A compound, in which some or all of the hydrogen atoms of the ethylene group constituting propionic acid in 3-[4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]phenyl]propionic acid have been substituted with deuterium, or a salt thereof, or an ester thereof, and a prodrug for releasing Am80 as an active medicament after absorption in the body, which comprises the compound or a salt thereof, or an ester thereof as an active ingredient.
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
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A compound represented by formula (I) (wherein each of R1-R3 represents an alkyl group, an aryl group or the like; n represents 0 or 1; R4 represents an amino group or -(CX2)m-COOH (wherein m represents a number of 0-3 and X represents a hydrogen atom); and R5 represents -(CY2)p-COOR6 (wherein p represents a number of 0-3, Y represents a hydrogen atom, and R6 represents a hydrogen atom or an alkyl group)) or a salt thereof.
Disclosed is a novel anti-bacterial agent comprising a compound represented by formula (I), a pharmaceutically acceptable salt of the compound, or a solvate of the compound or the pharmaceutically acceptable salt. [In formula (I), the ring A is a group represented by formula (A-1), (A-2), (A-3) or (A-4); the ring B represents an optionally substituted benzene ring; the ring C represents an optionally substituted 6-membered hetero ring which contains at least one N atom, contains C as an atom to which the ring B is bound, and has 1 to 3 double bonds in the ring; the ring D represents an optionally substituted 5-membered ring having 1 to 2 double bonds in the ring; A1 and A2 independently represent N or C; m represents a number of 0 or 1; R represents H, -NHC(=O)RA, -NHC(=S)RA, -NH-het1, -O-het1, -S-het1, -S(=O)-het1, -S(=O)2-het1, het2, -CONHRA, -OH, a lower alkyl, a lower alkoxy, or a lower alkenyl; and het1 and het2 independently represent a heterocyclic group.
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 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
Disclosed is a compound represented by general formula (I), which affects the gene transcription process. (I) (In the formula, R1 and R2 each represents a hydrogen atom, an alkyl group, a halogen atom or the like; R3 and R4 each represents a hydrogen atom, an alkyl group, an alkoxy group or an alkenyl group; R5 represents a hydrogen atom, an alkyl group or a nitro group; and R6 represents a hydrogen atom or an alkyl group.)
C07C 237/40 - 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 a carbon atom of a six-membered aromatic ring
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07C 233/81 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of 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 carboxyl groups
C07D 209/46 - Iso-indolesHydrogenated iso-indoles with an oxygen atom in position 1
C12Q 1/66 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving luciferase
A compound represented by the following general formula (I), which is converted into retinoid after being absorbed in vivo, or its salt or ester: wherein R1 to R5 represent each a hydrogen atom, an alkyl group or a trialkylsilyl group; X represents -NH-CO-, -CO-NH-, -N(COR6)-CO-, -CO-N(COR7)- (wherein R6 and R7 represent each a lower alkoxy group or a carboxy-substituted phenyl group), etc.; and Z represents -Y-CH(R12)-COOH, -CHO, -CH=CH-COOH or -COOR13 (wherein Y represents a single bond, -CH2-, -CH(OH)-, -CO-, -CO-NH- or -CO-NH-CH2-CO-NH-; R12 represents a hydrogen atom, or a lower alkyl group; and R13 represents a hydrogen atom, -CH(R14)-COOH (wherein R14 represents a hydrogen atom, a lower alkyl group or a hydroxyl group), -[CH2CH2-O]n-CH2-CH2-OH, -CH2-O-[CH2CH2-O]m-CH2-OH or -[CH(CH3)-CO-O]p-CH(CH3)-COOH (wherein n, m and p represent each an integer of 1 to 100).
C07C 235/84 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 235/88 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having the nitrogen atom of at least one of the carboxamide groups further acylated
C07C 237/48 - 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 six-membered aromatic ring being part of a condensed ring system of the same carbon skeleton
C07C 237/52 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the nitrogen atom of at least one of the carboxamide groups further acylated
C07C 271/30 - 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 six-membered aromatic ring to a carbon atom of a six-membered aromatic ring being part of a condensed ring system
C07F 7/10 - Compounds having one or more C—Si linkages containing nitrogen
6.
OXAZOLIDINONE DERIVATIVE HAVING 7-MEMBERED HETERO RING
Disclosed are a novel oxazolidinone derivative represented by the formula (I), a pharmaceutically acceptable salt thereof, and a solvate of the derivative or the pharmaceutically acceptable salt, which are useful as antibacterial agents. (I) wherein the ring A represents (A-1) a 7-membered monocyclic hetero ring having three N atoms, (A-2) a 7-membered monocyclic hetero ring having two N atoms and one O atom, or (A-3) a 7-membered monocyclic hetero ring having two N atoms and one S atom, SO or SO2, in which the monocyclic hetero ring may be substituted, may have an unsaturated bond, and may be fused with another ring; X1 represents a single bond, a hetero atom-containing group selected from the group consisting of -O-, -S-, -NR2-, -CO-, -CS-, -CONR3-, -NR4CO-, -SO2NR5- and -NR6SO2- [wherein R2 to R6 independently represent a hydrogen or a lower alkyl group], or a lower alkylene or alkenylene which may have the hetero atom-containing group therein; the ring B represents a carbon ring which may be substituted or a hetero ring which may be substituted; and R1 represents a hydrogen or an organic residue which can bind to position-5 in an oxazolidinone ring in an oxazolidinone antibacterial agent.
