Patent classifications
C07D225/02
Ester substituted ion channel blockers and methods for use
The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: ##STR00001## The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.
Charged Ion Channel Blockers and Methods for Use
The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof:
##STR00001##
The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.
Charged Ion Channel Blockers and Methods for Use
The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof:
##STR00001##
The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.
PHOTOIRRADIATION DEVICE, PHOTOREACTION METHOD USING THE SAME, AND METHOD FOR PRODUCING LACTAM
Provided are a photoirradiation device equipped with: a first optically transparent container for covering a light-emitting body provided with light-emitting diodes; a liquid phase section provided on the outside thereof and formed from a liquid having a refractive index closer to that of the first optically transparent container than that of a gas forming a gas phase section inside the first optically transparent container; and a second optically transparent container for covering the liquid phase section, a photoreaction method using the photoirradiation device, and a method for producing lactam by using the photoreaction method. The reflection of light between a target liquid and a light-emitting diode light source is suppressed, and a desired photoirradiation can be achieved with a high optical transparency.
CHIMERIC COMPOUNDS TARGETING PROTEINS, COMPOSITIONS, METHODS, AND USES THEREOF
The present invention provides chimeric compounds that modulate protein function, to restore protein homeostasis, including cytokine, aiolos, and/or ikaros activity, TNF-alpha activity, CK1-alpha activity and cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions, including in combination with other cytokine and inflammatory mediators, are provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions, such as cytokine-mediated diseases, disorders, and conditions, including inflammation, fibromyalgia, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, inflammatory bowel diseases, Crohn's disease, ulcerative colitis, uveitis, inflammatory lung diseases, chronic obstructive pulmonary disease, Alzheimer's disease, organ transplant rejection, and cancer, are provided.
CHIMERIC COMPOUNDS TARGETING PROTEINS, COMPOSITIONS, METHODS, AND USES THEREOF
The present invention provides chimeric compounds that modulate protein function, to restore protein homeostasis, including cytokine, aiolos, and/or ikaros activity, TNF-alpha activity, CK1-alpha activity and cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions, including in combination with other cytokine and inflammatory mediators, are provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions, such as cytokine-mediated diseases, disorders, and conditions, including inflammation, fibromyalgia, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, inflammatory bowel diseases, Crohn's disease, ulcerative colitis, uveitis, inflammatory lung diseases, chronic obstructive pulmonary disease, Alzheimer's disease, organ transplant rejection, and cancer, are provided.
PROCESS FOR THE CYCLOADDITION OF A (HETERO)ARYL 1,3-DIPOLE COMPOUND WITH A (HETERO)CYCLOALKYNE
A process is provided, comprising reacting a (hetero)aryl 1,3-dipole compound with a (hetero)cycloalkyne, wherein the (hetero)aryl 1,3-dipole compound comprises a 1,3-dipole functional group bonded to a (hetero)aryl group, and wherein the (hetero)aryl 1,3-dipole compound is a (hetero)aryl azide or a (hetero)aryl diazo compound; wherein: (i) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound comprises a substituent (ii) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound is an electron-poor (hetero)aryl group
and wherein the (hetero)cycloalkyne is a (hetero)cyclooctyne or a (hetero)cyclononyne according to Formula (1). The invention also relates to the products obtainable by the process according to the invention.
PROCESS FOR THE CYCLOADDITION OF A (HETERO)ARYL 1,3-DIPOLE COMPOUND WITH A (HETERO)CYCLOALKYNE
A process is provided, comprising reacting a (hetero)aryl 1,3-dipole compound with a (hetero)cycloalkyne, wherein the (hetero)aryl 1,3-dipole compound comprises a 1,3-dipole functional group bonded to a (hetero)aryl group, and wherein the (hetero)aryl 1,3-dipole compound is a (hetero)aryl azide or a (hetero)aryl diazo compound; wherein: (i) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound comprises a substituent (ii) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound is an electron-poor (hetero)aryl group
and wherein the (hetero)cycloalkyne is a (hetero)cyclooctyne or a (hetero)cyclononyne according to Formula (1). The invention also relates to the products obtainable by the process according to the invention.
THREE-PHASE AC/DC CONVERTER, PHOTOCHEMICAL REACTION DEVICE AND METHOD USING SAME, AND METHOD FOR PRODUCING LACTAM
Provided are a three-phase AC/DC converter disposed between a three-phase AC power supply and a light emitting diode group, the converter including a three-phase full bridge circuit in which pairs of switching elements are connected in parallel between DC buses for the three phases of the three-phase AC power supply; reactors connecting connection portions between the switching elements and corresponding phases of the three-phase AC power supply; a smoothing capacitor on the output side of the three-phase full bridge circuit; a DC voltage detection means; a power supply voltage phase detection means; and a pulse width modulation means for outputting pulse width modulation signals of the switching elements, wherein the pulse width modulation means outputs the pulse width modulation signals based on a power supply voltage phase and an output voltage between the DC buses.
DERIVATIVES OF 10-METHYLENE LIPIDS, PROCESS FOR PREPARING SUCH DERIVATIVES AND USE THEREOF
The present invention relates to derivatives of 10-methylene lipids, their preparation and their use.