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.
Abstract: A method for the production of the present disclosure comprises: a) a step of agitating a mixture containing a material to be ground, beads and a dispersion medium in a bead mill; and b) a step of adjusting the pH of the mixture. This method reduces a contamination caused by grinding process using a bead mill.
Abstract: The present invention provides a compound represented by a following formula. A compound represented by, wherein R1 is hydrogen, hydroxy, or the like; R2a and R2b may be taken together with an adjacent carbon atom to form ring B, ring B is a substituted or unsubstituted non-aromatic carbocycle or a substituted or unsubstituted non-aromatic heterocycle; R3a is hydrogen, halogen, hydroxy, or the like; R3b is hydrogen, halogen, hydroxy, or the like; R4a is a group represented by formula: L3 is a single bond or substituted or unsubstituted alkylene, R7 is hydrogen, halogen, hydroxy, or the like, and R4b is halogen, cyano, carboxy, or the like, or its pharmaceutically acceptable salt.
Abstract: The present invention provides a particle comprising pirfenidone and a lipid, particularly magnesium stearate, and having a mean particle diameter of 5 ?m or less, and a powder formulation comprising the particle and a carrier.
Abstract: The present invention provides a pharmaceutical composition containing the following compound having antiviral action: wherein each of the symbols is defined in the specification.
Abstract: The present invention provides industrially suitable processes for preparing intermediates in the production of substituted polycyclic pyridone derivatives having a cap-dependent endonuclease inhibitory activity. In the process as shown below, wherein each symbol is as defined in the specification, an optically active substituted tricyclic pyridone derivative of the formula (VII) is obtained in high yield and high enantioselectivity by subjecting a compound of the formula (III) or (VI) to intramolecular cyclization with controlling stereochemistry to obtain a compound of the formula (IV) having a removable functional group on an asymmetric carbon, and then removing the functional group thereof.
Abstract: The present invention provides the compound represented by the following formula (I): wherein a moiety represented by formula: or the like. The symbols are defined in the specification. The compounds of the present invention have MGAT2 inhibitory activity, and are useful as a medicine for treatment of MGAT2-associated diseases including obesity, metabolic syndrome, hyperlipidemia, hypertriglyceridemia, hyper-VLDL-triglyceridemia, hyperfattyacidemia, diabetes mellitus, and arteriosclerosis.
Abstract: Substituted 1,2,3,3a,4,5,7,9,13,13a-decahydropyrido[1?,2?:4,5]pyrazino[1,2-a]pyrrolo[1,2-c]pyrimidines having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a pharmaceutical composition containing the same, particularly an anti-HIV pharmaceutical composition.
Type:
Grant
Filed:
July 9, 2020
Date of Patent:
March 8, 2022
Assignees:
SHIONOGI & CO., LTD., VIIV HEALTHCARE COMPANY
Inventors:
Brian A. Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
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: 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 the compound represented by the following formula (I): wherein a moiety represented by formula: or the like. The symbols are defined in the specification. The compounds of the present invention have MGAT2 inhibitory activity, and are useful as a medicine for treatment of MGAT2-associated diseases including obesity, metabolic syndrome, hyperlipidemia, hypertriglyceridemia, hyper-VLDL-triglyceridemia, hyperfattyacidemia, diabetes mellitus, and arteriosclerosis.
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:
Application
Filed:
June 16, 2021
Publication date:
October 14, 2021
Applicant:
Shionogi & Co., Ltd.
Inventors:
Koji MASUDA, Shuichi SUGIYAMA, Toru YAMADA, Eiichi KOJIMA, Tomoyuki OGAWA, Naotake KOBAYASHI, Hiroyuki KAI
Abstract: Provided is a humanized monoclonal antibody or an antibody fragment thereof that selectively inhibits the enzymatic activity of vascular endothelial lipase and pharmaceutical compositions containing the same as an active ingredient useful for the treatment of arteriosclerosis or metabolic syndrome.
Abstract: The present invention offers the manufacturing method of the solid formulation wherein the standard deviation of the active ingredient content in the solid formulation becomes 5% or less by mixing the excipients which have a median particle size of 15 or more times, preferably 20 times or more to the median particle size of an active ingredient.
Abstract: A compound represented by Formula (I): wherein or the like Y1 is O or the like; Z1 is C(R4) or N; Z2a is C(R5a) or the like; Z3a is C(R6) or the like; R4, R5a and R6 are each independently a hydrogen atom or the like; R1 is substituted or unsubstituted aromatic carbocyclyl or the like; R2a, R2b, R2c and R2d are each independently a hydrogen atom or the like; X is N(R7a) or the like; R7a is a hydrogen atom or the like; R3 is or the like Ring B is a 6-membered aromatic carbocycle or the like; R9a and R10a are each independently halogen or the like; n is an integer from 1 to 5; m is an integer from 0 to 4; and p 1 is an integer from 0 to 3, or a pharmaceutically acceptable salt thereof.
Abstract: The present invention provides a compound having antiviral activity, especially having arenavirus proliferation inhibitory activity, and/or a medicament comprising the compound. More preferably, the present invention provides a compound having proliferation inhibitory activity on the Old World arenaviruses such as Luna virus, Lassa virus, and lymphocytic choriomeningitis virus and/or the New World arenaviruses such as Junin virus, and/or a medicament comprising the compound.
Type:
Application
Filed:
June 29, 2019
Publication date:
September 23, 2021
Applicants:
NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY, Shionogi & Co., Ltd.
Abstract: A compound represented by Formula (I): wherein or the like, Y1 is O or the like; Z1 is C(R4) or N; Z2a is C(R5a) or the like; Z3a is C(R6) or the like; R4, R5a and R6 are each independently a hydrogen atom or the like; R1 is substituted or unsubstituted aromatic carbocyclyl or the like; R2a, R2b, R2c and R2d are each independently a hydrogen atom or the like; X is N(R7a) or the like; R7a is a hydrogen atom or the like; R3 is or the like, Ring B is a 6-membered aromatic carbocycle or the like; R9a and R10a are each independently halogen or the like; n is an integer from 1 to 5; m is an integer from 0 to 4; and p1 is an integer from 0 to 3, or a pharmaceutically acceptable salt thereof.
Abstract: The solid preparation which improved the dissolution profile and the stability of the 6,7-unsaturation-7-carbamoyl morphinan derivative is provided. When 6,7-unsaturation-7-carbamoyl morphinan derivative, croscarmellose sodium and ferric oxide were contained, not titanium oxide in the solid preparations and the coating solid preparations, a dissolution rate after 15 minutes of the dissolution test is more than 85%, and stability, particularly, light stability can be improve.
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.