JP5923043B2 - Ａｋｔ活性の阻害剤 - Google Patents
Ａｋｔ活性の阻害剤 Download PDFInfo
- Publication number
- JP5923043B2 JP5923043B2 JP2012545434A JP2012545434A JP5923043B2 JP 5923043 B2 JP5923043 B2 JP 5923043B2 JP 2012545434 A JP2012545434 A JP 2012545434A JP 2012545434 A JP2012545434 A JP 2012545434A JP 5923043 B2 JP5923043 B2 JP 5923043B2
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- pyrido
- aminocyclobutyl
- dihydro
- oxazin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 0 C*(C)c1n[n]cc1C Chemical compound C*(C)c1n[n]cc1C 0.000 description 7
- TYPLXPVWCKUONI-UHFFFAOYSA-N CCN1c2cc(-c3ccccc3)c(-c3ccc(C4(CCC4)N)cc3)nc2OCC1=O Chemical compound CCN1c2cc(-c3ccccc3)c(-c3ccc(C4(CCC4)N)cc3)nc2OCC1=O TYPLXPVWCKUONI-UHFFFAOYSA-N 0.000 description 1
- SILGLOUOHSMKFL-FITUOABBSA-N CCc1nnc2[n]1C(CC(C)(c1ccccc1)C(c1ccc([C@](C3)(C[C@@]3(C)O)N)cc1)=N1)=C1OC2 Chemical compound CCc1nnc2[n]1C(CC(C)(c1ccccc1)C(c1ccc([C@](C3)(C[C@@]3(C)O)N)cc1)=N1)=C1OC2 SILGLOUOHSMKFL-FITUOABBSA-N 0.000 description 1
- HBBHBUDBNTYHEF-UHFFFAOYSA-N CN(C)CCN(CCc1c2cc(-c3ccccc3)c(-c3ccc(C4(CCC4)N)cc3)n1)C2=O Chemical compound CN(C)CCN(CCc1c2cc(-c3ccccc3)c(-c3ccc(C4(CCC4)N)cc3)n1)C2=O HBBHBUDBNTYHEF-UHFFFAOYSA-N 0.000 description 1
- HUNZOZRXVBGBRY-UHFFFAOYSA-N CN(C)CCN1c(cc(-c2ccccc2)c(-c2ccc(C3(CCC3)N)cc2)n2)c2OCC1=O Chemical compound CN(C)CCN1c(cc(-c2ccccc2)c(-c2ccc(C3(CCC3)N)cc2)n2)c2OCC1=O HUNZOZRXVBGBRY-UHFFFAOYSA-N 0.000 description 1
- WFWFLSFDCGGSPQ-UHFFFAOYSA-N CN(C)c1nnc2[n]1-c(cc(-c1ccccc1)c(-c1ccc(C3(CCC3)N)cc1)n1)c1OC2 Chemical compound CN(C)c1nnc2[n]1-c(cc(-c1ccccc1)c(-c1ccc(C3(CCC3)N)cc1)n1)c1OC2 WFWFLSFDCGGSPQ-UHFFFAOYSA-N 0.000 description 1
- CJCNPBJXBPTLDE-UHFFFAOYSA-N CN1c(cc(CC2CC2)c(-c2ccc(C3(CCC3)N)cc2)n2)c2OCC1=O Chemical compound CN1c(cc(CC2CC2)c(-c2ccc(C3(CCC3)N)cc2)n2)c2OCC1=O CJCNPBJXBPTLDE-UHFFFAOYSA-N 0.000 description 1
- QDKUJSJXDPWWRL-UHFFFAOYSA-N CNc1c(CCc2c-3cc(-c4ccccc4)c(-c4ccc(C5(CCC5)N)cc4)n2)c-3n[nH]1 Chemical compound CNc1c(CCc2c-3cc(-c4ccccc4)c(-c4ccc(C5(CCC5)N)cc4)n2)c-3n[nH]1 QDKUJSJXDPWWRL-UHFFFAOYSA-N 0.000 description 1
- GOFODIWMDFMZID-UHFFFAOYSA-N COCCN1c2cc(-c3ccccc3)c(-c3ccc(C4(CCC4)N)cc3)nc2OCC1=O Chemical compound COCCN1c2cc(-c3ccccc3)c(-c3ccc(C4(CCC4)N)cc3)nc2OCC1=O GOFODIWMDFMZID-UHFFFAOYSA-N 0.000 description 1
- OHXSUVOLMXOMGJ-UHFFFAOYSA-N COCCc1nnc2[n]1-c1cc(-c3ccccc3)c(-c3ccc(C4(CCC4)N)cc3)nc1OC2 Chemical compound COCCc1nnc2[n]1-c1cc(-c3ccccc3)c(-c3ccc(C4(CCC4)N)cc3)nc1OC2 OHXSUVOLMXOMGJ-UHFFFAOYSA-N 0.000 description 1
- MFQGZDBUYHCEIH-PLQXJYEYSA-N C[C@](C1)(C[C@]1(c(cc1)ccc1-c(c(-c1ccccc1)c1)nc(OC2)c1N(C)C2=O)N)O Chemical compound C[C@](C1)(C[C@]1(c(cc1)ccc1-c(c(-c1ccccc1)c1)nc(OC2)c1N(C)C2=O)N)O MFQGZDBUYHCEIH-PLQXJYEYSA-N 0.000 description 1
