http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CO-5180641-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_4bc4da062859d6b5059944a1abe5ac16 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C04B35-632 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D209-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4178 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D209-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-404 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-41 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-496 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-454 |
| filingDate | 2000-08-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ec0b4235dd62e99e0e2fc1ddcc396e1f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c5529ba247135452361bdf23602968d0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bea25436f32a4e2c4641573861885f39 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_28d08eaa0f7f97a73055bf9abd70234f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_420e693a14c1c928e58b1c2b5e26a03f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f82ec29cb1210810c9b68a6daff0980e |
| publicationDate | 2002-07-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CO-5180641-A1 |
| titleOfInvention | NEW INDOLINONES REPLACED, THEIR PREPARATION AND THEIR EMPLOYMENT AS MEDICINES |
| abstract | Substituted indolinones of the general formula (I): <EMI FILE = "00063885_1" ID = "1" MFI = JPEG> in which X means an oxygen or sulfur atom, R1 means a C2-3 alkenyl group, C2-3 alkynyl , aryl, aryl-C1-3alkyl, heteroaryl, heteroaryl-C1-3alkyl, trifluoromethyl or cyano, means a hydroxy group, C1-3alkoxy, hydroxy-C1-3alkyl, C1-3alkoxy-C1-3alkyl, aryloxy or heteroaryloxy, means a mercapto group, C1-3-alkylphenyl, phenylsulfenyl, benzylsulfenyl, C1-3-alkyl-sulfinyl, phenyulfinyl, benzylsulfinyl, C1-3-alkyl sulfonyl, phenylsulfonyl, benzylsulfonyl, sulfo, alkoxy, C1-3- sulfonyl, phenoxysulfonyl or benzyloxysulfonyl, means an amino group, C1-3-alkyl, di (C1-3 alkyl) -amino, hydroxycarbonyl-C1-3-amino alkyl, N- (C1-3 alkyl) -hydroxycarbonyl-alkyl C1-3-amino, C1-3alkoxy-C1-3alkyl-alkyl, N- (C1-3alkyl) -C1-3alkoxy-C1-3 -alkylamino, phenylamino, N-phenyl-alkyl C1-3-amino, N, N-diphenyl-amino, benzylamino, N-benzyl-alkyl C1-3-amino N, N-dibenzylamino, C1-3 alkylcarbonylamino, benzoylamino or benzylcarbonylamino or an N- (C1-3 alkyl) -C1-3 alkylcarbonylamino group in which the two alkyl groups can be replaced by a C2-5 n-alkylene bridge, or in which one or both alkyl groups may be replaced by a phenyl or benzyl group, means a C1-3 alkyl sulfonylamino, phenylsulfonylamino or benzylsulfonylamino group or an N- ( C1-3alkyl) -C1-3alkyl-sulfonylamino, in which the two alkyl groups may be replaced by a C2-5 n-alkylene bridge, or in which one or both alkyl groups may be replaced by a group phenyl or benzyl, means an aminosulfonyl, C1-3-aminosulfonyl, phenylaminosulfonyl, benzylaminosulfonyl, di- (C1-3 alkyl) -aminosulfonyl, N, N-diphenyl-aminosulfonyl or N, N-dibenzyl-aminosulfonyl group, - 2 - means a phosphono group, (C1-3 alkoxy) PO (H), (C1-3 alkoxy) PO (C1-3 alkyl), (C1-3 alkoxy) PO (OH), di- (C1-3 alkoxy) PO o (na C2-4-dioxy) -PO alkylene, means a ureido group, optionally mono-, di- or tri- substituted with C1-3 alkyl groups, means a 4- to 7-membered cycloalkyleneimino or cycloalkyleneimino-sulfonyl group, and may be replaced in in each case the methylene group in position 4 of a 6 or 7 membered cycloalkyleneimino group by an oxygen or sulfur atom, by a sulfinyl, sulfonyl, -NH or -N (C1-3 alkyl) group, R2 means an atom of hydrogen, fluorine, chlorine, bromine or iodine, means a C1-6 alkyl or trifluoromethyl group, means a hydroxy group, C1-3 alkoxy, mercapto, C1-3 alkyl sulfenyl, C1-3 alkyl sulfinyl, C1-3 alkyl -sulfonyl, sulfo, C1-3 alkoxy-sulfonyl, aminosulfonyl, C1-3-alkyl-aminosulfonyl or di-(C1-3) alkylsulfonyl means a nitro, amino, C1-3-alkyl or di- (C1-alkyl) -3) -amino, means a C1-3-alkylcarbonyl, cyano, carboxy, C1-3-alkoxycarbonyl, aminocarbonyl, C1-3-aminocarbonyl or di- (C1-3alkyl) -aminocarbonyl group, means a phosphono group, (C1-3 alkoxy) PO (H), (C1-3 alkoxy) PO (C1-3 alkyl), (C1-3 alkoxy) PO (OH) or di- (C1-3 alkoxy) PO means a cycloalkyleneimino, cycloalkyleneiminocarbonyl or cycloalkyleneiminosulfonyl group of 4 to 7 members, the methylene group in the 4 position of a 6 or 7 membered cycloalkyleneimino group being replaced in each case by an oxygen or sulfur atom, by a sulfinyl group, sulfonyl, -NH or -N (C1-3 alkyl), or R1 and R2 together mean a methylenedioxy, ethylenedioxy, n-propylene, n-butylene or 1,4-butadienylene group, R3 means a hydrogen atom, an alkyl group C1-6, C3-7 cycloalkyl, trifluoromethyl or heteroaryl, means a phenyl or naphthyl group, optionally mono- or di-substituted with a fluorine, chlorine, bromine or iodine atom, with a trifluoromethyl, C1-3 alkyl or alkoxy group C1-3, where, in the case of the substitution, the substituents may be the same or different which, additionally, may be substituted with a group or hydroxy, hydroxy-C1-3 alkyl or C1-3 alkoxy-C1-3 alkyl, with a cyano, cyano-C1-3 alkyl, cyano-C2-3 alkenyl, cyano-C2-3 alkynyl, carboxy, carboxy- C1-3 alkyl, C2-3 carboxy-alkenyl, C2-3 carboxy-alkynyl, C1-3 alkoxycarbonyl C2-3 or C1-3 alkoxycarbonyl-C2-3 alkynyl group, with a C1-3 alkyl group -carbonyl, C1-3alkyl-C1-3alkyl, C1-3alkyl-C2-3alkyl-alkenyl or C1-3alkyl-C2-3alkynyl, with an aminocarbonyl, aminocarbonyl-C1-3alkyl group , C2-3 aminocarbonyl-alkenyl, C2-3 aminocarbonyl-alkynyl, C1-3alkylcarbonyl, C1-3alkylcarbonyl-C1-3alkyl, C1-3alkylcarbonyl-C2-3alkyl, C1-3alkyl -Caminocarbonyl-C2-3 alkynyl, di- (C1-3alkyl) -aminocarbonyl, di- (C1-3alkyl) -aminocarbonyl-C1-3alkyl, di- (C1-3alkyl) -aminocarbonyl-C2-3alkenyl or di- (C1-3alkyl) -aminocarbonyl-C2-3alkyl, with a nitro group, nitro C1-3 alkyl, nitro C2-3 alkyne, or nitro C2-3 alkynyl, with an amino group, C1-3alkyl- to Mino, di- (C1-3 alkyl) -amino, amino C1-3 alkyl, C1-3 alkyl-C1-3 alkyl or di - (C1-3 alkyl) -amino-C1-3 alkyl, with a C1-3 alkylcarbonylamino, C1-3 alkylcarbonylamino C1-3 alkyl, N- (C1-3 alkyl) -C1-3-carbonylamino, N- (C1-3 alkyl) -C 1-3 alkyl- carbonylamino-C1-3 alkyl, C1-3 alkyl-sulfonylamino, C1-3 alkyl-sulfonylamino-C1-3 alkyl, N (C1-3 alkyl) -C1-3-sulfonylamino or N (C1-3 alkyl) -alkyl C1-3-sulfonylamino-C1-3 alkyl, with a cycloalkyleneimino, cycloalkyleneiminocarbonyl, cycloalkyleneiminosulfonyl, cycloalkyleneimino-C1-3 alkyl, cycloalkyleneiminocarbonyl-C1-3 alkyl or cycloalkyleneiminosulfonyl-C1-3 alkyl group of 4 to 7 members, and may be substituted in each case the methylene group in position 4 of a 6 or 7 membered cycloalkyleneimino group by an oxygen or sulfur atom, by a sulfinyl, sulfonyl, -NH or -N (C1-3 alkyl) group, or with a heteroaryl group or heteroaryl-C1-3alkyl, R4 means a hydrogen atom , a C1-3 alkyl group or a prodrug radical, wherein said prodrug radical is selected from a hydroxy group, an acyl group such as the benzoyl or pyridinoyl group, or a C1-16 alkanoyl group such as the formyl, acetyl, propionyl group , butanoyl, - 3 -pentanoílo or hexanoyl, an allyloxycarbonyl group, a C1-16 alkoxy-carbonyl group such as metho-xicarbonilo, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, butoxycarbonyl, tert-butoxycarbonyl, pentoxycarbonyl, hexyloxycarbonyl, oxtiloxicarbonilo, nonyloxycarbonyl, decyloxycarbonyl, undecyloxycarbonyl, dodecyloxycarbonyl or hexadecyloxycarbonyl, a phenyl-C 1-6 alkoxycarbonyl group such as the benzyloxycarbonyl, phenylethoxycarbonyl or phenylpropoxycarbonyl group, a C 1-3 alkyl sulfonyl C2-4 alkoxycarbonyl, C 1-3 alkoxy C2-4alkoxyC2-4alkoxycarbonyl or ReCO-O- (RfCRg) -O-CO, in which Re represents a C1-8 alkyl, C5-7 cycloalkyl, phenyl or phenyl-C1-3 alkyl group, Rf represents an atom of hydrogen, a C1-3 alkyl, C5-7 cycloalkyl or phenyl group and Rg represents a hydrogen atom, a C1-3 alkyl or ReCO-O- (RfCRg) -O group, in which Re to Rg are defined as mentioned above, R5 means a hydrogen atom or a C1-3 alkyl group and R6 means a hydrogen, fluorine, chlorine, bromine or iodine atom, means a trifluoromethyl or heteroaryl group, a C1-3 alkoxy group, optionally substituted with 1 to 3 fluorine atoms, a C1-3 amino-alkoxy group, C1-3-alkyl-C2-3-alkoxy or C2-3 benzylamino-alkoxy group, a C2-3 cycloalkyleneimino-alkoxy group with 4 to 7 members of the ring, a di- (C1-3 alkyl) -amino-C2-3 alkoxy or C1-3 alkyl-mercapto group, means a nitro, cyano, carboxy, C1-3 alkoxycarbonyl, aminocarbonyl, C1-3 alkyl- aminocarbonyl, di-C1-3 alkyl) -aminocarbonyl, piperidinocarbonyl or tetrazolyl, means a C1-3 alkylcarbonylamino group, optionally substituted on the nitrogen atom with a C1-3 alkyl group, means an imidazolyl or piperazino group, optionally substituted in the imino group with a C1-3 alkyl group, means a C1-4 alkyl group, which in the terminal position may be substituted with a hydroxy, C1-3 alkoxy, carboxy, C1 alkoxy group -3-carbonyl, amino, C 1-4 alkyl-amino, di (C 1-4 alkyl) -amino, phenylamino, N-phenyl-C 1-3 alkyl, phenyl-n-C 1-3 alkyl-amino, N- (C1-3 alkyl) -phenyl-n-C1-3-alkyl or di- (phenyl-n-C1-3 alkyl) -amino, with a methylene group linked to the imino group may be replaced by a carbonyl group or sulfonyl, one or two hydrogen atoms may be replaced in each case with a C1-3 alkyl group, and / or in each case the methylene group in position 4 of a 6 or 7 membered cycloalkyleneimino group may be substituted with a carboxy group , C1-3 alkoxycarbonyl, aminocarbonyl, C1-3alkylcarbonyl alkyl, di- (C1-3alkyl) -aminocarbonyl, phenyl-n-C1-3alkyl or N- (C1-3alkyl) -phenyl- n-C1-3-amino alkyl or may be replaced by an oxygen or sulfur atom, by a sulfinyl, sulfonyl, -NH or -N (C1-3 alkyl) group, it can be substituted with a 5- to 7-membered cycloalkenyleneimino group, in which the double bond is isolated from the atom of nitrogen, it can be substituted with a C4-7-amino, N- (C1-3-alkyl) -C4-7-amino-cycloalkyl or C5-7-amino cycloalkenyl group, in which the position 1 of the ring does not participate in the double bond and in which the nitrogen atom may be substituted with a C1-3 alkyl group, with a C1-3 alkylcarbonylamino, N- (C1-3 alkyl) -C1-3 alkylcarbonylamino, aminocarbonyl group, C1-3alkylcarbonyl or di- (C1-3alkyl) -aminocarbonyl, or R6 means a group of the formula-N (Ra) -CO- (CH2) n-Rb (II), in which Ra means a group C1-3 alkyl, n means one of the numbers 0.1 or 2 and Rb means an amino group, C1-4 alkyl, amino, phenylamino, N- (C1-4 alkyl) -phenylamino, benzylamino, N- (C1- alkyl 4) -benzylamino or di- (C1-4 alkyl) -amino, or means a gru by cycloalkyleneimino of 4 to 7 members, being able to be replaced |
| priorityDate | 1999-08-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 97.