IP Library Granted Patent US 8,759,336
Granted Patent B2
US 8,759,336 · App. 13/423,141 · Granted Jun 24, 2014

Antiviral compounds

Inventors: Clarence R. Hurt (Los Altos, CA); Vishwanath Lingappa (San Francisco, CA); Beverly Freeman (Albany, CA); Andy Atuegbu (Dublin, CA); Anatoliy Kitaygorodorskyy (San Francisco, CA)
Assignee: Prosetta Antiviral Inc.
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Quick Facts
Patent No.
US 8,759,336
App. No.
13/423,141
Granted
Jun 24, 2014
Kind
B2
Abstract

Novel compounds, methods, and compositions for treating various viral infections are described. In some embodiments the novel compounds of the invention are 3-oxo-phenothiazine derivatives; more specific embodiments include 3-oxo-phenothiazine derivatives having substituents at the 1-, 7-, and 9-positions of the phenothiazine parent ring. In other embodiments, the invention provides compositions and methods for treating viral infections, especially HIV.

Claims (58)

1. A compound having the structure:

and its pharmaceutically acceptable salts and hydrates, wherein:

R 9 is selected from the group consisting of: halo, cyano, nitro, amino, carboxyl, formyl, sulfo, sulfinyl, sulfeno, sulfenamoyl, sulfonamino, and optionally substituted loweralkyl, loweralkylcarbonyloxy, arylcarbonyloxy, heteroarylcarbonyloxy, cycloalkylcarbonyloxy, cycloheteroalkylcarbonyloxy, aralkycarbonyloxy, heteroaralkylcarbonyloxy, (cycloalkyl)alkylcarbonyloxy, (cycloheteroalkyl)alkylcarbonyloxy, loweralkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, cycloalkycarbonyl, cycloheteroalkycarbonyl, aralkycarbonyl, heteroaralkylcarbonyl, (cycloalkyl)alkylcarbonyl, (cycloheteroalkyl)alkylcarbonyl, loweralkylaminocarbonyl, arylaminocarbonyl, aralkylaminocarbonyl, heteroarylaminocarbonyl, heteroaralkylaminocarbonyl, loweralkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, cycloalkylcarbonylamino, cycloheteroalkylcarbonylamino, aralkylcarbonylamino, heteroaralkylcarbonylamino, (cycloalkyl)alkylcarbonylamino, (cycloheteroalkyl)alkylcarbonylamino, diloweralkylamino, arylamino, diarylamino, aralkylamino, diaralkylamino, heteroarylamino, diheteroarylamino, heteroaralkylamino, diheteroaralkylamino, loweralkylsulfonyl, arylsulfonyl, heteroarylsulfonyl, cycloalkylsulfonyl, loweralkylsulfonyldioxy, arylsulfonyldioxy, heteroarylsulfonyldioxy, loweralkylsulfo, arylsulfo, heteroarylsulfo, cycloalkylsulfo, loweralkylsulfinyl, arylsulfinyl, heteroarylsulfinyl, cycloalkylsulfinyl, loweralkylsulfeno, arylsulfeno, heteroarylsulfeno, cycloalkylsulfeno, loweralkylsulfoamino, arylsulfoamino, heteroarylsulfoamino, cycloalkylsulfoamino, sulfonaloweralkylcarbonylsulfenamoyl, arylcarbonylsulfenamoyl, heteroarylcarbonylsulfenamoyl, cycloalkylcarbonylsulfenamoyl, cycloheteroalkylcarbonylsulfenamoyl, aralkylcarbonylsulfenamoyl, heteroaralkylcarbonylsulfenamoyl, (cycloalkyl)alkylcarbonylsulfenamoyl, (cycloheteroalkyl)alkylcarbonylsulfenamoyl, diloweralkylsulfenamoyl, arylsulfenamoyl, diarylsulfenamoyl, aralkylsulfenamoyl, diaralkylsulfenamoyl, heteroarylsulfenamoyl, diheteroarylsulfenamoyl, heteroaralkylsulfenamoyl, diheteroaralkylsulfenamoyl, loweralkylcarbonylsulfinamoyl, arylcarbonylsulfinamoyl, heteroarylcarbonylsulfinamoyl, cycloalkylcarbonylsulfinamoyl, cycloheteroalkylcarbonylsulfinamoyl, aralkylcarbonylsulfinamoyl, heteroaralkylcarbonylsulfinamoyl, (cycloalkyl)alkylcarbonylsulfinamoyl, (cycloheteroalkyl)alkylcarbonylsulfinamoyl, diloweralkylsulfinamoyl, arylsulfinamoyl, diarylsulfinamoyl, aralkylsulfinamoyl, diaralkylsulfinamoyl, heteroarylsulfinamoyl, diheteroarylsulfinamoyl, heteroaralkylsulfinamoyl, diheteroaralkylsulfinamoyl, loweralkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, cycloalkyloxycarbonyl, cycloheteroalkyloxycarbonyl, aralyoxycarbonyloxloxycarbonyl, heteroaralkyloxycarbonyl, (cycloalkyl)alkyloxycarbonyl, (cycloheteroalkyl)alkyloxycarbonyl, iminoloweralkyl, iminocycloalkyl, iminocycloheteroalkyl, iminoaralkyl, iminoheteroaralkyl, (cycloalkyl)iminoalkyl, and (cycloheteroalkyl)iminoalkyl;

