JP2011525535A5 - - Google Patents
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- Publication number
- JP2011525535A5 JP2011525535A5 JP2011516533A JP2011516533A JP2011525535A5 JP 2011525535 A5 JP2011525535 A5 JP 2011525535A5 JP 2011516533 A JP2011516533 A JP 2011516533A JP 2011516533 A JP2011516533 A JP 2011516533A JP 2011525535 A5 JP2011525535 A5 JP 2011525535A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- hetero
- group
- compound
- 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.)
- Withdrawn
Links
- 125000000217 alkyl group Chemical group 0.000 claims 32
- 150000001875 compounds Chemical class 0.000 claims 26
- 229910052739 hydrogen Inorganic materials 0.000 claims 23
- 239000001257 hydrogen Substances 0.000 claims 23
- 125000005842 heteroatom Chemical group 0.000 claims 20
- 125000005843 halogen group Chemical group 0.000 claims 16
- 150000002431 hydrogen Chemical class 0.000 claims 15
- -1 cyano, hydroxyl Chemical group 0.000 claims 14
- 125000001424 substituent group Chemical group 0.000 claims 12
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 8
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 6
- 150000001334 alicyclic compounds Chemical class 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims 1
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000002723 alicyclic group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
- 125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=O 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- OHEURRCKFZFXCN-UHFFFAOYSA-N n-[5-(5-amino-6-chloropyridin-3-yl)-[1,3]thiazolo[5,4-d]pyrimidin-2-yl]acetamide Chemical compound N1=C2SC(NC(=O)C)=NC2=CN=C1C1=CN=C(Cl)C(N)=C1 OHEURRCKFZFXCN-UHFFFAOYSA-N 0.000 claims 1
- FQVXJCFYTSWIMB-UHFFFAOYSA-N n-[5-(6-aminopyridin-3-yl)-[1,3]thiazolo[5,4-d]pyrimidin-2-yl]acetamide Chemical compound N1=C2SC(NC(=O)C)=NC2=CN=C1C1=CC=C(N)N=C1 FQVXJCFYTSWIMB-UHFFFAOYSA-N 0.000 claims 1
- GEWZFIJSNQDMAD-UHFFFAOYSA-N n-[5-[5-(benzenesulfonamido)-6-chloropyridin-3-yl]-[1,3]thiazolo[5,4-d]pyrimidin-2-yl]acetamide Chemical compound N1=C2SC(NC(=O)C)=NC2=CN=C1C(C=1)=CN=C(Cl)C=1NS(=O)(=O)C1=CC=CC=C1 GEWZFIJSNQDMAD-UHFFFAOYSA-N 0.000 claims 1
- UWNLMWMXFKHKDP-UHFFFAOYSA-N n-[5-[6-chloro-5-(methanesulfonamido)pyridin-3-yl]-[1,3]thiazolo[5,4-d]pyrimidin-2-yl]acetamide Chemical compound N1=C2SC(NC(=O)C)=NC2=CN=C1C1=CN=C(Cl)C(NS(C)(=O)=O)=C1 UWNLMWMXFKHKDP-UHFFFAOYSA-N 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000005188 oxoalkyl group Chemical group 0.000 claims 1
- 125000005740 oxycarbonyl group Chemical group [*:1]OC([*:2])=O 0.000 claims 1
- 239000008194 pharmaceutical composition 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
- 150000003839 salts Chemical class 0.000 claims 1
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 0 Cc(c(*)nc(*)c1*)c1O* Chemical compound Cc(c(*)nc(*)c1*)c1O* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7513408P | 2008-06-24 | 2008-06-24 | |
| US61/075,134 | 2008-06-24 | ||
| PCT/US2009/048299 WO2010008847A2 (en) | 2008-06-24 | 2009-06-23 | Pi3k/m tor inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011525535A JP2011525535A (ja) | 2011-09-22 |
| JP2011525535A5 true JP2011525535A5 (enExample) | 2012-08-09 |
Family
ID=41550954
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011516533A Withdrawn JP2011525535A (ja) | 2008-06-24 | 2009-06-23 | ＰＩ３Ｋ／ｍＴＯＲ阻害剤 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20110178070A1 (enExample) |
| EP (2) | EP2311842A3 (enExample) |
| JP (1) | JP2011525535A (enExample) |
| WO (1) | WO2010008847A2 (enExample) |
