68776-57-8Relevant academic research and scientific papers
COMPOUNDS AND USE THEREOF FOR THE TREATMENT OF INFECTIOUS DISEASES AND CANCER
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Page/Page column 35; 37; 41, (2021/02/26)
The invention provides the imidazole, oxazole and thiazole compounds and use thereof in methods for treating a disease or a disorder, such as infectious diseases and cancer, wherein inhibition of sphingosine-1-phosphate lyase is beneficial to treat the disease or the disorder.
Inhibition of sphingosine 1-phosphate lyase for the treatment of rheumatoid arthritis: Discovery of (E)-1-(4-((1 R,2 S,3 R)-1,2,3,4-tetrahydroxybutyl)-1 H -imidazol-2-yl)ethanone oxime (LX2931) and (1 R,2 S,3 R)-1-(2-(Isoxazol-3-yl)-1 H -imidazol-4-yl)butane-1,2,3,4-tetraol (LX2932)
Bagdanoff, Jeffrey T.,Donoviel, Michael S.,Nouraldeen, Amr,Carlsen, Marianne,Jessop, Theodore C.,Tarver, James,Aleem, Saadat,Dong, Li,Zhang, Haiming,Boteju, Lakmal,Hazelwood, Jill,Yan, Jack,Bednarz, Mark,Layek, Suman,Owusu, Iris B.,Gopinathan, Suma,Moran, Liam,Lai, Zhong,Kramer, Jeff,Kimball, S. David,Yalamanchili, Padmaja,Heydorn, William E.,Frazier, Kenny S.,Brooks, Barbara,Brown, Philip,Wilson, Alan,Sonnenburg, William K.,Main, Alan,Carson, Kenneth G.,Oravecz, Tamas,Augeri, David J.
experimental part, p. 8650 - 8662 (2011/03/19)
Sphingosine 1-phosphate lyase (S1PL) has been characterized as a novel target for the treatment of autoimmune disorders using genetic and pharmacological methods. Medicinal chemistry efforts targeting S1PL by direct in vivo evaluation of synthetic analogues of 2-acetyl-4(5)-(1(R),2(S),3(R),4- tetrahydroxybutyl)-imidazole (THI, 1) led to the discovery of 2 (LX2931) and 4 (LX2932). The immunological phenotypes observed in S1PL deficient mice were recapitulated by oral administration of 2 or 4. Oral dosing of 2 or 4 yielded a dose-dependent decrease in circulating lymphocyte numbers in multiple species and showed a therapeutic effect in rodent models of rheumatoid arthritis (RA). Phase I clinical trials indicated that 2, the first clinically studied inhibitor of S1PL, produced a dose-dependent and reversible reduction of circulating lymphocytes and was well tolerated at dose levels of up to 180 mg daily. Phase II evaluation of 2 in patients with active rheumatoid arthritis is currently underway.
METHYLENE AMINES OF THIENO [2,3-D] PYRIMIDINE AND THEIR USE AS ADENOSINE A2A RECEPTOR ANTAGONISTS
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Page/Page column 49, (2010/04/30)
This invention relates to a novel thieno[2,3-d]pyrimidine, A, and its therapeutic and prophylactic uses, wherein R1 and R2 are definedin the specification. Disorders treated and/or prevented include Parkinson's Disease.
SOLID FORMS OF (1R,2S,3R)-1-(2-(ISOXAZOL-3-YL)-1H-IMIDAZOL-4-YL)BUTANE-1,2,3,4-TETRAOL AND METHODS OF THEIR USE
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Page/Page column 5, (2009/12/28)
Solid forms of (1R,2S,3R)-1-(2-(isoxazol-3-yl)-1H-imidazol-4-yl)butane-1,2,3,4-tetraol and hydrates thereof are disclosed, as well as compositions comprising them and methods of their use.
METHODS OF PREPARING IMIDAZOLE-BASED BICYCLIC COMPOUNDS
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Page/Page column 5-6, (2009/12/28)
Methods of preparing compounds of formula I are disclosed:
