JP2013513613A5 - - Google Patents
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- Publication number
- JP2013513613A5 JP2013513613A5 JP2012543295A JP2012543295A JP2013513613A5 JP 2013513613 A5 JP2013513613 A5 JP 2013513613A5 JP 2012543295 A JP2012543295 A JP 2012543295A JP 2012543295 A JP2012543295 A JP 2012543295A JP 2013513613 A5 JP2013513613 A5 JP 2013513613A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently selected
- haloalkyl
- halo
- heteroaryl
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 98
- 150000001875 compounds Chemical class 0.000 claims description 48
- 125000001188 haloalkyl group Chemical group 0.000 claims description 46
- 125000001475 halogen functional group Chemical group 0.000 claims description 44
- 125000000623 heterocyclic group Chemical group 0.000 claims description 38
- 229910052799 carbon Inorganic materials 0.000 claims description 37
- 125000003118 aryl group Chemical group 0.000 claims description 32
- 125000001072 heteroaryl group Chemical group 0.000 claims description 32
- 229910052739 hydrogen Inorganic materials 0.000 claims description 24
- 239000001257 hydrogen Substances 0.000 claims description 24
- 150000001721 carbon Chemical group 0.000 claims description 21
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 20
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 19
- 125000003342 alkenyl group Chemical group 0.000 claims description 18
- -1 and —OR a Chemical group 0.000 claims description 17
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 16
- 125000002252 acyl group Chemical group 0.000 claims description 14
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 14
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 14
- 125000003545 alkoxy group Chemical group 0.000 claims description 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 12
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 12
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 12
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 12
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 12
- 206010028980 Neoplasm Diseases 0.000 claims description 10
- 201000011510 cancer Diseases 0.000 claims description 10
- 125000005055 alkyl alkoxy group Chemical group 0.000 claims description 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 7
- 102100039905 Isocitrate dehydrogenase [NADP] cytoplasmic Human genes 0.000 claims description 6
- 125000000304 alkynyl group Chemical group 0.000 claims description 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 101710102690 Isocitrate dehydrogenase [NADP] cytoplasmic Proteins 0.000 claims description 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 4
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 4
- 238000012544 monitoring process Methods 0.000 claims description 4
- 230000035772 mutation Effects 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 239000001301 oxygen Substances 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 3
- 108700028369 Alleles Proteins 0.000 claims description 2
- 101001042041 Bos taurus Isocitrate dehydrogenase [NAD] subunit beta, mitochondrial Proteins 0.000 claims description 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 2
- 101000960234 Homo sapiens Isocitrate dehydrogenase [NADP] cytoplasmic Proteins 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000011737 fluorine Chemical group 0.000 claims description 2
- 229910052731 fluorine Inorganic materials 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 12
- 239000000203 mixture Substances 0.000 claims 7
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 description 11
- 238000000034 method Methods 0.000 description 7
- 0 BC(C(*=C(****)*=*)=C(CC)CC)(N1C(C)(C)CC(C)(C)CN(*)C(C)(C)CC(C)(C)C1)BrC Chemical compound BC(C(*=C(****)*=*)=C(CC)CC)(N1C(C)(C)CC(C)(C)CN(*)C(C)(C)CC(C)(C)C1)BrC 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 description 1
- 125000005151 nonafluorobutanesulfonyl group Chemical group FC(C(C(S(=O)(=O)*)(F)F)(F)F)(C(F)(F)F)F 0.000 description 1
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28512209P | 2009-12-09 | 2009-12-09 | |
| US61/285,122 | 2009-12-09 | ||
| US31353210P | 2010-03-12 | 2010-03-12 | |
| US61/313,532 | 2010-03-12 | ||
