16152-51-5Relevant articles and documents
PHENYL-TRIAZOLO-PYRIDINE COMPOUNDS
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Paragraph 0045, (2017/02/24)
The present invention provides a compound of the Formula (I) below: wherein R1 is selected from the group consisting of H, CH3, CN, —CH2CN, —C(CH3)2CN, F, Cl, and Br; R2 is selected from the group consisting of H, —O(C1-C3alkylene)R4, —CH2CN, CN, —OCH3, CF2, —C(CH3)2CN, —C(CH3)2, —S(O)2CH3, —S(O)2NH2, and —OCF2; R3 is selected from the group consisting of H, CH3, and —OCH3; and R4 is selected from the group consisting of H, —C(CH3)2CN, —OCH3, —S(O)2CH3, CN, and —C(CH3)2OH; or a pharmaceutical salt thereof, methods of treating type two diabetes using the compound and a process for preparing the compound.
Metabolically stable tert-butyl replacement
Barnes-Seeman, David,Jain, Monish,Bell, Leslie,Ferreira, Suzie,Cohen, Scott,Chen, Xiao-Hui,Amin, Jakal,Snodgrass, Brad,Hatsis, Panos
, p. 514 - 516 (2013/07/26)
Susceptibility to metabolism is a common issue with the tert-butyl group on compounds of medicinal interest. We demonstrate an approach of removing all the fully sp3 C-Hs from a tert-butyl group: replacing some C-Hs with C-Fs and increasing the s-character of the remaining C-Hs. This approach gave a trifluoromethylcyclopropyl group, which increased metabolic stability. Trifluoromethylcyclopropyl-containing analogues had consistently higher metabolic stability in vitro and in vivo compared to their tert-butyl-containing counterparts.
Propanoic acid derivatives
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, (2008/06/13)
Propanoic acid derivatives of formula (1) are described: Ar—X1—Ar1—Z—R??(1) in which Ar is a nitrogen base containing group; X1is linker atom or group; Ar1is an optionally substituted 5- or 6-membered nitrogen-containing aromatic or non-aromatic monocycle; Z is a group —CH(R13)CH2— [in which R13is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group], —C(R12a)(R13)—CH(R12b)— [in which R12aand R12btogether with the carbon atoms to which they are attached form a C3-7cycloalkyl group] or C(R13)═CH—; R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of αVintegrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
