JP2009508971A - アルコキシインドリノン系プロテインキナーゼ阻害剤 - Google Patents
アルコキシインドリノン系プロテインキナーゼ阻害剤 Download PDFInfo
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- JP2009508971A JP2009508971A JP2008532411A JP2008532411A JP2009508971A JP 2009508971 A JP2009508971 A JP 2009508971A JP 2008532411 A JP2008532411 A JP 2008532411A JP 2008532411 A JP2008532411 A JP 2008532411A JP 2009508971 A JP2009508971 A JP 2009508971A
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- alkyl
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- QUTSKIWJUHDULC-UHFFFAOYSA-N methyl 4-amino-3-hydroxybutanoate Chemical compound COC(=O)CC(O)CN QUTSKIWJUHDULC-UHFFFAOYSA-N 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- KXECLDXTZBKCPW-PDGQHHTCSA-N n-(2-ethoxy-3-morpholin-4-yl-3-oxopropyl)-5-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide Chemical compound CC=1NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C(C)C=1C(=O)NCC(OCC)C(=O)N1CCOCC1 KXECLDXTZBKCPW-PDGQHHTCSA-N 0.000 description 1
- ORIHSDHEMLNZCR-PGNDWZGLSA-N n-[(3s)-4-(dimethylamino)-3-ethoxy-4-oxobutyl]-5-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide Chemical compound CCO[C@H](C(=O)N(C)C)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C ORIHSDHEMLNZCR-PGNDWZGLSA-N 0.000 description 1
- IJDCPFZVPOXIBO-QMDZLVRISA-N n-[(3s)-4-(dimethylamino)-3-methoxy-4-oxobutyl]-5-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide Chemical compound CN(C)C(=O)[C@@H](OC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C IJDCPFZVPOXIBO-QMDZLVRISA-N 0.000 description 1
- VUWAKJWQZWPLMV-YBEGLDIGSA-N n-[3-(dimethylamino)-2-ethoxy-3-oxopropyl]-5-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide Chemical compound CCOC(C(=O)N(C)C)CNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C VUWAKJWQZWPLMV-YBEGLDIGSA-N 0.000 description 1
- RZHOFVFWCVNHPO-DHDCSXOGSA-N n-[3-(dimethylamino)-2-methoxy-3-oxopropyl]-5-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide Chemical compound CN(C)C(=O)C(OC)CNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C RZHOFVFWCVNHPO-DHDCSXOGSA-N 0.000 description 1
- HXWVCRBABUROFU-WQRHYEAKSA-N n-[4-(dimethylamino)-2-ethoxy-4-oxobutyl]-5-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide Chemical compound CN(C)C(=O)CC(OCC)CNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C HXWVCRBABUROFU-WQRHYEAKSA-N 0.000 description 1
- SPVIIPXHQXUWRM-YVLHZVERSA-N n-[4-(dimethylamino)-2-methoxy-4-oxobutyl]-5-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide Chemical compound CN(C)C(=O)CC(OC)CNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C SPVIIPXHQXUWRM-YVLHZVERSA-N 0.000 description 1
- 230000026731 phosphorylation Effects 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
- 238000011533 pre-incubation Methods 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 125000000341 threoninyl group Chemical group [H]OC([H])(C([H])([H])[H])C([H])(N([H])[H])C(*)=O 0.000 description 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
Images
Classifications
-
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- 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
-
- 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
- C07D403/14—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 three or more hetero rings
-
- 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
- C07D405/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US71947405P | 2005-09-22 | 2005-09-22 | |
| PCT/US2006/036946 WO2007038251A1 (en) | 2005-09-22 | 2006-09-21 | Alkoxy indolinone based protein kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009508971A true JP2009508971A (ja) | 2009-03-05 |
| JP2009508971A5 JP2009508971A5 (enExample) | 2009-11-12 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008532411A Withdrawn JP2009508971A (ja) | 2005-09-22 | 2006-09-21 | アルコキシインドリノン系プロテインキナーゼ阻害剤 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US20090305382A1 (enExample) |