R 1 , R 2 , R 4 , R 5 , and R 8 are selected independently from the group consisting of: hydrogen, halo, cyano, nitro, amino, carboxyl, formyl, sulfo, sulfinyl, sulfeno, sulfenamoyl, sulfonamino, and optionally substituted loweralkyl, loweralkylcarbonyloxy, arylcarbonyloxy, heteroarylcarbonyloxy, cycloalkylcarbonyloxy, cycloheteroalkylcarbonyloxy, aralkycarbonyloxy, heteroaralkylcarbonyloxy, (cycloalkyl)alkylcarbonyloxy, (cycloheteroalkyl)alkylcarbonyloxy, loweralkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, cycloalkycarbonyl, cycloheteroalkycarbonyl, aralkycarbonyl, heteroaralkylcarbonyl, (cycloalkyl)alkylcarbonyl, (cycloheteroalkyl)alkylcarbonyl, loweralkylaminocarbonyl, arylaminocarbonyl, aralkylaminocarbonyl, heteroarylaminocarbonyl, heteroaralkylaminocarbonyl, loweralkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, cycloalkylcarbonylamino, cycloheteroalkylcarbonylamino, aralkylcarbonylamino, heteroaralkylcarbonylamino, (cycloalkyl)alkylcarbonylamino, (cycloheteroalkyl)alkylcarbonylamino, diloweralkylamino, arylamino, diarylamino, aralkylamino, diaralkylamino, heteroarylamino, diheteroarylamino, heteroaralkylamino, diheteroaralkylamino, loweralkylsulfonyl, arylsulfonyl, heteroarylsulfonyl, cycloalkylsulfonyl, loweralkylsulfonyldioxy, arylsulfonyldioxy, heteroarylsulfonyldioxy, loweralkylsulfo, arylsulfo, heteroarylsulfo, cycloalkylsulfo, loweralkylsulfinyl, arylsulfinyl, heteroarylsulfinyl, cycloalkylsulfinyl, loweralkylsulfeno, arylsulfeno, heteroarylsulfeno, cycloalkylsulfeno, loweralkylsulfoamino, arylsulfoamino, heteroarylsulfoamino, cycloalkylsulfoamino, sulfonaloweralkylcarbonylsulfenamoyl, arylcarbonylsulfenamoyl, heteroarylcarbonylsulfenamoyl, cycloalkylcarbonylsulfenamoyl, cycloheteroalkylcarbonylsulfenamoyl, aralkylcarbonylsulfenamoyl, heteroaralkylcarbonylsulfenamoyl, (cycloalkyl)alkylcarbonylsulfenamoyl, (cycloheteroalkyl)alkylcarbonylsulfenamoyl, diloweralkylsulfenamoyl, arylsulfenamoyl, diarylsulfenamoyl, aralkylsulfenamoyl, diaralkylsulfenamoyl, heteroarylsulfenamoyl, diheteroarylsulfenamoyl, heteroaralkylsulfenamoyl, diheteroaralkylsulfenamoyl, loweralkylcarbonylsulfinamoyl, arylcarbonylsulfinamoyl, heteroarylcarbonylsulfinamoyl, cycloalkylcarbonylsulfinamoyl, cycloheteroalkylcarbonylsulfinamoyl, aralkylcarbonylsulfinamoyl, heteroaralkylcarbonylsulfinamoyl, (cycloalkyl)alkylcarbonylsulfinamoyl, (cycloheteroalkyl)alkylcarbonylsulfinamoyl, diloweralkylsulfinamoyl, arylsulfinamoyl, diarylsulfinamoyl, aralkylsulfinamoyl, diaralkylsulfinamoyl, heteroarylsulfenamoyl, diheteroarylsulfinamoyl, heteroaralkylsulfinamoyl, diheteroaralkylsulfinamoyl, loweralkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, cycloalkyloxycarbonyl, cycloheteroalkyloxycarbonyl, aralyoxycarbonyloxloxycarbonyl, heteroaralkyloxycarbonyl, (cycloalkyl)alkyloxycarbonyl, (cycloheteroalkyl)alkyloxycarbonyl, iminoloweralkyl, iminocycloalkyl, iminocycloheteroalkyl, iminoaralkyl, iminoheteroaralkyl, (cycloalkyl)iminoalkyl, and (cycloheteroalkyl)iminoalkyl;

