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43 条记录 (耗时 0.018 秒)

    Phenothiazine compounds
    31.
    发明公开
    Phenothiazine compounds 失效
    吩噻嗪化合物。

    公开(公告)号：EP0163551A1

    公开(公告)日：1985-12-04

    申请号：EP85303875.0

    申请日：1985-05-31

    申请人： THE WELLCOME FOUNDATION LIMITED

    发明人： Leighton, Harry Jefferson ,  Gillies, Iain

    IPC分类号： C07D279/28 ,  C07D417/04 ,  C07D417/06 ,  C07D453/02 ,  A61K31/54

    CPC分类号： C07D417/04 ,  C07D279/28 ,  C07D417/06 ,  C07D453/02 ,  C07F9/6547

    摘要： The present invention relates to compounds of the formula (I):
    or a salt, ester or amide thereof; wherein

    R' is a C 1-7 bivalent aliphatic hydrocarbon group or a single bond;
    R 2 and R 3 are the same or different and are each hydrogen,
    C 1-4 alkyl or taken together with the nitrogen comprise a nitrogen-containing heterocyclic ring having four to six ring members;
    R 4 is hydrogen, halogen, C 1-4 alkoxy, C 1-4 , alkyl optionallyu substituted by one to three halogen atoms; or a group R, C02H as hereinbefore defined; and
    A is C 1-4 alkylene orANR 2 R 3 forms a group -CH 2 -(CH 2 ) 2 or CH 2 -CH 2 ) 2
    B is an acidic group other than a mono-carboxylic acid group of comparable or greater acid strength than a carboxylic acid group in a similar chemical environment, provided that any sulphonamide group contains at least one N-H bond.

    Also disclosed are processes for the preparation of. the compounds of the formula (I), chemical intermediates for use in their preparation, and pharmaceutical formulations containing the said compounds.
    The compounds have antiallergic activity as defined by blockade of anaphylactoid activity. Certain of the compounds also have good antihistaminic activity.

    Benzo[a]phenothiazines and hydro-derivatives and pharmaceutical compositions containing them
    32.
    发明公开
    Benzo[a]phenothiazines and hydro-derivatives and pharmaceutical compositions containing them 失效
    苯并咪唑和水解衍生物及含有它们的药物组合物

    公开(公告)号：EP0136893A3

    公开(公告)日：1985-05-08

    申请号：EP84306641

    申请日：1984-09-28

    申请人： MERCK FROSST CANADA INC.

    发明人： Fortin, Rejean ,  Girard, Yves ,  Guindon, Yvan ,  Lau, Cheuk K. ,  Rokach, Joshua ,  Yoakim, Christiane

