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18 条记录 (耗时 0.03 秒)

    Morpholinyl substituted [1,2,4]-triazolo[1,5-a]triazine as antagonist
    1.
    发明授权
    Morpholinyl substituted [1,2,4]-triazolo[1,5-a]triazine as antagonist 失效
    吗啉基取代的[1,2,4] - 三唑并[1,5-a]三嗪为拮抗剂

    公开(公告)号：US5356894A

    公开(公告)日：1994-10-18

    申请号：US94572

    申请日：1993-07-21

    申请人： Peter W. Rodney ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    发明人： Peter W. Rodney ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    IPC分类号： C07D487/04 ,  A61K31/535 ,  C07D413/06

    CPC分类号： C07D487/04

    摘要： R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;R.sup.2 (when not as hereinbelow defined together with X) is (1-6C)alkyl substituted by a group of formula R.sup.10 Xb(CO).sub.m in which m is 0 or 1, provided that when m is 0, X and Xb are separated by at least two carbon atoms, Xb is an imino group of formula --NRb in which Rb together with R.sup.10 and the adjacent nitrogen atom forms a morpholino, thiomorpholino, piperidino or azetidino ring;and X is oxy, thio, sulphinyl, sulphonyl or an imino group of formula --NRa-- in which Ra is hydrogen, (1-6C)alkyl or together with R2 and the adjacent nitrogen atom forms a morpholino, thiomorpholino, piperidino or azetidino ring; andA is N or CT in which T is hydrogen or (1-4C)alkyl;or a pharmaceutically acceptable salt thereof; processes for the manufacture of the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.

    摘要翻译： 本发明涉及新颖的药学上有用的式I化合物，其中Q是任选带有1或2个独立地选自（1-4C）烷基和卤代的取代基的5元杂芳基; R1是氢，（1-6C）烷基或（1-4C）烷酰基; R2（当不与X一起定义时不同时）是由式R 10 X b（CO）m取代的（1-6C）烷基，其中m为0或1，条件是当m为0时，X和Xb被 至少两个碳原子，Xb是式-NRb的亚氨基，其中Rb与R10和相邻的氮原子一起形成吗啉代，硫代吗啉代，哌啶子基或氮杂环丁烷环; 并且X是式-NR a的氧基，硫基，亚磺酰基，磺酰基或亚氨基，其中R a是氢，（1-6C）烷基或与R 2一起并且相邻的氮原子形成吗啉代，硫代吗啉代，哌啶子基或氮杂环丁烷环 ; A为N或CT，其中T为氢或（1-4C）烷基; 或其药学上可接受的盐; 用于制备含有它们的化合物和药物组合物的方法。 这些化合物可用作腺苷拮抗剂。

    Azole derivatives
    2.
    发明授权
    Azole derivatives 失效
    唑衍生物

    公开(公告)号：US5290776A

    公开(公告)日：1994-03-01

    申请号：US886798

    申请日：1992-05-21

    申请人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    发明人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    IPC分类号： A61K31/53 ,  A61P9/00 ,  A61P9/08 ,  C07D487/04 ,  C07D405/14 ,  A51K31/53

    CPC分类号： C07D487/04

    摘要： A compound of the formula I ##STR1## wherein: R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;R.sup.2 is phenyl, a C-linked aromatic 5- or 6-membered heterocyclic ring containing one of oxygen and sulphur and/or one or two nitrogen, or (1-8C)alkyl, alkenyl or alkynyl unsubstituted or substituted by a phenyl or a C-linked aromatic 5- or 6-membered heterocylic ring containing one of oxygen and sulphur and/or one or two nitrogen, any phenyl being unsubstituted or substituted by one, two or three of (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, hydroxy, benzyloxy and (1-5C)alkanoyloxy;A is N or CT in which T is hydrogen or (1-4C)alkyl;or a pharmaceutically acceptable salt thereof, processes for the manufacture of the compounds, and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.

    摘要翻译： 式I化合物（*化学结构*）Ⅰ其中：R1为氢，（1-6C）烷基或（1-4C）烷酰基; R2是苯基，含有氧和硫之一和/或一个或两个氮的C-连接的芳香族5-或6-元杂环，或未被取代或被苯基取代或（1-8C）烷基， 含有一个氧和硫和/或一个或两个氮的C连接的芳族5-或6-元杂环，任何未被取代或被一个，两个或三个（1-4C）烷基取代的苯基（1-4C ）烷氧基，卤素，三氟甲基，羟基，苄氧基和（1-5C）烷酰氧基; A是N或CT，其中T是氢或（1-4C）烷基; 或其药学上可接受的盐，用于制备化合物的方法和含有它们的药物组合物。 这些化合物可用作腺苷拮抗剂。

    [1,2,4]-Triazolo[1,5-a]and pyrazolo[2,3-a][1,3,5]triazine derivatives
    3.
    发明授权
    [1,2,4]-Triazolo[1,5-a]and pyrazolo[2,3-a][1,3,5]triazine derivatives 失效
    [1,2,4]三唑并[1,5-a]和吡唑并[2,3-a] [1,3,5]三嗪衍生物

    公开(公告)号：US5270311A

    公开(公告)日：1993-12-14

    申请号：US708265

    申请日：1991-05-28

    申请人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    发明人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    IPC分类号： A61K31/53 ,  A61P9/08 ,  A61P9/10 ,  A61P25/04 ,  A61P25/06 ,  A61P43/00 ,  C07D487/04 ,  C07D403/14

