TN2012000370A1 - 5-alkynyl pyrimidines and their use as kinase inhibitors - Google Patents
5-alkynyl pyrimidines and their use as kinase inhibitorsInfo
- Publication number
- TN2012000370A1 TN2012000370A1 TNP2012000370A TN2012000370A TN2012000370A1 TN 2012000370 A1 TN2012000370 A1 TN 2012000370A1 TN P2012000370 A TNP2012000370 A TN P2012000370A TN 2012000370 A TN2012000370 A TN 2012000370A TN 2012000370 A1 TN2012000370 A1 TN 2012000370A1
- Authority
- TN
- Tunisia
- Prior art keywords
- kinase inhibitors
- pyrimidines
- alkynyl
- alkynyl pyrimidines
- medicament
- Prior art date
Links
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 230000004663 cell proliferation Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon 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
- C07D401/14—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
- 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
- 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
- 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
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10151722 | 2010-01-26 | ||
| PCT/EP2011/051060 WO2011092197A1 (en) | 2010-01-26 | 2011-01-26 | 5-alkynyl pyrimidines and their use as kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TN2012000370A1 true TN2012000370A1 (en) | 2014-01-30 |
Family
ID=42140100
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TNP2012000370A TN2012000370A1 (en) | 2010-01-26 | 2012-07-23 | 5-alkynyl pyrimidines and their use as kinase inhibitors |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US8618111B2 (enExample) |
| EP (1) | EP2528910B1 (enExample) |
| JP (1) | JP5670479B2 (enExample) |
| KR (1) | KR20130030742A (enExample) |
| CN (1) | CN102781931A (enExample) |
| AP (1) | AP2012006361A0 (enExample) |
| AR (1) | AR080019A1 (enExample) |
| AU (1) | AU2011209343A1 (enExample) |
| BR (1) | BR112012018454A2 (enExample) |
| CA (1) | CA2787396A1 (enExample) |
| CL (1) | CL2012001926A1 (enExample) |
| CO (1) | CO6592046A2 (enExample) |
| EA (1) | EA201201049A1 (enExample) |
| EC (1) | ECSP12012110A (enExample) |
| IN (1) | IN2012DN06600A (enExample) |
| MA (1) | MA33938B1 (enExample) |
| MX (1) | MX2012008359A (enExample) |
| PE (1) | PE20121527A1 (enExample) |
| PH (1) | PH12012501521A1 (enExample) |
| SG (1) | SG182676A1 (enExample) |
| TN (1) | TN2012000370A1 (enExample) |
| TW (1) | TW201139412A (enExample) |
| UY (1) | UY33198A (enExample) |
| WO (1) | WO2011092197A1 (enExample) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8633183B2 (en) * | 2010-01-26 | 2014-01-21 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
| US8466162B2 (en) * | 2011-01-26 | 2013-06-18 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyridines |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3832570A1 (de) * | 1988-09-24 | 1990-03-29 | Hoechst Ag | 7-substituierte derivate der 3,5-dihydroxyhept-6-insaeure, verfahren zur ihrer herstellung, ihre verwendung als arzneimittel, sowie zwischenprodukte |
| EP0674627A1 (en) | 1992-12-18 | 1995-10-04 | The Wellcome Foundation Limited | Pyrimidine, pyridine, pteridinone and indazole derivatives as enzyme inhibitors |
| US5622954A (en) | 1994-05-11 | 1997-04-22 | Fmc Corporation | 5[W(substituted aryl)alkenylene and alkynylene]-2,4-diaminopyrimidines as pesticides |
| JP5154728B2 (ja) * | 2000-07-24 | 2013-02-27 | クレニツキー・ファーマシューティカルズ，インコーポレイテッド | 神経栄養活性を有する置換５−アルキニルピリミジン |
| CA2517291C (en) * | 2003-03-19 | 2012-05-08 | Exelixis, Inc. | Ortho-substituted aryl and heteroaryl tie-2 modulators and methods of use |
| JP2007502298A (ja) * | 2003-08-14 | 2007-02-08 | スミスクライン ビーチャム コーポレーション | 化合物 |
| US20080027076A1 (en) | 2003-12-24 | 2008-01-31 | Astrazeneca Ab | Pyrimidines With Tie2 (Tek) Activity |
| US7776869B2 (en) | 2004-10-18 | 2010-08-17 | Amgen Inc. | Heteroaryl-substituted alkyne compounds and method of use |
| WO2006082373A1 (en) | 2005-02-01 | 2006-08-10 | Astrazeneca Ab | Pyrimidine compounds having ties (tek) inhibitory activity |
