31602-64-9Relevant academic research and scientific papers
MACROCYCLIC COMPOUNDS AS STING AGONISTS AND METHODS AND USES THEREOF
-
Paragraph 0241-0242, (2021/01/29)
Disclosed are macrocyclic compounds having the general Formula (I) or (II) and their tautomeric forms, stereoisomers, pharmaceutically acceptable salts, hydrates, solvates and prodrugs thereof, and their combination with suitable medicament, corresponding processes for the synthesis and pharmaceutical compositions and uses of compounds disclosed herein.
New thiadiazole derivatives
-
Page/Page column 49-50, (2011/04/25)
The present invention relates to thiadiazole derivatives of formula (I), to processes for their preparation and to pharmaceutical compositions containing them. These compounds are potent agonists of S1P1 receptors and thus, they are useful in the treatment, prevention or suppression of diseases and disorders known to be susceptible to improvement by sphingosine-1-phosphate receptors agonists (S1P1), such as autoimmune diseases, chronic immune and inflammatory diseases, transplant rejection, malignant neoplastic diseases, angiogenic-related disorders, pain, neurological diseases, viral and infectious diseases.
NEW THIADIAZOLE DERIVATIVES
-
Page/Page column 72, (2011/04/24)
The present invention relates to thiadiazole derivatives of formula (I), to processes for their preparation and to pharmaceutical compositions containing them. These compounds are potent agonists of S1P1 receptors and thus, they are useful In the treatment, prevention or suppression of diseases and disorders known to be susceptible to improvement by sphingosine-1-phosphate receptors agonists (S1P1), such as autoimmune diseases, chronic immune and inflammatory diseases, transplant rejection, malignant neoplastic diseases, angiogenic-related disorders, pain, neurological diseases, viral and infectious diseases.
Synthesis and preliminary evaluation of amiloride analogs as inhibitors of the urokinase-type plasminogen activator (uPA)
Matthews, Hayden,Ranson, Marie,Tyndall, Joel D.A.,Kelso, Michael J.
scheme or table, p. 6760 - 6766 (2011/12/05)
A known side-activity of the oral potassium-sparing diuretic drug amiloride is inhibition of the enzyme urokinase-type plasminogen activator (uPA, K i = 7 μM), a promising anticancer target. Several studies have demonstrated significant antitum
DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-α]IMIDAZOLE-3- CARBOXYLIC ACID AMIDES
-
Page/Page column 98-99, (2009/07/03)
Derivatives of 6,7-dihydro-5H-imidazo[1,2-α]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
VIGABATRIN BIOISOTERES AND RELATED METHODS OF USE
-
Page/Page column 7; 14, (2010/11/26)
Compounds bioisoteric to vigabatrin and related methods of use.
Carboxylate bioisosteres of pregabalin
Schwarz, Jacob B.,Colbry, Norman L.,Zhu, Zhijian,Nichelson, Brian,Barta, Nancy S.,Lin, Kristin,Hudack, Raymond A.,Gibbons, Sian E.,Galatsis, Paul,DeOrazio, Russell J.,Manning, David D.,Vartanian, Mark G.,Kinsora, Jack J.,Lotarski, Susan M.,Li, Zheng,Dickerson, Melvin R.,El-Kattan, Ayman,Thorpe, Andrew J.,Donevan, Sean D.,Taylor, Charles P.,Wustrow, David J.
, p. 3559 - 3563 (2007/10/03)
Several β-amino tetrazole analogs of gabapentin 1 and pregabalin 2 were prepared by one of two convergent, highly efficient routes, and their affinity for the α2-δ protein examined. Two select compounds with potent affinity for α2-δ,
New substrates and inhibitors of γ-aminobutyric acid aminotransferase containing bioisosteres of the carboxylic acid group: Design, synthesis, and biological activity
Yuan, Hai,Silverman, Richard B.
, p. 1331 - 1338 (2007/10/03)
A series of potential substrates of γ-aminobutyric acid aminotransferase (GABA-AT) with lipophilic bioisosteres of the carboxylic acid group (2-7) were synthesized and tested. Most of the synthesized compounds showed substrate activities with GABA-AT; 1H-tetrazole-5-propanamine (6) was the best of those tested. The potential time-dependent inhibitor of GABA-AT, 1H-tetrazole-5-(α-vinyl-propanamine) (8), was designed based on the structures of 6 and the antiepilepsy drug vigabatrin (4-aminohex-5-enoic acid, 1). The synthesized compound 8 showed time-dependent inhibition of GABA-AT, but its potency is lower than that of vigabatrin. Methylation of the tetrazole group in 8 resulted in loss of time-dependent activity, suggesting that the tetrazole ring, the carboxylate bioisostere, exists in its deprotonated form in the enzyme active site.
ORGANIC COMPOUNDS
-
Page/Page column 37, (2008/06/13)
Compounds of Formula (I); in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
Efficient syntheses of 5-aminoalkyl-1H-tetrazoles and of polyamines incorporating tetrazole rings
Athanassopoulos, Constantinos M.,Garnelis, Thomas,Vahliotis, Dimitrios,Papaioannou, Dionissios
, p. 561 - 564 (2007/10/03)
(Chemical Equation Presented) Linear Nω-tritylated ω-amino thiobenzylamides and Nα,Nω- ditritylated polyamino mono- or bisthioamides were efficiently converted to the corresponding tetrazole derivatives upon treatment with
