196519-70-7Relevant articles and documents
Retinoic acid agonists as preventive and therapeutic agents for nephritis
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, (2008/06/13)
The present invention provides a therapeutic or prophylactic agent as a substitute for conventional steroids or immunosuppressive agents to treat or prevent systemic erythematosus, glomerulonephritis, lupus nephritis, idiopathic thrombocytopenic purpura or autoimmune anemia. The agent comprises a retinoic acid receptor agonist, specifically a retinoic acid receptor subtype α (RARα) agonist, including for example: (1) carboxylic acid compounds having condensed rings represented by the following formula: ?(wherein the rings L and M are condensed, are the same as or different from each other, and represent an aromatic hydrocarbon which may have a substituent group or a heterocycle which may have a substituent group; the rings A and B are independent of each other and represent an aromatic hydrocarbon ring or heterocycle which may have a substituent group; and D represents a carboxyl group which may have a protective group), (2) 4-{[(3,5-bistrimethylsilylphenyl)carbonyl]amino}benzoic acid, 4-{2-[5-(3-methoxymethyl-5,6,7,8-tetrahydro-5,5,8,8-tetramethylnaphthalene-2-yl)pyrrolyl]}benzoic acid, etc.
Methods for preventing, inhibiting or treating graft rejection reactions in graft-versus-host disease (GVHD) and organ transplantation
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, (2008/06/13)
The present invention provides remedies for graft-versus-host disease (GVHD) and graft rejection reactions in organ transplantation which comprise retinoic acid receptor (RAR) agonists as an active ingredient. Main examples thereof include 9-(4-methoxy-2,3,6-trimethylphenyl)-7,8-dimethylnona-2,4,6,8-tetraen-1-oic acid, 4-[(E)-2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethylnaphthalen-2-yl)propenyl]benzoic acid, 4-{2-[5-(4,7-dimethylbenzofuran-2-yl)pyrroyl]}benzoic acid, 4-{2-[5-(5-chloro-7-ethylbenzofuran-2-yl)pyrrolyl]}benzoic acid and 4-{2-[5-(4,7-dimethylbenzothiophen-2-yl)pyrrolyl]}benzoic acid.
Discovery of novel and potent retinoic acid receptor α agonists: Syntheses and evaluation of benzofuranyl-pyrrole and benzothiophenyl-pyrrole derivatives
Yoshimura, Hiroyuki,Kikuchi, Kouichi,Hibi, Shigeki,Tagami, Katsuya,Satoh, Takashi,Yamauchi, Toshihiko,Ishibahi, Akira,Tai, Kenji,Hida, Takayuki,Tokuhara, Naoki,Nagai, Mitsuo
, p. 2929 - 2937 (2007/10/03)
In the course of our studies on retinoic acid receptor (RAR) agonists, we have designed and synthesized a series of benzofuran and benzothiophene derivatives. Some of these compounds (1a,b,e,f,j) markedly inhibited LPS- induced B-lymphocyte proliferation and exerted RARα selectivity. One of them, 4-[5-(4,7-dimethylbenzofuran-2-yl)pyrrol-2-yl]benzoic acid (1b), when orally administered significantly inhibited mouse antibody production and delayed type hypersensitivity (DTH) responses from a dose of 0.1 mg/kg.
Carboxylic acid derivatives having fused rings
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, (2008/06/13)
The present invention provides a medicament exhibiting excellent retinoic acid receptor agonism. A Carboxylic acid derivative having a fused ring which is represented by the following formula or a pharmacologically acceptable salt thereof: {wherein the symbol represents a single bond or a double bond; X, Y, Z, P, Q, U, V and W are each a group represented by the formula: -O- or -S-, or a group represented by the formula: [wherein Rk (k: 1 to 8) is hydrogen, halogeno, optionally substituted lower alkyl or the like, with either of R7 and R8 being a group represented by the formula: (wherein A and B are each independently an optionally substituted aromatic hydrocarbon ring or an optionally substituted unsaturated heterocycle; and D is optionally protected carboxyl)]}.
