http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-055193-A1

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filingDate 2005-09-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fa995b00e24ff1c32454a4f237a9b501
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publicationDate 2007-08-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-055193-A1
titleOfInvention CARBOESTIRILE COMPOUNDS AS POSITIVE REGULATORS OF TFF2
abstract Pharmaceutical compositions containing them, uses and method of preparation thereof. Claim 1: A carbostyril compound represented by the general formula (1) or its salt, characterized in that A is a direct bond, a lower alkylene group, or a lower alkylidene group; X is an oxygen atom or a sulfur atom; the link between positions 3 and 4 of the carbostyle nucleus is a single bond or a double bond; R4 and R5 each represent a hydrogen atom, with the proviso that, when the bond between positions 3 and 4 of the carbostyryl nucleus is a double bond, R4 and R5 can instead be linked to each other in the form of a group -CH = CH-CH = CH-; R1 is one of the following (1-1) to (1-29): (1-30) a hydrogen atom, (1-31) a lower alkyl group, (1-32) an optionally substituted phenyl lower alkyl group in the phenyl ring by one or more members selected from the group comprising a phenyl group, lower alkyl groups, lower alkoxy groups, halogen atoms, groups - (B) 1NR6R7, a nitro group, a carboxy group, lower alkoxycarbonyl groups , a cyano group, phenyl lower alkoxy groups, a phenoxy group, piperidinyl lower alkoxycarbonyl groups, inner amino alkoxycarbonyl groups optionally substituted by one or more cycloalkyl groups, 2-imidazolinylcarbonyl groups optionally substituted on the 2-imidazoline ring by one or more groups lower alkylthio, 3-pyrrolinylcarbonyl groups optionally substituted on the 3-pyrroline ring by one or more lower alkyl groups, thiazolidinylcarbonyl groups optionally substituted on the thiazolidine ring by a phe group ilo, 3- azabicyclo [3.2.2] nonylcarbonyl groups, piperidinyl lower alkyl groups, lower alkyl anilino groups optionally substituted in the amino group by one or more lower alkyl groups, phenylthio lower alkyl groups, indolinyl lower alkyl groups and optionally substituted piperidinylcarbonyl groups in the piperidine ring by one or more inner alkyl groups, (1-33) a lower alkyl cycloalkyl group, (1-34) a lower alkyl phenoxy group, (1-35) a lower alkyl naphthyl group, (1-36) ) a lower alkyl lower alkyl group, (1-37) a lower alkyl carboxy group, (1-38) a lower alkyl lower alkoxycarbonyl group, (1-39) a lower alkyl pyridyl group optionally substituted on the pyridine ring by one or more members selected from the group comprising halogen atoms; piperidinyl groups; a morpholino group; Piperazinyl groups optionally substituted on either piperazine ring by one or more members selected from the group comprising a phenyl group and a lower alkyl group; thienyl groups; a phenyl group; pyridyl groups; piperidinyl lower alkyl groups; phenylthio lower alkyl groups; biphenyl groups; lower alkyl groups optionally substituted by one or more halogen atoms; pyridylamino groups; pyridylcarbonylamino groups; lower alkoxy groups; lower alkyl anilino groups optionally substituted in the amino group by one or more lower alkyl groups; and aniline groups optionally substituted in the amino group by one or more lower alkyl groups, (1-40) a cyano lower alkyl group, (1-41) an A1-CONR8R9 group, (1-42) a group of the formula ( 2) ; (1-43) a phenyl group; (1-44) a lower alkyl quinolyl group, (1-45) a lower alkyl lower alkoxy group, substituted by lower alkoxy, (1-46) a lower alkyl group substituted by hydroxy, (1-47) a thiazolyl alkyl group lower optionally substituted on the thiazole ring by one or more members selected from the group comprising halogen atoms, a phenyl group, thienyl groups, pyridyl groups, (1-48) a lower alkyl group optionally substituted by one or more atoms of halogen, (1-49) a lower alkylsilyloxy lower alkyl group, (1-50) a lower alkyl phenoxy group optionally substituted on the phenyl ring by one or more members selected from the group comprising lower alkyl groups optionally substituted by one or more halogen atoms lower alkoxy groups; halogen atoms; lower alkenyl groups; cycloalkyl groups; a nitro group; and a phenyl group, (1-51) a phenylthio lower alkyl group optionally substituted on the phenyl ring by one or more halogen atoms, (1-52) piperidinyl inner alkyl groups optionally substituted on the piperidine ring by one or more members selected from the group comprising phenyl lower alkyl groups and a phenyl group, (1-53) a piperazinyl lower alkyl group optionally substituted on the piperazine ring by one or more phenyl groups, (1-54) a