ZA200301510B - Quinazoline derivatives as kinase inhibitors. - Google Patents
Quinazoline derivatives as kinase inhibitors. Download PDFInfo
- Publication number
- ZA200301510B ZA200301510B ZA200301510A ZA200301510A ZA200301510B ZA 200301510 B ZA200301510 B ZA 200301510B ZA 200301510 A ZA200301510 A ZA 200301510A ZA 200301510 A ZA200301510 A ZA 200301510A ZA 200301510 B ZA200301510 B ZA 200301510B
- Authority
- ZA
- South Africa
- Prior art keywords
- methoxy
- quinazolin
- piperazinyl
- carboxamide
- amended sheet
- Prior art date
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- 229940043355 kinase inhibitor Drugs 0.000 title description 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 title description 2
- 125000002294 quinazolinyl group Chemical class N1=C(N=CC2=CC=CC=C12)* 0.000 title 1
- -1 nitrogen-containing heterocyclic compound Chemical class 0.000 claims description 39
- 150000003839 salts Chemical class 0.000 claims description 39
- 150000001875 compounds Chemical class 0.000 claims description 30
- 238000000034 method Methods 0.000 claims description 23
- 125000004546 quinazolin-4-yl group Chemical group N1=CN=C(C2=CC=CC=C12)* 0.000 claims description 17
- 239000000203 mixture Substances 0.000 claims description 14
- 125000004193 piperazinyl group Chemical group 0.000 claims description 13
- 201000010099 disease Diseases 0.000 claims description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
- 230000002401 inhibitory effect Effects 0.000 claims description 12
- 150000004677 hydrates Chemical class 0.000 claims description 10
- 229940002612 prodrug Drugs 0.000 claims description 10
- 239000000651 prodrug Substances 0.000 claims description 10
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- 230000026731 phosphorylation Effects 0.000 claims description 8
- 238000006366 phosphorylation reaction Methods 0.000 claims description 8
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
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Classifications
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
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- 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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- 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
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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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- Chemical & Material Sciences (AREA)
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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
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US22612200P | 2000-08-18 | 2000-08-18 |
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ZA200301510B true ZA200301510B (en) | 2004-06-22 |
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ZA200301510A ZA200301510B (en) | 2000-08-18 | 2003-02-26 | Quinazoline derivatives as kinase inhibitors. |
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US (5) | US6982266B2 (no) |
EP (3) | EP1964839A3 (no) |
JP (1) | JP5073147B2 (no) |
KR (1) | KR100831116B1 (no) |
CN (1) | CN100358890C (no) |
AT (1) | ATE402169T1 (no) |
AU (1) | AU8544901A (no) |
BR (1) | BR0113356A (no) |
CA (1) | CA2426440C (no) |
CY (1) | CY1110460T1 (no) |
CZ (1) | CZ304061B6 (no) |
DE (1) | DE60134990D1 (no) |
DK (1) | DK1315715T3 (no) |
EA (1) | EA005809B1 (no) |
ES (1) | ES2311023T3 (no) |
HK (1) | HK1057206A1 (no) |
HU (1) | HU228668B1 (no) |
IL (2) | IL154514A0 (no) |
MX (1) | MXPA03001359A (no) |
NO (1) | NO323782B1 (no) |
NZ (1) | NZ524461A (no) |
PT (1) | PT1315715E (no) |
SI (1) | SI1315715T1 (no) |
WO (1) | WO2002016351A1 (no) |
ZA (1) | ZA200301510B (no) |
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PT1315715E (pt) * | 2000-08-18 | 2008-10-30 | Millennium Pharm Inc | Derivados de quianazolina utilizados como inibidores de quinase |
AU2002217999A1 (en) | 2000-11-01 | 2002-05-15 | Cor Therapeutics, Inc. | Process for the production of 4-quinazolinylpiperazin-1-carboxylic acid phenylamides |
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UA95641C2 (en) * | 2006-07-06 | 2011-08-25 | Эррей Биофарма Инк. | Hydroxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors |
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WO2008128072A2 (en) * | 2007-04-13 | 2008-10-23 | Supergen, Inc. | Axl kinase inhibitors useful for the treatment of cancer or hyperproliferative disorders |
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ES2834093T3 (es) | 2011-07-21 | 2021-06-16 | Sumitomo Dainippon Pharma Oncology Inc | Inhibidores de proteína quinasa heterocíclicos |
CN102942529B (zh) * | 2012-11-09 | 2015-06-24 | 贵州大学 | 4-(4-取代哌嗪)-5,6,7-三烷氧基喹唑啉类化合物及其制备方法和应用 |
UY35464A (es) | 2013-03-15 | 2014-10-31 | Araxes Pharma Llc | Inhibidores covalentes de kras g12c. |
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WO2015009889A1 (en) | 2013-07-18 | 2015-01-22 | Concert Pharmaceuticals, Inc. | Deuterated intedanib derivatives and their use for the treatment of proliferative disorders |
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JP2018513853A (ja) | 2015-04-10 | 2018-05-31 | アラクセス ファーマ エルエルシー | 置換キナゾリン化合物およびその使用方法 |
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EP3364977A4 (en) | 2015-10-19 | 2019-09-04 | Araxes Pharma LLC | PROCESS FOR SCREENING INHIBITORS OF RAS |
