专利号:US-6214847-B1 优先权日:1997-08-14 标题 :Crystalline 10,10-Bis((2-fluoro-4-pyridinyl)methyl)-9(10H)-Anthracenone and an improved process for preparing the same 发明人:PESTI JAAN A; FORTUNAK JOSEPH M; HUHN GEORGE F; MAURIN MICHAEL; YIN JIANGUO 权利人:DU PONT PHARM CO 摘要:The present invention relates to processes for the synthesis of a crystalline polymorph of 10,10-Bis((2-fluoro-4-pyridinyl)methyl)-9(10H)-Anthracenone in high purity. The product is useful in the synthesis of pharmaceutical compounds for the reduction of cholinergic system dysfunction.
专利号:US-8981092-B2 优先权日:2008-09-19 标题 :Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity 发明人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO 权利人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO; NERVIANO MEDICAL SCIENCES SRL 摘要:Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, n nor pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
专利号:US-8772301-B2 优先权日:2009-12-18 标题 :Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof 发明人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D 权利人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
专利号:US-8329686-B2 优先权日:2006-08-29 标题:Isatin analogues and uses therefor 发明人:MACH ROBERT H; WELCH MICHAEL; CHU WENHUA; ROTHFUSS JUSTIN 权利人:MACH ROBERT H; WELCH MICHAEL; CHU WENHUA; ROTHFUSS JUSTIN; UNIV WASHINGTON 摘要:Novel isatin analogues, including isatin analogues comprising Michael Acceptors (IMAs) are disclosed. Further disclosed are methods of synthesis of the isatin analogues, and uses of the analogues, including inhibition of caspase-3 and caspase-7, and in vivo imaging of apoptosis by Positron emission tomography (PET) or Single Photon Emission Computed Tomography (SPECT).
专利号:WO-2016097339-A1 优先权日:2014-12-19 标题 :Labelled coumarin derivatives 发明人:JACKSON ALEXANDER; WYNN DUNCAN GEORGE; NEWINGTON IAN; JOSE JINTO; RANGASWAMY CHITRALEKHA 权利人:GE HEALTHCARE LTD 摘要:The present invention relates to compounds having selective binding for MAO-B as compared with MAO-A. The invention also provides radioactive versions of these compounds, and precursor compounds for the synthesis of these radioactive compounds. The radioactive compounds of the invention can find use for in vivo imaging applications.
专利号:WO-2016097345-A1 优先权日:2014-12-19 标题 :Labelled chromone derivatives 发明人:JACKSON ALEXANDER 权利人:GE HEALTHCARE LTD 摘要:The present invention relates to compounds having selective binding for MAO-B as compared with MAO-A. The invention also provides radioactive versions of these compounds, and precursor compounds for the synthesis of these radioactive compounds. The radioactive compounds of the invention are particularly useful for in vivo imaging applications.