R 3 is selected from the group consisting of: halo, oxo, imino, iminoloweralkyl, iminocycloalkyl, iminocycloheteroalkyl, iminoaralkyl, iminoheteroaralkyl, (cycloalkyl)iminoalkyl, and (cycloheteroalkyl)iminoalkyl; and

R 6 and R 7 are selected independently from the group consisting of: hydrogen and optionally substituted loweralkyl, loweralkyloxyloweralkyl, aminoloweralkyl, loweralkylaminoloweralkyl, diloweralkylaminoloweralkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, arylcarbonyl, alkylcarbonyl, aralkylcarbonyl, heteroarylcarbonyl, and heteroaralkylcarbonyl; in addition, R 6 and R 7 , together with the nitrogen atom to which each is attached, can form an optionally substituted 4-, 5-, 6-, or 7-membered ring

wherein said optionally substituted is with a group which is hydrooxyl, nitro, amino, imino, cyano, halo, amidino, oxo, oxamidino, methoxamidino, imidino, guanidino, sulfonamido, carboxyl, formyl, lower alkyl, haloloweralkyl, loweralkoxy, haloloweralkoxy, lower alkoxyalkyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heteroarylcarbonyl, heteroaralkylcarbonyl, aminoalkyl, or cyanoalkyl.

2. A compound of claim 1 , wherein R 3 is oxo.

3. A compound of claim 2 , wherein R 6 and R 7 forms an optionally substituted pyrrolidinyl ring with the nitrogen atom to which they are attached.

4. A compound of claim 3 , wherein R 6 and R 7 , together with the nitrogen atom to which they are attached, is optionally substituted pyrrolidin-1-yl.

5. A compound of claim 4 , wherein at least one of R 1 and R 9 is selected from the group consisting of: halo, optionally substituted loweralkyloxy, and optionally substituted loweralkyl.

6. A compound of claim 5 , wherein at least one of R 1 and R 9 is halo.

7. A compound of claim 6 , wherein both R 1 and R 9 are halo.

8. A compound of claim 7 , wherein R 1 and R 9 are selected from the group consisting of: chloro and fluoro.

9. A compound of claim 8 , wherein R 1 and R 9 are both chloro or both fluoro.

10. A compound of claim 5 , wherein at least one of R 1 and R 9 is loweralkyloxy.

11. A compound of claim 10 , wherein both R 1 and R 9 are methoxy.

12. A compound of claim 2 , wherein R 6 and R 7 , together with the nitrogen atom to which they are attached, is optionally substituted piperazinyl.

13. A compound of claim 12 , wherein R 6 and R 7 , together with the nitrogen atom to which they are attached, is optionally substituted piperazin-1-yl.

14. A compound of claim 13 , wherein both R 1 and R 9 are selected from the group consisting of halo and optionally substituted loweralkyl.

15. A compound of claim 14 , wherein at least one of R 1 and R 9 is halo.

16. A compound of claim 15 , wherein R 1 and R 9 are both chloro or both fluoro.

17. A compound of claim 14 , wherein at least one of R 1 and R 9 is loweralkyl.

18. A compound of claim 17 , wherein at least one of R 1 and R 9 is methyl.

19. A method for treating a viral disease in a mammal afflicted with such disease, wherein said viral disease is selected from the group consisting of HCV, HIV, influenza, Ebola virus, Marburg virus, Dengue virus, Venezuelean equine encephalitis, Chikungunya virus, and West Nile virus, Easter Equine Encephalitis, Western Equine Encephalitis, Monkey Pox, Corona Virus, Respiratory Syncytial Virus, Adenovirus, Human Rhinovirus, and Herpes Simplex Virus, comprising administering to such mammal a therapeutically effective amount of the compound having the structure:

and its pharmaceutically acceptable salts and hydrates, wherein:

