Compounds, compositions and methods for treatment of hepatitis C
First Claim
Patent Images
1. A compound having the formula:
- ##STR9## wherein R1, R2, R3 and R4 are the same or different and represent substituents selected from the group consisting of hydrogen, alkyl (C1 -C6), halogen, hydroxy, alkoxy, carboxy, carbalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, amino, acetamido, sulfonamido, alkylamino, dialkylamino and NO2 ;
W and X represent the same or different linking moieties selected from the group consisting of alkylene (C1 -C5) and carbonyl (--(C═
O)--);
Y and Z represent the same or different substituents selected from the group consisting of ##STR10## wherein R5 represents a substituent selected from the group consisting of hydrogen, alkyl (C1 -C6) and acyl, and each R6 is the same or different and represents a substituent selected from the group consisting of hydrogen, alkyl (C1 -C6), halogen, hydroxy, alkoxy, carboxy, carbalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, amino, acetamido, sulfonamido, alkylamino, dialkylamino and NO2, and m is 1-4, and wherein R7 represents a substituent selected from the group consisting of hydrogen, alkyl and acyl, and n is from 3 to 5; and
the isomers and pharmaceutically acceptable salts of said compounds.
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Abstract
Derivatives of piperidine are useful in prophylaxis and treatment of hepatitis C virus infections.
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Citations
17 Claims
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1. A compound having the formula:
- ##STR9## wherein R1, R2, R3 and R4 are the same or different and represent substituents selected from the group consisting of hydrogen, alkyl (C1 -C6), halogen, hydroxy, alkoxy, carboxy, carbalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, amino, acetamido, sulfonamido, alkylamino, dialkylamino and NO2 ;
W and X represent the same or different linking moieties selected from the group consisting of alkylene (C1 -C5) and carbonyl (--(C═
O)--);
Y and Z represent the same or different substituents selected from the group consisting of ##STR10## wherein R5 represents a substituent selected from the group consisting of hydrogen, alkyl (C1 -C6) and acyl, and each R6 is the same or different and represents a substituent selected from the group consisting of hydrogen, alkyl (C1 -C6), halogen, hydroxy, alkoxy, carboxy, carbalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, amino, acetamido, sulfonamido, alkylamino, dialkylamino and NO2, and m is 1-4, and wherein R7 represents a substituent selected from the group consisting of hydrogen, alkyl and acyl, and n is from 3 to 5; and
the isomers and pharmaceutically acceptable salts of said compounds. - View Dependent Claims (9, 10, 11, 12, 13, 14, 15, 16, 17)
- ##STR9## wherein R1, R2, R3 and R4 are the same or different and represent substituents selected from the group consisting of hydrogen, alkyl (C1 -C6), halogen, hydroxy, alkoxy, carboxy, carbalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, amino, acetamido, sulfonamido, alkylamino, dialkylamino and NO2 ;
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2. A compound having the formula ##STR11## wherein R1 R2, R3 and R4 are the same or different and represent substituents selected from the group consisting of hydrogen, alkyl (C1 -C6), halogen, hydroxy, alkoxy, carboxy, carbalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, amino, acetamido, sulfonamido, alkylamino, dialkylamino and NO2 ;
- Y and Z represent the same or different substituent selected from the group consisting of ##STR12## wherein R5 represents a substituent selected from the group consisting of hydrogen, alkyl (C1 -C6) and acyl, and each R6 is the same or different and represents a substituent selected from the group consisting of hydrogen, alkyl (C1 -C6), halogen, hydroxy, alkoxy, carboxy, carbalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, amino, acetamido, sulfonamido, alkylamino, dialkylamino and NO2, and m is 1-4, and wherein R7 represents a substituent selected from the group consisting of hydrogen, alkyl and acyl, and n is from 3 to 5; and
the isomers and pharmaceutically acceptable salts of said compound. - View Dependent Claims (3, 4)
- Y and Z represent the same or different substituent selected from the group consisting of ##STR12## wherein R5 represents a substituent selected from the group consisting of hydrogen, alkyl (C1 -C6) and acyl, and each R6 is the same or different and represents a substituent selected from the group consisting of hydrogen, alkyl (C1 -C6), halogen, hydroxy, alkoxy, carboxy, carbalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, amino, acetamido, sulfonamido, alkylamino, dialkylamino and NO2, and m is 1-4, and wherein R7 represents a substituent selected from the group consisting of hydrogen, alkyl and acyl, and n is from 3 to 5; and
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5. A compound having the formula ##STR13## wherein R1, R2, R3 and R4 are the same or different and represent substituents selected from the group consisting of hydrogen, alkyl (C1 -C6), halogen, hydroxy, alkoxy, carboxy, carbalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, amino, acetamido, sulfonamido, alkylamino, dialkylamino and NO2 ;
- Y and Z represent the same or different substituent selected from the group consisting of ##STR14## wherein R5 represents a substituent selected from the group consisting of hydrogen, alkyl (C1 -C6) and acyl, and each R6 is the same or different and represents a substituent selected from the group consisting of hydrogen, alkyl (C1 -C6), halogen, hydroxy, alkoxy, carboxy, carbalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, amino, acetamido, sulfonamido, alkylamino, dialkylamino and NO2, and m is 1-4, and wherein R7 represents a substituent selected from the group consisting of hydrogen, alkyl and acyl, and n is from 3 to 5; and
the isomers and pharmaceutically acceptable salts of said compound. - View Dependent Claims (6)
- Y and Z represent the same or different substituent selected from the group consisting of ##STR14## wherein R5 represents a substituent selected from the group consisting of hydrogen, alkyl (C1 -C6) and acyl, and each R6 is the same or different and represents a substituent selected from the group consisting of hydrogen, alkyl (C1 -C6), halogen, hydroxy, alkoxy, carboxy, carbalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, amino, acetamido, sulfonamido, alkylamino, dialkylamino and NO2, and m is 1-4, and wherein R7 represents a substituent selected from the group consisting of hydrogen, alkyl and acyl, and n is from 3 to 5; and
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7. A compound having the formula ##STR15## wherein R8 represents a carbalkoxy (C1 -C6) substituent.
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8. A compound having the formula ##STR16## wherein R8 represents ##STR17##
Specification
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Current AssigneeWyeth (Pfizer Inc.)
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Original AssigneeViroPharma Inc. (Shire plc)
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InventorsBailey, Thomas R., Nitz, Theodore J., Diana, Guy D.
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Primary Examiner(s)Woodward, Michael P.
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Assistant Examiner(s)Brumback, Brenda G.
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Application NumberUS08/625,718Time in Patent Office949 DaysField of Search424/422, 546/184, 546/186, 546/187, 514/322US Class Current514/322CPC Class CodesC07D 211/58 attached in position 4C07D 211/62 attached in position 4C07D 401/14 containing three or more he...
