Abstract: A condensed heterocyclic compound has a sepiapterin reductase inhibitory action and is particularly useful for treatment of a pain. The condensed heterocyclic compound represented by Formula (I) below (R1 represents a hydrocarbon group or the like; R2 and R3 represent a hydrogen atom or the like; R4, X, and Y represent defined substituents), a tautomer or a pharmaceutically acceptable salt of the compound, or a solvate of any of these.
Type:
Application
Filed:
April 13, 2021
Publication date:
March 21, 2024
Applicants:
NISSAN CHEMICAL CORPORATION, SHIONOGI & CO., LTD.
Abstract: Provided are a compound having serotonin 5-HT2A receptor antagonism and/or inverse agonism, a pharmaceutically acceptable salt thereof, and a composition for serotonin 5-HT2A receptor antagonism and/or inverse agonism comprising them.
Abstract: The present invention provides a solid dosage form having good stability, suspensibility in water and fluidity by preparing a solid dosage form containing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a stabilizer, a sugar alcohol and/or a sugar, a water-soluble polymer and an inorganic substance.
Abstract: The present invention relates to a method for preventing transmission of influenza, wherein said method comprises administering an effective amount of a compound to a patient having an influenza virus infection, herein referred to as “index patient”, wherein the compound has one of the formulae (I) and (II), or its pharmaceutically acceptable salt. The compound to be used in the present invention reduces infectivity of the influenza virus of the index patient, and therefore, reduces the risk of the index patient to trigger an influenza epidemic or an influenza pandemic as compared to a control patient.
Type:
Grant
Filed:
December 23, 2021
Date of Patent:
February 27, 2024
Assignees:
Shionogi & Co., Ltd.
Inventors:
Takeshi Noshi, Takahiro Noda, Ryu Yoshida, Takao Shishido, Kaoru Baba, Aeron C. Hurt, Leo Yi Yang Lee, Steffen Wildum, Klaus Kuhlbusch, Barry Clinch, Jan Michal Nebesky, Annabelle Lemenuel, Wendy S. Barclay, Jean-Eric Charoin, Yoshinori Ando
Abstract: Novel compounds having D3 receptor antagonistic activity are provided. A compound represented by formula (I): wherein ring A is a heterocycle, X1 is each independently CR4aR4b, X2 is each independently CR4cR4d, Y1 and Y2 are each independently a carbon atom or a nitrogen atom, L is —N(R6)—C(?O)— or the like, W is cyclyl or the like, R2 and R3 are each independently substituted or unsubstituted alkyl or the like, R1a, R1b, R4a to R4d, and R6 are each independently hydrogen atoms or the like, p is 1 or 2, q is an integer of 1 to 3, n is an integer of 1 to 4, s is an integer of 0 to 4, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 21, 2022
Date of Patent:
February 13, 2024
Assignee:
SHIONOGI & CO., LTD.
Inventors:
Hiroyuki Tobinaga, Koji Masuda, Masanao Inagaki, Manami Masuda
Abstract: Provided is a pharmaceutical composition for treating chronic cough, which has substantially no side effects of taste disturbance. A pharmaceutical composition for treating chronic cough, comprising a compound represented by Formula (I): or a pharmaceutically acceptable salt thereof.
Abstract: The present invention provides a compound represented by formula (I): wherein the dashed line indicates the presence or absence of a bond; R1 is carboxy or the like; L is substituted or unsubstituted non-aromatic carbocyclyldiyl or the like; R2 is substituted or unsubstituted alkyl; R3 is a hydrogen atom or the like; X is ?CRX— or ?N—; Y is ?CRY— or ?N—; U is —CRU? or —N?; V is —CRV? or —N?; W is ?CRW— or ?N—; ZA is —C? or —N—; ZB is —CR5R6— or the like; ZC is —CR7R8— or the like; RX, RY, RV and RW are each independently a hydrogen atom or the like; RU is a hydrogen atom or the like; R5 and R6 are each independently a hydrogen atom or the like; R7 and R8 are each independently a hydrogen atom or the like; R4 is substituted or unsubstituted alkyloxy or the like, or a pharmaceutically acceptable salt thereof, having an antiviral activity; and a pharmaceutical composition comprising the same.
Abstract: The present invention provides a compound exhibiting coronavirus 3 CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same. Furthermore, the present invention provides a crystalline form useful as an active pharmaceutical ingredient, and a pharmaceutical composition comprising the same. A compound represented by Formula: or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 29, 2022
Date of Patent:
November 14, 2023
Assignees:
SHIONOGI & CO., LTD., NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY
Abstract: The present invention provides a process for preparing a compound of the formula (II): wherein R2 is unsubstituted alkyl, characterized by reacting a compound of the formula (I): wherein R1 is hydrogen or a protecting group other than unsubstituted alkyl, with a compound of the formula: R2—OH, wherein R2 is as defined above, in the presence of a sodium salt and/or a magnesium salt.
