Patent classifications
C07D239/38
Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith
Provided herein are Diaminopyrimidine Compounds having the following structures: ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
KETONE INHIBITORS OF LYSINE GINGIPAIN
The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
KETONE INHIBITORS OF LYSINE GINGIPAIN
The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
BUMETANIDE DERIVATIVES FOR THE THERAPY OF HYPERHIDROSIS
The present invention relates to bumetanide derivatives of formula (I) as well as pharmaceutical compositions comprising these compounds for use in the treatment or prevention of diseases/disorders involving Na.sup.+K.sup.+2Cl.sup.-cotransporters (NKCCs), and particularly for use in the treatment or prevention of hyperhidrosis.
##STR00001##
BUMETANIDE DERIVATIVES FOR THE THERAPY OF HYPERHIDROSIS
The present invention relates to bumetanide derivatives of formula (I) as well as pharmaceutical compositions comprising these compounds for use in the treatment or prevention of diseases/disorders involving Na.sup.+K.sup.+2Cl.sup.-cotransporters (NKCCs), and particularly for use in the treatment or prevention of hyperhidrosis.
##STR00001##
PROPANAMINE DERIVATIVES FOR TREATING PAIN AND PAIN RELATED CONDITIONS
The present invention relates to new compounds of formula (I) that show great affinity and activity towards the subunit 2 of voltage-gated calcium channels (VGCC), especially the 2-1 subunit of voltage-gated calcium channels or dual activity towards the subunit 2 of voltage-gated calcium channels (VGCC), especially the 2-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.
##STR00001##
NONAQUEOUS ELECTROLYTE, NONAQUEOUS ELECTROLYTE ENERGY STORAGE DEVICE, AND METHOD FOR PRODUCING NONAQUEOUS ELECTROLYTE ENERGY STORAGE DEVICE
Provided are a nonaqueous electrolyte capable of providing a nonaqueous electrolyte energy storage device with reduced direct current resistance and an increased capacity retention ratio after charge-discharge cycles, a nonaqueous electrolyte energy storage device including such a nonaqueous electrolyte, and a method for producing such a nonaqueous electrolyte energy storage device. One mode of the present invention is a nonaqueous electrolyte for an energy storage device, containing an additive represented by the following Formula (1) or Formula (2). In Formula (1), R.sup.1 to R.sup.4 are each independently a hydrogen atom or a group represented by NR, ORa, SRa, etc., with the proviso that at least one of R.sup.1 to R.sup.4 is a group represented by ORa, SRa, COORa, CORa, SO2Ra, or SO3Ra. In Formula (2), R.sup.5 to R.sup.7 are each independently a hydrogen atom or a group represented by NRb.sup.2, OR.sup.b, or SR.sup.b, with the proviso that at least one of R.sup.5 to R.sup.7 is a group represented by SRb.
##STR00001##
NONAQUEOUS ELECTROLYTE, NONAQUEOUS ELECTROLYTE ENERGY STORAGE DEVICE, AND METHOD FOR PRODUCING NONAQUEOUS ELECTROLYTE ENERGY STORAGE DEVICE
Provided are a nonaqueous electrolyte capable of providing a nonaqueous electrolyte energy storage device with reduced direct current resistance and an increased capacity retention ratio after charge-discharge cycles, a nonaqueous electrolyte energy storage device including such a nonaqueous electrolyte, and a method for producing such a nonaqueous electrolyte energy storage device. One mode of the present invention is a nonaqueous electrolyte for an energy storage device, containing an additive represented by the following Formula (1) or Formula (2). In Formula (1), R.sup.1 to R.sup.4 are each independently a hydrogen atom or a group represented by NR, ORa, SRa, etc., with the proviso that at least one of R.sup.1 to R.sup.4 is a group represented by ORa, SRa, COORa, CORa, SO2Ra, or SO3Ra. In Formula (2), R.sup.5 to R.sup.7 are each independently a hydrogen atom or a group represented by NRb.sup.2, OR.sup.b, or SR.sup.b, with the proviso that at least one of R.sup.5 to R.sup.7 is a group represented by SRb.
##STR00001##
BENZAMIDE DERIVATIVE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION FOR TREATING OR PREVENTING INFLAMMATORY DISEASE CONTAINING SAME AS ACTIVE INGREDIENT
The present invention relates to a benzamide derivative compound, a method for preparing the same, and a pharmaceutical composition for treating or preventing an inflammatory disease containing the same as an active ingredient. The benzamide derivative compound according to the present invention inhibits the expression of PDE4 and regulates the expression of an inflammatory disease-related substance such as IL-4 (interleukin-4), IL-5 (interleukin-4), IFN- (interferon-), IL-17 (interluekin-17), IgE (immunoglobulin E), and TNF- (tumor necrosis factor-), and thus may be utilized as a pharmaceutical composition for treating or preventing an inflammatory disease.
PYRIMIDINE DERIVATIVE KINASE INHIBITORS
The present invention relates to a kinase inhibitor, comprising a compound of Formula I or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite or prodrug thereof. The present invention also relates to a pharmaceutical composition comprising the kinase inhibitor, and to uses and methods for using these compounds and compositions to inhibit the activity of wild-type FLT3, mutant FLT3-ITD, PDGFR and/or PDGFR kinase in a cell or a subject, as well as uses and methods of these compounds and compositions to preventing or treating kinase-associated conditions in a subject.
##STR00001##