PHARMACEUTICAL COMPOSITION FOR TREATING HPV TESTED-POSITIVE CANCER OR HPV PRETESTED-POSITIVE CANCER PATHOLOGICAL CHANGE GENE, AND RECOMBINANT ADENOVIRUS VECTOR
This pharmaceutical composition is for treating human papilloma virus (HPV) tested-positive cancer or an HPV pretested-positive cancer pathological change gene, and includes: Cas guide RNA or a nucleic acid molecule encoding the same; and a Cas9 nickase or a nucleic acid molecule encoding the same. The Cas guide RNA or the nucleic acid molecule encoding the same includes a pair of specific Cas guide RNA or a pair of nucleic acid molecules encoding the same, or a combination of such pairs.
NATIONAL UNIVERSITY CORPORATION TOKAI NATIONAL HIGHER EDUCATION AND RESEARCH SYSTEM (Japan)
MICROBIAL CHEMISTRY RESEARCH FOUNDATION (Japan)
Inventor
Ueno Yoshihito
Kajino Ryohei
Chano Tokuhiro
Furuichi Yasuhiro
Kawade Miwa
Kakizawa Yuri
Sakamoto Shuichi
Abstract
Provided is a nucleoside represented by formula (1). [In formula (1): R1represents a hydroxyl group, a hydroxyl group in which the hydrogen atom is substituted by an alkyl or alkenyl group, or a protected hydroxyl group; R2nnR5R6(wherein n represents 0 or 1, and R5and R6are the same as or different from each other and represent any of a hydrogen atom, a hydroxyl group, a protected hydroxyl group, a mercapto group, a protected mercapto group, a lower alkoxy group, a cyano lower alkoxy group, an amino group or a substituted amino group, provided that when n is 1, then R5and R6cannot both be hydrogen atoms); R3represents a hydrogen atom, a protecting group of the hydroxyl group, a phosphate group, a protected phosphate group or a phosphorothioate group; R4represents a hydroxyl group, a protected hydroxyl group, an azide group or NHR7; R7 represents a hydrogen atom or a protecting group of the amino group; and B represents a purine base or a pyrimidine base.]
TOKYO UNIVERSITY OF PHARMACY AND LIFE SCIENCES (Japan)
MICROBIAL CHEMISTRY RESEARCH FOUNDATION (Japan)
Inventor
Sumiya, Tatsunobu
Nishigaya, Yosuke
Namie, Ryosuke
Hashimoto, Noriaki
Ito, Akihiro
Shirai, Fumiyuki
Kikuzato, Ko
Yoshida, Minoru
Abstract
A compound represented by the general formula (I) given below or a pharmacologically acceptable salt thereof has been found to have a strong G9a inhibitory effect. The compound (I) or the pharmacologically acceptable salt thereof inhibits G9a and thereby has high usefulness for the treatment, prevention or suppression of various pathological conditions (proliferative disease such as cancer, β-globin abnormality, fibrosis, pain, neurodegenerative disease, Prader-Willi syndrome, malaria, viral infection, myopathy, autism, etc.).
A compound represented by the general formula (I) given below or a pharmacologically acceptable salt thereof has been found to have a strong G9a inhibitory effect. The compound (I) or the pharmacologically acceptable salt thereof inhibits G9a and thereby has high usefulness for the treatment, prevention or suppression of various pathological conditions (proliferative disease such as cancer, β-globin abnormality, fibrosis, pain, neurodegenerative disease, Prader-Willi syndrome, malaria, viral infection, myopathy, autism, etc.).
C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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 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 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
Provided are a protective agent, a surfactant composition, a composition for blood sugar level control, an autophagy inducing agent, a stain for mycobacteria, or a protein extraction agent characterized by containing a compound represented by general formula (1).
A61K 31/7008 - Compounds having an amino group directly attached to a carbon atom of the saccharide radical, e.g. D-galactosamine, ranimustine
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 43/00 - Drugs for specific purposes, not provided for in groups
The following are provided: a novel adenovirus vector having a shortened backbone; a nucleic acid vector expressing five or more Cas guide RNA; a nucleic acid vector containing a Cas protein-coding gene and a Cas guide RNA expression unit; a composition for genome editing containing these vectors; and a gene therapeutic method using these.
TOKYO UNIVERSITY OF PHARMACY AND LIFE SCIENCES (Japan)
MICROBIAL CHEMISTRY RESEARCH FOUNDATION (Japan)
Inventor
Sumiya, Tatsunobu
Nishigaya, Yosuke
Namie, Ryosuke
Hashimoto, Noriaki
Ito, Akihiro
Shirai, Fumiyuki
Kikuzato, Ko
Yoshida, Minoru
Abstract
It was found that a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof has potent G9a inhibitory activity. Because of the ability to inhibit G9a, the compound (I) or a pharmaceutically acceptable salt thereof is highly useful in treatment, prevention or suppression of a variety of diseases (including proliferative diseases such as cancer, ß-globin abnormalities, fibrosis, pain, neurodegenerative diseases, Prader-Willi syndrome, malaria, viral infections, myopathy, and autism).
A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
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 31/444 - 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 31/4545 - 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
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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
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
A61P 25/00 - Drugs for disorders of the nervous system
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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 405/12 - 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 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
TOKYO UNIVERSITY OF PHARMACY AND LIFE SCIENCE (Japan)
MICROBIAL CHEMISTRY RESEARCH FOUNDATION (Japan)
Inventor
Sumiya Tatsunobu
Nishigaya Yosuke
Namie Ryosuke
Hashimoto Noriaki
Ito Akihiro
Shirai Fumiyuki
Kikuzato Ko
Yoshida Minoru
Abstract
It was found that a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof has potent G9a inhibitory activity. Because of the ability to inhibit G9a, the compound (I) or a pharmaceutically acceptable salt thereof is highly useful in treatment, prevention or suppression of a variety of diseases (including proliferative diseases such as cancer, β-globin abnormalities, fibrosis, pain, neurodegenerative diseases, Prader-Willi syndrome, malaria, viral infections, myopathy, and autism).
