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:
March 31, 2016
Publication date:
July 21, 2016
Applicants:
Shionogi & Co., Ltd., ViiV Healthcare Company
Inventors:
Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
Abstract: The present invention is related to a compound represented by formula (I) wherein —X— is —NH— or —S—; —Z— is —O— or —S—; R3, R5 and R6 are each independently a hydrogen atom, substituted or unsubstituted alkyl, or the like; R7 is a cyano, substituted or unsubstituted amino, or the like; R7? is each independently a halogen; b is 0 or 1; or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising thereof.
Abstract: Stable crystalline forms of a compound represented by the formula (IA): an acid addition salt, and/or a solvate thereof are provided by the present invention. Said crystalline forms are extremely useful as materials for preparing medicines. Novel processes for preparing 6,7-unsaturated-7-carbamoyl morphinan derivatives are also provided by the present invention.
Type:
Application
Filed:
March 15, 2016
Publication date:
July 7, 2016
Applicant:
Shionogi & Co., Ltd.
Inventors:
Masanao INAGAKI, Nobuhiro HAGA, Shinichi ODA
Abstract: The invention is a process for the preparation of a compound of the following formula (I): wherein R is —CHO, —CH(OH)2 or —CH(OH)(OR4); P1 is H or a hydroxyl protecting group; P3 is H or a carboxy protecting group; R3 is H, halogen, hydroxy, optionally substituted lower alkyl, optionally substituted cycloalkyl, etc.; Rx is H, halogen or R2—X—NR1—C(O)—; etc. as defined in the specification. The compounds are useful as intermediates in synthesizing compounds having HIV integrase inhibitory activity.
Type:
Grant
Filed:
November 10, 2015
Date of Patent:
June 14, 2016
Assignees:
SHIONOGI & CO., LTD., ViiV HEALTHCARE COMPANY
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:
January 20, 2016
Publication date:
May 19, 2016
Applicants:
Shionogi & Co., Ltd., ViiV Healthcare Company
Inventors:
Brian Alvin Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
Abstract: A compound having TRPV4 inhibitory activity or a pharmaceutically acceptable salt thereof is provided. The present invention is related to a compound represented by the formula (I), wherein R1a is substituted or unsubstituted alkyl or the like; R1b is hydrogen or substituted or unsubstituted alkyl; R1c is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted nonaromatic heterocyclic group or the like; -L- is —C(=0)—NR2? or the like; X is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or the like, or a pharmaceutically acceptable salt thereof.
Abstract: The present invention relates to cephalosporin antibacterial compounds of Formula (I): or corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods for bacterial infections, especially those caused by gram-negative bacteria.
Type:
Grant
Filed:
October 4, 2012
Date of Patent:
May 17, 2016
Assignees:
GLAXO GROUP LIMITED, SHIONOGI & CO., LTD
Inventors:
Xiangmin Liao, Neil David Pearson, Israil Pendrak, Masayuki Sano
Abstract: The present invention provides a novel compound which has a wide antimicrobial spectrum, and in particular exhibits potent antimicrobial activity against beta-lactamase producing Gram negative bacteria. Specifically, the present invention provides a compound of the formula (I): wherein each symbol is as defined in the specification, or an amino-protected compound when the amino group is present on the ring in the 7-side chain, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.
Abstract: Stable crystalline forms of a compound represented by the formula (IA): an acid addition salt, and/or a solvate thereof are provided by the present invention. Said crystalline forms are extremely useful as materials for preparing medicines. Novel processes for preparing 6,7-unsaturated-7-carbamoyl morphinan derivatives are also provided by the present invention.
Abstract: The present invention provides compounds shown by the formula: wherein Y1 is CR6 or N, Y2 is CR7 or N, Y3 is CR8 or N, R6, R7 and R8 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like, Bx is a nucleic acid base moiety, Z1 and Z2 are each independently, a hydrogen atom, a hydroxyl protecting group or a reactive phosphorus group, R1 to R5 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like, and n is an integer of 0 to 3, or salts thereof, that are novel nucleosides or nucleotides that can be useful as materials for synthesizing nucleic acid pharmaceuticals.
