ADMINISTRATION REGIME FOR NITROCATECHOLS

• US 20130324578A1
• Filed: 08/09/2013
• Published: 12/05/2013
• Est. Priority Date: 02/11/2011
• Status: Active Grant

• Current Assignee: BIAL Portela & Ca, SA
• Original Assignee: BIAL Portela & Ca, SA
• Inventors: SOARES DA SILVA, Patricio Manuel Vieira Araujo, NUNES, Teresa Lucia Silva Pereira, WRIGHT, Lyndon Christopher, PALMA, Pedro Nuno Leal, LEARMONTH, David Alexander
• Granted Patent: US 10,065,944 B2
• Time in Patent Office: Days
• US Class Current: 514/340
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/165 having aromatic rings, e.g. colchicine, atenolol, progabide
• CPC Class Codes: A61K 31/198 Alpha-amino acids, e.g. alanine or edetic acid [EDTA] betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00
• CPC Class Codes: A61K 31/4439 containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole nicotine A61K31/465
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 7/10 Antioedematous agents; Diuretics
• CPC Class Codes: A61P 9/12 Antihypertensives
• CPC Class Codes: C07D 413/12 linked by a chain containing hetero atoms as chain links

Abstract

A compound of formula (I)

where R₁, R₂, X, Y, n, m, R₃, R₄, R₅, R₆ and R₇ are as defined herein, for use in the prophylaxis or treatment of a central and peripheral nervous system disorder, wherein the compound of formula (I) is administered prior to sleep, before bedtime or at bedtime.

Claims

1-40. -40. (canceled)

41. A method of prophylaxis or treatment of a central and peripheral nervous system disorder, comprising administering to a patient suffering from said disorder, prior to sleep, before bedtime or at bedtime, a therapeutically effective amount of a compound of formula (I)

42. A method of prophylaxis or treatment of a central and peripheral nervous system disorder, comprising administering to a patient suffering from said disorder, without food and/or between intakes of food, a therapeutically effective amount of a compound of formula (I) as defined in claim 41.

43. The method according to claim 41, wherein the compound of formula (I) is 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol or its pharmacologically acceptable salts, esters, carbamates and phosphates.

44. The method according to claim 41, wherein the compound of formula (I) is administered in a single daily dose.

45. The method according to claim 42, wherein the compound of formula (I) is administered from 0.25 to 12 hours after an intake of food.

46. The method according to claim 42, wherein the compound of formula (I) is administered from 0.25 to 2 hours before an intake of food.

47. The method according to claim 42, wherein the compound of formula (I) is administered less than one hour prior to sleep, less than one hour before bedtime or at bedtime.

48. The method according to claim 41, wherein the compound of formula (I) is administered in combination with a catecholamine drug.

49. The method according to claim 48, wherein the catecholamine drug is levodopa.

50. The method according to claim 48, wherein the compound of formula (I) is administered sequentially with the catecholamine drug.

51. The method according to claim 48, wherein the compound of formula (I) is administered before or after the catecholamine drug.

52. The method according to claim 51, wherein the compound of formula (I) is administered from 30 to 150 minutes before or after the catecholamine drug.

53. The method according to claim 48, wherein the compound of formula (I) is administered once daily at least one hour before or after the last daily dose of the catecholamine drug.

55. The method according to claim 48, wherein the catecholamine drug is administered sequentially or concomitantly with an AADCi.

56. The method according to claim 55, wherein the AADCi is cardidopa or benserazide.

57. The method according to claim 41, wherein the central and peripheral nervous system disorder is a mood disorder, gastrointestinal disturbance, edema formation state, hypertension or a movement disorder.

58. The method according to claim 57, wherein the movement disorder is Parkinson'"'"'s disease.

59. A method for the prophlaxis or treatment of a central and peripheral nervous system disorder, particularly a movement disorder such as Parkinson'"'"'s disease, comprising administering to a patient suffering from said disorder between intakes of food, a therapeutically effective amount of a compound of formula (I) as defined in claim 41, or its pharmacologically acceptable salts, esters, carbamates and phosphates, in combination with a catecholamine drug, wherein the compound of formula (I) is administered once daily at least one hour after the last daily dose of the catecholamine drug and prior to sleep, before bedtime or at bedtime.

60. The method according to claim 59, wherein the compound of formula (I) is administered without food and/or at least one hour after the most recent intake of food and at least one hour before the next intake of food by the patient.

61. The method according to claim 42, wherein the compound of formula (I) is 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol or its pharmacologically acceptable salts, esters, carbamates and phosphates.

62. The method according to claim 42, wherein the compound of formula (I) is administered in a single daily dose.

63. The method according to claim 42, wherein the compound of formula (I) is administered in combination with a catecholamine drug.

64. The method according to claim 63, wherein the catecholamine drug is levodopa.

65. The method according to claim 63, wherein the compound of formula (I) is administered sequentially with the catecholamine drug.

66. The method according to claim 63, wherein the compound of formula (I) is administered before or after the catecholamine drug.

67. The method according to claim 66, wherein the compound of formula (I) is administered from 30 to 150 minutes before or after the catecholamine drug.

68. The method according to claim 63, wherein the compound of formula (I) is administered once daily at least one hour before or after the last daily dose of the catecholamine drug.

69. The method according to claim 63, wherein the catecholamine drug is administered sequentially or concomitantly with an AADCi.

70. The method according to claim 69, wherein the AADCi is cardidopa or benserazide.

71. The method according to claim 41, wherein the central and peripheral nervous system disorder is a mood disorder, gastrointestinal disturbance, edema formation state, hypertension or a movement disorder.

72. The method according to claim 71, wherein the movement disorder is Parkinson'"'"'s disease.

73. The method according to claim 59, wherein the catecholamine drug is levodopa.

74. The method according to claim 59, wherein the compound of formula (I) is 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol.

75. The method according to claim 45, wherein the compound of formula (I) is administered from 0.5 to 6 hours after an intake of food.

76. The method according to claim 45, wherein the compound of formula (I) is administered from 0.75 to 4 hours after an intake of food.

77. The method according to claim 46, wherein the compound of formula (I) is administered from 0.5 to 1.5 hours before an intake of food.

54. (canceled)