A61P 35/02 - Antineoplastic agents specific for leukemia
A61P 35/04 - Antineoplastic agents specific for metastasis
A61P 43/00 - Drugs for specific purposes, not provided for in groups
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 405/12 - 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 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
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 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
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 31/444 - 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 31/4545 - 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
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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
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
8.
Catalyst, method for forming amide bond, and method for producing amide compound
B01J 31/02 - Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07F 5/05 - Cyclic compounds having at least one ring containing boron but no carbon in the ring
9.
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
The present invention relates to: a novel adenovirus vector that has a shortened backbone; a nucleic acid vector that expresses 5 or more Cas guide RNAs; a nucleic acid vector that comprises a Cas protein and a Cas guide RNA-expressing unit; and a composition for editing a genome that comprises these vectors; and a method for gene therapy using same.
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
Provided is a catalyst represented by general formula (1). In general formula (1), R1-R14 each independently represent a hydrogen atom or a substituent.
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 233/11 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
C07C 233/13 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
C07C 233/22 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
C07C 233/29 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
C07C 269/06 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
13.
Catalyst, production method therefor, and method for producing optically active anti-1, 2-nitroalkanol compound
A catalyst including: neodymium; sodium; and a ligand, which is a compound expressed by Structural Formula (1) below, wherein the neodymium and the ligand form a complex at a molar ratio of 1:2 (neodymium:ligand):
C07C 201/12 - Preparation of nitro compounds by reactions not involving the formation of nitro groups
C07C 205/16 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by hydroxy groups having nitro groups and hydroxy groups bound to acyclic carbon atoms of a carbon skeleton containing six-membered aromatic rings
C07C 205/32 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups having nitro groups bound to acyclic carbon atoms and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07C 205/54 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups bound to acyclic carbon atoms and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07C 237/04 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
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.
The purpose of the present invention is to provide a method capable of analyzing an SMN protein nuclear body that serves as a more highly reliable biomarker. The method according to the present invention is a method for analyzing the expression of an SMN protein nuclear body, and comprises the steps of: labeling at least one surface antigen marker for blood-derived nucleated cells with at least one labeling antibody in a sample containing the nucleated cells; labeling the SMN protein in the nucleated cells; labeling the nuclei of the nucleated cells; selecting one cell mass from among multiple cell masses of the nucleated cells, the multiple cell masses being cell masses in which the nucleus and the SMN protein are labeled and which have been classified on the basis of the surface antigen marker labeled with the labeling antibody or the like; and subjecting the selected cell mass to analysis on the expression of the SMN protein nuclear body on the basis of the labeling of the SMN protein. The method involves carrying out imaging flow cytometry using an objective lens at a specific magnification.
A method for producing an optically active α-trifluoromethyl-β-amino acid derivative, the method including: allowing a compound represented by the following General Formula (1) and a compound represented by the following General Formula (2) to react in the presence of a copper-optically active phosphine complex obtained from a copper compound and an optically active phosphine compound, to thereby obtain an optically active α-trifluoromethyl-β-amino acid derivative represented by the following General Formula (3):
C07D 401/02 - 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
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
Provided is a catalyst represented by general formula (1), where R1-R16 in the general formula (1) individually represent a hydrogen atom or a substituent independently of each other.
B01J 31/02 - Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 233/05 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 233/13 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
C07C 233/29 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
C07C 233/59 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
C07C 233/65 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
C07C 235/34 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
This catalyst contains neodymium, sodium, and a ligand which is a compound represented by structural formula (1), wherein the neodymium and the ligand form a complex at a molar ratio of 1 : 2 (neodymium : ligand).
C07C 201/12 - Preparation of nitro compounds by reactions not involving the formation of nitro groups
C07C 205/16 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by hydroxy groups having nitro groups and hydroxy groups bound to acyclic carbon atoms of a carbon skeleton containing six-membered aromatic rings
C07C 205/32 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups having nitro groups bound to acyclic carbon atoms and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07C 205/54 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups bound to acyclic carbon atoms and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07C 237/04 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
Provided is a method for efficiently producing a compound represented by formula II, namely (2S)-2-hydroxyarbekacin or a salt thereof from (2S)-2-hydroxydibekacin represented by formula I or a salt thereof, which is characterized by using a compound represented by formula III or a salt thereof as a synthetic intermediate. (In the formulae, R1 represents an optionally substituted alkyloxycarbonyl group or an optionally substituted arylalkyloxycarbonyl group.)
C07H 15/234 - Cyclohexane rings, substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings attached to non-adjacent ring carbon atoms of the cyclohexane rings, e.g. kanamycins, tobramycin, nebramycin, gentamicin A2
Provided is a method for stably producing (2S)-2-hydroxydibekacin, said method being characterized by the use of 2-hydroxykanamycin C or 2-hydroxykanamycin B as a starting material or synthetic intermediate.
C07H 15/234 - Cyclohexane rings, substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings attached to non-adjacent ring carbon atoms of the cyclohexane rings, e.g. kanamycins, tobramycin, nebramycin, gentamicin A2
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
C07B 51/00 - Introduction of protecting groups or activating groups, not provided for in groups
Provided is a method for stably producing (2S)-2-hydroxydibekacin, said method being characterized by the use of 2-hydroxykanamycin C or 2-hydroxykanamycin B as a starting material or synthetic intermediate.
