中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

371 records (took 0.026 seconds)

    Cyclic imide derivatives
    51.
    发明公开
    Cyclic imide derivatives 失效
    推动冯·克里斯滕·艾米登。

    公开(公告)号：EP0520573A1

    公开(公告)日：1992-12-30

    申请号：EP92201844.5

    申请日：1992-06-23

    Applicant: GLAXO INC.

    Inventor： Myers, Peter Leslie c/o Glaxo Inc. ,  Mcelroy, Andrew Brian c/o Glaxo Inc. ,  Brown, Peter Jonathan c/o Glaxo Inc. ,  Drewry, David Harold c/o Glaxo Inc. ,  Foley, Michael Andrew c/o Glaxo Inc. ,  Gregson, Michael c/o Glaxo Group Research Limited ,  Davies, Howard G, c/o Glaxo Group Research Limited

    IPC: C07K5/02 ,  C07K1/06 ,  A61K37/64

    CPC classification number: C07K5/0222 ,  A61K38/00

    Abstract: Compounds are described of the formula

    wherein:
       R¹ is C₃₋₆alkyl or C₁₋₃alkylthioC₁₋₃alkyl;
       R² is an optionally substituted C₁₋₆alkyl or C₁₋₆alkoxy group, aryl, heteroaryl, arylC₁₋₄alkyl, heteroarylC₁₋₄alkyl or a side-chain of a natural α-amino acid;
       R³ is hydrogen, C₁₋₆alkyl, CHR⁴COR⁵ (where R⁴ is a side-chain of a natural α-amino acid and R⁵ is hydroxyl, C₁₋₆alkoxy or NHR⁶ where R⁶ represents a hydrogen atom or a C₁₋₆alkyl group) or a group (CH₂) n X (where n is 1 to 6 and X is hydroxyl, C₁₋₄alkoxy, heteroaryl or a group NR⁷R⁸ where R⁷ and R⁸ are each hydrogen or C₁₋₆alkyl or the group NR⁷R⁸ forms a 5 to 7 membered cyclic amine); and
       Het is an optionally substituted cyclic imide where the cyclic imide ring system has the formula (i), (ii) or (iii)

    in which A, B, C and D are each CH or 1 or 2 of A, B, C and D represents N and the others represent CH, and E and F may each independently represent CH or N; and physiologically acceptable salts and solvates thereof.
    These compounds inhibit metalloproteases involved in tissue degradation. Compounds of the invention may be formulated for use in a variety of conditions involving tissue degradation including arthropathy, dermatological conditions, bone resorption, inflammatory diseases, tumour invasion and multiple sclerosis and related diseases involving myelin degradation, and in the promotion of wound healing.

    Abstract translation: 化合物描述为式CHEM，其中：R 1是C 3-6烷基或C 1-3烷硫基C 1-3烷基; R 2是任选取代的C 1-6烷基或C 1-6烷氧基，芳基，杂芳基，芳基C 1-4烷基，杂芳基C 1-4烷基或天然α-氨基酸的侧链; R 3是氢，C 1-6烷基，CHR 4 COR 5（其中R 4是天然α-氨基酸的侧链，R 5是羟基，C 1-6烷氧基或NHR 其中R 6表示氢原子或C 1-6烷基）或基团（CH 2）n X（其中n为1至6，X为羟基，C 1-4烷氧基，杂芳基或基团NR 7） 其中R 7和R 8各自为氢或C 1-6烷基或NR 7 R 8基团形成5至7元环胺）; 并且Het是任选取代的环状酰亚胺，其中环状酰亚胺环系具有式（i），（ii）或（iii）其中A，B，C和D各自为CH或A或2的A， B，C和D表示N，其余表示CH，E和F各自独立地表示CH或N; 及其生理上可接受的盐和溶剂合物。 这些化合物抑制参与组织降解的金属蛋白酶。 本发明的化合物可以配制用于涉及组织降解的各种病症，包括关节病，皮肤病学，骨吸收，炎性疾病，肿瘤侵袭和多发性硬化以及涉及髓磷脂降解的相关疾病，以及促进伤口愈合。

    Substituted phenyl-1,3-dioxoloquinoline derivatives and their use as antitumor agents
    53.
    发明公开
    Substituted phenyl-1,3-dioxoloquinoline derivatives and their use as antitumor agents 失效
    取代基苯基-1,3-二氧杂环戊烯醇化物和维他命抗体。

    公开(公告)号：EP0496634A1

    公开(公告)日：1992-07-29

    申请号：EP92300618.3

    申请日：1992-01-24

    Applicant: GLAXO INC.