R 1 , R 2 , R 4 , R 5 , R 8 , and R 9 are selected independently from the group consisting of: hydrogen, halo, cyano, nitro, amino, carboxyl, formyl, sulfo, sulfinyl, sulfeno, sulfenamoyl, sulfonamino, and optionally substituted loweralkyl, loweralkylcarbonyloxy, arylcarbonyloxy, heteroarylcarbonyloxy, cycloalkylcarbonyloxy, cycloheteroalkylcarbonyloxy, aralkycarbonyloxy, heteroaralkylcarbonyloxy, (cycloalkyl)alkylcarbonyloxy, (cycloheteroalkyl)alkylcarbonyloxy, loweralkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, cycloalkycarbonyl, cycloheteroalkycarbonyl, aralkycarbonyl, heteroaralkylcarbonyl, (cycloalkyl)alkylcarbonyl, (cycloheteroalkyl)alkylcarbonyl, loweralkylaminocarbonyl, arylaminocarbonyl, aralkylaminocarbonyl, heteroarylaminocarbonyl, heteroaralkylaminocarbonyl, loweralkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, cycloalkylcarbonylamino, cycloheteroalkylcarbonylamino, aralkylcarbonylamino, heteroaralkylcarbonylamino, (cycloalkyl)alkylcarbonylamino, (cycloheteroalkyl)alkylcarbonylamino, diloweralkylamino, arylamino, diarylamino, aralkylamino, diaralkylamino, heteroarylamino, diheteroarylamino, heteroaralkylamino, diheteroaralkylamino, loweralkylsulfonyl, arylsulfonyl, heteroarylsulfonyl, cycloalkylsulfonyl, loweralkylsulfonyldioxy, arylsulfonyldioxy, heteroarylsulfonyldioxy, loweralkylsulfo, arylsulfo, heteroarylsulfo, cycloalkylsulfo, loweralkylsulfinyl, arylsulfinyl, heteroarylsulfinyl, cycloalkylsulfinyl, loweralkylsulfeno, arylsulfeno, heteroarylsulfeno, cycloalkylsulfeno, loweralkylsulfoamino, arylsulfoamino, heteroarylsulfoamino, cycloalkylsulfoamino, sulfonaloweralkylcarbonylsulfenamoyl, arylcarbonylsulfenamoyl, heteroarylcarbonylsulfenamoyl, cycloalkylcarbonylsulfenamoyl, cycloheteroalkylcarbonylsulfenamoyl, aralkylcarbonylsulfenamoyl, heteroaralkylcarbonylsulfenamoyl, (cycloalkyl)alkylcarbonylsulfenamoyl, (cycloheteroalkyl)alkylcarbonylsulfenamoyl, diloweralkylsulfenamoyl, arylsulfenamoyl, diarylsulfenamoyl, aralkylsulfenamoyl, diaralkylsulfenamoyl, heteroarylsulfenamoyl, diheteroarylsulfenamoyl, heteroaralkylsulfenamoyl, diheteroaralkylsulfenamoyl, loweralkylcarbonylsulfinamoyl, arylcarbonylsulfinamoyl, heteroarylcarbonylsulfinamoyl, cycloalkylcarbonylsulfinarnoyl, cycloheteroalkylcarbonylsulfinamoyl, aralkylcarbonylsulfinamoyl, heteroaralkylcarbonylsulfinamoyl, (cycloalkyl)alkylcarbonylsulfinamoyl, (cycloheteroalkyl)alkylcarbonylsulfinamoyl, diloweralkylsulfinamoyl, arylsulfinamoyl, diarylsulfinamoyl, aralkylsulfinamoyl, diaralkylsulfenamoyl, heteroarylsulfinamoyl, diheteroarylsulfenamoyl, heteroaralkylsulfinamoyl, diheteroaralkylsulfenamoyl, loweralkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, cycloalkyloxycarbonyl, cycloheteroalkyloxycarbonyl, aralyoxycarbonyloxloxycarbonyl, heteroaralkyloxycarbonyl, (cycloalkyl)alkyloxycarbonyl, (cycloheteroalkyl)alkyloxycarbonyl, iminoloweralkyl, iminocycloalkyl, iminocycloheteroalkyl, iminoaralkyl, iminoheteroaralkyl, (cycloalkyl)iminoalkyl, and (cycloheteroalkyl)iminoalkyl;

R 3 is selected from the group consisting of: halo, oxo, imino, iminoloweralkyl, iminocycloalkyl, iminocycloheteroalkyl, iminoaralkyl, iminoheteroaralkyl, (cycloalkyl)iminoalkyl, and (cycloheteroalkyl)iminoalkyl; and

