Patent classifications
C07D215/12
Quinoline compounds as modulators of RAGE activity and uses thereof
Quinoline compounds are disclosed that have a formula represented by the following: ##STR00001##
and wherein Cy, R.sup.1, R.sup.4a, R.sup.4b, and n are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diabetes complications, inflammation, and neurodegeneration, obesity, cancer, ischemia/reperfusion injury, cardiovascular disease and other diseases related to RAGE activity.
Quinoline compounds as modulators of RAGE activity and uses thereof
Quinoline compounds are disclosed that have a formula represented by the following: ##STR00001##
and wherein Cy, R.sup.1, R.sup.4a, R.sup.4b, and n are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diabetes complications, inflammation, and neurodegeneration, obesity, cancer, ischemia/reperfusion injury, cardiovascular disease and other diseases related to RAGE activity.
Amorphous dispersion of 4-methyl-3-quinolin-3-ylethynyl-benzoic acid n'-(2-chloro-6-methyl-benzoyl) hydrazide
An oral solid dosage form comprising a mixture of compound of formula I and a fusible polymeric carrier; and optionally pharmaceutically acceptable excipients, wherein the mixture is an amorphous dispersion. ##STR00001##
Amorphous dispersion of 4-methyl-3-quinolin-3-ylethynyl-benzoic acid n'-(2-chloro-6-methyl-benzoyl) hydrazide
An oral solid dosage form comprising a mixture of compound of formula I and a fusible polymeric carrier; and optionally pharmaceutically acceptable excipients, wherein the mixture is an amorphous dispersion. ##STR00001##
RETINOID DERIVATIVES WITH ANTITUMOR ACTIVITY
The present invention relates to compounds of formula (I) and to pharmaceutical compositions containing them:
##STR00001##
wherein meanings of the substituents are indicated in the description.
Such compounds for use in the treatment of cancer and other diseases related to altered angiogenesis, such as arthritic pathology, diabetic retinopathy, psoriasis and chronic inflammatory disease, are also within the scope of the present invention.
SYNTHESIS AND USE OF N-BENZYL SULFONAMIDES
Disclosed is a method for preparing N-benzyl sulfonamides. Also disclosed is a composition for treating cancer. The composition includes a N-benzyl sulfonamide and a metabolic inhibitor. Also disclosed is a method for determining the impact on cell ATP levels of a composition containing a N-benzyl sulfonamide with or without a metabolic inhibitor.
COMPOUND
A compound having a molecular weight of 3000 or less and a partial structure represented by Formula (X) is provided:
##STR00001##
In Formula (X), a ring W.sup.1 represents a ring structure having at least one double bond as a constituent element of the ring and having no aromaticity; and R.sup.3 represents a heterocyclic group, a halogen atom, a nitro group, a cyano group, a hydroxy group, a thiol group, a carboxy group, —SF.sub.5, —SF.sub.3, —SO.sub.3H, —SO.sub.2H, an aliphatic hydrocarbon group having 1 to 25 carbon atoms which may have a substituent, or an aromatic hydrocarbon group having 6 to 18 carbon atoms which may have a substituent.
COMPOUND
A compound having a molecular weight of 3000 or less and a partial structure represented by Formula (X) is provided:
##STR00001##
In Formula (X), a ring W.sup.1 represents a ring structure having at least one double bond as a constituent element of the ring and having no aromaticity; and R.sup.3 represents a heterocyclic group, a halogen atom, a nitro group, a cyano group, a hydroxy group, a thiol group, a carboxy group, —SF.sub.5, —SF.sub.3, —SO.sub.3H, —SO.sub.2H, an aliphatic hydrocarbon group having 1 to 25 carbon atoms which may have a substituent, or an aromatic hydrocarbon group having 6 to 18 carbon atoms which may have a substituent.
Heteroaromatic and Heterobicyclic Aromatic Derivatives for the Treatment of Ferroptosis-Related Disorders
The present application discloses heteroaromatic and heterobicyclic aromatic derivative compounds and compositions, and methods for treating ferroptosis-related disorders and diseases inpatients using the compounds and compositions as disclosed herein.
FUNCTIONALIZED FLUOROALKYL SILANE, AND SYNTHETIC METHOD THEREFOR AND APPLICATION THEREOF
Disclosed in the present invention are a functionalized fluoroalkyl silane compound and a synthetic method therefor. The method comprises: dissolving a halosilane and a fluoroalkyl source in an organic solvent; and synthesizing functionalized fluoroalkyl silane under the effect of an alkali or a tertiary phosphine compound. The functionalized fluoroalkyl silane can not only be used for constructing a series of high added-value compounds such as fluoroalkyl substituted alcohols, ketones and amines that can be constructed by conventional TMSR.sub.f, but also can transfer, by means of appropriate conversion, a functional group on a silicon protecting group to the obtained addition product in an addition reaction, for synthesizing some fluorine-containing compounds that cannot be synthesized by using a conventional TMSR.sub.f reagent, thereby greatly improving the synthesis efficiency and the atom economy of reactions. Also disclosed in the present invention are more excellent reaction efficiency and enantioselectivity, compared with conventional TMSCF.sub.3, exhibited by trifluoromethyl chloromethylsilane in synthesis of a 2-trifluoromethylquinoline compound and in an asymmetric trifluoromethylation reaction with α,β-unsaturated ketones.