CAS: 1020315-31-4; N-(Pyridazin-3-yl)-4-(3-((5-(Trifluoromethyl)Pyridin-2-yl)Oxy)Benzylidene)Piperidine-1-Carboxamide

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CAS号1020327-61-0 phenyl pyridazi... | CAS号76925-49-0 ethyl pyridazin... | CAS号1020325-30-7 2-(3-(氯甲基)苯氧基)-... | CAS号1020325-22-7 [3-[[5-(trifluo... | CAS号620-24-6 3-羟基苯甲醇 | CAS号52334-81-3 2-氯-5-三氟甲基吡啶

📜2-氯-5-三氟甲基吡啶置于盐酸,氯化亚砜,Potassium Tert-Butylate,水,Potassium Carbonate,N,N-二异丙基乙胺体系中,用 四氢呋喃,1,4-二氧六环,二氯甲烷,N,N-二甲基甲酰胺,乙腈 用作溶剂,化学反应 50.0H,反应生成N-哒嗪-3-基-4-(3-{[5-(三氟甲基)吡啶-2-基]醚}苯亚甲基丙酮)哌啶-1-羧酰胺
参考文献:Discovery Of Pf-04457845: A Highly Potent,Orally Bioavailable,And Selective Urea Faah Inhibitor
标题:Discovery Of Pf-04457845: A Highly Potent,Orally Bioavailable,And Selective Urea Faah Inhibitor
摘要:Fatty Acid Amide Hydrolase (Faah) Is An Integral Membrane Serine Hydrolase That Degrades The Fatty Acid Amide Family Of Signaling Lipids,Including The Endocannabinoid Anandamide. Genetic Or Pharmacological Inactivation Of Faah Leads To Analgesic And Anti-Inflammatory Phenotypes In Rodents Without Showing The Undesirable Side Effects Observed With Direct Cannabinoid Receptor Agonists,Indicating That. Faah May Represent An Attractive Therapeutic Target For The Treatment Of Inflammatory Pain And Other Nervous System Disorders. Herein,We Report The Discovery And Characterization Of A Highly Efficacious And Selective Faah Inhibitor Pr-04457845 (23). Compound 23 Inhibits Faah By A Covalent,Irreversible Mechanism Involving Carbamylation Of The Active-Site Serine Nucleophile Of Faah With High In Vitro Potency (K(Inact)/k(I) And Ic(50) Values Of 40300 M(-1) S(-1) And 7.2 Nm,Respectively,For Human Faah). Compound 23 Has Exquisite Selectivity For Faah Relative To Other Members Of The Serine Hydrolase Superfamily As Demonstrated By Competitive Activity-Based Protein Profiling. Oral Administration Of 23 At 0.1 Mg/kg Results In Efficacy Comparable To That Of Naproxen At 10 Mg/kg In A Rat Model Of Inflammatory Pain. Compound 23 Is Being Evaluated In Human Clinical Trials.
Doi:10.1021/ml100190T

专利信息

专利号:US-12194020-B2
优先权日:2017-12-22
标 题:Reversing baldness through cannabinoid receptor activation
发明人：POSTREL RICHARD
权利人:POSTREL RICHARD
摘要:This invention reverses male pattern baldness by shocking dormant hair follicles out of their androgen induced hibernation phase back to the active hair-growing anagenic phase. The invention integrates two functions: 1) It blocks synthesis of compounds holding the follicles in the telogenic/hibernating phase and 2) It stimulates synthesis of compounds animating the hair-growing/anagenic phase in the follicular activity cycle. One preferred embodiment comprises an enzyme inhibitor blocking the conversion of testosterone to dihydrotestosterone (DHT), a flavonoid simultaneously increasing synthesis of prostaglandins alternative to prostaglandin D2, and a selected cannabinoid compound stimulating restore the hair follicle to its normal growth cycle. This novel trimodal therapy restores the hair follicles to their normal cycling processes and maintains these restorative properties so long as this rebalance in maintained.