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43 条记录 (耗时 0.016 秒)

    4,7-Benzofurandione derivatives
    1.
    发明公开
    4,7-Benzofurandione derivatives 失效
    4,7- Benzofurandion衍。

    公开(公告)号：EP0301692A2

    公开(公告)日：1989-02-01

    申请号：EP88305388.6

    申请日：1988-06-13

    申请人： MERCK FROSST CANADA INC.

    发明人： Adams, Julian ,  Belanger, Patrice C. ,  Rokach, Joshua ,  Guindon, Yvan ,  Belly, Michel L.

    IPC分类号： C07D307/06 ,  C07D407/06 ,  C07D407/04 ,  C07D407/12 ,  A61K31/34 ,  A61K31/36

    CPC分类号： C07D407/06 ,  C07D307/86

    摘要： 4,7-Benzofurandione derivatives of Formula I, pharmaceutical compositions, and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardio­vascular disorders, inflammation, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents. Also disclosed are novel intermediates useful for the preparation of the 4,7-benzofurandiones of this invention.

    摘要翻译： 公开了式I的4,7-苯并呋喃二酮衍生物，药物组合物和治疗方法。 这些化合物可用作哺乳动物白三烯生物合成的抑制剂。 因此，这些化合物是治疗过敏性疾病，哮喘，心血管疾病，炎症，牛皮癣和过敏性结膜炎的有用的治疗剂。 这些化合物也可用作止痛剂和细胞保护剂。 还公开了可用于制备本发明的4,7-苯并呋喃二酸的新型中间体。 v

    4,7-diacyloxybenzofuran derivatives
    2.
    发明公开
    4,7-diacyloxybenzofuran derivatives 失效
    4,7-二酰氧基苯并呋喃衍生物

    公开(公告)号：EP0295851A1

    公开(公告)日：1988-12-21

    申请号：EP88305387.8

    申请日：1988-06-13

    申请人： MERCK FROSST CANADA INC.

    发明人： Adams, Julian ,  Guindon, Yvan

    IPC分类号： C07D307/86 ,  C07D407/06 ,  C07D407/04 ,  C07D407/12 ,  A61K31/34 ,  A61K31/36

    CPC分类号： C07D407/10 ,  C07D307/86

    摘要： 4,7-Diacyloxybenzofuran derivatives of Formula I, are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents.

    摘要翻译： 公开了式I的4,7-二酰氧基苯并呋喃衍生物。 这些化合物可用作哺乳动物白三烯生物合成的抑制剂。 因此，这些化合物是用于治疗变应性病症，哮喘，心血管病症，炎症，牛皮癣和变应性结膜炎的有用的治疗剂。 该化合物也可用作止痛剂和细胞保护剂。

    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.

    5-Lipoxygenase inhibitors
    8.
    发明公开
    5-Lipoxygenase inhibitors 失效
    5-脂氧合酶抑制剂

    公开(公告)号：EP0140709A3

    公开(公告)日：1986-03-05

    申请号：EP84307480

    申请日：1984-10-30

    申请人： MERCK FROSST CANADA INC.

    发明人： Atkinson, Joseph G. ,  Belanger, Patrice C. ,  Guindon, Yvan ,  Rokach, Joshua

    IPC分类号： A61K31/54 ,  A61K31/535 ,  A61K31/495 ,  C07D513/04 ,  C07D498/04 ,  C07D513/16 ,  C07D241/18 ,  C07D279/00 ,  C07D241/00

    CPC分类号： C07D513/04 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  C07D241/18

    摘要： Compounds of the Formula I:
    and their pharmaceutically acceptable salts are inhibitors of the mammalian 5-lipoxygenase enzyme system of the arachidonic acid cascade. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation and are incorporated into pharmaceutical compositions. Certain of the compounds are novel. In the formula,
    Z is O, NCN, SO or SO 2 ; R, is H, C 1-6 alkyl, benzyl, C 1-6 acyl, C 1-6 aminoacyl, (C 1-6 alkylacyloxy)-(C 1-6 alkyl), (C 1-6 alkoxy)-(C 1-6 alkyl), -(CH 2 ) n COOR 6 where n is, 0, 1, 2, 3 or 4, CN, (C 1-6 alkyl)acyloxy-(C 1-6 alkoxy)carbonyl, -C(R 7 ) = C(R 7 )COOR 6 or SO 2 R 10 ; 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 or -(CH 2 ) n M, where n is 0 or an integer from 1 to 6 and M is(a) OR 16 (b) halogen; (c) CF 3 . (d) SR 16 ; (e) phenyl; (f) substituted phenyl where the substituents(s) is/are C 1-3 alkyl, halogen, CN, C 1-3 alkoxy, OH, (CH 2 ) n NR 8 R 9 where n is 0, 1 or 2, CF 3 , COOR 6 or CH 2 COOR 6 ; (herein called «substituted phenyl as defined»); (g) COOR 6 ; (h) -CO-R 14 ; (i) tetrazolyl; (j) NH-CO-R 7 ; (k) NR 8 R 9 ; (I) NHSO 2 R 10 ; (m) -CO-CH 2 0H; (n) SOR 11 where R 11 is C 1-6 alkyl, phenyl, substituted phenyl as defined, (CH 2 ) m COOR 6 , where m is an integer from 1 to 6, or CF 3 ; (o) CONR 8 R 9 ; (p) SO 2 NR 8 R 9 ; (q) S0 2 R 13 where R 13 is OH, C 1-6 alkyl, H phenyl, substituted phenyl as defined, (CH 2 ) m COOR 6 or CF 3 ; (r) N0 2 ; (s) -OCO-R 14 ; (t) -OCO-NR 8 R 9 ; (u)-OCO-OR 7 ; or (v) -CN; each R 16 , independently of any other, is H; (C 1-6 alkoxy)-(C 1-6 alkyl); (C 1-6 alkyl)acyloxy(C 1-6 alkyl); C 1-6 alkyl; substituted phenyl as defined; -CH 2 ) m COOR 6 ; CN: C 1-5 alkylacyl; C 1-4 perfluoroalkyl; phenyl; benzyl; or CH 2 -R 12 where R 12 is C 1-5 alkyldimethylamino; each R 6 , independently of any other, is H, C 1-6 alkyl, benzyl or phenyl; each R 14 , independently of any other, is H, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkyl)acyloxy(C 1-6 alkoxy), (CH 2 ) n COOR 6 where n is 0 or an integer from 1 to 4, phenyl or substituted phenyl as defined or is such that R 14 COOH is an essential amino acid; each of R 8 and R 9 , independently of the others, is H, phenyl, substituted phenyl as defined or C 1-4 alkyl, or NR 8 R 9 is a heterocycloalkyl of 5 to 8 ring atoms; and each R 7 , independently of the others, is H, C 1-6 alkyl, benzyl, phenyl or (C 1-6 alkyl)acyloxy-(C 1-6 alkoxy); each R 10 is independently OH, C 1-6 alkyl, C 1-6 alkoxy, phenyl or p-tolyl; or any two of R,, R 2 , R 3 , R 4 or R 5 are joined to form an additional ring of 5 to 7 members that optionally contains a carbonyl group and/or a hydroxyl group as substituent(s), and that has 0, 1 or 2 double bonds, and such that, if R, is a constituent of the ring, one member is nitrogen and the others are carbon and if R 1 is not a constituent of the ring, all the members are carbon; and T is hydrogen or OR 15 where R 15 is hydrogen, C 1-6 alkyl, C 1-6 alkylacyl, phenyl-(C 1-8 alkyl)acyl, SO 2 R 10 , arylsulfonyl, -CO-phenyl or substituted phenyl as defined.