    CPC分类号： C07D487/04

    摘要： The invention concerns novel, pharmaceutically useful compounds of formula I in which Q is a 5-membered heteroaryl optionally bearing 1 or 2 substituents independently selected from (1-4C)alkyl and halogeno;R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;R.sup.2 (when not as hereinbelow defined together with X) is hydrogen, (3-12C)cycloalkyl, (3-6C)alkenyl, phenyl(3-6C)alkenyl, tetrafluorophenyl, pentafluorophenyl, 5- or 6-membered heteroaryl, optionally substituted (1-6C)alkyl or optionally substituted phenyl;X is oxy, thio, sulphinyl, sulphonyl or an imino group of formula --NRa-- in which Ra is hydrogen, (1-6C)alkyl or together with R2 and the adjacent nitrogen atom forms a 4 to 6-membered saturated heterocyclic ring; andA is N or CT in which T is hydrogen or (1-4C)alkyl; or a pharmaceutically acceptable salt thereof; processes for the manufacture of the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists. The invention further provides novel intermediates useful in the manufacture of the compounds of formula I. ##STR1##

    Heterocyclic compounds
    4.
    发明授权
    Heterocyclic compounds 失效

    公开(公告)号：US5246932A

    公开(公告)日：1993-09-21

    申请号：US887211

    申请日：1992-05-21

    申请人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    发明人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    IPC分类号： A61K31/53 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  C07D487/04 ,  C07D519/00

    CPC分类号： C07D519/00

    摘要： A compound of the formula I ##STR1## wherein: A.sup.1 and A.sup.2 are each independently N or CT in which T is hydrogen or (1-4C)alkyl;R.sup.1 and R.sup.2 are each independently hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;X.sup.1 and X.sup.2 are each independently O, S or NH; andL is a (3-7C)cycloalkylene group or a (1-8C)alkylene chain optionally interrupted or extended by a group selected from phenylene, phenyleneoxy or oxyphenyleneoxy, the phenylene portion of said group being unsubstituted or substituted by one of halogen, hydroxy and (1-4C)alkoxy, provided that all heteroatoms in the group X.sup.1 --L--X.sup.2 are separated from one another by at least two carbon atoms; or a pharmaceutically acceptable salt thereof, processes for preparing the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.

    Reinforced directional drilling assemblies and methods of forming same
    7.
    发明授权
    Reinforced directional drilling assemblies and methods of forming same 有权
    加固定向钻井组件及其形成方法

    公开(公告)号：US09228584B2

    公开(公告)日：2016-01-05

    申请号：US13293135

    申请日：2011-11-10

    申请人： Hossein Akbari ,  Geraint Jones

    发明人： Hossein Akbari ,  Geraint Jones

    IPC分类号： E21B4/02 ,  F04C2/107 ,  B29L31/00

    CPC分类号： E21B4/02 ,  B29L2031/7496 ,  F04C2/1075 ,  F04C2230/24 ,  F04C2230/91 ,  F04C2270/80 ,  F05C2225/00 ,  F05C2253/04 ,  Y10T156/10 ,  Y10T428/249939

    摘要： Reinforced directional drilling assemblies and methods of forming reinforced directional drilling assemblies are provided. Strengthening materials may be incorporated into a resilient layer and/or a polymer-based composite material within a directional drilling assembly to improve the durability and performance of a power section within the directional drilling assembly. Inclusion of strengthening materials within a directional drilling assembly may provide a method to detect the status of a power section and send a signal from downhole upon detecting status of the power section. Inclusion of strengthening materials also may provide a method to collect data about operating conditions, including pressure, temperature, torque, RPM, stress level, shock, vibration, downhole weight on bit, and/or equivalent circulating density to send to the surface or to MWD/LWD systems. The strengthening materials may collect data by themselves or in conjunction with a sensor.

    摘要翻译： 提供了强化定向钻井组件和形成加固定向钻井组件的方法。 加强材料可以被引入定向钻井组件内的弹性层和/或基于聚合物的复合材料中以改善定向钻井组件内的动力段的耐久性和性能。 在定向钻井组件中包括加强材料可以提供一种检测功率部分的状态并且在检测到功率部分的状态时从井下发送信号的方法。 包含强化材料还可以提供一种方法来收集关于操作条件的数据，包括压力，温度，扭矩，RPM，应力水平，冲击，振动，钻头上的井下重量和/或等效循环密度以发送到表面或 MWD / LWD系统。 强化材料可以自己或结合传感器收集数据。

    1-Phenyl-2-aminoethanol derivatives
    9.
    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

    申请人： Geraint Jones

    发明人： Geraint Jones

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

    CPC分类号： C07K5/06026 ,  A61K38/00

    摘要： 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.

    摘要翻译： 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。

    Heterocyclic compounds
    10.
    发明授权
    Heterocyclic compounds 失效
    杂环化合物

    公开(公告)号：US3933818A

    公开(公告)日：1976-01-20

    申请号：US495217

    申请日：1974-08-06

    申请人： Geraint Jones

    发明人： Geraint Jones

    IPC分类号： C07D237/28 ,  C07D209/70 ,  C07D225/06 ,  C07D491/056

    CPC分类号： C07D209/70 ,  Y10S514/826

    摘要： Optionally substituted 4-oxo-1,4-dihydrocinnolin-3-ylpropionic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and a method of treatment using them. A representative compound is ethyl 6-ethyl-1-methyl-4-oxo-1,4-dihydrocinnolin-3-ylpropionate. Compounds active as inhibitors of effects following the combination of reagin-like antibodies and their antigens.

    摘要翻译： 任选取代的4-氧代-1,4-二氢噌啉-3-基丙酸衍生物，其制备方法，含有它们的药物组合物和使用它们的治疗方法。 代表性的化合物是6-乙基-1-甲基-4-氧代-1,4-二氢噌啉-3-基丙酸乙酯。 化合物与抗原样抗体及其抗原组合后作为活性抑制剂活化的化合物。