JP2013519704A5 - - Google Patents
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- Publication number
- JP2013519704A5 JP2013519704A5 JP2012553296A JP2012553296A JP2013519704A5 JP 2013519704 A5 JP2013519704 A5 JP 2013519704A5 JP 2012553296 A JP2012553296 A JP 2012553296A JP 2012553296 A JP2012553296 A JP 2012553296A JP 2013519704 A5 JP2013519704 A5 JP 2013519704A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally
- alkyl
- group
- aryl
- cycloalkyl
- 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.)
- Granted
Links
- 125000005842 heteroatom Chemical group 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 15
- 239000000203 mixture Substances 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 15
- 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 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- -1 substituted Chemical class 0.000 claims 7
- 150000002431 hydrogen Chemical group 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 125000004193 piperazinyl group Chemical group 0.000 claims 6
- 125000005647 linker group Chemical group 0.000 claims 5
- 125000003386 piperidinyl group Chemical group 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 4
- 125000006710 (C2-C12) alkenyl group Chemical group 0.000 claims 3
- 125000005974 C6-C14 arylcarbonyl group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000002757 morpholinyl group Chemical group 0.000 claims 3
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000006711 (C2-C12) alkynyl group Chemical group 0.000 claims 2
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 208000031888 Mycoses Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 125000000480 butynyl group Chemical group [*]C#CC([H])([H])C([H])([H])[H] 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 238000004132 cross linking Methods 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000005592 polycycloalkyl group Polymers 0.000 claims 2
- 125000002568 propynyl group Chemical group [*]C#CC([H])([H])[H] 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 201000002909 Aspergillosis Diseases 0.000 claims 1
- 208000036641 Aspergillus infections Diseases 0.000 claims 1
- 206010071155 Autoimmune arthritis Diseases 0.000 claims 1
- 208000027496 Behcet disease Diseases 0.000 claims 1
- 208000009137 Behcet syndrome Diseases 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 208000003495 Coccidiosis Diseases 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000007336 Cryptococcosis Diseases 0.000 claims 1
- 241000221204 Cryptococcus neoformans Species 0.000 claims 1
- 206010012504 Dermatophytosis Diseases 0.000 claims 1
- 101000582926 Dictyostelium discoideum Probable serine/threonine-protein kinase PLK Proteins 0.000 claims 1
- 201000002563 Histoplasmosis Diseases 0.000 claims 1
- 206010023076 Isosporiasis Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 241001460074 Microsporum distortum Species 0.000 claims 1
- 208000003250 Mixed connective tissue disease Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 241000233870 Pneumocystis Species 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 102100031463 Serine/threonine-protein kinase PLK1 Human genes 0.000 claims 1
- 101710183160 Serine/threonine-protein kinase PLK1 Proteins 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 208000002474 Tinea Diseases 0.000 claims 1
- 206010061418 Zygomycosis Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 201000004988 autoimmune vasculitis Diseases 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 230000034303 cell budding Effects 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 208000011654 childhood malignant neoplasm Diseases 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000000394 mitotic effect Effects 0.000 claims 1
- 201000007524 mucormycosis Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 201000000317 pneumocystosis Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10153827.0 | 2010-02-17 | ||
| EP10153827 | 2010-02-17 | ||
| PCT/EP2011/052280 WO2011101369A1 (en) | 2010-02-17 | 2011-02-16 | Dihydropteridinones, method for production and use thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013519704A JP2013519704A (ja) | 2013-05-30 |
| JP2013519704A5 true JP2013519704A5 (enExample) | 2014-04-03 |
| JP5841548B2 JP5841548B2 (ja) | 2016-01-13 |
Family
ID=43864224
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012553296A Active JP5841548B2 (ja) | 2010-02-17 | 2011-02-16 | ジヒドロプテリジノン、その製造方法及び使用 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20120329803A1 (enExample) |
| EP (1) | EP2536725B1 (enExample) |
| JP (1) | JP5841548B2 (enExample) |
| WO (1) | WO2011101369A1 (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060035903A1 (en) | 2004-08-14 | 2006-02-16 | Boehringer Ingelheim International Gmbh | Storage stable perfusion solution for dihydropteridinones |
| US20060058311A1 (en) | 2004-08-14 | 2006-03-16 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation |
| US7439358B2 (en) | 2006-02-08 | 2008-10-21 | Boehringer Ingelheim International Gmbh | Specific salt, anhydrous and crystalline form of a dihydropteridione derivative |
