141060-29-9

Upstream product

• 3699-66-9 ethyl 2-diethoxyphosphorylpropionate 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 
• 24424-99-5 di-tert-butyl dicarbonate 
• 98080-15-0 2-[1-(phenylmethyl)-4-piperidinylidene]propanoic acid ethyl ester 
• 3612-20-2 1-phenylmethyl-4-piperidone 
• 1245507-18-9 4-(1-ethoxycarbonylethyl)-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester 
• 473837-03-5 tert-butyl 4-(1-ethoxy-1-oxopropan-2-ylidene)piperidine-1-carboxylate 

Downstream Products

• 141060-27-7 2-piperidin-4-ylpropionic acid ethyl ester 
• 1018325-29-5 4-(1-(4-chloro-5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)propan-2-yl)-1-(2,4-dichloro-5-methoxyphenyl)piperidine 
• 1018325-36-4 ethyl 2-(1-(2,4-dichloro-5-methoxyphenyl)piperidin-4-yl)propanoate 
• 1018325-34-2 ethyl 2-(1-(4-chloro-3-methoxyphenyl)piperidin-4-yl)propanoate 
• 1018325-38-6 2-(1-(2,4-dichloro-5-methoxyphenyl)piperidin-4-yl)propan-1-ol 

Relevant academic research and scientific papers

QUINOLINE AND QUINAZOLINE COMPOUNDS AND METHODS OF USE THEREOF

Compounds and methods for their preparation and use as therapeutic or prophylactic agents, fo example for treatment of cancer, bacterial or viral diseases by targeting Ectonucleotide Pyrophosphatase/Phosphodiesterase- 1 (ENPP1).

ARYL AND HETEROARYL ETHER DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE

Substituted aryl and heteroaryl ether compounds of the Formula (I) and pharmaceutically acceptable salts thereof, wherein X, R 1, R 2, R 3, L, R 4, L 1, Q, and R 5 are as defined herein. These compounds and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

Discovery of a novel series of indoline carbamate and indolinylpyrimidine derivatives as potent GPR119 agonists

GPR119 has emerged as an attractive target for anti-diabetic agents. We identified a structurally novel GPR119 agonist 22c that carries a 5-(methylsulfonyl)indoline motif as an early lead compound. To generate more potent compounds of this series, structural modifications were performed mainly to the central alkylene spacer. Installation of a carbonyl group and a methyl group on this spacer significantly enhanced agonistic activity, resulting in the identification of 2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]propyl 7-fluoro-5-(methylsulfonyl)-2,3-dihydro-1H-indole-1-carboxylate (20). To further expand the chemical series of indoline-based GPR119 agonists, several heterocyclic core systems were introduced as surrogates of the carbamate spacer that mimic the presumed active conformation. This approach successfully produced an indolinylpyrimidine derivative 37, 5-(methylsulfonyl)-1-[6-({1-[3-(propan-2- yl)-1,2,4-oxadiazol-5-yl]piperidin-4-yl}oxy)pyrimidin-4-yl]-2, 3-dihydro-1H-indole, which has potent GPR119 agonist activity. In rat oral glucose tolerance tests, these two indoline-based compounds effectively lowered plasma glucose excursion and glucose-dependent insulin secretion after oral administration.

COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS

The present invention is directed to therapeutic compotmds of the following formula (I) which have activity as agonists of GPR 119 and are useful for the treatment of metabolic disorders including type II diabetes.

PURINE DERIVATIVES USEFUL AS PI3 KINASE INHIBITORS

This invention provides a compound which is a purine of formula (Ia) or (Ib): and the pharmaceutically acceptable salts thereof that are inhibitors of PI3K and a selective for the p110δ isoform, which is a class Ia PI3 kinase, over other class Ia PI3 kinases and over class Ib kinases. The compounds may be used to treat diseases and disorders arisi from abnormal cell growth, function or behaviour associated with PI3 kinase such as cance immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.

CYCLIC DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY

The present application describes modulators of MIP-1α of formula (I), or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, A, T, R1, R2 and R8, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.

BENZIMIDAZOLONE DERIVATIVES

This invention relates to benzimidazolone derivatives, represented by compounds of a general formula [I] ???[in which R1 and R2 stand for, e.g., hydrogen atoms; R3a, R3b, R4, R5 stand for, e.g., hydrogen atoms and alkyl groups; R6 stands for e.g., aryl or heteroaryl groups; A ring stands for 5- to 8-membered aliphatic heterocyclic ring containing one nitrogen atom; and Z stands for carbonyl group or sulfonyl group]. The benzimidazolone derivatives of the invention exhibit antagonism to muscarinic acetylcholine receptors, and are useful as treating agent and/or prophylactic of Parkinson's disease; drug-induced parkinsonism, dystonia, akinesia, pancreatitis, bilestone/cholecystitis, biliary dyskinesia, achalasia, pain, itch, cholinergic urticaria, irritable bowel syndrome, vomiting, nausea, dizziness, Meniere's disease, motion sickness and urinary disturbance.