A pharmaceutical which exhibits sufficient anticancer effects by using an antibody which binds to a mutant CALR protein and another anticancer agent in combination. A pharmaceutical for preventing and/or treating a cancer, including an antibody which specifically binds to a mutant calreticulin protein or a functional fragment thereof and a drug selected from the group consisting of an alkylating agent, a platinum preparation, an antimetabolite, a ribonucleotide reductase inhibitor, a nucleotide analog, a topoisomerase inhibitor, a microtubule polymerization inhibitor, an antitumor antibiotic, an interferon, a cytokine preparation, a molecular targeting drug, a nucleic acid synthesis inhibitor, a jak inhibitor, and a cancer immunotherapeutic agent in combination.
NATIONAL CENTER OF NEUROLOGY AND PSYCHIATRY (Japan)
TOKYO UNIVERSITY OF PHARMACY & LIFE SCIENCES (Japan)
MEIJI SEIKA PHARMA CO., LTD. (Japan)
Inventor
Araki Toshiyuki
Tokunaga Shinji
Funakoshi Masabumi
Ito Hisanaka
Kawamoto Yuichiro
Abe Hideki
Yamada Atsushi
Ishida Natsuki
Nomoto Masahiro
Nangou Fumi
Abstract
Provided are: a novel compound that is useful for the treatment of diseases to be prevented, ameliorated, and/or treated by suppressing axon degeneration; and a pharmaceutical composition containing the same. The present invention relates to: a compound represented by general formula (I) [in the formula, Ra, Rb, X1, R1, L1, L2, and R2 are as disclosed in the specification and as set forth in the claims] or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing the same.
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/455 - Nicotinic acid, i.e. niacinDerivatives thereof, e.g. esters, amides
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing alicyclic rings
C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
The purpose of the present invention is to provide a medicine exhibiting a satisfactory anti-cancer effect by combining an antibody capable of binding to a mutant CALR protein with another anti-cancer agent. Provided is a medicine for preventing and/or treating cancer, the medicine comprising a combination of (A) an antibody capable of binding specifically to a mutant calreticulin protein or a functionalfragment thereof and (B) at least one drug selected from an alkylating agent, a platinum preparation, an antimetabolite, a ribonucleotide reductase inhibitor, a nucleotide analogue,a topoisomerase inhibitor, a microtubule assembly inhibiting drug, an anti-tumor antibiotic, an interferon, a cytokine preparation, a molecule targeting drug, a nucleic acid synthesis inhibitor, a JAK inhibitor and an immuno-oncology drug.
The present invention provides a pharmaceutical composition containing an antibody or a functional fragment thereof capable of binding to a mutant CALR to exhibit a therapeutic effect. The present invention relates to a bispecific antibody or a functional fragment thereof having a first domain that specifically binds to an epitope of a mutant CALR protein and a second domain that specifically binds to a CD3 antigen, wherein: a CDR in the first domain has (a) an amino acid sequence having 80% or higher homology with amino acid sequences represented by SEQ ID NO: 6 (VHCDR1), SEQ ID NO: 7 (VHCDR2), and SEQ ID NO: 8 (VHCDR3), and an amino acid sequence having 80% or higher homology with amino acid sequences represented by SEQ ID NO: 9 (VLCDR1), SEQ ID NO: 10 (VLCDR2) and SEQ ID NO: 11 (VLCDR3); and a CDR in the second domain has an amino acid sequence having 80% or higher homology with an amino acid sequence represented by SEQ ID NO: 12 (VHCDR1), SEQ ID NO: 13 (VHCDR2) or SEQ ID NO: 14 (VHCDR3), and an amino acid sequence having 80% or higher homology with an amino acid sequence represented by SEQ ID NO: 15 (VLCDR2), SEQ ID NO:16 (VLCDR2) or SEQ ID NO: 17 (VLCDR3).
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A crystalline form I of a compound represented by Formula (VII-1):
A crystalline form I of a compound represented by Formula (VII-1):
A crystalline form I of a compound represented by Formula (VII-1):
having characteristic peaks appearing at lattice spacing (d) of 7.34, 5.66, 5.53, 5.30, 5.02, 4.66, 4.37, 4.28, 4.06, 3.68, 3.62, 3.47, 3.36, 3.30, 3.16, 3.11, 3.03, 2.99 and 2.50 Å in the powder X-ray diffraction pattern.
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
FOUNDATION FOR BIOMEDICAL RESEARCH AND INNOVATION AT KOBE (Japan)
NATIONAL INSTITUTES OF BIOMEDICAL INNOVATION, HEALTH AND NUTRITION (Japan)
MEIJI SEIKA PHARMA CO., LTD. (Japan)
Inventor
Honjo, Tasuku
Ohta, Akio
Tajima, Masaki
Kamada, Haruhiko
Nagata, Satoshi
Suzuki, Kensuke
Fukushima, Takayoshi
Tokumaru, Yosuke
Abstract
Conditions necessary for antibodies to human PD-1 to have agonist activity are searched and an optimized agonist antibody is provided based on the conditions and used as a therapeutic for human inflammatory diseases. An agonist antibody to human PD-1 or a functional fragment thereof, wherein the antibody or a functional fragment thereof binds to domain #7 of human PD-1 as shown in SEQ ID NO: 9 is provided.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
8.
