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    Process for preparation of substituted amino alcohols
    22.
    发明申请
    Process for preparation of substituted amino alcohols 失效
    取代氨基醇的制备方法

    公开(公告)号：US20050124806A1

    公开(公告)日：2005-06-09

    申请号：US11006936

    申请日：2004-12-08

    Applicant: Yanzhong Wu ,  Arkadiy Rubezhov ,  Jean Schmid ,  Jay Afragola

    Inventor： Yanzhong Wu ,  Arkadiy Rubezhov ,  Jean Schmid ,  Jay Afragola

    IPC: C07C213/02 ,  C07C213/04 ,  C07C215/08 ,  C07D487/04 ,  C07D265/30 ,  C07D207/46 ,  C07D211/20

    CPC classification number: C07D487/04 ,  C07C213/02 ,  C07C215/08

    Abstract: There is provided a process for the preparation of substituted amino alcohols HO—(CH2)n—NR1R2 from haloalcohols HO—(CH2)n—X, where X is Cl, Br or I, by reaction with an amine HNR1R2, in water as solvent at a temperature range of about 20° C. to about 90° C. optionally in the presence of a catalytic amount of an iodide source metal iodides. The haloalcohols are useful in the preparation of 6-[(substituted)phenyl]-triazolopyrimidine compounds which are useful in the treatment of cancer.

    Abstract translation: 提供了用于制备取代的氨基醇HO-（CH 2）n - NR 1 - ， - O 2的方法， 其中X是Cl，Br或I，通过与胺HNR 1反应而得到的卤代醇HO-（CH 2）n -X 在约20℃至约90℃的温度范围内的水溶液中，任选地在催化量的碘化物源金属碘化物的存在下进行。 卤代醇可用于制备可用于治疗癌症的6 - [（取代的）苯基] - 三唑并嘧啶化合物。

    Amine derivative with potassium channel regulatory function, its preparation and use
    24.
    发明申请
    Amine derivative with potassium channel regulatory function, its preparation and use 有权
    胺衍生物具有钾通道调节功能，其制备和应用

    公开(公告)号：US20040266822A1

    公开(公告)日：2004-12-30

    申请号：US10466712

    申请日：2004-08-12

    Inventor： Hai Wang ,  Liuhong Yun ,  Huasong Feng ,  Fulin Li ,  Xingehun Tang ,  Huamei He ,  Rifang Yang ,  Wenyu Cui ,  Qixiu Gao ,  Gang Hu ,  Rusheng Zhao ,  Wei Liu ,  Chaoliang Long ,  Lin Wang ,  Xinqiang Lu ,  Lijun Liu ,  Yuan Yan

    IPC: C07D211/20 ,  A61K031/445 ,  A01N043/36 ,  C07D207/04 ,  A61K031/13

    CPC classification number: C07D213/82 ,  A61K31/13 ,  C07C211/08

    Abstract: The present invention provides amine derivatives represented by formula I, its isomers, racemes or optical isomers, pharmaceutical salts thereof, its amides or esters, pharmaceutical compositions containing said compounds and the preparation methods thereof. The invention also relates to the use of the above mentioned compounds in the preparation of drugs for the prophylaxis or treatment of cardiovascular diseases, diabetes, bronchial and urinary smooth muscle spasm as well as ischemic and anoxic nerve injury. The above compounds can be used to treat hypertension, angina diaphragmatic, myocardial infarction, congestive heart failure, arrhythmia, diabetes, spasmodic bronchial diseases, spasmodic bladder or ureter diseases, and depression. 1

    Abstract translation: 本发明提供由式I表示的胺衍生物，其异构体，消旋体或光学异构体，其药用盐，其酰胺或酯，含有所述化合物的药物组合物及其制备方法。 本发明还涉及上述化合物在制备用于预防或治疗心血管疾病，糖尿病，支气管和尿平滑肌痉挛以及缺血性和缺氧性神经损伤的药物中的用途。 上述化合物可用于治疗高血压，心绞痛，心肌梗塞，充血性心力衰竭，心律失常，糖尿病，痉挛性支气管疾病，痉挛性膀胱或输尿管疾病以及抑郁症。

    Triphenylalkene derivatives and their use as selective estrogen receptor modulators
    27.
    发明申请
    Triphenylalkene derivatives and their use as selective estrogen receptor modulators 有权
    三苯基烯烃衍生物及其作为选择性雌激素受体调节剂的用途

    公开(公告)号：US20030225130A1

    公开(公告)日：2003-12-04

    申请号：US10408303

    申请日：2003-04-08

    Applicant: HORMOS MEDICAL OY LTD.

    Inventor： Marja-Liisa Sodervall ,  Arja Kalapudas ,  Lauri Kangas ,  Risto Lammintausta ,  Pirkko Harkonen ,  Kalervo Vaananen

    IPC: A61K031/445 ,  C07D211/26 ,  C07D211/20 ,  A61K031/40 ,  C07D207/08 ,  C07D207/10 ,  A61K031/137

    CPC classification number: C07D295/088 ,  C07C43/225 ,  C07C43/23 ,  C07C59/68 ,  C07C211/10 ,  C07C215/16 ,  C07C217/20 ,  C07C323/12 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

    Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula: 1 wherein R1 and R2, which are the same or different are a) H, halogen, OCH3, OH; or 2 nullwhere X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, nullCH2CnullCH or nullCH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or c) nullYnull(CH2)nCH2nullOnullR6 nullwhere Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, nullCH2CH2OH, or nullCH2CH2Cl; or d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and R3 is H, halogen, OH or nullOCH3; stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.

