CA2781056A1 - Kinase inhibitors - Google Patents
Kinase inhibitors Download PDFInfo
- Publication number
- CA2781056A1 CA2781056A1 CA2781056A CA2781056A CA2781056A1 CA 2781056 A1 CA2781056 A1 CA 2781056A1 CA 2781056 A CA2781056 A CA 2781056A CA 2781056 A CA2781056 A CA 2781056A CA 2781056 A1 CA2781056 A1 CA 2781056A1
- Authority
- CA
- Canada
- Prior art keywords
- substituted
- unsubstituted
- heteroaryl
- heterocycloalkyl
- alkyl
- 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.)
- Abandoned
Links
- 229940043355 kinase inhibitor Drugs 0.000 title claims abstract description 190
- 239000003757 phosphotransferase inhibitor Substances 0.000 title claims abstract description 188
- 108091000080 Phosphotransferase Proteins 0.000 claims abstract description 135
- 102000020233 phosphotransferase Human genes 0.000 claims abstract description 135
- 238000000034 method Methods 0.000 claims abstract description 90
- 230000002401 inhibitory effect Effects 0.000 claims abstract description 26
- 125000001072 heteroaryl group Chemical group 0.000 claims description 234
- 125000000217 alkyl group Chemical group 0.000 claims description 171
- 125000003118 aryl group Chemical group 0.000 claims description 162
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 160
- 150000001875 compounds Chemical class 0.000 claims description 154
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 144
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 138
- 229910052739 hydrogen Inorganic materials 0.000 claims description 116
- 239000001257 hydrogen Substances 0.000 claims description 114
- -1 1H-pyrrolo[2,3-b]pyridinyl Chemical group 0.000 claims description 105
- 229910052736 halogen Inorganic materials 0.000 claims description 94
- 150000002367 halogens Chemical class 0.000 claims description 92
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 89
- 150000002431 hydrogen Chemical class 0.000 claims description 88
- 230000002441 reversible effect Effects 0.000 claims description 87
- 108060006633 protein kinase Proteins 0.000 claims description 84
- 102000001253 Protein Kinase Human genes 0.000 claims description 83
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 83
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 80
- 230000000694 effects Effects 0.000 claims description 52
- 125000002947 alkylene group Chemical group 0.000 claims description 39
- 125000004474 heteroalkylene group Chemical group 0.000 claims description 39
- 125000005549 heteroarylene group Chemical group 0.000 claims description 39
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims description 36
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- 125000002993 cycloalkylene group Chemical group 0.000 claims description 35
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- 125000001997 phenyl group Chemical class [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 11
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- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims description 6
- 125000002541 furyl group Chemical group 0.000 claims description 6
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 6
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- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims description 6
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 6
- 125000004076 pyridyl group Chemical group 0.000 claims description 6
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 6
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- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 5
- 125000005955 1H-indazolyl group Chemical group 0.000 claims description 4
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- 125000001544 thienyl group Chemical group 0.000 claims description 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 3
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- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims description 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 2
- 125000001422 pyrrolinyl group Chemical group 0.000 claims description 2
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- 125000003831 tetrazolyl group Chemical group 0.000 claims description 2
- 125000005306 thianaphthenyl group Chemical group 0.000 claims description 2