METHOD FOR PRODUCING BENZOXAZOLE DERIVATIVE HAVING BICYCLIC PIPERAZINE RING OR SALT THEREOF, AND METHOD FOR PRODUCING MATERIAL THEREOF
A method for producing a compound represented by formula (1):
A method for producing a compound represented by formula (1):
A method for producing a compound represented by formula (1):
or a salt thereof, comprising:
a step B of producing a compound represented by formula (3):
A method for producing a compound represented by formula (1):
or a salt thereof, comprising:
a step B of producing a compound represented by formula (3):
A method for producing a compound represented by formula (1):
or a salt thereof, comprising:
a step B of producing a compound represented by formula (3):
[in the formula (3), Boc represents a tert-butoxycarbonyl group]
or a salt thereof by using a compound represented by formula (2):
A method for producing a compound represented by formula (1):
or a salt thereof, comprising:
a step B of producing a compound represented by formula (3):
[in the formula (3), Boc represents a tert-butoxycarbonyl group]
or a salt thereof by using a compound represented by formula (2):
A method for producing a compound represented by formula (1):
or a salt thereof, comprising:
a step B of producing a compound represented by formula (3):
[in the formula (3), Boc represents a tert-butoxycarbonyl group]
or a salt thereof by using a compound represented by formula (2):
[in the formula (2),
Ra represents a hydrogen atom or an optionally substituted arylmethyl group,
Rb represents an optionally substituted alkyl or cyclic alkyl group,
R3 represents a hydrogen atom, a halogen atom, or a thiazol-2-yl group, and
Xa represents a hydrogen atom or a halogen atom] or a salt thereof; and
a step C of producing the compound represented by the formula (1) or the salt thereof by using the compound represented by the formula (3) or the salt thereof.
A compound represented by general formula (I): [in formula (I), n represents an integer of 0 to 2; X represents CH, CF, CCl, N, CHCH=N, CHCH=CH, or CHCH=CF; Y represents O, NH, or a single bond; Z represents a hydroxy group or an oxo group; R1represents a hydrogen atom, a C1 to C6 alkyl group, a three- to six-membered cycloalkyl group, a four- to eight-membered heterocycloalkyl group, a six- to ten-membered aryl group, a five- to ten-membered heteroaryl group, a C2 to C6 alkenyl group, a C2 to C6 alkynyl group, a group represented by -CO-R2, a group represented by -COO-R2, a group represented by -CONH-R2, or a group represented by -B(OR4)OR5, and these groups may be substituted; R2, R4, and R5 each represent a hydrogen atom, alkyl group, etc.] or a pharmaceutically acceptable salt thereof.
C07D 493/22 - Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
The present invention addresses the problem of providing a novel method for treating T cell tumor, whereby it becomes possible to induce the cell damage of a tumor cell and which is less likely to cause immunodeficiency. According to the present invention, a T cell tumor therapeutic agent comprising a bispecific antigen-binding molecule is provided, in which the bispecific antigen-binding molecule includes (1) at least one segment capable of binding specifically to a target tumor antigen expressed in a T cell tumor cell and (2) at least one segment capable of binding specifically to a normal T cell-side target antigen having a subtype. The target tumor antigen expressed in a T cell tumor cell is not present in a normal T cell. If the target tumor antigen is present in a normal T cell, when the bispecific antigen-binding molecule is bound to an antigen that is the same as the target tumor antigen and is present in a normal T cell, the normal T cell is not substantially activated. When the bispecific antigen-binding molecule is bound to a normal T cell-side target antigen, the normal T cell is activated and the subtype of the normal T cell-side target antigen is present at a ratio that is sufficient for providing a sufficient number of activated T cell for the treatment of T cell tumor.
A61P 35/02 - Antineoplastic agents specific for leukemia
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
A bispecific antibody including a first domain which specifically binds to a mutant calreticulin protein and a second domain which specifically binds to a CD3 antigen. A pharmaceutical composition including the bispecific antibody or a functional fragment thereof. A diagnostic method for a myeloproliferative neoplasm, including detecting a polypeptide in a biological sample with the bispecific antibody.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
A process for preparing a diazabicyclooctane compound represented by the following formula (I):
1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c):
wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/43 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/545 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine
A61K 31/546 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine containing further heterocyclic rings, e.g. cephalothin
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07F 7/08 - Compounds having one or more C—Si linkages
The purpose of the present invention is to provide a medicine exhibiting a satisfactory anti-cancer effect by combining an antibody capable of binding to a mutant CALR protein with another anti-cancer agent. Provided is a medicine for preventing and/or treating cancer, the medicine comprising a combination of (A) an antibody capable of binding specifically to a mutant calreticulin protein or a functional fragment thereof and (B) at least one drug selected from an alkylating agent, a platinum preparation, an antimetabolite, a ribonucleotide reductase inhibitor, a nucleotide analogue, a topoisomerase inhibitor, a microtubule assembly inhibiting drug, an anti-tumor antibiotic, an interferon, a cytokine preparation, a molecule targeting drug, a nucleic acid synthesis inhibitor, a JAK inhibitor and an immuno-oncology drug.
Foundation for Biomedical Research and Innovation at Kobe (Japan)
National Institutes of Biomedical Innovation, Health and Nutrition (Japan)
Meiji Seika Pharma Co., Ltd. (Japan)
Inventor
Honjo, Tasuku
Ohta, Akio
Tajima, Masaki
Kamada, Haruhiko
Nagata, Satoshi
Suzuki, Kensuke
Oshiro, Yuya
Tokumaru, Yosuke
Abstract
A novel use of agonist to PD-1 is developed. Provided is a pharmaceutical composition for treating or preventing Th2-mediated diseases, the composition comprising an effective amount of a PD-1 agonist.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A method for producing a compound represented by formula (1) or a salt thereof, the method comprising: a step B for producing a compound represented by formula (3) [in formula (3), Boc represents a tert-butoxycarbonyl group] or a salt thereof by using a compound represented by formula (2) [in formula (2), Ra represents a hydrogen atom or an optionally substituted arylmethyl group, Rb represents an optionally substituted alkyl group or a cyclic alkyl group, R3 represents a hydrogen atom, a halogen atom, or a thiazol-2-yl group, and Xa represents a hydrogen atom or a halogen atom] or a salt thereof; and a step C for producing the compound represented by formula (1) or a salt thereof by using the compound represented by formula (3) or a salt thereof.
