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The present disclosure relates to compounds according to Formula (I), useful for treating diseases.

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4-Substituted-4-aminopiperidine is an interesting structural motif found in a number of bioactive compounds. An efficient and convenient method for the synthesis of 4-differently substituted-4-aminopiperidine derivatives was described, employing isonipecotate as a starting material and Curtius rearrangement as a key step. The alkylation of isonipecotate could introduce various substituents at the 4-position of the piperidine ring. With this key building block, we are able to efficiently synthesize piperazino-piperidine based CCR5 antagonist in a highly convergent manner free of using toxic reagents such as diethylaluminum cyanide. The concise synthesis of a potent bioavailable CCR5 antagonist as HIV-1 entry inhibitor, Sch-350634 (1) was accomplished in excellent yield using N?-Boc-4-methyl-4-aminopiperidine 5a as a smart building block. The new methodology provides a facile and practical access to the piperazino-piperidine amide analogs as HIV-1 entry inhibitors.

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 343788-69-2, molcular formula is C11H22N2O2, introducing its new discovery. Product Details of 343788-69-2

The present invention relates to novel indole derivatives such as compounds of the formula (I): which possess antagonist potency at the 5-HT6 receptor and the use of such compounds or pharmaceutically acceptable salts or solvates thereof in the treatment of Alzheimer’s disease and other CNS disorders.

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HEPATITIS B CAPSID ASSEMBLY MODULATORS

Described herein are hepatitis B capsid assembly modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of hepatitis B.

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Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors

A therapeutic rationale is proposed for the treatment of inflammatory diseases, such as rheumatoid arthritis (RA), by specific targeting of the JAK1 pathway. Examination of the preferred binding conformation of clinically effective, pan-JAK inhibitor 1 led to identification of a novel, tricyclic hinge binding scaffold 3. Exploration of SAR through a series of cycloamino and cycloalkylamino analogues demonstrated this template to be highly tolerant of substitution, with a predisposition to moderate selectivity for the JAK1 isoform over JAK2. This study culminated in the identification of subnanomolar JAK1 inhibitors such as 22 and 49, having excellent cell potency, good rat pharmacokinetic characteristics, and excellent kinase selectivity. Determination of the binding modes of the series in JAK1 and JAK2 by X-ray crystallography supported the design of analogues to enhance affinity and selectivity.

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EXAMPLE 284; tert-Butyl 4-[7-faminocarbonyl)-2H-indazol-2-yll-4-methylpiperidine-l-carboxylate (TJU3); Step 1: tert-Butyl 4-{[3-(methoxycarbonyl)-2-nitrobenzylidene]amino}-4-methylpiperidine- 1-carboxylate (UUl).; A mixture of methyl 3-formyl-2-nitrobenzoate Example 1, (A3) (1.0 eq.) and tert-butyl 4-amino- 4-methylpiperidine- 1-carboxylate (WO 2005/101989)(1.05 eq.) in EtOH (0.2 M) was stirred at reflux for 24 hr. Evaporation of the solvent gave the title imine which was used in the next step without further purification., 343788-69-2

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Reference£º
Patent; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI SPA; WO2007/113596; (2007); A1;,
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