IP Library Granted Patent US 7,230,015
Granted Patent B2
US 7,230,015 · App. 11/079,327 · Granted Jun 12, 2007

Method of treating of demyelinating diseases or conditions

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Quick Facts
Patent No.
US 7,230,015
App. No.
11/079,327
Granted
Jun 12, 2007
Kind
B2
Abstract

N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain.

Claims (15)

1. A method of treating Over Active Bladder said method comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I

wherein

m is 0, 1 or 2;

n is 0, 1 or 2;

p is 0 or 1;

each R is independently hydrogen, halogen, trifluoromethyl, C 1 –C 6 alkyl, C 1 –C 6 alkoxy, benzyloxy, hydroxy, nitro or amino;

each R 1 is independently hydrogen, C 1 –C 6 alkyl, C 1 –C 6 alkenyl,

C 1 –C 6 alkanoyl, halogen, cyano, —C(O)C 1 –C 6 alkyl, —C 1 –C 6 alkyleneCN, —C 1 –C 6 alkyleneNR′R″ wherein

R′ and R″ are each independently hydrogen or C 1 –C 6 alkyl,

—C 1 –C 6 alkyleneOC(O)C 1 –C 6 alkyl, or —CH(OH)R 4 wherein R 4 is hydrogen or C 1 –C 6 alkyl;

R 2 is hydrogen, C 1 –C 6 alkyl optionally substituted with halogen, hydroxy or benzyloxy, C 1 –C 6 alkenyl, C 1 –C 6 alkynyl,

—CO 2 C 1 –C 6 alkyl, or —R 5 —NR′ R″ wherein R 5 is C 1 –C 6 alkylene, C 1 –C 6 alkenylene or C 1 –C 6 alkynylene and R′ and R″ are each independently hydrogen, C 1 –C 6 alkyl or alternatively the group —NR′R″ as a whole is 1-pyrrolidinyl; and

R 3 is hydrogen, nitro, amino, halogen, C 1 –C 6 alkoxy, hydroxy or C 1 –C 6 alkyl

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 wherein the compound has the following formula:

Assignments (2)
MERGER Recorded Jan 19, 2015
From: AVENTIS PHARMACEUTICALS INC.
To: AVENTISUB LLC
Reel/Frame 034781/0334 →
CERTIFICATE OF CONVERSION Recorded Dec 9, 2014
From: AVENTISUB INC.
To: AVENTISUB LLC
Reel/Frame 034566/0976 →