C07H 15/234 - Cyclohexane rings, substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings attached to non-adjacent ring carbon atoms of the cyclohexane rings, e.g. kanamycins, tobramycin, nebramycin, gentamicin A2
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
METHOD FOR DETERMINING IMMUNE STATUS, METHOD FOR PREDICTING INCREASE IN NUMBER OF CD4+ T CELLS, METHOD FOR PREDICTING DECREASE IN NUMBER OF CD4+ T CELLS, AND KIT THEREFOR
Provided is a method for determining the immune status of a patient after starting treatment using an anti-human immunodeficiency virus drug, said method including a detection step for detecting a transcript up to 200 bases from a transcription start point of human immunodeficiency virus RNA in peripheral blood mononuclear cells, and a step for evaluating whether the patient's immunity is in an activated state using the detection or non-detection of the transcript as an index.
Disclosed are: a compound represented by general formula (I), or a pharmaceutically acceptable salt of the compound, or a solvate of the compound or the pharmaceutically acceptable salt; a pharmaceutical composition containing the compound, the pharmaceutically acceptable salt or the solvate; a use of the compound, the pharmaceutically acceptable salt or the solvate for the prevention or treatment of infectious diseases; and a method for preventing or treating infectious diseases using the compound, the pharmaceutically acceptable salt or the solvate. The compound represented by general formula (I) has an antibacterial activity against both gram-positive bacteria and gram-negative bacteria, and is therefore useful for the prevention or treatment of infectious diseases induced by these bacteria.
C07H 15/12 - Acyclic radicals, not substituted by cyclic structures attached to a nitrogen atom of a saccharide radical
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 15/234 - Cyclohexane rings, substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings attached to non-adjacent ring carbon atoms of the cyclohexane rings, e.g. kanamycins, tobramycin, nebramycin, gentamicin A2
27.
EFFECTIVE AMINOGLYCOSIDE ANTIBIOTIC FOR MULTIDRUG-RESISTANT BACTERIA
Disclosed are: a compound represented by general formula (I), or a pharmaceutically acceptable salt of the compound, or a solvate of the compound or the pharmaceutically acceptable salt; a pharmaceutical composition containing the compound, the pharmaceutically acceptable salt or the solvate; a use of the compound, the pharmaceutically acceptable salt or the solvate for the prevention or treatment of infectious diseases; and a method for preventing or treating infectious diseases using the compound, the pharmaceutically acceptable salt or the solvate. The compound represented by general formula (I) has an antibacterial activity against both gram-positive bacteria and gram-negative bacteria, and is therefore useful for the prevention or treatment of infectious diseases induced by these bacteria.
C07H 15/12 - Acyclic radicals, not substituted by cyclic structures attached to a nitrogen atom of a saccharide radical
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 15/234 - Cyclohexane rings, substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings attached to non-adjacent ring carbon atoms of the cyclohexane rings, e.g. kanamycins, tobramycin, nebramycin, gentamicin A2
This method for producing a compound represented by general formula (1) comprises a reaction step for reacting a compound represented by general formula (2) with a compound represented by general formula (3) in the presence of a catalyst containing an asymmetric ligand represented by general formula (A), to obtain the compound represented by general formula (1). However, in general formula (1) and general formula (2), R1 represents either a hydrogen atom or a protecting group for an amino group and R2 represents either a hydrogen atom or a protecting group for an amino group. In general formula (1) and general formula (3), R11 represents an optionally substituted aromatic group, R12 represents an optionally substituted aromatic group, and R13 represents either a hydrogen atom or a protecting group for an amino group. However, in general formula (A), R represents any one of an alkyl group having 1-6 carbon atoms, an aryl group, a substituted aryl group, an aralkyl group, and a ring-substituted aralkyl group.
A compound represented by structural formula (A) or (B); a method for producing the compound; a microorganism having an ability of producing the compound represented by the formula (A) or (B); and a compound-containing composition and an anti-cancer agent, each of which contains the compound.
C12P 1/02 - Preparation of compounds or compositions, not provided for in groups , by using microorganisms or enzymesGeneral processes for the preparation of compounds or compositions by using microorganisms or enzymes by using fungi
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
Provided is a cancer cell growth inhibitor, which includes at least one selected from the compounds represented by structural formulas (1) through (8), wherein the cancer cells are at least cancer cells that over-express wild epithelial growth factor receptor or cancer cells that express epithelial growth factor receptor mutant vIII.
C07D 241/44 - Benzopyrazines 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 to carbon atoms of the hetero ring
C12Q 1/02 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving viable microorganisms
31.
NOVEL COMPOUND, METHOD FOR PRODUCING SAME, AND USE THEREOF
An autophagy inducing agent that comprises at least one member selected from a compound represented by structural formula (A), a compound represented by structural formula (B), and a compound represented by structural formula (C).
A61K 31/7028 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
A61K 31/7032 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a polyol, i.e. compounds having two or more free or esterified hydroxy groups, including the hydroxy group involved in the glycosidic linkage, e.g. monoglucosyl-diacylglycerides, lactobionic acid, gangliosides
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
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 39/06 - Free radical scavengers or antioxidants
A61P 43/00 - Drugs for specific purposes, not provided for in groups
32.