Families Citing this family (69)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US20100048913A1 (en) | 2008-03-14 | 2010-02-25 | Angela Brodie | Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity |
| WO2009155121A2 (en) | 2008-05-30 | 2009-12-23 | Amgen Inc. | Inhibitors of pi3 kinase |
| RU2478636C2 (ru) | 2008-08-05 | 2013-04-10 | Дайити Санкио Компани, Лимитед | ПРОИЗВОДНЫЕ ИМИДАЗОПИРИДИН-2-ОНА, ОБЛАДАЮЩИЕ mTOR ИНГИБИРУЮЩЕЙ АКТИВНОСТЬЮ |
| EA024252B1 (ru) | 2009-01-08 | 2016-08-31 | Кьюрис, Инк. | Ингибиторы фосфоинозитид-3-киназ с цинксвязывающей группой |
| US20110312916A1 (en) | 2009-02-05 | 2011-12-22 | Tokai Pharmaceuticals, Inc. | Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens |
| EP2440058A4 (en) * | 2009-06-12 | 2012-11-21 | Dana Farber Cancer Inst Inc | MELTED HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF |
| UA111579C2 (uk) | 2009-08-17 | 2016-05-25 | Інтеллікіне Ллк | ГЕТЕРОЦИКЛІЧНІ ПОХІДНІ 2-АМІНОБЕНЗО[d]ОКСАЗОЛУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА ЇХ ЗАСТОСУВАННЯ ДЛЯ ЛІКУВАННЯ ЗАХВОРЮВАННЯ, ПОВ'АНОГО З РІ3-КІНАЗОЮ |
| AU2010343102B2 (en) | 2009-12-29 | 2016-03-24 | Dana-Farber Cancer Institute, Inc. | Type II Raf kinase inhibitors |
| US20110319405A1 (en) * | 2010-06-28 | 2011-12-29 | The Board Of Trustees Of The Leland Stanford Junior University | Treatment and prevention of diffuse parenchymal lung disease by selective active-site mTOR inhibitors |
| UY33337A (es) | 2010-10-18 | 2011-10-31 | Respivert Ltd | DERIVADOS SUSTITUIDOS DE 1H-PIRAZOL[ 3,4-d]PIRIMIDINA COMO INHIBIDORES DE LAS FOSFOINOSITIDA 3-QUINASAS |
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| US9682141B2 (en) | 2011-11-11 | 2017-06-20 | Intellikine Llc | Combination of kinase inhibitors and uses thereof |
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| US20150023954A1 (en) * | 2012-03-23 | 2015-01-22 | Memorial Sloan-Kettering Cancer Center | Potentiating antibody-induced complement-mediated cytotoxicity via pi3k inhibition |
| EP2897644B1 (en) * | 2012-09-20 | 2018-06-06 | Novartis AG | Pharmaceutical combination comprising a phosphatidylinositol 3-kinase inhibitor and an aromatase inhibitor |
| US10112927B2 (en) | 2012-10-18 | 2018-10-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| WO2014063054A1 (en) | 2012-10-19 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof |
| WO2014063061A1 (en) | 2012-10-19 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| US9073946B2 (en) * | 2013-01-15 | 2015-07-07 | Kineta, Inc. | Anti-viral compounds |
| US20140275564A1 (en) * | 2013-03-13 | 2014-09-18 | Dow Agrosciences Llc | Process for the preparation of certain triaryl rhamnose carbamates |
| US20140275560A1 (en) * | 2013-03-13 | 2014-09-18 | Dow Agrosciences Llc | Preparation of 1,3-(substituted-diaryl)-1,2,4-triazoles and intermediates therefrom |
| KR20150127720A (ko) | 2013-03-14 | 2015-11-17 | 유니버시티 오브 매릴랜드, 발티모어 | 안드로겐 수용체 하향 조절제 및 그의 용도 |
| EP3033088A4 (en) | 2013-08-12 | 2017-03-08 | Tokai Pharmaceuticals, Inc. | Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies |
| EP3053926B1 (en) | 2013-09-30 | 2018-08-08 | Shanghai Yingli Pharmaceutical Co. Ltd. | Fused pyrimidine compound, intermediate, preparation method therefor, and composition and application thereof |
| EP3057956B1 (en) | 2013-10-18 | 2021-05-05 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7) |
| EP3057955B1 (en) | 2013-10-18 | 2018-04-11 | Syros Pharmaceuticals, Inc. | Heteroaromatic compounds useful for the treatment of prolferative diseases |
| US9732095B2 (en) | 2014-01-13 | 2017-08-15 | Aurigene Discovery Technologies Limited | Bicyclic heterocyclyl derivatives as IRAK4 inhibitors |
| EP3094326A4 (en) | 2014-01-14 | 2017-07-26 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
