专利号:US-9353112-B2 优先权日:2012-03-07 标 题 :Synthesis of polycyclic alkaloids 发明人:GOFF DANE; PAYAN DONALD G; BRASELMANN SYLVIA 权利人:RIGEL PHARMACEUTICALS INC 摘要:Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.
专利号:US-7858808-B2 优先权日:2002-05-31 标 题:Multi-substituted imidazolines and method of use thereof 发明人:TEPE JETZE J; PEDDIBHOTLA SATYAMAHESHWAR 权利人:UNIV MICHIGAN STATE 摘要:A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-κB as well as potent activity against the Gram (+) bacterium B. subtillus and B. cereus with MIC values in the range of 50 μm/mL.
专利号:US-12194020-B2 优先权日:2017-12-22 标 题:Reversing baldness through cannabinoid receptor activation 发明人:POSTREL RICHARD 权利人:POSTREL RICHARD 摘要:This invention reverses male pattern baldness by shocking dormant hair follicles out of their androgen induced hibernation phase back to the active hair-growing anagenic phase. The invention integrates two functions: 1) It blocks synthesis of compounds holding the follicles in the telogenic/hibernating phase and 2) It stimulates synthesis of compounds animating the hair-growing/anagenic phase in the follicular activity cycle. One preferred embodiment comprises an enzyme inhibitor blocking the conversion of testosterone to dihydrotestosterone (DHT), a flavonoid simultaneously increasing synthesis of prostaglandins alternative to prostaglandin D2, and a selected cannabinoid compound stimulating restore the hair follicle to its normal growth cycle. This novel trimodal therapy restores the hair follicles to their normal cycling processes and maintains these restorative properties so long as this rebalance in maintained.
专利号:US-2018312534-A1 优先权日:2015-10-16 标题:Fluorescent anticancer platinum drugs 发明人:SARKAR ARINDAM; MANDAL SWADHIN KUMAR; SENGUPTA ANIRUDDHA; BISWAS GOUTAM; DUTTA PRADIP; SHARMA RUPALI; RAJ JUSTIN PAUL; SURYAVANSHI HEMANT; KUMARI SMITA 权利人:INVICTUS ONCOLOGY PVT LTD 摘要:The present disclosure is in relation to the field of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to fluorescent platinum based compounds. The disclosure further relates to synthesis of said fluorescent platinum based compounds, nanoparticles and compositions comprising said fluorescent platinum based compounds/nanoparticles. The disclosure also relates to methods of managing cancer by the fluorescence changes between aforesaid platinum based compounds and corresponding free ligands, nanoparticles and compositions.
专利号:US-7345078-B2 优先权日:2002-05-31 标题 :NF-κB inhibitors and uses thereof 发明人:TEPE JETZE J; PEDDIBHOTLA SATYAMAHESHWAR 权利人:UNIV MICHIGAN STATE 摘要:A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma, etc.), antibacterial agents, and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-κB as well as potent activity against the Gram (+) bacterium. The compositions are also useful for treating autoimmune diseases and for inhibiting rejection of organ and tissue transplants.
专利号:US-7888394-B2 优先权日:2006-08-21 标 题:Synthesis, polymorphs, and pharmaceutical formulation of FAAH inhibitors 发明人:PUTMAN DAVID; DASSE OLIVIER 权利人:ORGANON NV 摘要:Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. The alkylcarbamic acid aryl ester of Formula (I), KDS-4103, is a FAAH inhibitor. Described herein is a process for the preparation of the compound of Formula (I), characterization of polymorphs of the FAAH inhibitor, and their uses therof.
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合成参考文献
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