C07D 263/58 - BenzoxazolesHydrogenated benzoxazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
A method for producing a compound represented by formula (1) or a salt thereof, the method comprising: a step B for producing a compound represented by formula (3) [in formula (3), Boc represents a tert-butoxycarbonyl group] or a salt thereof by using a compound represented by formula (2) [in formula (2), Rarepresents a hydrogen atom or an optionally substituted arylmethyl group, Rbrepresents an optionally substituted alkyl group or a cyclic alkyl group, R3represents a hydrogen atom, a halogen atom, or a thiazol-2-yl group, and Xa represents a hydrogen atom or a halogen atom] or a salt thereof; and a step C for producing the compound represented by formula (1) or a salt thereof by using the compound represented by formula (3) or a salt thereof.
C07D 263/58 - BenzoxazolesHydrogenated benzoxazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
29.
ANTI-HUMAN PD-1 AGONIST ANTIBODY AND PHARMACEUTICAL COMPOSITION COMPRISING THE ANTIBODY FOR TREATING OR PREVENTING INFLAMMATORY DISEASES
NATIONAL INSTITUTES OF BIOMEDICAL INNOVATION, HEALTH AND NUTRITION (Japan)
FOUNDATION FOR BIOMEDICAL RESEARCH AND INNOVATION AT KOBE (Japan)
Inventor
Honjo, Tasuku
Ohta, Akio
Tajima, Masaki
Kamada, Haruhiko
Nagata, Satoshi
Suzuki, Kensuke
Fukushima, Takayoshi
Tokumaru, Yosuke
Abstract
The present invention pertains to a search for conditions necessary for an antibody against human PD-1 to possess an agonist activity, establishing of an agonist antibody optimized on the basis of such necessary conditions, and application of said agonist antibody as a drug for human inflammatory diseases. An agonist antibody against human PD-1 or a functional fragment thereof according to the present invention is characterized in that the antibody or the functional fragment thereof binds to domain #7, of human PD-1, represented by SEQ ID: 9.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
FOUNDATION FOR BIOMEDICAL RESEARCH AND INNOVATION AT KOBE (Japan)
NATIONAL INSTITUTES OF BIOMEDICAL INNOVATION, HEALTH AND NUTRITION (Japan)
MEIJI SEIKA PHARMA CO., LTD. (Japan)
Inventor
Honjo,tasuku
Ohta,akio
Tajima,masaki
Kamada, Haruhiko
Nagata, Satoshi
Suzuki, Kensuke
Fukushima, Takayoshi
Tokumaru, Yosuke
Abstract
The present invention pertains to a search for conditions necessary for an antibody against human PD-1 to possess an agonist activity, establishing of an agonist antibody optimized on the basis of such necessary conditions, and application of said agonist antibody as a drug for human inflammatory diseases. An agonist antibody against human PD-1 or a functional fragment thereof according to the present invention is characterized in that the antibody or the functional fragment thereof binds to domain #7, of human PD-1, represented by SEQ ID: 9.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
31.
Crystalline forms of diazabicyclooctane derivative and production process thereof
A crystalline form I of a compound represented by Formula (VII-1):
having characteristic peaks appearing at lattice spacing (d) of 7.34, 5.66, 5.53, 5.30, 5.02, 4.66, 4.37, 4.28, 4.06, 3.68, 3.62, 3.47, 3.36, 3.30, 3.16, 3.11, 3.03, 2.99 and 2.50 Å in the powder X-ray diffraction pattern.
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A control agent comprising, as an active ingredient, a specific quinoline derivative compound such as 8-fluoro-2,3-dimethyl-6-(1,1-dimethylethyl)-4-(methylcarbonyl)oxyquinoline, azoxystrobin, picoxystrobin, pyraclostrobin, kresoxim-methyl, trifloxystrobin, metominostrobin, orysastrobin, famoxadone, fluoxastrobin, pyribencarb, cyazofamid, amisulbrom, flutolanil, mepronil, isofetamid, fluopyram, carboxin, thifluzamide, fluxapyroxad, furametpyr, penflufen, penthiopyrad, boscalid, diflumetorim, fluazinam, ferimzone, fenpyroximate, or an acid addition salt of any of these compounds shows an excellent controlling effect on Mesostigmata mites.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
A diagnostic, preventive, or therapeutic agent may be used for a myeloproliferative neoplasm. An antibody or a functional fragment thereof that binds to a cleaved mutant CALR protein, may include an antigen-recognition site in (a) a polypeptide chain having an amino acid sequence set forth in SEQ ID NO: 1 or (b) a polypeptide chain having an amino acid sequence having deletion, substitution, or addition of one to several amino acids in SEQ ID NO: 1; and a diagnostic, preventive, or therapeutic agent for a myeloproliferative neoplasm containing the antibody.
Provided are: a higher-performance bispecific antibody that specifically binds to a mutant calreticulin protein; and a pharmaceutical composition that contains said antibody. Provided is a bispecific antibody having: a first domain that specifically binds to a mutant calreticulin protein; and a second domain that specifically binds to a CD3 antigen.
A61P 35/02 - Antineoplastic agents specific for leukemia
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
Provided are: a higher-performance bispecific antibody that specifically binds to a mutant calreticulin protein; and a pharmaceutical composition that contains said antibody. Provided is a bispecific antibody having: a first domain that specifically binds to a mutant calreticulin protein; and a second domain that specifically binds to a CD3 antigen.
A61P 35/02 - Antineoplastic agents specific for leukemia
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A Mesostigmata mite control composition comprising, as active ingredients: a specific quinoline derivative compound such as 8-fluoro-2,3-dimethyl-6-(1,1-dimethylethyl)-4-(methylcarbonyl)oxyquinoline; and at least one of other pest control agents exhibits an excellent control effect on Mesostigmata mites.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A01N 53/00 - Biocides, pest repellants or attractants, or plant growth regulators containing cyclopropane carboxylic acids or derivatives thereof
A01N 57/14 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-oxygen bonds or phosphorus-to-sulfur bonds containing aromatic radicals
A01N 57/12 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-oxygen bonds or phosphorus-to-sulfur bonds containing acyclic or cycloaliphatic radicals
A01N 43/16 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom six-membered rings with oxygen as the ring hetero atom
According to the present invention, the expression of a target protein is promoted in mammalian cells by co-introducing a polynucleotide containing an expression cassette of the target protein, a polynucleotide containing IR/MAR and a polynucleotide promoting the expression of the target protein, each as a separate polynucleotide, into the mammalian cells.