| EP (1) | EP1926725A4 (enExample) |
| JP (1) | JP2009508971A (enExample) |
| KR (1) | KR20080046701A (enExample) |
| CN (1) | CN101282965A (enExample) |
| AU (1) | AU2006294600A1 (enExample) |
| BR (1) | BRPI0616378A2 (enExample) |
| CA (1) | CA2621809A1 (enExample) |
| RU (1) | RU2008110083A (enExample) |
| WO (1) | WO2007038251A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2621809A1 (en) * | 2005-09-22 | 2007-04-05 | The Scripps Research Institute | Alkoxy indolinone based protein kinase inhibitors |
| JP2010502741A (ja) | 2006-09-11 | 2010-01-28 | キュリス，インコーポレイテッド | Ｐｔｋインヒビターとしての亜鉛結合部分を含む置換２−インドリノン |
| AU2007294686B2 (en) | 2006-09-15 | 2013-10-31 | Equinox Sciences, Llc | Kinase inhibitor compounds |
| IN2014MN02105A (enExample) | 2012-04-20 | 2015-09-11 | Annji Pharm Co Ltd | |
| EP3114128B1 (en) | 2014-03-07 | 2019-01-02 | F. Hoffmann-La Roche AG | Novel 6-fused heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection |
| ES2798598T3 (es) | 2015-03-16 | 2020-12-11 | Hoffmann La Roche | Tratamiento combinado con un agonista de TLR7 y un inhibidor de ensamblaje de la cápside del VHB |
| ES2894605T3 (es) | 2016-09-13 | 2022-02-15 | Hoffmann La Roche | Tratamiento combinado con un agonista de TLR7 y un inhibidor del ensamblaje de la cápside del VHB |
| CN110016052B (zh) * | 2018-01-08 | 2021-09-28 | 四川海思科制药有限公司 | N-去乙基舒尼替尼的磷酰胺衍生物及其制备方法 |
| WO2020193459A1 (en) | 2019-03-25 | 2020-10-01 | F. Hoffmann-La Roche Ag | Solid forms of a compound of hbv core protein allosteric modifier |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US72934A (en) * | 1867-12-31 | Improvement in marking-gauge fob sswim-mgohines | ||
| AR042586A1 (es) * | 2001-02-15 | 2005-06-29 | Sugen Inc | 3-(4-amidopirrol-2-ilmetiliden)-2-indolinona como inhibidores de la protein quinasa; sus composiciones farmaceuticas; un metodo para la modulacion de la actividad catalitica de la proteinquinasa; un metodo para tratar o prevenir una afeccion relacionada con la proteinquinasa |
| TWI259081B (en) * | 2001-10-26 | 2006-08-01 | Sugen Inc | Treatment of acute myeloid leukemia with indolinone compounds |
| US20080044881A1 (en) * | 2003-11-26 | 2008-02-21 | Congxin Liang | Advanced Indolinone Based Protein Kinase Inhibitors |
| CA2621809A1 (en) * | 2005-09-22 | 2007-04-05 | The Scripps Research Institute | Alkoxy indolinone based protein kinase inhibitors |
-
2006
- 2006-09-21 CA CA002621809A patent/CA2621809A1/en not_active Abandoned
- 2006-09-21 EP EP06815164A patent/EP1926725A4/en not_active Withdrawn
- 2006-09-21 KR KR1020087008492A patent/KR20080046701A/ko not_active Withdrawn
- 2006-09-21 BR BRPI0616378-5A patent/BRPI0616378A2/pt not_active IP Right Cessation
- 2006-09-21 US US11/991,971 patent/US20090305382A1/en not_active Abandoned
- 2006-09-21 US US11/525,291 patent/US7629339B2/en not_active Expired - Fee Related
- 2006-09-21 WO PCT/US2006/036946 patent/WO2007038251A1/en not_active Ceased
- 2006-09-21 CN CNA2006800352235A patent/CN101282965A/zh active Pending
- 2006-09-21 JP JP2008532411A patent/JP2009508971A/ja not_active Withdrawn
- 2006-09-21 RU RU2008110083/04A patent/RU2008110083A/ru not_active Application Discontinuation
- 2006-09-21 AU AU2006294600A patent/AU2006294600A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| KR20080046701A (ko) | 2008-05-27 |
| CN101282965A (zh) | 2008-10-08 |
| US7629339B2 (en) | 2009-12-08 |
| US20070072934A1 (en) | 2007-03-29 |
| CA2621809A1 (en) | 2007-04-05 |
| AU2006294600A1 (en) | 2007-04-05 |
| BRPI0616378A2 (pt) | 2011-06-21 |
| EP1926725A1 (en) | 2008-06-04 |
| RU2008110083A (ru) | 2009-10-27 |
| EP1926725A4 (en) | 2010-10-06 |
| US20090305382A1 (en) | 2009-12-10 |
| WO2007038251A1 (en) | 2007-04-05 |
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