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    Derivatives of thienylacetic acid amides and their pharmaceutically acceptable acid salts and a process for the preparation thereof
    2.
    发明授权
    Derivatives of thienylacetic acid amides and their pharmaceutically acceptable acid salts and a process for the preparation thereof 失效
    噻吩乙酸酰胺衍生物及其药学上可接受的酸式盐及其制备方法

    公开(公告)号：US4499286A

    公开(公告)日：1985-02-12

    申请号：US554416

    申请日：1983-11-22

    Applicant: Dieter Binder

    Inventor： Dieter Binder

    IPC: A61K31/38 ,  A61K31/381 ,  A61P25/04 ,  C07D333/24 ,  C07D333/28 ,  C07C103/82

    CPC classification number: C07D333/24 ,  C07D333/28

    Abstract: Novel derivatives of thienylacetic acid amides of the general formula ##STR1## in which the two nitrogens on the cyclohexane ring are transconnected, the basic acetic acid amide radical is in position 2 or 3 of the thiophene nucleus, R is C.sub.1 -C.sub.3 alkyl, R.sub.1 and R.sub.2 are independently C.sub.1 -C.sub.3 -alkyl or represent together with the nitrogen atom to which they are attached a pyrrolidine or piperidine ring and X and Y are independently hydrogen, chlorine or bromine in position 2 to 5 of the thiophene nucleus in dependence on the position of the basic acetic acid amide group, and their pharmaceutically acceptable acid addition salts are .mu.-specific analgetics, which do not cause any physical dependence. Therefore, they are suitable for protracted treatment of pain conditions.

    Abstract translation: 环己烷环上的两个氮原子转移的通式为“IMAGE”（I）的噻吩乙酸酰胺的新型衍生物，碱性乙酸酰胺基位于噻吩核的2位或3位，R为C1-C3 烷基，R 1和R 2独立地为C 1 -C 3 - 烷基，或与它们所连接的氮原子一起与吡咯烷或哌啶环一起表示，并且X和Y独立地为噻吩核的2至5位的氢，氯或溴。 对碱性乙酸酰胺基的位置的依赖性及其药学上可接受的酸加成盐是mu特异性止痛剂，其不会引起任何物理依赖性。 因此，它们适合于持续治疗疼痛状况。

    Aromatic amine-amides and use as chain-extenders
    4.
    发明授权
    Aromatic amine-amides and use as chain-extenders 失效
    芳香胺酰胺，用作扩链剂

    公开(公告)号：US4191706A

    公开(公告)日：1980-03-04

    申请号：US895840

    申请日：1978-04-13

    Applicant: Edward T. Marquis ,  Ernest L. Yeakey

    Inventor： Edward T. Marquis ,  Ernest L. Yeakey

    IPC: C08G18/00 ,  C07C67/00 ,  C07C231/00 ,  C07C231/02 ,  C07C231/10 ,  C07C237/32 ,  C07C255/58 ,  C08G18/38 ,  C08G18/50 ,  C08G18/65 ,  C08G18/82 ,  C08G65/333 ,  C07C103/28 ,  C07C99/04 ,  C07C103/78 ,  C07C103/82

    CPC classification number: C08G65/33396 ,  C08G18/5039

    Abstract: Covers certain aromatic-amine amides which comprise the reaction product of a polyoxypropylene polyamine selected from the group consisting of diamines, triamines and mixtures thereof, and having an average molecular weight of 190 to about 3000 and an isatoic anhydride of the formula: ##STR1## where R is selected from the group consisting of hydrogen, alkyl, nitro, halo, hydroxy, amino, and cyano, and n is a number of 1-4. Also covers the use of said compounds as chain-extenders in polyurethane compositions. Such chain-extenders provide for the production of polyurethane elastomers having improved tensile strength, tear strength and elongation properties.

