A61K31/33

Methods of using L-butylphthalide for the prevention and treatment of cerebral ischemia disease

The inventive subject matter relates to the use of L-butylphthalide in the manufacturing of medicaments for the prevention and treatment of cerebral ischemia-induced disease. Cerebral ischemia of the animals or human induces cerebral infarction, neurological deficit, memory disorder, cerebral edema, cerebral apoplexy, metabolic disorder of energy, changes of cerebral blood flow, and the like. The in vivo experiments show that L-butylphthalide can effectively reduce the above-mentioned adverse symptoms induced by cerebral ischemia.

AMINOSULFONYL COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF

Disclosed are aminosulfonyl-based compounds represented by the general formula I or tautomers, enantiomers, racemates or pharmaceutically acceptable salts thereof, a method for preparing the same, pharmaceutical compositions and uses thereof. The compounds can be used to treat epilepsy, convulsions, obesity and the like.

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Method of administration of gamma hydroxybutyrate with monocarboxylate transporters
11253494 · 2022-02-22 · ·

One embodiment of the present invention is to improve the safety and efficacy of the administration of GHB or a salt thereof to a patient. It has been discovered that the concomitant administration of an MCT inhibitor, such as diclofenac, valproate, or ibuprofen, will affect GHB administration. For example, it has been discovered that diclofenac lowers the effect of GHB in the body, thereby potentially causing an unsafe condition. Furthermore, it has been discovered that valproate increases the effect of GHB on the body, thereby potentially causing an unsafe condition.

Method of administration of gamma hydroxybutyrate with monocarboxylate transporters
11253494 · 2022-02-22 · ·

One embodiment of the present invention is to improve the safety and efficacy of the administration of GHB or a salt thereof to a patient. It has been discovered that the concomitant administration of an MCT inhibitor, such as diclofenac, valproate, or ibuprofen, will affect GHB administration. For example, it has been discovered that diclofenac lowers the effect of GHB in the body, thereby potentially causing an unsafe condition. Furthermore, it has been discovered that valproate increases the effect of GHB on the body, thereby potentially causing an unsafe condition.

Anti-fugetactic agents for the treatment of ovarian cancer

This invention provides methods and compositions for modulating movement of eukaryotic cells with migratory capacity. More specifically, the invention provides anti-fugetactic agents and methods for the use thereof in enhancing an immune response.

Anti-fugetactic agents for the treatment of ovarian cancer

This invention provides methods and compositions for modulating movement of eukaryotic cells with migratory capacity. More specifically, the invention provides anti-fugetactic agents and methods for the use thereof in enhancing an immune response.

Conjugates And Conjugating Reagents
20170290925 · 2017-10-12 · ·

The invention relates to a conjugate of a protein or peptide with a therapeutic, diagnostic or labelling agent, said conjugate containing a protein or peptide bonding portion and a polyethylene glycol portion; in which said protein or peptide bonding portion has the general formula:

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in which Pr represents said protein or peptide, each Nu represents a nucleophile present in or attached to the protein or peptide, each of A and B independently represents a C.sub.1-4alkylene or alkenylene chain, and W′ represents an electron withdrawing group or a group obtained by reduction of an electron withdrawing group; and in which said polyethylene glycol portion is or includes a pendant polyethylene glycol chain which has a terminal end group of formula —CH.sub.2CH.sub.2OR in which R represents a hydrogen atom, an alkyl group, or an optionally substituted aryl group. Also claimed are a method for making such a conjugate, and novel reagents useful in that method.

Conjugates And Conjugating Reagents
20170290925 · 2017-10-12 · ·

The invention relates to a conjugate of a protein or peptide with a therapeutic, diagnostic or labelling agent, said conjugate containing a protein or peptide bonding portion and a polyethylene glycol portion; in which said protein or peptide bonding portion has the general formula:

##STR00001##

in which Pr represents said protein or peptide, each Nu represents a nucleophile present in or attached to the protein or peptide, each of A and B independently represents a C.sub.1-4alkylene or alkenylene chain, and W′ represents an electron withdrawing group or a group obtained by reduction of an electron withdrawing group; and in which said polyethylene glycol portion is or includes a pendant polyethylene glycol chain which has a terminal end group of formula —CH.sub.2CH.sub.2OR in which R represents a hydrogen atom, an alkyl group, or an optionally substituted aryl group. Also claimed are a method for making such a conjugate, and novel reagents useful in that method.

URAT1 INHIBITOR

Provided are a compound represented by the following Formula (III), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt or solvate thereof used as a therapeutic agent for gout or hyperuricemia. (In the Formula (III), R.sup.1a, R.sup.2a, R.sup.6a, and R.sup.7a represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, or a cyano group, R.sup.3a and R.sup.8a form a benzene ring or a 5-membered heteroaryl ring containing 1 to 3 heteroatoms, as a ring constituent element, selected from nitrogen atoms, oxygen atoms, and sulfur atoms together with two carbon atoms to which R.sup.3a and R.sup.8a are bonded, R.sup.4a and R.sup.5a form a benzene ring together with two carbon atoms to which R.sup.4a and R.sup.5a are bonded or represent any of the groups represented by R.sup.1a described above, W.sup.a represents CR.sup.10a or N, and where, R.sup.10a represents any of the groups represented by R.sup.1a, X.sup.a represents an oxygen atom or a sulfur atom, Y.sup.a represents an alkylene chain having 1 to 8 carbon atoms, and where, the alkylene chain may be substituted with an alkyl group having 1 to 8 carbon atoms and the alkylene chain may be a linear or branched alkylene chain, the branched alkylene chain may have a 3- to 7-membered ring formed by side chains bonded to carbon atoms which are the same as or different from each other, together with the carbon atoms to which the side chains are bonded and may have a double bond in the middle thereof, and Z.sup.a represents CO.sub.2H.)

##STR00001##

URAT1 INHIBITOR

Provided are a compound represented by the following Formula (III), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt or solvate thereof used as a therapeutic agent for gout or hyperuricemia. (In the Formula (III), R.sup.1a, R.sup.2a, R.sup.6a, and R.sup.7a represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, or a cyano group, R.sup.3a and R.sup.8a form a benzene ring or a 5-membered heteroaryl ring containing 1 to 3 heteroatoms, as a ring constituent element, selected from nitrogen atoms, oxygen atoms, and sulfur atoms together with two carbon atoms to which R.sup.3a and R.sup.8a are bonded, R.sup.4a and R.sup.5a form a benzene ring together with two carbon atoms to which R.sup.4a and R.sup.5a are bonded or represent any of the groups represented by R.sup.1a described above, W.sup.a represents CR.sup.10a or N, and where, R.sup.10a represents any of the groups represented by R.sup.1a, X.sup.a represents an oxygen atom or a sulfur atom, Y.sup.a represents an alkylene chain having 1 to 8 carbon atoms, and where, the alkylene chain may be substituted with an alkyl group having 1 to 8 carbon atoms and the alkylene chain may be a linear or branched alkylene chain, the branched alkylene chain may have a 3- to 7-membered ring formed by side chains bonded to carbon atoms which are the same as or different from each other, together with the carbon atoms to which the side chains are bonded and may have a double bond in the middle thereof, and Z.sup.a represents CO.sub.2H.)

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