专利号:US-2012077802-A1 优先权日:2009-06-10 标题 :Histamine h3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are spiro-cyclic compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
专利号:US-11034695-B2 优先权日:2016-09-23 标 题:Dopamine-β-hydroxylase inhibitors 发明人:SOARES DA SILVA PATRÃ?CIO; ROSSI TINO; KISS LASZLO ERNO; BELIAEV ALEXANDER; LEAL PALMA PEDRO NUNO 权利人:BIAL—PORTELA & CA S A; BIAL—PORTELA & Cᵃ S A 摘要:This invention relates to: (a) compounds of Formula Ia (with R1, R4, R5, R6, n and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-β-hydroxylase inhibitors; (b) pharmaceutical compositions comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.
专利号:US-2008096883-A1 优先权日:2004-08-11 标题 :Trifluoromethyl substituted benzamides as kinase inhibitors 发明人:CARAVATTI GIORGIO; FURET PASCAL; IMBACH PATRICIA; MARTINY-BARON GEORG; PEREZ LAWRENCE BLAS; SHENG TAO 权利人:CARAVATTI GIORGIO; FURET PASCAL; IMBACH PATRICIA; MARTINY-BARON GEORG; PEREZ LAWRENCE BLAS; SHENG TAO 摘要:The invention relates to trifluoromethyl substituted benzamide compounds of the formula (I), pharmaceuticals comprising these compounds, their use as or for the manufacture of pharmaceuticals, particularly as inhibitors of protein kinases and/or the treatment of a condition, disorder or disease state mediated by a protein kinase activity and/or a proliferative disease, methods of treatment comprising administering the compounds, especially of therapeutic and prophylactic treatment, methods for the manufacture of the compounds and novel intermediates and partial steps for their synthesis.
专利号:EA-020243-B1 优先权日:2009-05-29 标题:SPYROEPOXIDES AS INTERMEDIATE PRODUCTS OF SYNTHESIS
[参考文献]: Keith W Woods, Et Al. Synthesis And Sar Of Indazole-Pyridine Based Protein Kinase B/akt Inhibitors. Bioorg Med Chem. 2006 Oct 15;14(20):6832-46.
合成参考文献
摘要:Sapeta, K.; Kerr, M. A., Science of Synthesis Knowledge Updates, (2011) 1, 18.