- 102220587413 N-acetylserotonin O-methyltransferase-like protein_R23A_mutation Human genes 0.000 claims 2
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims 1
- 101000945096 Homo sapiens Ribosomal protein S6 kinase alpha-5 Proteins 0.000 claims 1
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- 210000004027 cell Anatomy 0.000 description 54
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Classifications
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- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07—ORGANIC CHEMISTRY
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- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
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- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C07—ORGANIC CHEMISTRY
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- C07D473/00—Heterocyclic compounds containing purine ring systems
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
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Landscapes
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Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
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| US26169609P | 2009-11-16 | 2009-11-16 | |
| US61/261,696 | 2009-11-16 | ||
| US33027110P | 2010-04-30 | 2010-04-30 | |
| US61/330,271 | 2010-04-30 | ||
| PCT/US2010/056890 WO2011060440A2 (en) | 2009-11-16 | 2010-11-16 | Kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
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| CA2781056A1 true CA2781056A1 (en) | 2011-05-19 |
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| Application Number | Title | Priority Date | Filing Date |
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| CA2781056A Abandoned CA2781056A1 (en) | 2009-11-16 | 2010-11-16 | Kinase inhibitors |
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| Country | Link |
|---|---|
| US (2) | US20130035325A1 (enExample) |
| EP (1) | EP2558099A4 (enExample) |
| JP (1) | JP2013510886A (enExample) |
| CN (1) | CN102711765A (enExample) |
| AU (1) | AU2010319964A1 (enExample) |
| BR (1) | BR112012011528A2 (enExample) |
| CA (1) | CA2781056A1 (enExample) |
| MX (1) | MX2012005678A (enExample) |
| WO (1) | WO2011060440A2 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11524968B2 (en) | 2017-10-18 | 2022-12-13 | Hk Inno.N Corporation | Heterocyclic compound as a protein kinase inhibitor |
| US12180185B2 (en) | 2018-11-15 | 2024-12-31 | Hk Inno.N Corporation | Compound as protein kinase inhibitor, and pharmaceutical composition comprising thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2710005T1 (sl) | 2011-05-17 | 2017-03-31 | Principia Biopharma Inc. | Zaviralci tirozinske kinaze |
| US9376438B2 (en) | 2011-05-17 | 2016-06-28 | Principia Biopharma, Inc. | Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors |
| BR112013029508B1 (pt) * | 2011-05-17 | 2022-05-03 | Principia Biopharma, Inc. | Composto, composição farmacêutica, e, uso do referido composto |
| MX368112B (es) | 2012-06-18 | 2019-09-18 | Principia Biopharma Inc | Pirrolo- o pirazolopirimidinas covalentes reversibles utiles para el tratamiento del cancer y de enfermedades autoinmunitarias. |
| JP2015526520A (ja) | 2012-08-31 | 2015-09-10 | プリンシピア バイオファーマ インコーポレイテッド | Itk阻害剤としてのベンズイミダゾール誘導体 |
| RS58956B1 (sr) | 2012-09-10 | 2019-08-30 | Principia Biopharma Inc | Jedinjenja pirazolopirimidina kao inhibitori kinaze |
| WO2014093230A2 (en) | 2012-12-10 | 2014-06-19 | Merck Patent Gmbh | Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity |
| US8957080B2 (en) | 2013-04-09 | 2015-02-17 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| EA033900B1 (ru) | 2014-02-21 | 2019-12-06 | Принсипиа Биофарма Инк. | СОЛЕВЫЕ И АМОРФНЫЕ ФОРМЫ 2-[(3R)-3-[4-АМИНО-3-(2-ФТОР-4-ФЕНОКСИФЕНИЛ)ПИРАЗОЛО[3,4-d]ПИРИМИДИН-1-ИЛ]ПИПЕРИДИН-1-КАРБОНИЛ]-4-МЕТИЛ-4-[4-(ОКСЕТАН-3-ИЛ)ПИПЕРАЗИН-1-ИЛ]ПЕНТ-2-ЕННИТРИЛА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ И СПОСОБ ЛЕЧЕНИЯ ПУЗЫРЧАТКИ ОБЫКНОВЕННОЙ И ПУЗЫРЧАТКИ ЛИСТОВИДНОЙ С ИХ ПРИМЕНЕНИЕМ |
| PL3166608T3 (pl) | 2014-07-07 | 2019-07-31 | Jiangsu Hengrui Medicine Co., Ltd. | Związki aminopirydazynonowe jako inhibitory kinaz białkowych |
