专利号:US-3959322-A 优先权日:1960-09-22 标 题:Synthesis of 13-alkyl-gon-4-ones 发明人:HUGHES GORDON ALAN; SMITH HERCHEL 权利人:SMITH HERCHEL 摘要:The preparation of 13-methylgon-4-enes and novel 13-polycarbonalkylgon-4-enes by a new total synthesis is described. 13-Alkylgon-4-enes having progestational, anabolic and androgenic activities are prepared by forming a tetracylic gonane structure unsaturated in the 1,3,5(10),9(11) and 14-positions, selectively reducing in the B- and C-rings, and converting the aromatic A-ring compounds so-produced to gon-4-enes by Birch reduction and hydrolysis.
专利号:US-8188113-B2 优先权日:2006-09-14 标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC 摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
专利号:US-2025289827-A1 优先权日:2022-12-02 标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof 发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN 权利人:C4 THERAPEUTICS INC 摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
专利号:US-5656634-A 优先权日:1991-03-21 标题 :N-aryl and N-heteroarylamide and urea derivatives as inhibitors of acyl coenzyme A: cholesterol acyl transferase (ACAT) 发明人:CHANG GEORGE; HAMANAKA ERNEST S; MCCARTHY PETER A; TRUONG THIEN V; WALKER FREDERICK J 权利人:PFIZER 摘要:Compounds of the formula ##STR1## the pharmaceutically acceptable salts thereof, wherein Q and R 1 are as defined below, and novel carboxylic acid and acid halide intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
专利号:US-3620700-A 优先权日:1969-08-15 标 题:Recovery of entrained carbon in synthesis gas 发明人:SCHLINGER WARREN G; SLATER WILLIAM L; DILLE ROGER M; TASSONEY JOSEPH P 权利人:WARREN G SCHLINGER; WILLIAM L SLATER; ROGER M DILLE; JOSEPH P TASSONEY 摘要:Free carbon soot entrained in the product gas of a free-flow synthesis gas generator is recovered in a sedimentation vessel as part of a thickened dispersion of solids in water from which clear supernatant water is easily separated by supplying particulate petroleum coke to the sedimentation vessel or to the reaction zone of said gas generator as a portion of the fuel, or by mixing the carbon soot-water dispersion in the sedimentation vessel with a thickened water slurry of unconverted petroleum coke such as produced by quenching in water the product gas of a second free-flow synthesis gas generator in which the fuel comprises raw particulate petroleum coke and the thickened underflow from said sedimentation vessel.
专利号:US-11434242-B2 优先权日:2017-12-04 标题:Dopamine-b-hydroxylase inhibitors 发明人:KISS LASZLO ERNO; BELIAEV ALEXANDER; ROSSI TINO; PALMA PEDRO NUNO LEAL; SOARES DA SILVA PATRÃ?CIO MANUEL VIEIRA ARAUJO; PINTO RUI; CARDONA FRANCISCO 权利人:BIAL PORTELA & Cª S A; BIAL—PORTELA & CA S A 摘要:This invention relates to: (a) compounds of formula Ia (with R1, R4 to R6, n and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-β-hydroxylase inhibitors; (b) pharmaceutical compositions (comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.
1: Yu X, Guo WH, Lin H, Cheng R, Monroy EY, Jin F, Ding L, Lu D, Qi X, Wang MC, Wang J. Discovery of a potent BTK and IKZF1/3 triple degrader through reversible covalent BTK PROTAC development. Curr Res Chem Biol. 2022;2:100029. doi: 10.1016/j.crchbi.2022.100029. Epub 2022 May 17. 2: Byun JY, Koh YT, Jang SY, Witcher JW, Chan JR, Pustilnik A, Daniels MJ, Kim YH, Suh KH, Linnik MD, Lee YM. Target modulation and pharmacokinetics/pharmacodynamics translation of the BTK inhibitor poseltinib for model-informed phase II dose selection. Sci Rep. 2021 Sep 21;11(1):18671. doi: 10.1038/s41598-021-98255-7. 3: Genovese MC, Spindler A, Sagawa A, Park W, Dudek A, Kivitz A, Chao J, Chan LSM, Witcher J, Barchuk W, Nirula A. Safety and Efficacy of Poseltinib, Bruton's Tyrosine Kinase Inhibitor, in Patients With Rheumatoid Arthritis: A Randomized, Double-blind, Placebo-controlled, 2-part Phase II Study. J Rheumatol. 2021 Jul;48(7):969-976. doi: 10.3899/jrheum.200893. Epub 2020 Dec 15.
合成参考文献
参考文献:10.1186/1756-8722-6-59 摘要:Akinleye A, Chen Y, Mukhi N, Song Y, Liu D. Ibrutinib and novel BTK inhibitors in clinical development. Journal of Hematology & Oncology. 2013 Aug 19;6(1):59. doi: 10.1186/1756-8722-6-59.