Patent classifications
A61K31/4035
Lactuloside compounds and preparation and use thereof
The present disclosure relates to the field of pharmaceutical chemistry, and particularly to a compound represented by Formula (I), a preparation method and medical use thereof. In the compound represented by Formula (I), a lactulosyl group is connected to a heteroatom of genin (G) via a glycosidic bond, wherein the genin (G) is a group formed by removing one hydrogen atom from a heteroatom of an active pharmaceutical molecule, and “” indicates that the lactulosyl group is connected to the heteroatom of the genin (G) via an α-glycosidic bond or a β-glycosidic bond. Pharmacokinetic experiments prove that the lactuloside compound according to the present disclosure can pass through the gastrointestinal tract of a mammal without being absorbed significantly by the gastrointestinal tract and hydrolyzed significantly by endogenous enzymes of a mammal host. Therefore, the lactuloside compound can arrive at the colon site of the mammal, and release an active drug in the colon under the action of colon flora. The lactuloside compound has a function of colon-localized drug release, and can be used for preventing or treating an intestinal disease. ##STR00001##
Lactuloside compounds and preparation and use thereof
The present disclosure relates to the field of pharmaceutical chemistry, and particularly to a compound represented by Formula (I), a preparation method and medical use thereof. In the compound represented by Formula (I), a lactulosyl group is connected to a heteroatom of genin (G) via a glycosidic bond, wherein the genin (G) is a group formed by removing one hydrogen atom from a heteroatom of an active pharmaceutical molecule, and “” indicates that the lactulosyl group is connected to the heteroatom of the genin (G) via an α-glycosidic bond or a β-glycosidic bond. Pharmacokinetic experiments prove that the lactuloside compound according to the present disclosure can pass through the gastrointestinal tract of a mammal without being absorbed significantly by the gastrointestinal tract and hydrolyzed significantly by endogenous enzymes of a mammal host. Therefore, the lactuloside compound can arrive at the colon site of the mammal, and release an active drug in the colon under the action of colon flora. The lactuloside compound has a function of colon-localized drug release, and can be used for preventing or treating an intestinal disease. ##STR00001##
Inhibitors of histone deacetylase
The present invention relates to compounds of formula (I): ##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
Inhibitors of histone deacetylase
The present invention relates to compounds of formula (I): ##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
METHOD OF DECREASING AMYLOID BETA MONOMER LEVELS IN PATIENTS WITH COGNITIVE DECLINE
The present disclosure relates to methods of decreasing amyloid β monomers and methods of treating cognitive decline in a subject, wherein the treatment results in an increase in amyloid β oligomers and a reduction in cognitive decline. The present disclosure relates to treating cognitive decline, wherein target engagement can be measured in the clinic after treating.
METHOD OF DECREASING AMYLOID BETA MONOMER LEVELS IN PATIENTS WITH COGNITIVE DECLINE
The present disclosure relates to methods of decreasing amyloid β monomers and methods of treating cognitive decline in a subject, wherein the treatment results in an increase in amyloid β oligomers and a reduction in cognitive decline. The present disclosure relates to treating cognitive decline, wherein target engagement can be measured in the clinic after treating.
Methods of Treatment of Spontaneous Preterm Birth
Spontaneous preterm birth (sPTB) is premature delivery prior to 37 weeks of pregnancy and is a leading cause of infant mortality worldwide. sPTB is associated with a unique gene expression profile. Identified herein are numerous safe and proven therapeutic compositions used for unrelated indications that have the biological effect of reversing, in part, the gene expression profile of sPTB and which can be used in preventative or interventional treatments to prevent, delay, or ameliorate sPTB. The repurposed drugs include several Class A and Class B therapeutics that are regarded as safe or low risk in pregnant subjects.
Methods of Treatment of Spontaneous Preterm Birth
Spontaneous preterm birth (sPTB) is premature delivery prior to 37 weeks of pregnancy and is a leading cause of infant mortality worldwide. sPTB is associated with a unique gene expression profile. Identified herein are numerous safe and proven therapeutic compositions used for unrelated indications that have the biological effect of reversing, in part, the gene expression profile of sPTB and which can be used in preventative or interventional treatments to prevent, delay, or ameliorate sPTB. The repurposed drugs include several Class A and Class B therapeutics that are regarded as safe or low risk in pregnant subjects.
COMPOSITIONS FOR THE TREATMENT OF HYPERTENSION
Provided herein are pharmaceutical compositions that are useful for the treatment of hypertension comprising an angiotensin II receptor blocker, a diuretic, and a calcium channel blocker.
COMPOSITIONS FOR THE TREATMENT OF HYPERTENSION
Provided herein are pharmaceutical compositions that are useful for the treatment of hypertension comprising an angiotensin II receptor blocker, a diuretic, and a calcium channel blocker.