US2012208820A1PendingUtilityA1

Diazabicyclic central nervous system active agents

58
Assignee: SCHRIMPF MICHAEL RPriority: Apr 27, 2000Filed: Jan 31, 2012Published: Aug 16, 2012
Est. expiryApr 27, 2020(expired)· nominal 20-yr term from priority
A61P 25/28A61P 25/00A61P 25/16A61P 25/34C07D 487/04C07D 471/04A61P 25/18A61P 25/24A61P 29/00
58
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Claims

Abstract

Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.

Claims

exact text as granted — not AI-modified
1 .- 9 . (canceled) 
     
     
         10 . A compound according to claim  1  of formula VI 
       
         
           
           
               
               
           
         
       
       or pharmaceutically acceptable salts thereof,
 wherein 
 Y is selected from the group consisting of a covalent bond, CH 2 , and CH 2 CH 2 ; 
 Z is selected from the group consisting of a covalent bond, CH 2 , CH 2 CH 2 , provided that when Y is CH 2 CH 2 , then Z is a covalent bond and further provided that when Z is CH 2 CH 2 , then Y is a covalent bond; 
 R 1  is selected from the group consisting of 
 
       
         
           
           
               
               
           
         
         R 3  is selected from the group consisting of hydrogen, alkyl, and halogen; 
         R 4  is selected from the group consisting of hydrogen, alkoxy, alkyl, amino, halogen, and nitro; 
         R 5  is selected from the group consisting of hydrogen, alkenyl, alkoxy, alkoxyalkoxy, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkyl, alkylcarbonyl, alkylcarbonyloxy, alkylthio, alkynyl, amino, aminoalkyl, aminocarbonyl, aminocarbonylalkyl, aminosulfonyl, carboxy, carboxyalkyl, cyano, cyanoalkyl, formyl, formylalkyl, haloalkoxy, haloalkyl, halogen, hydroxy, hydroxyalkyl, mercapto, mercaptoalkyl, nitro, 5-tetrazolyl, —NR 6 S(O) 2 R 7 , —C(NR 6 )NR 7 R 8 , —CH 2 C(NR 6 )NR 7 R 8 , C(NOR 6 )R 7 , —C(NCN)R 6 , —C(NNR 6 R 7 )R 8 , —S(O) 2 OR 6 , and —S(O) 2 R 6 ; 
         R 6 , R 7  and R 8  are independently selected from the group consisting of hydrogen and alkyl; and 
         R 9  is selected from the group consisting of hydrogen, alkoxycarbonyl, alkyl, amino, aminoalkyl, aminocarbonylalkyl, benzyloxycarbonyl, cyanoalkyl, dihydro-3-pyridinylcarbonyl, hydroxy, hydroxyalkyl, and phenoxycarbonyl. 
       
     
     
         11 . A compound according to  claim 10  wherein Y is CH 2  and Z is a covalent bond. 
     
     
         12 . A compound according to  claim 10  wherein Y is a covalent bond and Z is CH 2 . 
     
     
         13 . A compound according to  claim 10  wherein Y is CH 2 CH 2  and Z is a covalent bond. 
     
     
         14 . A compound according to  claim 10  wherein Y is CH 2  and Z is CH 2 . 
     
     
         15 . A compound according to  claim 10  wherein Y is a covalent bond and Z is a covalent bond. 
     
     
         16 . A compound according to  claim 10  wherein Y is a covalent bond and Z is CH 2 CH 2 . 
     
     
         17 .- 32 . (canceled) 
     
     
         33 . A pharmaceutical composition comprising a therapeutically effective amount of a compound of  claim 10  in combination with a pharmaceutically acceptable carrier. 
     
     
         34 . (canceled) 
     
     
         35 . A method of treating a disorder wherein the disorder is ameliorated by controlling neurotransmitter release in a host mammal in need of such treatment comprising administering a therapeutically effective amount of a compound of  claim 10  wherein the disorder is selected from the group consisting of Alzheimer's disease, Parkinson's disease, attention deficit hyperactivity disorder, depression, nicotinic withdrawal syndrome, Tourette's syndrome, schizophrenia, and pain. 
     
     
         36 .- 37 . (canceled) 
     
     
         38 . A method of treating pain in a mammal comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of  claim 10  in combination with an agent selected from the group consisting of a non-steroid anti-inflammatory agent, an opioid agent, a tricyclic antidepressant, or an anticonvulsant, and a pharmaceutically acceptable carrier. 
     
     
         39 .- 41 . (canceled)

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