专利号:US-9765027-B2 优先权日:2014-08-22 标题 :Substituted 1-arylethyl-4-acylaminopiperidine derivatives as opioid/alpha-adrenoreceptor modulators and method of their preparation 发明人:VARDANYAN RUBEN S; HRUBY VICTOR J 权利人:THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZAONA; UNIV ARIZONA 摘要:The invention provides compounds that bind with high affinities to the μ-, δ- and κ-opioid receptors and α 2 -adrenoreceptor. In addition to providing these compounds with novel pharmacological binding properties, the invention also describes detailed novel methods for the preparation of representative compounds and a scheme for the synthesis of related compounds that bind to the opioid receptors and/or α 2 -adrenoreceptor.
专利号:WO-0054773-A1 优先权日:1999-03-12 标题:Dopamine agonists in combination with nitric oxide donors, compositions and methods of use 发明人:GARVEY DAVID S 权利人:NITROMED INC; GARVEY DAVID S 摘要:The present invention is directed to novel compositions comprising at least one dopamine agonist in combination with at least one nitric oxide donor (i.e. compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are substrates for nitric oxide synthase). The novel compositions may optionally comprise at least one therapeutic agent, such as, a vasoactive agent, an antimetic agent, and mixtures thereof. The dopamine agonist is preferably apomorphine. The present invention is also directed to methods for treating and/or preventing sexual dysfunctions and/or enhancing sexual responses in patients. In other embodiments, the present invention is directed to methods treating or preventing neurodegenerative diseases, mitochondrial diseases, spinal cord injury, central or psychostimulant addiction, senile dementia, circulatory disorders, cardiovascular disorders, hyperprolactinaemia or myopia. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.
专利号:US-9994558-B2 优先权日:2013-09-20 标题 :Multicyclic compounds and methods of using same 发明人:BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).
专利号:US-10363247-B2 优先权日:2015-08-18 标 题:(S,E)-3-(6-aminopyridin-3-yl)-N-((5-(4-(3-fluoro-3-methylpyrrolidine-1-carbonyl)phenyl-7-(4-fluorophenyl)benzofuran-2-yl)methyl)acrylamide for the treatment of cancer 发明人:BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to substituted benzofuranyl compounds and, more particularly, to a compound represented by Structural Formula 1a: (I) or a pharmaceutically acceptable salt thereof. The invention also includes the synthesis and use of the compound of Structural Formula 1a, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of diseases or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, an inflammatory diseases or an immune system disease (e.g., a T-Cell mediated autoimmune disease) in a subject in need thereof. The method comprises administering to a subject in need thereof a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof, or a composition comprising a compound of the invention, or a pharmaceutically acceptable salt thereof.
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-2023271983-A1 优先权日:2020-07-29 标题 :Functionalized isonitriles and products, preparation and uses thereof 发明人:SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA 权利人:UNIV SANTIAGO COMPOSTELA 摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.
1: Campos HM, Pereira RM, de Oliveira Ferreira PY, Uchenna N, Branco da Silva CR, Pruccoli L, Sanz G, Rodrigues MF, Vaz BG, Rivello BG, Batista da Rocha AL, de Carvalho FS, Oliveira GAR, Lião LM, Georg RC, Leite JA, Dos Santos FCA, Costa EA, Menegatti R, Tarozzi A, Ghedini PC. A novel arylpiperazine derivative (LQFM181) protects against neurotoxicity induced by 3- nitropropionic acid in in vitro and in vivo models. Chem Biol Interact. 2024 May 25;395:111026. doi: 10.1016/j.cbi.2024.111026. Epub 2024 Apr 26. 124(4):28-35. Russian. doi: 10.17116/jnevro202412404128. 16(2):e53631. doi: 10.7759/cureus.53631. 4: Pokhabov DV, Tunik ME, Pokhabov DD, Katunina EA, Zalyalova ZA. Postural'naya ustoichivost' i khod'ba pri bolezni Parkinsona [Postural stability and walking in Parkinson's disease]. Zh Nevrol Psikhiatr Im S S Korsakova. 2023;123(11):29-32. Russian. doi: 10.17116/jnevro202312311129. 30(4):e14531. doi: 10.1111/cns.14531. Epub 2023 Nov 20. 6: Theleritis C, Siarkos K, Politis A, Smyrnis N, Papageorgiou C, Politis AM. A Systematic Review of Pharmacological Interventions for Apathy in Aging Neurocognitive Disorders. Brain Sci. 2023 Jul 12;13(7):1061. doi: 10.3390/brainsci13071061.
合成参考文献
参考文献:10.1016/j.neuropharm.2011.06.022 摘要:Sahlholm K, Barchad-Avitzur O, Marcellino D, Gómez-Soler M, Fuxe K, Ciruela F, Arhem P. Agonist-specific voltage sensitivity at the dopamine D2S receptor--molecular determinants and relevance to therapeutic ligands. Neuropharmacology. 2011 Oct;61(5-6):937–49. doi: 10.1016/j.neuropharm.2011.06.022.