JP5860031B2 - Ｐｄｋ１阻害薬としてのヘテロ環式カルボン酸アミド - Google Patents
Ｐｄｋ１阻害薬としてのヘテロ環式カルボン酸アミド Download PDFInfo
- Publication number
- JP5860031B2 JP5860031B2 JP2013505483A JP2013505483A JP5860031B2 JP 5860031 B2 JP5860031 B2 JP 5860031B2 JP 2013505483 A JP2013505483 A JP 2013505483A JP 2013505483 A JP2013505483 A JP 2013505483A JP 5860031 B2 JP5860031 B2 JP 5860031B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkylene
- mmol
- independently
- hydrogen
- 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.)
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Links
- 0 CC(C)*(C=*C=C1C(C)C)C1=O Chemical compound CC(C)*(C=*C=C1C(C)C)C1=O 0.000 description 9
- PCQIXXZSEBJRDI-UHFFFAOYSA-N C#CCNC(C1=CN=CN(Cc(cc2F)ccc2F)C1=O)=O Chemical compound C#CCNC(C1=CN=CN(Cc(cc2F)ccc2F)C1=O)=O PCQIXXZSEBJRDI-UHFFFAOYSA-N 0.000 description 1
- BUZZIOYVTKBDSO-UHFFFAOYSA-N CC(C)(C)OC(NCCBOC(C)(C)C(C)(C)O)=O Chemical compound CC(C)(C)OC(NCCBOC(C)(C)C(C)(C)O)=O BUZZIOYVTKBDSO-UHFFFAOYSA-N 0.000 description 1
- QNMJLYNNPQMCGB-UHFFFAOYSA-N CC(C)C(CC1)C=C1C(C)C Chemical compound CC(C)C(CC1)C=C1C(C)C QNMJLYNNPQMCGB-UHFFFAOYSA-N 0.000 description 1
- KJZNHDOCJJUHRD-UHFFFAOYSA-N CC(C)Nc1cnc(ccc(C#CCNC(C2=CN=CN(Cc(cc3)cc(F)c3F)C2=O)=O)c2)c2n1 Chemical compound CC(C)Nc1cnc(ccc(C#CCNC(C2=CN=CN(Cc(cc3)cc(F)c3F)C2=O)=O)c2)c2n1 KJZNHDOCJJUHRD-UHFFFAOYSA-N 0.000 description 1
- YZSZJUYQOVCVLE-RITPCOANSA-N CC(C)[C@@H]([C@@H](C)F)F Chemical compound CC(C)[C@@H]([C@@H](C)F)F YZSZJUYQOVCVLE-RITPCOANSA-N 0.000 description 1
- KVDVZFUAJXOTTK-UHFFFAOYSA-N CCN(CC1)CCC1Nc1cnc(ccc(C#CCNC(C2=CN=CN(Cc(cc3F)ccc3F)C2=O)=O)c2)c2n1 Chemical compound CCN(CC1)CCC1Nc1cnc(ccc(C#CCNC(C2=CN=CN(Cc(cc3F)ccc3F)C2=O)=O)c2)c2n1 KVDVZFUAJXOTTK-UHFFFAOYSA-N 0.000 description 1
- MFBWHMJOEBEUCQ-UHFFFAOYSA-N CN(C)CCCOc1ncnc(cc2)c1cc2C#CCNC(C1=CN=CN(Cc(cc2F)ccc2F)C1=O)=O Chemical compound CN(C)CCCOc1ncnc(cc2)c1cc2C#CCNC(C1=CN=CN(Cc(cc2F)ccc2F)C1=O)=O MFBWHMJOEBEUCQ-UHFFFAOYSA-N 0.000 description 1
- WQUGFFLYMGIGOZ-UHFFFAOYSA-N CN(C)CCCOc1ncnc(cc2)c1cc2I Chemical compound CN(C)CCCOc1ncnc(cc2)c1cc2I WQUGFFLYMGIGOZ-UHFFFAOYSA-N 0.000 description 1
- YUCJYTFPJFQSPI-UHFFFAOYSA-N CN(CCC1)CC1Nc1cnc(ccc(C#CCNC(C2=CN=CN(Cc(cc3)cc(F)c3F)C2=O)=O)c2)c2n1 Chemical compound CN(CCC1)CC1Nc1cnc(ccc(C#CCNC(C2=CN=CN(Cc(cc3)cc(F)c3F)C2=O)=O)c2)c2n1 YUCJYTFPJFQSPI-UHFFFAOYSA-N 0.000 description 1
- WZSZGPMHUOIAHO-UHFFFAOYSA-N CNc1ncnc(cc2F)c1cc2Br Chemical compound CNc1ncnc(cc2F)c1cc2Br WZSZGPMHUOIAHO-UHFFFAOYSA-N 0.000 description 1
- QANMRDJSEHKTQZ-UHFFFAOYSA-N Fc(c(Br)c1)cc2c1c(Cl)ncn2 Chemical compound Fc(c(Br)c1)cc2c1c(Cl)ncn2 QANMRDJSEHKTQZ-UHFFFAOYSA-N 0.000 description 1
- QKQAXRDHBACXNP-MEMLXQNLSA-N N[C@H](CC1)CC[C@@H]1Nc1cnc(ccc(C#CCNC(C2=CN=CN(Cc(cc3)cc(F)c3F)C2=O)=O)c2)c2n1 Chemical compound N[C@H](CC1)CC[C@@H]1Nc1cnc(ccc(C#CCNC(C2=CN=CN(Cc(cc3)cc(F)c3F)C2=O)=O)c2)c2n1 QKQAXRDHBACXNP-MEMLXQNLSA-N 0.000 description 1
