利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

24 条记录 (耗时 0.015 秒)

    Benzo[a]phenothiazines and hydro-derivatives and pharmaceutical compositions containing them
    4.
    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.

    Phenothiazone derivatives and analogs
    6.
    发明公开
    Phenothiazone derivatives and analogs 失效
    苯并噻唑衍生物和类似物

    公开(公告)号：EP0115394A3

    公开(公告)日：1985-01-30

    申请号：EP84300239

    申请日：1984-01-16

    申请人： MERCK FROSST CANADA INC.

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

    IPC分类号： A61K31/54 ,  A61K31/535 ,  A61K31/495 ,  C07D279/18 ,  C07D265/38 ,  C07D241/46 ,  C07D293/10 ,  C07D279/34 ,  C07D279/36 ,  C07D265/34

    CPC分类号： C07D293/10 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  C07C46/06 ,  C07D241/46 ,  C07D265/34 ,  C07D265/38 ,  C07D279/18 ,  C07D279/34 ,  C07D279/36 ,  C07C50/28

    摘要： Phenothiazine compounds of formula
    where
    X is in the 1 or 3 position and is O, S or NR; R is H, C 1 -C 6 branched or linear alkyl, CN or phenyl; Y is 0, Se, S, SO, SO 2 or NR; and the broken line represents an optional double bond between the 1 and 2 or 2 and 3 position; each of R 1 , R 2 , R 3 and R 4 , independently of the others, is
    (1) hydrogen (2) C 1-6 alkyl, (3) C 2-6 alkenyl, (4) -(CH 2 ) n M where n is 0 or an integer from 1 to 6 and M is
    (a) OR 5 , (b) halogen, (c) CF 3 , (d) SR 5 where R 5 is H;
    alkoxyalkyl; acyloxyalkyl; C 1-6 alkyl; benzyl;
    phenyl or substituted phenyl where the substituents are C 1-3 alkyl, halogen, CN, CF 3 , COOR 6 , CH 2 COOR 6 , (CH 2 ) n NR 8 R 9 where n is 0, 1 or 2, C 1-3 alkoxy, OH, C 1-6 haloalkyl, -(CH 2 ) m COOR 6 , where m is 0 or an integer from 1 to 6 and R 6 is H, phenyl or C 1-6 alkyl; CN, formyl; perfluoroalkyl; or CH 2 -R 12 , where R 12 is C 1-5 alkyl, phenyl or dimethylamino; (e) phenyl or substituted phenyl as defined above for R 5 ; (f) COOR 6 ; (g)
    where R 14 is H, (CH 2 ) n COOR 6 where n is 0 or an integer from 1 to 4, C 1-6 alkyl, CF 3 , phenyl, or substituted phenyl as defined above for R 5 ; (h) tetrazole; (i)
    where R 7 is C 1-8 alkyl, benzyl or phenyl; (j) -NR 8 R 9 where R e and R 9 are independently selected from H, phenyl or substituted phenyl as defined above for R 5 , C 1 -C 4 alkyl or C 1 -C 4 alkylaminoalkyl, or are joined through the N to form a heterocycloalkyl of 5-8 ring atoms; (k) -NHSO 2 R 10 where R 10 is OH, C 1 -C 6 alkyl, C 1 -C 6 - alkoxy, phenyl or CF 3 ;
    (m) -SOR 11 where R 11 is C 1 -C 6 alkyl, phenyl or substituted phenyl as defined above for R 5 , (CH 2 ) m COOR 6 where m is 1 to 6, CN, formyl or C 1-4 perfluoroalkyl;
    (p) -SO 2 R 13 where R 13 is OH, H, C 1 -C 6 alkyl, phenyl or substituted phenyl as defined above for R 5 , (CH 2 ) m COOR 6 where m is 1 to 6, CN or C 1-4 perfluoroalkyl; (q) NO 2 ; (r)
    (s)
    (t)
    (u) -CN; or (v) NR 15 R 16 where R 15 and R 16 are such that HNR 15 R 16 is an essential amino acid;
    or any two of R 1 , R 2 , R 3 and R 4 are joined to form a fourth saturated or unsaturated C 5-6 ring, and T is H, halogen or CF 3 . are useful as inhibitors of mammalian leukotriene biosynthesis and therefore are useful therapeutic agents for treatng pain, skin conditions, allergic conditions, pulmonary conditions, asthma, cardiovascular disorders and inflammation. They are included in pharmaceutical compositions. Certain of the compounds are novel.