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
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 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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
Disclosed is a compound represented by the general formula (I) below, which has an action of regulating the physiological activity of a retinoid and is useful as an active ingredient of pharmaceutical products. (In the formula, R1 represents a hydrogen atom or a C1-6 alkyl group; A and B each represents -(CH2)2-, -(CH2)3- or -(CH2)4-; X represents -N(R2)- (wherein R2 represents a hydrogen atom or a C1-6 alkyl group), -CO-, -C(=N-R3)- (wherein R3 represents a hydrogen atom or a C1-6 alkyl group), or -C(=C(R4)(R5))- (wherein R4 and R5 independently represent a hydrogen atom or a C1-6 alkyl group); and Ar represents an aryldiyl group or a heteroaryldiyl group.)
C07C 229/60 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in meta- or para- positions
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61P 43/00 - Drugs for specific purposes, not provided for in groups
Disclosed is a compound represented by the general formula (I) below, which has retinoid activity and is useful as an active ingredient of a pharmaceutical product. (In the formula, R1 and R2 each represents a C3-10 alkyl group; X represents -S-, -O- or -NH-; Y represents C or N; R3 represents a hydrogen atom or a C1-10 alkyl group; Z represents -CO-N(R5)- (wherein R5 represents a hydrogen atom or a C1-6 alkyl group) or -C(R6)=C(R7)-CO-NH- (wherein R6 and R7 each represents a hydrogen atom or a C1-6 alkyl group); Ar represents an aryldiyl group or a heteroaryldiyl group; and R4 represents -COOH, -OCH2-COOH, -CH2-COOH or -CH2-CH2-COOH.)
C07D 207/416 - 2,5-Pyrrolidine-diones 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 other ring carbon atoms
A61K 31/341 - 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 not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/401 - ProlineDerivatives thereof, e.g. captopril
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 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 307/54 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 307/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 333/24 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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
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
Disclosed is a compound represented by the general formula (I) below, which has retinoid action and is useful as an active ingredient of pharmaceutical products. (In the formula, R1 represents a hydrogen atom or a C1-6 alkyl group; A and B each represents -(CH2)2-, -(CH2)3- or -(CH2)4-; X represents -N(R2)-CO- (wherein R2 represents a hydrogen atom or a C1-6 alkyl group), -CO-N(R3)- (wherein R3 represents a hydrogen atom or a C1-6 alkyl group), -C(R4)=C(R5)- (wherein R4 and R5 each represents a hydrogen atom or a C1-6 alkyl group) or -N(R6)-SO2- (wherein R6 represents a hydrogen atom or a C1-6 alkyl group); and Ar represents an aryldiyl group or a heteroaryldiyl group.)
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
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07C 233/81 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of 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 carboxyl groups
C07C 311/21 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
Disclosed is a novel oxazolidinone derivative represented by the formula (I). Also disclosed is an antibacterial agent comprising the derivative, wherein the ring A represents an at least 7-membered monocyclic carbocyclic ring which may be substituted and whose ring may be fused; X1 represents a heteroatom-containing group selected from the group consisting of -O-, -S-, -NR2-, -CO-, -CS-, -CONR3-, -NR4CO-, -SO2NR5- and -NR6SO2- (wherein R2 to R6 independently represent a hydrogen, a lower alkyl, or a lower alkoxycarbonyl) or a lower alkylene or alkenylene which may contain the heteroatom-containing group; the ring B represents a carbocyclic or heterocyclic ring which may be substituted; and R1 represents a hydrogen or an organic residue which can bind to position-5 of an oxazolidinone ring in an oxazolidinone-type antibacterial agent (wherein a combination of -CH2O- as X1 and a hydroxymethylene which may be substituted as R1 is excluded).
A61K 31/421 - 1,3-Oxazoles, e.g. pemoline, trimethadione
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A61K 31/435 - 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
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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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
Disclosed are a novel oxazolidinone derivative represented by the formula (I) below and an antibacterial agent containing the oxazolidinone derivative. (I) [In the formula, ring A may be substituted or fused and represents (A-1) at least 7-membered monocyclic heterocyclic ring containing at least three N atoms, (A-2) at least 6-membered monocyclic heterocyclic ring containing at least two N atoms and at least one O atom, or (A-3) at least 7-membered monocyclic heterocyclic ring containing at least two N atoms and at least one S atom; X1 represents a single bond, -O-, -S-, -NR2-, -CO-, -CS-, -CONR3-, -NR4CO-, -SO2NR5-, -NR6SO2- (wherein R2-R6 independently represent a hydrogen or a lower alkyl), or a lower alkylene or lower alkenylene in which one of the preceding groups may intervene; ring B represents an optionally substituted carbon ring or heterocyclic ring; R1 represents a hydrogen or an organic residue which can be bonded to the 5-position of an oxazolidinone ring of an oxazolidinone antibacterial agent.]
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
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 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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 417/14 - 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
patents