OPTICALLY ACTIVE Α-TRIFLUORMETHYL-Β-AMINO ACID DERIVATIVE PRODUCTION METHOD
Provided is a production method for an optically active α-trifluormethyl-β-amino acid derivative whereby: a compound indicated by general formula (1) and a compound indicated by general formula (2) are reacted in the presence of a copper-optically active phosphine complex comprising a copper compound and an optically active phosphine compound; and an optically active α-trifluormethyl-β-amino acid derivative indicated by general formula (3) is obtained.
C07B 57/00 - Separation of optically-active organic compounds
C07C 269/06 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
A catalyst, which is obtained by mixing a compound expressed by the following Structural Formula (1), a nitroalkane compound, a neodymium-containing compound, a sodium-containing compound, and a carbon structure:
C07C 201/12 - Preparation of nitro compounds by reactions not involving the formation of nitro groups
C07C 205/02 - Compounds containing nitro groups bound to a carbon skeleton having nitro groups bound to acyclic carbon atoms of a saturated carbon skeleton
C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
B01J 31/02 - Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
A method for producing an optically active anti-1,2-nitroalkanol compound, the method including a supplying step for continuously supplying an aldehyde compound and a C2 or higher nitroalkane compound to a reaction container, a reaction step for reacting the aldehyde compound and the C2 or higher nitroalkane compound in the reaction container and obtaining an optically active anti-1,2-nitroalkanol compound, and a discharge step for continuously discharging the optically active anti-1,2-nitroalkanol compound from the reaction container, and the reaction container including a catalyst obtained by mixing a compound represented by structural formula (1), anitroalkane compound, a neodymium-containing compound, a sodium-containing compound, and a carbon structure.
C07C 201/12 - Preparation of nitro compounds by reactions not involving the formation of nitro groups
C07C 205/32 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups having nitro groups bound to acyclic carbon atoms and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
Compound; tautomer and geometric isomer thereof; salt of said compound, tautomer, or geometric isomer; method for manufacturing said compound, tautomer, isomer, or salt; antimicrobial agent; and anti-infective drug
The present invention provides compounds belonging to 3-acyloxyindole compounds or 3-acyl-4-hydroxycoumarin compounds, a tautomer or geometric isomer thereof, or a salt thereof and methods for producing the same, which compounds are useful as antibacterial agent and as therapeutic drugs against infectious diseases.
C07D 311/56 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms in positions 2 and 4 without hydrogen atoms in position 3
Provided is a method for detecting the expression of SMN protein, said method comprises: a step for labeling SMN protein in a sample, said sample containing nucleated cells derived from blood; a step for labeling the nuclei of the nucleated cells in the sample; a step for selecting cell masses wherein the nuclei of the nucleated cells and the SMN protein are labeled; and a step for detecting the expression of the SMN protein on the basis of the label bound to the SMN protein in the cell masses that are selected above.
G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers
G01N 33/49 - Physical analysis of biological material of liquid biological material blood
C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
38.
COMPOUND AND METHOD FOR MANUFACTURING SAME, AND METHOD FOR MANUFACTURING VORICONAZOLE
A method for manufacturing voriconazole, said method including: a step for converting a compound represented by general formula (1) into a compound represented by general formula (2); a step for converting the compound represented by general formula (2) into a compound represented by general formula (3); and a step for converting the compound represented by general formula (3) into voriconazole. In general formula (1), R1 represents either a hydrogen atom or a protecting group of a hydroxyl group, and R2 represents a halogen atom. In general formula (2), R3 and R4 each independently represent either a hydrogen atom or a protecting group of a hydroxyl group, and R5 represents a halogen atom. In general formula (3), X represents any of the divalent groups represented by the structural formulae.
C07D 403/06 - 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 only aliphatic carbon atoms
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
39.
COMPOUND, MANUFACTURING METHOD THEREFOR, AND METHOD FOR MANUFACTURING OPTICALLY ACTIVE α-AMINOPHOSPHONATE DERIVATIVE
A manufacturing method for a compound represented by general formula (1), the method comprising a reaction process for reacting a compound represented by general formula (3) with a compound represented by general formula (4). general formula (1) In general formula (1), R1 and R2 represent either aliphatic groups that may have a substituent or aromatic groups that may have a substituent (provided R1 and R2 are different groups). R3 represents an aromatic group that may have a substituent. R4 represents either an aliphatic group that may have a substituent or an aromatic group that may have a substituent. general formula (3) In general formula (3), R1 and R2 represent either aliphatic groups that may have a substituent or aromatic groups that may have a substituent (provided R1 and R2 are different groups). R3 represents an aromatic group that may have a substituent. general formula (4) In general formula (4), R4 represents either an aliphatic group that may have a substituent or an aromatic group that may have a substituent.
COLORADO STATE UNIVERSITY RESEARCH FOUNDATION (USA)
Inventor
Ishizaki, Yoshimasa
Igarashi, Masayuki
Brennan, Patrick Joseph
Crick, Dean Calvin
Abstract
A combined antibacterial agent for acid-fast bacteria that combines an activity inhibitor of WecA or an ortholog thereof, with an activity inhibitor of MurX or an ortholog thereof and/or an RNA synthesis inhibitor; a screening method for antibacterial agents for acid-fast bacteria; and an activity inhibitor of WecA or an ortholog thereof.
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 31/7072 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
Provided are: a compound represented by structural formula (1); a production method therefor; a microorganism capable of producing said compound; and a compound-containing composition, an anticancer agent, and an anti-Helicobacter pylori agent which include said compound.
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 215/58 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
Provided are: a compound represented by any one from among structural formulae (1) to (13); a production method therefor; and a compound-containing composition, an anticancer agent, and an anti-Helicobacter pylori agent which include said compound.
