专利号:WO-2006046949-A1 优先权日:2004-10-22 标 题 :SYNTHESIS AND ANTIMALARIAL ACTIVITY OF PYRROLO[3,2-f]QUINAZOLINE-1,3- DIAMINE DERIVATIVES 发明人:AI J LIN; JIAN GUAN; QUAN ZHANG; SKILLMAN DONALD R 权利人:WALTER REED ARMY INST OF RES W; AI J LIN; JIAN GUAN; QUAN ZHANG; SKILLMAN DONALD R 摘要:The invention relates to derivatives of pyrroloquinazolinediamine, more specifically derivatives of 7-(substituted)-7H-pyrrolo[3,2-F] quinazoline-1,3-diamines that are non-toxic and are also effective in the treatment of malaria, including P. falciparum and P.vivax strains. The derivatives are certain carbamate derivatives, succinimide derivatives, alkylcarboxamides derivatives and acetamide derivative, phthalimides, alkylamines and all other amide and imide derivatives and their 1-hydroxy analogs,. The derivatives of the present invention are also soluble in common organic solvents to facilitate the purification in a large scale synthesis of the composition.
专利号:US-8293290-B2 优先权日:2003-04-08 标题:Annatto extract compositions, including geranyl geraniols and methods of use 发明人:TAN BARRIE 权利人:TAN BARRIE; AMERICAN RIVER NUTRITION INC 摘要:Annatto extract composition (AEC), including cis and trans geranyl geraniols (GG) and tocopherol-free C-5 unsubstituted tocotrienols (T3), increases the de novo synthesis of intermediate isoprenoid and distal protein products, including endogenous coenzyme Q10 (CoQ10), dolichols (DL) and all subsequent GG-prenylated and DL-glycosylated proteins, including GG-porphyrinated hemes. This intermediate and distal product replenishment by AEC reverses maladies of myotoxicity (of both drug and non-drug origins), including maladies that affect the muscle, kidney, eye, GI tract and skin, nerve, blood, and CoQ10-related syndromes of energetics and LDL protection. AEC anabolically increases the endogenous de novo CoQ10 synthesis via GG elongation/prenylation of side-chain and conversely CoQ10 catabolically increases the endogenous de novo GG synthesis via beta-oxidation of CoQ10. Also, such AEC decreases de novo synthesis and increases disposal of triglycerides (TG) in humans via PPAR activation and SREBP deactivation. Such drop in TG by AEC reverses maladies of insulin resistance (IR) and metabolic syndrome (MS), prediabetes, diabetes and diabetes-related cardiovascular diseases (CVD). GG activates PPAR and down regulates SREBP transcription factors. This AEC, containing GG, inhibits cancer growth whether or not GG involvement in protein prenylation is required.
专利号:US-7253177-B2 优先权日:2004-10-22 标 题:Synthesis and antimalarial activity of pyrrolo[3,2-f]quinazoline-1,3-diamine derivatives 发明人:LIN AI J; GUAN JIAN; ZHANG QUAN; SKILLMAN DONALD R 权利人:US ARMY 摘要:The invention relates to derivatives of pyrroloquinazolinediamine, more specifically derivatives of 7-(substituted)-7H-pyrrolo[3,2-F] quinazoline-1,3-diamines that are non-toxic and are also effective in the treatment of malaria, including P. falciparum and P. vivax strains. The derivatives are certain carbamate derivatives, succinimide derivatives, alkylcarboxamides derivatives and acetamide derivative, phthalimides, alkylamines and all other amide and imide derivatives and their 1-hydroxy analogs. The derivatives of the present invention are also soluble in common organic solvents to facilitate the purification in a large scale synthesis of the composition.
专利号:US-8067465-B2 优先权日:2002-01-15 标题:Tricyclic-bis-enone derivatives and methods of use thereof 发明人:HONDA TADASHI; FAVALORO FRANK G; GRIBBLE GORDON W; SPORN MICHAEL B; SUH NANJOO 权利人:HONDA TADASHI; FAVALORO FRANK G; GRIBBLE GORDON W; SPORN MICHAEL B; SUH NANJOO; DARTMOUTH COLLEGE 摘要:Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.
专利号:US-2009234012-A1 优先权日:2002-03-21 标题 :Administration of dopa precursors with sources of dopa to effectuate optimal catecholamine neurotransmitter outcomes 发明人:HINZ MARTIN C 权利人:HINZ MARTIN C 摘要:A method of treating neurotransmitter dysfunction in a patient by optimizing catecholamine levels by administration of L-3,4-dihydroxyphenylalanine (L-Dopa or Dopa) precursors in combination with a source of L-Dopa. The dopa precursor is preferably administered in such quantities such that the amount of dopa from the dopa precursors does not fluctuate and affect outcomes in the synthesis of dopamine from dopa administration. The dopa precursor source is preferably tyrosine, but may alternatively be phenylalanine, N-acetyl-tyrosine, any active isomer thereof, or any other dopa precursor. The source of L-Dopa may include any natural or synthetic source, including, but not limited to, Mucuna pruriens.
专利号:US-7339065-B2 优先权日:2003-07-21 标题 :Design and synthesis of optimized ligands for PPAR 发明人:AVERY MITCHELL A; PERSHADSINGH HARRIHAR A 权利人:BETHESDA PHARMACEUTICALS INC; UNIV MISSISSIPPI 摘要:This invention provides new chemical entities useful for treating a variety of clinical disorders including those that are influenced by the activity of peroxisome proliferator activated receptors (PPAR). The structures of the compounds and methods to design, make and use the compounds are provided. Compounds and methods for administering therapeutic compositions comprising the compounds in cases of the disease psoriasis are provided. An exemplary compound having the formula compound is 5adamantan-2-yl-pentanoic acid {2-[4-(2,4-dioxo-thiazolidin-5-yl-methyl)-phenoxy]-ethyl}-methyl-amide is provided.
参考标题:Spontaneous Biomimetic Formation Of (+/-)‐dictazole B Under Irradiation With Artificial Sunlight 作者:Adam Skiredj,Mehdi A. Beniddir,Delphine Joseph,Karine Leblanc,Guillaume Bernadat,Laurent Evanno,Erwan Poupon |发布日期:2014.6.16 摘要:Guided By Biosynthetic Considerations, The Total Synthesis Of Dictazole B Is Reported For The First Time. Experimental Evidence For An Easy Access To Challenging Cyclobutane Alkaloids Of Marine Origin, Which Are Often Postulated To Be Biosynthetic Precursors Of More Complex Structures, Is Provided.
合成参考文献
摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 270. 摘要:S. P. Datta and A. K. Grzybowski. In Biochemists’ Handbook, (Ed. C. Long), p. 43, E. and F. N. Spon, Ltd., London (1961). 摘要:HANSCH,C ET AL. (1995) 摘要:A.K. Grzybowski and S.P. Datta. J. Chem. Soc. 1964, 187.