ZA200209412B - Substituted quinazoline derivatives and their use as inhibitors. - Google Patents
Substituted quinazoline derivatives and their use as inhibitors. Download PDFInfo
- Publication number
- ZA200209412B ZA200209412B ZA200209412A ZA200209412A ZA200209412B ZA 200209412 B ZA200209412 B ZA 200209412B ZA 200209412 A ZA200209412 A ZA 200209412A ZA 200209412 A ZA200209412 A ZA 200209412A ZA 200209412 B ZA200209412 B ZA 200209412B
- Authority
- ZA
- South Africa
- Prior art keywords
- optionally substituted
- group
- formula
- alkyl
- salkyl
- Prior art date
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- 239000003112 inhibitor Substances 0.000 title description 3
- 125000002294 quinazolinyl group Chemical class N1=C(N=CC2=CC=CC=C12)* 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims description 96
- -1 1-methyl-4-nitro-1H-imidazol-5-yl Chemical group 0.000 claims description 79
- 229910052739 hydrogen Inorganic materials 0.000 claims description 67
- 239000001257 hydrogen Substances 0.000 claims description 67
- 125000000217 alkyl group Chemical group 0.000 claims description 58
- 125000000623 heterocyclic group Chemical group 0.000 claims description 54
- 239000000203 mixture Substances 0.000 claims description 41
- 150000002148 esters Chemical class 0.000 claims description 37
- 150000002431 hydrogen Chemical class 0.000 claims description 37
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 33
- 125000003118 aryl group Chemical group 0.000 claims description 31
- 125000001424 substituent group Chemical group 0.000 claims description 31
- 241000282414 Homo sapiens Species 0.000 claims description 30
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 29
- 238000000034 method Methods 0.000 claims description 28
- 125000005843 halogen group Chemical group 0.000 claims description 27
- 108090000461 Aurora Kinase A Proteins 0.000 claims description 26
- 229910052757 nitrogen Inorganic materials 0.000 claims description 26
- 241001465754 Metazoa Species 0.000 claims description 25
- 150000003839 salts Chemical class 0.000 claims description 25
- 102100032311 Aurora kinase A Human genes 0.000 claims description 24
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 24
- 229910052799 carbon Inorganic materials 0.000 claims description 21
- 125000003545 alkoxy group Chemical group 0.000 claims description 20
- 125000001072 heteroaryl group Chemical group 0.000 claims description 19
- 238000001727 in vivo Methods 0.000 claims description 19
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 18
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 16
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 16
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 16
- 229910052760 oxygen Inorganic materials 0.000 claims description 15
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- 125000005842 heteroatom Chemical group 0.000 claims description 14
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 13
- 239000003814 drug Substances 0.000 claims description 12
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 11
- 230000002401 inhibitory effect Effects 0.000 claims description 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 10
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- 229910052717 sulfur Inorganic materials 0.000 claims description 9
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 8
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- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims description 5
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Classifications
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—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
- C07D409/12—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—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 C07D415/00
- C07D417/02—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 C07D415/00 containing two hetero rings
- C07D417/12—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 C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—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 C07D415/00
- C07D417/14—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 C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (1)
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EP00401842 | 2000-06-28 |
Publications (1)
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ZA200209412A ZA200209412B (en) | 2000-06-28 | 2002-11-19 | Substituted quinazoline derivatives and their use as inhibitors. |
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EP (1) | EP1299381B1 (is) |
JP (1) | JP2004501914A (is) |
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CN (1) | CN1267431C (is) |
AR (1) | AR030432A1 (is) |
AT (1) | ATE394102T1 (is) |
AU (1) | AU2001266505A1 (is) |
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CA (1) | CA2412592A1 (is) |
CZ (1) | CZ20024120A3 (is) |
DE (1) | DE60133897D1 (is) |
EE (1) | EE200200715A (is) |
ES (1) | ES2305081T3 (is) |
HK (1) | HK1053124A1 (is) |
HU (1) | HUP0301236A2 (is) |
IL (1) | IL153246A0 (is) |
IS (1) | IS6656A (is) |
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NZ (1) | NZ522696A (is) |
PL (1) | PL360439A1 (is) |
RU (1) | RU2283311C2 (is) |
SK (1) | SK18102002A3 (is) |
WO (1) | WO2002000649A1 (is) |
ZA (1) | ZA200209412B (is) |
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GB9922171D0 (en) | 1999-09-21 | 1999-11-17 | Zeneca Ltd | Chemical compounds |
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2001
- 2001-06-21 HU HU0301236A patent/HUP0301236A2/hu unknown
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- 2001-06-21 CN CNB018146201A patent/CN1267431C/zh not_active Expired - Fee Related
- 2001-06-21 DE DE60133897T patent/DE60133897D1/de not_active Expired - Fee Related
- 2001-06-21 KR KR1020027017913A patent/KR20030014411A/ko not_active Application Discontinuation
- 2001-06-21 ES ES01944061T patent/ES2305081T3/es not_active Expired - Lifetime
- 2001-06-21 CA CA002412592A patent/CA2412592A1/en not_active Abandoned
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- 2001-06-21 EP EP01944061A patent/EP1299381B1/en not_active Expired - Lifetime
- 2001-06-21 MX MXPA02011974A patent/MXPA02011974A/es unknown
- 2001-06-21 JP JP2002505773A patent/JP2004501914A/ja active Pending
- 2001-06-21 US US10/311,916 patent/US6919338B2/en not_active Expired - Fee Related
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- 2001-06-21 RU RU2003102389/04A patent/RU2283311C2/ru not_active IP Right Cessation
- 2001-06-21 AU AU2001266505A patent/AU2001266505A1/en not_active Abandoned
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NO20026010L (no) | 2002-12-13 |
WO2002000649A1 (en) | 2002-01-03 |
RU2283311C2 (ru) | 2006-09-10 |
SK18102002A3 (sk) | 2003-07-01 |
AU2001266505A1 (en) | 2002-01-08 |
DE60133897D1 (de) | 2008-06-19 |
BG107376A (bg) | 2003-09-30 |
EP1299381B1 (en) | 2008-05-07 |
CA2412592A1 (en) | 2002-01-03 |
US20030187002A1 (en) | 2003-10-02 |
HK1053124A1 (en) | 2003-10-10 |
WO2002000649A9 (en) | 2007-09-20 |
CN1496364A (zh) | 2004-05-12 |
MXPA02011974A (es) | 2004-09-06 |
AR030432A1 (es) | 2003-08-20 |
NZ522696A (en) | 2004-08-27 |
EE200200715A (et) | 2004-08-16 |
BR0111754A (pt) | 2003-04-29 |
ATE394102T1 (de) | 2008-05-15 |
US6919338B2 (en) | 2005-07-19 |
CZ20024120A3 (cs) | 2003-03-12 |
ES2305081T3 (es) | 2008-11-01 |
JP2004501914A (ja) | 2004-01-22 |
PL360439A1 (en) | 2004-09-06 |
US20060046987A1 (en) | 2006-03-02 |
HUP0301236A2 (hu) | 2003-10-28 |
CN1267431C (zh) | 2006-08-02 |
IL153246A0 (en) | 2003-07-06 |
NO20026010D0 (no) | 2002-12-13 |
IS6656A (is) | 2002-12-17 |
KR20030014411A (ko) | 2003-02-17 |
EP1299381A1 (en) | 2003-04-09 |
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