685827-77-4

Usage

Common Use

Pharmaceutical research and development

Derivative of

Piperidine (a six-membered heterocyclic ring containing nitrogen)

Role

Building block for the synthesis of various pharmaceuticals

Applications

Antihistamines, antipsychotics, neurological disorders, and cancer treatment

Chemical Structure

Versatile molecule for the development of new drugs and therapeutic agents

Upstream product

• 1068-57-1 acetic acid hydrazide 
• 84358-13-4 N-[(tert-butoxy)carbonyl]piperidine-4-carboxylic acid 

Downstream Products

• 280110-69-2 4-(5-methyl-[1,3,4]oxadiazol-2-yl)-piperidine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

Development of autotaxin inhibitors: A series of tetrazole cinnamides

A series of inhibitors of Autotaxin (ATX) have been developed from a high throughput screening hit, 1a, which shows an alternative binding mode to known catalytic site inhibitors. Selectivity over the hERG channel and microsomal clearance were dependent on the lipophilicity of the compounds, and this was optimised by reduction of clogD whilst maintaining high affinity ATX inhibition. Compound 15a shows good oral exposure, and concentration dependent inhibition of formation of LPA in vivo, as shown in pharmacokinetic-pharmacodynamic (PK/PD) experiments.

2,3-DIHYDROFURO[2,3-B]PYRIDINE COMPOUNDS

The present invention provides a compound of Formula I: wherein R is H or F; or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula I for treatment of neurodegenerative diseases, such as Alzheimer's disease.

AUTOTAXIN INHIBITORS COMPRISING A HETEROAROMATIC RING-BENZYL-AMIDE-CYCLE CORE

The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.

TRIAZOLE COMPOUNDS FOR THE TREATMENT OF DYSMENORRHOEA

A compound of formula (I), a pharmaceutically acceptable salt or solvate thereof, wherein R' represents C,-C6 alkyl,-(CH2)c-[C3-C8 cycloalkyl]-,-(CH2)C-W or-(CH2)C-Z-(CH2)dW; W represents C1-C6 alkyl, C1-C6 alkyloxy,-C02[C1-C6 alkyl],-CONR4R5, an optionally substituted phenyl group, NR4R5, het2 or het3; Z represents O or S(O)g; g represents 0, 1 or 2; R2 represents a phenyl group, optionally fused to a 5-or 6-membered aryl or heterocyclic group which may contain one or more heteroatoms selected from N, O or S; the phenyl group and the optionally fused group being optionally substituted; Ring A represents a 4-, 5-or 6-membered saturated heterocyclic group containing at least one N; Ring B represents a phenyl group or het1, each group being optionally substituted; R7 independently represents H1 C1-C6alkyl, OR3,-(CH2)e-R3 or-(CH2)f-O-(CH2)e-R3; at each occurrence R3 independently represents H1 C1-C6 alkyl optionally substituted by Y,-(CH2)g [C3-C8 cycloalkyl], phenyl, benzyl, pyridyl or pyrimidyl; at each occurrence R4 and R5independently represent H1 Cl-C6 alkyl (optionally substituted with Cl-C6alkyloxy), (CH2)gC02-[C1-C6 alkyl],-S02Me,-(CH2)g[C3-C8 cycloalkyl], S02Me, phenyl, benzyl, pyridyl or pyrimidyl; or R4 and R5 together with the N atom to which they are attached represent a heterocyclic group of from 3 to 8 atoms; Y independently represents a phenyl group, NR4R5 or het4, the phenyl group being optionally substituted; het1 represents a 4-, 5-or 6-membered saturated, or unsaturated, heterocyclic group containing at least one N (but which may also contain one or more O or S atoms); het2 and het4 represent an optionally substituted 4-, 5-, 6-or 7-membered saturated, or unsaturated, heterocyclic group containing at least one N (but which may 5 also contain one or more O or S atoms); het3 represents an optionally substituted 4-, 5-, 6-or 7-membered saturated, or unsaturated, heterocyclic group containing at least one O (but which may also contain one or mare N or S atoms); at each occurrence R6 independently represents H1 C1-C6 alkyl optionally substituted by Y, =(CH2)g [C3-C8 cycloalkyl], phenyl, benzyl, pyridyl or pyrimidyl; a and b independently represent 0 or 1; c,, d, a end g independently represent 0, 1, 2, 3 or 4; . f índeperldently represents 1, 2, 3 or 4; provided that: (i) a + b cannot equal 0; and províded,that,when R1 represents-(CH2)c-Z-(CH2)d-W and W represents.NR4R5 or any N linked heterocyclic, group then d must not be, 0 or 1; and (iii), provided that when R2 represents a phenyl group substituted by a group of, formula-(CH2)eOR3,-(CH2)e-OCOR3 or-(CH2)e,OCOR3 ;or het1,and/or het2 are substituted by a group of formula-(CH2)eOR3, (CH2),-CO2R3 or-(CH2)eOCOR3; or when R7 represents-OR3 or-(CH2)f-0-(CH2)e-R3 and e is 0; or when W represents a phenyl group substituted with-OR3 or-C02R3 and R3 represents an alkyl group substituted with Y, and Y represents NR4R5 or an N-Finked het3; then, R3, must,represent,C2-C6 alkyl substituted with. Y. are useful in the treatment of dysmenorrhoea.