专利号:WO-9517903-A1 优先权日:1993-12-28 标 题:Modular design and synthesis of oxazolone-derived molecules 发明人:HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 权利人:ARQULE PARTNERS L P; HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 摘要:The design and synthesis of novel oxazolone-derived molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recognition agents useful in the design and synthesis of drugs, and have applications in separations and materials science.
专利号:US-8198465-B2 优先权日:2005-10-17 标 题 :3-alkyl-5- (4-alkyl-5-oxo-tetrahydrofutran-2-yl) pyrrolidin-2-one derivatives as intermediates in the synthesis of renin inhibitors 发明人:SEDELMEIER GOTTFRIED; GRIMLER DOMINIQUE; ACEMOGLU MURAT 权利人:SEDELMEIER GOTTFRIED; GRIMLER DOMINIQUE; ACEMOGLU MURAT; NOVARTIS AG 摘要:The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula II, n nor a salt thereof, and a compound of formula VIn n nor a salt thereof, wherein R 3 and R 4 as well as Act are as defined in the specification, and processes of manufacturing these.n n Additionally transformation of compounds (VI) with metallo organic compounds (VII) give rise to the new compounds (VIII) which are direct precursors for the preparation of Aliskiren.
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-4599198-A 优先权日:1985-08-02 标题 :Intermediates in polypeptide synthesis 发明人:HOOVER DENNIS J 权利人:PFIZER 摘要:Bis(t-butoxycarbonyl) derivatives of phenylalanylhistidine as intermediates in the synthesis of rennin inhibiting polypeptides.
专利号:US-6413957-B1 优先权日:1998-04-21 标题:Methods of inhibiting cell proliferation using indeno [1,2-c]pyrazol-4-ones 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SUIBB PHARMA COM 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-6077962-A 优先权日:1998-12-24 标题 :N-3, 3-dimethylbutyl-L-aspartic acid and esters thereof, the process of preparing the same, and the process for preparing N-(N-(3,3-dimethylbutyl) -α L-aspartyl)-L- phenylalanine 1-methyl ester therefrom 发明人:PRAKASH INDRA; CHAPEAU MARIE-CHRISTINE D 权利人:NUTRASWEET CO 摘要:This invention relates to the chemical synthesis of N-[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester using peptide coupling methods. The coupling reaction is conducted by condensation of an activated derivative of novel N-neohexyl-L-aspartic acid with L-phenylalanine or L-phenylalanine methyl ester or by enzymatic coupling of N-neohexyl-L-aspartic acid with L-phenylalanine or L-phenylalanine methyl ester. This invention also relates to novel N-(3,3-dimethylbutyl)-L-aspartic acid, derivatives thereof and the preparation thereof. The activated derivative of N-neohexyl-L-aspartic acid may be an anhydride, mixed anhydride, active ester or an intermediate activated derivative thereof.
摘要:Wang, K. K., Science of Synthesis, (2008) 44, 259. 摘要:Bubnov, Yu. N.; Kolomnikova, G. D., Science of Synthesis Knowledge Updates, (2012) 3, 272. 摘要:Witt, D., Science of Synthesis Knowledge Updates, (2011) 3, 284. 摘要:Ishihara, K.; Sakakura, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 110. 摘要:Singh, R. P.; Deng, L., Science of Synthesis: Asymmetric Organocatalysis, (2012) 2, 48.