A process for preparing a diazabicyclooctane compound represented by the following formula (I):
1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c):
wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/43 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems
A61K 31/545 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine
A61K 31/546 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine containing further heterocyclic rings, e.g. cephalothin
C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
C07F 7/08 - Compounds having one or more C—Si linkages
39.
PD-1 AGONIST-CONTAINING PHARMACEUTICAL COMPOSITION FOR TREATING OR PREVENTING Th2-MEDIATED DISEASE
FOUNDATION FOR BIOMEDICAL RESEARCH AND INNOVATION AT KOBE (Japan)
NATIONAL INSTITUTES OF BIOMEDICAL INNOVATION, HEALTH AND NUTRITION (Japan)
MEIJI SEIKA PHARMA CO., LTD. (Japan)
Inventor
Honjo,tasuku
Ohta,akio
Tajima,masaki
Kamada, Haruhiko
Nagata, Satoshi
Suzuki, Kensuke
Oshiro, Yuya
Tokumaru, Yosuke
Abstract
In the present invention, novel uses for PD-1 agonists have been developed. Provided is a pharmaceutical composition for treating or preventing Th2-mediated diseases, the composition containing an effective amount of a PD-1 agonist.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
Provided are: a novel compound, and a pharmaceutically acceptable salt thereof, represented by formula (1), the compound having a histamine H4 receptor-regulating effect and being useful in the treatment and/or prevention of an illness or state in which histamine H4 receptor participates; the use of the same; and a medical composition containing the same.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 475/08 - Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
41.
Therapeutic agent for inflammatory diseases, autoimmune diseases, fibrotic diseases, and cancer diseases
A therapeutic agent for treating at least one disease selected from the group consisting of inflammatory diseases, autoimmune diseases, fibrotic diseases, and cancer diseases, comprising: at least one selected from the group consisting of a compound represented by the following general formula (1) and pharmacologically acceptable salts thereof as an active ingredient.
2—; and Z represents a hydrogen atom or a hydroxyl group.]
A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
A composition for lysing at least one type of staphylococcus bacteria selected from the group consisting of Staphylococcus hyicus, Staphylococcus chromogenes, Staphylococcus simulans, Staphylococcus schleiferi, and Staphylococcus felis, or for the prevention or treatment of diseases caused by said bacteria, said composition containing, as active ingredients: at least one bacteriophage selected from the group consisting of bacteriophages identified by accession number NITE BP-693 and bacteriophages identified by accession number NITE BP-694; and an endolysin, which is a protein specified by an amino acid sequence of SEQ ID NO: 1.
A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
The present invention relates to: a homogeneous composition which comprises a steroid compound and olopatadine and in which the steroid compound and olopatadine are present stably in a suspended state and in a dissolved state, respectively; and a method for producing the composition.
A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
Provided are crystals of 1-((2-(3,6-diazabicyclo[3.1.1]heptan-3-yl)-7-(thiazol-2-yl)benzo[d]oxazol-4-yl)oxy)-1,1-difluoro-2-methylpropan-2-ol represented by formula (1),
This composition for lysis of Staphylococcus aureus or this composition for prevention or therapy of diseases caused by Staphylococcus aureus contains as active ingredients: at least one bacteriophage selected from the group consisting of the bacteriophage identified by Accession No. NITE BP-693 and the bacteriophage identified by Accession No. NITE BP-694; and an endolysin that is at least one protein selected from the group consisting of (a) a protein having the amino acid sequence of SEQ ID NO: 1; (b) proteins having an amino acid sequence having 80% or more identity to the amino acid sequence of SEQ ID NO: 1; and (c) proteins having an amino acid sequence obtained by providing one or more amino acid substitutions, deletions, additions, and/or insertions to the amino acid sequence of SEQ ID NO: 1.
This composition is for lysing Staphylococcus aureus or treating or preventing diseases caused by Staphylococcus aureus, and contains, as active ingredients, at least one bacteriophage selected from the group consisting of the bacteriophage specified by Deposit No. NITE BP-693 and the bacteriophage specified by Deposit No. NITE BP-694, and an endolysin, which is at least one protein selected from the group consisting of (a) a protein having the amino acid sequence described in SEQ ID NO: 1, (b) proteins having amino acid sequences having at least 80% identity with the amino acid sequence described in SEQ ID NO: 1, and (c) proteins having amino acid sequences obtained by providing at least one amino acid substitution, deletion, addition, and/or insertion to the amino acid sequence described in SEQ ID NO: 1.
A composition for lysing Staphylococcus aureus or a composition for preventing or treating a disease caused by Staphylococcus aureus, said composition comprising, as active ingredients, at least one bacteriophage selected from the group consisting of a bacteriophage identified under accession number NITE BP-693 and a bacteriophage identified under accession number NITE BP-694, and an endolysin that is at least one protein selected from the group consisting of (a) a protein having the amino acid sequence represented by SEQ ID NO: 1, (b) a protein that has an amino acid sequence having at least 80% identity to the amino acid sequence represented by SEQ ID NO: 1, and (c) a protein that has an amino acid sequence with the substitution, deletion, addition and/or insertion of one or more amino acids in the amino acid sequence represented by SEQ ID NO: 1.
Provided is a compound represented by the following formula (1) and a pharmacologically acceptable salt, which have a regulatory activity for a histamine H4 receptor and are useful for the treatment and/or prevention of diseases or conditions in which the histamine H4 receptor is involved; use of the same; and a pharmaceutical composition comprising the same.
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
An agent for controlling scald disease, said agent comprising as an active ingredient a lactic acid bacterium that has an ability to control scald disease.