    IPC分类号： A61K31/54 ,  A61K31/535 ,  C07D279/36 ,  C07D265/34 ,  C07F09/65

    CPC分类号： C07F9/6547 ,  A61K31/535 ,  A61K31/54 ,  C07D265/34 ,  C07D279/36

    摘要： Pharmaceutical compositions contain a compound for the Formula
    or a pharmaceutically acceptable salt thereof. Certain compounds of Formula I are novel. Compounds of Formula I are useful in treating allergic conditions, asthma, cardrovascular disorders, inflammation and pain and are useful as cytoprotective agents.
    In Formula 1. X is O, S, SO or SO 2 ; R, is H; C,- 6 alkyl; C, - 6 acyl; C 1-6 aminoacyl; (C 1-6 acyloxy)-(C 1-6 alkyl); (C 1-6 alkoxy)-(C l - 6 alkyl); benzoyl; substituted benzoyl in which the substitution in the phenyl ring (herein called "substituted as herein defined") is halogen, C 1-3 alkyl, C 1-3 alkoxy, CN, CF 3 , COOR 6 , OH, CH 2 COOR 6 or (CH 2 ) n NR 8 R 9 where n is 0, 1 or 2; carbamoyl; CONHR 7 ; COOR 7 ; p-toluenesulfonyl; methane sulfonyl; or an acyl group such that R,-OH is an essential amino acid; each of R 2 , R 3 , R 4 and R 5 , independently of the others, is hydrogen; C 1-6 alkyl; C 2-6 alkenyl; -(CHR 6 ) p COOR 6 , p being 0 or an integer from 1 to 4; or -(CH 2 ) m M where m is 0 or an integer from 1 to 6 and M is (a) OR, s ; (b) halogen; (c) CF 3 ; (d) SR 15 ; (e) phenyl or substituted phenyl as herein defined; (f) COOR 6 ; (g) CO-R 14 ; (h) tetrazolyl; (i) -NH-CO-R 7 ; (j) -NR 8 R 9 ; (k) -NHSO 2 R 10 where R 10 is OH, C 1-6 alkyl, C 1-6 alkoxy, or phenyl; (I) -COCH 2 0H; (m) -SOR 11 where R 11 is C 1-6 alkyl; phenyl; substituted phenyl as herein defined; (CH 2 ) m COOR 6 ;CN; formyl or C 1-4 perfluoroalkyl; (n) -CONR 8 R 9 ; (o) -SO 2 NR 8 R 9 ; (p) -SO 2 R 13 where R 13 is a hydrogen atom or a radical of the type defined for R 11 ; (q) NO 2 ; (r) O-CO-R 14 ; (s) O-CO-NR 8 R 9 ; (t) -CN; or (u) -OPO(OR 6 ) 2 : each R 6 , independently of any other, is H, phenyl or C 1-6 alkyl; each R 7 , independently of any other, is C 1-6 alkyl, benzyl, phenyl or (C 1-6 acyloxyl-(C 1-6 alkyl); each R 8 and each R 9 , independently of any other, is phenyl, substituted phenyl as herein defined, or C 1-4 alkyl, or NR 8 R 9 represents a heterocycloalkyl radical of 5 to 8 ring atoms; each R 14 , independently of any other, is H. (CH 2 ) p COOR 6 , C, 6 alkyl, C 1-6 alkoxy, (C 1-6 acyloxy)-(C 1-6 alkoxy), phenyl, substituted phenyl as herein defined, or C, -6 aminoalkyl, or R 14 is such that R 14 CO 2 H is an essential amino acid; R 15 is H, (C 1-6 alkoxy)-(C 1-6 alkyl), (C, 6 acyloxyl-(C 1-6 alkyl), C 1-6 alkyl, benzyl, -(CH 2 ) m COOR 6 , CN, formyl, C 1-4 perfluoroalkyl, CH 2 -R 12 where R 12 is C 1-5 alkyldimethylamino or phenyl, phenyl, or substituted phenyl as herein defined; the broken lines in ring A represent optional double bonds; R 2 , R 3 , R 4 and R 5 may be positioned anywhere in the structure.

    Novel 3-oxo-1, 4-benzothiazine derivatives
    39.
    发明公开
    Novel 3-oxo-1, 4-benzothiazine derivatives 失效
    3-氧代-1,4- Benzothiazinderivate。

    公开(公告)号：EP0657444A1

    公开(公告)日：1995-06-14

    申请号：EP94119182.7

    申请日：1994-12-05

    申请人： SANTEN PHARMACEUTICAL CO., LTD.

    发明人： Kawashima, Yoichi ,  Ota, Atsuigaoka ,  Morikawa, Yuko ,  Mibu, Hiroyuki

    IPC分类号： C07D279/16 ,  C07D417/06 ,  C07F9/6547 ,  C07D417/12 ,  C07D417/14 ,  A61K31/54

    CPC分类号： C07D417/06 ,  C07D279/16 ,  C07F9/6547 ,  Y02P20/55

    摘要： This invention relates to the compounds of the formula [I] which are useful for the treatment of cataracts, and the synthetic intermediates of the formula [II],

    wherein

    R¹ is hydroxy which can be protected by a protective group;
    R² is lower alkyl;
    R³ is hydrogen, lower alkyl, hydroxy, which can be protected by a protective group, or lower alkoxy, and the said lower alkyl can be substituted by hydroxy, which can be protected by a protective group, amino or lower alkylamino;
    R⁴ is tetrazolyl, phosphonyl or lower alkyl ester thereof, or sulfonyl or lower alkyl ester thereof, and
    A is alkylene.

