420-04-2 + 4885-03-4 = 79463-77-7 [标题:Reaction Conditions 标题:Diphenyl Cyanocarbonimidate. A Versatile Synthon For The Construction Of Heterocyclic Systems 作者:Webb,R. Lee; Labaw,Clifford S. 参考文献:Journal Of Heterocyclic Chemistry 日期:1982 卷标:19(5) 页码:1205-6]
420-04-2 + 4885-03-4 = 79463-77-7 [标题:Reaction Conditions 标题:Imidic Acids And Derivatives,Isoureas And Derivatives,Sulfur And Selenium Equivalents,And Analogously Substituted Methylenephosphines 作者:Gilchrist,T. L. 参考文献:Science Of Synthesis 日期:2005 卷标:18 页码:1001-1076
专利号:WO-2008105759-A1 优先权日:2007-02-27 标 题:Methods for synthesis of modified peptides 发明人:BROWER JUSTIN O 权利人:ARGOLYN BIOSCIENCE INC; BROWER JUSTIN O 摘要:Methods for the synthesis of peptides and peptide analogs containing aminoacid residues bearing substituted amino- and guanido- sidechains, such as alkyl lysine and arginine residues, are provided.
专利号:US-2008214827-A1 优先权日:2004-02-03 标 题:Synthesis of Cyanoimino-Benzoimidazoles 发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN 权利人:EURO CELTIQUE SA 摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.
专利号:US-5710249-A 优先权日:1989-10-30 标题 :Amino acids and processes for making peptides using same 发明人:HOEGER CARL A; RIVIER JEAN E F; PORTER JOHN S 权利人:SALK INST FOR BIOLOGICAL STUDI 摘要:Methods of making unnatural amino acids are provided which unnatural amino acids can be incorporated into peptides which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. These unnatural amino acids are useful in the synthesis of peptides and have the formula (a): where W is (CH2) or n is an integer from 1 to 6; j=1, 2 or 3, and preferably, Y is N-CN, X is NH and R2 is alkyl, modified alkyl, alkenyl, alkynyl, aryl or methyl pyridyl. Disclosed are peptides that are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions.
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.
专利号:US-5169932-A 优先权日:1989-10-30 标题 :Gnrh analogs 发明人:HOEGER CARL A; RIVIER JEAN E F; THEOBALD PAULA G; PORTER JOHN S; RIVIER CATHERINE L; VALE JR WYLIE W 权利人:SALK INST FOR BIOLOGICAL STUDI 摘要:Peptides which include unnatural amino acides and which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such peptides that are GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The antagonists may be used to treat steroid-dependent tumors, such as prostatic and mammary tumors. The peptides are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-position, the 5-position, the 6-position and/or the 8-position. Such unnatural amino acids are useful in the synthesis of peptides and have the formula U*: where n is an integer from 1 to 6; Y is N-CN, N-CONHR9, S, O or CH-NO2; R9 is H, Ac, lower alkyl, aromatic or heterocyclic; X is NH, O, S, M1(CHq)pM2 or M1-(CH2)p'-M2(CH2)p''-M3, where M1 is NR10, O, S or CHR3 wherein R3 is methyl, ethyl, propyl, phenyl, pyridinyl, pyrimidinyl or purinyl, q is 1 or 2; p, p' and p'' are integers between O and 6; R10 is H, lower alkyl or the like, and M2 and M3 are M1, COOH, CONH2, COOR3 or CN; R1 is H, alkyl, modified alkyl, alkenyl, alkynyl, aryl or a direct bond to X; R2 is R1, OH, NH2, NHR1, or heterocycle.
专利号:WO-0009116-A1 优先权日:1998-08-14 标 题:Grp receptor ligands 发明人:XIANG JIA-NING; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV 权利人:SMITHKLINE BEECHAM CORP; XIANG JIA NING; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV 摘要:Novel GRP receptor antagonists are provided. Methods of using the present compounds to antagonize GRP receptors are also provided. The present invention further involves the synthesis of the present compounds.
[参考文献]: Bassem Sadek, Et Al. Synthesis And Dual Histamine H And H Receptor Antagonist Activity Of Cyanoguanidine Derivatives. Molecules. 2013 Nov 15;18(11):14186-202.
合成参考文献
摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003). 摘要:Curtis, A. D. M., Science of Synthesis, (2004) 13, 606. 摘要:Gilchrist, T. L., Science of Synthesis, (2005) 18, 1029. 摘要:Gilchrist, T. L., Science of Synthesis, (2005) 18, 1038. 摘要:Drabowicz, J.; Lewkowski, J.; Kudelska, W.; Girek, T., Science of Synthesis, (2008) 39, 179.