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    Synthesis of antiulcer compounds
    1.
    发明授权
    Synthesis of antiulcer compounds 失效
    抗溃疡化合物的合成

    公开(公告)号：US5030738A

    公开(公告)日：1991-07-09

    申请号：US527680

    申请日：1990-05-22

    申请人： Alberto Reiner

    发明人： Alberto Reiner

    IPC分类号： C07C335/06 ,  C07C67/00 ,  C07C313/00 ,  C07C323/25 ,  C07C323/44 ,  C07C325/00 ,  C07D233/64 ,  C07D307/52 ,  C07D317/58 ,  C07D407/00 ,  C07D407/12

    CPC分类号： C07D407/12 ,  C07D317/58

    摘要： To synthesize molecules with antiulcer action, specifically ranitidine, niperotidine and cimetidine, having the formula: ##STR1## wherein R.sub.1 is hydrogen or together with R.sub.2 represents the rest of a cycloaliphatic or heterocyclic optionally substituted ring with 5 or 6 carbon atoms, R.sub.2 represents H, alkyl, alkyl substituted with a simple or substituted aromatic ring or with a single or substituted heterocyclic ring, Ar represents a simple or substituted phenyl group, a simple or substituted heterocyclic aromatic group, N=1, 2, 3, 4, 5 or 6 and X represents CH--NO.sub.2, S, N--C.tbd.N, the compound (II) is prepared through the following process sequence: ##STR2## wherein Z=H, NO.sub.2, halogen and R.sub.3 =--(CH.sub.2).sub.n Ar, --(CH.sub.2).sub.n --SH, --(CH.sub.2).sub.n --S--S--(CH.sub.2).sub.n, --(CH.sub.2).sub.n --S--CH.sub.2 Ar Y being halogen.The urea of formula ##STR3## is converted in a first stage into the corresponding carbodiimide ##STR4## by reaction with triphenylphosphine and bromine in the presence of a strong base and in a second stage is obtained the desired compound by reaction with nitromethane or with a saline derivative of cynamide.

    摘要翻译： 为了合成具有抗溃疡作用的分子，特别是具有以下分子式的雷尼替丁，尼泊替定和西咪替丁：其中R1是氢或与R2一起代表其余的具有5或6个碳原子的脂环族或杂环任意取代的环， R 2表示H，烷基，被简单或取代的芳环或单取代的杂环取代的烷基，Ar表示简单或取代的苯基，简单或取代的杂环芳基，N = 1,2,3,4 ，5或6，X表示CH-NO 2，S，NC 3 N N，化合物（II）通过以下方法制备：其中Z = H，NO2 卤素和R 3 = - （CH 2）n Ar， - （CH 2）n -SH， - （CH 2）nSS-（CH 2）n - ，（CH 2）n S-CH 2 Ar Y是卤素。 通过在强碱的存在下，通过与三苯基膦和溴反应，将式（II）的脲在第一阶段转化成相应的碳二亚胺（VI），并且在第二阶段中通过 与硝基甲烷或与cynamide的盐水衍生物反应。

    2,4-pentadienoic acid derivatives having retinoid-like biological activity
    3.
    发明授权
    2,4-pentadienoic acid derivatives having retinoid-like biological activity 失效
    具有类视黄醇样生物活性的2,4-戊二烯酸衍生物

    公开(公告)号：US6114533A

    公开(公告)日：2000-09-05

    申请号：US390825

    申请日：1999-09-07

    申请人： Vidyasagar Vuligonda ,  Roshantha A. Chandraratna

    发明人： Vidyasagar Vuligonda ,  Roshantha A. Chandraratna

    IPC分类号： A61K31/35 ,  A61K31/20 ,  A61K31/23 ,  A61K31/38 ,  A61K31/47 ,  A61P17/00 ,  A61P43/00 ,  C07C57/50 ,  C07C69/618 ,  C07C215/02 ,  C07C215/18 ,  C07C311/58 ,  C07C335/06 ,  C07C403/00 ,  C07D277/22 ,  C07D311/58 ,  C07D333/54 ,  C07D335/06 ,  C07D215/06 ,  C07D215/12

