313490-35-6

Usage

Uses

Used in Pharmaceutical Industry:
1-Boc-4-(2-pyridyloxy)piperidine is used as a reactant for the preparation of pyrrolo and pyrazolopyrimidines, which are important classes of compounds with potential therapeutic applications. Specifically, these synthesized compounds serve as ubiquitin-specific protease 7 (USP7) inhibitors.
The inhibition of USP7 is of interest because this enzyme plays a crucial role in regulating the stability of proteins involved in cell cycle progression, DNA repair, and apoptosis. By targeting USP7, these pyrrolo and pyrazolopyrimidine derivatives may have potential applications in the treatment of various diseases, including cancer, by modulating the ubiquitin-proteasome pathway and affecting the degradation of key regulatory proteins.

Upstream product

• 142-08-5 2-hydroxypyridin 
• 109384-19-2 t-butyl 4-hydroxy piperidine-1-carboxylate 
• 1972-28-7 diethylazodicarboxylate 
• 109-09-1 2-chloropyridine 
• 109-04-6 2-bromo-pyridine 

Downstream Products

• 127806-46-6 2-(piperidin-4-yloxy)pyridine 
• 313490-36-7 2-(piperidin-4-yloxy)pyridine dihydrochloride 
• 868833-80-1 N-(4-chlorophenyl)-4-(pyridin-2-yloxy)piperidine-1-carbothioamide 
• 442198-38-1 (2E)-3-(4-Chlorophenyl)-N-[(1S)-2-oxo-2-({2-oxo-2-[4-(2-pyridyloxy)-1-piperidinyl]ethyl}amino)-1-(2-pyridylmethyl)ethyl]-acrylamide 
• 333990-02-6 1-Acetyl-N-(3-chlorophenyl)-N-[3-[4-(2-pyridinyloxy)-1-piperidinyl]propyl]-4-piperidinecarboxamide Trifluoroacetate 
• 1185308-16-0 2-(piperidin-4-yloxy)pyridine dihydrochloride 

Relevant academic research and scientific papers

Identification of a new series of benzothiazinone derivatives with excellent antitubercular activity and improved pharmacokinetic profiles

Nitrobenzothiazinone (BTZ) is a promising scaffold with potent activity against M. tuberculosis by inhibiting decaprenylphosphoryl-beta-d-ribose 2′-oxidase (DprE1). But unfavorable durability poses a challenge to further development of this class of agents. Herein, a series of BTZs bearing a variety of different substituents at the C-2 position were designed and synthesized. Compounds were screened for their antimycobacterial activity against Mycobacterium tuberculosis H37Ra and were profiled for metabolic stability, plasma protein-binding capacity and pharmacokinetics in vivo. In general, these new BTZs containing N-piperazine, N-piperidine or N-piperidone moiety have excellent antitubercular activity and low cytotoxicity. Several of the compounds showed improved microsomal stability and lower plasma protein-binding, opening a new direction for further lead optimization. And we obtained compound 3o, which maintained good anti-tuberculosis activity (MIC = 8 nM) and presented better in vitro ADME/T and in vivo pharmacokinetic profiles than reported BTZ compound PBTZ169, which may serve as a candidate for the treatment of tuberculosis.

PYRROLO AND PYRAZOLOPYRIMIDINES AS UBIQUITIN-SPECIFIC PROTEASE 7 INHIBITORS

The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where m, n, X1, X2, R1-R5, R5′ and R6 are described herein.

PHARMACEUTICAL COMPOUNDS

Fused pyrimidines of formula (I); wherein A represents a thiophene or furan ring; n is 1 or 2; R1 is a group of formula (II); wherein m is 0 or 1; R30 is H or C1-C6 alkyl; R4 and R5 form, together with the N atom to which they are attached, a 5- or 6-membered saturated N-containing heterocyclic group which includes 0 or 1 additional heteroatoms selected from N, S and O, which may be fused to a benzene ring and which is unsubstituted or substituted; or one of R4 and R5 is alkyl and the other is a 5- or 6-membered saturated N-containing heterocyclic group as defined above or an alkyl group which is substituted by a 5- or 6-membered saturated N-containing heterocyclic group as defined above; R2 is selected from formula (a); wherein R6 and R7 form, together with the nitrogen atom to which they are attached, a morpholine, thiomorpholine, piperidine, piperazine, oxazepane or thiazepane group which is unsubstituted or substituted; and formula (b); wherein Y is a C2-C4 alkylene chain which contains, between constituent carbon atoms of the chain and/or at one or both ends of the chain, 1 or 2 heteroatoms selected from O, N and S, and which is unsubstituted or substituted; and R3 is an indazole group which is unsubstituted or substituted; and the pharmaceutically acceptable salt thereof have activity as inhibitors of P13K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with P13 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.

3-HETEROCYCLYL-4-PHENYL-TRIAZOLE DERIVATIVES AS INHIBITORS OF THE VASOPRESSIN V1A RECEPTOR

Compounds of formula (I): or a pharmaceutically acceptable derivative thereof, wherein R represents C1-6alkyl (optionally substituted by C1-6alkyloxy or Het) or C1-6alkyloxy; R1 and R2 independently r

Peptide compounds

The present invention relates to a compound of the formula (I)wherein R1 is benzofuranyl substituted by halogen, or styryl substituted by halogen; R2 is substituted hydroxy, substituted mercapto or substituted sulfonyl; and X is or pharmaceutically acceptable salts thereof. The compound (1) of the present invention and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NO-mediated diseases in human being and animals.

Cyclic amine compounds as CCR5 antagonists

A compound of formula (I) (wherein R1is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1and R2may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Y?(R5is a hydrocarbon group; Y?is a counter anion); R3is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; R4is a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; G1is a bond, CO or SO2; G2is CO, SO2, NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent C1-3aliphatic hydrocarbon which may be substituted; provided that J is methine when G2is OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when G1is a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).