JP2008510771A5 - - Google Patents
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- JP2008510771A5 JP2008510771A5 JP2007528834A JP2007528834A JP2008510771A5 JP 2008510771 A5 JP2008510771 A5 JP 2008510771A5 JP 2007528834 A JP2007528834 A JP 2007528834A JP 2007528834 A JP2007528834 A JP 2007528834A JP 2008510771 A5 JP2008510771 A5 JP 2008510771A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- hydrogen
- halogen
- alkyl
- pseudohalogen
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 125000002577 pseudohalo group Chemical group 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- -1 C 2-12 -alkynyl Chemical group 0.000 claims 5
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000035143 Bacterial infection Diseases 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 101000582926 Dictyostelium discoideum Probable serine/threonine-protein kinase PLK Proteins 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 206010028116 Mucosal inflammation Diseases 0.000 claims 2
- 201000010927 Mucositis Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 230000001580 bacterial effect Effects 0.000 claims 2
- 208000022362 bacterial infectious disease Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 201000004384 Alopecia Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 102100031463 Serine/threonine-protein kinase PLK1 Human genes 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000003302 alkenyloxy group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000004419 alkynylene group Chemical group 0.000 claims 1
- 125000005133 alkynyloxy group Chemical group 0.000 claims 1
- 231100000360 alopecia Toxicity 0.000 claims 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 1
- 230000001028 anti-proliverative effect Effects 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 125000000480 butynyl group Chemical group [*]C#CC([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 208000022605 chemotherapy-induced alopecia Diseases 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000001613 neoplastic effect Effects 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 230000002018 overexpression Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 108010056274 polo-like kinase 1 Proteins 0.000 claims 1
- 125000002568 propynyl group Chemical group [*]C#CC([H])([H])[H] 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04020339 | 2004-08-27 | ||
| PCT/EP2005/054099 WO2006021548A1 (de) | 2004-08-27 | 2005-08-19 | Dihydropteridinone, verfahren zu deren herstellung und deren verwendung als arzneimittel |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008510771A JP2008510771A (ja) | 2008-04-10 |
| JP2008510771A5 true JP2008510771A5 (enExample) | 2008-10-09 |
Family
ID=34926318
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007528834A Pending JP2008510771A (ja) | 2004-08-27 | 2005-08-19 | ジヒドロプテリジノン、その製造方法および医薬薬剤としてのその使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US7371753B2 (enExample) |
| EP (1) | EP1784406A1 (enExample) |
| JP (1) | JP2008510771A (enExample) |
| CA (1) | CA2578560A1 (enExample) |
| WO (1) | WO2006021548A1 (enExample) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6861422B2 (en) * | 2003-02-26 | 2005-03-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions |
| DE102004029784A1 (de) * | 2004-06-21 | 2006-01-05 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel |
| DE102004033670A1 (de) | 2004-07-09 | 2006-02-02 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Pyridodihydropyrazinone, Verfahren zu Ihrer Herstellung und Ihre Verwendung als Arzneimittel |
| US20060035903A1 (en) * | 2004-08-14 | 2006-02-16 | Boehringer Ingelheim International Gmbh | Storage stable perfusion solution for dihydropteridinones |
