专利号:US-9464021-B2 优先权日:2013-11-01 标题 :Method of preparation of stereospecific quinone derivatives 发明人:MEHTA DILIP S; MOHAN PRIYA; SHASTRI MAYANK; REID TED 权利人:MEHTA DILIP S; MOHAN PRIYA; SHASTRI MAYANK; REID TED 摘要:The description provides processes for the regio and stereospecific synthesis of polyprenylatedquinone derivatives, such as Vitamin K1, K2 and Ubiquinone, exploiting dithioacetals, especially 1,3-dithiane, mediated Umpolung chemistry which works along a new concept “Inhibiting resonance delocalization (IRD)†to overcome isomerization generated due to delocalization of allyliccarbanion on the Ï€-electron cloud of an allylic systems by the conventional synthesis.
专利号:US-8853228-B2 优先权日:2007-06-04 标 题:Heterocyclic analogs of propargyl-linked inhibitors of dihydrofolate reductase 发明人:ANDERSON AMY C; WRIGHT DENNIS L; FREY KATHLEEN MARY; PAULSEN JANET LEIGH; SCOCCHERA ERIC WILLIAM; VISWANATHAN KISHORE 权利人:ANDERSON AMY C; WRIGHT DENNIS L; FREY KATHLEEN MARY; PAULSEN JANET LEIGH; SCOCCHERA ERIC WILLIAM; VISWANATHAN KISHORE; UNIV CONNECTICUT 摘要:The compositions and methods described herein disclose the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus , fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii . These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.
专利号:US-8426432-B2 优先权日:2007-06-04 标 题 :Inhibitors of dihydrofolate reductase with antibacterial antiprotozoal, antifungal and anticancer properties 发明人:ANDERSON AMY C; WRIGHT DENNIS L; PELPHREY PHILLIP M; JOSKA TAMMY M; BOLSTAD ERIN S D; BOLSTAD DAVID B; POPOV VELJKO 权利人:ANDERSON AMY C; WRIGHT DENNIS L; PELPHREY PHILLIP M; JOSKA TAMMY M; BOLSTAD ERIN S D; BOLSTAD DAVID B; POPOV VELJKO; UNIV CONNECTICUT 摘要:The compositions and methods described herein discloses the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus , fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii . These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.
专利号:CN-118878430-A 优先权日:2024-08-13 标 题 :Compound, synthesis method thereof and synthesis method of 5, 6-dihydroxyindole
专利号:US-2007099880-A1 优先权日:2003-11-24 标 题:Estrogen receptor modulators 发明人:BLIZZARD TIMOTHY A; GUDE CANDIDO; MORGAN JERRY D II 权利人:BLIZZARD TIMOTHY A; GUDE CANDIDO; MORGAN JERRY D II 摘要:The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.
专利号:WO-2025026392-A1 优先权日:2023-08-02 标题 :Kinesin kif18a inhibitor and use thereof 发明人:XIAO YISONG; LAI KUNMIN; GU XIAOHUI; WANG MINGHUA; DENG JIACHEN; HU MIN 权利人:SHANGHAI APEIRON THERAPEUTICS COMPANY LTD 摘要:A KIF18 inhibitor having a structure as shown in formula (I) and a synthesis method therefor. The compound can be used to adjust the KIF18A protein, thereby affecting a cell cycle and cell proliferation process for the treatment of cancer and cancer-related diseases. Further disclosed are a pharmaceutical composition containing the compound, and a method for the treatment of conditions associated with KIF18A activity.
参考标题:Divergent Enantioselective Synthesis Of (−)-Galanthamine And (−)-Morphine 作者:Barry M. Trost,Weiping Tang,F. Dean Toste |发布日期:2005.10.1 摘要:Tricyclic Intermediate Is Available In Six Steps From 2-Bromovanillin And The Monoester Of Methyl 6-Hydroxycyclohexene-1-Carboxylate. This Intermediate Requires Only Two Steps To Convert To (-)-Galanthamine. Using A Heck Vinylation, We Found That The Fourth Ring Of Codeine/morphine Could Be Formed. The Final Ring Formation Involves A Novel Visible Light-Promoted Hydroamination. Thus, Six Steps Are Required