    摘要翻译： 本发明涉及可用于治疗白内障的式[I]化合物和式[II]，CHEM的合成中间体，其中R 1是可被保护基保护的羟基 ; R 2是低级烷基; R 3是氢，低级烷基，可被保护基保护的羟基或低级烷氧基，所述低级烷基可以被羟基取代，其可被保护基，氨基或低级烷基氨基保护; R 4是四唑基，膦酰基或其低级烷基酯，或其磺酰基或低级烷基酯，A是亚烷基。

    TARGETED DRUG DELIVERY VIA MIXED PHOSPHATE DERIVATIVES
    40.
    发明公开
    TARGETED DRUG DELIVERY VIA MIXED PHOSPHATE DERIVATIVES 失效
    靶器官展望现役BY混合磷酸盐衍生物。

    公开(公告)号：EP0577725A1

    公开(公告)日：1994-01-12

    申请号：EP92909373.0

    申请日：1992-03-27

    申请人： UNIVERSITY OF FLORIDA

    发明人： BODOR, Nicholas S.

    IPC分类号： A61K31 ,  A61K47 ,  A61P43 ,  C07F9 ,  C07H15 ,  C07H19 ,  C07J51 ,  C07J63 ,  C07J71

    CPC分类号： C07H19/10 ,  A61K47/54 ,  C07F9/091 ,  C07F9/094 ,  C07F9/5532 ,  C07F9/5535 ,  C07F9/5537 ,  C07F9/5722 ,  C07F9/5728 ,  C07F9/5765 ,  C07F9/591 ,  C07F9/592 ,  C07F9/645 ,  C07F9/65061 ,  C07F9/65068 ,  C07F9/650958 ,  C07F9/65121 ,  C07F9/65125 ,  C07F9/6547 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/65611 ,  C07F9/65613 ,  C07F9/65616 ,  C07H19/04 ,  C07H19/20 ,  C07J51/00 ,  C07J63/008 ,  C07J71/0031

    摘要： L'invention décrit des composés de la formule (I) et leurs sels pharmaceutiquement acceptables, formule dans laquelle [D] est le résidu d'un médicament ayant un groupe fonctionnel réactif, ledit groupe fonctionnel étant accolé, directement ou par le biais d'un groupe de pontage, par l'intermédiaire d'une liaison oxygène-phosphore, à l'atome de phosphore de la fraction (a); R1 est alkyle C1-C8, aryle C6-C10 ou aralkyle C7-C12, à condition que lorsque [D] est le résidu d'un médicament ayant un groupe fonctionnel hydroxyle réactif, ledit groupe fonctionnel étant accolé directement à l'atome de phosphore de la fraction (a) par l'intermédiaire d'une liaison oxygène-phosphore, R1, pris conjointement avec l'atome d'oxygène adjacent, puisse également être le résidu d'un médicament ayant un groupe hydroxyle réactif, ledit groupe fonctionnel étant accolé directement à l'atome de phosphore de la fraction (b) par l'intermédiaire d'une liaison oxygène-phosphore, -OR1 étant identique à ou différent de [D]; R2 est hydrogène, alkyle C1-C8, aryle C6-C10, hétéroaryle C4-C9, cycloalkyle C3-C7, cyclohétéroalkyle C3-C7 ou bien aralkyle C7-C12; et R3 est sélectionné dans le groupe composé de alkyle C1-C8; alcényle C2-C8 ayant une ou deux doubles liaisons; (cycloalkyle C3-C7)-CrH2r- où r vaut zéro, un, deux ou trois, la partie cycloalkyle étant non substituée ou portant 1 ou 2 substituants alkyle C1-C4 sur la partie noyau; (aryloxy C6-C10) alkyle C1-C8; 2-, 3-ou 4-pyridyle; et phényle-CrH2r- où r vaut zéro, un, deux ou trois et phényle est non substitué, ou est substitué par 1 à 3 alkyle ayant chacun 1 à 4 atomes de carbone, alkoxy ayant 1 à 4 atomes de carbone, halo, trifluorométhyle, dialkylamino ayant 2 à 8 atomes de carbone ou alcanoylamino ayant 2 à 6 atomes de carbone. Ces composés conviennent à un apport médicamenteux ciblé, notamment au cerveau.