Patent classifications
A01N43/00
Pharmaceutical composition
To provide pharmaceutical preparation exhibiting satisfactory dissolution property in a wide pH range. The pharmaceutical composition is characterized by containing (A) N.sup.1-(5-chloropyridin-2-yl)-N.sup.2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide, represented by the following formula (1), a pharmacologically acceptable salt thereof, or a hydrate of any of these, and (B) one or more species selected from the group consisting of a sugar alcohol and a water-swelling additive. ##STR00001##
Heterobicyclo-substituted [1,2,4]triazolo[1,5-C]quinazolin-5-amine compounds with A2A antagonist properties
Disclosed are compounds of Formula G1 (structurally represented): where RG3 Rd1 to Rd4, n, m, p, W, X, Y, and Z are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions. ##STR00001##
Methods of treating Dravet syndrome
Methods of treating a developmental disorder such as Dravet syndrome by administering a pharmaceutical composition of gaboxadol or a pharmaceutically acceptable salt thereof are provided.
Sorbic and benzoic acid and derivatives thereof enhance the activity of a neuropharmaceutical
Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.
2,3-dihydroquinazolin-4(1H)-one derivatives for use in the treatment of viral infections
Use of 2,3-dihydroquinazolin-4(1H)-one cyclic derivatives of formula (I) for the treatment of infection with viruses entering cells by endocytosis, especially filovirus such as Ebolavirus. ##STR00001##
USE OF PHENYLPYRAZOLIN-3-CARBOXYLATES FOR IMPROVING PLANT YIELD
Compounds (A) can be used for increasing the yield of useful plants or crop plants with respect to their harvested plant organs, wherein the Compound (A) is selected from compounds of the formula (I) or salts thereof,
##STR00001## in which (R.sup.1).sub.n is n radicals R.sup.1 where the R.sup.1 are identical or different and are each halogen or (C.sub.1-C.sub.4)-haloalkyl, n is an integer from 1 to 3, R.sup.2 is hydrogen, (C.sub.1-C.sub.6)-alkyl, (C.sub.1-C.sub.4)-alkoxy-(C.sub.1-C.sub.4)-alkyl, (C.sub.3-C.sub.6)-cycloalkyl, tri-(C.sub.1-C.sub.4)-alkyl-silyl or tri-(C.sub.1-C.sub.4)-alkyl-silylmethyl, R.sup.3 is hydrogen, (C.sub.1-C.sub.6)-alkyl, (C.sub.1-C.sub.6)-haloalkyl, (C.sub.2-C.sub.6)-alkenyl, (C.sub.2-C.sub.6)-alkynyl or (C.sub.3-C.sub.6)-cycloalkyl, and R.sup.4 is hydrogen or (C.sub.1-C.sub.12)-alkyl, preferably mefepyr-diethyl (Compound (A1)]
Fused heterocyclic derivatives as S1P modulators
The present invention relates to a fused heterocyclic derivative of the formula (I) The variables R1-R4, z, A, Q, X and Y are as defined in the claims. The following heterocycles are exemplified sub-structures of formula (I): The compounds of formula (I) are modulators of the S1P receptor (Sphingosine-1-phosphate receptor), More specifically, they are agonists of S1P5. The compounds have therapeutic use in treatment of cognitive disorders, age-relate cognitive decline and dementia.
Substituted benzoazepines as toll-like receptor modulators
Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-versus-host disease.
Parenteral carbamazepine formulation
The present invention is directed to a carbamazepine-cyclodextrin inclusion complex useful for the parenteral administration of carbamazepine. The carbamazepine-cyclodextrin inclusion complex is prepared by the admixture of a modified cyclodextrin and carbamazepine in a physiologically acceptable fluid. Modified cyclodextrins include 2-hydroxypropyl-beta-cyclodextrin and sulfoalkyl cyclodextrins. More particularly, the sulfoalkyl cyclodextrins are those described and disclosed in U.S. Pat. Nos. 5,134,127 and 5,376,645. A physiologically acceptable fluid includes sterile isotonic water, Ringer's lactate, D5W (5% dextrose in water), physiological saline, and similar fluids suitable for parenteral administration.
Uses of hypoxia-inducible factor inhibitors
The present invention relates to treating a hematologic cancer using a Hypoxia-Inducible Factor (HIF inhibitor). The invention also relates to inducing acute myeloid leukemia remission using the HIF inhibitor. The invention further relates to inhibiting a maintenance or survival function of a cancer stem cell (CSC) using the HIF inhibitor.