    CPC分类号： C07D333/54 ,  A61K31/20 ,  A61K31/23 ,  C07C57/50 ,  C07C69/618 ,  C07D311/58 ,  C07D335/06

    摘要： Compounds of Formula 1 ##STR1## wherein Z is Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is phenyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is NR.sub.5 ; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lover alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and a is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, CR.sub.7 OR.sub.13 O, or tri-lower alkylsilyl, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 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Z是式3，Y是任选被一个或两个R 4基团取代的3至8个碳的环烷基或环烯基，或Y是苯基，所述基团任选被一个或两个R 4基团取代，二价Y基团 被相邻碳上的Z和-CR1 = CR1-CR1 = CR1基团取代; X是NR5; R1和R2独立地为H，低级烷基或氟代烷基; R3是氢，有情人烷基，Cl或Br; R4是低级烷基，氟烷基或卤素; R5是H或低级烷基，a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） CR 7OR 13 O或三低级烷基甲硅烷基，其中R 7为含有1至5个碳的烷基，环烷基或烯基，R 8为碳原子数1至10的烷基，碳原子数为5至10的环烷基或烷基具有的三甲基甲硅烷基烷基 1至10个碳，或R8为苯基或低级烷基苯基，R9和R10独立地为氢，1-10个碳原子的烷基或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，具有类视黄醇类生物活性。

    2,4-Pentadienoic acid derivatives having retinoid-like biological activity
    4.
    发明授权
    2,4-Pentadienoic acid derivatives having retinoid-like biological activity 失效
    具有类视黄醇样生物活性的2,4-二戊烯酸衍生物

    公开(公告)号：US5780647A

    公开(公告)日：1998-07-14

    申请号：US805793

    申请日：1997-02-25

    申请人： Vidyasagar Vuligonda ,  Roshantha A. Chandraratna

    发明人： Vidyasagar Vuligonda ,  Roshantha A. Chandraratna

    IPC分类号： A61K31/35 ,  A61K31/20 ,  A61K31/23 ,  A61K31/38 ,  A61K31/47 ,  A61P17/00 ,  A61P43/00 ,  C07C57/50 ,  C07C69/618 ,  C07C215/02 ,  C07C215/18 ,  C07C311/58 ,  C07C335/06 ,  C07C403/00 ,  C07D277/22 ,  C07D311/58 ,  C07D333/54 ,  C07D335/06 ,  C07D311/04 ,  C07D409/02

    CPC分类号： C07D333/54 ,  A61K31/20 ,  A61K31/23 ,  C07C57/50 ,  C07C69/618 ,  C07D311/58 ,  C07D335/06

    摘要： Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, CR.sub.7 OR.sub.13 O, or tri-lower alkylsilyl, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 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Z选自由式2和式3所示的基团组成的组。式3 Y是3至8个碳的环烷基或环烯基，任选地 被一个或两个R 4基取代，或Y选自苯基，吡啶基，噻吩基，呋喃基，吡咯基，哒嗪基，嘧啶基，吡嗪基，噻唑基，恶唑基和咪唑基，所述基团任选被一个或两个R 4基团取代，二价 Y基团被相邻碳上的Z和-CR1 = CR1-CR1 = CR1基团取代; X是S，O或NR5; n为1或2; R1和R2独立地为H，低级烷基或氟代烷基; R3是氢，低级烷基，Cl或Br; R4是低级烷基，氟烷基或卤素; R 5是H或低级烷基，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） CR 7OR 13 O或三低级烷基甲硅烷基，其中R 7为含有1至5个碳的烷基，环烷基或烯基，R 8为碳原子数1至10的烷基，碳原子数为5至10的环烷基或烷基具有的三甲基甲硅烷基烷基 1至10个碳，或R8为苯基或低级烷基苯基，R9和R10独立地为氢，1-10个碳原子的烷基或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，具有类视黄醇类生物活性。

    Phenethyl-thiourea compounds and use
    10.
    发明授权
    Phenethyl-thiourea compounds and use 失效
    苯乙基 - 硫脲化合物和用途

    公开(公告)号：US6362228B2

    公开(公告)日：2002-03-26

    申请号：US74256300

    申请日：2000-12-20

    申请人： PARKER HUGHES INST

    发明人： UCKUN FAITH M ,  VENTATACHALAM TARACAD K

    IPC分类号： A61K31/44 ,  A61P31/18 ,  C07D213/75 ,  A61K31/17 ,  C07C335/06

    CPC分类号： C07D213/75

    摘要： Novel phenylethyl-thiourea (PHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.

    摘要翻译： 新型苯乙基 - 硫脲（PHET）化合物作为逆转录酶的抑制剂和用于治疗HIV感染的有效药物，包括突变型，药物敏感型，耐药性和多重耐药性HIV病毒株。