- QKQAXRDHBACXNP-OYRHEFFESA-N N[C@H](CC1)CC[C@H]1Nc1cnc(ccc(C#CCNC(C2=CN=CN(Cc(cc3)cc(F)c3F)C2=O)=O)c2)c2n1 Chemical compound N[C@H](CC1)CC[C@H]1Nc1cnc(ccc(C#CCNC(C2=CN=CN(Cc(cc3)cc(F)c3F)C2=O)=O)c2)c2n1 QKQAXRDHBACXNP-OYRHEFFESA-N 0.000 description 1
- RPHQHEBXMAGQKB-UHFFFAOYSA-N Nc(cc(c(Br)c1)F)c1C(O)=O Chemical compound Nc(cc(c(Br)c1)F)c1C(O)=O RPHQHEBXMAGQKB-UHFFFAOYSA-N 0.000 description 1
- YJIKLVKCLNJNBK-UHFFFAOYSA-N O=C(C1=CN=CN(Cc(cc2)cc(F)c2F)C1=O)NCC#Cc1cc2nc(NC(CC3)CCN3C3CC3)cnc2cc1 Chemical compound O=C(C1=CN=CN(Cc(cc2)cc(F)c2F)C1=O)NCC#Cc1cc2nc(NC(CC3)CCN3C3CC3)cnc2cc1 YJIKLVKCLNJNBK-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- 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
- A61P31/04—Antibacterial agents
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
- C07D403/02—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
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10160552.5 | 2010-04-21 | ||
| EP10160552 | 2010-04-21 | ||
| PCT/EP2011/056368 WO2011131741A1 (en) | 2010-04-21 | 2011-04-20 | Heterocyclic carboxylic acid amides as pdk1 inihibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013525333A JP2013525333A (ja) | 2013-06-20 |
| JP2013525333A5 JP2013525333A5 (enExample) | 2014-06-19 |
| JP5860031B2 true JP5860031B2 (ja) | 2016-02-16 |
Family
ID=42306748
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013505483A Active JP5860031B2 (ja) | 2010-04-21 | 2011-04-20 | Ｐｄｋ１阻害薬としてのヘテロ環式カルボン酸アミド |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8575203B2 (enExample) |
| EP (1) | EP2560967B1 (enExample) |
| JP (1) | JP5860031B2 (enExample) |
| TW (1) | TW201204362A (enExample) |
| UY (1) | UY33349A (enExample) |
| WO (1) | WO2011131741A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011144622A1 (en) * | 2010-05-17 | 2011-11-24 | Boehringer Ingelheim International Gmbh | 1h - imidazo [4, 5 - c] quinolines |
| EP2780013A4 (en) * | 2011-11-18 | 2015-07-01 | Constellation Pharmaceuticals Inc | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF |
| US9206128B2 (en) * | 2011-11-18 | 2015-12-08 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| JP5989805B2 (ja) | 2012-02-10 | 2016-09-07 | コンステレーション・ファーマシューティカルズ・インコーポレイテッドＣｏｎｓｔｅｌｌａｔｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | メチル基変更酵素の調節物質、組成物及びその使用 |
| EP2825533B1 (en) | 2012-03-13 | 2016-10-19 | Basf Se | Fungicidal pyrimidine compounds |
| CN102775358B (zh) * | 2012-08-22 | 2015-05-27 | 山东齐都药业有限公司 | 6-氟-3-羟基-2-吡嗪酰胺的制备方法 |
| EP2903978B1 (en) | 2012-10-05 | 2022-12-07 | Rigel Pharmaceuticals, Inc. | Gdf-8 inhibitors |
| US9745305B2 (en) | 2013-03-15 | 2017-08-29 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| US9969716B2 (en) | 2013-08-15 | 2018-05-15 | Constellation Pharmaceuticals, Inc. | Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof |
| EP3046915A1 (en) | 2013-09-16 | 2016-07-27 | Basf Se | Fungicidal pyrimidine compounds |
| WO2015036059A1 (en) | 2013-09-16 | 2015-03-19 | Basf Se | Fungicidal pyrimidine compounds |
| JP6800158B2 (ja) | 2015-02-20 | 2020-12-16 | ライジェル ファーマシューティカルズ， インコーポレイテッド | Ｇｄｆ−８阻害剤 |