Abstract: By administering a liposome formulation in which an antibacterial agent is bound to a liposome, in particular, a lipid-soluble side chain of the antibacterial agent is bound to a lipid of the liposome, and the antibacterial agent extends outward from a surface of the liposome, it is possible to provide a liposome formulation in which blood retention of an active ingredient is increased, an amount of the active ingredient taken by a reticuloendothelial system such as a liver is reduced, an amount of the active ingredient transferred into a kidney is reduced, and antibacterial activity can also be increased with little resistance.
Abstract: An estimation system obtains brain wave measurement data and functional magnetic resonance imaging measurement data simultaneously measured from a subject, calculates first functional connectivity for each channel combination based on correlation between channels included in the brain wave measurement data, calculates second functional connectivity for each brain network based on correlation between regions of interest included in the functional magnetic resonance imaging measurement data, calculates a disorder-likelihood label by calculating a score representing disorder-likelihood to be estimated with the use of a plurality of second functional connectivities, and determines an estimation model for estimating disorder-likelihood based on prescribed first functional connectivity by machine learning using the first functional connectivity for each channel combination and the disorder-likelihood label.
Type:
Application
Filed:
July 1, 2021
Publication date:
September 21, 2023
Applicants:
ADVANCED TELECOMMUNICATIONS RESEARCH INSTITUTE INTERNATIONAL, SHIONOGI & CO., LTD.
Abstract: The present invention provides the following compounds having anti-viral activity. A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is CR4AR4B, S or O; the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A1, is 1 or 2; R1A and R1B are each independently hydrogen, halogen, alkyl, or the like; R2A and R2B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B are each independently hydrogen, halogen, alkyl, or the like; R4A and R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together to form non-aromatic carbocycle or non-aromatic heterocycle; X is CH2, S or O; R1 is each independently halogen, hydroxy, or the like; m is any integer of 0 to 2; and n is any integer of 1 to 2.
Abstract: There is provided a therapy selection support device that generates a discriminator (identifier) as a diagnostic marker or a classifier as a stratification marker through machine learning on the basis of measurement data on brain activities and that uses the discriminator or the classifier as a biomarker. A therapy selection support system 300a, 300b, 500 includes a clustering device 300b that executes stratification in which the results of measurement of brain functional connectivity correlation values acquired from a plurality of second subjects are divided into a plurality of clusters through a clustering process.
Type:
Application
Filed:
July 15, 2021
Publication date:
September 14, 2023
Applicants:
ADVANCED TELECOMMUNICATIONS RESEARCH INSTITUTE INTERNATIONAL, HIROSHIMA UNIVERSITY, SHIONOGI & CO., LTD.
Abstract: The present invention provides novel aclidinium salt of the formula (I) and a process for the production of the aclidinium salt. wherein R1 is C1-C6 alkyl or C1-C6 alkyloxy; R2 is hydrogen or C1-C6 alkyloxy; R3 is hydrogen, halogen, C1-C6 alkyl or C1-C6 alkyloxy; R4 is hydrogen, C1-C6 alkyloxy, halo C1-C6 alkyloxy or C1-C6 alkylamino; R5 is C1-C3 alkyl; and X? is an anion.
Abstract: The present invention provides a compound represented by Formula (I): wherein ring A is a substituted or unsubstituted heterocycle; ring C is a benzene ring or the like; R1 is halogen or the like; R2a and R2b are each independently hydrogen or the like; R3 is substituted or unsubstituted alkyl or the like; R4 is hydrogen or the like; and n is an integer of 1 to 3.
Abstract: The present invention provides a compound exhibiting coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same. Furthermore, the present invention provides a crystalline form useful as an active pharmaceutical ingredient, and a pharmaceutical composition comprising the same. A compound represented by Formula: , or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
April 29, 2022
Publication date:
July 6, 2023
Applicants:
Shionogi & Co., Ltd., NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY
Abstract: Provided is a pharmaceutical composition for treating and/or preventing fatty liver disease, particularly nonalcoholic fatty liver disease, the pharmaceutical composition having an excellent ACC2-selective inhibitory action and having no side effects such as an increase in plasma triglyceride or a decrease in platelet concentration. A pharmaceutical composition for treating and/or preventing fatty liver disease, the pharmaceutical composition comprising a compound represented by Formula (I): wherein R1 is haloalkyl or non-aromatic carbocyclyl, R2 is a hydrogen atom or halogen, R3 is halogen, ring A is a group represented by the formula: -L1- is —O—(CH2)—, —(CH2)2—, or the like, R4 is alkyl or haloalkyl, and R5 is alkylcarbonyl or carbamoyl, or a pharmaceutically acceptable salt thereof.
Abstract: Provided are a novel compound having an antagonistic activity for the P2X7 receptor, and a pharmaceutical composition having an antagonistic activity for the P2X7 receptor.
Type:
Grant
Filed:
June 16, 2021
Date of Patent:
June 27, 2023
Assignee:
Shionogi & Co., Ltd.
Inventors:
Koji Masuda, Shuichi Sugiyama, Toru Yamada, Eiichi Kojima, Tomoyuki Ogawa, Naotake Kobayashi, Hiroyuki Kai