Abstract: Objective of the present invention is to provide a novel monoclonal antibody against Nav1.7. The present invention discloses a monoclonal antibody against Nav1.7 or its antibody fragment, having specific six CDRs (CDR1 to CDR3 of a heavy chain and CDR1 to CDR3 of a light chain) or specific heavy/light chain variable regions. The monoclonal antibody and the like can be used for treating or preventing pain, pruritus and so on.
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:
Grant
Filed:
October 16, 2017
Date of Patent:
July 20, 2021
Assignee:
SHIONOGI & CO., LTD.
Inventors:
Koji Masuda, Shuichi Sugiyama, Toru Yamada, Eiichi Kojima, Tomoyuki Ogawa, Naotake Kobayashi, Hiroyuki Kai
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, is combined
Abstract: A reference standard set for BNP measurement, including a plurality of reference standards including BNP-32 and proBNP, wherein the ratio BNP-32/proBNP (mole ratio) differs between the reference standards, and when a reference standard having a high mole ratio and a reference standard having a low mole ratio are compared, the BNP concentration, which is the sum total of the BNP-32 concentration and the proBNP concentration, is lower in the reference standard having a high mole ratio than in the reference standard having a low mole ratio.
Abstract: A peptide which can be utilized as an active ingredient of a composition for use in stimulation of migration of PDGFR?-positive cells, a composition for use in recruitment of bone marrow mesenchymal stem cells from bone marrow to peripheral blood, a composition for use in regeneration of tissues, or a composition for use in stimulation of migration of bone marrow-derived stromal cells is provided.
Abstract: The present invention provides a compound represented by the following formula (I): wherein, ring A is a substituted or unsubstituted non-aromatic heterocycle; ring C is a benzene ring or the like; Q is a 5-membered aromatic heterocycle or the like; each R1 is independently halogen or the like; L is substituted or unsubstituted alkylene; 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 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 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 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 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 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 formulation containing the compound represented by formula (I) or a pharmaceutically acceptable salt thereof, or their crystals, with a light-stabilizing substance and a polymer, particularly with one or more of titanium oxide and talc used as the light-stabilizing substance, and hypromellose used as the polymer, which hardly increase the amount of the related substances, and the formulation is hardly colored under light irradiation.
Abstract: The purpose of the present invention is to provide double-stranded oligonucleotides comprising the CpG oligonucleotide mentioned below, as a nucleic acid derivative having an immunostimulatory activity. An adjuvant comprising a double-stranded oligonucleotide, wherein a first strand is a CpG oligonucleotide consisting of 8 to 50 nucleotides, a second strand is an oligonucleotide consisting of 8 to 60 nucleotides and comprising a sequence capable of hybridizing with the first strand, and a lipid binds to the second strand through a linker.
Abstract: Novel compounds having a D3 receptor antagonistic activity are provided. The compound represented by Formula (I): wherein Ring A is a non-aromatic heterocycle or the like substituted with substituted or unsubstituted aromatic heterocyclyl or the like; R2a to R2d are each independently a hydrogen atom or the like; n is an integer of 0 to 3; Ring B is a non-aromatic carbocycle or the like; R3 is each independently halogen or the like: r is an integer of 0 to 4; -L- is —N(R10)—C(?O), or the like; R10 is a hydrogen atom or the like; R4 is substituted or unsubstituted aromatic heterocyclyl or the like, or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
January 25, 2019
Publication date:
February 18, 2021
Applicant:
Shionogi & Co., Ltd.
Inventors:
Yusuke ICHIHASHI, Masanao INAGAKI, Koji MASUDA
Abstract: Novel compounds having a D3 receptor antagonistic effect are provided. The compound represented by Formula (IA)?: wherein A is S or O; R1a is substituted or unsubstituted alkyloxy or the like, R2a to R2d are each independently hydrogen atoms or the like, ring B is a 4- to 8-membered non-aromatic carbocycle or the like, R3 is each independently halogen or the like, r is an integer of 0 to 4, R4 is substituted or unsubstituted aromatic heterocyclyl or the like, or a pharmaceutically acceptable salt thereof.
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: 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: 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.