    Abstract translation: 涵盖某些芳族胺酰胺，其包含选自二胺，三胺及其混合物，并且具有190至约3000的平均分子量的聚氧丙烯多胺的反应产物和下式的盐酸酐： 其中R选自氢，烷基，硝基，卤素，羟基，氨基和氰基，n为1-4的数。 还涉及所述化合物在聚氨酯组合物中作为增链剂的用途。 这种增链剂提供具有改进的拉伸强度，撕裂强度和伸长性能的聚氨酯弹性体的生产。

    1-Phenyl-2-aminoethanol derivatives
    6.
    发明授权
    1-Phenyl-2-aminoethanol derivatives 失效
    1-苯基-2-氨基乙醇衍生物

    公开(公告)号：US4303649A

    公开(公告)日：1981-12-01

    申请号：US43425

    申请日：1979-05-29

    Applicant: Geraint Jones

    Inventor： Geraint Jones

    IPC: A61K31/16 ,  A61K31/165 ,  A61K31/22 ,  A61K38/00 ,  A61P17/00 ,  C07C237/10 ,  C07C237/22 ,  C07K1/113 ,  C07K5/04 ,  C07K5/06 ,  C07C103/82

    CPC classification number: C07K5/06026 ,  A61K38/00

    Abstract: The invention concerns new topical anti-inflammatory 1-phenyl-2-aminoethanol derivatives of the general formula:R.sup.1 .multidot.CH(OH).multidot.CH.sub.2 NH.multidot.CR.sup.2 R.sup.3 .multidot.A.sup.1 .multidot.NH[CO.multidot.Y.multidot.NH].sub.n .multidot.Qwherein R.sup.1 is a phenyl bearing specific combinations of (2-12C)alkanoyloxy,[(2-12C)alkanoyloxy]methyl,chloro and amino substituents, R.sup.2 and R.sup.3 are independently hydrogen or (1-4C)alkyl, A.sup.1 is a (1-4C)alkylene, Y is a (1-4C)alkylene optionally bearing a (1-4C)alkyl or benzyl, n is an integer from 1 to 4, and Q is an optionally substituted benzoyl, phenylacetyl, or phenoxyacetyl together with the acid-addition salts thereof; and the pharmaceutical compositions thereof, for use in the treatment of inflammatory skin diseases and conditions. The invention also concerns processes for the manufacture of derivatives of formula I.A representative compound of the invention is 1-[3,4-bis(pivaloyloxy)phenyl]-2-{2-[(N-benzoylglycyl)amino]-1,1-dimethyl-ethylamino}ethanol.

    Abstract translation: 本发明涉及以下通式的新的局部抗炎1-苯基-2-氨基乙醇衍生物：R1xCH（OH）xCH2NHxCR2R3xA1xNH [COxYxNH] nxQ其中R1是具有（2-12C）烷酰氧基，[（2- 12C）烷酰氧基]甲基，氯和氨基取代基，R2和R3独立地为氢或（1-4C）烷基，A1为（1-4C）亚烷基，Y为（1-4C） 4C）烷基或苄基，n是1至4的整数，Q是任选取代的苯甲酰基，苯乙酰基或苯氧基乙酰基及其酸加成盐; 及其药物组合物，用于治疗炎性皮肤疾病和病症。 本发明还涉及制备式I衍生物的方法。本发明的代表性化合物是1- [3,4-双（新戊酰氧基）苯基] -2- {2 - [（N-苯甲酰基甘氨酰基）氨基] -1 ，1-二甲基 - 乙基氨基}乙醇。

    Substituted anilide esters of PGE.sub.1
    8.
    发明授权
    Substituted anilide esters of PGE.sub.1 失效
    取代的PGE（HD 1

    公开(公告)号：US3968140A

    公开(公告)日：1976-07-06

    申请号：US431599

    申请日：1974-01-08

    Applicant: Walter Morozowich

    Inventor： Walter Morozowich

    IPC: C07C405/00 ,  C07C133/08 ,  C07C103/82

    CPC classification number: C07C405/00

    Abstract: Substituted phenyl and naphthyl esters of PGE.sub.1, 15-alkyl-PGE.sub.1, and 15(R)-15-alkyl-PGE.sub.1, and their racemic forms, and processes for producing them are disclosed. The products are useful for the same pharmacological and medical purposes as PGE.sub.1, 15-alkyl-PGE.sub.1, and 15(R)-15-alkyl-PGE.sub.1, and are also useful as a means for obtaining highly purified PGE.sub.1, 15-alkyl-PGE.sub.1, and 15(R)-15-alkyl-PGE.sub.1 products.