A catalyst which is obtained by mixing a compound represented by structural formula (1), a nitroalkane compound, a neodymium-containing compound, a sodium-containing compound and a carbon structure.
C07C 201/12 - Preparation of nitro compounds by reactions not involving the formation of nitro groups
C07C 205/15 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by hydroxy groups having nitro groups and hydroxy groups bound to acyclic carbon atoms of a saturated carbon skeleton
C07C 205/16 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by hydroxy groups having nitro groups and hydroxy groups bound to acyclic carbon atoms of a carbon skeleton containing six-membered aromatic rings
C07C 205/26 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by hydroxy groups and being further substituted by halogen atoms
C07C 205/32 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups having nitro groups bound to acyclic carbon atoms and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07C 205/02 - Compounds containing nitro groups bound to a carbon skeleton having nitro groups bound to acyclic carbon atoms of a saturated carbon skeleton
C07C 237/36 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
44.
ANTICANCER AGENT, AND COMBINATION USE ANTICANCER AGENT
Provided are an anticancer agent containing ellagitannin, and a combination use anticancer agent in which the anticancer agent containing ellagitannin and an anticancer agent containing anthracycline are used in combination.
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 36/00 - Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
45.
E-CADHERIN BINDING AGENT, PROTEIN SYNTHESIS INHIBITOR, CANCER CELL GROWTH INHIBITOR, AND ANTITUMORAL AGENT
An E-cadherin binding agent containing GAPDH protein and/or analogous proteins, a protein synthesis inhibitor containing the E-cadherin binding agent, a cancer cell growth inhibiting drug containing E-cadherin binding agent and/or the protein synthesis inhibitor, and an antitumoral agent containing the cancer cell growth inhibitor.
COMPOUND; TAUTOMER AND GEOMETRIC ISOMER THEREOF; SALT OF SAID COMPOUND, TAUTOMER, OR GEOMETRIC ISOMER; METHOD FOR MANUFACTURING SAID COMPOUND, TAUTOMER, ISOMER, OR SALT; ANTIMICROBIAL AGENT; AND ANTI-INFECTIVE DRUG
A compound characterized in being represented by any of general formulae (1) to (5); a tautomer or a geometric isomer thereof; a salt of the compound, tautomer, or geometric isomer; and the like. (In the formulae, X1 represents a single bond or a C1-8 alkylene group; Y1 represents a single bond, -O-, -NHCO-, etc.; Z1 represents a C8-30 alkyl group optionally having a halogen atom; X2 represents a single bond, -CO-, etc.; Y2 represents a hydrogen atom or an optionally-substituted C1-30 hydrocarbon group; Z2 represents a C5-30 hydrocarbon group optionally having a halogen atom; X3 represents a single bond, or -NH-; Y3 represents -O-, -NH-, etc.; X4 represents a C1-8 alkylene group; Z represents a hydrogen atom, a halogen atom, a C1-6 alkoxy group, or a C1-20 hydrocarbon group; R1 represents an optionally-substituted C1-30 hydrocarbon group; and Z3 represents a halogen atom, a C1-6 alkoxy group, or a C1-20 hydrocarbon group).
C07D 311/56 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms in positions 2 and 4 without hydrogen atoms in position 3
47.
COMPOUND, METHOD FOR PRODUCING SAID COMPOUND, METHOD FOR PRODUCING ACETATE DERIVATIVE, METHOD FOR PRODUCING ATORVASTATIN, AND METHOD FOR COLLECTING ASYMMETRIC LIGAND
A compound represented by general formula (1). In general formula (1), R1 represents either one of a protective group for a hydroxy group and a hydrogen atom, and R2 and R3 independently represent a protective group for an amino group.
C07C 217/28 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines
C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
C07C 215/10 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
C07C 229/30 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and unsaturated
C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
C07D 319/06 - 1,3-DioxanesHydrogenated 1,3-dioxanes not condensed with other rings
A compound represented by general formula (I); a method for producing the compound; a microorganism capable of producing the compound; a pharmaceutical composition containing the compound; an anti-tumor agent comprising the pharmaceutical composition; and others. In general formula (I), X represents a group represented by general formula (IA) or general formula (IB). In general formula (IA) and general formula (IB), * represents a bond.
A treatment agent for salt-containing organic waste liquid, the treatment agent including: Scuticociliatida, wherein the treatment agent treats salt-containing organic waste liquid; and a treatment method for salt-containing organic waste liquid, the treatment method including: bringing Scuticociliatida and salt-containing organic waste liquid into contact with each other to treat the salt-containing organic waste liquid.
MEDICAL & BIOLOGICAL LABORATORIES CO., LTD. (Japan)
Inventor
Kawada Manabu
Inoue Hiroyuki
Sakamoto Shuichi
Kajikawa Masunori
Sugiura Masahito
Urano Sakiko
Abstract
In order to provide an antibody that can detect a target molecules useful for cancer treatment or the like and that can specifically bind to said molecules, and an anti-cancer agent that uses said antibody as an active component, a comparison between prostate cancer cell lines (between LNCaP-CR cells and LNCaP cells) was carried out using SST-REX, and CXADR was identified as a molecule that is involved in tumorigenicity and the like. Furthermore, monoclonal antibodies against CXADR were produced, and because the monoclonal antibodies were found to exhibit anti-cancer activity, ADCC activity, CDC activity and the like, it was discovered that the antibody that binds to the epitope present at position 181-230 on human-derived CXADR protein exhibits an anti-cancer effect against prostate cancer cells, pancreatic cancer cells and colorectal cancer cells. It was also demonstrated that said antibody has ADCC activity and CDC activity. The structure of the variable region of the heavy and light chains of the antibody was successfully determined.
