专利号:WO-0061545-A1 优先权日:1999-04-14 标题 :Methods for solid phase combinatorial synthesis of integrin inhibitors 发明人:GOPALSAMY ARIAMALA; YANG HUI YU 权利人:AMERICAN HOME PROD 摘要:Compounds of the formula (I) are useful in the treatment of various disorders including, but not limited to, cancer (tumor metathesis, tumorgenesis/tumor growth), angiogenesis (as in cancer, diabetic retinopathy, rheumatoid arthritis), restenosis (following balloon angioplasty or stent implantation), inflammation (as in rheumatoid arthritis, psoriasis), bone diseases (osteopenia induced by bone metastases, immobilization and glucocortocoid treatment, periodontal disease, hyperparathyroidism and rheumatoid arthritis), and as antiviral agents. Novel method of making compounds of formula (I) are also provided.
专利号:US-6586187-B1 优先权日:1999-04-14 标题:Methods for solid phase combinatorial synthesis of integrin inhibitors 发明人:GOPALSAMY ARIAMALA; YANG HUI Y 权利人:WYETH CORP 摘要:Compounds of the formulaare useful in the treatment of various disorders including, but not limited to, cancer (tumor metathesis, tumorgenesis/tumor growth), angiogenesis (as in cancer, diabetic retinopathy, rheumatoid arthritis), restenosis (following balloon angioplasty or stent implantation), inflammation (as in rheumatoid arthritis, psoriasis), bone diseases (osteopenia induced by bone metastases, immobilization and glucocortocoid treatment, periodontal disease, hyperparathyroidism and rheumatoid arthritis), and as antiviral agents. Novel method of making compounds of formula I are also provided.
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.
参考标题:Synthesis Of [1,2-A]-Fused Tricyclic Dihydroquinolines By Palladium-Catalyzed Intramolecular C-N Cross-Coupling Of Polarized Heterocyclic Enamines 作者:Břetislav Brož,Zdeňka Růžičková,Petr šimůnek 摘要:A Simple Methodology For [1,2-A]-Fused Tricyclic Dihydroquinolines Is Established. The Key Step Of The Methodology Is An Intramolecular Buchwald-Hartwig Amination Reaction Of Suitable Halogenated (Both Bromo And Chloro) Cyclic Enaminoketones, Enaminoesters And Enaminonitriles With Various Ring Size (From Fiveto Seven-Membered). Optimal Reaction Conditions (Palladium Source, Base, Ligand) Depend On
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摘要:Dekeukeleire, S.; D'hooghe, M.; De Kimpe, N., Science of Synthesis Knowledge Updates, (2011) 3, 104.