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| CA2972239A1 (en) | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| CN107427521B (zh) | 2015-03-27 | 2021-08-03 | 达纳-法伯癌症研究所股份有限公司 | 细胞周期蛋白依赖性激酶的抑制剂 |
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| EP4019515A1 (en) | 2015-09-09 | 2022-06-29 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| US11116754B2 (en) | 2015-11-13 | 2021-09-14 | The Trustees Of Columbia University In The City Of New York | Inhibition of TOR complex 2 increases immunity against bacterial infection |
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| CN107641118B (zh) * | 2016-07-22 | 2020-11-06 | 爱科诺生物医药股份有限公司 | 具有细胞坏死抑制活性的化合物及其组合物和应用 |
| CN110691589A (zh) * | 2017-03-31 | 2020-01-14 | 奥列基因发现技术有限公司 | 用于治疗血液病的化合物和组合物 |
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| JP7768505B2 (ja) | 2018-06-01 | 2025-11-12 | コーネル・ユニバーシティー | Ｐｉ３ｋに関連する疾患または障害に対する併用療法 |
| EP3802548B1 (en) | 2018-06-08 | 2024-08-14 | AC Immune SA | Novel compounds for diagnosis |
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| ES3014591T3 (en) | 2018-09-11 | 2025-04-23 | Curis Inc | Combination therapy with a phosphoinositide 3-kinase inhibitor with a zinc binding moiety |
| CN109320511A (zh) * | 2018-10-26 | 2019-02-12 | 广安凯特制药有限公司 | 一种高纯度帕博西尼中间体产品及其制备方法 |
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| MX2021010122A (es) | 2019-02-22 | 2021-09-23 | 1St Biotherapeutics Inc | Compuestos de imidazopiridinilo y su uso para el tratamiento de trastornos neurodegenerativos. |
| EP3934702B1 (en) * | 2019-03-07 | 2024-05-08 | 1st Biotherapeutics, Inc. | [ 18f]-labeled benzothiazole derivative as pet radiotracer |
| US10385046B1 (en) | 2019-03-19 | 2019-08-20 | 1ST Biotherapeutics, Inc. | Processes for preparing benzothiazol compounds and methods of using the same for treating neurodegenerative disorders |
| CN113631554B (zh) * | 2019-03-28 | 2024-06-21 | 第一生物治疗股份有限公司 | 苯并噻唑化合物的药用盐、多晶型物及其制备方法 |
| CN110256466A (zh) * | 2019-07-31 | 2019-09-20 | 昆山迪安医学检验实验室有限公司 | 一种噻唑[5,4-b]-吡啶基生物活性化合物的制备方法及其抗肿瘤活性的检测 |
| EP4073102A4 (en) | 2019-12-12 | 2024-05-08 | Ting Therapeutics LLC | Compositions and methods for the prevention and treatment of hearing loss |
| WO2021242955A1 (en) * | 2020-05-28 | 2021-12-02 | Senda Biosciences, Inc. | Fused azole heterocycles as ahr antagonists |
| CN115968362B (zh) * | 2020-08-21 | 2025-06-13 | 第一生物治疗股份有限公司 | 作为pet放射性示踪剂的[18f]-标记的咪唑并吡啶衍生物 |
| US12398156B2 (en) * | 2020-08-21 | 2025-08-26 | 1ST Biotherapeutics, Inc. | Compounds for prevention or treatment of neurodegenerative disorders |
| WO2022064459A1 (en) * | 2020-09-28 | 2022-03-31 | 1ST Biotherapeutics, Inc. | Indazoles as hematopoietic progenitor kinase 1 (hpk1) inhibitors and methods of using same |
| IL307465A (en) | 2021-04-08 | 2023-12-01 | Curis Inc | Combined therapies for cancer treatment |
| CA3223081A1 (en) | 2021-07-15 | 2023-01-19 | Samir Mitragotri | Compositions and methods relating to cells with adhered particles |
| CZ310416B6 (cs) * | 2023-12-15 | 2025-05-28 | Univerzita Hradec Králové | 1-(3-Chlor-4-hydroxyfenyl)-3-(6-((trifluormethyl)thio)benzo[d]thiazol-2-yl)močovina pro použití pro léčbu rakoviny |
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-
2009
- 2009-06-23 JP JP2011516533A patent/JP2011525535A/ja not_active Withdrawn
- 2009-06-23 US US12/996,662 patent/US20110178070A1/en not_active Abandoned
- 2009-06-23 EP EP11153222A patent/EP2311842A3/en not_active Withdrawn
- 2009-06-23 EP EP09789905A patent/EP2303886A2/en not_active Withdrawn
- 2009-06-23 WO PCT/US2009/048299 patent/WO2010008847A2/en not_active Ceased
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