NZ540092A - Cyanoguanidines and cyanoamidines as ErbB2 and EGFR inhibitors - Google Patents
Cyanoguanidines and cyanoamidines as ErbB2 and EGFR inhibitorsInfo
- Publication number
- NZ540092A NZ540092A NZ540092A NZ54009203A NZ540092A NZ 540092 A NZ540092 A NZ 540092A NZ 540092 A NZ540092 A NZ 540092A NZ 54009203 A NZ54009203 A NZ 54009203A NZ 540092 A NZ540092 A NZ 540092A
- Authority
- NZ
- New Zealand
- Prior art keywords
- compound
- nr7r9
- heteroaryl
- aryl
- heterocyclyl
- Prior art date
Links
- QGBSISYHAICWAH-UHFFFAOYSA-N dicyandiamide Chemical class NC(N)=NC#N QGBSISYHAICWAH-UHFFFAOYSA-N 0.000 title claims description 5
- 229940121647 egfr inhibitor Drugs 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 94
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract description 79
- 125000003118 aryl group Chemical group 0.000 claims abstract description 77
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract description 75
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 57
- 125000003710 aryl alkyl group Chemical group 0.000 claims abstract description 52
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims abstract description 51
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims abstract description 51
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 48
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract description 46
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- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims abstract description 34
- 125000003342 alkenyl group Chemical group 0.000 claims abstract description 33
- 125000000304 alkynyl group Chemical group 0.000 claims abstract description 33
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract description 33
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract description 31
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 27
- 201000010099 disease Diseases 0.000 claims abstract description 26
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- -1 enantiomers Chemical class 0.000 claims description 52
- 239000000203 mixture Substances 0.000 claims description 49
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- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims description 25
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- 125000005842 heteroatom Chemical group 0.000 claims description 13
- 150000002431 hydrogen Chemical group 0.000 claims description 13
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- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims description 9
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- 125000005865 C2-C10alkynyl group Chemical group 0.000 claims description 7
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- 239000011737 fluorine Chemical group 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
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- 229910052794 bromium Inorganic materials 0.000 claims description 5
- 125000002837 carbocyclic group Chemical group 0.000 claims description 5
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- OUYYNZDOJHSQBW-UHFFFAOYSA-N cyanomethanimidamide Chemical group NC(=N)C#N OUYYNZDOJHSQBW-UHFFFAOYSA-N 0.000 claims description 3
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 2
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Classifications
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- 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
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Virology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42754402P | 2002-11-20 | 2002-11-20 | |
| PCT/US2003/035670 WO2004046101A2 (en) | 2002-11-20 | 2003-11-10 | Cyanoguanidines and cyanoamidines as erbb2 and egfr inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ540092A true NZ540092A (en) | 2007-06-29 |
Family
ID=32326558
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ540092A NZ540092A (en) | 2002-11-20 | 2003-11-10 | Cyanoguanidines and cyanoamidines as ErbB2 and EGFR inhibitors |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP1567506A4 (enExample) |
| JP (1) | JP4611745B2 (enExample) |
| AU (1) | AU2003291394B2 (enExample) |
| CA (1) | CA2506503A1 (enExample) |
| NZ (1) | NZ540092A (enExample) |
| WO (1) | WO2004046101A2 (enExample) |
Families Citing this family (21)
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|---|---|---|---|---|