| CA2970723C (en) | 2014-12-18 | 2023-09-05 | Principia Biopharma Inc. | Treatment of pemphigus |
| EP3313839A1 (en) | 2015-06-24 | 2018-05-02 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| WO2017118277A1 (zh) * | 2016-01-05 | 2017-07-13 | 江苏恒瑞医药股份有限公司 | 一种btk激酶抑制剂的结晶形式及其制备方法 |
| CN106939002B (zh) * | 2016-01-05 | 2019-09-24 | 江苏恒瑞医药股份有限公司 | 一种btk激酶抑制剂的结晶形式及其制备方法 |
| SG11201811255WA (en) | 2016-06-29 | 2019-01-30 | Principia Biopharma Inc | Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| CN115209899A (zh) | 2019-10-14 | 2022-10-18 | 普林斯匹亚生物制药公司 | 通过施用(R)-2-[3-[4-氨基-3-(2-氟-4-苯氧基-苯基)吡唑并[3,4-d]嘧啶-1-基]哌啶-1-羰基]-4-甲基-4-[4-(氧杂环丁-3-基)哌嗪-1-基]戊-2-烯腈治疗免疫性血小板减少症的方法 |
| MX2022009009A (es) | 2020-01-22 | 2022-08-15 | Principia Biopharma Inc | Formas cristalinas de 2-[3-[4-amino-3-(2-fluoro-4-fenoxi-fenil)-1h -pirazolo[3,4-d]pirimidin-1-il]piperidin-1-carbonil]-4-metil-4-[4 -(oxetan-3-il)piperazin-1-il]pent-2-enonitrilo. |
| CN111205232B (zh) * | 2020-02-26 | 2022-07-01 | 浙江天宇药业股份有限公司 | 一种替格瑞洛中间体的合成方法 |
| TW202307005A (zh) | 2021-05-28 | 2023-02-16 | 美商邊際分析公司 | 以核醣體蛋白質S6激酶α-1 (RSK1)及核醣體蛋白質S6激酶α-3 (RSK2)之調節劑治療神經病症之方法 |
| CN116332996B (zh) * | 2023-05-04 | 2025-04-01 | 南京颐媛生物医学研究院有限公司 | L-呋喃核糖型抗冠状病毒化合物及其制备方法和应用 |
| CN116410228B (zh) * | 2023-05-04 | 2025-10-31 | 南京颐媛生物医学研究院有限公司 | 一种抗冠状病毒核苷类化合物的制备方法及其应用 |
| CN116284135B (zh) * | 2023-05-04 | 2025-03-21 | 南京颐媛生物医学研究院有限公司 | 抗冠状病毒核苷类化合物的制备方法及其应用 |
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| US4444770A (en) * | 1980-05-29 | 1984-04-24 | Bayer Aktiengesellschaft | New imidazoazole-alkenoic acid amide compounds, intermediate products for their production, their production, and their medicinal use |
| DE3216416A1 (de) * | 1982-05-03 | 1983-11-03 | Bayer Ag, 5090 Leverkusen | Heteroarylthiovinyl-verbindungen, ein verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel |
| US4911920A (en) | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
| DE3502264A1 (de) * | 1985-01-24 | 1986-07-24 | Bayer Ag, 5090 Leverkusen | Imidazoalkensaeurederivate, ein verfahren zu ihrer herstellung und ihre verwendung fuer die herstellung pharmazeutischer wirkstoffe |
| FR2588189B1 (fr) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
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| WO2008005954A2 (en) * | 2006-06-30 | 2008-01-10 | The Board Of Regents Of The University Of Texas System | Tryphostin-analogs for the treatment of cell proliferative diseases |
| JP5600004B2 (ja) * | 2006-09-05 | 2014-10-01 | エモリー ユニバーシティー | 感染の予防または治療のためのチロシンキナーゼ阻害剤 |
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2010
- 2010-11-16 MX MX2012005678A patent/MX2012005678A/es not_active Application Discontinuation
- 2010-11-16 US US13/510,272 patent/US20130035325A1/en not_active Abandoned
- 2010-11-16 CN CN2010800615701A patent/CN102711765A/zh active Pending
- 2010-11-16 EP EP10830919.6A patent/EP2558099A4/en not_active Withdrawn
- 2010-11-16 JP JP2012539076A patent/JP2013510886A/ja active Pending
- 2010-11-16 WO PCT/US2010/056890 patent/WO2011060440A2/en not_active Ceased
- 2010-11-16 CA CA2781056A patent/CA2781056A1/en not_active Abandoned
- 2010-11-16 AU AU2010319964A patent/AU2010319964A1/en not_active Abandoned
- 2010-11-16 BR BR112012011528A patent/BR112012011528A2/pt not_active IP Right Cessation
-
2014
- 2014-08-18 US US14/462,158 patent/US9505766B2/en active Active
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11524968B2 (en) | 2017-10-18 | 2022-12-13 | Hk Inno.N Corporation | Heterocyclic compound as a protein kinase inhibitor |
| US12180185B2 (en) | 2018-11-15 | 2024-12-31 | Hk Inno.N Corporation | Compound as protein kinase inhibitor, and pharmaceutical composition comprising thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2010319964A1 (en) | 2012-06-07 |
| US9505766B2 (en) | 2016-11-29 |
| CN102711765A (zh) | 2012-10-03 |
| US20130035325A1 (en) | 2013-02-07 |
| WO2011060440A2 (en) | 2011-05-19 |
| JP2013510886A (ja) | 2013-03-28 |
| WO2011060440A3 (en) | 2011-11-03 |
| EP2558099A2 (en) | 2013-02-20 |
| EP2558099A4 (en) | 2013-07-17 |
| US20150045343A1 (en) | 2015-02-12 |
| MX2012005678A (es) | 2012-09-07 |
| BR112012011528A2 (pt) | 2019-09-24 |
| AU2010319964A2 (en) | 2012-08-02 |
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