142121-94-6Relevant academic research and scientific papers
HETEROARYL DERIVATIVES
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Paragraph 0502; 0503; 0504; 0505, (2015/06/17)
Compounds of formula (I) described herein are both phosphodiesterase 4 (PDE4) enzyme inhibitors and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction.
HETEROARYL DERIVATIVES FOR THE TREATMENT OF RESPIRATORY DISEASES
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Page/Page column 116; 117, (2015/06/18)
The invention relates to novel compounds of formula (I) which are both phosphodiesterase 4 (PDE4) enzyme inhibitors and muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
PHENYLETHYLPYRIDINE DERIVATIVES AS PDE4-INHIBITORS
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Page/Page column 69; 70, (2014/06/24)
The invention relates to novel compounds which are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
NOVEL COMPOUNDS
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Page/Page column 33, (2014/06/23)
Compounds of formula (I) defined herein are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of a disease of the respiratory tract characterized by airway obstruction.
GLYCINE DERIVATIVES AND THEIR USE AS MUSCARINIC RECEPTOR ANTAGONISTS
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Page/Page column 64-65, (2012/06/15)
The present invention relates to alkaloid aminoester derivatives acting as muscarinic receptor antagonists, processes for their preparation, compositions comprising them and therapeutic uses thereof.
GLYCINE DERIVATIVES AND MEDICINAL COMPOSITIONS THEREOF
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Page/Page column 30, (2012/06/16)
Alkaloid aminoester derivatives according to formula (I) and (VI) act as muscarinic receptor antagonists.
One-pot synthesis of α-amino acids from imines through CO2 incorporation: An alternative method for strecker synthesis
Mita, Tsuyoshi,Chen, Jianyang,Sugawara, Masumi,Sato, Yoshihiro
, p. 1393 - 1396 (2011/04/22)
Itas a gas: A novel one-pot process for the synthesis of α-amino acids from imine equivalents using CO2 gas as a carbon source has been developed. This reaction was made possible by the reagent combination of TMSSnBu3 and CsF (see scheme). Three successive reactions (imine formation, stannylation, and carboxylation) proceeded in the same flask under these conditions to give products in up to 79 % yield. Boc=tert-butoxycarbonyl, TMS=trimethylsilyl.
Highly selective tripeptide thrombin inhibitors
Shuman,Rothenberger,Campbell,Smith,Gifford-Moore,Gesellchen
, p. 314 - 319 (2007/10/02)
Tripeptide aldehydes such as Boc-D-Phe-Pro-Arg-H (5l) exhibit potent direct inhibition of thrombin. This distinction offers important insight for the design of more potent and selective serine protease inhibitors which may be useful pharmacological tools and hold promise for development of clinically useful agents. The structure-activity relationships (SAR) on a series of anticoagulant peptides with high selectivity for the enzyme thrombin are discussed. The SAR is centered on a series of di- and tripeptide arginine aldehydes based on the structure of 5l. The structural and conformational role of the amino acid residue in position 1 was investigated by substitution with conformationally restricted aromatic amino acids, aromatic acids, and a dipeptide isostere containing the ψ[CH2N] amide bond replacement. Many of these peptides demonstrate potent antithrombotic activity along with selectivity toward thrombin, determined by comparison of in vitro inhibitory effects on trypsin, plasmin, factor Xa, and tissue plasminogen activator. Compound 5f, D-1-Tiq-Pro-Arg-H · sulfate is highly active and the most selective tripeptide aldehyde inhibitor of thrombin reported to date.
Site selective substitution of carbamate and carbamoyl protected benzylamines
Katsoulos,Schlosser
, p. 6263 - 6264 (2007/10/02)
Methoxy and fluoro substituted benzylamines can be metalated optionally at the position adjacent to the nitrogen bearing side chain or adjacent to the hetero substituent as a function of the acyl type protective group.