| US7728134B2 (en) * | 2004-08-14 | 2010-06-01 | Boehringer Ingelheim International Gmbh | Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament |
| US20060074088A1 (en) * | 2004-08-14 | 2006-04-06 | Boehringer Ingelheim International Gmbh | Dihydropteridinones for the treatment of cancer diseases |
| US7759485B2 (en) * | 2004-08-14 | 2010-07-20 | Boehringer Ingelheim International Gmbh | Process for the manufacture of dihydropteridinones |
| US20060058311A1 (en) | 2004-08-14 | 2006-03-16 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation |
| EP1630163A1 (de) * | 2004-08-25 | 2006-03-01 | Boehringer Ingelheim Pharma GmbH & Co.KG | Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
| EP1632493A1 (de) * | 2004-08-25 | 2006-03-08 | Boehringer Ingelheim Pharma GmbH & Co.KG | Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
| DE102004058337A1 (de) * | 2004-12-02 | 2006-06-14 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung von annelierten Piperazin-2-on Derivaten |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| GB0525957D0 (en) | 2005-12-21 | 2006-02-01 | Astrazeneca Ab | Methods |
| US7439358B2 (en) * | 2006-02-08 | 2008-10-21 | Boehringer Ingelheim International Gmbh | Specific salt, anhydrous and crystalline form of a dihydropteridione derivative |
| TW200808325A (en) * | 2006-07-06 | 2008-02-16 | Astrazeneca Ab | Novel compounds |
| EP2223925A1 (en) * | 2006-10-09 | 2010-09-01 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| JP2010505962A (ja) | 2006-10-09 | 2010-02-25 | 武田薬品工業株式会社 | キナーゼ阻害剤 |
| ES2627352T3 (es) * | 2006-10-19 | 2017-07-27 | Signal Pharmaceuticals, Llc | Compuestos heteroarilo, sus composiciones y su uso como inhibidores de proteínas quinasas |
| GB0621203D0 (en) * | 2006-10-25 | 2006-12-06 | Chroma Therapeutics Ltd | PLK inhibitors |
| BRPI0718120A2 (pt) * | 2006-10-25 | 2013-11-12 | Chroma Therapeutics Ltd | Derivados de pteridina como inibidores de cinase do tipo pólo úteis no tratamento de câncer |
| WO2008144222A2 (en) * | 2007-05-16 | 2008-11-27 | Eli Lilly And Company | Triazolyl aminopyrimidine compounds |
| EP2185559A1 (en) * | 2007-08-03 | 2010-05-19 | Boehringer Ingelheim International GmbH | Crystalline form of a dihydropteridione derivative |
| BRPI0817315A2 (pt) * | 2007-09-25 | 2015-03-17 | Takeda Pharmaceutical | Inibidores de quinase do tipo polo |
| WO2009067547A1 (en) * | 2007-11-19 | 2009-05-28 | Takeda Pharmaceutical Company Limited | Polo-like kinase inhibitors |
| EP2215091B1 (en) * | 2007-12-04 | 2016-03-30 | Nerviano Medical Sciences S.r.l. | Substituted dihydropteridin-6-one derivatives, process for their preparation and their use as kinase inhibitors |
| EP2100894A1 (en) | 2008-03-12 | 2009-09-16 | 4Sc Ag | Pyridopyrimidines used as Plk1 (polo-like kinase) inhibitors |
| EP2112152A1 (en) | 2008-04-22 | 2009-10-28 | GPC Biotech AG | Dihydropteridinones as Plk Inhibitors |
| GB0807451D0 (en) * | 2008-04-24 | 2008-05-28 | Chroma Therapeutics Ltd | Inhibitors of PLK |
| WO2010025073A1 (en) * | 2008-08-28 | 2010-03-04 | Takeda Pharmaceutical Company Limited | Dihydroimidazo [ 1, 5-f] pteridines as polo-like kinase inhibitors |
| EP2325185A1 (en) | 2009-10-28 | 2011-05-25 | GPC Biotech AG | Plk inhibitor |
| US8546566B2 (en) | 2010-10-12 | 2013-10-01 | Boehringer Ingelheim International Gmbh | Process for manufacturing dihydropteridinones and intermediates thereof |
| US9358233B2 (en) | 2010-11-29 | 2016-06-07 | Boehringer Ingelheim International Gmbh | Method for treating acute myeloid leukemia |
| US8546443B2 (en) | 2010-12-21 | 2013-10-01 | Boehringer Ingelheim International Gmbh | Benzylic oxindole pyrimidines |
| JP5931933B2 (ja) | 2011-02-25 | 2016-06-08 | 武田薬品工業株式会社 | Ｎ−置換オキサジノプテリジンおよびオキサジノプテリジノン |
