http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-039203-A1

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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0a910d33c239980f3a705e312c5bad6a
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filingDate 2003-03-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ff7807f944795f366cd012bdbe4eaffb
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1237042c631dc381f80c33b943103269
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1711464c50297875721d805f71f65db1
publicationDate 2005-02-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-039203-A1
titleOfInvention QUINAZOLINE DERIVATIVES
abstract Quinazoline derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-proliferative agent in the prevention or treatment of tumors that are sensitive to erbB inhibition of receptor tyrosine kinases . Claim 1: A quinazoline derivative characterized in that it responds to formula (1), wherein G1 and G2 each independently is halogen; X1 is a direct link or O; R1 is selected from H and C1-6 alkyl, where the C1-6 alkyl group is optionally substituted by one or more substituents, which may be the same or different, selected from hydroxy and halogen, and / or a substituent selected from amino, nitro , carboxy, cyano, halogen C1-6 alkoxy, hydroxy (C1-6) alkoxy, C2-8 alkenyl, C2-8 alkynyl; C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, C1-6 alkylamino, di [(C1-6) alkyl] amino, carbamoyl, N- (C1-6) alkylcarbamoyl, N, N-di [(C1 -6) alkyl] carbamoyl, C2-6 alkanoyl, C2-6 alkanoyloxy, C2-6 alkanoylamino, N- (C1-6) alkyl- (C2-6) alkanoylamino, C1-6 alkoxycarbonyl, sulfamoyl, N- (C1- 6) alkylsulfamoyl, N, N-di - [(C1-6) alkyl] sulfamoyl, (C1-6) alkanesulfonylamino and N- (C1-6) alkyl- (C1-6) alkanesulfonylamino, X2 is a direct bond or [ CR2R3] m, where m is an integer between 1 and 6, and each of R2 and R3 independently is selected from H, hydroxy, C1-4 alkyl and hydroxy (C1-4) alkyl; Q1 is (C3-7) cycloalkyl or heterocyclyl, where Q1 optionally has 1, 2 or 3 substituents, which may be the same or different, selected from halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, hydroxy, amino, carboxy, carbamoyl, acryloyl , C1-6 alkyl, C2-8 alkenyl, C2-8 alkynyl, C1-6 alkoxy, C2-6 alkenyloxy, C2-6 alkynyloxy C1-6 alkylthio, C2-6 alkenylthio, C2-6 alkynylthio, C1-6 alkylsulfinyl, C2-6 alkenylsulfinyl, C2-6 alkylsulfinyl, C1-6 alkylsulfonyl, C2-6 alkenylsulfonyl, C2-6 alkylsulfonyl, C1-6 alkylamino, di [(C1-6) alkyl] amino, C1-6 alkoxycarbonyl, N- (C1 -6) alkylcarbamoyl, N, N-di - [(C1-6) alkyl] carbamoyl, C2-6 alkanoyl, C2-6 alkanoyloxy, C2-6 alkanoylamino, N- (C1-6) alkyl- (C2- 6) alkanoylamino, sulfamoyl, N- (C1-6) alkylsulfamoyl, N, N-di [(C1-6) alkyl] sulfamoyl, C1-6 alkanesulfonylamino, N- (C1-6) alkyl- (C1-6) alkanesulfonylamino , carbamoyl (C1-6) alkyl, N- (C1-6) alkylcarbamoyl (C1-6) alkyl, N, N-di - [(C1-6) alkyl] carbamoyl (C1-6) alkyl yl, sulfamoyl (C1-6) alkyl, N- (C1-6) alkylsulfasmoyl (C1-6) alkyl, NN-di - [(C1-6) alkyl] sulfamoyl (C1-6) alkyl, (C2-6) (C1-6) alkanoyl, C2-6) alkyl (C1-6) alkanoyloxy, (C2-6) alkanoylamino (C1-6) alkyl, N- (C1-6) alkyl- (C2-6) alkanoylamino and ( C1-6) (C1-6) alkoxycarbonyl alkyl, or between a group of the formula Q2-X3- where X3 is CO and Q2 is heterocyclyl, and where Q2 optionally has 1 or 2 substituents, which may be the same or different, selected between halogen, hydroxy, (C1-4) alkyl, (C2-4) alkanoyl and C1-4) alkylsulfonyl; and where any (C1-6) alkyl, C2-8 alkenyl, C2-8 alkynyl, and C2-6 alkanoyl group within Q1 optionally has one or more substituents that may be the same or different selected from halogen, hydroxy and C1-6 alkyl and / or optionally a substituent selected from cyano, nitro, carboxy, C2-8 alkenyl, C2-8 alkynyl, C1-6 alkoxy, C1-6 hydroxyalkoxy, (C1-4) alkoxy (C1-6) alkoxy, C2 alkanoyl -6, C2-6 alkanoyloxy and NRaRb, where Ra is H or C1-4 alkyl and Rb is H or C1-4 alkyl, and where any C1-4 alkyl in Ra or Rb optionally has one or more substituents, which may be same or different, selected from halogen and hydroxy and / or optionally a substituent selected from cyano, nitro, C2-4 alkenyl, C2-4 alkynyl, C1-4 alkoxy, hydroxy (C1-4) alkoxy and (C1-2) alkoxy (C1-4) alkoxy, or Ra and Rb together with the N atom to which they are attached form a ring of 4, 5 or 6 members, which optionally has 1 or 2 substituents, which may be the same or differ tes, on a C atom of the ring selected from halogen, hydroxy, C1-4 alkyl, and C1-3 alkylenedioxy, and optionally a substituent (as long as the ring does not quaternize) may be selected on any available N of the ring between C1-4 alkyl, C2-4 alkanoyl and C1-4 alkylsulfonyl, and where any C1-4 alkyl or C2-4 alkanoyl group present as a substituent on the ring formed by Ra and Rb together with the N atom to which they are optionally bound has one or more substituents, which may be the same or different, selected from halogen and hydroxy and / or optionally a substituent selected from C1-4 alkyl and C1-4 alkoxy, and where any heterocyclyl group within the group Q1-X2- , optionally has 1 or 2 oxo (= O) or thioxo (= S) substituents; or a salt acceptable for pharmaceutical use thereof.
priorityDate 2002-03-28-04:00^^<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: 47.