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: 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: A compound represented by Formula (I): Chemical Formula 1 wherein Chemical Formula 2 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 Chemical Formula 3 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 is an integer from 0 to 3, or a pharmaceutically acceptable salt thereof.
Abstract: A medicament characterized in that (A) a compound represented by the formula (I): its pharmaceutically acceptable salt, or a solvate thereof, wherein P is hydrogen or a group to form a prodrug; A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is each independently 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 A4 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 are each independently hydrogen, halogen, alkyl, or the like; R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together with an adjacent carbon atom to form non-aromatic carbocycle or non-aromatic heterocycle; n is any integer of 1 to 2; and R1 is or the like,
Abstract: Provided is a monoclonal antibody or a 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 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 disclosure provides a method of measuring an efficacy of a drug composition for cancer and a method for treating a cancer by administering to a subject an effective amount of a pharmaceutical composition having a polypeptide that binds to a peptide produced by cDNA of GenBank ACC No. NM_005201.3 or NM_007720.2.
Type:
Application
Filed:
January 2, 2020
Publication date:
July 23, 2020
Applicants:
Shionogi & Co., Ltd., Osaka University
Abstract: The disclosure provides a pharmaceutical composition with a polypeptide that binds to a peptide produced by cDNA of GenBank ACC No. NM_005201.3 or NM_007720.2, and methods of use thereof.
Type:
Application
Filed:
January 2, 2020
Publication date:
July 16, 2020
Applicants:
Shionogi & Co., Ltd., Osaka University
Abstract: The present invention is the following Amphotericin B derivative: wherein each symbol is defined in description. The compound of the present invention has 16th position (X) is urea structure, cyclic structure, hydroxyalkyl or substituted monoalkylcarbamoyl. The compound of the present invention has antifungal activity.
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: The present invention provides a compound having a TrkA inhibitory activity or a pharmaceutically acceptable salt thereof. The present invention relates to a compound represented by Formula (I): wherein -L- is —C(?X)—, or the like, —Z— is —NR5—, or the like, —ZA— is —NR5A—, or the like, B is substituted or unsubstituted aromatic carbocyclyl, or the like, Y is a single bond, or the like, the ring C is a substituted or unsubstituted aromatic heterocycle, or the like, R2 is a hydrogen atom, or the like, and the group represented by is a group represented by Formula: or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.
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: The present invention is related to a method for evaluation of drug efficacy of a medicine having a therapeutic or preventive effect against a disease related to EL activity wherein phosphatidylinositol or lysophosphatidylinositol is used as an indicator. The present invention is also related to a method for screening an inhibitor of EL activity using phosphatidylinositol and a kit for use in the method.
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: 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 provides a novel compound having antiviral activity, especially HIV replication inhibitory activity and a medicament containing the same. The compound represented by the formula: wherein A3 is CR3A, CR3AR3B, N or NR3C; R3A, R3B, R4A and R4B are each independently a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkynyl, or substituted or unsubstituted non-aromatic carbocyclyl; R3C is a hydrogen atom, substituted or unsubstituted alkyl, or substituted or unsubstituted non-aromatic carbocyclyl; ring T1 is substituted or unsubstituted nitrogen-containing non-aromatic heterocycle; R1 is a hydrogen atom, halogen, cyano, or substituted or unsubstituted alkyl; R2 is each independently substituted or unsubstituted alkyl or the like: n is 1 or 2; R3 is substituted or unsubstituted aromatic carbocyclyl or the like; R4 is a hydrogen atom or a carboxy protecting group.
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. The compound represented by Formula (I): wherein the symbols are defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
October 16, 2017
Publication date:
February 13, 2020
Applicant:
Shionogi & Co., Ltd.
Inventors:
Koji MASUDA, Shuichi SUGIYAMA, Toru YAMADA, Eiichi KOJIMA, Tomoyuki OGAWA, Naotake KOBAYASHI, Hiroyuki KAI
Abstract: The present invention provides a compound having TrkA inhibitory activity, or a pharmaceutically acceptable salt thereof. The present invention relates to a compound represented by Formula (I): wherein ?X is ?O or the like, R5 and R5A are hydrogen atoms or the like, -A- is —NR1— or the like, B is substituted or unsubstituted aromatic carbocyclyl or the like, R1 is substituted or unsubstituted alkyl or the like, R2 is a hydrogen atom or the like, —W— is —CH2— or the like, —WA— is —CH2— or the like, R13 is substituted or unsubstituted aromatic carbocyclyl or the like, R14 is substituted or unsubstituted aromatic heterocyclyl or the like, R15 is substituted or unsubstituted alkyl or the like, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same.
Abstract: The present invention relates to a compound represented by Formula (I): wherein -L- is —C(?X)—, or the like, —Z— is —NR5—, or the like, —ZA— is —NR5A—, or the like, —W— is —C(R8R9)n-, —WA— is —C(R3R4)m-, B is substituted or unsubstituted aromatic carbocyclyl, or the like, Y is a bond, or the like, the ring C is a substituted or unsubstituted aromatic heterocycle, or the like, R2 is a hydrogen atom, or the like, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising thereof.