R 6 and R 7 are selected independently from the group consisting of: hydrogen and optionally substituted loweralkyl, loweralkyloxyloweralkyl, aminoloweralkyl, loweralkylaminoloweralkyl, diloweralkylaminoloweralkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, arylcarbonyl, alkylcarbonyl, aralkylcarbonyl, heteroarylcarbonyl, and heteroaralkylcarbonyl; in addition, R 6 and R 7 , together with the nitrogen atom to which each is attached, can form an optionally substituted 4-, 5-, 6-, or 7-membered ring

wherein said optionally substituted is with a group which is hydrooxyl, nitro, amino, imino, cyano, halo, amidino, oxo, oxamidino, methoxamidino, imidino, guanidino, sulfonamido, carboxyl, formyl, lower alkyl, haloloweralkyl, loweralkoxy, haloloweralkoxy, lower alkoxyalkyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heteroarylcarbonyl, heteroaralkylcarbonyl, aminoalkyl, or cyanoalkyl.

20. A compound of claim 2 , wherein R 6 and R 7 are optionally substituted loweralkyl, alkyloxyalkyl, alkylaminoalkyl, and dialkylaminoalkyl.

21. A compound of claim 2 , wherein R 6 and R 7 are optionally substituted lower alkyl or optionally substituted loweralkyloxyloweralkyl.

22. A compound of claim 2 , wherein R 6 and R 7 are optionally substituted methyl, ethyl, or propyl.

23. A compound of claim 2 , wherein R 6 and R 7 are optionally substituted methyl.

24. A compound of claim 1 , wherein R 6 and R 7 , together with the nitrogen atom to which each is attached, form an optionally substituted 4-, 5-, 6-, or 7-membered ring, and the ring is an optionally substituted pyrrolidinyl, piperidyl, morpholinyl, piperazinyl, azetidinyl, quinuclidinyl, or azepanyl.

25. A compound of claim 1 , which is 7-(1,4-diazepan-1-yl)-1,9-dimethyl-phenothiazin-3-one.

26. A compound of claim 1 , which is 7-(dimethylamino)-1,9-dimethyl-phenothiazin-3-one, 1,9-dimethyl-7-(4-methylpiperazin-1-yl)phenothiazin-3-one, 7-[bis(2-methoxyethyl)amino]-1,9-dimethylphenothiazin-3-one, 1,9-dimethyl-7-morpholino-phenothiazin-3-one, tert-butyl 4-(1,9-dimethyl-7-oxo-phenothizin-3-yl)piperazine-1-carboxylate, 1,9-dimethyl-7-piperazin-1-yl-phenothiazin-3-one, 1,9-dimethyl-7-pyrrolidin-1-yl-phenothiazin-3-one, tert-butyl 4-(1,9-dimethyl-7-oxo-phenothiazin-3-yl)-1,4-diazepane-1-carboxylate, 7-(azepan-1-yl)-1,9-dimethyl-phenothiazin-3-one, 7-(azetidin-1-yl)-1,9-dimethyl-phenothiazin-3-one, 7-(4-isopropylpiperazin-1-yl)-1,9-dimethylphenothiazin-3-one, 1,9-dimethyl-7-(4-methylsulfonylpiperazin-1-yl)phenothiazin-3-one, 1-(1,9-dimethyl-7-oxo-phenothiazin-3-yl)piperidine-4-carboxamide, 1,9-dimethyl-7-[4-(trifluoromethylsulfonyl)piperazin-1-yl]phenothiazin-3-one, 7-(4-isopropylsulfonylpiperazin-1-yl)-1,9-dimethyl-phenothiazin-3-one, 7-(4,4-difluoro-1-piperidyl)-1,9-dimethyl-phenothiazin-3-one, 1-(1,9-dimethyl-7-oxo-phenothiazin-3-yl)piperidine-4-carboxamidine, or 7-(azepan-1-yl)-1,9-diethyl-phenothiazin-3-one.

27. A compound of claim 1 , which is 1,9-dichloro-7-pyrrolidin-1-yl-phenothiazin-3-one, 1,9-dichloro-7-(dimethylamino)phenothiazin-3-one, N-tert-butyl-4-(1,9-dichloro-7-oxo-phenothiazin-3-yl)piperazine-1-carboxamide, 7-[bis(2-methoxyethyl)amino]-1,9-dichlorophenothiazin-3-one, 4-(1,9-dichloro-7-oxo-phenothiazin-3-yl)-N,N-dimethyl-piperazine-1-sulfonamide, 1,9-dichloro-7-[4-(trifluoromethylsulfonyl)piperazin-1-yl]phenothiazin-3-one, tert-butyl 4-(1,9-dichloro-7-oxo-phenothiazin-3-yl)piperazine-1-carboxylate, or 1,9-difluoro-7-pyrrolidin-1-yl-phenothiazin-3-one.

