Patent classifications
C07F9/65742
Phytosphingosine-1-phosphate derivative, preparation method therefor, and composition for preventing and treating hair loss or for growing hair comprising same
The present invention provides: O-cyclic phytospingosine-1-phosphate (O-C-P1P), N-cyclic phytospingosine-1-phosphate (N-C-P1P), a pharmaceutically acceptable salt thereof, or a solvate thereof; a preparation method therefor; a cosmetic composition comprising the same for preventing hair loss or for growing hair; and a pharmaceutical composition for preventing and treating hair loss or for growing hair.
METFORMIN DERIVATIVES
The present invention relates to novel biguanide derivatives including their pharmaceutically acceptable salts. The invention also relates processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions containing and the uses of such compounds in treating disorders such as diabetes.
Uridine diphosphate derivatives, prodrugs, compositions and uses thereof
This disclosure relates to the use of uridine diphosphate (UDP) derivatives, salts and/or prodrugs thereof for the treatment of inflammatory conditions (e.g., psoriasis) and glaucoma, to prodrugs of UDP derivatives, compositions comprising therapeutically effective amounts of those prodrugs of the UDP derivatives and methods of using those prodrugs for treating various disorders including, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma, and inflammatory conditions, e.g., psoriasis and rheumatoid arthritis.
Organophosphorus compounds for flame retardant polyurethane foams
An organophosphorus compound useful in a phosphorus containing flame retardant and a flame retardant polyurethane foam, where the organophosphorus compound is shown in Formula (I) where Y is selected from the group consisting of an —OH group, an —NH.sub.2 group, an —NHR.sup.3 group, and an —SH group, where R.sup.3 is a monovalent hydrocarbyl group having 1 to 10 carbon atoms; R is a divalent hydrocarbyl group; X is a heteroatom group; and R.sup.1 and R.sup.2 are each independently a substituted or unsubstituted hydrocarbyl group, wherein R.sup.1 and R.sup.2 can be optionally joined to form a ring. ##STR00001##
CRYSTAL OF CYCLIC PHOSPHONIC ACID SODIUM SALT AND METHOD FOR MANUFACTURING SAME
An object of the present invention is to provide a crystal of a cyclic phosphonic acid sodium salt (2ccPA) with high purity and excellent storage stability and a method for producing the crystal. The present invention provides a crystal of a cyclic phosphonic acid sodium salt (2ccPA) represented by formula (1):
##STR00001##
METHOD FOR THE SYNTHESIS OF HETEROCYCLIC HYDROGEN PHOSPHINE OXIDE
A method for the synthesis of a heterocyclic hydrogen phosphine oxide, having the general formula:
##STR00001##
wherein:
R is a aliphatic or aromatic divalent group optionally including one or more heteroatoms and optionally having one or more substituents and
X and Y are independently selected from —O—, —C(O)O— and —NR′—
wherein R′ is a monovalent group optionally having one or more heteroatoms including the steps of:
a) forming a reaction mixture by mixing a compound having the general formula HX—R—YH and tetraphosphorus hexaoxide; and
b) recovering the resulting compound comprising the heterocyclic hydrogen phosphine oxide.
Tricyclic sulfones as RORγ modulators
There are described RORγ modulators of the formula (I), ##STR00001##
and formula (II) ##STR00002##
or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
SELECTIVE DETECTION OF BED BUGS
A device, system, and method of controlling pests are disclosed. A pest control device includes a sensor having a sensor cell and a controller. A surface of the sensor cell is coated with an agent that reacts with a targeted biochemical analyte secreted by pests. The controller is coupled to the sensor and is configured to receive sensor data from the sensor cell indicative of a rate of change in sensor mass detected on the surface of the sensor cell, determine whether the rate of change in the sensor mass based on the received sensor data exceeds a predefined threshold rate, and transmit a pest detection alert notification to a server in response to a determination that the rate of change exceeds the predetermined threshold rate.
METABOLICALLY STABLE PRODRUGS
Provided are prodrugs of various therapeutic agents that provide enhanced bioavailability of the therapeutic agent, and methods of treatment conditions in a subject by administration of the one or prodrugs. As provided herein a prodrug includes a therapeutic agent covalently attached to a cap, the cap having a structure according to formula (I) where: R.sup.1 is a branched or linear substituted or unsubstituted C2-C6 alkyl, alkenyl, or alkynl; X is —S(0).sub.2-; R.sup.2 is a branched or linear substituted or unsubstituted C4-C20 alkyl, alkenyl, or alkynyl; and R.sup.3 is —H, C3-C5 cycloalkyl, C3-C5 cycloheteroalkyl, —C(CH.sub.3).sub.3, —CF.sub.3, —C(CF.sub.3).sub.3, or a substituted or unsubstituted phenyl.
##STR00001##
RADIO-AND CHEMO-PROTECTIVE COMPOUNDS
The present disclosure relates to prodrugs, double prodrugs, derivatives and analogues of 3-(methylamino)-2-((methylamino)methyl)propane-1-thiol. Their use as radio- and chemo-protectors is also described.