JP2015532281A5 - - Google Patents
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- Publication number
- JP2015532281A5 JP2015532281A5 JP2015534612A JP2015534612A JP2015532281A5 JP 2015532281 A5 JP2015532281 A5 JP 2015532281A5 JP 2015534612 A JP2015534612 A JP 2015534612A JP 2015534612 A JP2015534612 A JP 2015534612A JP 2015532281 A5 JP2015532281 A5 JP 2015532281A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- carbonyl group
- alkyl
- hydroxyl
- alkylamino
- 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 29
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 15
- -1 ethoxyl Chemical group 0.000 claims 15
- 239000000203 mixture Substances 0.000 claims 9
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 8
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 102100029823 Tyrosine-protein kinase BTK Human genes 0.000 claims 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 7
- 210000004027 cell Anatomy 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 125000006698 (C1-C3) dialkylamino group Chemical group 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims 5
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims 5
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 claims 4
- ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 claims 4
- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims 4
- 229960002448 dasatinib Drugs 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 208000023275 Autoimmune disease Diseases 0.000 claims 3
- 125000003282 alkyl amino group Chemical group 0.000 claims 3
- 125000004663 dialkyl amino group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 2
- 102000001714 Agammaglobulinaemia Tyrosine Kinase Human genes 0.000 claims 2
- 108010029445 Agammaglobulinaemia Tyrosine Kinase Proteins 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 210000000601 blood cell Anatomy 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 238000001514 detection method Methods 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 230000036210 malignancy Effects 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 102000003989 Aurora kinases Human genes 0.000 claims 1
- 108090000433 Aurora kinases Proteins 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 101100278318 Dictyostelium discoideum dohh-2 gene Proteins 0.000 claims 1
- 230000037057 G1 phase arrest Effects 0.000 claims 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 210000004671 cell-free system Anatomy 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000000155 isotopic effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- VBUBYMVULIMEHR-UHFFFAOYSA-N propa-1,2-diene;prop-1-yne Chemical compound CC#C.C=C=C VBUBYMVULIMEHR-UHFFFAOYSA-N 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261706084P | 2012-09-26 | 2012-09-26 | |
| US61/706,084 | 2012-09-26 | ||
| US201361757331P | 2013-01-28 | 2013-01-28 | |
| US61/757,331 | 2013-01-28 | ||
| US201361785992P | 2013-03-14 | 2013-03-14 | |
| US61/785,992 | 2013-03-14 | ||
| PCT/US2013/061548 WO2014052365A1 (en) | 2012-09-26 | 2013-09-25 | Multiple kinase pathway inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015532281A JP2015532281A (ja) | 2015-11-09 |
| JP2015532281A5 true JP2015532281A5 (enExample) | 2016-11-17 |
Family
ID=50388917
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015534612A Pending JP2015532281A (ja) | 2012-09-26 | 2013-09-25 | 複数キナーゼ経路阻害剤 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US9493454B2 (enExample) |
| EP (1) | EP2900668A4 (enExample) |
| JP (1) | JP2015532281A (enExample) |
| CN (1) | CN104812756A (enExample) |
| AU (1) | AU2013323736A1 (enExample) |
| CA (1) | CA2886275A1 (enExample) |
| HK (1) | HK1212683A1 (enExample) |
| WO (1) | WO2014052365A1 (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9416132B2 (en) | 2011-07-21 | 2016-08-16 | Tolero Pharmaceuticals, Inc. | Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors |
| JP2015532281A (ja) * | 2012-09-26 | 2015-11-09 | マンカインド コーポレイション | 複数キナーゼ経路阻害剤 |
| DK2970205T3 (da) | 2013-03-14 | 2019-07-29 | Tolero Pharmaceuticals Inc | JAK2- og ALK2-inhibitorer og fremgangsmåder til anvendelse deraf |
| CN104418853B (zh) * | 2013-08-28 | 2016-09-07 | 北大方正集团有限公司 | 取代的萘啶-2-酮化合物、制备方法、用途及药物组合物 |
| CN105622638B (zh) * | 2014-10-29 | 2018-10-02 | 广州必贝特医药技术有限公司 | 嘧啶或吡啶并吡啶酮类化合物及其制备方法和应用 |
