- Thiadiazole amide compound and application thereof
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The invention discloses a thiadiazole amide compound and application thereof, and belongs to the field of medicines. The structural general formula of the compound is shown as a formula (I) and is a novel compound with androgen receptor antagonistic activity, wherein one of the key targets is a binding pocket between the androgen receptor ligand binding domain dimer interface. The compound provided by the invention has high activity for antagonizing the transcription of androgen receptor and is at the molecular level. The cell level and the animal level all show good biological activity, and have better safety. , The invention can be applied to the preparation of drugs for treating androgen receptor abnormal expression tumors, including but not limited to prostate cancer, metastatic prostate cancer, castration-resistant prostate cancer, breast cancer and ovarian cancer.
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Paragraph 0064; 0451-0456
(2021/09/29)
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- ISOXAZOLIDINES AS RIPK1 INHIBITORS AND USE THEREOF
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The present invention relates to isoxazolidines of formula I and their use as receptor-interacting protein kinase 1 inhibitors, for example in the treatment of diseases and disorders mediated by RIP kinase (1) such as rheumatoid arthritis (RA), psoriasis, inflammatory bowel disease (IBD), Crohn's disease or ulcerative colitis.
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Page/Page column 196
(2021/12/31)
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- Artificial Ligands of Streptavidin (ALiS): Discovery, Characterization, and Application for Reversible Control of Intracellular Protein Transport
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Artificial ligands of streptavidin (ALiS) with association constants of 106 M-1 were discovered by high-throughput screening of our chemical library, and their binding characteristics, including X-ray crystal structure of the streptavidin complex, were determined. Unlike biotin and its derivatives, ALiS exhibits fast dissociation kinetics and excellent cell permeability. The streptavidin-ALiS system provides a novel, practical compound-dependent methodology for repeated reversible cycling of protein localization between intracellular organella.
- Terai, Takuya,Kohno, Moe,Boncompain, Gaelle,Sugiyama, Shigeru,Saito, Nae,Fujikake, Ryo,Ueno, Tasuku,Komatsu, Toru,Hanaoka, Kenjiro,Okabe, Takayoshi,Urano, Yasuteru,Perez, Franck,Nagano, Tetsuo
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supporting information
p. 10464 - 10467
(2015/09/28)
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- INHIBITORS OF AKT ACTIVITY
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Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 54
(2008/12/08)
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- IMIDAZOLOPYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
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Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula ( I ) represented by the following:The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, arthritis, inflammation, and others.
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Page/Page column 92
(2008/06/13)
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- FURAN DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
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A compound of formula: (I); or a salt, solvate and chemically protected form thereof, wherein one of R2 and R5 is: (i) H or an optionally substituted C1-4 alkyl group; or (ii)an optionally substituted C5-7 aryl;
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Page/Page column 44-45
(2008/06/13)
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- Synthetic studies on prehispanolone and 14,15-dihydroprehispanolone
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Employing an intramolecular Michael addition as a pivotal step, butenolide 5, furans 6 and 7 have been converted to dioxaspiro compounds 8, 9, 10 and 11, whose heterocyclic frameworks constitute important structural units of prehispanolone (2) as well as 14,15-dihydroprehispanolones (3) and (4), respectively. Hispanolone (1) was converted to 2, 3 and 4 by utilizing a similar strategy.
- Wang, En Si,Choy, Yuen Min,Wong, Henry N. C.
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p. 12137 - 12158
(2007/10/03)
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- Two Syntheses of Manoalide via Heteroatom-Assisted Alkyne Carbometallation
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Two approaches to the sesterterpenoid phospholipase A2 inhibitors seco-manoalide (3) and manoalide (1) are described based on carbometallation of propargylic alcohols to generate the functionalised C6-C7 trisubstituted alkene.Both syntheses also deploy the photooxidation of a furan in order to generate a 4-substituted 5-hydroxy-2(5H)-furanone moiety.
- Bury, Paul,Hareau, Georges,Kocienski, Philip,Dhanak, Dashyant
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p. 8793 - 8808
(2007/10/02)
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- SYNTHESIS OF SOME FURYL- AND THIENYLACRYLATES OR DIACRYLATES AND ACRYLIC ACIDS BY THE PALLADIUM CATALYSED VINYLATION OF SUBSTITUTED BROMOFURANS AND BROMOTHIOPHENES
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Furyl- and thienylacrylates (8-14) and acrylic acids (8a,10a-14a) are prepared in moderate yields by palladium catalysed coupling of substituted bromofurans and bromothiophenes with ethyl acrylate.
- Karminski-Zamola, Grace,Dogan, Jasna,Bajic, Miroslav,Blazevic, Jelena,Malesevic, Miroslav
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p. 759 - 768
(2007/10/02)
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- Palladium Catalysis in the Synthesis of Hydroxymethylfuryl Pyrimidinyl Ketones
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Furylmethyl silyl ethers have been stannylated by means of metal-metal exchange from the corresponding lithiofurans.Unsymmetrical heteroaryl ketones are formed in palladium-catalyzed coupling reactions between the stannylfurans and 2-methylthiopyrimidine-5-carbonyl chloride.Oxidation of the sulfenyl group and subsequent hydrolysis yield 5-furoyl-2(1H)-pyrimidinones.
- Arukwe, Joseph,Undheim, Kjell
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p. 914 - 918
(2007/10/02)
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- FURANS IN SYNTHESIS 4. SILYL FURANS AS BUTENOLIDE EQUIVALENTS
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The preparation and utilization of butenolide anion equivalents 5 and 6 in alkylation sequences is described.Treatment with CH3CO3H unmasks a latent butenolide moiety providing a general route to 3- and 4-alkyl 2(5H)-furanones.
- Tanis, Steven P.,Head, David B.
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p. 4451 - 4454
(2007/10/02)
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