Hepatitis B Antiviral Agents
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Accused Products
Abstract
The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
57 Citations
69 Claims
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1-46. -46. (canceled)
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47. A compound of Formula II:
- View Dependent Claims (48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69)
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48. The compound of claim 47, or a pharmaceutically acceptable salt thereof;
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wherein ring B is a monocyclic aryl ring; R2 and R5 are independently selected at each occurrence from the group consisting of halo, -(L)m-OR8, -(L)m-N(R8)2, -(L)m-C(═
O)N(R8)2, -(L)m-C(═
O)R9, -(L)mCO2R8, —
C1-C6 alkyl, and —
C1-C6 heteroalkyl;R4 is H; each R6 is independently selected from the group consisting of C1-C6 alkyl, and wherein the alkyl group is optionally substituted with 0-5 substituents selected from R2, or the R6 groups attached to the same N atom are taken together with the N atom to which they are attached to form an optionally substituted C2-C10 heterocycloalkyl ring, wherein the ring optionally comprises a moiety selected from 0, and wherein the heterocycloalkyl ring is optionally substituted with 0-5 substituents selected from R2; each R8 is independently, at each occurrence, H, C1-C6 alkyl; R9 is C3-C10 cycloalkyl or aryl; each occurrence of x and y is independently selected from the group consisting of 0, 1, 2, 3 and 4; and, each occurrence of m is independently 0.
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49. The compound of claim 47, or a pharmaceutically acceptable salt thereof;
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wherein ring B is a monocyclic aryl ring; R2 and R5 are independently selected at each occurrence from the group consisting of halo, -(L)m-OR8, and —
C1-C6 alkyl;R4 is H; each R6 is independently selected from the group consisting of C1-C6 alkyl, and wherein the alkyl group is optionally substituted with 0-5 substituents selected from R2, or the R6 groups attached to the same N atom are taken together with the N atom to which they are attached to form an optionally substituted C2-C10 heterocycloalkyl ring, wherein the ring optionally comprises a moiety selected from 0, and wherein the heterocycloalkyl ring is optionally substituted with 0-5 substituents selected from R2; each R8 is independently, at each occurrence, H, C1-C6 alkyl; each occurrence of x and y is independently selected from the group consisting of 0, 1, 2, 3 and 4; and, each occurrence of m is independently 0.
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50. The compound of claim 47, or a pharmaceutically acceptable salt thereof;
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wherein ring B is a phenyl ring.
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51. The compound of claim 47, or a pharmaceutically acceptable salt thereof;
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wherein the compound of Formula II is selected from;
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52. A composition comprising a compound according to claim 47, or a salt, solvate or N-oxide thereof.
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53. The composition of claim 52, wherein the composition is pharmaceutical and further comprises at least one pharmaceutically acceptable carrier.
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54. A method of treating, eradicating, reducing, slowing, or inhibiting an HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of a compound according to claim 47.
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55. A method of reducing the viral load associated with an HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of a compound according to claim 47.
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56. A method of reducing reoccurrence of an HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of a compound according to according to claim 47.
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57. A method of reducing an adverse physiological impact of an HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of a compound according to claim 47.
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58. A method of inducing remission of hepatic injury from an HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of a compound according to claim 47.
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59. A method of reducing the physiological impact of long-term antiviral therapy for HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of a compound according to claim 47.
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60. A method of prophylactically treating an HBV infection in an individual in need thereof, wherein the individual is afflicted with a latent HBV infection, comprising administering to the individual a therapeutically effective amount according to claim 47.
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61. The method of claim 54, further comprising administering to the individual at least one additional therapeutic agent selected from the group consisting of a HBV polymerase inhibitor, interferon, viral entry inhibitor, viral maturation inhibitor, literature-described capsid assembly modulator, reverse transcriptase inhibitor, a TLR-agonist, and agents of distinct or unknown mechanism, and a combination thereof.
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62. The method of claim 61, wherein the reverse transcriptase inhibitor is at least one of Zidovudine, Didanosine, Zalcitabine, ddA, Stavudine, Lamivudine, Abacavir, Emtricitabine, Entecavir, Apricitabine, Atevirapine, ribavirin, acyclovir, famciclovir, valacyclovir, ganciclovir, valganciclovir, Tenofovir, Adefovir, PMPA, cidofovir, Efavirenz, Nevirapine, Delavirdine, or Etravirine.
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63. The method of claim 61, wherein the TLR-7 agonist is selected from the group consisting of SM360320 (9-benzyl-8-hydroxy-2-(2-methoxy-ethoxy)adenine) and AZD 8848 (methyl[3-({[3-(6-amino-2-butoxy-8-oxo-7,8-dihydro-9H-purin-9-yl)propyl][3-(4-morpholinyl)propyl]amino}methyl)phenyl]acetate).
