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 |
|---|---|---|---|---|
| EP2734205B1 (en) | 2011-07-21 | 2018-03-21 | Tolero Pharmaceuticals, Inc. | Heterocyclic protein kinase inhibitors |
| CN104812756A (zh) * | 2012-09-26 | 2015-07-29 | 曼凯德公司 | 多激酶通路抑制剂 |
| JP6433974B2 (ja) | 2013-03-14 | 2018-12-05 | 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 | Ｊａｋ２およびａｌｋ２阻害剤およびその使用方法 |
| 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 |
| PL3298021T3 (pl) | 2015-05-18 | 2019-11-29 | Tolero Pharmaceuticals Inc | Proleki alvocidibu o zwiększonej biodostępności |
| WO2017024073A1 (en) | 2015-08-03 | 2017-02-09 | Tolero Pharmaceuticals, Inc. | Combination therapies for 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 |
| WO2018094275A1 (en) | 2016-11-18 | 2018-05-24 | Tolero Pharmaceuticals, Inc. | Alvocidib prodrugs and their use as protein kinase inhibitors |
| KR102513448B1 (ko) * | 2016-12-16 | 2023-03-23 | 씨스톤 파마슈티컬즈 | Cdk4/6 억제제 |
| 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 |
| US11174255B2 (en) * | 2017-05-15 | 2021-11-16 | University Of Houston System | Pyrido[2,3-d]pyrimidin-7-ones 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 |
| BR112020020246A8 (pt) | 2018-04-05 | 2022-10-18 | Sumitomo Dainippon Pharma Oncology Inc | Inibidores de cinase axl e uso dos mesmos |
| CA3095580A1 (en) | 2018-04-13 | 2019-10-17 | Sumitomo Dainippon Pharma Oncology, Inc. | Pim kinase inhibitors for treatment of myeloproliferative neoplasms and fibrosis associated with cancer |
| WO2020023910A1 (en) | 2018-07-26 | 2020-01-30 | Tolero Pharmaceuticals, Inc. | Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same |
| JP2022511029A (ja) | 2018-12-04 | 2022-01-28 | スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド | がんの処置のための薬剤としての使用のためのｃｄｋ９インヒビターおよびその多形 |
| MX2021005075A (es) * | 2018-12-07 | 2021-07-15 | Sumitomo Pharma Oncology Inc | Metodos para el tratamiento de cancer de prostata resistente a la castracion y sensible a la castracion. |
| AU2020221247B2 (en) | 2019-02-12 | 2024-12-12 | Sumitomo Pharma America, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
| JP2022525149A (ja) | 2019-03-20 | 2022-05-11 | スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド | ベネトクラクスが失敗した急性骨髄性白血病（ａｍｌ）の処置 |
| 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 |
| JP2026509318A (ja) | 2022-10-31 | 2026-03-18 | スミトモ・ファーマ・アメリカ・インコーポレイテッド | 骨髄増殖性新生物を治療するためのｐｉｍ１阻害剤 |
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 |
| AU742999B2 (en) * | 1997-08-20 | 2002-01-17 | Warner-Lambert Company | Naphthyridinones for inhibiting protein tyrosine kinase and cell cycle kinase mediated cellular proliferation |
| US6303652B1 (en) * | 1998-08-21 | 2001-10-16 | Hughes Institute | BTK inhibitors and methods for their identification and use |
| MXPA05007503A (es) * | 2003-01-17 | 2005-09-21 | Warner Lambert Co | Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular. |
| JP4758349B2 (ja) * | 2003-10-08 | 2011-08-24 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤としての化合物および組成物 |
| MX2008014618A (es) | 2006-05-15 | 2008-11-28 | Irm Llc | Composiciones y metodos para inhibidores de cinasas del receptor fgf. |
| AU2007254179B2 (en) | 2006-05-18 | 2013-03-21 | Pharmacyclics Llc | Intracellular kinase inhibitors |
| CN104812756A (zh) * | 2012-09-26 | 2015-07-29 | 曼凯德公司 | 多激酶通路抑制剂 |
-
2013
- 2013-09-25 CN CN201380060317.8A patent/CN104812756A/zh active Pending
- 2013-09-25 JP JP2015534612A patent/JP2015532281A/ja active Pending
- 2013-09-25 CA CA 2886275 patent/CA2886275A1/en active Pending
- 2013-09-25 WO PCT/US2013/061548 patent/WO2014052365A1/en not_active Ceased
- 2013-09-25 AU AU2013323736A patent/AU2013323736A1/en not_active Abandoned
- 2013-09-25 HK HK16100505.0A patent/HK1212683A1/zh unknown
- 2013-09-25 EP EP13840649.1A patent/EP2900668A4/en not_active Withdrawn
- 2013-09-25 US US14/431,476 patent/US9493454B2/en not_active Expired - Fee Related
-
2016
- 2016-09-26 US US15/276,604 patent/US9714247B2/en not_active Expired - Fee Related
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