28. A compound of claim 1 , which is 1,9-dimethoxy-7-(4-methylpiperazin-1-yl)phenothiazin-3-one or 1,9-dimethoxy-7-pyrrolidin-1-yl-phenothiazin-3-one.

29. A compound of claim 1 , which is 7-(dimethylamino)-1-fluoro-phenothiazin-3-one, 7-(dimethylamino)-1-(trifluoromethyl)phenothiazin-3-one, 7-[bis(2-methoxyethyl)amino]-3-oxo-phenothiazine-1-carbonitrile, or 1-tert-butyl-7-pyrrolidin-1-yl-phenothiazin-3-one.

30. A method of claim 19 , wherein said compound has the structure:

and its pharmaceutically acceptable salts and hydrates, wherein:

R 9 is selected from the group consisting of: halo, cyano, nitro, amino, carboxyl, formyl, sulfo, sulfinyl, sulfeno, sulfenamoyl, sulfonamino, and optionally substituted loweralkyl, loweralkylcarbonyloxy, arylcarbonyloxy, heteroarylcarbonyloxy, cycloalkylcarbonyloxy, cycloheteroalkylcarbonyloxy, aralkycarbonyloxy, heteroaralkylcarbonyloxy, (cycloalkyl)alkylcarbonyloxy, (cycloheteroalkyl)alkylcarbonyloxy, loweralkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, cycloalkycarbonyl, cycloheteroalkycarbonyl, aralkycarbonyl, heteroaralkylcarbonyl, (cycloalkyl)alkylcarbonyl, (cycloheteroalkyl)alkylcarbonyl, loweralkylaminocarbonyl, arylaminocarbonyl, aralkylaminocarbonyl, heteroarylaminocarbonyl, heteroaralkylaminocarbonyl, loweralkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, cycloalkylcarbonylamino, cycloheteroalkylcarbonylamino, aralkylcarbonylamino, heteroaralkylcarbonylamino, (cycloalkyl)alkylcarbonylamino, (cycloheteroalkyl)alkylcarbonylamino, diloweralkylamino, arylamino, diarylamino, aralkylamino, diaralkylamino, heteroarylamino, diheteroarylamino, heteroaralkylamino, diheteroaralkylamino, loweralkylsulfonyl, arylsulfonyl, heteroarylsulfonyl, cycloalkylsulfonyl, loweralkylsulfonyldioxy, arylsulfonyldioxy, heteroarylsulfonyldioxy, loweralkylsulfo, arylsulfo, heteroarylsulfo, cycloalkylsulfo, loweralkylsulfinyl, arylsulfinyl, heteroarylsulfinyl, cycloalkylsulfinyl, loweralkylsulfeno, arylsulfeno, heteroarylsulfeno, cycloalkylsulfeno, loweralkylsulfoamino, arylsulfoamino, heteroarylsulfoamino, cycloalkylsulfoamino, sulfonaloweralkylcarbonylsulfenamoyl, arylcarbonylsulfenamoyl, heteroarylcarbonylsulfenamoyl, cycloalkylcarbonylsulfenamoyl, cycloheteroalkylcarbonylsulfenamoyl, aralkylcarbonylsulfenamoyl, heteroaralkylcarbonylsulfenamoyl, (cycloalkyl)alkylcarbonylsulfenamoyl, (cycloheteroalkyl)alkylcarbonylsulfenamoyl, diloweralkylsulfenamoyl, arylsulfenamoyl, diarylsulfenamoyl, aralkylsulfenamoyl, diaralkylsulfenamoyl, heteroarylsulfenamoyl, diheteroarylsulfenamoyl, heteroaralkylsulfenamoyl, diheteroaralkylsulfenamoyl, loweralkylcarbonylsulfinamoyl, arylcarbonylsulfinamoyl, heteroarylcarbonylsulfinamoyl, cycloalkylcarbonylsulfinamoyl, cycloheteroalkylcarbonylsulfinamoyl, aralkylcarbonylsulfinamoyl, heteroaralkylcarbonylsulfinamoyl, (cycloalkyl)alkylcarbonylsulfinamoyl, (cycloheteroalkyl)alkylcarbonylsulfinamoyl, diloweralkylsulfinamoyl, arylsulfinamoyl, diarylsulfinamoyl, aralkylsulfinamoyl, diaralkylsulfinamoyl, heteroarylsulfinamoyl, diheteroarylsulfinamoyl, heteroaralkylsulfinamoyl, diheteroaralkylsulfinamoyl, loweralkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, cycloalkyloxycarbonyl, cycloheteroalkyloxycarbonyl, aralyoxycarbonyloxloxycarbonyl, heteroaralkyloxycarbonyl, (cycloalkyl)alkyloxycarbonyl, (cycloheteroalkyl)alkyloxycarbonyl, iminoloweralkyl, iminocycloalkyl, iminocycloheteroalkyl, iminoaralkyl, iminoheteroaralkyl, (cycloalkyl)iminoalkyl, and (cycloheteroalkyl)iminoalkyl;

