45511-81-7Relevant academic research and scientific papers
PYRIDOPYRIMIDINE COMPOUNDS ACTING AS MTORC 1/2 DOUBLE-KINASE INHIBITORS
-
, (2020/11/30)
Disclosed are a series of pyridopyrimidine compounds and a use of same in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors, and specifically disclosed is a use of the compounds as shown in formula (IV), tautomers thereof or pharmaceutically acceptable salts thereof in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors.
NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS
-
Page/Page column 35, (2008/12/07)
The present application relates to thiazolylidene containing compounds of formula (I) wherein R1, R2, R3, R4, L2 and A are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
Sulfone substituted imidazo ring ethers
-
Page/Page column 46, (2010/11/27)
Imidazo ring compounds (e.g., imidazoquinolines, 6,7,8,9-tetrahydroimidazoquinolines, imidazonaphthyridines, and 6,7,8,9-tetrahydroimidazonaphthyridines) with a sulfide-, sulfinyl-, or sulfonyl-containing ether substituent at the 1-position, pharmaceutica
SUBSTITUTED IMIDAZOQUINOLINES, IMIDAZOPYRIDINES, AND IMIDAZONAPHTHYRIDINES
-
Page/Page column 89, (2010/10/20)
Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
ARYL SUBSTITUTED IMIDAZONAPHTHYRIDINES
-
Page/Page column 132, (2008/06/13)
Imidazonaphthyridine ring systems substituted with an aryl substituent, pharmaceutical compositions containing the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of
Importance of the Aromatic Ring in Andrenergic Amines. 5. Nonaromatic Analogues of Phenylethanolamine as Inhibitors of Phenylethanolamine N-Methyltransferase: Role of Hydrophobic and Steric Interactions
Vincek, William C.,Aldrich, Constance S.,Borchardt, Ronald T.,Grunewald, Gary L.
, p. 7 - 12 (2007/10/02)
The synthesis of five classes of nonaromatic analogues of β-phenylethanolamine and an evaluation of their inhibitory potency (IC50) for phenylethanolamine N-methyltransferase (PNMT) are described.The key intermediates for the synthesis of the ethanolamines were the appropriate aldehydes or ketones.The aldehydes 11a (cyclobutyl) and 13a (cycloheptyl) of type A were prepared from the correspondingacids by reduction of the acid to the alcohol with lithium aluminum hydride and oxidation of the alcohol to the aldehyde with pyridinium chlorochromate (PCC).The aldehydes 15a (cycloundecyl) and 41a (adamantyl) of type A were prepared by oxidation of the corresponding alcohols with PCC.The first reported synthesis of cyclononanecarboxaldehyde (type A, 14a) is described.This aldehyde was prepared via a multistep route beginning with a Favorskii rearrangement of 2-bromocyclodecanone to cyclononanecarboxylic acid.The acid was reduced with lithium aluminum hydride to the corresponding alcohol, which was subsequently oxidized to the aldehyde with PCC.The aldehydes or ketones were converted (with trimethylsilyl cyanide) into their cyanohydrin ethers, which were subsequently reduced to the desired ethanolamine with lithium aluminum hydride.The ethanolamines were tested as inhibitors (LCEC assay) of PNMT.The most potent inhibitors were the type A compounds 8 (cyclooctyl), 13c (cycloheptyl), 14c (cyclononyl), and 15c (cycloundecyl) and the type D compounds 26c (cyclononyl) and 27c (cycloundecyl) with IC50 values from 6 to 17 μM.It isconcluded that the binding site of PNMT accepts hydrophobic groups of an optimal length (ca. 6.4 Angstroem) and width (ca. 2.5 Angstroem) and has a significant height restriction for the hydrophobic group.The ethanolamine side chain prefers to lie away from and in the longitudinal axis of the hydrophobic group.An ethanolamine side chain attached to a cycloalkyl ring of n carbon atoms (types A and D) is almost always considerably more potent at inhibiting PNMT than the open-chain compounds of n total carbon atoms (types B, C, and E).
Labelling of a new hypolipaemic agent with carbon 14, preparation of 1,1 bis[4 (1 carboxy 1 methylpropoxy)phenyl]cyclohexane 2 14C
Yoshitake,Makari,Kawahara,Doi
, p. 247 - 257 (2007/10/05)
1,1 Bis[4 (1 carboxy 1 methylpropoxy)phenyl] cyclohexane (S 8527) (I), a new hypolipemic agent, was labelled as C 2 with carbon 14 for the use of metabolic studies. Cyclohexane 2 14C which was prepared from potassium cyanide 14C was condensed with phenol to produce 1,1 bis(4 hydroxyphenyl)cyclohexane 2 14C (VI). Condensation of VI with ethyl methyl ketone and chloroform under a strong base (potassium hydroxide) gave S 8527 2 14C (I). A total of 3.11 mCi of pure S 8527 2 14C (I) was obtained, representing a 12% radiochemical yield from potassium cyanide 14C. Furthermore, a new radioactive by product was isolated and elucidated its structure as X.