The purpose of the present invention is to provide a novel agent for suppressing bitterness in asenapine. According to the present invention, there is provided an agent for suppressing bitterness in asenapine, the agent including, as an active ingredient, at least one selected from the group consisting of polyols (other than aromatic polyols), aliphatic hydroxy acids, saccharine, acesulfame potassium, alkyl sulfate, povidone, magnesium stearate, talc, and sodium stearyl fumarate. This agent for suppressing bitterness can be used when administering an asenapine-containing composition, the asenapine-containing composition preferably being a sublingual orally disintegrating tablet, and more preferably being a lyophilized sublingual orally disintegrating tablet.
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
Provided is a solid formulation for rice pest control, which is a coated granule or extruded granule and comprises at least one effective component selected from the group consisting of flupyrimin as represented by formula (1): and salts thereof, and also a solid carrier, a surfactant, and a binder.
A01N 25/26 - Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of applicationSubstances for reducing the noxious effect of the active ingredients to organisms other than pests in coated particulate form
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
This plant parasitic nematode controlling agent for Tylenchoidea contains, as an active ingredient, at least one compound selected from the group consisting of the compound represented by formula (1), the compound represented by formula (2), the compound represented by formula (3), an enantiomer thereof, and an agriculturally and horticulturally acceptable acid addition salt thereof.
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
54.
ANTIBODIES THAT BIND TO CLEAVED FORM OF MUTANT CALRETICULIN, AND DIAGNOSTIC, PREVENTIVE, OR THERAPEUTIC AGENT FOR MYELOPROLIFERATIVE NEOPLASM
Provided is a diagnostic, prophylactic or therapeutic drug for myeloproliferative neoplasms. An antibody which can bind to a truncated mutant CALR protein and has an antigen-recognition site in (a) a polypeptide chain comprising the amino acid sequence represented by SEQ ID NO: 1 or (b) a polypeptide chain comprising such an amino acid sequence that one amino acid residue or several amino acid residues are deleted, substituted or added in SEQ ID NO: 1, or a functional fragment of the antibody; and a diagnostic, prophylactic or therapeutic drug for myeloproliferative neoplasms, which comprises the antibody.
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
Provided is a diagnostic, prophylactic or therapeutic drug for myeloproliferative neoplasms. An antibody which can bind to a truncated mutant CALR protein and has an antigen-recognition site in (a) a polypeptide chain comprising the amino acid sequence represented by SEQ ID NO: 1 or (b) a polypeptide chain comprising such an amino acid sequence that one amino acid residue or several amino acid residues are deleted, substituted or added in SEQ ID NO: 1, or a functional fragment of the antibody; and a diagnostic, prophylactic or therapeutic drug for myeloproliferative neoplasms, which comprises the antibody.
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
the treatment of osteoarthritis and joint disease;
prepackaged injectable medicines; prepackaged injectable
sodium hyaluronate solutions for medical use; pre-filled
syringes for medical purposes; pre-filled syringes
containing sodium hyaluronate solutions for the treatment of
osteoarthritis and joint disease. Medical apparatus and instruments; syringes for injections;
injection devices for pharmaceuticals; injectors for medical
purposes; medical apparatus, namely, self-contained syringes
for injecting prepackaged injectable medicine, medical
self-contained syringes for injecting prepackaged injectable
sodium hyaluronate solutions.
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
the treatment of osteoarthritis and joint disease;
prepackaged injectable medicines; prepackaged injectable
sodium hyaluronate solutions for medical use; pre-filled
syringes for medical purposes; pre-filled syringes
containing sodium hyaluronate solutions for the treatment of
osteoarthritis and joint disease. Medical apparatus and instruments; syringes for injections;
injection devices for pharmaceuticals; injectors for medical
purposes; medical apparatus, namely, self-contained syringes
for injecting prepackaged injectable medicine, medical
self-contained syringes for injecting prepackaged injectable
sodium hyaluronate solutions.
58.
Crystalline forms of diazabicyclooctane derivative and production process thereof
A crystalline form I of a compound represented by Formula (VII-1):
having characteristic peaks appearing at lattice spacing (d) of 7.34, 5.66, 5.53, 5.30, 5.02, 4.66, 4.37, 4.28, 4.06, 3.68, 3.62, 3.47, 3.36, 3.30, 3.16, 3.11, 3.03, 2.99 and 2.50 Å in the powder X-ray diffraction pattern.
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
59.
Effective aminoglycoside antibiotic for multidrug-resistant bacteria
A compound represented by the following general formula (I) or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutical composition thereof, and the use thereof to prevent or treat infectious diseases and a method to prevent or treat infectious diseases using those regimen are disclosed. The compound represented by formula (I) has an antibacterial activity against both gram-positive and gram-negative bacteria, and is useful in the prevention or treatment of infectious diseases caused by these bacteria.
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
C07H 15/224 - Cyclohexane rings, substituted by at least two nitrogen atoms with only one saccharide radical directly attached to the cyclohexane rings, e.g. destomycin, fortimicin, neamine
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A01N 25/30 - Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of applicationSubstances for reducing the noxious effect of the active ingredients to organisms other than pests characterised by the surfactants
The present invention provides a plant disease control agent which contains a compound represented by formula (1). (In the formula, each of X1and X4represents a fluorine atom, a chlorine atom or the like; each of X2and X3represents a hydrogen atom or the like; Xa represents a group expressed by formula (2) or (3); each of Ja and Jb represents an oxygen atom or the like; G represents an optionally substituted phenyl group or the like; Aa represents an optionally substituted alkyl group, a phenyl group or the like; Q represents an oxygen atom or the like; and Ab represents a heterocyclic group which may be substituted by a halogen atom or the like.)
