KR900018105A - 5-aryl-substituted-2,3-dihydro-imidazo [1,2-a] furo and-thienopyridine - Google Patents

Abstract

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Description

5-aryl-substituted-2,3-dihydro-imidazo [1,2-a] furo and-thienopyridine

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Claims (22)

Compound of formula (I) in free base or acid addition salt form. Wherein each R is independently hydrogen or methyl: Wherein R ₁ is hydrogen or methyl; and R ₂ is straight or branched C _1-6 alkyl: tri-C _1-3 alkylsilyl: a group of formula—CH ₂ —N (R ₃ ) ₂ [ Wherein R ₃ is each independently linear or branched C _1-4 alkyl, or two R ₃ together with their bound nitrogen atom Where n is an integer 4,5 or 6. Or general formula Form a group wherein X is -O- -S- or -NCH ₃ In which Y is-(CH ₂ ) _1-3 , -OCH ₂ -or -OCH ₂ CH ₂ -and each R ₄ is independently hydrogen or C _1-3 alkoxy. The compound according to claim 1, represented by the following general formula (Is) in free base or acid addition salt form. Wherein T is as defined in claim 1 wherein R _2S is a straight chain branched C _1-4 alkyl: tri C _1-3 alkyl silyl: or Is a group of wherein Y _S is-(CH ₂ ) _1-3 -and 4 _4S are each independently C _1-3 alkoxy. The compound of formula (Is) according to claim 2, wherein T is a group of formula (a), (c) or (d). The compound of formula (I) according to claim 1, wherein the substituents are as defined in claim 1, provided that T is not a group of formula (b) or (c). The compound of claim 1, wherein R is hydrogen, R ₂ is 2- (3,4,5-trimethoxyphenyl) ethyl present at the 4 ′ position, and T is a group (d) where R ₁ is hydrogen A compound of formula (I) in free base or acid addition salt form. The compound of claim 1, wherein R is hydrogen, R ₂ is 2- (3,4,5-trimethoxyphenyl) ethyl present at the 4 ′ position, and T is group (a), wherein R ₁ is oxygen Is methyl present at a position adjacent to the atom) or group (c), where R ₁ is methyl at a position adjacent to the sulfur atom, or: hydrogen, R ¹ , and T is group (c), where R ₁ is methyl present at the position adjacent to the sulfur atom) and R ₂ is tert-butyl present at the 4 ′ position or trimethylsilyl at the 4 ′ position of the free base or acid addition salt form of general formula (I) compound. A pharmaceutical composition comprising a compound in the form of a free base or a pharmaceutically acceptable acid addition salt according to any one of claims 1 to 6. The compound according to any one of claims 1 to 6, in free base or pharmaceutically acceptable acid addition salt form, for use as a medicament. The method of claim 8, which inhibits PAF-mediated bronchial contraction, inhibits PAF-mediated blood loss, modulates overreactivity of the airways caused by PAF or allergens, prevents endotoxin-induced hypotension, Compounds for use in preventing induced death. The compound of claim 8 for use in inhibiting the growth of lymphomas, sarcomas, myeloma and leukemia cell systems. The compound of formula (V) is dehydrated and the resulting compound of formula (I) is recovered in the form of free base or acid addition salt, thereby preparing a compound according to claim 1 in free base or acid addition salt form. How to. Wherein R, T and R ₂ are the same as defined in claim 1. A process for preparing a pharmaceutical composition, characterized in that the compound of formula (I) as defined in claim 1 in free base or pharmaceutically acceptable acid addition salt form is characterized by a pharmaceutically acceptable carrier or diluent and a compound. Use of a compound of formula (I) as defined in claim 1 in the form of a free base or a pharmaceutically acceptable acid addition salt, for the preparation of a pharmaceutical composition according to the method of claim 12. ※ Note: The disclosure is based on the initial application.