    Abstract translation: 公开了取代的PGE1,15-烷基-GE-PGE1和15（R）-15-烷基-GE-PGE1的苯基和萘基酯及其外消旋形式及其制备方法。 该产品可用于与PGE1,15-烷基-GE-PGE1和15（R）-15-烷基-GFPE1相同的药理学和医学目的，并且也可用作获得高度纯化的PGE1,15-烷基-GE-PGE1的手段 和15（R）-15-烷基-PGEE产物。

    Substituted tolyl esters of PGA.sub.2
    9.
    发明授权
    Substituted tolyl esters of PGA.sub.2 失效
    取代的PGA的甲苯基酯（HD 2

    公开(公告)号：US3932486A

    公开(公告)日：1976-01-13

    申请号：US531992

    申请日：1974-12-12

    Applicant: Walter Morozowich

    Inventor： Walter Morozowich

    IPC: C07C405/00 ,  C07C133/08 ,  C07C103/82

    CPC classification number: C07C405/00 ,  Y10S514/826

    Abstract: Substituted phenyl and naphthyl esters of PGA.sub.2, 15-alkyl-PGA.sub.2, and 15(R)-15-alkyl-PGA.sub.2, and their racemic forms, and processes for producing them are disclosed. The products are useful for the same pharmacological and medical purposes as PGA.sub.2, 15-alkyl-PGA.sub.2, and 15(R)-15-alkyl-PGA.sub.2, and are also useful as a means for obtaining highly purified PGA.sub.2, 15-alkyl-PGA.sub.2, and 15(R)-15-alkyl-PGA.sub.2 products.

    Abstract translation: 公开了取代的PGA2,15-烷基-PGA2和15（R）-15-烷基-PGA2的苯基和萘基酯及其外消旋形式及其制备方法。 该产品可用于与PGA2,15-烷基-PGA2和15（R）-15-烷基-PGA2相同的药理和医学目的，并且也可用作获得高度纯化的PGA2,15-烷基-PGA2的手段 ，和15（R）-15-烷基-PGA2产物。

    Substituted tolyl esters of PGE.sub.1
    10.
    发明授权
    Substituted tolyl esters of PGE.sub.1 失效
    取代的PGE {甲基丙烯酸甲酯

    公开(公告)号：US3931285A

    公开(公告)日：1976-01-06

    申请号：US531996

    申请日：1974-12-12

    Applicant: Walter Morozowich

    Inventor： Walter Morozowich

    IPC: C07C405/00 ,  C07C133/08 ,  C07C103/82

    CPC classification number: C07C405/00

    Abstract: Substituted phenyl and naphthyl esters of PGE.sub.1, 15-alkyl-PGE.sub.1, and 15(R)-15-alkyl-PGE.sub.1, and their racemic forms, and processes for producing them are disclosed. The products are useful for the same pharmacological and medical purposes as PGE.sub.1, 15-alkyl-PGE.sub.1, and 15(R)-15-alkyl-PGE.sub.1, and are also useful as a means for obtaining highly purified PGE.sub.1, 15-alkyl-PGE.sub.1, and 15(R)-alkyl-PGE.sub.1 products.

    Abstract translation: 公开了取代的PGE1,15-烷基-GE-PGE1和15（R）-15-烷基-GE-PGE1的苯基和萘基酯及其外消旋形式及其制备方法。 该产品可用于与PGE1,15-烷基-GE-PGE1和15（R）-15-烷基-GFPE1相同的药理学和医学目的，并且也可用作获得高度纯化的PGE1,15-烷基-GE-PGE1的手段 和15（R） - 烷基-PGEE产物。

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