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Last Updated: April 19, 2024

Details for Patent: 6,750,244


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Title: Compounds active at a novel site on receptor-operated calcium channels useful for treatment of neurological disorders and diseases
Abstract:Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).
Inventor(s): Mueller; Alan L. (Salt Lake City, UT), Moe; Scott T. (Salt Lake City, UT)
Assignee: NPS Pharmaceuticals, Inc. (Salt Lake City, UT)
Filing Date:Apr 02, 2001
Application Number:09/825,373
Claims:1. A compound of Formula VIII: ##STR189##

wherein: Z is selected from the group consisting of: --S--CH.sub.2 --, --O--CH.sub.2 --, --O--, and --S--; X.sup.1 and X.sup.2 are independently selected from the group consisting of F, --Cl, --CH.sub.3, --OH, and lower O-alkyl in the 1-, 3-, 7-, or 9-substituent positions; m is independently an integer from 0 to 2, provided that at least one of m is not 0; --NHR is selected from the group consisting of --NH.sub.2, --NHCH.sub.3, and --NHC.sub.2 H.sub.5 ; R.sup.1 is selected from the group consisting of --H, alkyl, hydroxyalkyl, --OH, --O-alkyl, and --O-acyl, and R.sup.2 is selected from the group consisting of --H, alkyl, hydroxyalkyl, and pharmaceutically acceptable salts and complexes thereof, wherein the compound is active at an NMDA receptor.

2. A compound of Formula VIII: ##STR190## wherein: Z is selected from the group consisting of: --S--CH.sub.2 --, --O--CH.sub.2 --, --O--, and --S--; X.sup.1 and X.sup.2 are independently selected from the group consisting of: F, --Cl, --CH.sub.3, --OH, and lower O-alkyl in the 1-, 3-, 7-, or 9-substituent positions; m is independently an integer from 1 to 2; --NHR is selected from the group consisting of --NH.sub.2, --NHCH.sub.3, and --NHC.sub.2 H.sub.5 ; R.sup.1 is selected from the group consisting of --H, alkyl, hydroxyalkyl, --OH, --O-alkyl, and --O-acyl, and R.sup.2 is selected from the group consisting of --H, alkyl, hydroxyalkyl, and pharmaceutically acceptable salts and complexes thereof, wherein the compound is active at an NMDA receptor.

3. A pharmaceutical composition comprising a compound of claim 1, and a pharmaceutically acceptable carrier.

4. A method of treating a patient having a neurological disease or disorder comprising administering a compound of Formula VIII: ##STR191##

wherein: Z is selected from the group consisting of: --O--, --O--CH.sub.2 --, --S--CH.sub.2, and --S--; X.sup.1 and X.sup.2 are independently selected from the group consisting of --F, --Cl, --CH.sub.3, --OH, and lower O-alkyl in the 1-, 3-, 7-, or 9-substituent positions; m is independently an integer from 0 to 2; --NHR is selected from the group consisting of --NH.sub.2, --NHCH.sub.3, and --NHC.sub.2 H.sub.5 ; R.sup.1 is selected from the group consisting of --H, alkyl, hydroxyalkyl, --OH, --O-alkyl, and --O-acyl, and R.sup.2 is selected from the group consisting of --H, alkyl, hydroxyalkyl, and pharmaceutically acceptable salts and complexes thereof, wherein the compound is active at an NMDA receptor.

5. A method of treating a patient having a neurological disease or disorder comprising administering a compound of a structure selected from the group consisting of: ##STR192##

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