摘要:
Compounds represented by formula (I) wherein N1 represents an atom to which a donor hydrogen atom in a hydrogen bond donor group is bonded or a hydrogen bond acceptor atom in a hydrogen bond acceptor group; N3 represents a hydrogen bond acceptor atom in a hydrogen bond acceptor group; and N2, N4 and N5 represent each an arbitrary carbon atom constituting a hydrophobic group; having an atom corresponding to N3 and atoms corresponding to at least two atoms selected from N1, N2, N4 and N5 among the five atoms constituting a pharmacophore specified by the interatomic distances among N1, N2, N3, N4 and N5; and, in the optimized stereochemical structure thereof, the interatomic distances between the atom corresponding to N3 and atoms corresponding to at least two atoms selected from N1, N2, N4 and N5 fall within the scope of the pharmacophore interatomic distance, or salts thereof. Because of having an effect of inhibiting the activity of a transcription factor AP-1, these compounds are useful as preventives/remedies for diseases in which the excessive expression of AP-1 participates and as AP-1 inhibitors.
摘要:
Compounds of the formula wherein R 1 is hydrogen or C 1 -C 4 alkyl; R 2 is hydrogen, C 1 -C 4 alkyl or wherein R 8 is C 1 -C 4 alkyl; R 1 and R 2 together are alkylene having 3 to 6 carbon atoms; R 3 is hydrogen or C 1 -C 4 alkyl; R 4 is hydrogen or C 1 -C 4 alkvl, R 5 is hydrogen or C 1 -C 4 alkyl; R 6 is hydrogen or C 1 -C 4 alkyl; and R 7 and R 8 independently are (1) hydrogen; (2) halogen; (3) C,-C 4 alkyl; (4) C 1 -C 4 alkoxy; (5) OCF 3 ; (6) cyano; (7) nitro; (8) C 1 -C 4 haloalkyl; (9) R b SO n - wherein n is the integer 0, 1 or 2; and R b is (a) C 1 -C 4 alkyl; (b) C 1 -C 4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10) -NR c R d wherein R c and R d independently are hydrogen or C 1 -C 4 alkyl; (11) R 6 C(O)-wherein R e is C 1 -C 4 alkyl or C 1 -C 4 alkoxy; or (12) SO 2 NR c R d wherein R c and R d are as defined, with the proviso that R 7 is not attached to the 6-position, are effective as herbicides.
摘要翻译:式CHEM的化合物,其中R 1是氢或C 1 -C 4烷基; R 2是氢,C 1 -C 4烷基或R a-O - ,其中R a是C 1 -C 4烷基; R 1和R 2一起是具有3至6个碳原子的亚烷基; R 3是氢或C 1 -C 4烷基; R 4是氢或C 1 -C 4烷基,R 5是氢或C 1 -C 4烷基; R 6是氢或C 1 -C 4烷基; 和R 7和R 8独立地是(1)氢; (2)卤素; (3)C 1 -C 4烷基; (4)C1-C4烷氧基; (5)OCF3; (6)氰基; (7)硝基; (8)C 1 -C 4卤代烷基; (9)R bnn-其中n是整数0,1或2; 和R b是(a)C 1 -C 4烷基; (b)被卤素或氰基取代的C 1 -C 4烷基; (c)苯基; 或(d)苄基; (10)-NR c R d其中R c和R d独立地是氢或C 1 -C 4烷基; (11)R e(O) - 其中R e是C 1 -C 4烷基或C 1 -C 4烷氧基; 或(12)SO 2 NR c R d其中R c和R d如上所定义,条件是R 7不与6-位连接,作为除草剂是有效的。
摘要:
The present invention concerns 2,6-quinolinyl and 2,6-naphthyl derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals for the treatment of VLA-4 dependent inflammatory diseases such as for example asthma, allergic rhinitis, sinusitis, conjunctivitis, food allergy, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis and atherosclerosis. Formula (I): wherein X is N or CH.
摘要:
The present invention is directea to compounds or the formula (I) useful as anti-sickling agents and to pharmaceutical compositions of these compounds wherein formula
V is selected from:
which R, is ethyl, propyl or isopropyl;
in which R 2 is H or lower alkyl; in which R 3 is lower alkyl;
W is selected from:
. A 2 is (CH 2 )n 2 -C(CH 3 ) 2 , -C(CH 2 ) 3 - and n 2 = 1 to 5; X is 0 or 1;
R3 is HO- or
A3 is -(CH 2 )n 3 or -C(CH 2 ) 3 - and n 3 = 1 to 5; m is 0 or 1; and Y is H, Cl or OCH 3 ; Z is H or Cl; provided that
(i) when W is and Y and Z are Cl; (ii) when W is Y and Z are Cl, with the proviso that when R 2 is C 2 H 5 , R 2 is H and X is O, n 2 is 2 to 5; (iii) When W is with the proviso that when R3 is OH, Y is H or Cl and m is 1, n 3 = 4 or 5; (iv) when W is and Y and Z are Cl.
摘要:
The present invention concerns 2,6-quinolinyl and 2,6-naphthyl derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals for the treatment of VLA-4 dependent inflammatory diseases such as for example asthma, allergic rhinitis, sinusitis, conjunctivitis, food allergy, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis and atherosclerosis. Formula (I): wherein X is N or CH.
摘要:
The invention concerns compounds having the formula wherein R 1 , R 2 , R 3 , R 4 can mean identical or different radicals in any desired position on the benzene ring, namely fluoro, chloro, bromo, iodo, cyano, or nitro radicals, alkyl radicals having from 1 to 4 carbon atoms, cyclo alkyl radicals having from 3 to 7 carbon atoms, phenyl, phenylsulfonyl and phenoxy radicals and hydrogen;
n can mean a number with the value of 1 or 2 and x can mean CH 2 , and where n = 1, O-CH 2 as well.
The named compounds show efficiency as fungicides.
摘要:
The present invention concerns 2,6-quinolinyl and 2,6-naphthyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use for the treatment of VLA-4 dependent diseases.