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
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
C12N 15/02 - Preparation of hybrid cells by fusion of two or more cells, e.g. protoplast fusion
Provided is a compound represented by general formula (1). (1) In general formula (1), R1 is either a protecting group for a hydroxyl group or a hydrogen atom. R2 is either a methyl group or an ethyl group.
C07C 323/12 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
A compound represented by structural formula (A) or a salt thereof. The compound or the salt thereof is produced suitably from a microorganism belonging to the genus Saccharothrix and can be used suitably as a prostaglandin production inhibitor.
C07H 15/203 - Monocyclic carbocyclic rings other than cyclohexane ringsBicyclic carbocyclic ring systems
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
A tripropeptin derivative represented by general formula (1) or (2), or a pharmacologically acceptable salt thereof. In general formula (1), R1 represents an organic group having 1-20 carbon atoms. In general formula (2), R2 represents an organic group having 1-20 carbon atoms.
Provided is a compound represented by general formula (1). Also provided is a method for producing a compound represented by formula (1) that comprises a reaction step for reacting a compound represented by general formula (2), a compound represented by general formula (3), and a compound represented by general formula (4). In general formulas (1) through (4), R1 is a protector group of a carboxyl group or a hydrogen atom; R2 and R3 are each independently a protector group of an amino group or a hydrogen atom; and R4 is a protector group of a carboxyl group or a hydrogen atom.
C07C 229/30 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and unsaturated
C07C 227/10 - Formation of amino groups in compounds containing carboxyl groups with simultaneously increasing the number of carbon atoms in the carbon skeleton
C07C 227/16 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions not involving the amino or carboxyl groups
C07C 227/32 - Preparation of optical isomers by stereospecific synthesis
C07C 229/48 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms of the same non-condensed ring
C07C 269/04 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups from amines with formation of carbamate groups
C07C 269/06 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
C07C 271/24 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
THIOAMIDE COMPOUND, METHOD FOR PRODUCING THIOAMIDE COMPOUND, METHOD FOR PRODUCING [(4R,6R)-6-AMINOETHYL-1,3-DIOXANE-4-YL]ACETATE DERIVATIVE, AND METHOD FOR PRODUCING ATORVASTATIN
Provided is the thioamide compound represented by general formula (1). In general formula (1): R1 represents -OR11 or -NR12R13; R2 and R3 each independently represent a protecting group of an amide group or a hydrogen atom; R11 represents a protecting group of a hydroxide group or a hydrogen atom; and R12 and R13 each independently represent a protecting group of an amino group or a hydrogen atom (moreover, R12 and R13 may together form a ring-structured protecting group).
C07C 327/42 - Amides of thiocarboxylic acids having carbon atoms of thiocarboxamide groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of a saturated carbon skeleton
A61K 31/40 - 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
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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
C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
A peptide comprising at least any one amino acid sequence selected from the amino acid sequences represented by SEQ ID NO:1 to SEQ ID NO:4 shown below. ALGDSLYGAASLN (SEQ ID NO:1) MTVDNPASTTNKDKLFSVWK (SEQ ID NO:2) PGAVPEK (SEQ ID NO:3) STKDLTTY (SEQ ID NO:4)
AGENT FOR TREATMENT OF SALT-CONTAINING ORGANIC LIQUID WASTE, SALT CONCENTRATION REDUCING AGENT, METHOD FOR TREATMENT OF SALT-CONTAINING ORGANIC LIQUID WASTE, AND ENTRAPPING IMMOBILIZATION CARRIER
An agent for treating a salt-containing organic liquid waste, which contains at least a Scuticociliatida ciliate and can treat the salt-containing organic liquid waste; and a method for treating a salt-containing organic liquid waste, comprising an salt-containing organic liquid waste treatment step of bringing a Scuticociliatida ciliate into contact with the salt-containing organic liquid waste to thereby treat the salt-containing organic liquid waste.
Disclosed is a microorganism belonging to the genus Bacillus, which is characterized by being a strain that is selected from among Bacillus subtilis strain 104-1-3-1 (Accession No. NITE P-680) and strains induced therefrom and by producing a thrombolytic enzyme that decomposes waste.
A method for treating an individual infected with XDR-TB, the method including administering to the individual an anti-XDR-TB drug which comprises a compound having a structure expressed by Structural Formula (1) below:
C07H 19/067 - Pyrimidine radicals with ribosyl as the saccharide radical
A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/7072 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
61.
READ THROUGH INDUCER, AND THERAPEUTIC AGENT FOR NONSENSE-MUTATION-TYPE GENETIC DISEASES
A read through inducer for an immature termination codon formed by a nonsense mutation, which comprises a compound represented by structure formula (A); and a therapeutic agent for nonsense-mutation-type genetic diseases, which comprises the read through inducer.
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
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 9/02 - Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
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 37/06 - Immunosuppressants, e.g. drugs for graft rejection
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07H 15/234 - Cyclohexane rings, substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings attached to non-adjacent ring carbon atoms of the cyclohexane rings, e.g. kanamycins, tobramycin, nebramycin, gentamicin A2
62.
ANTIBACTERIAL AGENT FOR DRUG-RESISTANT BACTERIA, METHOD FOR SCREENING FOR SAME, AND USE OF SAME
An antibacterial agent for drug-resistant bacteria, which comprises either nibomycin and/or a derivative thereof and is effective on drug-resistant bacteria each having resistance to at least one drug.