| WO2011079114A1 (en) | 2009-12-23 | 2011-06-30 | Elan Pharmaceuticals, Inc. | Pteridinones as inhibitors of polo - like kinase |
| US8981083B2 (en) | 2010-05-14 | 2015-03-17 | Dana Farber Cancer Institute, Inc. | Compositions and methods for treating neoplasia, inflammatory disease and other disorders |
| CA2799381A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Male contraceptive compositions and methods of use |
| MX373121B (es) | 2010-05-14 | 2020-04-30 | Dana Farber Cancer Inst Inc | Composiciones y metodos para el tratamiento de leucemia. |
| 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 |
| US9370535B2 (en) | 2011-05-17 | 2016-06-21 | Boehringer Ingelheim International Gmbh | Method for treatment of advanced solid tumors |
| US9714946B2 (en) | 2013-03-14 | 2017-07-25 | Dana-Farber Cancer Institute, Inc. | Bromodomain binding reagents and uses thereof |
| BR112016001457A2 (pt) | 2013-07-25 | 2017-08-29 | Dana Farber Cancer Inst Inc | Inibidores de fatores de transcrição e usos dos mesmos |
| WO2015011236A1 (en) | 2013-07-26 | 2015-01-29 | Boehringer Ingelheim International Gmbh | Treatment of myelodysplastic syndrome |
| KR20160072261A (ko) | 2013-11-08 | 2016-06-22 | 다나-파버 캔서 인스티튜트 인크. | 브로모도메인 및 엑스트라-말단 (bet) 단백질 저해제를 이용한 암 치료를 위한 조합 요법 |
| MX2016009974A (es) | 2014-01-31 | 2016-10-31 | Dana Farber Cancer Inst Inc | Derivados de diaminopirimidina bencensulfona y sus usos. |
| WO2015117087A1 (en) * | 2014-01-31 | 2015-08-06 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
| KR20160111036A (ko) * | 2014-01-31 | 2016-09-23 | 다나-파버 캔서 인스티튜트 인크. | 디아제판 유도체 및 그의 용도 |
| RU2722179C2 (ru) | 2014-02-28 | 2020-05-28 | Тэнша Терапеутикс, Инк. | Лечение состояний, ассоциированных с гиперинсулинемией |
| EP3177626A4 (en) * | 2014-08-08 | 2017-12-27 | Dana Farber Cancer Institute, Inc. | Diazepane derivatives and uses thereof |
| WO2016022970A1 (en) | 2014-08-08 | 2016-02-11 | Dana-Farber Cancer Institute, Inc. | Dihydropteridinone derivatives and uses thereof |
| US9867831B2 (en) | 2014-10-01 | 2018-01-16 | Boehringer Ingelheim International Gmbh | Combination treatment of acute myeloid leukemia and myelodysplastic syndrome |
| UA122130C2 (uk) | 2014-10-27 | 2020-09-25 | Тенша Терапеутікс, Інк. | Інгібітори бромодомену |
| WO2016105518A1 (en) * | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| WO2016135046A1 (en) * | 2015-02-24 | 2016-09-01 | Academisch Medisch Centrum | Inhibitors of raf1, mst1, and pkl1 for use in the treatment of a retrovirus |
| US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| US11306105B2 (en) | 2015-09-11 | 2022-04-19 | Dana-Farber Cancer Institute, Inc. | Cyano thienotriazolodiazepines and uses thereof |
| JP2018526424A (ja) | 2015-09-11 | 2018-09-13 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | アセトアミドチエノトリアゾロジアゼピンおよびこれらの使用 |
| CR20180336A (es) | 2015-11-25 | 2018-08-06 | Dana Farber Cancer Inst Inc | Inhibidores de bromodominio bivalentes y usos de los mismos |
| DE102017005089A1 (de) | 2016-05-30 | 2017-11-30 | Bayer Pharma Aktiengesellschaft | Substitulerte 3,4-Dihydrochinoxalin-2(1H)-one |
| DE102017005091A1 (de) | 2016-05-30 | 2017-11-30 | Bayer Pharma Aktiengesellschaft | Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2623900A (en) | 1999-01-22 | 2000-08-07 | American Home Products Corporation | Compounds which inhibit leukocyte adhesion mediated by vla-4 |
| EA005287B1 (ru) | 1999-09-15 | 2004-12-30 | Уорнер-Ламберт Компани | Птеридиноны в качестве ингибиторов киназ |
| EP1427730B1 (de) | 2001-09-04 | 2006-07-12 | Boehringer Ingelheim Pharma GmbH & Co.KG | Neue dihydropteridinone, verfahren zu deren herstellung und deren verwendung als arzneimittel |
| BR0313160A (pt) | 2002-08-08 | 2005-07-12 | Smithkline Beecham Corp | Composto, composição farmacêutica, métodos para tratar uma condição e um neoplasmo suscetìvel em um animal em um animal, processo para preparar um composto e uso de um composto |
| UA80743C2 (en) | 2003-02-26 | 2007-10-25 | Boehringer Ingelheim Pharma | Dihydropteridinones, method for the production and use thereof in the form of drugs |
| 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 |
| US20060058311A1 (en) * | 2004-08-14 | 2006-03-16 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation |
| US20060074088A1 (en) * | 2004-08-14 | 2006-04-06 | Boehringer Ingelheim International Gmbh | Dihydropteridinones for the treatment of cancer diseases |
| 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 |
| CA2575804A1 (en) * | 2004-08-26 | 2006-03-02 | Boehringer Ingelheim International Gmbh | Pteridinones used as plk (polo like kinase) inhibitors |
| EP2100894A1 (en) * | 2008-03-12 | 2009-09-16 | 4Sc Ag | Pyridopyrimidines used as Plk1 (polo-like kinase) inhibitors |
-
2011
- 2011-02-16 US US13/576,220 patent/US20120329803A1/en not_active Abandoned
- 2011-02-16 EP EP11705850.3A patent/EP2536725B1/en active Active
- 2011-02-16 WO PCT/EP2011/052280 patent/WO2011101369A1/en not_active Ceased
- 2011-02-16 JP JP2012553296A patent/JP5841548B2/ja active Active
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