173382-28-0Relevant academic research and scientific papers
ALTERNATIVE PROCESS FOR THE PREPARATION OF 4-PHENYL-5-ALKOXYCARBONYL-2-THIAZOL-2-YL-1,4-DIHYDROPYRIMIDIN-6-YL]METHYL]-3-OXO-5,6,8,8A-TETRAHYDRO-1H-IMIDAZO[1,5-A]PYRAZIN-2-YL]-CARBOXYLIC ACID
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Page/Page column 45-46, (2020/12/29)
The present invention relates to an alternative process for synthesizing a compound of formula (I), R1 is phenyl, which is unsubstituted or substituted with one, two or three substituents independently selected from halogen and C1-6alkyl; R2 is C1-6alkyl; R3 is -CxH2x-; x is 1, 2, 3, 4, 5, 6 or 7; or pharmaceutically acceptable salt or diastereomer thereof, which is useful for prophylaxis and treatment of a viral disease in a patient relating to hepatitis B infection or a disease caused by hepatitis B infection.
Inhibitors of 15-Prostaglandin Dehydrogenase To Potentiate Tissue Repair
Antczak, Monika I.,Zhang, Yongyou,Wang, Changguang,Doran, Jennifer,Naidoo, Jacinth,Voruganti, Sukesh,Williams, Noelle S.,Markowitz, Sanford D.,Ready, Joseph M.
, p. 3979 - 4001 (2017/05/19)
The enzyme 15-prostaglandin dehydrogenase (15-PGDH) catalyzes the first step in the degradation of prostaglandins including PGE2. It is a negative regulator of tissue repair and regeneration in multiple organs. Accordingly, inhibitors of 15-PGDH are anticipated to elevate in vivo levels of PGE2 and to promote healing and tissue regeneration. The small molecule SW033291 (1) inhibits 15-PGDH with Ki = 0.1 nM in vitro, doubles PGE2 levels in vivo, and shows efficacy in mouse models of recovery from bone marrow transplantation, ulcerative colitis, and partial hepatectomy. Here we describe optimized variants of 1 with improved solubility, druglike properties, and in vivo activity.
HEDGEHOG PATHWAY SIGNALING INHIBITORS AND THERAPEUTIC APPLICATIONS THEREOF
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Paragraph 0234; 0235, (2014/08/06)
The hedgehog (Hh) signaling pathway is a pathway which regulates patterning, growth and cell migration during embryonic development, but in adulthood is limited to tissue maintenance and repair. Mutational inactivation of the inhibitory pathway components leads to constitutive ligand-independent activation of the Hh signaling pathway, results in cancers such as basal cell carcinoma and medulloblastoma. Ligand-dependent activation of Hh signaling is involved in prostate cancer, pancreatic cancer, breast cancer and blood cancers. Therefore, inhibition of the aberrant Hh signaling represents a promising approach toward novel anticancer therapy. The invention provides novel molecules of formula I that inhibit hedgehog pathway signaling and provides therapeutic applications for the treatment of malignancies (basal cell carcinoma, medulloblastoma, glioblastoma, non-small cell lung cancer, prostate cancer, pancreatic cancer, blood cancers, mesenchymal cancers, etc.), prevention of tumor regrowth, sensitization of radio-chemo therapies, and other diseases (inflammation, fibrosis and immune disorders).
THIAZOLE COMPOUND AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0035, (2014/04/03)
The present invention relates to thiazole compounds of formula I , the method for preparation and use thereof. More specifically, the present invention relates to novel derivatives of natural product largazole, the method for preparing them and their uses
MULTIPLE KINASE PATHWAY INHIBITORS
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Page/Page column 200-201, (2014/04/17)
Kinase with inhibitory activity against kinases disposed in multiple signaling pathways and their therapeutic uses.
Platinum complex and light-emitting device
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Page/Page column 32-33, (2010/11/23)
A platinum complex represented by the general formula 1, useful as a phosphorescence emission material, a tetradentate ligand useful for synthesizing the platinum complex, and a light-emitting device containing at least one of the platinum complex. In the