EA038635B9 (ru) | 2015-11-16 | 2021-10-26 | Араксис Фарма Ллк | 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения |
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CN110036010A (zh) | 2016-09-29 | 2019-07-19 | 亚瑞克西斯制药公司 | Kras g12c突变蛋白的抑制剂 |
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CN110382482A (zh) | 2017-01-26 | 2019-10-25 | 亚瑞克西斯制药公司 | 稠合的杂-杂二环化合物及其使用方法 |
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JP2020521741A (ja) | 2017-05-25 | 2020-07-27 | アラクセス ファーマ エルエルシー | がんの処置のための化合物およびその使用の方法 |
BR112019024674A2 (pt) | 2017-05-25 | 2020-06-16 | Araxes Pharma Llc | Inibidores covalentes da kras |
CA3096984A1 (en) | 2018-04-05 | 2019-10-10 | Sumitomo Dainippon Pharma Oncology, Inc. | Axl kinase inhibitors and use of the same |
CN108570039B (zh) * | 2018-04-25 | 2022-09-23 | 上海美迪西生物医药股份有限公司 | 一类具有抑制抗凋亡蛋白活性的化合物及其制备和应用 |
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CN111773440A (zh) * | 2020-05-22 | 2020-10-16 | 南京大学 | 一种基于类酶催化反应的抗凝血材料 |
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WO1992020642A1 (en) | 1991-05-10 | 1992-11-26 | Rhone-Poulenc Rorer International (Holdings) Inc. | Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase |
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TW225528B (no) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
GB9510757D0 (en) | 1994-09-19 | 1995-07-19 | Wellcome Found | Therapeuticaly active compounds |
EP0882717B1 (en) * | 1996-10-01 | 2010-09-08 | Kyowa Hakko Kirin Co., Ltd. | Nitrogenous heterocyclic compounds |
AU3053999A (en) * | 1998-03-31 | 1999-10-25 | Kyowa Hakko Kogyo Co. Ltd. | Nitrogenous heterocyclic compounds |
EP1309568B1 (en) | 2000-08-18 | 2011-02-16 | Millennium Pharmaceuticals, Inc. | [(quinazolin-4-yl)piperazin-4-yl]thiocarboxamide compounds as inhibitors of the phosphorylation of a PDGF receptor |
ATE483693T1 (de) | 2000-08-18 | 2010-10-15 | Millennium Pharm Inc | N-aryl-ä4-ä7-(alkoxy)chinazolin-4- ylüpiperazinylücarboxamid-verbindungen als pdgf- rezeptoren hemmer |
PT1315715E (pt) * | 2000-08-18 | 2008-10-30 | Millennium Pharm Inc | Derivados de quianazolina utilizados como inibidores de quinase |
AU2001293207A1 (en) | 2000-08-18 | 2002-03-04 | Cor Therapeutics, Inc. | Nitrogenous heterocyclic compounds |
AU2002254152A1 (en) | 2001-03-08 | 2002-09-24 | Millennium Pharmaceuticals | (homo) piperazine substituted quinolines for inhibiting the phosphorylation of kinases |
US7132427B2 (en) * | 2001-06-21 | 2006-11-07 | Ariad Pharmaceuticals, Inc. | Quinazolines and uses thereof |
US7456189B2 (en) * | 2003-09-30 | 2008-11-25 | Boehringer Ingelheim International Gmbh | Bicyclic heterocycles, medicaments containing these compounds, their use and processes for their preparation |
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2001
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- 2001-08-17 KR KR1020037002381A patent/KR100831116B1/ko not_active IP Right Cessation
- 2001-08-17 CN CNB018173527A patent/CN100358890C/zh not_active Expired - Fee Related
- 2001-08-17 DE DE60134990T patent/DE60134990D1/de not_active Expired - Lifetime
- 2001-08-17 ES ES01964612T patent/ES2311023T3/es not_active Expired - Lifetime
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- 2001-08-17 DK DK01964612T patent/DK1315715T3/da active
- 2001-08-17 MX MXPA03001359A patent/MXPA03001359A/es active IP Right Grant
- 2001-08-17 CZ CZ20030765A patent/CZ304061B6/cs not_active IP Right Cessation
- 2001-08-17 EP EP08075237A patent/EP1964839A3/en not_active Ceased
- 2001-08-17 IL IL15451401A patent/IL154514A0/xx active IP Right Grant
- 2001-08-17 AT AT01964612T patent/ATE402169T1/de active
- 2001-08-17 EP EP10182322A patent/EP2277877A1/en not_active Withdrawn
- 2001-08-17 HU HU0302615A patent/HU228668B1/hu not_active IP Right Cessation
- 2001-08-17 US US10/344,736 patent/US6982266B2/en not_active Expired - Fee Related
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- 2001-08-17 EP EP01964612A patent/EP1315715B1/en not_active Expired - Lifetime
- 2001-08-17 SI SI200130872T patent/SI1315715T1/sl unknown
- 2001-08-17 BR BR0113356-0A patent/BR0113356A/pt active Search and Examination
- 2001-08-17 WO PCT/US2001/041752 patent/WO2002016351A1/en active IP Right Grant
- 2001-08-17 EA EA200300265A patent/EA005809B1/ru not_active IP Right Cessation
- 2001-08-17 AU AU8544901A patent/AU8544901A/xx active Pending
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- 2003-02-18 IL IL154514A patent/IL154514A/en not_active IP Right Cessation
- 2003-02-26 ZA ZA200301510A patent/ZA200301510B/en unknown
- 2003-11-28 HK HK03108720A patent/HK1057206A1/xx not_active IP Right Cessation
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2005
- 2005-08-22 US US11/210,028 patent/US7560461B2/en not_active Expired - Fee Related
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2008
- 2008-10-21 CY CY20081101177T patent/CY1110460T1/el unknown
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2009
- 2009-05-22 US US12/471,280 patent/US8324205B2/en not_active Expired - Fee Related
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2012
- 2012-11-02 US US13/667,489 patent/US20130274252A1/en not_active Abandoned
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