CN101389622B - 用作pi-3激酶抑制剂的嘧啶衍生物 - Google Patents
用作pi-3激酶抑制剂的嘧啶衍生物 Download PDFInfo
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- CN101389622B CN101389622B CN2007800063742A CN200780006374A CN101389622B CN 101389622 B CN101389622 B CN 101389622B CN 2007800063742 A CN2007800063742 A CN 2007800063742A CN 200780006374 A CN200780006374 A CN 200780006374A CN 101389622 B CN101389622 B CN 101389622B
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- Prior art keywords
- pyrimidine
- compound
- amine
- unsubstituted
- amino
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- ILLRAZLNZVSGBY-UHFFFAOYSA-N Nc(nc1)cc(C(F)(F)F)c1-c1nc(N2CCOCC2)nc(Cl)c1 Chemical compound Nc(nc1)cc(C(F)(F)F)c1-c1nc(N2CCOCC2)nc(Cl)c1 ILLRAZLNZVSGBY-UHFFFAOYSA-N 0.000 description 1
- KJCYBNURWMAKHV-LLVKDONJSA-N Nc(nc1)cc(C(F)(F)F)c1-c1nc(N2CCOCC2)nc(O[C@H]2CNCC2)c1 Chemical compound Nc(nc1)cc(C(F)(F)F)c1-c1nc(N2CCOCC2)nc(O[C@H]2CNCC2)c1 KJCYBNURWMAKHV-LLVKDONJSA-N 0.000 description 1
- WCCFLOQQACDOAX-UHFFFAOYSA-N Nc1nccc(F)c1 Chemical compound Nc1nccc(F)c1 WCCFLOQQACDOAX-UHFFFAOYSA-N 0.000 description 1
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- DWGNYHYXTUHLFJ-UHFFFAOYSA-N Oc1nc(N2CCOCC2)nc(O)c1F Chemical compound Oc1nc(N2CCOCC2)nc(O)c1F DWGNYHYXTUHLFJ-UHFFFAOYSA-N 0.000 description 1
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Images
Classifications
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- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- 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
- C07D405/12—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 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
- C07D405/14—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
- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US76078906P | 2006-01-20 | 2006-01-20 | |
| US60/760,789 | 2006-01-20 | ||
| PCT/US2007/001708 WO2007084786A1 (en) | 2006-01-20 | 2007-01-22 | Pyrimidine derivatives used as pi-3 kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101389622A CN101389622A (zh) | 2009-03-18 |
| CN101389622B true CN101389622B (zh) | 2013-04-17 |
Family
ID=37951939
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2007800063742A Active CN101389622B (zh) | 2006-01-20 | 2007-01-22 | 用作pi-3激酶抑制剂的嘧啶衍生物 |
Country Status (40)
Families Citing this family (366)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| TW200808739A (en) | 2006-04-06 | 2008-02-16 | Novartis Vaccines & Diagnostic | Quinazolines for PDK1 inhibition |
| JP5534811B2 (ja) | 2006-08-24 | 2014-07-02 | アストラゼネカ アクチボラグ | 増殖性疾患の治療に有用なモルホリノピリミジン誘導体 |
| WO2008070740A1 (en) | 2006-12-07 | 2008-06-12 | F.Hoffmann-La Roche Ag | Phosphoinositide 3-kinase inhibitor compounds and methods of use |
| AU2008213808B2 (en) * | 2007-02-06 | 2011-11-10 | Novartis Ag | PI 3-kinase inhibitors and methods of their use |
| WO2008128984A1 (en) * | 2007-04-20 | 2008-10-30 | Probiodrug Ag | Aminopyrimidine derivatives as glutaminyl cyclase inhibitors |
| WO2008145681A2 (en) | 2007-05-31 | 2008-12-04 | Boehringer Ingelheim International Gmbh | Ccr2 receptor antagonists and uses thereof |
| US8138183B2 (en) | 2007-07-09 | 2012-03-20 | Astrazeneca Ab | Morpholino pyrimidine derivatives used in diseases linked to mTOR kinase and/or PI3K |
| WO2009017838A2 (en) * | 2007-08-01 | 2009-02-05 | Exelixis, Inc. | Combinations of jak-2 inhibitors and other agents |
| JP2011500823A (ja) * | 2007-10-22 | 2011-01-06 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Pi3キナーゼ阻害物質としてのピリドスルホンアミド誘導体 |
| WO2009066084A1 (en) * | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
| WO2009093981A1 (en) * | 2008-01-23 | 2009-07-30 | S Bio Pte Ltd | Triazine compounds as kinase inhibitors |
| US20110033453A1 (en) | 2008-03-05 | 2011-02-10 | Carlos Garcia-Echeverria | Use of pyrimidine derivatives for the treatment of egfr dependent diseases or diseases that have acquired resistance to agents that target egfr family members |
| AU2012203914C1 (en) * | 2008-03-26 | 2013-11-28 | Novartis Ag | 5imidazoquinolines and pyrimidine derivatives as potent modulators of VEGF-driven angiogenic processes |
| EP2474323A3 (en) | 2008-03-26 | 2012-10-10 | Novartis AG | Imidazoquinolines and pyrimidine derivatives as potent modulators of vegf-driven angiogenic processes |
| JP2011515462A (ja) * | 2008-03-27 | 2011-05-19 | アウククランド ウニセルビセス リミテッド | 置換されたピリミジン、及びトリアジン、並びに癌療法におけるこれらの使用 |