| US9370535B2 (en) | 2011-05-17 | 2016-06-21 | Boehringer Ingelheim International Gmbh | Method for treatment of advanced solid tumors |
| US8865716B2 (en) | 2012-02-23 | 2014-10-21 | Boehringer Ingelheim International Gmbh | Dihydropteridinones II |
| US9006226B2 (en) | 2012-02-23 | 2015-04-14 | Boehringer Ingelheim International Gmbh | Dihydropteridinones I |
| UY34893A (es) | 2012-07-10 | 2014-02-28 | Takeda Pharmaceutical | Derivados de azaindol |
| EP2958919B1 (en) * | 2013-02-21 | 2019-05-22 | Boehringer Ingelheim International GmbH | Dihydropteridinones i |
| JP6072308B2 (ja) * | 2013-02-21 | 2017-02-01 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ジヒドロプテリジノンｉｉ |
| WO2015011084A1 (de) * | 2013-07-23 | 2015-01-29 | Bayer Pharma Aktiengesellschaft | Substituierte dihydropyrido[3,4-b]pyrazinone als duale inhibitoren von bet-proteinen und polo-like kinasen |
| BR112016001457A2 (pt) | 2013-07-25 | 2017-08-29 | Dana Farber Cancer Inst Inc | Inibidores de fatores de transcrição e usos dos mesmos |
| JP2016525532A (ja) | 2013-07-26 | 2016-08-25 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 骨髄異形成症候群の処置 |
| US9371321B2 (en) | 2014-01-09 | 2016-06-21 | Astrazeneca Ab | Azaindole derivatives |
| MX2016009974A (es) | 2014-01-31 | 2016-10-31 | Dana Farber Cancer Inst Inc | Derivados de diaminopirimidina bencensulfona y sus usos. |
| EP3099693A4 (en) | 2014-01-31 | 2017-08-16 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
| KR20160111520A (ko) * | 2014-01-31 | 2016-09-26 | 다나-파버 캔서 인스티튜트 인크. | 디히드로프테리디논 유도체 및 그의 용도 |
| WO2015193228A1 (de) * | 2014-06-19 | 2015-12-23 | Bayer Pharma Aktiengesellschaft | Bet-proteininhibitorische 1,4-dihydropyrido[3,4-b]pyrazinone mit para-substituierter aromatischer amino- oder ethergruppe |
| RU2017104897A (ru) | 2014-08-08 | 2018-09-10 | Дана-Фарбер Кэнсер Инститьют, Инк. | Производные диазепана и их применения |
| US9867831B2 (en) | 2014-10-01 | 2018-01-16 | Boehringer Ingelheim International Gmbh | Combination treatment of acute myeloid leukemia and myelodysplastic syndrome |
| CA2986441A1 (en) | 2015-06-12 | 2016-12-15 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| RU2018112953A (ru) | 2015-09-11 | 2019-10-14 | Дана-Фарбер Кэнсер Инститьют, Инк. | Ацетамидтиенотриазолодиазепины и пути их применения |
| US11306105B2 (en) | 2015-09-11 | 2022-04-19 | Dana-Farber Cancer Institute, Inc. | Cyano thienotriazolodiazepines and uses thereof |
| CR20180336A (es) | 2015-11-25 | 2018-08-06 | Dana Farber Cancer Inst Inc | Inhibidores de bromodominio bivalentes y usos de los mismos |
| DE102017005091A1 (de) | 2016-05-30 | 2017-11-30 | Bayer Pharma Aktiengesellschaft | Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one |
| DE102017005089A1 (de) | 2016-05-30 | 2017-11-30 | Bayer Pharma Aktiengesellschaft | Substitulerte 3,4-Dihydrochinoxalin-2(1H)-one |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003509425A (ja) * | 1999-09-15 | 2003-03-11 | ワーナー−ランバート・カンパニー | キナーゼ阻害剤としてのプテリジノン |
| UY27427A1 (es) * | 2001-09-04 | 2003-03-31 | Boehringer Ingelheim Pharma | Nuevas dihidro-pteridinonas, procedimientos para su preparación y su utilización como medicamentos |
| DE50307267D1 (de) * | 2003-02-26 | 2007-06-21 | Boehringer Ingelheim Pharma | Dihydropteridinone, verfahren zu deren herstellung und deren verwendung als arzneimittel |
-
2005
- 2005-08-19 WO PCT/EP2005/054099 patent/WO2006021548A1/de not_active Ceased
- 2005-08-19 EP EP05779168A patent/EP1784406A1/de not_active Withdrawn
- 2005-08-19 CA CA002578560A patent/CA2578560A1/en not_active Abandoned
- 2005-08-19 JP JP2007528834A patent/JP2008510771A/ja active Pending
- 2005-08-25 US US11/211,783 patent/US7371753B2/en not_active Expired - Lifetime