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- Withdrawn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 (https=) | 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 (https=) |
| EP (2) | EP2303886A2 (https=) |
| JP (1) | JP2011525535A (https=) |
| WO (1) | WO2010008847A2 (https=) |
Families Citing this family (71)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2211615A4 (en) * | 2007-10-22 | 2010-10-13 | Glaxosmithkline Llc | PYRIDOSULFONAMIDE DERIVATIVES AS PI3 KINASE INHIBITORS |
| 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 |
| CA2725014C (en) | 2008-05-30 | 2014-06-17 | Amgen Inc. | Inhibitors of pi3 kinase |
| BRPI0917540A2 (pt) | 2008-08-05 | 2015-11-17 | Daiichi Sankyo Co Ltd | composto, sal farmacologicamente aceitavél, composição farmacêutica, e, uso de um composto ou sal farmacologicamente aceitável |
| 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 |
| US8765747B2 (en) * | 2009-06-12 | 2014-07-01 | Dana-Farber Cancer Institute, Inc. | Fused 2-aminothiazole compounds |
| NZ598220A (en) | 2009-08-17 | 2014-02-28 | Intellikine Llc | Heterocyclic compounds and uses thereof |
| WO2011090738A2 (en) | 2009-12-29 | 2011-07-28 | 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 |
| WO2012116237A2 (en) | 2011-02-23 | 2012-08-30 | Intellikine, Llc | Heterocyclic compounds and uses thereof |
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| JP2014528412A (ja) * | 2011-09-30 | 2014-10-27 | キネタ・インコーポレイテツド | 抗ウイルス化合物 |
| HK1202333A1 (en) * | 2011-11-11 | 2015-09-25 | Intellikine, Llc | Combination of kinase inhibitors and uses thereof |
| US9382239B2 (en) | 2011-11-17 | 2016-07-05 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-Jun-N-terminal kinase (JNK) |
| WO2013142245A1 (en) * | 2012-03-23 | 2013-09-26 | Memorial Sloan-Kettering Cancer Center | Potentiating antibody-induced complement-mediated cytotoxicity via pi3k inhibition |
| PT2897644T (pt) * | 2012-09-20 | 2018-10-16 | Novartis Ag | Associação farmacêutica compreendendo um inibidor de fosfatidilinositol 3-quinase e um inibidor da aromatase |
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| RU2015137617A (ru) | 2013-03-14 | 2017-04-18 | Юниверсити Оф Мэриленд, Балтимор Офис Оф Текнолоджи Трансфер | Агенты, подавляющие андрогенные рецепторы, и их применение |
| CN105636594A (zh) | 2013-08-12 | 2016-06-01 | 托凯药业股份有限公司 | 使用雄激素靶向疗法用于治疗肿瘤性疾病的生物标记物 |
| 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) |
| WO2015058126A1 (en) | 2013-10-18 | 2015-04-23 | Syros Pharmaceuticals, Inc. | Heteroaromatic compounds useful for the treatment of prolferative diseases |
| LT3466955T (lt) | 2014-01-13 | 2021-02-25 | Aurigene Discovery Technologies Limited | Oksazol[4,5-b]piridino ir tiazol[4,5-b]piridino darinių, kaip irak4 inhibitorių, skirtų vėžio gydymui, gamybos būdas |
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| US9862688B2 (en) | 2014-04-23 | 2018-01-09 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged 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 |
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| JP6854762B2 (ja) | 2014-12-23 | 2021-04-07 | 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（ｃｄｋ７）の阻害剤 |
| USRE50776E1 (en) | 2015-03-27 | 2026-02-03 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
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| AU2016319125B2 (en) | 2015-09-09 | 2021-04-08 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| 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 |
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| 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 |
| EP3600270B1 (en) * | 2017-03-31 | 2023-06-14 | Aurigene Oncology Limited | Compounds and compositions for treating hematological disorders |
| AU2018289581C1 (en) * | 2017-06-23 | 2025-01-30 | VelosBio Inc. | ROR1 antibody immunoconjugates |
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| 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 |
| AU2018346051B2 (en) | 2017-10-02 | 2022-11-10 | 1st Biotherapeutics Inc. | Benzothiazol compounds and methods using the same for treating neurodegenerative disorders |
| CA3102279A1 (en) | 2018-06-01 | 2019-12-05 | Cornell University | Combination therapy for pi3k-associated disease or disorder |
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| CN113164466B (zh) | 2018-09-11 | 2025-07-08 | 柯瑞斯公司 | 使用具有锌结合部分的磷酸肌醇3-激酶抑制剂的联合治疗 |
| 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 |
| US12281126B2 (en) | 2018-12-28 | 2025-04-22 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 and uses thereof |
| AU2020224401A1 (en) | 2019-02-22 | 2021-10-14 | 1ST Biotherapeutics, Inc. | Imidazopyridinyl compounds and use thereof for treatment of neurodegenerative disorders |
| EP3934702B1 (en) * | 2019-03-07 | 2024-05-08 | 1st Biotherapeutics, Inc. | [ 18f]-labeled benzothiazole derivative as pet radiotracer |
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| KR20210134065A (ko) * | 2019-03-28 | 2021-11-08 | 주식회사 퍼스트바이오테라퓨틱스 | 벤조티아졸 화합물의 약제학적 염, 다형체 및 이들의 제조 방법 |
| 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 |
| US12570638B2 (en) | 2020-05-20 | 2026-03-10 | Sail Biomedicines, Inc. | Fused imidazole derivatives as AHR antagonists |
| US20230234967A1 (en) * | 2020-05-28 | 2023-07-27 | Senda Biosciences, Inc. | Fused Azole Heterocycles as AHR Antagonists |
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| WO2022064459A1 (en) * | 2020-09-28 | 2022-03-31 | 1ST Biotherapeutics, Inc. | Indazoles as hematopoietic progenitor kinase 1 (hpk1) inhibitors and methods of using same |
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| WO2023288046A1 (en) | 2021-07-15 | 2023-01-19 | President And Fellows Of Harvard College | Compositions and methods relating to cells with adhered particles |
| CZ2023489A3 (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 |
| GB202415232D0 (en) | 2024-10-16 | 2024-11-27 | Nacamed As | Composition |
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| GB1429184A (en) | 1972-04-20 | 1976-03-24 | Allen & Hanburys Ltd | Physically anti-inflammatory steroids for use in aerosols |
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-
2009
- 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 EP EP11153222A patent/EP2311842A3/en not_active Withdrawn
- 2009-06-23 JP JP2011516533A patent/JP2011525535A/ja not_active Withdrawn
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