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- Withdrawn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 (OSRAM) | 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 (OSRAM) |
| EP (2) | EP2311842A3 (OSRAM) |
| JP (1) | JP2011525535A (OSRAM) |
| WO (1) | WO2010008847A2 (OSRAM) |
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 |
| US20100048524A1 (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 |
| CA2725014C (en) | 2008-05-30 | 2014-06-17 | Amgen Inc. | Inhibitors of pi3 kinase |
| PL2308877T3 (pl) | 2008-08-05 | 2014-07-31 | Daiichi Sankyo Co Ltd | Pochodne imidazopirydyn-2-onu |
| EA024252B1 (ru) | 2009-01-08 | 2016-08-31 | Кьюрис, Инк. | Ингибиторы фосфоинозитид-3-киназ с цинксвязывающей группой |
| CN102686600A (zh) | 2009-02-05 | 2012-09-19 | 托凯药业股份有限公司 | 甾体cyp17抑制剂/抗雄激素物质的新型药物前体 |
| CN102480966B (zh) * | 2009-06-12 | 2015-09-16 | 达娜-法勃肿瘤研究所公司 | 融合的杂环化合物及其用途 |
| CN102573846B (zh) | 2009-08-17 | 2015-10-07 | 因特利凯公司 | 杂环化合物及其用途 |
| 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 |
| US9127000B2 (en) | 2011-02-23 | 2015-09-08 | Intellikine, LLC. | Heterocyclic compounds and uses thereof |
| HUE028910T2 (en) | 2011-04-01 | 2017-01-30 | Curis Inc | Phosphoinositide 3-kinase inhibitor with a zinc binding moiety |
| WO2013049407A2 (en) | 2011-09-30 | 2013-04-04 | Kineta, Inc | Anti-viral compounds |
| EP2776837A4 (en) * | 2011-11-11 | 2015-05-20 | Intellikine Llc | COMBINATION OF KINASEINHIBITORS AND THEIR USE |
| EP2822935B1 (en) | 2011-11-17 | 2019-05-15 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| EP2827903A4 (en) * | 2012-03-23 | 2016-02-10 | Sloan Kettering Inst Cancer | POTENTIATION OF ANTIBODY-INDUCED COMPLEMENT-MEDIATED CYTOTOXICITY BY PI3K INHIBITION |
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| US10112927B2 (en) | 2012-10-18 | 2018-10-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| US10000483B2 (en) | 2012-10-19 | 2018-06-19 | 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 |
| WO2014158646A1 (en) * | 2013-03-13 | 2014-10-02 | Dow Agrosciences Llc | Improved 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 |
| CA2904170A1 (en) | 2013-03-14 | 2014-09-25 | University Of Maryland, Baltimore | Androgen receptor down-regulating agents and uses thereof |
| JP2016528252A (ja) | 2013-08-12 | 2016-09-15 | トーカイ ファーマシューティカルズ， インコーポレイテッド | アンドロゲン標的治療を使用する新生物障害の処置のためのバイオマーカー |
| CN104513254B (zh) | 2013-09-30 | 2019-07-26 | 上海璎黎药业有限公司 | 稠合嘧啶类化合物、中间体、其制备方法、组合物和应用 |
| ES2676734T3 (es) | 2013-10-18 | 2018-07-24 | Syros Pharmaceuticals, Inc. | Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas |
| EP3057956B1 (en) | 2013-10-18 | 2021-05-05 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7) |
| PL3805233T3 (pl) | 2014-01-13 | 2024-06-10 | Aurigene Oncology Limited | ENANCJOMERY (R) I (S) (S)-N-(5-(3-hydroksypirolidyn-1-ylo)-2-morfolinooksazolo[4,5-b]pirydyn-6-ylo)-2-(2-metylopirydyn-4-ylo)oksazolo-4-karboksyamidu jako inhibitory IRAK4 do leczenia nowotworu złośliwego |
| MX2016009135A (es) | 2014-01-14 | 2016-10-05 | Millennium Pharm Inc | Heteroarilos y usos de estos. |
| US10202373B2 (en) | 2014-01-14 | 2019-02-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| CA2943609A1 (en) | 2014-03-27 | 2015-10-01 | The Brigham And Women's Hospital, Inc. | Metabolically-activated drug conjugates to overcome resistance in cancer therapy |
| WO2015164604A1 (en) | 2014-04-23 | 2015-10-29 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged janus kinase inhibitors and uses thereof |
| US10017477B2 (en) | 2014-04-23 | 2018-07-10 | Dana-Farber Cancer Institute, Inc. | Janus kinase inhibitors and uses thereof |
| CN105130973B (zh) * | 2014-05-26 | 2018-05-01 | 海南国瑞堂中药制药有限公司 | 5-吡啶基-2-氨基-苯并[d]噁唑衍生物及其制备方法和用途 |
| EP3148564B1 (en) | 2014-06-02 | 2020-01-08 | Children's Medical Center Corporation | Methods and compositions for immunomodulation |