| EP2300013B2 (en) | 2008-05-21 | 2024-11-13 | Takeda Pharmaceutical Company Limited | Phosphorous derivatives as kinase inhibitors |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| US20110105500A1 (en) * | 2008-06-27 | 2011-05-05 | S*Bio Pte Ltd. | Pyrazine substituted purines |
| CA2729914A1 (en) * | 2008-07-11 | 2010-01-14 | Novartis Ag | Combination of (a) a phosphoinositide 3-kinase inhibitor and (b) a modulator of ras/raf/mek pathway |
| CA2731909A1 (en) * | 2008-07-29 | 2010-02-04 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
| US20100068204A1 (en) * | 2008-09-12 | 2010-03-18 | Wyeth | 4-aryloxyquinolin-2(1h)-ones as mtor kinase and pi3 kinase inhibitors, for use as anti-cancer agents |
| WO2010037715A1 (en) * | 2008-10-01 | 2010-04-08 | Novartis Ag | Smoothened antagonism for the treatment of hedgehog pathway-related disorders |
| TWI378933B (en) | 2008-10-14 | 2012-12-11 | Daiichi Sankyo Co Ltd | Morpholinopurine derivatives |
| RU2538683C2 (ru) * | 2008-10-31 | 2015-01-10 | Новартис Аг | КОМБИНАЦИЯ ИНГИБИТОРА ФОСФАТИДИЛИНОЗИТОЛ-3-КИНАЗЫ (Р13К) И ИНГИБИТОРА mTOR |
| CA2744154A1 (en) * | 2008-11-20 | 2010-05-27 | Genentech, Inc. | Pyrazolopyridine pi3k inhibitor compounds and methods of use |
| DK2379525T3 (en) | 2008-12-19 | 2015-10-19 | Boehringer Ingelheim Int | Cyclic pyrimidin-4-carboxamides, as CCR2 receptor antagonists for the treatment of inflammation, asthma and COPD |
| BRPI1006113A2 (pt) | 2009-03-05 | 2016-02-16 | Daiichi Sankyo Co Ltd | "derivado de piridina". |
| AU2010229468A1 (en) | 2009-03-27 | 2011-10-13 | Vetdc, Inc. | Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy |
| JP2012523429A (ja) * | 2009-04-09 | 2012-10-04 | オンコシレオン,インコーポレイテッド | 線維症を処置するための方法およびpi−3キナーゼインヒビターの組成物 |
| UY32582A (es) | 2009-04-28 | 2010-11-30 | Amgen Inc | Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero |
| MX2011012201A (es) * | 2009-05-15 | 2011-12-08 | Novartis Ag | Combinacion de un inhibidor de cinasa de fosfoinositida-3 y un compuesto anti-diabetico. |
| SG175708A1 (en) * | 2009-05-27 | 2011-12-29 | Genentech Inc | Bicyclic pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use |
| US8486939B2 (en) | 2009-07-07 | 2013-07-16 | Pathway Therapeutics Inc. | Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy |
| US20120065166A1 (en) * | 2009-08-12 | 2012-03-15 | Virginia Espina | Bone Modulators And Methods Therewith |
| CN101993416B (zh) * | 2009-08-27 | 2013-09-11 | 中国科学院上海药物研究所 | 喹啉类化合物、其制备方法、包含该化合物的药物组合物及该化合物的用途 |
| RU2595718C2 (ru) * | 2009-09-09 | 2016-08-27 | Селджен Авиломикс Рисерч,Инк. | Ингибиторы pi3-киназы и их применение |
| WO2011047323A2 (en) * | 2009-10-16 | 2011-04-21 | Rib-X Pharmaceuticals, Inc. | Antimicrobial compounds and methods of making and using the same |
| BR112012008759A2 (pt) | 2009-10-16 | 2020-08-25 | Rib-X Pharmaceuticals, Inc. | compostos antimicrobianos e métodos de fabricação e uso dos mesmos |
| WO2011073154A1 (en) | 2009-12-17 | 2011-06-23 | Boehringer Ingelheim International Gmbh | New ccr2 receptor antagonists and uses thereof |
| GB201004200D0 (en) | 2010-03-15 | 2010-04-28 | Univ Basel | Spirocyclic compounds and their use as therapeutic agents and diagnostic probes |
| US8877745B2 (en) | 2010-05-12 | 2014-11-04 | Boehringer Ingelheim International Gmbh | CCR2 receptor antagonists, method for producing the same, and use thereof as medicaments |
| EP2569295B1 (en) | 2010-05-12 | 2014-11-19 | Boehringer Ingelheim International GmbH | New ccr2 receptor antagonists, method for producing the same, and use thereof as medicaments |
| US8841313B2 (en) | 2010-05-17 | 2014-09-23 | Boehringer Ingelheim International Gmbh | CCR2 antagonists and uses thereof |
| US9018212B2 (en) | 2010-05-25 | 2015-04-28 | Boehringer Ingelheim International Gmbh | Pyridazine carboxamides as CCR2 receptor antagonists |
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|---|---|---|---|---|
| WO2004048365A1 (en) * | 2002-11-21 | 2004-06-10 | Chiron Corporation | 2,4,6-trisubstituted pyrimidines as phosphotidylinositol (pi) 3-kinase inhibitors and their use in the treatment of cancer |
| WO2005028444A1 (en) * | 2003-09-24 | 2005-03-31 | Novartis Ag | 1,4-disubstituted isoquinilone derivatives as raf-kinase inhibitors useful for the treatment of proliferative diseases |
| WO2006005914A1 (en) * | 2004-07-09 | 2006-01-19 | Astrazeneca Ab | 2, 4, 6-trisubstituted pyrimidines as phosphotidylinositol (pi) 3-kinase inhibitors and their use in the treatment of cancer |
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