| WO2017040190A1 (en) | 2015-08-28 | 2017-03-09 | Constellation Pharmaceuticals, Inc. | Crystalline forms of (r)-n-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1h-indole-3-carboxamide |
| MX2018004109A (es) | 2015-10-05 | 2018-09-27 | Univ Columbia | Activadores de flujo autofágico y fosfolipasa d y depuración de acumulaciones de proteína que incluyen tau y tratamiento de proteinopatías. |
| US10457640B2 (en) | 2016-10-19 | 2019-10-29 | Constellation Pharmaceuticals, Inc. | Synthesis of inhibitors of EZH2 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2632639B1 (fr) | 1988-06-09 | 1990-10-05 | Sanofi Sa | Derives d'amino-4 carboxy-3 naphtyridines, leur preparation et compositions pharmaceutiques qui les contiennent |
| KR100735639B1 (ko) | 2004-12-29 | 2007-07-04 | 한미약품 주식회사 | 암세포 성장 억제 효과를 갖는 퀴나졸린 유도체 및 이의제조방법 |
| US20090264415A2 (en) | 2004-12-30 | 2009-10-22 | Steven De Jonghe | Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment |
| CA2612788A1 (en) | 2005-06-24 | 2006-12-28 | Steven Cesar Alfons De Jonghe | Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for treating hepatitis c |
| DE102006012251A1 (de) | 2006-03-15 | 2007-11-08 | Grünenthal GmbH | Substituierte 4-Amino-chinazolin-Derivate und ihre Verwendung zur Herstellung von Arzneimitteln |
| US20120088746A1 (en) | 2006-05-10 | 2012-04-12 | Pfizer Inc. | Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same |
| US8778977B2 (en) | 2006-06-30 | 2014-07-15 | Sunesis Pharmaceuticals, Inc. | Pyridinonyl PDK1 inhibitors |
| WO2008020302A2 (en) | 2006-08-17 | 2008-02-21 | Pfizer Products Inc. | Heteroaromatic quinoline-based compounds as phosphodiesterase (pde) inhibitors |
| EP1990342A1 (en) | 2007-05-10 | 2008-11-12 | AEterna Zentaris GmbH | Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof |
| UY31982A (es) * | 2008-07-16 | 2010-02-26 | Boehringer Ingelheim Int | Derivados de 1,2-dihidropiridin-3-carboxamidas n-sustituidas |
| UY31984A (es) | 2008-07-16 | 2010-02-26 | Boehringer Ingelheim Int | DERIVADOS DE 1-(3,4-difluorobencil)-6-oxo-1,6-dihidropirimidin-5-carboxamidas N-sustituidas y de 2-(3,4-difluorobencil)-3-oxo-2,3-dihidro-1H-pirazol-4-carboxamidas N-sustituidas. |
-
2011
- 2011-04-19 US US13/089,614 patent/US8575203B2/en active Active
- 2011-04-20 EP EP11716881.5A patent/EP2560967B1/en active Active
- 2011-04-20 JP JP2013505483A patent/JP5860031B2/ja active Active
- 2011-04-20 WO PCT/EP2011/056368 patent/WO2011131741A1/en not_active Ceased
- 2011-04-20 TW TW100113756A patent/TW201204362A/zh unknown
- 2011-04-25 UY UY0001033349A patent/UY33349A/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| TW201204362A (en) | 2012-02-01 |
| US20120094976A1 (en) | 2012-04-19 |
| EP2560967A1 (en) | 2013-02-27 |
| UY33349A (es) | 2011-12-01 |
| WO2011131741A1 (en) | 2011-10-27 |
| EP2560967B1 (en) | 2017-12-20 |
| US8575203B2 (en) | 2013-11-05 |
| JP2013525333A (ja) | 2013-06-20 |
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