US2020397783A1PendingUtilityA1

Prevention of hiv-infection

73
Assignee: JANSSEN SCIENCES IRELAND UNLIMITED COPriority: Apr 4, 2005Filed: Sep 2, 2020Published: Dec 24, 2020
Est. expiryApr 4, 2025(expired)· nominal 20-yr term from priority
A61K 47/16A61K 31/505A61K 47/10A61K 9/0019A61P 31/18A61P 43/00A61P 31/00
73
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Claims

Abstract

This invention relates to the use of a parenteral formulation comprising the NNRTI TMC278 for the long term prevention of HIV infection in a subject at risk of being infected by HIV, which comprises the intermittent administration of the said formulation at long time intervals.

Claims

exact text as granted — not AI-modified
1 - 9 . (canceled) 
     
     
         10 . A method for the avoidance of human immunodeficiency virus 1 (HIV-1) infection in an individual at risk of being infected by HIV-1 comprising administrating to such an individual, intermittently at a time interval of at least one week, a sustained release parenteral formulation containing an effective amount of an HIV inhibitor 4-[[4-[[-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]-amino]benzonitrile, the E isomeric form thereof or the Z-isomeric form thereof; or a pharmaceutically acceptable acid-addition salt thereof, and a pharmaceutically acceptable carrier, wherein the effective amount is selected such that the blood plasma level is kept at a level above about 4 ng/ml. 
     
     
         11 . The method according to  claim 10  wherein the formulation is administered once every two weeks. 
     
     
         12 . The method according to  claim 10  wherein the formulation is administered once every month. 
     
     
         13 . The method according to  claim 10  wherein the blood plasma level is kept at a level equal to or above about 15 ng/ml. 
     
     
         14 . The method according to  claim 10  wherein the blood plasma level is kept at a level equal to or above 20 ng/ml. 
     
     
         15 . The method according to  claim 10  wherein the formulation is administered subcutaneously or intramuscularly. 
     
     
         16 . The method according to  claim 10  wherein the HIV inhibitor 4-[[4-[[-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]-amino]benzonitrile is in base form. 
     
     
         17 - 30 . (canceled) 
     
     
         31 . The method according to  claim 10  wherein the formulation is administered once every two months. 
     
     
         32 . The method according to  claim 10  wherein the formulation is administered intramuscularly. 
     
     
         33 . The method according to  claim 16  wherein the base form of 4-[[4-[[-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]-amino]benzonitrile occurs in its E-isomeric form. 
     
     
         34 - 38 . (canceled)

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