    Inventor： Luzzio, Michael J. ,  Besterman, Jeffrey M. ,  Evans, Michael G. ,  Johnson, Ross M.

    IPC: C07D491/056 ,  A61K31/47

    CPC classification number: C07D491/04

    Abstract: The present invention relates to the compounds of formula (I),

    wherein:
       R¹ is hydrogen, hydroxy or amino;
       R² is hydrogen, hydroxy, methoxy or methoxymethoxy;
       R³ is hydrogen, hydroxy, amino, methoxy, methoxymethoxy or, taken together with R², methylenedioxy (also known as 1,3 dioxolo);
       R⁴ is hydrogen, hydroxy, methoxy, methoxymethoxy, benzyl, di(C₁₋₄)alkylaminomethyl or, taken together with R³, methylenedioxy;
       R⁵ is hydrogen or hydroxy;
    provided that at least one of R¹ through R⁵ is other than hydrogen; and


    i) X² is hydroxy or methoxy with X¹, X³ and X⁴ being hydrogen; or
    ii) X¹ taken together with X²,
       X² taken together with X³ or
       X³ taken together with X⁴, is methylenedioxy, provided that each of the remaining respective X¹, X², X³ and X⁴ substituents are hydrogen,
    intermediates in the synthesis of them, pharmaceutical formulation containing them, their use as inhibitors of topoisomerase and their use in the treatment of tumors.

    Abstract translation: 本发明涉及式（I）化合物，其中：R 1是氢，羟基或氨基; R 2是氢，羟基，甲氧基或甲氧基甲氧基; R 3为氢，羟基，氨基，甲氧基，甲氧基甲氧基，或与R 2一起亚甲二氧基（也称为1,3-二氧杂环戊烷）一起使用。 R 4是氢，羟基，甲氧基，甲氧基甲氧基，苄基，二（C1-4）烷基氨基甲基或与R 3一起亚甲二氧基; R 5是氢或羟基; 条件是R 1至R 5中的至少一个不是氢; 和i）X 2是羟基或甲氧基，X 1，X 3和X 4是氢; 或ii）与X 2一起X，X 2与X 3或X 3一起与X 4一起使用的X 1是亚甲二氧基，条件是剩余的各自的X X 1，X 3和X 4取代基是氢，它们的合成中的中间体，含有它们的药物制剂，它们作为拓扑异构酶的抑制剂的用途及其在治疗肿瘤中的用途。

    57.
    发明专利
    未知

    公开(公告)号：NL192819C

    公开(公告)日：1998-03-04

    申请号：NL8901199

    申请日：1989-05-12

    Applicant: GLAXO INC

    IPC: A61K9/30 ,  A61K9/28 ,  A61K9/36 ,  A61K31/34 ,  A61K47/14 ,  A61K47/30 ,  A61K47/38 ,  A61P43/00

    Abstract: This invention relates to an improved polymeric film coating for a ranitidine Hydrocholride (HCl) tablet in which the plasticizer triacetin had been added to the polymeric film coating medium. A tablet of this invention has been found to have great stability than a tablet coating with a polymeric film which does not contain triacetin.

    METERED AEROSOL DISPENSING APPARATUS AND METHOD OF USE THEREOF
    58.
    发明专利
    METERED AEROSOL DISPENSING APPARATUS AND METHOD OF USE THEREOF 未知

    公开(公告)号：IL111465A

    公开(公告)日：1998-01-04

    申请号：IL11146594

    申请日：1994-10-31

    Applicant: GLAXO INC

    IPC: B65D83/44 ,  B05B9/04 ,  B65D83/14 ,  B05B11/06 ,  G01F11/36

    Abstract: The present invention relates to an aerosol dispensing apparatus, more particularly to aerosol dispensing valves incorporating a controlled metered dispensing function wherein the metering chamber holding the next aerosolized dose is in fluidic communication with the reservoir allowing homogenous mixing of the next aerosolized dose to be dispensed.

    59.
    发明专利
    未知

    公开(公告)号：NL192819B

    公开(公告)日：1997-11-03

    申请号：NL8901199

    申请日：1989-05-12

    Applicant: GLAXO INC

    IPC: A61K9/30 ,  A61K9/28 ,  A61K9/36 ,  A61K31/34 ,  A61K47/14 ,  A61K47/30 ,  A61K47/38 ,  A61P43/00

    Abstract: This invention relates to an improved polymeric film coating for a ranitidine Hydrocholride (HCl) tablet in which the plasticizer triacetin had been added to the polymeric film coating medium. A tablet of this invention has been found to have great stability than a tablet coating with a polymeric film which does not contain triacetin.

Patent Agency Ranking