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A01N 43/80 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms, as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,2
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A composition for controlling mesostigmata mites exhibits an excellent control effect on mesostigmata mites, the composition including as active ingredients: a specific quinoline derivative compound such as 8-fluoro-2,3-dimethyl-6-(1,1-dimethylethyl)-4-(methylcarbonyl) oxyquinoline; and at least one other pest control agent.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
A01N 47/06 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having no bond to a nitrogen atom containing —O—CO—O— groupsThio-analogues thereof
A01N 53/04 - Esters containing the group , wherein the carbon atom marked with an asterisk is acyclic or part of a ring or ring systemThio-analogues thereof having heterocyclic rings
A01N 53/08 - Esters containing the group , wherein the carbon atom marked with an asterisk is acyclic or part of a ring or ring systemThio-analogues thereof the carbon atom marked with an asterisk being acyclic and directly bound to a carbon atom of a six-membered aromatic ring, e.g. benzyl estersThio-analogues thereof with aryloxy groups bound to the six-membered aromatic ring, e.g. phenoxybenzyl estersThio-analogues thereof
A01N 57/14 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-oxygen bonds or phosphorus-to-sulfur bonds containing aromatic radicals
A01N 57/20 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-carbon bonds containing acyclic or cycloaliphatic radicals
Provided are a plant disease control agent and a plant disease control method, the plant disease control agent containing a compound represented by formula (1) as an active ingredient. (In the formula, X1and X4each independently represent a fluorine atom or the like, X2and X3 each independently represent a hydrogen atom or a fluorine atom, Xa is a group represented by formula (2), (3), (4), (5) or (6), J represents an oxygen atom or the like, Q represents an oxygen atom or the like, A represents a phenyl group or the like which may have a substituent, Aa represents a piperidin-1-yl group or the like, Qb represents an oxygen atom or the like, Ab represents a hydrogen atom or the like, Z represents a hydrogen atom or the like, m represents an integer of 1-3, Ja and Jb each independently represent an oxygen atom or the like, G represents a phenyl group or the like, and Ad represents an alkyl group, an alkyloxy group, or the like.)
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A01N 43/52 - 1,3-DiazolesHydrogenated 1,3-diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A01N 43/80 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms, as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,2
A01N 43/84 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms, as ring hetero atoms six-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,4
A01N 43/86 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms, as ring hetero atoms six-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,3
A01N 47/02 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having no bond to a nitrogen atom
A01N 47/12 - Carbamic acid derivatives, i.e. containing the group —O—CO—NThio-analogues thereof containing a —O—CO—N group, or a thio-analogue thereof, neither directly attached to a ring nor the nitrogen atom being a member of a heterocyclic ring
A process for preparing a diazabicyclooctane compound represented by the following formula (I):
1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c):
wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.
C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/546 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine containing further heterocyclic rings, e.g. cephalothin
A61K 31/43 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/545 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine
C07F 7/08 - Compounds having one or more C—Si linkages
Staphylococcus hyicusStaphylococcus chromogenesStaphylococcus chromogenes and the like. This finding enables the provision of: a composition for lysing these staphylococcal bacteria; a composition for treating or preventing diseases associated with these staphylococcal bacteria; and others.
Provided is a crystal of 1-((2-(3, 6-diazabicyclo[3.1.1]heptane-3-yl)-7-(thiazole-2-yl)benzo[d]oxazole-4-yl)oxy)-1,1-difluoro-2-methylpropane-2-ol represented by formula (1).
A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
68.
THERAPEUTIC AGENT FOR INFLAMMATORY DISEASES, AUTOIMMUNE DISEASES, FIBROTIC DISEASES, AND CANCER DISEASES
A therapeutic agent for treating at least one disease selected from the group consisting of inflammatory diseases, autoimmune diseases, fibrotic diseases, and cancer diseases, wherein the therapeutic agent contains as an active ingredient a compound represented by general formula (1) and/or a pharmacologically acceptable salt thereof. [In formula (1), R1and R21-61-6 alkyl group, etc.; R3represents a hydrogen atom; R4222222222-; and Z represents a hydrogen atom or a hydroxyl group.]
Provided is a crystal of 1-((2-(3, 6-diazabicyclo[3.1.1]heptane-3-yl)-7-(thiazole-2-yl)benzo[d]oxazole-4-yl)oxy)-1,1-difluoro-2-methylpropane-2-ol represented by formula (1).
A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
The present invention discloses a water-dispersible agrochemical composition which is in a solid state at 30°C, and which contains: an agrochemically active ingredient (A) that is a compound represented by formula (I) or an agriculturally and horticulturally acceptable acid addition salt thereof; one or more additives; and one or more surfactants. This water-dispersible agrochemical composition has excellent storage stability and excellent physical properties for preparations.
A01N 47/06 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having no bond to a nitrogen atom containing —O—CO—O— groupsThio-analogues thereof
A01N 25/30 - Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of applicationSubstances for reducing the noxious effect of the active ingredients to organisms other than pests characterised by the surfactants
A01N 43/16 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom six-membered rings with oxygen as the ring hetero atom
A01N 47/24 - Carbamic acid derivatives, i.e. containing the group —O—CO—NThio-analogues thereof containing the groups , or Thio-analogues thereof
A01N 51/00 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds having the sequences of atoms O—N—S, X—O—S, N—N—S, O—N—N or O-halogen, regardless of the number of bonds each atom has and with no atom of these sequences forming part of a heterocyclic ring
A01N 57/16 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-oxygen bonds or phosphorus-to-sulfur bonds containing heterocyclic radicals
Disclosed are: a method for manufacturing a compound (5-epi-4"-N-(L-isoceryl)apramycin) and 5-epiapramycin; and an intermediate used for said method. The method of the present invention is useful in that the compound (5-epi-4"-N-(L-isoceryl)apramycin) can be efficiently and completely produced.
C07H 15/224 - Cyclohexane rings, substituted by at least two nitrogen atoms with only one saccharide radical directly attached to the cyclohexane rings, e.g. destomycin, fortimicin, neamine
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
A compound represented by the general formula (1) below or a pharmacologically acceptable salt thereof:
2—; and Z represents a hydrogen atom or a hydroxyl group].
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for the treatment of osteoarthritis and joint disease; prepackaged injectable medicine; prepackaged injectable sodium hyaluronate solutions; pre-filled syringes for medical purposes. Injectors for medical purposes; medical apparatus, including self-contained syringes for injecting prepackaged injectable medicine; medical apparatus, including self-contained syringes for injecting prepackaged injectable sodium hyaluronate solutions.
