专利号:US-9879043-B1 优先权日:2013-06-06 标 题:Synthesis of non-natural cofactor analogs of S-adenosyl-L-methionine using methionine adenosyltransferase 发明人:THORSON JON; HUBER TYLER; ZHANG JIANJUN; Singh Shanteri 权利人:UNIV KENTUCKY RES FOUND 摘要:The present disclosure relates to the synthesis of non-natural analogs of S-adenosyl-L-methionine (SAM) and/or of Se-adenosyl-L-methionine (SeAM) by reacting a methionine analog and adenosine triphosphate (ATP) in the presence of at least one methionine adenosyltransferase (MAT), and to use thereof with downstream SAM and/or SeAM utilizing enzymes. The non-natural analogs of SAM and/or SeAM have the general formula: n nwhere X is S or Se, and R 1 is an alkyl group.
专利号:US-9402842-B2 优先权日:2012-04-13 标题:Synthesis and use of dual tyrosyl-DNA phosphodiesterase I (Tdp1)—topoisomerase I (Top1) inhibitors 发明人:CUSHMAN MARK S; NGUYEN TRUNG X; CONDA-SHERIDAN MARTIN M; POMMIER YVES GEORGE 权利人:PURDUE RESEARCH FOUNDATION 摘要:The invention described herein pertains to the synthesis and use of certain N-substituted indenoisoquinoline compounds which inhibit the activity Tyrosyl-DNA Phosphodiesterase I (Tdp1) or Topoisomerase I (Top1) or both, or otherwise demonstrate anticancer activity. Also disclosed are novel N-substituted indenoisoquinoline compounds and pharmaceutical compositions comprising the novel N-substituted indenoisoquinoline compounds.
专利号:WO-2019013789-A1 优先权日:2017-07-12 标 题 :ANTIMICROBIAL COMPOUNDS 发明人:REDDY HARIPRASADA R KANNA; SEBAHAR PAUL R; SERRANO CATHERINE M; LOOPER RYAN E 权利人:CURZA GLOBAL LLC; THE UNIV OF UTAH RESEARCH FOUNDATION 摘要:The invention relates to compounds of formula I or their pharmaceutically acceptable salts. The compounds of formula I are antimicrobial agents which inhibit, for example, Mycobacterium tuberculosis (Mtb) H37Ra. The compounds of formula I also have anti-tuberculous activity, exhibit limited cytotoxicity and inhibit protein synthesis. The invention also relates to methods of making compounds of formula I, as well as methods of using compounds of formula I for the treatment of bacterial infections, particularly tuberculosis.
专利号:WO-0027817-A1 优先权日:1998-11-10 标 题:Oxazolidinones useful as alpha 1a adrenoceptor antagonists 发明人:NERENBERG JENNIE B; BOCK MARK G; PATANE MICHAEL A; SELNICK HAROLD G 权利人:MERCK & CO INC; NERENBERG JENNIE B; BOCK MARK G; PATANE MICHAEL A; SELNICK HAROLD G 摘要:Novel hydroxymethyl- and alkoxymethyl-oxazolidinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered uring flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
专利号:WO-0027827-A1 优先权日:1998-11-10 标题:Oxazolidinones useful as alpha 1a adrenoceptor antagonists 发明人:NERENBERG JENNIE B; BOCK MARK G; SELNICK HAROLD G; PAYNE LINDA 权利人:MERCK & CO INC; NERENBERG JENNIE B; BOCK MARK G; SELNICK HAROLD G; PAYNE LINDA 摘要:Novel oxazolidinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
专利号:EP-1200395-B1 优先权日:1999-07-28 标 题:Urea derivatives as inhibitors of ccr-3 receptor 发明人:PADIA JANAK; HOCKER MICHAEL D; OHASHI HIROSHI; NISHITOBA TSUYOSHI; SAWA EIJI 权利人:KIRIN BREWERY 摘要:Urea and thiourea derivatives inhibit cell function of the chemokine receptor CCR-3. These compounds offer an effective means for treating a range of diseases thought to be mediated by the CCR-3 receptor. A variety of useful urea and thiourea derivatives can be synthesized using liquid and solid phase synthesis protocols.
[参考文献]: Alexei Pushechnikov, Et Al. Rational Design Of Ligands Targeting Triplet Repeating Transcripts That Cause Rna Dominant Disease: Application To Myotonic Muscular Dystrophy Type 1 And Spinocerebellar Ataxia Type 3. J Am Chem Soc. 2009 Jul 22;131(28):9767-79. [参考文献]: H Kinemuchi, Et Al. Inhibition Of Tissue-Bound Semicarbazide-Sensitive Amine Oxidase By Two Haloamines, 2-Bromoethylamine And 3-Bromopropylamine. Arch Biochem Biophys. 2001 Jan 1;385(1):154-61. [参考文献]: M W Crankshaw, Et Al. Modification Of Cysteine. Curr Protoc Protein Sci. 2001 May:Chapter 15:Unit15.1. [参考文献]: Qiang Chen, Et Al. Direct Pore Binding As A Mechanism For Isoflurane Inhibition Of The Pentameric Ligand-Gated Ion Channel Elic. Sci Rep. 2015 Sep 8:5:13833. [参考文献]: R A Jue, Et Al. Identification Of Cysteine Residues Alkylated With 3-Bromopropylamine By Protein Sequence Analysis. Anal Biochem. 1993 Apr;210(1):39-44.
合成参考文献
摘要:Podlech, J., Science of Synthesis Knowledge Updates, (2013) 2, 276.