专利号:US-9346851-B2 优先权日:2008-02-22 标 题 :Chemical modification of proteins 发明人:BERNARDES GONCALO; CHALKER JUSTIN; DAVIS BENJAMIN 权利人:BERNARDES GONCALO; CHALKER JUSTIN; DAVIS BENJAMIN; RP SCHERER TECHNOLOGIES LLC 摘要:The invention relates to methods for selectively converting a cysteine residue in a peptide or protein to the dehydroalanine (Dha) residue. The method also works on selenocysteine and substituted cysteine and selenocysteine residues, resulting in the Dha residue which may be converted to any natural or unnatural amino acid residue desired without the alteration of the remainder of the peptide or protein. The invention also allows ligation of a desired peptide at any point rather than at a point where there should be a naturally occurring cysteine, thereby allowing native chemical ligation to be used in the synthesis of peptides that do not contain cysteine. The methodology allows for the synthesis of very large peptides.
专利号:US-11512097-B2 优先权日:2019-11-25 标题 :Heterocyclic compounds as Delta-5 desaturase inhibitors and methods of use 发明人:ALLEN JENNIFER R; BELTRANI MICHELA; BOURBEAU MATTHEW P; DAMYANOVA TEODORA P; LINGARD IAIN; MINATTI ANA E; VINCETTI PAOLO 权利人:AMGEN INC 摘要:The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase (“D5Dâ€?). The compounds have a general Formula I n nwherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-6586615-B1 优先权日:2001-01-10 标题:α-aminoboronic acids prepared by novel synthetic methods 发明人:KETTNER CHARLES A; JAGANNATHAN SHARADA; FORSYTH TIMOTHY PATRICK 权利人:BRISTOL MYERS SQUIBB CO 摘要:The present invention relates to a novel class of alpha-aminoboronic acids of Formula (V),which are useful as intermediates in synthetic processes for inhibitors of the serine proteases, leukocyte elastase, pancreatic elastase, cathepsin G, and chymotrypsin. More specifically, the alpha-aminoboronic acids are useful as intermediates for the synthesis of Hepatitis C Virus (HCV) protease inhibitors. This invention also generally relates to novel methods for the preparation of alpha-aminoboronic acids.
专利号:US-8722887-B2 优先权日:2006-09-22 标 题:Sulfonylpyrazole and sulfonylpyrazoline carboxamidine derivatives as 5-HT6 antagonists 发明人:VAN LOEVEZIJN ARNOLD; IWEMA BAKKER WOUTER I; KEIZER HISKIAS G; ZORGDRAGER JAN; VAN DER NEUT MARTINA A W; KRUSE CORNELIS G 权利人:VAN LOEVEZIJN ARNOLD; IWEMA BAKKER WOUTER I; KEIZER HISKIAS G; ZORGDRAGER JAN; VAN DER NEUT MARTINA A W; KRUSE CORNELIS G; ABBVIE BAHAMAS LTD 摘要:This invention concerns compounds of the general formula (1): n nand derivatives thereof, which are antagonists of 5-HT 6 receptors, wherein the symbols have the meanings given in the description. The invention also concerns methods for the preparation of these compounds, to novel intermediates useful for their synthesis, and to uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in treating at least on disease or condition chosen from Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes.
专利号:US-2011237659-A1 优先权日:2008-11-17 标题:Chromenone derivatives as trpv3 antagonists 发明人:CHAUDHARI SACHIN SUNDARLAL; THOMAS ABRAHAM; KADAM ASHOK BHAUSAHEB; DHONE SACHIN VASANTRAO; ADIK BHARAT GANGADHAR; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI 权利人:GLENMARK PHARMACEUTICALS SA 摘要:The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.
专利号:US-7696246-B2 优先权日:1999-08-27 标题:Bicyclic androgen and progesterone receptor modulator compounds and methods 发明人:ZHI LIN; VAN OEVEREN CORNELIS ARJAN; MARTINBOROUGH ESTHER 权利人:LIGAND PHARM INC 摘要:The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.
参考标题:Synthesis And Biological Activity Of Substituted 2,4-Diaminopyrimidines That Inhibit Bacillus Anthracis 作者:Baskar Nammalwar,Richard A. Bunce,K. Darrell Berlin,Christina R. Bourne,Philip C. Bourne,Esther W. Barrow,William W. Barrow |发布日期:2012.8 摘要:The Lowest Mics With Values Of 0.5 μg/ml And 0.375-1.5 μg/ml, Respectively. It Is Likely That The S Isomers Of 1 Will Bind The Substrate-Binding Pocket Of Dihydrofolate Reductase (Dhfr) As In B. Anthracis Was Found For (S)-1A. The Final Step In The Convergent Synthesis Of Target Systems 1 From (+/-)-1-(1-Substituted-2(1H)-Phthalazinyl)-2-Propen-1-Ones 6 With 2,4-Diamino-5-(5-Iodo-3,4-Dimethoxybenzyl)Pyrimidine
合成参考文献
摘要:Li, Y.; Xie, W.; Jiang, X., Science of Synthesis Knowledge Updates, (2016) 2, 27. 摘要:Gondo, C. A.; Bode, J. W., Science of Synthesis Knowledge Updates, (2012) 2, 210.