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for the treatment of osteoarthritis and joint disease; prepackaged injectable medicine; prepackaged injectable sodium hyaluronate solutions; pre-filled syringes for medical purposes. Injectors for medical purposes; medical apparatus, including self-contained syringes for injecting prepackaged injectable medicine; medical apparatus, including self-contained syringes for injecting prepackaged injectable sodium hyaluronate solutions.
This liquid agent for external use for prevention and treatment of onychomycosis contains a drug with anti-onychomycotic activity, a volatile alcohol, and a delivery enhancer.
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
This liquid agent for external use for prevention and treatment of onychomycosis contains a drug with anti-onychomycotic activity, a volatile alcohol, and a delivery enhancer.
A process for producing crystals of a compound represented by the following formula (I):
by crystallizing the compound from an aqueous solution containing the compound and an inorganic salt, such as sodium chloride. Such crystals can be subjected to lyophilization to provide a lyophilized composition having a desirable storage stability.
A61K 9/19 - Particulate form, e.g. powders lyophilised
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
[Problem] To provide a method for producing and isolating a target quinolone derivative using general industrial facilities with high purity. [Solution] The present invention provides a method for producing a quinolone derivative, the method comprising performing a reaction between a ketone and an anthranilic acid derivative using an aluminium halide and removing the aluminium halide under a basic condition.
When the sealedness of a luer nozzle is breached at the same time as that of a luer lock portion during capping or uncapping, uncapping becomes less easy and leakage of drug solution inside the syringe increases. A tip cap 10 includes: a thick disk-like base portion 11 which has a top face 15 on one side; a cylindrical inner tube portion 13 which is protrudingly formed from the other side opposite (in the thickness direction) the top face 15 of the base portion 11 and is for coveringly sealing, with at least an inner circumferential surface thereof, a luer nozzle; and a cylindrical outer tube portion 14 which is protrudingly and surroundingly formed coaxial with the inner tube portion from the other side opposite (in the thickness direction) the top face 15 of the base portion 11 and which is for coveringly sealing a luer lock. The outer tube portion 14 has an inner circumferential surface 141 that covers the luer lock and an outer circumferential surface that is connected to an outer circumferential surface of the base portion 11 to form an outer circumferential surface 17 of the cap. The cap has, formed on the outer circumferential surface at a location closer to the top face than the base of the outer tube portion, an annular groove 18 that extends in a circumferential direction.
To provide an optical probe that can be miniaturized with ease and that changes the direction of light emitted from a light source and guided by an optical fiber to a direction of side illumination using a very simple method so that irradiation is made more efficient and heat generation is reduced, the optical probe 11 is provided with: a substantially cylindrical probe distal end 13 that has a substantially cylindrical first light transmissive region 22 and a second light transmissive region 23 that covers an outer surface of the first light transmissive region 22; and an optical fiber 12 that optically connects the light source to the probe distal end 13; wherein when light emitted from the core 2 of the optical fiber 12 enters the first light transmissive region 22, the optical probe 11 satisfies the relationship n1
A61B 18/22 - Surgical instruments, devices or methods for transferring non-mechanical forms of energy to or from the body by applying electromagnetic radiation, e.g. microwaves using laser the beam being directed along or through a flexible conduit, e.g. an optical fibreHand-pieces therefor
82.
CRYSTALLINE FORMS OF DIAZABICYCLOOCTANE DERIVATIVES AND PRODUCTION PROCESS THEREOF
The present invention relates to crystalline forms of a diazabicyclooctane derivative represented by Compound I, the process for producing the same and methods for using the same: (I).
The present invention relates to a process for producing crystalline and amorphous forms of a diazabicyclooctane derivative represented by Compound (I) and methods for producing the same.
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
The present invention relates to a pharmaceutical composition and a lyophilisate of a diazabicyclooctane derivative represented by Compound I, a process for producing the same and methods for using the same. (I)
A61K 9/19 - Particulate form, e.g. powders lyophilised
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
85.
Processes for producing diazabicyclooctane compounds
A process for producing a compound of the following Formula (VII-CR):
The process involving providing a compound represented by the following Formula (VI):
1-6 alkyl or a heterocycle.
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
NATIONAL INSTITUTE OF ADVANCED INDUSTRIAL SCIENCE AND TECHNOLOGY (Japan)
Inventor
Nagata, Hirotaka
Minowa, Nobuto
Nakanishi, Nozomu
Shimura, Katsuya
Fujitani, Tadahiro
Abstract
A method for producing methyl dichlorophosphane, said method comprising a step for reacting methane with phosphorus trichloride in the presence of an additive with the use of a metal compound and/or a metal compound held on a support.
A compound represented by the formula, which has an RORγt inhibiting effect and is useful as a prophylactic or therapeutic agent for autoimmune diseases, allergic diseases, etc., or a salt thereof.
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/46 - 8-Azabicyclo [3.2.1] octaneDerivatives thereof, e.g. atropine, cocaine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 451/02 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof
Acremonium cellulolyticus, and various primers were designed based on the information. PCR was carried out using the various primers thus designed and genomic DNA or cDNA as a template. As a result, gene fragments of endoglucanases and β-glucosidases were obtained. Primers were designed based on the gene fragments, and PCR was carried out to amplify nine genes of endoglucanases and β-glucosidases. The nucleotide sequences thereof were sequenced, and the present invention was completed.
Provided is a compound represented by the formula, or a salt thereof, the compound having RORγt-inhibiting activity and being useful as a prophylactic or therapeutic agent for autoimmune or allergic diseases.
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
90.