- GJODULUTTYSFEC-UHFFFAOYSA-N Cc1nc(-c2cc(-c3ccccc3)c(-c3ccc(C4(CCC4)N)cc3)nc2CC2)c2[nH]1 Chemical compound Cc1nc(-c2cc(-c3ccccc3)c(-c3ccc(C4(CCC4)N)cc3)nc2CC2)c2[nH]1 GJODULUTTYSFEC-UHFFFAOYSA-N 0.000 description 1
- XFRVVQLYJIBPIS-UHFFFAOYSA-N Cc1nnc(-c2c[n](C)cn2)[nH]1 Chemical compound Cc1nnc(-c2c[n](C)cn2)[nH]1 XFRVVQLYJIBPIS-UHFFFAOYSA-N 0.000 description 1
- RZVVNYSMQZPUFY-UHFFFAOYSA-N NC1(CCC1)c(cc1)ccc1-c(nc(c(N1C2CCOCC2)c2)OCC1=O)c2-c1ccccc1 Chemical compound NC1(CCC1)c(cc1)ccc1-c(nc(c(N1C2CCOCC2)c2)OCC1=O)c2-c1ccccc1 RZVVNYSMQZPUFY-UHFFFAOYSA-N 0.000 description 1
- XRDQCONVRPMHOA-UHFFFAOYSA-N NC1(CCC1)c(cc1)ccc1-c(nc(c(N1CCCC#N)c2)OCC1=O)c2-c1ccccc1 Chemical compound NC1(CCC1)c(cc1)ccc1-c(nc(c(N1CCCC#N)c2)OCC1=O)c2-c1ccccc1 XRDQCONVRPMHOA-UHFFFAOYSA-N 0.000 description 1
- YFSRGCQKJRDHNS-UHFFFAOYSA-N NC1(CCC1)c(cc1)ccc1-c(nc(c(N1CCCCC#N)c2)OCC1=O)c2-c1ccccc1 Chemical compound NC1(CCC1)c(cc1)ccc1-c(nc(c(N1CCCCC#N)c2)OCC1=O)c2-c1ccccc1 YFSRGCQKJRDHNS-UHFFFAOYSA-N 0.000 description 1
- QYNXYGYYSUZFIY-UHFFFAOYSA-N NC1(CCC1)c(cc1)ccc1-c(nc(c(N1CCO)c2)OCC1=O)c2-c1ccccc1 Chemical compound NC1(CCC1)c(cc1)ccc1-c(nc(c(N1CCO)c2)OCC1=O)c2-c1ccccc1 QYNXYGYYSUZFIY-UHFFFAOYSA-N 0.000 description 1
- GYEMFQKVWHAVNP-UHFFFAOYSA-N NC1(CCC1)c(cc1)ccc1-c(nc(c(N1c2cnccc2)c2)OCS1(=O)=O)c2-c1ccccc1 Chemical compound NC1(CCC1)c(cc1)ccc1-c(nc(c(N1c2cnccc2)c2)OCS1(=O)=O)c2-c1ccccc1 GYEMFQKVWHAVNP-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Quinoline Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0922589.7A GB0922589D0 (en) | 2009-12-23 | 2009-12-23 | Pharmaceutical compounds |
| GB0922589.7 | 2009-12-23 | ||
| PCT/GB2010/002329 WO2011077098A1 (en) | 2009-12-23 | 2010-12-23 | Inhibitors of akt activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013515710A JP2013515710A (ja) | 2013-05-09 |
| JP2013515710A5 JP2013515710A5 (https=) | 2013-10-31 |
| JP5923043B2 true JP5923043B2 (ja) | 2016-05-24 |
Family
ID=41716932
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012545434A Active JP5923043B2 (ja) | 2009-12-23 | 2010-12-23 | Ａｋｔ活性の阻害剤 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US9221838B2 (https=) |
| EP (1) | EP2516435B8 (https=) |
| JP (1) | JP5923043B2 (https=) |
| KR (1) | KR20140015157A (https=) |
| CN (1) | CN102791708B (https=) |
| AU (1) | AU2010334591C1 (https=) |
| BR (1) | BR112012015677A2 (https=) |
| CA (1) | CA2783340C (https=) |
| CY (1) | CY1115686T1 (https=) |
| DK (1) | DK2516435T3 (https=) |
| ES (1) | ES2503794T3 (https=) |
| GB (1) | GB0922589D0 (https=) |
| IL (1) | IL220153A (https=) |
| MX (1) | MX2012007274A (https=) |