    Abstract translation: 本发明提供了以下通式的新型选择性雌激素受体调节剂化合物：其中相同或不同的R 1和R 2是a）H，卤素，OCH 3，OH; 或其中X为O，NH或S; n为1〜4的整数。 和R 4和R 5相同或不同，为1至4个碳原子的烷基，H，-CH 2 C = CH或-CH 2 CH 2 OH; 或R 4和R 5形成含N的五元或六元环或杂芳环; 或c）-Y-（CH 2）n CH 2 -O-R 6，其中Y是O，NH或S，n是1至4的整数; 并且R 6是H，-CH 2 CH 2 OH或-CH 2 CH 2 Cl; 或d）2,3-二羟基丙氧基，2-甲基亚磺酰基乙氧基，2-氯乙氧基，1-乙基-2-羟基乙氧基，2,2-二乙基-2-羟基乙氧基或羧甲氧基; 且R 3为H，卤素，OH或-OCH 3; 其立体异构体及其无毒的药学上可接受的盐和酯及其混合物，其表现出有价值的药理学性质。

    Method for the production of $g(v)-aminoalkylsphonic acids
    29.
    发明申请
    Method for the production of $g(v)-aminoalkylsphonic acids 失效
    生产$ g（v） - 氨基烷基苯磺酸的方法

    公开(公告)号：US20030187295A1

    公开(公告)日：2003-10-02

    申请号：US10275753

    申请日：2002-11-08

    Inventor： Volker Schaefer ,  Wolfgang Knoll ,  Alexander Schmitt ,  Christoph Huettner

    IPC: C07D211/20 ,  C07D207/04 ,  C07C39/14 ,  C07D279/12

    CPC classification number: C07D295/088 ,  C07C303/02 ,  C07C309/14

    Abstract: The invention relates to a method for the production of null-aminoalkylsulphonic acids of general formula (I), where R1 and R2nulloptionally substituted alkyl groups with 1 20 C atoms and nnulla whole number from 2 6, whereby an amine of formula (II), where R1 and R2 have the above meanings is reacted with an alkyl dihalide of formula (III), where n has the above meaning and X1 and X2nullchlorine or bromine, with addition of alkali hydroxide at a pH of 8 10. The pH is then adjusted to a value of 0 1, by addition of a hydrohalic acid and excess alkyl dihalide is separated off, before the reaction solution is adjusted to a pH of 6 7.5 with alkali liquor, alkali sulphite is added and the product (I) formed at elevated temperate.

    Abstract translation: 本发明涉及一种制备通式（I）的ω-氨基烷基磺酸的方法，其中R 1和R 2 =具有1-20个碳原子的任选取代的烷基，n = 2-6的整数，由此得到式 （II），其中R1和R2具有上述含义与式（III）的烷基二卤化物反应，其中n具有上述含义，X 1和X 2 =氯或溴，加入pH8.0的碱金属氢氧化物 然后，通过加入氢卤酸将pH调节至零值，分离出过量的烷基二卤化物，然后用碱液将反应溶液调节至pH6.5的pH，并加入碱金属亚硫酸盐 （I）在升高的温度下形成。

    Method for producing delta-aminopentadienoate derivatives
    30.
    发明申请
    Method for producing delta-aminopentadienoate derivatives 失效
    生产δ-氨基戊二酸衍生物的方法

    公开(公告)号：US20030181483A1

    公开(公告)日：2003-09-25

    申请号：US10395166

    申请日：2003-03-25

    Inventor： Akihiko Ikegawa ,  Masuji Motoki ,  Katsuyoshi Yamakawa

    IPC: A61K031/445 ,  A61K031/40 ,  A61K031/22 ,  C07D211/20

    CPC classification number: C07C227/02 ,  C07C315/04 ,  C07C317/48

    Abstract: The invention is a method for producing null-aminopentadienoate derivatives of formula (1), the method comprising reacting a streptocyanine derivative of formula (2) with an ester derivative of formula (3) in the presence of an organic base. In formulae (1) to (3), R1 represents an alkyl group or an aryl group; R2, R3, R4 and R5 independently represent a hydrogen atom or an alkyl group; R2 and R3, or R4 and R5 may bond to each other to form a ring; Y represents an electron attractive group; X represents an acid radical; n indicates 0 or a positive number, which is no more than 5; Y may bond to R1 to form a ring. 1

    Abstract translation: 本发明是一种生产式（1）的三氨基戊二酸衍生物的方法，该方法包括使式（2）的链花青衍生物与式（3）的酯衍生物在有机碱的存在下反应。 在式（1）至（3）中，R 1表示烷基或芳基; R 2，R 3，R 4和R 5独立地表示氢原子或烷基; R 2和R 3，或R 4和R 5可以彼此键合形成环; Y表示吸电子基团; X表示酸基; n表示0或正数，不大于5; Y可以与R 1键合形成环。

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