193739-32-1Relevant academic research and scientific papers
PHARMACEUTICAL FORMULATIONS USEFUL TO TREAT INFLAMMATORY AND IMMUNE DISORDERS
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, (2008/06/13)
A pharmaceutical formulation is provided for the treatment of inflammatory and/or immune disorders, particularly those mediated by platelet activating factor (“PAF”) or a product of 5-lipoxygenase. The formulation, in one embodiment, is an essentially anhydrous ointment containing an active agent selected from the group consisting of 2,5-diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines, and an enhancer composition containing one or more C3-18 esters such as diethyl succinate, propylene carbonate, diisopropyl adipate and glyceryl triacetate. In another embodiment, the formulation is a cream, gel, lotion, oil, or the like, containing the: active agent in crystalline form. The invention also encompasses the novel crystalline form of the active agent, and methods for using the formulations to treat individuals with inflammatory and/or immune disorders. Also encompassed is use of isopropyl alcohol (IPA) to enhance stability of the active agent and pharmaceutical formulations.
Synthesis of (± )trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-cyanophenyl]-5-(3,4, 5-trimethoxyphenyl) tetrahydrofuran
Balram,Ram,Ram, S. Raghu
, p. 2059 - 2062 (2007/10/03)
The synthesis of a potent platelet activating factor is described utilising commercially available acetovanillone and ethyl 3,4,5-trimethoxybenzoylacetate.
(±)-Trans-2-[3-methoxy-4-(4-chlorophenyl thioethoxy)-5-cyanophenyl]-5- (3,4,5-trimethoxyphenyl)tetrahydrofuran, a potent PAF-receptor antagonist
Ram,Balram,Sai Prakash
, p. 10163 - 10172 (2007/10/03)
The synthesis of (±)-trans-2-[3-methoxy-4- (chlorophenylthioethoxyphenyl)-5-cyanophenyl]-5-(3,4,5- trimethoxyphenyl)tetrahydrofuran from commercially available acetovanillone and 3,4,5-trimethoxybenzaldehyde is described.
(+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist.
Cai,Scannell,Yaeger,Hussoin,Killian,Qian,Eckman,Hwang,Libertine-Garahan,Yeh,Ip,Shen
, p. 1970 - 1979 (2007/10/03)
By incorporating an N-hydroxyurea functionality onto diaryltetrahydrofurans, a novel series of compounds was investigated as dual 5-lipoxygenese (5-LO) inhibitor and platelet-activating factor (PAF) receptor antagonist. These dual functional compounds wer