| NZ (1) | NZ600453A (https=) |
| PL (1) | PL2516435T3 (https=) |
| PT (1) | PT2516435E (https=) |
| RU (1) | RU2579513C2 (https=) |
| SG (1) | SG181517A1 (https=) |
| SI (1) | SI2516435T1 (https=) |
| WO (1) | WO2011077098A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201205164D0 (en) | 2012-03-23 | 2012-05-09 | Almac Discovery Ltd | Pharmaceutical compounds |
| CA2971763A1 (en) * | 2014-12-23 | 2016-06-30 | Bergenbio Asa | Inhibitors of akt kinase |
| CN111943962A (zh) * | 2015-02-27 | 2020-11-17 | 大鹏药品工业株式会社 | 咪唑并噁嗪晶体、含有所述晶体的药物组合物和制备所述晶体的方法 |
| GB201603779D0 (en) | 2016-03-04 | 2016-04-20 | Mission Therapeutics Ltd | Novel compounds |
| US11208478B2 (en) | 2016-08-07 | 2021-12-28 | The Wistar Institute Of Anatomy And Biology | Methods of detecting and treating a tumor expressing pT346 PDK1 |
| PE20200696A1 (es) * | 2017-06-22 | 2020-06-16 | Curadev Pharma Ltd | Moduladores de moleculas pequenas de sting humana |
| KR102917509B1 (ko) | 2017-09-07 | 2026-01-26 | 오거스타 유니버시티 리서치 인스티튜트, 인크. | 특이적 akt3 활성제 및 이의 용도 |
| GB2600384A (en) * | 2020-09-30 | 2022-05-04 | Vaderis Therapeutics Ag | Allosteric AKT inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia |
| WO2025250545A1 (en) * | 2024-05-28 | 2025-12-04 | Alterome Therapeutics, Inc. | Akt1 modulators |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUT76853A (en) * | 1994-11-14 | 1997-12-29 | Warner Lambert Co | 6-aryl pyrido[2,3-d]pyrimidines and naphthyridines for inhibiting protein tyrosine kinase mediated cellular proliferation and pharmaceutical compositions containing the same |
| TWI301760B (en) * | 2004-02-27 | 2008-10-11 | Merz Pharma Gmbh & Co Kgaa | Tetrahydroquinolinones and their use as antagonists of metabotropic glutamate receptors |
| US7910561B2 (en) * | 2004-12-15 | 2011-03-22 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| US8008317B2 (en) * | 2005-06-10 | 2011-08-30 | Merck Sharp & Dohme Corp. | Inhibitors of akt activtiy |
| CA2656507C (en) * | 2006-07-17 | 2012-03-20 | Amgen Inc. | Quinazoline and pyridopyrimidine derivatives as p38 kinase inhibitors |
| JP2010512312A (ja) | 2006-12-06 | 2010-04-22 | メルク エンド カムパニー インコーポレーテッド | Ａｋｔ活性の阻害剤 |
| AR064010A1 (es) | 2006-12-06 | 2009-03-04 | Merck & Co Inc | Inhibidores de la actividad de la akt |
| US7999107B2 (en) * | 2007-01-31 | 2011-08-16 | Merck Sharp & Dohme Corp. | Substituted pyrano[2,3-B]pyridine derivatives as cannabinoid-1 receptor modulators |
| CA2726317A1 (en) | 2008-06-03 | 2009-12-10 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| EP2299825B1 (en) | 2008-06-03 | 2013-07-31 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
-
2009
- 2009-12-23 GB GBGB0922589.7A patent/GB0922589D0/en not_active Ceased