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64. The method of claim 61, wherein the compound and the at least one additional therapeutic agent are co-formulated.
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65. The method of claim 61, wherein the compound and the at least one additional therapeutic agent are co-administered.
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66. The method of claim 61, wherein administering the compound allows for administering of the at least one additional therapeutic agent at a lower dose or frequency as compared to the administering of the at least one additional therapeutic agent alone that is required to achieve similar results in prophylactically treating an HBV infection in an individual in need thereof.
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67. The method of claim 61, wherein before administering the therapeutically effective amount of the compound of formula (I) the individual is known to be refractory to a compound selected from the group consisting of a HBV polymerase inhibitor, interferon, viral entry inhibitor, viral maturation inhibitor, distinct capsid assembly modulator, antiviral compounds of distinct or unknown mechanism, and combination thereof.
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68. The method of claim 61, wherein the administering of the compound reduces viral load in the individual to a greater extent compared to the administering of a compound selected from the group consisting of a HBV polymerase inhibitor, interferon, viral entry inhibitor, viral maturation inhibitor, distinct capsid assembly modulator, antiviral compounds of distinct or unknown mechanism, and combination thereof.
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69. The method of claim 61, wherein the administering of the compound causes a lower incidence of viral mutation and/or viral resistance than the administering of a compound selected from the group consisting of a HBV polymerase inhibitor, interferon, viral entry inhibitor, viral maturation inhibitor, distinct capsid assembly modulator, antiviral compounds of distinct or unknown mechanism, and combination thereof.
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48. The compound of claim 47, or a pharmaceutically acceptable salt thereof;
Specification
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Current AssigneeNovira Therapeutics, Inc. (Johnson & Johnson)
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Original AssigneeNovira Therapeutics, Inc. (Johnson & Johnson)
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InventorsHartman, George D., Flores, Osvaldo A.
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Granted Patent
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Time in Patent OfficeDays
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Field of Search
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US Class Current1/1
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CPC Class CodesA61K 2300/00 Mixtures or combinations of...A61K 31/167 having the nitrogen of a ca...A61K 31/18 Sulfonamides compounds cont...A61K 31/397 having four-membered rings,...A61K 31/40 having five-membered rings ...A61K 31/4015 having oxo groups directly ...A61K 31/407 condensed with other hetero...A61K 31/445 Non condensed piperidines, ...A61K 31/4453 only substituted in positio...A61K 31/451 having a carbocyclic group ...A61K 31/454 containing a five-membered ...A61K 31/4545 containing a six-membered r...A61K 31/495 having six-membered rings w...A61K 31/496 Non-condensed piperazines c...A61K 31/513 having oxo groups directly ...A61K 31/52 Purines, e.g. adenineA61K 31/522 having oxo groups directly ...A61K 31/536 ortho- or peri-condensed wi...A61K 31/5375 1,4-Oxazines, e.g. morpholineA61K 31/551 having two nitrogen atoms, ...A61K 31/675 : having nitrogen as a ring h...A61K 31/7072 : having two oxo groups direc...A61K 38/21 : Interferons [IFN]A61K 45/06 : Mixtures of active ingredie...A61P 1/16 : for liver or gallbladder di...A61P 31/12 : AntiviralsA61P 31/20 : for DNA virusesA61P 43/00 : Drugs for specific purposes...C07C 211/46 : AnilineC07C 211/48 : N-alkylated aminesC07C 211/50 : with at least two amino gro...C07C 311/46 : Y being a hydrogen or a car...C07D 205/04 : having no double bonds betw...C07D 207/08 : with hydrocarbon radicals, ...C07D 207/09 : Radicals substituted by nit...C07D 207/12 : Oxygen or sulfur atomsC07D 207/14 : Nitrogen atoms not forming ...C07D 207/16 : Carbon atoms having three b...C07D 207/48 : Sulfur atomsC07D 211/22 : by oxygen atomsC07D 211/32 : by oxygen atomsC07D 211/42 : attached in position 3 or 5C07D 211/46 : having a hydrogen atom as t...C07D 211/48 : having an acyclic carbon at...C07D 211/50 : Aroyl radicalC07D 211/52 : having an aryl radical as t...C07D 211/58 : attached in position 4C07D 211/62 : attached in position 4C07D 211/96 : Sulfur atomC07D 213/74 : Amino or imino radicals sub...C07D 213/82 : in position 3C07D 265/30 : not condensed with other ringsC07D 265/32 : with oxygen atoms directly ...C07D 295/195 : Radicals derived from nitro...C07D 295/26 : Sulfur atomsC07D 401/06 : linked by a carbon chain co...C07D 401/12 : linked by a chain containin...