group 1,2 , 3,4-tetrahydroisoquinolyl lower alkyl, (1-55) a naphthyloxy lower alkyl group, (1-56) a lower alkyl benzothiazolyloxy group optionally in the benzothiazole ring by one or more alkyl groups, (1-57) a group lower alkyl substituted by one or more members selected from the group comprising quinolyloxy groups and isoquinolyloxy groups, (1-58) a lower alkyl pyridyloxy group optionally substituted on the pyridine ring by one or more alkyl groups i lower; R2 is one of the following (2-1) to (2-33): (2-1) a hydrogen atom, (2-2) a lower alkoxy group, (2-3) a lower alkyl group, (2 -4) a lower alkoxy carboxy group, (2-5) a lower alkoxycarbonyl alkoxy group, (2-6) a hydroxy group, (2-7) an internal phenyl alkoxy group optionally substituted on the phenyl ring by one or more members selected from the group comprising halogen atoms; lower alkyl groups optionally substituted by one or more halogen atoms; lower alkylthio groups optionally substituted by one or more halogen atoms; lower alkoxy groups; a nitro group; lower alkylsulfonyl groups; lower alkoxycarbonyl groups; phenyl lower alkenyl groups; lower alkanoyloxy groups; and 1,2,3-thiadiazolyl groups, (2-8) a piperidinyl lower alkoxy group optionally substituted on the piperidine ring by one or more lower alkyl groups, (2-9) a lower alkoxy group substituted by amino optionally substituted by one or more lower alkyl groups, (2-10) a lower alkenyloxy group, (2-11) a lower pyridyl alkoxy group optionally substituted on the pyridine ring by one or more lower alkyl groups, where each lower alkyl substituent is optionally substituted by one or more halogen atoms, (2-12) a lower alkynyloxy group, (2-13) a phenyl lower alkynyloxy group, (2-14) a phenyl lower alkenyloxy group, (2-15) a furyl alkoxy group bottom optionally substituted on the furan ring by one or more alkoxycarbonyl groups, (2-16) an internal tetrazolyl group optionally substituted on the tetrazole ring by a member selected from the group comprising a phenyl group, phenyl groups lower alkyl, and cycloalkyl lower alkyl groups, (2-17) a 1,2,4-oxadiazolyl lower alkoxy group optionally substituted on the 1,2,4-oxadiazole ring by a phenyl group, and the phenyl substituent is substituted optionally in the phenyl ring by one or more lower alkyl groups, (2-18) an isoxazolyl lower alkoxy group optionally substituted in the isoxazol ring by linen O plus lower alkyl groups, (2-19) a group 1,3, 4-oxadiazole lower alkoxy optionally substituted on the 1,3,4-oxadiazole ring) by a phenyl group, and the phenyl substituent is optionally substituted on the phenyl ring by one or more lower alkyl groups, (2-20) a lower alkoxy lower alkoxy group, (2-21) a lower alkoxy thiazolyl group optionally substituted on the thiazole ring by one or more members selected from the group comprising lower alkyl groups and a phenyl group, where each phenyl substituent is optionally you are substituted on the phenyl ring by one or more halogen atoms, (2-22) a piperidinyloxy group optionally substituted on the piperidine ring by one or more benzoyl groups, where each benzoyl substituent is optionally substituted on the phenyl ring by one or more halogen atoms, (2-23) a lower thienyl alkoxy group, (2-24) a phenylthio lower alkoxy group, (2-25) a lower alkoxy group substituted by carbamoyl optionally substituted by one or more alkyl groups lower, (2-26) a lower benzoyl alkoxy group, (2- 27) a lower pyridylcarbonyl alkoxy group, (2-28) a lower imidazolyl alkoxy group optionally substituted on the imidazole ring by one or more lower alkyl phenyl groups, (2-29) a phenoxy lower alkoxy group, (2-30) a lower alkoxy group substituted by phenyl lower alkoxy, (2-31) a group 2, 3dihydro-1H-indenyloxy, (2-32) an isoindolinyl alkoxy group bottom optionally substituted on the iso ring indoline for one or more oxo groups, (2-23) a phenyl group; R3 is one of the following (3-1) to (3-19); (3-1) a hydrogen atom, (3-2) a lower alkyl group substituted by hydroxy, (3-4) a cycloalkyl lower alkyl group, (3-5) a lower alkyl carboxy group, (3-6) a lower alkoxycarbonyl lower alkyl group, (3-7) a phenyl lower alkyl group optionally substituted on the phenyl ring by one or more members selected from the group comprising halogen atoms; lower alkyl groups optionally substituted by one or more halogen atoms; lower alkoxy groups optionally substituted by one or more halogen atoms; a phenyl group; lower alkoxycarbonyl groups; a phenoxy group; lower alkylthio groups; lower alkylsulfonyl groups; phenyl lower alkoxy groups; and amino groups optionally substituted by one or more alkanoyl groups, (3-8) a naphthyl alkyl group
priorityDate 2004-09-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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