    Leukotriene antagonists
    7.
    发明公开
    Leukotriene antagonists 失效
    Leukotrienantagonisten。

    公开(公告)号：EP0123541A1

    公开(公告)日：1984-10-31

    申请号：EP84302718.6

    申请日：1984-04-19

    申请人： MERCK FROSST CANADA INC.

    发明人： Belanger, Patrice ,  Guindon, Yvan ,  Fortin, Rejean ,  Yaokim, Christiane ,  Rokach, Joshua

    IPC分类号： C07C59/90 ,  C07C51/347 ,  C07C149/40 ,  C07C147/107 ,  C07D317/14 ,  C07D233/78 ,  C07D207/44 ,  C07D303/02 ,  A61K31/19

    CPC分类号： C07D285/10 ,  C07C45/71 ,  C07C49/84 ,  C07C49/86 ,  C07C59/90 ,  C07C255/00 ,  C07D257/04

    摘要： Compounds of the formula:
    and their pharmaceutically acceptable salts, which are novel, are antagonists of leukotrienes of C4, D4 and E., the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic and anti-inflammatory agents and are made into pharmaceutical compositions.
    In the formula, R, is a radical of formula COOR 3 , where R 3 is hydrogen or an alkyl or cycloalkyl group containing not more than six carbon atoms; CH 2 OH; CHO; CH 2 NHSO 2 R 4 , where R 4 is OH; C 1-6 alkyl, C 1-6 alkoxy phenyl, phenyl substituted by Ci-3 alkyl or Ci- 3 alkoxy, halogen, hydroxy, haloalkyl, COOH, CN, formyl, C 1-6 acyl or C 1-4 perfluoroalkyl; CN; or CON(R 5 ) 2 , where each R 5 , independently of the other, is H, OH or C 1-4 alkyl; a tetrazolyl radical, a monocyclic or bicyclic heterocyclic ring containing an acidic hydroxyl group; or a radical of formula
    where each s, independently of the other, is 0,1, 2 or 3; R 7 is

    (A) a monocyclic or bicyclic heterocyclic radical containing from 3 to 12 nuclear carbon atoms and 1 or 2 nuclear heteroatoms, one being N, and the other (if any) being N or S, each ring in the heterocyclic radical having 5 or 6 atoms, or
    (B) a radical X-R 8 where X is O, S or NH and R 8 contains up to 21 carbon atoms and is (1) a hydrocarbon radical or (2) an acyl radical derived from an organic acyclic or monocyclic carboxylic acid containing not more than 1 heteroatom that is N, 0 or S in the ring; and each R 10 , independently of the other is H or Ci-4 alkyl;
    R 6 is H or Ci-4 alkyl;
    R 2 is a halogen atom; and
    R 9 is a hydrogen atom or hydroxyl group.

    摘要翻译： 下式的化合物及其药物上可接受的盐是C4，D4和E4的白三烯拮抗剂，即过敏反应缓慢的物质。 这些化合物可用作抗哮喘，抗过敏和抗炎剂并制成药物组合物。 在该式中，R 1是式COOR 3的基团，其中R 3是氢或含有不超过6个碳原子的烷基或环烷基; CH2OH; CHO; CH2NHSO2R4，其中R4是OH; C 1-6烷基，C 1-6烷氧基苯基，被C 1-3烷基或C 1-3烷氧基取代的苯基，卤素，羟基，卤代烷基，COOH，CN，甲酰基，C 1-6酰基或C 1-4四氟烷基; CN; 或CON（R5）2，其中每个R5独立于H，OH或C1-4烷基; 四唑基，含有酸性@羟基的单环或双环杂环; 或式的基团，其中每个s独立于0,2,2或3; R2是（A）含有3至12个核碳原子和1或2个核杂原子的单环或双环杂环基，一个为N，另一个为N或S，杂环基中的每个环均为5 或6个原子，或（B）基团X-R8，其中X是O，S或NH和R8含有至多21个碳原子，并且是（1）烃基或（2）衍生自有机非环或 在环中含有不多于1个N，O或S的杂原子的单环羧酸; 每个R 10独立地为H或C 1-4烷基; R6是H或C1-4烷基; R2是卤原子; R9为氢原子或羟基。