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A novel compound represented by general formula (1) and salts thereof, which are obtained by subjecting amycolamicin obtained from a microorganism belonging to the genus Amycolatopsis or a salt thereof to decomposition under acid conditions, and which exhibit inhibitory activity against cell proliferation. In general formula (1), R is a hydrogen atom or an alkyl group.
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
A61K 31/4025 - 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
NOVEL COMPOUND, HISTONE ACETYLASE INHIBITOR, NUCLEAR RECEPTOR TRANSCRIPTION ACTIVATION INHIBITOR, DEUTEROMYCETES BELONGING TO GENUS PENICILLIUM, AND PRODUCTION PROCESS
Disclosed are: a compound represented by structural formula (1) or a pharmacologically acceptable salt thereof; a histone acetylase inhibitor; a nuclear receptor transcription activation inhibitor; a deuteromycetes belonging to the genus Penicillium, which can produce the compound; a process for producing the compound, which comprises a culturing step of culturing the microorganism and a collection step of collecting the compound from a culture produced in the culturing step; and others.
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
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 11/00 - Drugs for disorders of the respiratory system
C07K 5/027 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link in which at least a gamma-amino acid is involved, e.g. statine
C12P 1/02 - Preparation of compounds or compositions, not provided for in groups , by using microorganisms or enzymesGeneral processes for the preparation of compounds or compositions by using microorganisms or enzymes by using fungi
C12P 17/00 - Preparation of heterocyclic carbon compounds with only O, N, S, Se, or Te as ring hetero atoms
65.
NOVEL COMPOUND AMYCOLAMICIN, METHOD FOR PRODUCTION THEREOF, AND USE THEREOF
Disclosed are: a novel compound which has an excellent antibacterial activity against a wide variety of pathogenic bacteria including drug-resistant bacteria and bacteria causing pneumonia in domestic livestock, a tautomer of the compound, or a salt of the compound or the tautomer; a method for producing the compound, the tautomer or the salt; and others. Specifically disclosed are: a compound characterized by being represented by structural formula (1), a tautomer of the compound, or a salt of the compound or the tautomer; a method for producing the compound, the tautomer or the salt, which is characterized by culturing a microorganism belonging to the genus Amycolatopsis and capable of producing the compound, the tautomer or the salt to produce a culture, and collecting the compound, the tautomer or the salt from the culture; and others.
C12P 17/16 - Preparation of heterocyclic carbon compounds with only O, N, S, Se, or Te as ring hetero atoms containing two or more hetero rings
A61K 31/4025 - 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
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
An anti-XDR-TB drug including a compound having a structure expressed by Structural Formula (1) below; an anti-MDR-TB drug including a compound having a structure expressed by Structural Formula (1) below; and a combination anti-tuberculosis drug including a drug containing a compound having a structure expressed by Structural Formula (1) below, and at least one anti-tuberculosis drug selected from an anti-tuberculosis drug containing rifampicin (RFP) and an anti-tuberculosis drug containing isonicotinic acid hydrazide (INH). (see formula 1)
A61K 31/7072 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
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
A61P 31/06 - Antibacterial agents for tuberculosis
C07H 19/067 - Pyrimidine radicals with ribosyl as the saccharide radical
67.
ANTI-XDR-TB AGENT, ANTI-MDR-TB AGENT, AND COMBINED ANTI-TUBERCULOUS AGENT
Disclosed are: an anti-XDR-TB agent having excellent pharmacological efficacy against extremely drug-resistant tuberculosis bacteria; an anti-MDR-TB agent having excellent pharmacological efficacy against multi-drug-resistant tuberculosis bacteria; and a combined anti-tuberculous agent having excellent pharmacological efficacy against tuberculosis bacteria having susceptibility to existing anti-tuberculous agents. Specifically disclosed are: an anti-XDR-TB agent comprising a compound represented by structural formula (1); an anti-MDR-TB agent comprising a compound represented by structural formula (1); and a combined anti-tuberculous agent which comprises a combination of a pharmaceutical agent comprising a compound represented by structural formula (1) and at least one anti-tuberculous agent selected from an anti-tuberculous agent comprising rifampicin (RFP) and an anti-tuberculous agent comprising isonicotinic acid hydrazide (INH).
C07H 19/067 - Pyrimidine radicals with ribosyl as the saccharide radical
A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/7072 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
A61P 31/06 - Antibacterial agents for tuberculosis
A61P 43/00 - Drugs for specific purposes, not provided for in groups
68.
ANTI-XDR-TB AGENT, ANTI-MDR-TB AGENT, AND COMBINED ANTI-TUBERCULOSIS AGENT
An anti-XDR-TB drug including a compound having a structure expressed by Structural Formula (1) below; an anti-MDR-TB drug including a compound haying a structure expressed by Structural Formula (1) below; and a combination anti-tuberculosis drug including a drug containing a compound having a structure expressed by Structural Formula (1) below, and at least one anti-tuberculosis drug selected from an anti-tuberculosis drug containing rifampicin (RFP) and an anti-tuberculosis drug containing isonicotinic acid hydrazide (INH). (see Structural Formula (1))
A61K 31/7072 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
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
A61P 31/06 - Antibacterial agents for tuberculosis
69.
NOVEL COMPOUND CERAMIDASTIN, PROCESS FOR PRODUCTION THEREOF, AND USE THEREOF
Disclosed are: a novel compound having an excellent inhibitory activity against at least one of a neutral ceramidase and an alkaline ceramidase; a process for producing the compound; a novel microorganism capable of producing the novel compound; and a ceramidase inhibitor or a pharmaceutical composition comprising the novel compound. Specifically disclosed are: a compound characterized by being represented by structural formula (1); a process for producing the compound, which is characterized by comprising a culture step of culturing a microorganism belonging to the genus Penicillium and capable of producing the compound and a collection step of collecting the compound from a culture obtained in the culture step; and others.