R 1 , R 2 , R 4 , R 5 , and R 8 are selected independently from the group consisting of: hydrogen, halo, cyano, nitro, amino, carboxyl, formyl, sulfo, sulfinyl, sulfeno, sulfenamoyl, sulfonamino, and optionally substituted loweralkyl, loweralkylcarbonyloxy, arylcarbonyloxy, heteroarylcarbonyloxy, cycloalkylcarbonyloxy, cycloheteroalkylcarbonyloxy, aralkycarbonyloxy, heteroaralkylcarbonyloxy, (cycloalkyl)alkylcarbonyloxy, (cycloheteroalkyl)alkylcarbonyloxy, loweralkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, cycloalkycarbonyl, cycloheteroalkycarbonyl, aralkycarbonyl, heteroaralkylcarbonyl, (cycloalkyl)alkylcarbonyl, (cycloheteroalkyl)alkylcarbonyl, loweralkylaminocarbonyl, arylaminocarbonyl, aralkylaminocarbonyl, heteroarylaminocarbonyl, heteroaralkylaminocarbonyl, loweralkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, cycloalkylcarbonylamino, cycloheteroalkylcarbonylamino, aralkylcarbonylamino, heteroaralkylcarbonylamino, (cycloalkyl)alkylcarbonylamino, (cycloheteroalkyl)alkylcarbonylamino, diloweralkylamino, arylamino, diarylamino, aralkylamino, diaralkylamino, heteroarylamino, diheteroarylamino, heteroaralkylamino, diheteroaralkylamino, loweralkylsulfonyl, arylsulfonyl, heteroarylsulfonyl, cycloalkylsulfonyl, loweralkylsulfonyldioxy, arylsulfonyldioxy, heteroarylsulfonyldioxy, loweralkylsulfo, arylsulfo, heteroarylsulfo, cycloalkylsulfo, loweralkylsulfinyl, arylsulfinyl, heteroarylsulfinyl, cycloalkylsulfinyl, loweralkylsulfeno, arylsulfeno, heteroarylsulfeno, cycloalkylsulfeno, loweralkylsulfoamino, arylsulfoamino, heteroarylsulfoamino, cycloalkylsulfoamino, sulfonaloweralkylcarbonylsulfenamoyl, arylcarbonylsulfenamoyl, heteroarylcarbonylsulfenamoyl, cycloalkylcarbonylsulfenamoyl, cycloheteroalkylcarbonylsulfenamoyl, aralkylcarbonylsulfenamoyl, heteroaralkylcarbonylsulfenamoyl, (cycloalkyl)alkylcarbonylsulfenamoyl, (cycloheteroalkyl)alkylcarbonylsulfenamoyl, diloweralkylsulfenamoyl, arylsulfenamoyl, diarylsulfenamoyl, aralkylsulfenamoyl, diaralkylsulfenamoyl, heteroarylsulfenamoyl, diheteroarylsulfenamoyl, heteroaralkylsulfenamoyl, diheteroaralkylsulfenamoyl, loweralkylcarbonylsulfinamoyl, arylcarbonylsulfinamoyl, heteroarylcarbonylsulfinamoyl, cycloalkylcarbonylsulfinamoyl, cycloheteroalkylcarbonylsulfinamoyl, aralkylcarbonylsulfinamoyl, heteroaralkylcarbonylsulfinamoyl, (cycloalkyl)alkylcarbonylsulfinamoyl, (cycloheteroalkyl)alkylcarbonylsulfinamoyl, diloweralkylsulfinamoyl, arylsulfinamoyl, diarylsulfinamoyl, aralkylsulfinamoyl, diaralkylsulfinamoyl, heteroarylsulfinamoyl, diheteroarylsulfinamoyl, heteroaralkylsulfinamoyl, diheteroaralkylsulfinamoyl, loweralkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, cycloalkyloxycarbonyl, cycloheteroalkyloxycarbonyl, aralyoxycarbonyloxloxycarbonyl, heteroaralkyloxycarbonyl, (cycloalkyl)alkyloxycarbonyl, (cycloheteroalkyl)alkyloxycarbonyl, iminoloweralkyl, iminocycloalkyl, iminocycloheteroalkyl, iminoaralkyl, iminoheteroaralkyl, (cycloalkyl)iminoalkyl, and (cycloheteroalkyl)iminoalkyl;

