专利号:US-6479685-B2 优先权日:1998-01-09 标题 :Metallocene catalysts for synthesis of high-melting polyolefin copolymer elastomers 发明人:WAYMOUTH ROBERT M; KRAVCHENKO RAISA L; MACIEJEWSKI PETOFF JENNIFER; HUNG JOYCE 权利人:TRUSTEES OF THE LELAND STANDAR 摘要:Metallocene catalysts having plural coordination geometries for synthesis of high melting polyolefin copolymers suitable as thermoplastic elastomers. The inventive catalysts comprise unbridged, substituted or unsubstituted cyclopentadienyl metallocene catalysts that are capable of inter-converting between states with different polymerization or copolymerization characteristics, which interconversion is controlled by selecting the substituents of the cyclopentadienyl ligands so that the rate of interconversion of the two states is within several orders of magnitude of the rate of formation of a single polymer chain. Where r i >r f the polymer can be characterized as multiblock; where r i 专利号:US-6133409-A 优先权日:1996-12-19 标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds 发明人:SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F 权利人:AVENTIS PHARM PROD INC 摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.
专利号:US-11524957-B2 优先权日:2018-04-02 标 题 :Process for the synthesis of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one 发明人:ZHU LEI; BAILEY JOHN DANIEL; DURAK LANDON; WAETZIG JOSHUA DAVID; MIZUNO MASAHIRO; MAEDA KAZUHIRO; YASUMA TSUNEO; YAMAGUCHI HIROSHI; FUKUOKA KOICHIRO; AKIYAMA KAZUYUKI 权利人:TAKEDA PHARMACEUTICALS CO 摘要:The present invention provides processes and synthetic intermediates for the synthesis of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4 {3H)-one or a salt, hydrate, or tautomer thereof, or any combination thereof, which are Cdc7 kinase inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with Cdc7 activity.
专利号:US-7915201-B2 优先权日:2003-03-20 标 题:Ligational encoding of small molecules 发明人:FRANCH THOMAS; JACOBSEN SOEREN NYBOE; RASMUSSEN TORBEN RAVN; NEVE SOEREN; PEDERSEN HENRIK; GOULIAEV ALEX HAAHR 权利人:NUEVOLUTION AS 摘要:The invention relates to a method for synthesising a bifunctional complex comprising an encoded molecule and an identifier polynucleotide identifying the chemical entities having participated in the synthesis of the encoded molecule, said method comprising the steps of i) providing a) at least one template comprising one or more codons capable of hybridising to an anti-codon, wherein said template is optionally associated with one or more chemical entities, and b) a plurality of building blocks each comprising an anti-codon associated with one or more chemical entities, and ii) hybridising the anti-codon of one or more of the provided building blocks to the template, iii) covalently linking said anti-codons and/or linking the at least one template with the anti-codon of at least one building block, thereby generating an identifier polynucleotide capable of identifying chemical entities having participated in the synthesis of the encoded molecule, iv) separating the template from one or more of the anti-codons hybridised thereto, thereby generating an at least partly single stranded identifier polynucleotide associated with a plurality of chemical entities, v) generating a bifunctional complex comprising an encoded molecule and an identifier polynucleotide identifying the chemical entities having participated in the synthesis of the encoded molecule, wherein said encoded molecule is generated by reacting at least two of said plurality of chemical entities associated with the identifier polynucleotide, and wherein said at least two chemical entities are provided by separate building blocks.
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-6906046-B2 优先权日:2000-12-22 标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes 发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY 权利人:CELLTECH R & D INC 摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
1: Kurasawa O, Miyazaki T, Homma M, Oguro Y, Imada T, Uchiyama N, Iwai K, Yamamoto Y, Ohori M, Hara H, Sugimoto H, Iwata K, Skene R, Hoffman ID, Ohashi A, Nomura T, Cho N. Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Anti-Tumor Agent. J Med Chem. 2020 Jan 2. doi: 10.1021/acs.jmedchem.9b01427. [Epub ahead of print] doi: 10.1038/s41598-019-50732-w. 3: Iwai K, Nambu T, Dairiki R, Ohori M, Yu J, Burke K, Gotou M, Yamamoto Y, Ebara S, Shibata S, Hibino R, Nishizawa S, Miyazaki T, Homma M, Oguro Y, Imada T, Cho N, Uchiyama N, Kogame A, Takeuchi T, Kurasawa O, Yamanaka K, Niu H, Ohashi A. Molecular mechanism and potential target indication of TAK-931, a novel CDC7-selective inhibitor. Sci Adv. 2019 May 22;5(5):eaav3660. doi: 10.1126/sciadv.aav3660. eCollection 2019 May.
合成参考文献
参考文献:10.1055/s-0040-1707629 摘要:Synthesis of Simurosertib (TAK-931). Synfacts. 2020 Mar 18;16(04):0378. doi: 10.1055/s-0040-1707629. 参考文献:10.1002/cpdd.1075 摘要:Zhou X, Diderichsen PM, Gupta N. Assessment of Effects of Investigational TAK-931, an Oral Cell Division Cycle 7 Kinase Inhibitor on the QTc Intervals in Patients With Advanced Solid Tumors. Clin Pharmacol Drug Dev. 2022 Jun;11(6):770–9.