CAS: 197516-48-6; 5-Hydrazinyl-2-Methylpyridine

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CAS号80287-53-2 3-氨基-6-甲基吡啶 | CAS号323578-37-6 N-B°C-6-甲基-3-氨基吡啶 | CAS号21203-68-9 2-甲基-5-硝基吡啶 | CAS号4548-45-2 2-氯-5-硝基吡啶 | CAS号280132-79-8 di-tert-butyl 1... | CAS号110-86-1 吡啶

📜2-甲基-5-硝基吡啶置于palladium On Activated Charcoal 盐酸,氢气,Sodium Nitrite体系中,用 1,4-二氧六环 用作溶剂,化学反应 29.5H,反应生成5-肼基-2-甲基吡啶
参考文献:Structure−activity Relationships Of The P38α Map Kinase Inhibitor 1-(5-Tert-Butyl-2-P-Tolyl-2H-Pyrazol-3-yl)-3-[4-(2-Morpholin-4-Yl-Ethoxy)Naph-Thalen-1-Yl]Urea (Birb 796)
标题:Structure−activity Relationships Of The P38α Map Kinase Inhibitor 1-(5-Tert-Butyl-2-P-Tolyl-2H-Pyrazol-3-yl)-3-[4-(2-Morpholin-4-Yl-Ethoxy)Naph-Thalen-1-Yl]Urea (Birb 796)
摘要:We Report On The Structure-Activity Relationships (Sar) Of 1-(5-Tert-Butyl-2-P-Tolyl-2H-Pyrazol-3-yl)-3-[4-(2-Morpholin-4-Yl-Ethoxy)Naphthalen-1-Yl]Urea (Birb 796),An Inhibitor Of P38Alpha Map Kinase Which Has Advanced Into Human Clinical Trials For The Treatment Of Autoimmune Diseases. Thermal Denaturation Was Used To Establish Molecular Binding Affinities For This Class Of P38Alpha Inhibitors. The Tert-Butyl Group Remains A Critical Binding Element By occupying A Lipophilic Domain In The Kinase Which Is Exposed Upon Rearrangement Of The Activation Loop. An Aromatic Ring Attached To N-2 Of The Pyrazole Nucleus Provides Important Pi-Ch2 Interactions With The Kinase. The Role Of Groups Attached Through An Ethoxy Group To The 4-Position Of The Naphthalene And Directed Into The Atp-Binding Domain Is Elucidated. Pharmacophores With Good Hydrogen Bonding Potential,Such As Morpholine,Pyridine,And Imidazole,Shift The Melting Temperature Of P38Alpha By 16-17 Degreesc Translating Into K-D Values Of 50-100 Pm. Finally,We Describe Several Compounds That Potently Inhibit Tnf-Alpha Production When Dosed Orally In Mice.
Doi:10.1021/jm030121K

专利信息

专利号:US-8188113-B2
优先权日:2006-09-14
标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
发明人：FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC
摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

专利号:US-6492529-B1
优先权日:2000-01-18
标题 :Bis pyrazole-1H-pyrazole intermediates and their synthesis
发明人：KAPADIA SURESH R; SONG JINHUA J; YEE NATHAN K
权利人:BOEHRINGER INGELHEIM PHARMA
摘要:Disclosed are aromatic heterocyclic compounds of the formula (I) wherein Ar 1 , Ar 2 , L, Q and X are described herein, and intermediate compounds useful for making such compounds. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. n Also disclosed are processes of making compounds of the formula (I), their intermediates and processes of making such intermediates, including bis pyrazole-1H-pyrazole intermediates of the formula: n wherein Alk, R x and R z are described herein.

专利号:US-2004210052-A1
优先权日:2001-11-02
标题:Efficient synthesis of 5-heteroatom-containing-pyrazoles