C12P 17/18 - Preparation of heterocyclic carbon compounds with only O, N, S, Se, or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
Disclosed are: a novel compound which exhibits an excellent antibacterial activity against a wide variety of pathogenic bacteria including drug-resistant bacteria and plant-disease-causing bacteria, or exhibits an inhibitory activity against enzymes secreted from the bacteria, through the inhibition of the two-component regulatory systems of the bacteria; a method for producing the compound; a novel microorganism capable of producing the novel compound; and a compound-containing composition, an antibacterial agent, or an enzymatic activity inhibitor each utilizing the novel compound. Specifically disclosed are: a compound represented by the structural formula (1); a compound represented by the structural formula (2); a method for producing each of the compounds, which comprises a culture step of culturing a microorganism belonging to the genus Streptomyces and capable of producing the desired compound and a collection step of collecting the desired compound from the culture produced in the culture step; and others.
C12P 17/12 - Nitrogen as only ring hetero atom containing a six-membered hetero ring
A01N 43/36 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings
A01N 63/02 - Substances produced by, or obtained from, microorganisms or animals
A61K 31/4015 - 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 having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 207/44 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
This invention relates to solvated and non-solvated crystalline forms of 20,23- dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from)such crystalline forms, methods for making medicaments comprising (or derived from)such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.
This invention relates to solvated and non-solvated crystalline forms of 20,23- dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from)such crystalline forms, methods for making medicaments comprising (or derived from)such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.
It is intended to provide an excellent antitumor agent which can specifically and effectively inhibit the proliferation of tumor cells in vivo and shows a high safety with little side effect and a medicinal composition which contains the antitumor agent as described above. Namely, an antitumor agent characterized by comprising at least one of a sulfostin-related compound represented by the following general formula (I), a pharmacologically acceptable salt thereof and a hydrate of the same as the active ingredient and a medicinal composition which contains the antitumor agent. General formula (I) wherein n stands for an integer of from 1 to 3.
C07D 211/92 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
Disclosed is an antibacterial agent having an excellent antibacterial activity against Mycobacterium avium subsp. paratuberculosis. The antibacterial agent has an antibacterial activity against comprises a caprazamycin derivative represented by the general formula (II) or the like. (II) wherein Me represents a methyl group; R1 represents a linear or substantially linear C5-21 alkyl group, a linear or substantially linear C5-21 alkenyl group, a C5-12 cycloalkyl group, or a phenyl group having a linear C1-14 alkyl group, a linear C1-9 alkoxy group or a C5-12 cycloalkyl group at the para-position.
A01N 43/62 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms three- or four-membered rings or rings with more than six members
A61K 31/7072 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
This invention relates to a method for making macrolides, and, in particular, to a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl- tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides.
This invention relates to a method for making macrolides, and, in particular, to a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl- tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides.
Disclosed are: a novel aminoglycoside antibiotic which has an excellent anti-bacterial activity against an infection-inducing bacterium, particularly MRSA, and also has low renal toxicity; and a process for production of the antibiotic. More specifically, disclosed are: a compound represented by the formula (Ia) or a pharmacologically acceptable salt or solvate thereof, or a diastereomeric mixture of the compound, the salt or the solvate; an antibacterial agent comprising the compound, the salt, the solvate or the diastereomeric mixture; and a process for production of the compound. [Chemical formula 1] (Ia)
C07H 15/234 - Cyclohexane rings, substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings attached to non-adjacent ring carbon atoms of the cyclohexane rings, e.g. kanamycins, tobramycin, nebramycin, gentamicin A2
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
The invention provides novel dioctatin derivatives, a process for the production thereof, novel dioctatin derivatives useful as aflatoxin production inhibitor, and a method for controlling aflatoxin pollution by the use of an aflatoxin production inhibitor containing one or more of the dioctatin derivatives. The invention relates to dioctatin derivatives characterized by being represented by the structural formula (I): wherein R1 and R2 are each hydrogen, CH3-(CH2)n-, (CH3)2CH-CH2-, or C6H5-CH2-; n is an integer of 2 to 6; X1 and X2 are each CH3 or hydrogen; and Y is 2-amino-2-butenoic acid or an amino acid residue, with the proviso that the cases wherein both R1 and R2 are CH3-(CH2)4-; X2 is hydrogen; and Y is 2-amino-2-butenoic acid are excepted.
C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
A01N 43/36 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07D 207/08 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
C07K 5/023 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link in which at least a beta-amino acid is involved
79.
AFLATOXIN PRODUCTION INHIBITOR, AND METHOD FOR CONTROL OF AFLATOXIN POISONING USING THE SAME
Disclosed are: an aflatoxin production inhibitor which can inhibit the production of aflatoxin specifically and effectively and is highly safe and practically useful; a process for producing the inhibitor with good efficiency; and a method for controlling the aflatoxin poisoning using the aflatoxin production inhibitor. An aflatoxin production inhibitor comprising at least one of a dioctane represented by the structural formula (I): (I) wherein R represents a hydrogen or a methyl group, and a derivative thereof as an active ingredient; a process for preparing an aflatoxin production inhibitor by culturing a dioctane-producing bacterium and then performing a method for separation/purification of the aflatoxin production inhibitor from a culture by centrifugal liquid-liquid partition chromatography or by chemical synthesis; and a method for controlling the aflatoxin poisoning comprising inhibiting the production of aflatoxin by an aflatoxin-producing bacterium using the aflatoxin production inhibitor.