(4-甲氧基苯基)-1-吡咯烷甲酮置于cro3-3.5-Dimethylpyrazole体系中,用 二氯甲烷 作为反应溶剂,化学反应 24.0H,以70%的收率获得产物阿尼西坦 参考文献:Oxidation Of N-Acyl-Pyrrolidones To Imides With Cro3.3,5-Dimethylpyrazole 标题:Oxidation Of N-Acyl-Pyrrolidones To Imides With Cro3.3,5-Dimethylpyrazole 摘要:N-Acyl-Pyrrolidones Are Easily Obtained By Treatment Of N-Acyl-Pyrrolidines With Cro3 . 3,5-Dimethylpyrazole Complex (Cro3 . 3,5-Dmp) At Room Temperature. (C) 1997 Elsevier Science Ltd. DOI:10.1016/s0040-4039(97)10161-7
专利号:US-9662347-B2 优先权日:2010-05-11 标题 :Method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of age-albumin in cells of the mononuclear phagocyte system 发明人:LEE BONG HEE; BYUN KYUNG HEE 权利人:LEE BONG HEE; BYUN KYUNG HEE; GACHON UNIV OF INDUSTRY-ACADEMIC COOP FOUND 摘要:The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death. Therefore, the AGE-albumin synthesis inhibitor of the present invention can be valuably used in the diagnosis or treatment of degenerative diseases or autoimmune diseases such as Alzheimer's disease, strokes, Parkinson's disease, amyotrophic lateral sclerosis, rheumatoid arthritis, diabetic retinopathy, AIDS, aging, pulmonary fibrosis, spinal cord injuries, etc.
专利号:US-9371387-B2 优先权日:2011-11-10 标题 :Composition for prevention or treatment of ischemic cardiac disease, comprising inhibitor against age-albumin synthesis or release of mononuclear phagocyte system cells as active ingredient 发明人:LEE BONG HEE; BYUN KYUNG HEE 权利人:UNIV GACHON IND ACAD COOP FOUND 摘要:Disclosed is a pharmaceutical composition for the prevention or treatment of ischemic heart diseases, comprising as an active ingredient an inhibitor which acts to restrain mononuclear phagocyte system cells from synthesizing or releasing AGE-albumin, which induces the apoptosis of cardiomyocytes upon the onset of the ischemic heart disease. Also, a method is provided for screening an inhibitor against the AGE-albumin synthesis or release of mononuclear phagocyte system cells. Inhibitory or suppressive of AGE-albumin-induced cell death, the pharmaceutical composition comprising as an active ingredient an inhibitor against the AGE-albumin synthesis or release of mononuclear phagocyte system cells can be applied to the prevention or treatment of a wide spectrum of ischemic heart diseases including myocardial infarction.
专利号:WO-2023061999-A1 优先权日:2021-10-12 标 题 :Process for preparing a phenolic hydrocarbon 发明人:CORNELLA JOSEP; LE VAILLANT FRANCK 权利人:STUDIENGESELLSCHAFT KOHLE GGMBH 摘要:The present invention discloses a distinct mode of action of a nickel catalyst to forge C-0 bonds to unlock the mild utilization of N2O as O-atom transfer reagent in the synthesis of complex phenols from the corresponding aryl halides.
专利号:US-2009176740-A1 优先权日:2007-11-30 标题:Treatment of neurological conditions by the co-administration of aniracetam and l-alpha glycerylphosphorylcholine 发明人:PHILLIPS II DAUGLAS JAMES 权利人:PHILLIPS II DAUGLAS JAMES 摘要:Aniracetam (1-[(4-methoxybenzoyl)]-2-pyrrolidinone) is co-administered with the acetylcholine precursor 1-alpha glycerylphosphorylcholine (Alpha GPC, choline alfoscerate, choline alphoscerate) to potentiate cognition enhancing effects in healthy subjects and patients suffering from neurological conditions including Alzheimer's Disease (AD), attention deficit disorder (ADD), Parkinson's Disease, schizophrenia, vascular dementia, post stroke aphasia, anxiety disorders, cerebral atrophy, chronic alcoholism, Down syndrome, dyslexia, and various other neurodegenerative conditions. The co-administration of aniracetam (and other racetam derivatives including oxiracetam) with the acetylcholine precursor 1-alpha glycerylphosphorylcholine decreases negative side-effects such as severe headaches while increasing the synthesis and release of the neurotransmitters acetylcholine and glutamate to facilitate proper brain functioning.
专利号:US-9751877-B2 优先权日:2012-09-21 标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders 发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-4701465-A 优先权日:1985-04-16 标 题:N-acylpyrrolidine derivative and synthesis and use thereof 发明人:TANAKA TAKAHARU; SAITOH MASAYUKI; HASHIMOTO MASAKI; HIGUCHI NAOKI 权利人:SUNTORY LTD 摘要:The present invention relates to N-acylpyrrolidine derivatives of the general formula (I): (I) wherein R1 is a hydrogen atom, a C1-4 alkyl group or the phenyl group, with the proviso that when R1 is a hydrogen atom, R2 is phenoxy group, benzoyl, the phenyl group, or a phenyl group which is mono-substituted by a halogen atom or a C1-4 alkoxy group, and that when R1 is a C1-4 alkyl group or the phenyl group, R2 is an aralkyl group of 7 to 10 carbon atoms, a C1-4 alkyl group, the phenyl group or a phenyl group mono-substituted by a halogen atom or a C1-4 alkoxy group; or R1 and R2 together form an unsubstituted benzylidene group or a benzylidene group which may be mono-substituted by a C1-4 alkoxy group; wherein n is an integer of 0 to 5; and pharmaceutical compositions thereof which are useful as anti-amnesic agents.
1: Elston TW, Pandian A, Smith GD, Holley AJ, Gao N, Lugo JN. Aniracetam does not alter cognitive and affective behavior in adult C57BL/6J mice. PLoS One. 2014 Aug 6;9(8):e104443. doi: 10.1371/journal.pone.0104443. 2: Koliaki CC, Messini C, Tsolaki M. Clinical efficacy of aniracetam, either as monotherapy or combined with cholinesterase inhibitors, in patients with cognitive impairment: a comparative open study. CNS Neurosci Ther. 2012 Apr;18(4):302-12. doi: 10.1111/j.1755-5949.2010.00244.x. doi: 10.1080/10731190902908387. doi: 10.1055/s-0031-1296547. doi: 10.1016/j.pbb.2008.10.006. doi: 10.1016/j.jpba.2011.06.005.
合成参考文献
摘要:Casano, G.; Ouari, O., Science of Synthesis, (2021) , 59. 摘要:Medicamentos de Actualidad., 30(9), 1994 摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198 参考文献:10.1152/jn.1996.75.3.1051 摘要:Schreurs BG, Oh MM, Alkon DL. Pairing-specific long-term depression of Purkinje cell excitatory postsynaptic potentials results from a classical conditioning procedure in the rabbit cerebellar slice. Journal of Neurophysiology. 1996 Mar 01;75(3):1051–60. doi: 10.1152/jn.1996.75.3.1051.