| US6562319B2 (en) | 2001-03-12 | 2003-05-13 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Radiolabeled irreversible inhibitors of epidermal growth factor receptor tyrosine kinase and their use in radioimaging and radiotherapy |
| SG135193A1 (en) * | 2003-08-18 | 2007-09-28 | Pfizer Prod Inc | Dosing schedule for erbb2 anticancer agents |
| JP2007505101A (ja) * | 2003-09-11 | 2007-03-08 | イッサム リサーチ ディベロップメント カンパニー オブ ザ ヘブリュー ユニバーシティー オブ エルサレム | 放射性標識されたアニリノキナゾリン型化合物ならびに放射線画像化および放射線治療におけるその使用 |
| GB0326459D0 (en) | 2003-11-13 | 2003-12-17 | Astrazeneca Ab | Quinazoline derivatives |
| AU2005284796A1 (en) | 2004-09-15 | 2006-03-23 | Janssen Pharmaceutica, N.V. | Thiazolopyridine kinase inhibitors |
| US7579356B2 (en) | 2005-05-04 | 2009-08-25 | Janssen Pharmaceutica Nv | Thia-tetraazaacenaphthylene kinase inhibitors |
| DE102006012251A1 (de) * | 2006-03-15 | 2007-11-08 | Grünenthal GmbH | Substituierte 4-Amino-chinazolin-Derivate und ihre Verwendung zur Herstellung von Arzneimitteln |
| CL2007003158A1 (es) | 2006-11-02 | 2008-05-16 | Astrazeneca Ab | Procedimiento de preparacion de compuestos derivados de quinazolina o sus sales farmaceuticamente aceptables; compuestos intermediarios; procedimiento de preparacion. |
| EP2220054A2 (en) | 2007-10-29 | 2010-08-25 | Natco Pharma Limited | Novel 4-(tetrazol-5-yl)-quinazoline derivatives as anti cancer agents |
| CA2804190A1 (en) * | 2009-07-02 | 2011-01-06 | Newgen Therapeutics, Inc. | Phosphorus containing quinazoline compounds and methods of use |
| US9353122B2 (en) | 2013-02-15 | 2016-05-31 | Kala Pharmaceuticals, Inc. | Therapeutic compounds and uses thereof |
| US9688688B2 (en) | 2013-02-20 | 2017-06-27 | Kala Pharmaceuticals, Inc. | Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof |
| US9353123B2 (en) | 2013-02-20 | 2016-05-31 | Kala Pharmaceuticals, Inc. | Therapeutic compounds and uses thereof |
| KR20160099084A (ko) | 2013-11-01 | 2016-08-19 | 칼라 파마슈티컬스, 인크. | 치료 화합물의 결정질 형태 및 그의 용도 |
| US9890173B2 (en) | 2013-11-01 | 2018-02-13 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| WO2017122205A1 (en) | 2016-01-13 | 2017-07-20 | Hadasit Medical Research Services And Development Ltd. | Radiolabeled erlotinib analogs and uses thereof |
| WO2018048750A1 (en) | 2016-09-08 | 2018-03-15 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| US10253036B2 (en) | 2016-09-08 | 2019-04-09 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| EP3509421A4 (en) | 2016-09-08 | 2020-05-20 | Kala Pharmaceuticals, Inc. | CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF |
| CN108285421A (zh) * | 2018-01-26 | 2018-07-17 | 黑龙江鑫创生物科技开发有限公司 | 一种微通道反应器合成拉帕替尼中间体的方法 |
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Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE446955T1 (de) * | 1995-03-30 | 2009-11-15 | Pfizer Prod Inc | Chinazolinone derivate |
| GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| CA2242425C (en) * | 1996-02-13 | 2006-07-18 | Zeneca Limited | Quinazoline derivatives as vegf inhibitors |
| HRP970371A2 (en) | 1996-07-13 | 1998-08-31 | Kathryn Jane Smith | Heterocyclic compounds |
| DE69943144D1 (de) | 1998-03-31 | 2011-03-03 | Kyowa Hakko Kirin Co Ltd | Stickstoffenthaltende heterocyclische verbindungen |
| GB2345486A (en) | 1999-01-11 | 2000-07-12 | Glaxo Group Ltd | Heteroaromatic protein tyrosine kinase inhibitors |
| UA71945C2 (en) | 1999-01-27 | 2005-01-17 | Pfizer Prod Inc | Substituted bicyclic derivatives being used as anticancer agents |
| CN1437594A (zh) | 2000-06-22 | 2003-08-20 | 辉瑞产品公司 | 用于治疗异常细胞生长的取代的双环衍生物 |
-
2003
- 2003-11-10 NZ NZ540092A patent/NZ540092A/en not_active IP Right Cessation
- 2003-11-10 EP EP03768789A patent/EP1567506A4/en not_active Withdrawn
- 2003-11-10 JP JP2004553551A patent/JP4611745B2/ja not_active Expired - Fee Related
- 2003-11-10 WO PCT/US2003/035670 patent/WO2004046101A2/en not_active Ceased
- 2003-11-10 CA CA002506503A patent/CA2506503A1/en not_active Abandoned
- 2003-11-10 AU AU2003291394A patent/AU2003291394B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JP4611745B2 (ja) | 2011-01-12 |
| EP1567506A4 (en) | 2007-06-20 |
| EP1567506A2 (en) | 2005-08-31 |
| AU2003291394B2 (en) | 2009-06-25 |
| WO2004046101A2 (en) | 2004-06-03 |
| AU2003291394A1 (en) | 2004-06-15 |
| JP2006508979A (ja) | 2006-03-16 |
| CA2506503A1 (en) | 2004-06-03 |
| WO2004046101A3 (en) | 2004-09-16 |
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