Abstract: The present invention is directed to N-[(2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide of the formula: or a pharmaceutically acceptable salt or stereoisomer thereof, and pharmaceutical compositions comprising the same. The present invention has HIV integrase inhibitory activity.
Type:
Grant
Filed:
May 1, 2019
Date of Patent:
February 23, 2021
Assignees:
SHINOGI & CO., LTD., VIIV HEALTHCARE COMPANY
Inventors:
Brian A. Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
Abstract: The invention relates to compounds of Formula (I), salts thereof, combinations, pharmaceutical compositions thereof, as well as therapeutic methods of treatment and prevention.
Type:
Application
Filed:
October 5, 2020
Publication date:
January 14, 2021
Applicants:
GlaxoSmithKline Intellectual Property Development Limited, The University of North Carolina at Chapel Hill, ViiV Healthcare Company
Inventors:
Martha DE LA ROSA, Richard M. DUNHAM, David MARGOLIS, Vincent Wing-Fai TAI, Jun TANG
Abstract: The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
Type:
Application
Filed:
March 6, 2019
Publication date:
December 31, 2020
Applicants:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO. 2) LIMITED, VIIV HEALTHCARE COMPANY
Inventors:
Martha Alicia DE LA ROSA, John Franklin MILLER, David TEMELKOFF, Emile Johann VELTHUISEN
Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
Type:
Application
Filed:
July 9, 2020
Publication date:
October 29, 2020
Applicants:
Shionogi & Co., Ltd., ViiV Healthcare Company
Inventors:
Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
Abstract: The invention relates a compound of the formula: a pharmaceutically acceptable salt thereof, compositions thereof, and methods of therapeutic treatment using the same.
Type:
Application
Filed:
June 10, 2020
Publication date:
September 24, 2020
Applicants:
GlaxoSmithKline Intellectual Property Development Limited, The University of North Carolina at Chapel Hill, ViiV Healthcare Company
Inventors:
Richard M DUNHAM, David MARGOLIS, Vincent Wing-Fai TAI, Jun TANG
Abstract: Methods for treating HIV or AIDS in a human are provided using two drug regimens comprising a bictegravir and rilpivirine, as well as compositions containing such compounds.
Abstract: The present invention relates to combinations of compounds comprising HIV integrase inhibitors and other therapeutic agents. Such combinations are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
Abstract: The present invention is to provide a novol compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X? is a single bond, a hetoro atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound; including e.g., a tricyclic or tetracyclic compound.
Type:
Application
Filed:
May 1, 2019
Publication date:
September 19, 2019
Applicants:
Shionogi & Co., Ltd., ViiV Healthcare Company
Inventors:
Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X? is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylrene in which the hetero atom group may intervene; R2 is optionally substituted aryl; Ra is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4and Z2 part taken together forms a ring, to forma polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
Type:
Application
Filed:
January 10, 2019
Publication date:
May 23, 2019
Applicants:
ViiV Healthcare Company
Inventors:
Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
Abstract: The present invention relates to intermediates in the preparation of carbamoylpyridone derivatives, such as compounds of formula (III) and/or compounds of formula (IV): wherein R is alkyl, aryl or benzyl.
Type:
Grant
Filed:
February 28, 2018
Date of Patent:
January 8, 2019
Assignee:
ViiV Healthcare Company
Inventors:
Steven N. Goodman, Huan Wang, Douglas Mans, Matthew Kowalski
Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
Type:
Application
Filed:
September 7, 2017
Publication date:
December 28, 2017
Applicants:
Shionogi & Co., Ltd., ViiV Healthcare Company
Inventors:
Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
Type:
Application
Filed:
May 18, 2017
Publication date:
September 21, 2017
Applicants:
Shionogi & Co., Ltd., ViiV Healthcare Company
Inventors:
Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
Type:
Application
Filed:
May 18, 2017
Publication date:
September 14, 2017
Applicants:
ViiV Healthcare Company
Inventors:
Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylane or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound; including e.g., a tricyclic or tetracyclic compound.
Type:
Application
Filed:
May 17, 2017
Publication date:
September 7, 2017
Applicants:
Shionogi & Co., Ltd., ViiV Healthcare Company
Inventors:
Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
Type:
Application
Filed:
April 27, 2017
Publication date:
August 10, 2017
Applicants:
Shionogi & Co., Ltd., ViiV Healthcare Company
Inventors:
Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA