http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-045687-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f2d3599fb8f8f479dba95ca9bb504884 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C229-40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-93 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-88 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C229-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-94 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-06 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-88 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-94 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-93 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-529 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 |
| filingDate | 2004-05-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-11-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-045687-A1 |
| titleOfInvention | MACROCICLES DERIVED FROM QUINAZOLINE, PREPARATION PROCESSES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
| abstract | Preparation process, and pharmaceutical compositions containing them. Claim 1: A compound having the formula (1), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, CH2, NH or S; in particular Z represents NH; Y represents -C3-9-, -C3-9 -alkenyl, -C3-9 -alkyl-, -C3-7-CO-NH-alkyl optionally substituted with amino, mono- or di (C1-4 alkyl ) amino or C1-4 alkyloxycarbonylamino-, - C3-7-CO-NH- alkenyl optionally substituted with amino, mono- or di (C1-4 alkyl) amino or C1-4- alkyloxycarbonylamino, -C3-7 -CO-alkynyl NH- optionally substituted with amino, mono- or di (C1-4 alkyl) amino or C1-4 alkyloxycarbonylamino, -C1-5 alkyloxy-C1-5 alkyl-, -C1-5-NR13-C1-5 alkyl- , -C1-5-NR14-CO-C1-5 alkyl -, - C1-5 alkyl-CO-NR15-C1-5 alkyl-, -C 1-6 alkyl-CO-NH-, -C 1-6 alkyl- NH-CO-, - C1-3 alkyl-NH-CS-Het20 -, - C1-3 alkyl-NH-CO-Het20-, C1-2 alkyl-CO-Het21-CO-, - Het22-CH2-CO- NH-C1-3 alkyl, -CO-NH-C1-6 alkyl, -NH-CO-C1-6 alkyl, -CO-C1-7 alkyl, -C 1-7 alkyl-CO-, -alkyl C1-6-CO-C1-6- alkyl, -C1-2 alkyl-NH-CO-CR16R17-NH-, -C1-2 alkyl-CO-NH-CR18R19-CO-, -C1-2 alkyl-CO- NR20-C1-3-alkyl-, -C1-2-NR21-CH2-CO-NH-C1-3- alkyl, or - alkyl-NH-; X1 represents a direct bond, O, -O-C1-2- alkyl, CO, -CO-C1-2- alkyl, NR11, -NR11-C1-2- alkyl, -CH2-, -ON = CH- or - C1-2- alkyl; X2 represents a direct bond, O, -O-C1-2- alkyl, CO, -CO-C1-2- alkyl, NR12, -NR12-C1-2- alkyl, -CH2-, -ON = CH- or - C1-2- alkyl; R 1 represents hydrogen, cyano, halo, hydroxy, formyl, C 1-6 alkoxy, C 1-6 alkyl, halophenylcarbonylamino, C 1-6 alkoxy substituted by halo, C 1-4 alkyl substituted with one or whenever possible two or more substituents selected from hydroxy or halo; R2 represents hydrogen, cyano, halo, hydroxy. hydroxycarbonyl-, Het16-carbonyl-, C1-4- alkyloxycarbonyl, C1-4 alkylcarbonyl-, aminocarbonyl-, mono- or di (C1-4 alkyl) aminocarbonyl-, Het1, formyl, C1-4- alkyl, C2-6 alkynyl -, C3-6- cycloalkyl, C3-6- cycloalkyloxy, C1-6- alkoxy, Ar5, Ar1-oxy- dihydroxyborane, C1-6 alkoxy substituted by halo, C1-4 alkyl substituted with one or whenever possible two or more substituents selected from halo, hydroxy or NR5R6, C 1-4 alkylcarbonyl, wherein said C 1-4 alkyl is optionally substituted with one or whenever possible two or more substituents selected from hydroxy or C 1-4 alkyloxy; R 3 represents hydrogen, C 1-4 alkyl, or C 1-4 alkyl substituted with one or more substituents selected from halo, C 1-4 alkyloxy, amino-, mono- or di (C 1-4 alkyl) amino-, C 1-4 alkylsulfonyl - or phenyl; R4 represents hydrogen, hydroxy, Ar3-oxy, Ar4-C1-4 alkyloxy, C1-4 alkyloxy, C2-4 alkenyloxy optionally substituted with Het12 or R4 represents C1-4 alkyloxy substituted with one or whenever possible two or more substituents selected from C1-4- alkyloxy, hydroxy, halo, Het2-, NR7R8, -carbonyl-NR9R10 or Het3-carbonyl-; R5 and R6 are each independently selected from hydrogen or C1-4 alkyl; R7 and R8 are each independently selected from hydrogen, C1-4 alkyl, Het8, aminosulfonyl-, mono- or di (C1-4 alkyl) -aminosulfonyl, hydroxy-C1-4 alkyl, C1-4 alkyloxy-C1- alkyl 4, hydroxycarbonylalkylC 1-4, cycloalkylC3-6, Het9-carbonylalkylC 1-4, Het10-carbonyl, polyhydroxyalkylC 1-4, Het11-alkylC 1-4 or Ar2-alkylC 1-4; R9 and R10 are each independently selected from hydrogen, C1-4 alkyl, C3-6 cycloalkyl, Het4, C1-4 hydroxyalkyl, C1-4 alkyloxy-C1-4 alkyl or C1-4 polyhydroxyalkyl; R11 represents hydrogen, C1-4 alkyl, Het5, Het6-C1-4 alkyl-C2-4 alkenylcarbonyl, optionally substituted with Het7-C1-4 alkylaminocarbonyl, C2-4 alkenylsulfonyl, C1-4 alkyloxy-C1-4 alkyl or phenyl optionally substituted with one or whenever possible two or more substituents selected from hydrogen, hydroxy, amino, C1-4 alkyloxy; R12 represents hydrogen, C1-4 alkyl, C1-4 alkyloxycarbonyl, Het16-C1-4 alkyl, phenylC 1-4 alkyloxycarbonyl, Het17, C2-4 alkenylcarbonyl optionally substituted with Het19 C 1-4 alkylaminocarbonyl, C2-4 alkylsulfonyl C1-4 alkyl or phenyl substituted with one or whenever possible two or more substituents selected from hydrogen, hydroxy, amino or C1-4 alkyloxy; R13 represents hydrogen, C1-4 alkyl, Het13, Het14-C1-4 alkyl or phenyl optionally substituted with one or whenever possible two or more substituents selected from hydrogen, hydroxy, amino or C1-4 alkyloxy; R14 and R15 are independently selected from hydrogen, C1-4 alkyl, Het15-C1-4 alkyl or C1-4 alkyloxy-C1-4 alkyl; R16 and R17 independently represent hydrogen or C1-4 alkyl optionally substituted with phenyl, indolyl, methylsulfide, hydroxy, thiol, hydroxyphenyl, aminocarbonyl, hydroxycarbonyl, amine, imidazoyl or guanidino; R18 and R19 each independently represent hydrogen or C1-4 alkyl optionally substituted with phenyl, indolyl, methylsulfide, hydroxy, thiol, hydroxyphenyl, aminocarbonyl, hydroxycarbonyl, amino, imidazoyl or guanidino; R20 and R22 independently each represent hydrogen or C1-4 alkyl optionally substituted with hydroxy or C1-4 alkyloxy; R21 represents hydrogen, C1-4 alkyl, Het23-C1-4 alkylcarbonyl or R21 represents mono- or di (C1-4 alkyl) aminoC 1-4 alkylcarbonyl optionally substituted with hydroxy, pyrimidinyl, dimethylamino or C1-4 alkyloxy; Het1 represents a heterocycle selected from piperidinyl, morpholinyl, piperazinyl, furanyl, pyrazolyl, dioxolanyl, thiazolyl, oxazolyl, imidazolyl, isoxazolyl, oxadiazolyl, pyridinyl or pyrrolidinyl wherein said Het1 is optionally substituted with amino, C1-4alkyl, hydroxyalkyl , C1-4 phenylalkyl, C1-4 alkyloxy-C1-4 alkyl, mono- or di (C1-4 alkyl) amino- or aminocarbonyl; Het2 represents a heterocycle selected from morpholinyl, piperazinyl, piperidinyl, pyrrolidinyl, thiomorpholinyl or dithianyl where said Het2 is optionally substituted with one or whenever possible two or more substituents selected from hydroxy, halo, amino, C1-4 alkyl, C1 hydroxyalkyl -4-, C 1-4 alkyloxyC 1-4 