CAS: 216976-30-6; 3-Fluoro-5-Methylbenzonitrile

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CAS号189628-39-5 3-氟--5-甲基苯甲醛 | CAS号853368-35-1 3-(溴甲基)-5-氟苯甲腈

3-氟--5-甲基苯甲醛置于吡啶,盐酸羟胺体系中,化学反应生成3-氟-5-甲基苯腈
参考文献:1,2-Diarylimidazoles As Potent,Cyclooxygenase-2 Selective,And Orally Active Antiinflammatory Agents
标题:1,2-Diarylimidazoles As Potent,Cyclooxygenase-2 Selective,And Orally Active Antiinflammatory Agents
摘要:Series Of 1,2-Diarylimidazoles Has Been Synthesized And Found To Contain Highly Potent And Selective Inhibitors Of The Human Cox-2 Enzyme. The Paper Describes A Short Synthesis Of The Target 1,2-Diarylimidazoles Starting With Aryl Nitriles. Different Portions Of The Diarylimidazole (I) Were Modified To Establish Sar. Systematic Variations Of The Substituents In The Aryl Ring B Have Yielded Very Potent (Ic50 = 10-100 Nm) And Selective (1000-12500) Inhibitors Of The Cox-2 Enzyme. The Study On The Influence Of Substituents In The Imidazole Ring Established That A Cf3 Group At Position 4 Gives The Optimum Oral Activity. A Number Of The Diarylimidazoles Showed Excellent Inhibition In The Adjuvant Induced Arthritis Model (E.G.,Ed50 = 0.02 Mph For 22 And 34). The Diarylimidazoles Are Also Potent Inhibitors Of Carrageenan-Induced Edema (Ed50 = 9-30 Mph) Sind Hyperalgesia (Ed50 = 11-40 Mpk). Several Orally Active Diarylimidazoles Show No Gi Toxicity In The Rat And Mouse Up To 200 Mpk.
Doi:10.1021/jm9700225

专利信息

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-9303000-B2
优先权日:2011-01-17
标 题 :Olefin containing nuclear transport modulators and uses thereof
发明人：SANDANAYAKA VINCENT P; SHACHAM SHARON; SHECHTER SHARON; MCCAULEY DILARA
权利人:SANDANAYAKA VINCENT P; SHACHAM SHARON; SHECHTER SHARON; MCCAULEY DILARA; KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).

专利号:US-9550757-B2
优先权日:2010-03-05
标题:Nuclear transport modulators and uses thereof
发明人：SHACHAM SHARON; KAUFFMAN MICHAEL; SANDANAYAKA VINCENT P; SHECHTER SHARON
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).