-
2010
- 2010-12-23 ES ES10800980.4T patent/ES2503794T3/es active Active
- 2010-12-23 SG SG2012041232A patent/SG181517A1/en unknown
- 2010-12-23 RU RU2012131115/04A patent/RU2579513C2/ru not_active IP Right Cessation
- 2010-12-23 EP EP10800980.4A patent/EP2516435B8/en active Active
- 2010-12-23 SI SI201030774T patent/SI2516435T1/sl unknown
- 2010-12-23 DK DK10800980.4T patent/DK2516435T3/da active
- 2010-12-23 AU AU2010334591A patent/AU2010334591C1/en not_active Ceased
- 2010-12-23 BR BRBR112012015677-2A patent/BR112012015677A2/pt not_active Application Discontinuation
- 2010-12-23 WO PCT/GB2010/002329 patent/WO2011077098A1/en not_active Ceased
- 2010-12-23 KR KR1020127019033A patent/KR20140015157A/ko not_active Ceased
- 2010-12-23 CA CA2783340A patent/CA2783340C/en not_active Expired - Fee Related
- 2010-12-23 MX MX2012007274A patent/MX2012007274A/es active IP Right Grant
- 2010-12-23 PT PT108009804T patent/PT2516435E/pt unknown
- 2010-12-23 US US13/517,219 patent/US9221838B2/en active Active
- 2010-12-23 JP JP2012545434A patent/JP5923043B2/ja active Active
- 2010-12-23 PL PL10800980T patent/PL2516435T3/pl unknown
- 2010-12-23 NZ NZ600453A patent/NZ600453A/xx not_active IP Right Cessation
- 2010-12-23 CN CN201080059321.9A patent/CN102791708B/zh active Active
-
2012
- 2012-06-04 IL IL220153A patent/IL220153A/en not_active IP Right Cessation
-
2014
- 2014-10-31 CY CY20141100899T patent/CY1115686T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN102791708B (zh) | 2016-03-02 |
| HK1171013A1 (en) | 2013-03-15 |
| US9221838B2 (en) | 2015-12-29 |
| CY1115686T1 (el) | 2017-01-25 |
| WO2011077098A9 (en) | 2012-04-19 |
| IL220153A0 (en) | 2012-07-31 |
| PT2516435E (pt) | 2014-11-13 |
| CA2783340C (en) | 2015-11-24 |
| RU2012131115A (ru) | 2014-01-27 |
| MX2012007274A (es) | 2012-10-03 |
| EP2516435B1 (en) | 2014-08-06 |
| BR112012015677A2 (pt) | 2015-06-30 |
| CN102791708A (zh) | 2012-11-21 |
| JP2013515710A (ja) | 2013-05-09 |
| AU2010334591B2 (en) | 2014-04-10 |
| SG181517A1 (en) | 2012-07-30 |
| AU2010334591A1 (en) | 2012-06-21 |
| GB0922589D0 (en) | 2010-02-10 |
| CA2783340A1 (en) | 2011-06-30 |
| US20130116243A1 (en) | 2013-05-09 |
| IL220153A (en) | 2015-05-31 |
| WO2011077098A1 (en) | 2011-06-30 |
| PL2516435T3 (pl) | 2015-01-30 |
| NZ600453A (en) | 2013-10-25 |
| EP2516435B8 (en) | 2014-10-15 |
| AU2010334591C1 (en) | 2014-07-31 |
| ES2503794T3 (es) | 2014-10-07 |
| KR20140015157A (ko) | 2014-02-06 |
| SI2516435T1 (sl) | 2014-12-31 |
| RU2579513C2 (ru) | 2016-04-10 |
| DK2516435T3 (da) | 2014-10-13 |
| EP2516435A1 (en) | 2012-10-31 |
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