R 3 is selected from the group consisting of: halo, oxo, imino, iminoloweralkyl, iminocycloalkyl, iminocycloheteroalkyl, iminoaralkyl, iminoheteroaralkyl, (cycloalkyl)iminoalkyl, and (cycloheteroalkyl)iminoalkyl; and

R 6 and R 7 are selected independently from the group consisting of: hydrogen and optionally substituted loweralkyl, loweralkyloxyloweralkyl, aminoloweralkyl, loweralkylaminoloweralkyl, diloweralkylaminoloweralkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, arylcarbonyl, alkylcarbonyl, aralkylcarbonyl, heteroarylcarbonyl, and heteroaralkylcarbonyl; in addition, R 6 and R 7 , together with the nitrogen atom to which each is attached, can form an optionally substituted 4-, 5-, 6-, or 7-membered ring

wherein said optionally substituted is with a group which is hydrooxyl, nitro, amino, imino, cyano, halo, amidino, oxo, oxamidino, methoxamidino, imidino, guanidino, sulfonamido, carboxyl, formyl, lower alkyl, haloloweralkyl, loweralkoxy, haloloweralkoxy, lower alkoxyalkyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heteroarylcarbonyl, heteroaralkylcarbonyl, aminoalkyl, or cyanoalkyl.

31. A method of claim 19 , wherein said viral disease is selected from the group consisting of wherein said viral disease is selected from the group consisting of HCV, HIV, influenza, Ebola virus, Marburg virus, Dengue virus, Venezuelean equine encephalitis, Chikungunya virus, and West Nile virus.

32. A method of claim 19 , wherein said viral disease is HIV.

33. A method of claim 19 , wherein said viral disease is influenza.

34. A compound of claim 1 , wherein said R 6 and R 7 , together with the nitrogen atom to which each is attached, can form an optionally substituted cycloheteroalkyl ring.

35. A compound of claim 1 , wherein said R 6 and R 7 , together with the nitrogen atom to which each is attached, can form an optionally substituted cycloalkylamino ring.

36. A compound of claim 1 , wherein said R 6 and R 7 , together with the nitrogen atom to which each is attached, can form an optionally substituted cycloheteroalkylamino ring.

37. A compound of claim 1 , wherein said R 6 and R 7 , together with the nitrogen atom to which each is attached, can form an optionally substituted pyrrolidinyl, piperidyl, morpholinyl, piperazinyl, azetidinyl, quinuclidinyl, or azepanyl.

38. A method of claim 19 , wherein said R 6 and R 7 , together with the nitrogen atom to which each is attached, can form an optionally substituted cycloheteroalkyl ring.

39. A method of claim 19 , wherein said R 6 and R 7 , together with the nitrogen atom to which each is attached, can form an optionally substituted cycloalkylamino ring.

40. A method of claim 19 , wherein said R 6 and R 7 , together with the nitrogen atom to which each is attached, can form an optionally substituted cycloheteroalkylamino ring.

41. A method of claim 19 , wherein said R 6 and R 7 , together with the nitrogen atom to which each is attached, can form an optionally substituted pyrrolidinyl, piperidyl, morpholinyl, piperazinyl, azetidinyl, quinuclidinyl, or azepanyl.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 16, 2012
From: HURT, CLARENCE R.; FREEMAN, BEVERLY; LINGAPPA, VISHWANATH; ATUEGBU, ANDY; KITYAGORODORSKYY, ANATOLIY
To: PROSETTA ANTIVIRAL INC.
Reel/Frame 028053/0828 →
Continuity (8)
Continuation In Part 13099006 · May 2, 2011
Continuation In Part 13316423 · Dec 9, 2011
Provisional Application 61453571 · Mar 17, 2011
Provisional Application 61468614 · Mar 29, 2011
Provisional Application 61477203 · Apr 20, 2011
Provisional Application 61479351 · Apr 26, 2011
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