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-2009131714-A1 优先权日:2005-06-08 标题:Synthesis of betulonic and betulinic aldehydes 发明人:KRASUTSKY PAVEL A; MUNSHI KALYAN 权利人:KRASUTSKY PAVEL A; MUNSHI KALYAN 摘要:The present invention provides for methods of selectively converting betulin to betulonic aldehyde. The present invention also provides for methods of selectively converting 3-substituted triterpen-28-ols to the corresponding 3-substituted triterpen-28-carboxaldehydes. Additionally, the present invention provides for methods of preparing betulonic aldehyde, betulonic acid, betulinic acid, and corresponding 3-substituted triterpenes.
专利号:US-8778958-B2 优先权日:2008-07-10 标题 :Synthesis of metabolically stable agents for alcohol and drug abuse 发明人:CASHMAN JOHN R 权利人:CASHMAN JOHN R 摘要:The disclosed opioid-related compounds and pharmaceutical compositions thereof, are useful in a variety of applications relating to the modulation of receptors and receptor signaling within and outside the nervous system. For example, the compounds and compositions are useful in methods for the treatment of addictions and other CNS-related disorders. The disclosed compounds can be delivered or administered to a mammal including humans, alone in the form of a pharmaceutically acceptable salt or hydrolysable precursor thereof, or in the form of a pharmaceutical composition, wherein a therapeutically effective amount of a compound is mixed with suitable carriers or excipients.
专利号:US-2009012088-A1 优先权日:2005-07-26 标 题:Compounds for the Treatment of Neurodegeneration and Stroke 发明人:HERGENROTHER PAUL J; PUTT KARSON S; LIU XIANJUN 权利人:HERGENROTHER PAUL J; PUTT KARSON S; LIU XIANJUN 摘要:Compounds and related methods for synthesis, and the use of compounds for the treatment of neurodegenerative diseases are disclosed. Compounds are disclosed in connection with PARG and/or PARP inhibition. Therapeutic applications are relevant for preventing or inhibiting neurological cell death for a variety of neurodegenerative conditions including Parkinson's disease, ischemia, and stroke. Also disclosed is a high-throughput screen for identifying compounds capable of inhibiting PARG and/or PARP.
专利号:US-7709465-B2 优先权日:2006-05-19 标 题:Phosphorous containing compounds including triphenylmethylphosphonate esters for the treatment of melanoma and other cancers 发明人:HERGENROTHER PAUL J; NESTERENKO VITALIY; PUTT KARSON S; PALCHAUDHURI RAHUL 权利人:UNIV ILLINOIS 摘要:Compounds and related methods for synthesis, and the use of compounds and combination therapies for the treatment of cancer and modulation of apoptosis in cells are disclosed. Particularly disclosed are phosphonate esters. Compounds, methods of making the compounds, medicaments and method of manufacture of medicaments and therapeutic methods with applications against cancer including breast cancer, melanoma, colon cancer, leukemia and lymphoma, and other cancer cells are described.
专利号:US-7807140-B2 优先权日:2006-05-03 标题 :Magnetic resonance imaging contrast agents synthesized using ring-opening metathesis polymerization 发明人:KIESSLING LAURA L; RAINES RONALD T; ALLEN MATTHEW J 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Polymeric chelating agents and metal chelates, particularly those of lanthanide metals and more specifically those of Gd(III), useful as contrast agents in magnetic resonance imaging (MRI) for therapeutic and diagnostic applications as well as clinical and biomedical research applications. The polymeric chelates are generated using ring-opening metathesis polymerization (ROMP). Polymers can have multiple sites for functionalization allowing for the synthesis of multimodal and targeted contrast agents. Hydroxypyridonate (HOPO)-based chelating moieties are integrated into a ROMP-derived polymer. More specifically, the HOPO-based chelating moiety is integrated into a benzonorbornadiene unit that constitutes the backbone of the polymer. The ROMP-derived polymer chelators can comprise multiple metal ions, particularly Gd(III) ions, in polymers of varying lengths to provide a series of agents with controlled relaxivites. Polymer chelates include those that are water-soluble.
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