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1. (WO2010072598) HETEROCYCLIC ANTIVIRAL COMPOUNDS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/072598 International Application No.: PCT/EP2009/067028
Publication Date: 01.07.2010 International Filing Date: 14.12.2009
Chapter 2 Demand Filed: 31.08.2010
IPC:
C07D 405/04 (2006.01) ,C07D 237/14 (2006.01) ,C07D 239/36 (2006.01) ,C07D 239/52 (2006.01) ,C07D 239/54 (2006.01) ,C07D 241/18 (2006.01) ,C07D 253/07 (2006.01) ,A61K 31/4965 (2006.01) ,A61K 31/497 (2006.01) ,A61K 31/50 (2006.01) ,A61K 31/513 (2006.01) ,A61K 31/53 (2006.01) ,A61P 31/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
237
Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
02
not condensed with other rings
06
having three double bonds between ring members or between ring members and non-ring members
10
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
14
Oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
32
One oxygen, sulfur or nitrogen atom
34
One oxygen atom
36
as doubly bound oxygen atom or as unsubstituted hydroxy radical
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
52
Two oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
52
Two oxygen atoms
54
as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
241
Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
02
not condensed with other rings
10
having three double bonds between ring members or between ring members and non-ring members
14
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
18
Oxygen or sulfur atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
253
Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/166
02
not condensed with other rings
06
1,2,4-Triazines
065
having three double bonds between ring members or between ring members and non-ring members
07
with hetero atoms, or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4965
Non-condensed pyrazines
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4965
Non-condensed pyrazines
497
containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
50
Pyridazines; Hydrogenated pyridazines
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
513
having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
53
having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
Applicants:
F. HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124 CH-4070 Basel, CH (AllExceptUS)
LI, Jim [US/US]; US (UsOnly)
SCHOENFELD, Ryan, Craig [US/US]; US (UsOnly)
STEINER, Sandra [CH/US]; US (UsOnly)
TALAMAS, Francisco, Xavier [US/US]; US (UsOnly)
Inventors:
LI, Jim; US
SCHOENFELD, Ryan, Craig; US
STEINER, Sandra; US
TALAMAS, Francisco, Xavier; US
Agent:
KJELLSAA-BERGER, Hanny; Grenzacherstrasse 124 CH-4070 Basel, CH
Priority Data:
61/139,98222.12.2008US
61/156,44227.02.2009US
Title (EN) HETEROCYCLIC ANTIVIRAL COMPOUNDS
(FR) COMPOSÉS ANTIVIRAUX HÉTÉROCYCLIQUES
Abstract:
(EN) Compounds having the formula (I) wherein A, R1, R2, R3, R4a, R4b, R4c, R5, R6, R7a, R7b, Ar1, Rc, Rd, Re, Rf, X, n and p are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
(FR) La présente invention concerne des composés de formule (I) dans laquelle A, R1, R2, R3, R4a, R4b, R4c, R5, R6, R7a, R7b, Ar1, Rc, Rd, Re, Rf, X, n et p sont tels que définis dans le présent document, qui sont des inhibiteurs de la polymérase NS5b du virus de l'hépatite C. La présente invention concerne également des compositions et des procédés de traitement d'une infection par le HCV et d'inhibition de la réplication du HCV.
front page image
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
IL213102MXMX/a/2011/006647SG172778EP2379534JP2012513434CN102256968
CA2745865KR1020110094352AU2009331660IN4397/CHENP/2011