CAS: 142880-36-2; (R)-N1-((S)-3-(1H-Indol-3-yl)-1-(Methylamino)-1-Oxopropan-2-yl)-N4-Hydroxy-2-Isobutylsuccinamide

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CAS号171347-80-1 (R)-N1-((S)-3-(... | CAS号53708-63-7 (S)-2-amino-3-(... | CAS号18908-20-8 (2-甲基-2-丙烯基)琥珀酸酐 | CAS号142880-34-0 methyl (R)-3-((... | CAS号122900-21-4 b°C-trp-nhme | CAS号13139-14-5 N-B°C-L-色氨酸 | CAS号14035-83-7 dihydro-3-(RS)-... | CAS号162678-79-7 (2R)-2-(2-metho...

(2R)-N-[(2S)-3-(1H-Indol-3-yl)-1-(Methylamino)-1-Oxopropan-2-Yl]-2-(2-Methylpropyl)-N'-Phenylmethoxybutanediamide置于palladium On Activated Charcoal 氢气体系中,用 甲醇 用作溶剂,化学反应生成伊洛马司他
参考文献:Inhibition Of Membrane-Type 1 Matrix Metalloproteinase By Hydroxamate Inhibitors: An Examination Of The Subsite Pocket
标题:Inhibition Of Membrane-Type 1 Matrix Metalloproteinase By Hydroxamate Inhibitors: An Examination Of The Subsite Pocket
摘要:The Membrane-Type 1 Matrix Metalloproteinase (Mt1-Mmp) Has Been Reported To Mediate The Activation Of Pro-Gelatinase A (Prommp-2),Which Is Associated With Tumor Proliferation And Metastasis. Mt1-Mmp Can Also Digest Extracellular Matrix (Ecm) Such As Interstitial Collagens,Gelatin,And Proteoglycan And Thus May Play An Important Role In Pathophysiological Digestion Of Ecm. We Studied The Inhibitory Effect Of Various Hydroxamate Mmp Inhibitors,Including Known Inhibitors Such As Bb-94,Bb-2516,Gm6001,And Ro31-9790,On A Deletion Mutant Of Mt1-Mmp Lacking The Transmembrane Domain (Delta Mt1) To Further Characterize The Enzyme And Develop A Selective Inhibitor For Mt1-Mmp. The Evaluation Of The Inhibitory Activities Of Various Hydroxamates Reveals General Structural Profiles Affecting Selectivities Toward Mmps. In Particular,A Longer Side Chain At The P1' Position Is Preferable For The Binding To Mmp-2,-3,And-9 And Mt1-Mmp. For The P2' Position,An A-Branched Alkyl Group Is Critical For The Binding Toward Delta Mt1,While The Introduction Of A Bulky Group At The A-Position Of Hydroxamic Acid Seems To Diminish The Activity Against Delta Mt1. Summation Of The Data On The Sensitivity Of Delta Mt1 To Various Hydroxamate Inhibitors Indicates That (1) The Volume Of The S1' Subsite Of Delta Mt1 Is Similar To That Of Mmp-2,-3,And-9,Which Is Bigger Than That Of Mmp-1,And (2) The S1 And S2' Subsites Are Narrower Than Those In Other Mmps. On The Basis Of These Results,The Hydroxamates With A P1' Phenylpropyl And P2' Alpha-Branched Alkyl Group Were Synthesized And Evaluated For Inhibitory Activity. These Inhibitors (1H,I) Showed Strong Activity Against Delta Mt1 Over Mmp-1,But No Selectivity Between Delta Mt1 And Mmp-9. These Results Are Explained Using Molecular Modeling Studies Conducted On Mt1-Mmp.
Doi:10.1021/jm970404A

专利信息

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:US-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人：ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

专利号:US-2013035307-A1
优先权日:2010-01-26
标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
发明人：PRESTWICH GLENN D; KENNEDY THOMAS P
权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

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-9220714-B2
优先权日:2006-03-16
标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis
发明人：SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG
权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND
摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.