128225-42-3

Basic information

• Product Name: 1-Piperidinecarboxylicacid,4-amino-3-methoxy-,ethylester(9CI)
• Synonyms: 1-Piperidinecarboxylicacid,4-amino-3-methoxy-,ethylester(9CI);ethyl 4-amino-3-methoxypiperidine-1-carboxylate
• CAS NO: 128225-42-3
• Molecular Formula: C9H18N2O3
• Molecular Weight: 202.25
• Product Categories: AMINOACID
• Mol File: 128225-42-3.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 1-Piperidinecarboxylicacid,4-amino-3-methoxy-,ethylester(9CI)(CAS DataBase Reference)
• NIST Chemistry Reference: 1-Piperidinecarboxylicacid,4-amino-3-methoxy-,ethylester(9CI)(128225-42-3)
• EPA Substance Registry System: 1-Piperidinecarboxylicacid,4-amino-3-methoxy-,ethylester(9CI)(128225-42-3)

Safety Data

• Hazardous Substances Data: 128225-42-3(Hazardous Substances Data)

Upstream product

• 83898-43-5 ethyl 3-hydroxy-4,4-dimethoxy-1-piperidinecarboxylate 
• 83863-71-2 ethyl (3RS,4SR)-4-amino-3-methoxypiperidine-1-carboxylic acid hydrochloride Salt 
• 83863-72-3 (-)-ethyl 3-methoxy-4-oxo-1-piperidine-carboxylate 
• 83863-73-4 (-)-ethyl 3,4,4-trimethoxy-1-piperidinecarboxylate 
• 29976-53-2 N-ethoxycarbonyl-4-piperidone 
• 907543-85-5 ethyl (3R,4S)-4-(benzylamino)-3-methoxypiperidine-1-carboxylate 
• 907543-86-6 ethyl (3S,4R)-4-(benzylamino)-3-methoxypiperidine-1-carboxylate 
• 100-46-9 benzylamine 

Relevant articles and documents

Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent

A series of novel benzamide derivatives, altering the 4-fluorophenylalkyl moiety in cisapride, were synthesized as 5-HT4 receptor agonists, and SAR of these analogs was examined on in vitro and in vivo prokinetic activities. These compounds were synthesized for high 5-HT4 receptor binding affinities and low hERG affinities. Several types of analogs were obtained and screened for 5-HT4 binding, hERG blocking, agonism, and gastric emptying assessment. Among the analogues, compound 23g showed promising results compared with the other analogs with respect to gastric emptying rates in rats. Therefore, we suggest that it may be a clinical candidate for the development of a potent prokinetic agent to treat GI disorders.

Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099)

AZD5099 (compound 63) is an antibacterial agent that entered phase 1 clinical trials targeting infections caused by Gram-positive and fastidious Gram-negative bacteria. It was derived from previously reported pyrrolamide antibacterials and a fragment-based approach targeting the ATP binding site of bacterial type II topoisomerases. The program described herein varied a 3-piperidine substituent and incorporated 4-thiazole substituents that form a seven-membered ring intramolecular hydrogen bond with a 5-position carboxylic acid. Improved antibacterial activity and lower in vivo clearances were achieved. The lower clearances were attributed, in part, to reduced recognition by the multidrug resistant transporter Mrp2. Compound 63 showed notable efficacy in a mouse neutropenic Staphylococcus aureus infection model. Resistance frequency versus the drug was low, and reports of clinical resistance due to alteration of the target are few. Hence, 63 could offer a novel treatment for serious issues of resistance to currently used antibacterials.

CONDENSED PYRIDINE COMPOUND

The present invention provides a compound having excellent JAK3 inhibitory activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases. As a result of investigations with respect to novel condensed heterocyclic derivatives, the inventors have verified that a condensed pyridine compound has excellent JAK3 inhibitory activity, thereby completing the present invention. More specifically, it has been verified that since the compound according to the present invention has inhibitory activity against JAK3, the compound is useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transduction (e.g., rejection during live organ/tissue transplantation, autoimmune diseases, asthma, atopic dermatitis, rheumatism, psoriasis and atherosclerotic disease), or diseases caused by abnormal cytokine signal transduction (e.g., cancer and leukemia).

CHEMICAL COMPOUNDS

Compounds of formula (I) and their pharmaceutically acceptable salts are described: formula (I). Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.

DIMETHYLBENZOFURAN AND DIMETHYLBENZOPYRAN DERIVATIVES AND THEIR USE AS 5-HT3 ANTAGONISTS

Method of treating 5-HT 3-mediated disorders, which comprises systemic administration of an effective amount of a compound of formula (I) STR1 the pharmaceutically acceptable acid addition salt forms and the stereochemically isomeric forms thereof, wherein R 1 and R 2 represent hydrogen, or R 1 and R 2 taken together form a bivalent radical of formula--CH=CH--CH=CH--(a),--CH=C(Cl)--CH= CH--(b) or--CH=CH--C(Cl)=CH--(c); n represents 2, 3 or 4; R. sup.3 represents hydrogen or methoxy; m represents 1 or 2; R 4 represents hydrogen, amino or C 1-3-alkylcarbonylamino; and R 5 represents hydrogen or halo; novel compounds; compositions; processes for preparing novel compounds and intermediates.

4-(aroylamino)piperidine-butanimide derivatives

A method of treating warm-blooded animals suffering from diarrhea, which method comprises the administration of particular 4-(aroylamino)piperidinebutanamide derivatives and compositions containing the same. Novel 4-(aroylamino)piperidinebutanamide deriva

Novel N-(3-hydroxy-4-piperidinyl)benzamide derivatives

Novel N-(3-hydroxy-4-piperidinyl)benzamides and derivatives thereof, said compounds being useful as stimulators of the motility of the gastro-intestinal system.