AQUEOUS FORMULATION, AQUEOUS FORMULATION IN INJECTOR, ANTIBODY PROTEIN DISAGGREGATING AGENT, AND ANTIBODY PROTEIN DISAGGREGATION METHOD
DONG-A SOCIO HOLDINGS CO., LTD. (Republic of Korea)
Inventor
Kaya Arpansiree
Fujita Michinari
Abstract
Provided is an aqueous formulation containing: ustekinumab; at least one selected from histidine and a salt thereof; and water. The content of histidine and/or a salt thereof is 50 to 90 mM in terms of histidine.
A control agent comprising, as an active ingredient, a specific quinoline derivative compound such as 8-fluoro-2,3-dimethyl-6-(1,1-dimethylethyl)-4-(methylcarbonyl)oxyquinoline, azoxystrobin, picoxystrobin, pyraclostrobin, kresoxim-methyl, trifloxystrobin, metominostrobin, orysastrobin, famoxadone, fluoxastrobin, pyribencarb, cyazofamid, amisulbrom, flutolanil, mepronil, isofetamid, fluopyram, carboxin, thifluzamide, fluxapyroxad, furametpyr, penflufen, penthiopyrad, boscalid, diflumetorim, fluazinam, ferimzone, fenpyroximate, or an acid addition salt of any of these compounds shows an excellent controlling effect on Mesostigmata mites.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
A01N 47/06 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having no bond to a nitrogen atom containing —O—CO—O— groupsThio-analogues thereof
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A01N 43/52 - 1,3-DiazolesHydrogenated 1,3-diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A01N 43/80 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms, as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,2
A01N 43/84 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms, as ring hetero atoms six-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,4
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A control agent exhibiting an excellent control effect on Mesostigmata mites and having as effective components thereof: a specific quinoline derivative compound such as 8–fluoro–2, 3–dimethyl–6–(1,1–dimethylethyl)–4–(methylcarbonyl) oxyquinoline; azoxystrobin; picoxystrobin; pyraclostrobin; kersoxim methyl; trifloxystrobin; metominostrobin; olisastrobin; famoxadone; fluoxastrobin; pyribencarb; cyazofamid; amisulbrom; flutolanil; mepronil; isofetamid; fluopyram; carboxin; thifluzamide; fluxapyroxad; furametpyr; penflufen; penthiopyrad; boscalid; diflumetorim; fluazinam; ferimzone; fenpyroximate; or an acid addition salt of these compounds.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
A01N 47/06 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having no bond to a nitrogen atom containing —O—CO—O— groupsThio-analogues thereof
A process for preparing a diazabicyclooctane compound represented by the following formula (I):
1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c):
wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.
C07D 211/06 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
C07D 295/00 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/43 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems
A61K 31/545 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine
A61K 31/546 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine containing further heterocyclic rings, e.g. cephalothin
C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
C07F 7/08 - Compounds having one or more C—Si linkages
95.
Effective aminoglycoside antibiotic for multidrug-resistant bacteria
A compound represented by the following general formula (I) or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutical composition thereof, and the use thereof to prevent or treat infectious diseases and a method to prevent or treat infectious diseases using those regimen are disclosed. The compound represented by formula (I) has an antibacterial activity against both gram-positive and gram-negative bacteria, and is useful in the prevention or treatment of infectious diseases caused by these bacteria.
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
C07H 15/224 - Cyclohexane rings, substituted by at least two nitrogen atoms with only one saccharide radical directly attached to the cyclohexane rings, e.g. destomycin, fortimicin, neamine
Disclosed are: a compound represented by general formula (I), a pharmaceutically acceptable salt thereof or a solvate of the same; a medicinal composition comprising the same; use of the same for preventing or treating infectious diseases; and a method for preventing or treating infectious diseases, said method comprising using the same. The compound represented by general formula (I), which has an antibacterial activity against both of gram-positive bacteria and gram-negative bacteria, is useful for preventing or treating infectious diseases caused by these bacteria.
Provided is a compound represented by general formula (1) or a pharmaceutically-acceptable salt thereof. [In formula (1), R1 and R2 may be the same or different from each other, and each represents a hydrogen atom, a halogen atom, a hydroxy group, a carboxy group, a cyano group, or an optionally-substituted C1-6 alkyl group or the like; R3 represents a hydrogen atom; R4 represents an optionally-substituted 4- to 10-membered monocyclic heterocyclic group containing 1-4 heteroatoms selected from an oxygen atom, a nitrogen atom, and a sulfur atom; X represents a group represented by -CH2-, -CH2-CH2-, -CH2-CH2-CH2-, or -CH2-O-CH2-; and Z represents a hydrogen atom or a hydroxy group.]
A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
The present invention relates to a benzoxazole derivative with a bicyclic piperazine ring represented by the general formula (1) below or a pharmacologically acceptable salt thereof: In particular, the invention relates to the compound and a pharmacologically acceptable salt thereof which has excellent type IV phosphodiesterase inhibitory activity and metabolic stability, which can be used to prevent and treat various inflammatory diseases, fibroses, central nervous system diseases, cancerous diseases, and metabolic diseases.
A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Provided is a compound or a salt thereof, represented by the formula shown, which has a RORγt inhibitory effect and is useful as a preventive or therapeutic agent for autoimmune diseases, allergies, and the like.
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
100.
Method of producing epirubicin and novel production intermediate thereof
According to the present invention, it is possible to efficiently remove 13-dihydroepi-daunorubicin and 4′-epi-feudomycin, which are typical impurities possibly contained in 4′-epi-daunorubicin as a starting material, by using an organic acid salt of 4′-epi-daunorubicin or a hydrate or solvate thereof as a novel production intermediate, thus making it possible to produce high-purity epirubicin.
C07B 63/02 - PurificationSeparation specially adapted for the purpose of recovering organic compoundsStabilisationUse of additives by treatment giving rise to a chemical modification
C07C 49/423 - Saturated compounds containing a keto group being part of a ring polycyclic a keto group being part of a condensed ring system
C07H 15/252 - Naphthacene radicals, e.g. daunomycins, adriamycins
A61K 31/7008 - Compounds having an amino group directly attached to a carbon atom of the saccharide radical, e.g. D-galactosamine, ranimustine
