专利号:US-2012253038-A1 优先权日:2009-04-13 标 题:Processes for the synthesis of bazedoxifene acetate and intermediates thereof 发明人:JOSHI SHREERANG; BHUTA SACHIN; TALUKDAR SANJAY; SAWANT SUDHIR; VENKATRAMAN DEEPAK 权利人:JOSHI SHREERANG; BHUTA SACHIN; TALUKDAR SANJAY; SAWANT SUDHIR; VENKATRAMAN DEEPAK; SANDOZ AG 摘要:Efficient processes for the synthesis of pharmaceutically useful compounds such as (1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1H-indol-5-ol acetic acid commonly known as bazedoxifene acetate (Formula IX) using cyanomethoxybenzyl halides of Formula III, where X=Halogens e.g., Cl, F, Br, I; G=Any electron donating or electron withdrawing substituent.
专利号:US-3985835-A 优先权日:1973-07-30 标题 :Halogenated esters of phosphorus-containing acids 发明人:D ALELIO GAETANO F 权利人:ALELIO GAETANO F D 摘要:This invention deals with new phosphorus-containing esters having the formula R'''2NP(O) (ORCX=CXR')2 wherein X represents Cl or Br; R represents a divalent hydrocarbon radical of 1-20 carbon atoms; R' represents H, X or R''; R'' represents a monovalent hydrocarbon radical of 1-20 carbon atoms; R''' represents hydrogen, a monovalent hydrocarbon radical of 1-20 carbon atoms, a divalent saturated aliphatic hydrocarbon group having 5 carbon atoms between valencies and forming a cyclic structure with the N, or a derivative of said monovalent hydrocarbon radical in which the derivative group is hydroxy, NH2, NHR'', NR''2, -NR''''K, R''''NHNHC(O)-, R''''NHC(O)NH-, -(N-R-)n-NR'''' , ¦¦ KK R''COO-, R''CONH- or R''O, R'''' represents hydrogen or R''; n represents an integer having a value of 0-50; and K represents hydrogen, R'' or -P(O) (ORCX=CXR')2. These new esters are useful particularly as fire retardants, agricultural chemicals, fuel additives, plasticizers, monomers and intermediates for the synthesis of other useful derivatives.
专利号:US-9724682-B2 优先权日:2013-02-26 标 题 :Synthesis of acyclic and cyclic amines using iron-catalyzed nitrene group transfer 发明人:BETLEY THEODORE ALEXANDER; HENNESSY ELISABETH THERESE 权利人:HARVARD COLLEGE 摘要:The present invention provides novel synthetic methods for making acyclic secondary amines by reacting an azide with a compound bearing one or more C—H groups, catalyzed by a Fe II -dipyrromethene complex. The acyclic secondary amines are thought to be formed through an intermolecular nitrene transfer. Also provided herein are methods of synthesizing protected (e.g., Boc- or Fmoc-protected) cyclic secondary amines (e.g., 5-, 6-, and 7-membered cyclic secondary amines) by reacting an azide that bears one or more C—H groups, catalyzed by a Fe II -dipyrromethene complex. The protected cyclic secondary amines are thought to be formed through an intramolecular nitrene transfer and may be subsequently deprotected to yield cyclic secondary amines.
专利号:US-2025188083-A1 优先权日:2021-06-25 标 题:Modulators of Histone Acetyltransferase 1 and Methods of Treatment Thereof 发明人:GRUBER JOSHUA JAMES; LIPCHIK ANDREW; SNYDER MICHAEL P; SCHOW STEVEN R 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Small molecules compounds and methods of their synthesis are provided. Small molecules identified can inhibit histone acetyltransferase 1 activity. Formulations and medicaments are also provided that are directed to the treatment of human disorders and conditions, such as, for example, neoplasms, cancers, viral, fungal, and parasitic infections, and aging. Therapeutics are also provided containing a therapeutically effective dose of one or more small molecule compounds, present either as pharmaceutically effective salt or in pure form, including, but not limited to, formulations for oral, intravenous, or intramuscular administration.
专利号:EP-3904354-A1 优先权日:2020-04-30 标 题:New imidazolone derivatives as inhibitors of protein kinases in particular dyrk1a, clk1 and/or clk4 权利人:PERHA PHARMACEUTICALS 摘要:The present invention relates to a compound of formula (I)n nwherein R 1 represents a (C 1 -C 6 )alkyl group, a spiro(C 5 -C 11 )bicyclic ring, a fused phenyl group, a substituted phenyl group, a R'-L- group, wherein L is either a single bond or a (Ci-C3)alkanediyl group, and R' represents a (C 3 -C 8 )cycloalkyl group, a bridged (C6-C 10 )cycloalkyl group, a (C 3 -C 8 )heterocycloalkyl group, or a (C 3 -C 8 )heteroaryl group, or a R'-L- group wherein L is a (Ci-C3)alkanediyl group, and R' is a an optionally substituted phenyl group or any of its pharmaceutically acceptable salt. n The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates. n It also relates to said compound for use as a medicament, in particular in the treatment and/or prevention of cognitive deficits associated with Down syndrome; Alzheimer's disease; dementia; tauopathies; Parkinson's disease; CDKL5 Deficiency Disorder; Phelan-McDermid syndrome; autism; diabetes; regulation of folate and methionine metabolism; osteoarthritis; Duchenne muscular dystrophy; several cancers; neuroinflammation, anemia and infections and for regulating body temperature.
专利号:US-5064962-A 优先权日:1989-02-23 标题:Diaminothiophenes 发明人:WIESENFELDT MATTHIAS; ETZBACH KARL-HEINZ 权利人:BASF AG 摘要:Diaminothiophenes of the formula or tautomers thereof, where R1 and R2 are each hydrogen or together are where T1 is hydrogen, alkyl or phenyl, T2 and T3 are, independently of one another, alkyl or phenyl, or T2 and T3 together with the nitrogen linking them are a heterocyclic radical, R3 is substituted amino and R4 is alkanoyl, benzoyl, cyano, nitro or where T4 is hydrogen, alkyl or phenyl and T5 is the radical of a primary amine or of an active methylene compound, are prepared as described. The present diaminothiophene compound is useful in the synthesis of dyes, crop protection agents and pharmaceuticals.
摘要:Wessjohann, L. A.; Kaluđerović, G. N.; Neves Filho, R. A. W.; Morejon, M. C.; Lemanski, G.; Ziegler, T., Science of Synthesis: Multicomponent Reactions, (2013) 1, 449. 摘要:Monguchi, Y.; Sajiki, H., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 2, 353.