| WO2006082371A1 (en) | 2005-02-01 | 2006-08-10 | Astrazeneca Ab | Pyrimidine compounds having tie2 (tek) inhibitory activity |
| GB0502418D0 (en) * | 2005-02-05 | 2005-03-16 | Astrazeneca Ab | Compounds |
| US20070135437A1 (en) | 2005-03-04 | 2007-06-14 | Alsgen, Inc. | Modulation of neurodegenerative diseases |
| WO2006106721A1 (ja) * | 2005-03-30 | 2006-10-12 | Shionogi & Co., Ltd. | チロシンキナーゼ阻害作用を有するピリミジン誘導体 |
| EP1893605A2 (en) | 2005-03-31 | 2008-03-05 | AstraZeneca AB | Saminopyrimidine derivates with tie2 inhibiting activity |
| KR20080083188A (ko) * | 2006-01-11 | 2008-09-16 | 아스트라제네카 아베 | 모르폴리노 피리미딘 유도체 및 요법에서의 그 유도체의용도 |
| GB0616747D0 (en) * | 2006-08-24 | 2006-10-04 | Astrazeneca Ab | Novel compounds |
| US20090325957A1 (en) | 2006-08-24 | 2009-12-31 | Astrazeneca Ab | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| US8318736B2 (en) | 2006-12-29 | 2012-11-27 | Janssen R&D Ireland | HIV inhibiting 5,6-substituted pyrimidines |
| EP2022785A1 (en) | 2007-06-20 | 2009-02-11 | Bayer Schering Pharma Aktiengesellschaft | Alkynylpyrimidines as Tie2 kinase inhibitors |
| WO2010012740A1 (en) * | 2008-07-29 | 2010-02-04 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
| JP2010018601A (ja) * | 2009-02-16 | 2010-01-28 | Tetsuya Nishio | 複素環化合物、その製造法および用途 |
| US8633183B2 (en) * | 2010-01-26 | 2014-01-21 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
-
2011
- 2011-01-24 US US13/012,081 patent/US8618111B2/en active Active
- 2011-01-24 UY UY0001033198A patent/UY33198A/es not_active Application Discontinuation
- 2011-01-25 AR ARP110100240A patent/AR080019A1/es unknown
- 2011-01-25 TW TW100102687A patent/TW201139412A/zh unknown
- 2011-01-26 CN CN2011800114539A patent/CN102781931A/zh active Pending
- 2011-01-26 BR BR112012018454A patent/BR112012018454A2/pt not_active Application Discontinuation
- 2011-01-26 JP JP2012550423A patent/JP5670479B2/ja active Active
- 2011-01-26 EP EP11701988.5A patent/EP2528910B1/en active Active
- 2011-01-26 PE PE2012001051A patent/PE20121527A1/es not_active Application Discontinuation
- 2011-01-26 SG SG2012054375A patent/SG182676A1/en unknown
- 2011-01-26 CA CA2787396A patent/CA2787396A1/en not_active Abandoned
- 2011-01-26 MX MX2012008359A patent/MX2012008359A/es not_active Application Discontinuation
- 2011-01-26 KR KR1020127022284A patent/KR20130030742A/ko not_active Withdrawn
- 2011-01-26 IN IN6600DEN2012 patent/IN2012DN06600A/en unknown
- 2011-01-26 EA EA201201049A patent/EA201201049A1/ru unknown
- 2011-01-26 AU AU2011209343A patent/AU2011209343A1/en not_active Abandoned
- 2011-01-26 AP AP2012006361A patent/AP2012006361A0/xx unknown
- 2011-01-26 WO PCT/EP2011/051060 patent/WO2011092197A1/en not_active Ceased
- 2011-01-26 PH PH1/2012/501521A patent/PH12012501521A1/en unknown
-
2012
- 2012-07-10 CL CL2012001926A patent/CL2012001926A1/es unknown
- 2012-07-18 MA MA35082A patent/MA33938B1/fr unknown
- 2012-07-23 TN TNP2012000370A patent/TN2012000370A1/en unknown
- 2012-07-27 CO CO12126469A patent/CO6592046A2/es not_active Application Discontinuation
- 2012-08-20 EC ECSP12012110 patent/ECSP12012110A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2011209343A1 (en) | 2012-08-02 |
| AR080019A1 (es) | 2012-03-07 |
| EA201201049A1 (ru) | 2013-02-28 |
| BR112012018454A2 (pt) | 2016-04-19 |
| CA2787396A1 (en) | 2011-08-04 |
| MA33938B1 (fr) | 2013-01-02 |
| EP2528910A1 (en) | 2012-12-05 |
| ECSP12012110A (es) | 2012-09-28 |
| KR20130030742A (ko) | 2013-03-27 |
| SG182676A1 (en) | 2012-08-30 |
| JP2013518078A (ja) | 2013-05-20 |
| CN102781931A (zh) | 2012-11-14 |
| US8618111B2 (en) | 2013-12-31 |
| EP2528910B1 (en) | 2015-03-18 |
| MX2012008359A (es) | 2012-08-08 |
| AP2012006361A0 (en) | 2012-08-31 |
| US20120028958A1 (en) | 2012-02-02 |
| CL2012001926A1 (es) | 2012-11-30 |
| CO6592046A2 (es) | 2013-01-02 |
| TW201139412A (en) | 2011-11-16 |
| IN2012DN06600A (enExample) | 2015-10-23 |
| PE20121527A1 (es) | 2012-11-21 |
| WO2011092197A1 (en) | 2011-08-04 |
| UY33198A (es) | 2011-08-31 |
| JP5670479B2 (ja) | 2015-02-18 |
| PH12012501521A1 (en) | 2012-10-22 |
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