Methods and fluorinated compositions for treating amyloid-related diseases

• US 20060183800A1
• Filed: 11/14/2005
• Published: 08/17/2006
• Est. Priority Date: 11/12/2004
• Status: Abandoned Application

• Current Assignee: Bellus Health (Interational) Limited
• Original Assignee: Bellus Health (Interational) Limited
• Inventors: Wu, Xinfu, Migneault, David, Kong, Xianqi, Bellini, Francesco, Bouzide, Abderrahim, Valade, Isabelle
• Application Number:
  US11/274,761
• Publication Number:
  US 20060183800A1
• Time in Patent Office: Days
• US Class Current: 514/553
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: C07C 229/08 the nitrogen atom of the amino group being further bound to hydrogen atoms
• CPC Class Codes: C07C 229/20 the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
• CPC Class Codes: C07C 2601/02 with a three-membered ring
• CPC Class Codes: C07C 2601/08 the ring being saturated
• CPC Class Codes: C07C 2601/14 The ring being saturated
• CPC Class Codes: C07C 2601/18 with a ring being at least seven-membered
• CPC Class Codes: C07C 2602/08 the other ring being five-membered, e.g. indane
• CPC Class Codes: C07C 2602/10 the other ring being six-membered, e.g. tetraline
• CPC Class Codes: C07C 2603/74 Adamantanes
• CPC Class Codes: C07C 309/14 containing amino groups bound to the carbon skeleton
• CPC Class Codes: C07C 309/15 the nitrogen atom of at least one of the amino groups being part of any of the groups , X being a hetero atom, Y being any atom
• CPC Class Codes: C07C 309/19 of a saturated carbon skeleton containing rings
• CPC Class Codes: C07C 309/24 of a carbon skeleton containing six-membered aromatic rings
• CPC Class Codes: C07C 313/04 Sulfinic acids; Esters thereof
• CPC Class Codes: C07C 323/25 the carbon skeleton being acyclic and saturated

Abstract

Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease. Also described are methods, compounds, pharmaceutical compositions and kits for detecting, diagnosing, monitoring and treating or preventing amyloid-related disease.

Claims

1. A compound of Formula I:

65. A kit for use in treating amyloid related disease comprising a compound of claim 1, and instructions for use in the method of the instant invention.

66. A method of treating an amyloid-related disease in a subject, comprising administering to a subject in need thereof a compound of claim 1 or depicted in the Tables in an amount effective to treat an amyloid related disease.

67. The method according to claim 66, wherein said amyloid-related disease is Alzheimer'"'"'s disease, cerebral amyloid angiopathy, inclusion body myositis, macular degeneration, MCI, or Down'"'"'s syndrome.

68. The method of claim 66, according to claim 66, wherein amyloid fibril formation or deposition, neurodegeneration, microglial inflammatory response, cellular toxicity, or neuronal cell death is reduced or inhibited upon administration of said compound.

69. The method according to claim 66, wherein said amyloid-related disease is diabetes, AA amyloidosis, AL amyloidosis, or hemodialysis related amyloidosis (β

₂M).

70. The method according to claim 66, wherein said subject is a human.

71. The method of claim 66, wherein said subject has Alzheimer'"'"'s disease, Mild Cognitive Impairment, or cerebral amyloid angiopathy, and stabilization of cognitive function, prevention of a further decrease in cognitive function, or prevention, slowing, or stopping of disease progression occurs in said patient upon administration.

72. A pharmaceutical composition for the treatment or prevention of an amyloid-related disease comprising a compound of claim 1.

73. A pharmaceutical composition comprising a compound of claim 1.

74. A method of treating Alzheimer'"'"'s Disease in a subject, comprising administering to a subject in need thereof a compound of claim 1 in an amount effective to treat Alzheimer'"'"'s Disease.

75. A method of treating Mild Cognitive Impairment in a subject, comprising administering to a subject in need thereof a compound of claim 1 in an amount effective to treat Mild Cognitive Impairment.

76. A method of treating neurotoxicity associated with Aβ

amyloid in a subject, comprising administering to a subject in need thereof a compound of claim 1 in an amount effective to treat neurotoxicity associated with Aβ

amyloid.

2-43. -43. (canceled)

44. The compound of formula (I), wherein said compound is selected from the group consisting of:

45. A compound of formula (II):

46-63. -63. (canceled)

64. The compound of formula (II), wherein said compound is selected from the group consisting of: