Treatment of cerebrovascular disease
AssigneeMedicure International Inc.
InventorsWasimul Haque, Rajat Sethi
Life of this patent
Estimating the term…
Abstract
A method of treating a cerebrovascular disease, particularly stroke, is described. A method of treating a cerebrovascular disease includes administering pyridoxal-5′-phosphate, pyridoxal, pyridoxine, pyridoxamine, 3-acylated analogues of pyridoxal, 3-acylated analogues of pyridoxal-4,5-aminal, pyridoxine phosphonate analogues, or pharmaceutical compositions thereof.
Claims67
A method of treating cerebral ischemia, cerebral hemorrhage, ischemic stroke, or hemorrhagic stroke in a mammal comprising administering a therapeutically effective amount of at least one of pyridoxal-5′-phosphate, pyridoxal, pyridoxine, or pyridoxamine.
A method of treating cerebral ischemia, cerebral hemorrhage, ischemic stroke, or hemorrhagic stroke in a mammal comprising administering a therapeutically effective amount of at least one compound of the formula
- 55
- wherein
- R1 is alkyl or alkenyl, in which alkyl or alkenyl can be interrupted by nitrogen, oxygen, or sulfur, and can be substituted at the terminal carbon by hydroxy, alkoxy, alkanoyloxy, alkanoyloxyaryl, alkoxyalkanoyl, alkoxycarbonyl, or dialkylcarbamoyloxy;
- alkoxy;
- dialkylamino;
- alkanoyloxy;
- alkanoyloxyaryl;
- alkoxyalkanoyl;
- alkoxycarbonyl;
- dialkylcarbamoyloxy;
- aryl, aryloxy, arylthio, or aralkyl, in which aryl can be substituted by alkyl, alkoxy, amino, hydroxy, halo, nitro, or alkanoyloxy;
- or
- a pharmaceutically acceptable salt thereof.
A method of treating cerebral ischemia, cerebral hemorrhage, ischemic stroke, or hemorrhagic stroke in a mammal comprising administering a therapeutically effective amount of at least one compound of the formula
- 56
- wherein
- R1 is alkyl or alkenyl, in which alkyl or alkenyl can be interrupted by nitrogen, oxygen, or sulfur, and can be substituted at the terminal carbon by hydroxy, alkoxy, alkanoyloxy, alkanoyloxyaryl, alkoxyalkanoyl, alkoxycarbonyl, or dialkylcarbamoyloxy;
- alkoxy;
- dialkylamino;
- alkanoyloxy;
- alkanoyloxyaryl;
- alkoxyalkanoyl;
- alkoxycarbonyl;
- dialkylcarbamoyloxy;
- aryl, aryloxy, arylthio, or aralkyl, in which aryl can be substituted by alkyl, alkoxy, amino, hydroxy, halo, nitro, or alkanoyloxy;
- and
- R2 is a secondary amino group;
- or
- a pharmaceutically acceptable salt thereof.
A method of treating cerebral ischemia, cerebral hemorrhage, ischemic stroke, or hemorrhagic stroke in a mammal comprising administering a therapeutically effective amount of at least one compound of the formula
- 58
- wherein
- R1 is hydrogen or alkyl;
- R2 is —CHO, —CH2OH, —CH3, —CO2R6 in which R6 is hydrogen, alkyl, or aryl;
- or
- R2 is —CH2—O-alkyl- in which alkyl is covalently bonded to the oxygen at the 3-position instead of R1;
- R3 is hydrogen and R4 is hydroxy, halo, alkoxy, alkanoyloxy, alkylamino or arylamino;
- or
- R3 and R4 are halo;
- and
- R5 is hydrogen, alkyl, aryl, aralkyl, or —CO2R7 in which R7 is hydrogen, alkyl, aryl, or aralkyl;
- or a pharmaceutically acceptable salt thereof.
38 The method of claim 32, wherein said R5 is t-butyl or benzyl.
A method of treating cerebral ischemia, cerebral hemorrhage, ischemic stroke, or hemorrhagic stroke in a mammal comprising administering a therapeutically effective amount of at least one compound of the formula
- 73
- wherein
- R1 is hydrogen or alkyl;
- R2 is CHO, —CH2OH, —CH3 or —CO2R5 in which R5 is hydrogen, alkyl, or aryl;
- or
- R2 is —CH2—O-alkyl- (in which alkyl is covalently bonded to the oxygen at the 3-position instead of R1);
- R3 is hydrogen, alkyl, aryl, or aralkyl;
- R4 is hydrogen, alkyl, aryl, aralkyl, or —CO2R6 in which R6 is hydrogen, alkyl, aryl, or aralkyl;
- and
- n is 1 to 6;
- or a pharmaceutically acceptable salt thereof.
