 H, -CF, -CHF, -CHF, -OH, -O-(C-C알킬), -SOR, -O-(C-C사이클로알킬), -NRR, -SONRR, -NRSOR, -NRCOR, -NR(CONRR), -CONRR, -COOR, C-C사이클로알킬, R-아릴, R-헤테로아릴인데, 단 n이 0인경우에는 G가 H가아니며; R, R, R및 R은 H, 알킬, 사이클로알킬, -CHF, -CHF 또는 -CF이거나; R및 R는이들이부착된탄소와함께, 알킬렌환을형성하거나; 또는 R및 R는함께 =O이고; R은 R또는 -OH이며; 나머지변수들은본원명세서에서정의된바와같다. 본원에는또한, 청구항 1의화합물의유효량및 하나이상의약제학적으로허용되는담체를, 선택적인세로토닌재흡수억제제의유효량과조합하여포함하는약제학적조성물이기재되어있다.

    Abstract translation: 由结构式（I）表示的化合物或其药学上可接受的盐，其中Ar 1和Ar 2是任选取代的杂芳基或任选取代的苯基; X 1是-O - ， - S - ， - SO - ， - SO 2 - ， - NR 12 - ， - NR C 12 - 或-NR 12 SO 2 R 15。 （a）选自（b），（c），（d）和（e）; X 2是-O - ， - S-或-NR 5 - ; Y = O，= S或= NR 11; Y 1是H，C 1 -C 6烷基，-NR 17 R 13，-SCH 3，R 19 - 芳基（CH 2）n6-，R 19 - 杂芳基 - （CH 2）n6-， - （CH 2）n 6-杂环烷基， - （C 1 -C 3）烷基-NH-C（O）O（C 1 -C 6）烷基或-NHC（O）R 15; R 5是H或 - （CH 2）n1-G，其中n1是0-5G是H，-CF3，-CHF2，-CH2F，-OH，-O-（C1-C6烷基），-SO2R 13 C，-O-（C 3 -C 8环烷基），-NR 13 R 14，-SO 2 NR 13 R 14，-NR 13 SO 2 R 15，-NR 13 COR R 12，-NR 12（CONR 13 R 14），-CONR 13 R 14，-COOR 12，C 3 -C 8环烷基，R 19 - 芳基，R 19 当n1 = 0时，G不为H; R 1，R 2，R 3和R 7是H，烷基，环烷基，-CHF 2，-CH 2 F或-CF 3; 或R 1和R 2与它们所连接的碳一起形成亚烷基环; 或R 1和R 2一起为= O; R 6是R 7或-OH; 并且剩余的变量如规定中所定义，治疗易受神经激肽拮抗剂治疗的疾病的方法，以及包含所述化合物的药物组合物。 还公开了包含有效量的权利要求1的化合物，至少一种药学上可接受的载体和与有效量的选择性5-羟色胺再摄取抑制剂组合的药物组合物。

    4-히드록시벤즈알데히드 및 그의 유도체의 제조 방법
    90.
    发明公开
    4-히드록시벤즈알데히드 및 그의 유도체의 제조 방법 无效
    制备4-羟基苯甲醛和衍生物的方法

    公开(公告)号：KR1020000053360A

    公开(公告)日：2000-08-25

    申请号：KR1019997004388

    申请日：1997-11-19

    Applicant: 로디아 쉬미

    Inventor： 메띠비에빠스깔

    IPC: C07C45/67

    CPC classification number: C07C45/676 ,  C07C39/11 ,  C07C41/30 ,  C07C45/38 ,  C07C51/235 ,  C07C47/58 ,  C07C47/575 ,  C07C65/21 ,  C07C43/23

    Abstract: PURPOSE: Provided is a method for preparing a 4-hydroxybenzaldehyde and derivatives. More particularly it concerns the preparation of 3-methoxy-4-hydroxybenzaldehyde and of 3-ethoxy-4-hydroxybenzaldehyde called "vanillin" and "ethylvanillin" respectively. CONSTITUTION: A method for preparing a 4-hydroxybenzaldehyde and derivatives is characterized in that it consists in selectively oxidising the group in position 2 relative to the hydroxyl group, in carboxylic group, present in the phenolic compounds of a mixture containing at least: a phenolic compound (A) bearing formyl and/or hydroxymethyl groups in position 2 and 4; a phenolic compound (B) bearing a formyl or hydroxymethyl group in position 4; a phenolic compound (C) bearing a formyl or hydroxymethyl group in position 2; thus leading to a mixture containing a 3-carboxy-4-hydroxybenzaldehyde, a 4-hydroxybenzaldehyde, a 2-hydroxybenzoic acid, which is then subjected to a decarboxylation for obtaining the 4-hydroxybenzaldehyde and a phenol which can be optionally recycled.

    Abstract translation: 目的：提供4-羟基苯甲醛及其衍生物的制备方法。 更具体地，涉及分别称为“香草醛”和“乙基香草醛”的3-甲氧基-4-羟基苯甲醛和3-乙氧基-4-羟基苯甲醛的制备。 构成：一种制备4-羟基苯甲醛及其衍生物的方法的特征在于它包括选择性氧化相对于羟基的位置2的基团，在羧基中存在于至少含有酚类的混合物的酚类化合物中 位置2和4中含有甲酰基和/或羟甲基的化合物（A）; 在4位带有甲酰基或羟甲基的酚类化合物（B） 在2位含有甲酰基或羟甲基的酚类化合物（C） 从而导致含有3-羧基-4-羟基苯甲醛，4-羟基苯甲醛，2-羟基苯甲酸的混合物，然后将其进行脱羧以获得4-羟基苯甲醛和可任意回收的苯酚。

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