Abstract: Stable crystalline forms of a compound represented by the formula (IA): an acid addition salt, and/or a solvate thereof are provided by the present invention. Said crystalline forms are extremely useful as materials for preparing medicines. Novel processes for preparing 6,7-unsaturated-7-carbamoyl morphinan derivatives are also provided by the present invention.
Type:
Grant
Filed:
August 4, 2015
Date of Patent:
March 29, 2016
Assignee:
Shionogi & Co., Ltd.
Inventors:
Masanao Inagaki, Kenji Morimoto, Nobuhiro Haga, Shinichi Oda
Abstract: Provided is a monoclonal antibody or a fragment thereof that selectively inhibits enzyme activity of EL and pharmaceutical compositions containing the same as an active ingredient useful for the treatment of arteriosclerosis or metabolic syndrome.
Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof wherein A represents a group represented by one of formulae (i)-(iii); B represents a group represented by formula (v) or (vi); and E represents a substituted or unsubstituted heterocyclic group having a cationic nitrogen atom.
Type:
Grant
Filed:
October 3, 2012
Date of Patent:
March 22, 2016
Assignee:
SHIONOGI & CO., LTD
Inventors:
Kenji Yamawaki, Masayuki Sano, Jun Sato
Abstract: The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-? proteins. A compound of the formula (I): wherein R1, R2 a, R2 b, R3, R4 a, R4 b, ring A and the dashed lines are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
Abstract: The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound.
Abstract: A synthesis approach providing an early ring attachment via a bromination to compound l-l yielding compound II-Il, whereby a final product such as AA can be synthesized. In particular, the 2,4-difluorophenyl-containing sidechain is attached before creation of the additional ring Q.
Abstract: The disclosure relates to Compounds of Formula (I) and pharmaceutically acceptable derivatives thereof, where R1, R4, R8, R9, and m are as defined herein, compositions comprising an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, pain associated with osteoarthritis, osteoarthritis, UI, an ulcer, IBD, and IBS, comprising administering to an animal in need thereof an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof.
Abstract: The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid ? protein, for example, a compound represented by the formula: wherein Ry is halogeno lower alkyl; ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group, R1 is optionally substituted lower alkyl or the like, R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or the like, R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy, optionally substituted lower alkyl or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof.
Abstract: The present invention is directed to a class of substituted pyrido[1?2?:4,5]pyrazino[1,2-a]-pyrimidines useful as intermediates in the production of anti-HIV agents. The compounds have the formula (I-24b): wherein Re is one or two halogen; Rz is C1-8alkyl; Rz is hydrogen, C3-6cycloalkyl, heterocyclyl, or C1-8alkyl optionally substituted with hydroxy, C3-6cycloalkyl, alkoxy, heterocyclyl, heteroaryl, C6-14aryl, or amino, wherein said amino may be optionally substituted with —C(O)C1-8alkyl or C1-8alkyl; and P1 is C6-14arylC1-8alkyl; or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 30, 2015
Date of Patent:
March 1, 2016
Assignees:
Shionogi & Co., Ltd., ViiV Healthcare Company
Inventors:
Brian A. Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
Abstract: A method for detecting a colorectal cancer, including the steps of measuring an amount of exosomes expressing CD147 in a body fluid sample derived from a test individual with an anti-CD147 monoclonal antibody or a fragment thereof; and comparing a signal intensity of exosomes in the step with a signal intensity in a control individual, wherein a case where the signal intensity in the test individual is found to be stronger than the signal intensity in the control individual serves as an index of the presence of the colorectal cancer. According to the method of the present invention, whether or not a sample provider has a high possibility of developing a colorectal cancer can be judged. Therefore, the method is useful because the sample provider can take a means of inhibiting the progression of cancer.
Type:
Application
Filed:
March 19, 2014
Publication date:
February 18, 2016
Applicants:
THEORIA SCIENCE INC., SHIONOGI & CO., LTD.