A method of treating cerebral ischemia, cerebral hemorrhage, ischemic stroke, or hemorrhagic stroke in a mammal comprising administering a therapeutically effective amount of at least one compound of the formula
- 75
- in which
- R1 is hydrogen or alkyl;
- R2 is —CHO, —CH2OH, —CH3 or —CO2R8 in which R8 is hydrogen, alkyl, or aryl;
- or
- R2 is —CH2—O-alkyl- in which alkyl is covalently bonded to the oxygen at the 3-position instead of R1;
- R3 is hydrogen and R4 is hydroxy, halo, alkoxy or alkanoyloxy;
- or
- R3 and R4 can be taken together to form ═O;
- R5 and R6 are hydrogen;
- or
- R5 and R6 are halo;
- and
- R7 is hydrogen, alkyl, aryl, aralkyl, or —CO2R8 in which R8 is hydrogen, alkyl, aryl, or aralkyl;
- or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of pyridoxal-5′-phosphate, pyridoxal, pyridoxine, or pyridoxamine.
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one compound of the formula
- 77
- wherein
- R1 is alkyl or alkenyl, in which alkyl or alkenyl can be interrupted by nitrogen, oxygen, or sulfur, and can be substituted at the terminal carbon by hydroxy, alkoxy, alkanoyloxy, alkanoyloxyaryl, alkoxyalkanoyl, alkoxycarbonyl, or dialkylcarbamoyloxy;
- alkoxy;
- dialkylamino;
- alkanoyloxy;
- alkanoyloxyaryl;
- alkoxyalkanoyl;
- alkoxycarbonyl;
- dialkylcarbamoyloxy;
- aryl, aryloxy, arylthio, or aralkyl, in which aryl can be substituted by alkyl, alkoxy, amino, hydroxy, halo, nitro, or alkanoyloxy;
- or
- a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one compound of the formula
- 78
- wherein
- R1 is alkyl or alkenyl, in which alkyl or alkenyl can be interrupted by nitrogen, oxygen, or sulfur, and can be substituted at the terminal carbon by hydroxy, alkoxy, alkanoyloxy, alkanoyloxyaryl, alkoxyalkanoyl, alkoxycarbonyl, or dialkylcarbamoyloxy;
- alkoxy;
- dialkylamino;
- alkanoyloxy;
- alkanoyloxyaryl;
- alkoxyalkanoyl;
- alkoxycarbonyl;
- dialkylcarbamoyloxy;
- aryl, aryloxy, arylthio, or aralkyl, in which aryl can be substituted by alkyl, alkoxy, amino, hydroxy, halo, nitro, or alkanoyloxy;
- and
- R2 is a secondary amino group;
- or
- a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one compound of the formula
- 79
- wherein
- R1 is hydrogen or alkyl;
- R2 is —CHO, —CH2OH, —CH3, —CO2R6 in which R6 is hydrogen, alkyl, or aryl;
- or
- R2 is —CH2—O-alkyl- in which alkyl is covalently bonded to the oxygen at the 3-position instead of R1;
- R3 is hydrogen and R4 is hydroxy, halo, alkoxy, alkanoyloxy, alkylamino or arylamino;
- or
- R3 and R4 are halo;
- and
- R5 is hydrogen, alkyl, aryl, aralkyl, or —CO2R7 in which R7 is hydrogen, alkyl, aryl, or aralkyl;
- or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one compound of the formula
- 80
- wherein
- R1 is hydrogen or alkyl;
- R2 is —CHO, —CH2OH, —CH3 or —CO2R5 in which R5 is hydrogen, alkyl, or aryl;
- or
- R2 is —CH2—O-alkyl- (in which alkyl is covalently bonded to the oxygen at the 3-position instead of R1);
- R3 is hydrogen, alkyl, aryl, or aralkyl;
- R4 is hydrogen, alkyl, aryl, aralkyl, or —CO2R6 in which R6 is hydrogen, alkyl, aryl, or aralkyl;
- and
- n is 1 to 6;
- or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one compound of the formula
- 81
- in which
- R1 is hydrogen or alkyl;
- R2 is —CHO, —CH2OH, —CH3 or —CO2R8 in which R8 is hydrogen, alkyl, or aryl;
- or
- R2 is —CH2—O-alkyl- in which alkyl is covalently bonded to the oxygen at the 3-position instead of R1;
- R3 is hydrogen and R4 is hydroxy, halo, alkoxy or alkanoyloxy;
- or
- R3 and R4 can be taken together to form ═O;
- R5 and R6 are hydrogen;
- or
- R5 and R6 are halo;
- and
- R7 is hydrogen, alkyl, aryl, aralkyl, or —CO2R8 in which R8 is hydrogen, alkyl, aryl, or aralkyl;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.