    摘要翻译： 式I化合物及其药学上可接受的盐是花生四烯酸级联的哺乳动物5-脂氧合酶系统的抑制剂。 这样，这些化合物是用于治疗过敏性疾病，哮喘，心血管疾病和炎症的有用的治疗剂，并且被掺入到药物组合物中。 某些化合物是新颖的。 在该式中，Z是O，NCN，SO或SO 2; （C1-6烷基） - （C1-6烷基），（C1-6烷氧基） - （C1-6烷基），（C1-6烷基） - （C1-6烷基） - （CH 2）n COOR 6其中n是0,1,2,3或4，CN，（C 1-6烷基）酰氧基 - （C 1-6烷氧基）羰基，-C（R 7）= C（R 7）COOR 6或 SO 2 R; R 2，R 3，R 4和R 5各自独立地为氢，C 1-6烷基，C 2-6烯基或 - （CH 2）n M，其中n为0或1至6的整数，且M为（a ）OR16（b）卤素; （c）CF3。 （d）SR16; （e）苯基; （f）其中取代基为C 1-3烷基，卤素，CN，C 1-3烷氧基，OH，（CH 2）n NR 8 R 9，其中n为0,1或2，CF 3，COOR 6或CH 2 COOR 6的取代的苯基; （在此称为“定义的取代苯基”）; （g）COOR6; （h）-CO-R14; （i）四唑基; （j）NH-CO-R7; （k）NR8R9; （I）NHSO2R10; （m）-CO-CH 2 OH; （n）SOR11，其中R11是C1-6烷基，苯基，如所定义的取代的苯基，（CH2）mCOOR6，其中m是1至6的整数，或CF3; （o）CONR8R9; （p）SO2NR8R9; （q）SO 2 R 13，其中R 13是OH，C 1-6烷基，H苯基，如所定义的取代的苯基，（CH 2）m COOR 6或CF 3; （r）NO 2; （s）-OCO-R14; （t）-OCO-NR 8 R 9; （U）-OCO-OR7; 或（v）-CN; 每个R16独立于任何其他，是H; （C 1-6烷氧基） - （C 1-6烷基）; （C 1-6烷基）酰氧基（C 1-6烷基）; C 1-6烷基; 如定义的取代的苯基; -CH 2）mCOOR6; CN：C 1-5烷基酰基; C1-4全氟烷基; 苯基; 苄基; 或CH 2 -R 12，其中R 12是C 1-5烷基二甲基氨基; 每个R6彼此独立地为H，C1-6烷基，苄基或苯基; 每个R 14彼此独立地为H，C 1-6烷基，C 1-6烷氧基，C 1-6烷基）酰氧基（C 1-6烷氧基），（CH 2）n COOR 6，其中n为0或1至4的整数， 苯基或取代的苯基，或者是这样的，即R 14 COOH是必需氨基酸; R8和R9中的每一个相互独立地为H，苯基，如所定义的取代的苯基或C1-4烷基，或NR8R9为具有5至8个环原子的杂环烷基; 并且每个R 7相互独立地为H，C 1-6烷基，苄基，苯基或（C 1-6烷基）酰氧基 - （C 1-6烷氧基）; 每个R 10独立地为OH，C 1-6烷基，C 1-6烷氧基，苯基或对甲苯基; 或者R 1，R 2，R 3，R 4或R 5中的任意两个连接形成另外的5至7元环，其任选地含有羰基和/或羟基作为取代基，并且具有0,1 或2个双键，并且如果R 1是环的组分，则一个成员是氮并且其他是碳，并且如果R 1不是环的组成部分，则所有成员都是碳; 和T是氢或OR 15，其中R 15是氢，C 1-6烷基，C 1-6烷基酰基，苯基 - （C 1-8烷基）酰基，SO 2 R 10，芳基磺酰基，-CO-苯基或取代的苯基。