| WO2016161248A1 (en) * | 2015-04-02 | 2016-10-06 | Tolero Pharmaceuticals, Inc. | Targeting pim kinases in combination with btk inhibition |
| JP6510075B2 (ja) | 2015-05-18 | 2019-05-08 | トレロ ファーマシューティカルズ， インコーポレイテッド | バイオアベイラビリティが高いアルボシジブプロドラッグ |
| EP3331510A4 (en) | 2015-08-03 | 2019-04-03 | Tolero Pharmaceuticals, Inc. | COMBINATION THERAPIES FOR THE TREATMENT OF CANCER |
| CN105130986B (zh) * | 2015-09-30 | 2017-07-18 | 广州科擎新药开发有限公司 | 嘧啶或吡啶并吡啶酮类化合物及其应用 |
| US11279694B2 (en) | 2016-11-18 | 2022-03-22 | Sumitomo Dainippon Pharma Oncology, Inc. | Alvocidib prodrugs and their use as protein kinase inhibitors |
| JP7044801B2 (ja) * | 2016-12-16 | 2022-03-30 | シーストーン・ファーマスーティカルズ・（スージョウ）・カンパニー・リミテッド | Ｃｄｋ４／６阻害剤 |
| CN108264511B (zh) * | 2017-01-03 | 2021-04-13 | 浙江海正药业股份有限公司 | 杂环类衍生物及其制备方法和其在医药上的用途 |
| WO2018213219A1 (en) * | 2017-05-15 | 2018-11-22 | University Of Houston System | Pyrido[2,3-d]pyrimidin-7ones and related compounds as inhibitors of protein kinases |
| WO2019055579A1 (en) | 2017-09-12 | 2019-03-21 | Tolero Pharmaceuticals, Inc. | TREATMENT REGIME FOR CANCERS THAT ARE INSENSITIVE TO BCL-2 INHIBITORS USING THE MCL-1 ALVOCIDIB INHIBITOR |
| WO2019195753A1 (en) | 2018-04-05 | 2019-10-10 | Tolero Pharmaceuticals, Inc. | Axl kinase inhibitors and use of the same |
| EP3773560A4 (en) | 2018-04-13 | 2022-01-19 | Sumitomo Dainippon Pharma Oncology, Inc. | PIM KINASE INHIBITORS FOR THE TREATMENT OF MYELOPROLIFERATIVE NEOPLASMS AND CANCER-ASSOCIATED FIBROSIS |
| CN112512597A (zh) | 2018-07-26 | 2021-03-16 | 大日本住友制药肿瘤公司 | 用于治疗与acvr1表达异常相关的疾病的方法以及用于此的acvr1抑制剂 |
| US11034710B2 (en) | 2018-12-04 | 2021-06-15 | Sumitomo Dainippon Pharma Oncology, Inc. | CDK9 inhibitors and polymorphs thereof for use as agents for treatment of cancer |
| KR20210100145A (ko) * | 2018-12-07 | 2021-08-13 | 스미토모 다이니폰 파마 온콜로지, 인크. | 거세-저항성 및 거세-민감성 전립선암의 치료 방법 |
| CA3127502A1 (en) | 2019-02-12 | 2020-08-20 | Sumitomo Dainippon Pharma Oncology, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
| US11793802B2 (en) | 2019-03-20 | 2023-10-24 | Sumitomo Pharma Oncology, Inc. | Treatment of acute myeloid leukemia (AML) with venetoclax failure |
| CN117430597A (zh) * | 2022-07-14 | 2024-01-23 | 浙江同源康医药股份有限公司 | 用作cdk4激酶抑制剂的化合物及其应用 |
| AU2023372386A1 (en) | 2022-10-31 | 2025-05-08 | Sumitomo Pharma America, Inc. | Pim1 inhibitor for treating myeloproliferative neoplasms |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL117923A (en) | 1995-05-03 | 2000-06-01 | Warner Lambert Co | Anti-cancer pharmaceutical compositions containing polysubstituted pyrido¬2,3-d¾pyrimidine derivatives and certain such novel compounds |
| US5945422A (en) | 1997-02-05 | 1999-08-31 | Warner-Lambert Company | N-oxides of amino containing pyrido 2,3-D! pyrimidines |
| DE69828408T2 (de) * | 1997-08-20 | 2005-12-08 | Warner-Lambert Co. Llc | Naphthyridinone zur hemmung der durch protein-tyrosin-kinase und zellzyklus kinase hervorgerufenen zellvermehrung |
| US6303652B1 (en) * | 1998-08-21 | 2001-10-16 | Hughes Institute | BTK inhibitors and methods for their identification and use |
| WO2004065378A1 (en) * | 2003-01-17 | 2004-08-05 | Warner-Lambert Company Llc | 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation |
| EP1673343A4 (en) | 2003-10-08 | 2008-09-10 | Irm Llc | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS |
| EP2018167A4 (en) * | 2006-05-15 | 2010-07-14 | Irm Llc | COMPOSITIONS AND METHODS AS INHIBITORS OF FGF RECEPTOR KINASES |
| CA2651732C (en) | 2006-05-18 | 2014-10-14 | Mannkind Corporation | Intracellular kinase inhibitors |
| JP2015532281A (ja) * | 2012-09-26 | 2015-11-09 | マンカインド コーポレイション | 複数キナーゼ経路阻害剤 |
-
2013
- 2013-09-25 JP JP2015534612A patent/JP2015532281A/ja active Pending
- 2013-09-25 CA CA 2886275 patent/CA2886275A1/en active Pending
- 2013-09-25 AU AU2013323736A patent/AU2013323736A1/en not_active Abandoned
- 2013-09-25 US US14/431,476 patent/US9493454B2/en not_active Expired - Fee Related
- 2013-09-25 EP EP13840649.1A patent/EP2900668A4/en not_active Withdrawn
- 2013-09-25 CN CN201380060317.8A patent/CN104812756A/zh active Pending
- 2013-09-25 WO PCT/US2013/061548 patent/WO2014052365A1/en not_active Ceased
- 2013-09-25 HK HK16100505.0A patent/HK1212683A1/zh unknown
-
2016
- 2016-09-26 US US15/276,604 patent/US9714247B2/en not_active Expired - Fee Related
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