alkyl, hydroxyC 1-4 alkyloxyC 1-4 alkyl, mono- or di (C 1-4 alkyl) amino-, mono- or di (C 1-4 alkyl) amino-alkyl C1-4-, C1-4- aminoalkyl, mono- or di (C1-4 alkyl) amino-sulfonyl, aminosulfonyl; Het3, Het4 and Het8 each independently represents a heterocycle selected from morpholinyl, piperazinyl, piperidinyl, furanyl, pyrazolyl, dioxolanyl, thiazolyl, oxazolyl, imidazolyl, isoxazolyl, oxadiazolyl, pyridinyl or pyrrolidinyl wherein said Het3, Het4 are substituted for optionally with one or whenever possible two or more substituents selected from hydroxy-, amino-, C1-4 alkyl, C3-6 cycloalkyl C1-4 alkyl, aminosulfonyl, mono- or di (C1-4 alkyl) aminosulfonyl or aminoalkyl C1- 4; Het5 represents a heterocycle selected from pyrrolidinyl or piperidinyl optionally substituted with one or whenever possible two or more substituents selected from C1-4 alkyl, C3-6 cycloalkyl, C1-4 hydroxyalkyl, C1-4 alkyloxyC1-4 alkyl or polyhydroxy- C1-4 alkyl; Het6 and Het7 each independently represent a heterocycle selected from morpholinyl, pyrrolidinyl, piperazinyl or piperidinyl optionally substituted with one or whenever possible two or more substituents selected from C1-4 alkyl, C3-6 cycloalkyl, C1-4- hydroxyalkyl, C1-4 alkyloxy C1-4alkyl or C1-4 polyhydroxyalkyl; Het9 and Het10 each independently represent a heterocycle selected from furanyl, piperidinyl, morpholinyl, piperazinyl, pyrazolyl, dioxolanyl, thiazolyl, oxazolyl, imidazolyl, isoxazolyl, oxadiazolyl, pyridinyl wherein said Het9 or Het10 are optionally substituted with C1-4 alkyl, C3-6 cycloalkylC 1-4 alkyl- or C1-4 aminoalkyl; Het11 represents a heterocycle selected from indolyl or of formula (2); Het12 represents a heterocycle selected from morpholinyl, piperazinyl, piperidinyl, pyrrolidinyl, thiomorpholinyl or dithianyl where said Het12 is optionally substituted with one or whenever possible two or more substituents selected from hydroxy, halo, amino, C1-4- alkyl, hydroxyalkyl C1-4-, C1-4 alkyloxy C1-4 alkyl, hydroxy C1-4 alkyl-C1-4 alkyl, mono- or di (C1-4 alkyl) amino- or mono- or di (C1-4 alkyl) amino-C1 alkyl -4-; Het13 represents a heterocycle selected from pyrrolidinyl or piperidinyl optionally substituted with one or whenever possible two or more substituents selected from C1-4alkyl, C3-6cycloalkyl, C1-4- hydroxyalkyl, C1-4alkyloxyC1-4alkyl or polyhydroxyalkyl C1-4; Het14 represents a heterocycle selected from morpholinyl, pyrrolidinyl, piperazinyl or piperidinyl optionally substituted with one or whenever possible two or more substituents selected from C1-4 alkyl, C3-6 cycloalkyl, C1-4 hydroxyalkyl, C1-4 alkyloxy C1-4 or C1-4 polyhydroxyalkyl; Het15 represents a heterocycle selected from morpholinyl, pyrrolidinyl, piperazinyl or piperidinyl optionally substituted with one or whenever possible two or more substituents selected from C1-4 alkyl, C3-6 cycloalkyl, C1-4 hydroxyalkyl, C1-4 alkyloxy C1-4 or C1-4 polyhydroxyalkyl; Het16 represents a heterocycle selected from morpholinyl, pyrrolidinyl, piperazinyl 1,3,2-dioxaborolane or piperidinyl wherein said heterocycle is optionally substituted with one or more substituents selected from C1-4 alkyl; and Het17 represents a heterocycle selected from pyrrolidinyl or piperidinyl optionally substituted with one or whenever possible two or more substituents selected from C1-4 alkyl, cycloalkyl |
| priorityDate | 2003-05-27-04:00^^<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: 42.