Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-12-06
1998-11-24
Higel, Floyd D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514266, 514269, 544 54, 544 55, 544281, 544299, 544300, 546121, A61K 3144, A61K 31505, C07D40500, C07D40900, C07D23972
Patent
active
058407324
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP95/01192 filed Jun. 18, 1995.
TECHNICAL FIELD
The present invention relates to a new condensed imidazole compound that inhibits adhesion molecule expression and is useful as a therapeutic and prophylactic agent for diabetic nephritis and/or autoimmune diseases and as an immunosuppressor for organ transplantation, a method of its production and its composition.
BACKGROUND ART
In recent years, inhibitors of adhesion molecules expression designed to suppress inflammatory cell infiltration or prevent binding of immune cells 9, p. 289 (1991); Immunology Today, Vol. 10, p. 375 (1989)!.
In insulin-dependent diabetes mellitus, severe complications, namely retinopathy, nephropathy and neuropathy, occur, despite insulin therapy, 10 to 20 years after onset, which can threaten the patient's life, as well as quality of life. Diabetic nephropathy, in particular, is a severe complication seen in about 20-30% of diabetics, with no well-established effective therapy.
In organ transplantation, several kinds of immunosuppressors must be used for immunosuppression therapy to control graft rejection. Moreover, the functional survival of grafts depends on a delicate equilibrium between the kinds of immunosuppressors and the patient's capability of immune response. It is therefore desirable to be able to select drugs out of as many kinds of immunosuppressors as possible.
On the other hand, Japanese Patent Unexamined Publication No. 125048/1993 discloses that a pyridine derivative represented by the following formula (or salt or solvate thereof) is useful as an immunotherapeutic drug, therapeutic drug for transplantation immune response, etc.: ##STR1## wherein R.sup.1 and R.sup.2, whether identical or not, represent a hydrogen atom, a halogen, a lower alkyl group, a lower alkenyl group, a lower alkoxy group, a hydroxyl group, a nitro group, a cyano group, an amino group, a carbamoyl group, an acylamino group, a lower alkylamino group, a lower alkenylamino group or an aralkylamino group; X represents an oxygen atom or --S(O).sub.n -- (n represents 0, 1 or 2); A represents a divalent C.sub.1-5 hydrocarbon residue that may be substituted at a branch thereof; Y represents an atom of oxygen or sulfur; R.sup.3 represents a hydrogen atom or a hydrocarbon residue that may be substituted; R.sup.4 represents (1) a C.sub.2-30 alkyl group, (2) a C.sub.2-30 alkenyl group, (3) a lower alkyl group substituted by a halogen, an aryl or a heterocyclic group, (4) a lower alkenyl group substituted by a halogen or a heterocyclic group, (5) an aralkyl group that may be substituted, (6) an aryl group that may be substituted, or (7) a monocyclic or bicyclic heterocyclic group that may be substituted.
Japanese Patent Unexamined Publication No. 51383/1993 discloses that a calmodulin-inhibiting compound represented by the following formula (or salt thereof) is useful as an anti-inflammatory drug etc.: ##STR2## wherein X represents S, S(O), S(O).sub.2, O or NR.sup.3 (R.sup.3 represents a hydrogen or a hydrocarbon group that may be substituted); A represents a divalent linear or branched C.sub.1-15 hydrocarbon group that may contain ethereal oxygen at any possible position thereof and that may be substituted at a branch thereof; B.sup.1 represents an amino group acylated by an acyl group derived from a carboxylic acid, sulfonic acid, carbamic acid or thiocarbamic acid having 2 or more carbon atoms; R.sup.1 and R.sup.2, whether identical or not, represent a hydrogen, a hydrocarbon group that may be substituted, a halogen, a nitro group, a nitroso group, an amino group that may be protected, a lower alkoxycarbonyl group or a lower alkylcarbamoyl group. In examples of that patent publication, the following compounds were synthesized. ##STR3##
Japanese Patent Unexamined Publication No. 39221/1993 discloses an angiogenesis inhibitor containing a compound represented by the formula (or pharmaceutically acceptable salt thereof): ##STR4## wherein A represents a divalent linear or branched C.sub.1-15 hydrocarbon group that may
REFERENCES:
patent: 2514649 (1950-07-01), Knott
patent: 4105767 (1978-08-01), Bochis et al.
patent: 4414390 (1983-11-01), Tominaga et al.
patent: 4470986 (1984-09-01), Browne
patent: 4507481 (1985-03-01), Davidson et al.
patent: 4590196 (1986-05-01), Smith et al.
patent: 4782055 (1988-11-01), Ueda et al.
patent: 5112834 (1992-05-01), Senn-Bilfinger
patent: 5244908 (1993-09-01), Takatani et al.
patent: 5260303 (1993-11-01), Becker et al.
patent: 5491161 (1996-02-01), Jannsen et al.
Ricci et al., Ann. Chim. (Rome), 53(5), 577-587 (1963).
Meth-Cohn et al., Synthesis (1), 58-60 (1978).
Mylari et al., "Potent, Orally Active Reductase Inhibitors Related to Zopolrestat: Surrogates for Benzothiazole Side Chain," J. Med. Chem. 1992, 35, pp. 457-465.
Abe Hidenori
Iida Kyoko
Ikeda Hitoshi
Takatani Muneo
Higel Floyd D.
Takeda Chemical Industries Ltd.
LandOfFree
Imidazopyridine or imidazopyrimidine compounds, their production does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Imidazopyridine or imidazopyrimidine compounds, their production, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Imidazopyridine or imidazopyrimidine compounds, their production will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1702539