| US10870651B2 (en) | 2014-12-23 | 2020-12-22 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| AU2016243529B2 (en) | 2015-03-27 | 2021-03-25 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| JP7028766B2 (ja) | 2015-09-09 | 2022-03-02 | 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 | サイクリン依存性キナーゼの阻害剤 |
| WO2017083835A1 (en) * | 2015-11-13 | 2017-05-18 | The Trustees Of Columbia University In The City Of New York | Inhibition of tor complex 2 increases immunity against bacterial infection |
| WO2017156350A1 (en) | 2016-03-09 | 2017-09-14 | K-Gen, Inc. | Methods of cancer treatment |
| WO2018017435A1 (en) * | 2016-07-22 | 2018-01-25 | Accro Bioscience Inc. | Heteroaryl compounds as inhibitors of necrosis, composition and application thereof |
| 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 |
| CN120267671A (zh) * | 2017-03-31 | 2025-07-08 | 奥锐金肿瘤有限公司 | 用于治疗血液病的化合物和组合物 |
| WO2018237370A1 (en) * | 2017-06-23 | 2018-12-27 | Accro Bioscience Inc. | Heteroaryl compounds as inhibitors of necrosis, composition and method using the same |
| KR102736878B1 (ko) * | 2017-06-23 | 2024-12-05 | 벨로스바이오 인코포레이티드 | Ror1 항체 면역접합체 |
| CN109111464B (zh) * | 2017-06-23 | 2021-02-26 | 爱科诺生物医药股份有限公司 | 一种具有细胞坏死抑制活性的杂环化合物 |
| HUE062526T2 (hu) | 2017-10-02 | 2023-11-28 | 1St Biotherapeutics Inc | Benzotiazol vegyületek és azokat alkalmazó eljárások neurodegeneratív rendellenességek kezelésére |
| CN113194752A (zh) | 2018-06-01 | 2021-07-30 | 康奈尔大学 | Pi3k相关疾病或病症的组合疗法 |
| SG11202012150UA (en) | 2018-06-08 | 2021-01-28 | Ac Immune Sa | Novel compounds for diagnosis |
| AU2019295632B2 (en) | 2018-06-25 | 2025-03-06 | Dana-Farber Cancer Institute, Inc. | Taire family kinase inhibitors and uses thereof |
| WO2020055840A1 (en) | 2018-09-11 | 2020-03-19 | 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 |
| JP7660063B2 (ja) | 2018-12-28 | 2025-04-10 | 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 | サイクリン依存性キナーゼ７のインヒビターおよびそれらの使用 |
| US11098044B2 (en) | 2019-02-22 | 2021-08-24 | 1ST Biotherapeutics, Inc. | Imidazopyridinyl compounds and use thereof for treatment of neurodegenerative disorders |
| JP7456641B2 (ja) * | 2019-03-07 | 2024-03-27 | ファースト・バイオセラピューティクス・インコーポレイテッド | Ｐｅｔ放射性トレーサーとしての［１８ｆ］標識ベンゾチアゾール誘導体 |
| 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 |
| JP7604387B2 (ja) | 2019-03-28 | 2024-12-23 | ファースト・バイオセラピューティクス・インコーポレイテッド | ベンゾチアゾール化合物の薬学的塩、多形体及びその製造方法 |
| 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 |
| CN118767143A (zh) | 2019-12-12 | 2024-10-15 | 听治疗有限责任公司 | 用于预防和治疗听力损失的组合物和方法 |
| US20230234967A1 (en) * | 2020-05-28 | 2023-07-27 | Senda Biosciences, Inc. | Fused Azole Heterocycles as AHR Antagonists |
| WO2022038574A1 (en) * | 2020-08-21 | 2022-02-24 | 1ST Biotherapeutics, Inc. | Compounds for prevention or treatment of neurodegenerative disorders |
| EP4200269A1 (en) * | 2020-08-21 | 2023-06-28 | 1st Biotherapeutics, Inc. | [ 18F]-LABELED IMIDAZOPYRIDINE DERIVATIVES AS PET RADIOTRACER
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| US11834467B2 (en) | 2020-09-28 | 2023-12-05 | 1ST Biotherapeutics, Inc. | Substituted indazoles as hematopoietic progenitor kinase 1 (HPK1) inhibitors |
| CN117120054A (zh) | 2021-04-08 | 2023-11-24 | 柯里斯公司 | 治疗癌症的组合疗法 |
| EP4370160A1 (en) | 2021-07-15 | 2024-05-22 | President And Fellows Of Harvard College | 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 EP EP11153222A patent/EP2311842A3/en not_active Withdrawn
- 2009-06-23 WO PCT/US2009/048299 patent/WO2010008847A2/en not_active Ceased
- 2009-06-23 US US12/996,662 patent/US20110178070A1/en not_active Abandoned
- 2009-06-23 EP EP09789905A patent/EP2303886A2/en not_active Withdrawn
- 2009-06-23 JP JP2011516533A patent/JP2011525535A/ja not_active Withdrawn
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