| PCT/US2010/059778 WO2011072174A1 (en) | 2009-12-09 | 2010-12-09 | Therapeutically active compounds for use in the treatment of cancer characterized as having an idh mutation |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015113075A Division JP2015193633A (ja) | 2009-12-09 | 2015-06-03 | Ｉｄｈ変異体をもつことを特徴とする癌治療用の治療的活性化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013513613A JP2013513613A (ja) | 2013-04-22 |
| JP2013513613A5 true JP2013513613A5 (OSRAM) | 2014-01-30 |
| JP5967827B2 JP5967827B2 (ja) | 2016-08-10 |
Family
ID=43638711
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012543295A Expired - Fee Related JP5967827B2 (ja) | 2009-12-09 | 2010-12-09 | Ｉｄｈ変異体をもつことを特徴とする癌治療用の治療的活性化合物 |
| JP2015113075A Withdrawn JP2015193633A (ja) | 2009-12-09 | 2015-06-03 | Ｉｄｈ変異体をもつことを特徴とする癌治療用の治療的活性化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015113075A Withdrawn JP2015193633A (ja) | 2009-12-09 | 2015-06-03 | Ｉｄｈ変異体をもつことを特徴とする癌治療用の治療的活性化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US20130035329A1 (OSRAM) |
| EP (1) | EP2509600B1 (OSRAM) |
| JP (2) | JP5967827B2 (OSRAM) |
| ES (1) | ES2642109T3 (OSRAM) |
| WO (1) | WO2011072174A1 (OSRAM) |
Families Citing this family (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2406389B1 (en) | 2009-03-13 | 2019-05-08 | Agios Pharmaceuticals, Inc. | Methods and compositions for cell-proliferation-related disorders |
| EP2417123A2 (en) | 2009-04-06 | 2012-02-15 | Agios Pharmaceuticals, Inc. | Therapeutic compositions and related methods of use |
| EP2448581B1 (en) | 2009-06-29 | 2016-12-07 | Agios Pharmaceuticals, Inc. | Therapeutic compositions and related methods of use |
| CA2944788C (en) | 2009-06-29 | 2023-08-22 | Agios Pharmaceuticals, Inc. | Compounds, and compositions thereof, which modulate pyruvate kinase m2, and methods of making same |
| CA2793835C (en) | 2009-10-21 | 2021-07-20 | Agios Pharmaceuticals, Inc. | Methods and compositions for cell-proliferation-related disorders |
| WO2011050211A2 (en) | 2009-10-21 | 2011-04-28 | Agios Pharmaceuticals, Inc. | Methods and compositions for cell-proliferation-related disorders |
| JP5837091B2 (ja) | 2010-12-17 | 2015-12-24 | アジオス ファーマシューティカルズ， インコーポレイテッド | ピルビン酸キナーゼｍ２（ｐｋｍ２）調節剤としての新規ｎ−（４−（アゼチジン−１−カルボニル）フェニル）−（ヘテロ−）アリールスルホンアミド誘導体 |
| JP6092118B2 (ja) | 2010-12-21 | 2017-03-08 | アジオス ファーマシューティカルズ， インコーポレイテッド | ニ環式ｐｋｍ２活性化剤 |
| TWI549947B (zh) | 2010-12-29 | 2016-09-21 | 阿吉歐斯製藥公司 | 治療化合物及組成物 |
| KR101873543B1 (ko) | 2011-05-03 | 2018-07-02 | 아지오스 파마슈티컬스 아이엔씨. | 치료에 사용하기 위한 피루베이트 키나아제 활성제 |
| CN102827073A (zh) * | 2011-06-17 | 2012-12-19 | 安吉奥斯医药品有限公司 | 治疗活性组合物和它们的使用方法 |
| CN102827170A (zh) | 2011-06-17 | 2012-12-19 | 安吉奥斯医药品有限公司 | 治疗活性组合物和它们的使用方法 |
| JP6026544B2 (ja) | 2011-09-27 | 2016-11-16 | ノバルティス アーゲー | 変異体ｉｄｈの阻害剤としての３−ピリミジン−４−イル−オキサゾリジン−２−オン類 |
| SG11201403878QA (en) | 2012-01-06 | 2014-08-28 | Agios Pharmaceuticals Inc | Therapeutically active compounds and their methods of use |
| US9474779B2 (en) * | 2012-01-19 | 2016-10-25 | Agios Pharmaceuticals, Inc. | Therapeutically active compositions and their methods of use |
| UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
| HK1213798A1 (zh) | 2012-10-15 | 2016-07-15 | 安吉奥斯医药品有限公司 | 治療性化合物和組合物 |
| US9296733B2 (en) | 2012-11-12 | 2016-03-29 | Novartis Ag | Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases |
| HK1213251A1 (zh) * | 2013-03-14 | 2016-06-30 | Novartis Ag | 作为突变idh抑制剂的3-嘧啶-4-基-恶唑烷-2-酮化合物 |
| WO2014197835A2 (en) | 2013-06-06 | 2014-12-11 | The General Hospital Corporation | Methods and compositions for the treatment of cancer |
| WO2015003355A2 (en) * | 2013-07-11 | 2015-01-15 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and their methods of use |
| WO2015003360A2 (en) | 2013-07-11 | 2015-01-15 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and their methods of use |
| CA2917671A1 (en) | 2013-07-11 | 2015-01-15 | Agios Pharmaceuticals, Inc. | 2,4-or 4,6-diaminopyrimidine compounds as idh2 mutants inhibitors for the treatment of cancer |
| NZ715738A (en) | 2013-07-11 | 2021-06-25 | Agios Pharmaceuticals Inc | N,6-bis(aryl or heteroaryl)-1,3,5-triazine-2,4-diamine compounds as idh2 mutants inhibitors for the treatment of cancer |
| US9579324B2 (en) | 2013-07-11 | 2017-02-28 | Agios Pharmaceuticals, Inc | Therapeutically active compounds and their methods of use |
| US20150031627A1 (en) | 2013-07-25 | 2015-01-29 | Agios Pharmaceuticals, Inc | Therapeutically active compounds and their methods of use |
| NZ720092A (en) | 2013-12-05 | 2019-05-31 | Pfizer | Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides |
| US9951027B2 (en) | 2014-02-11 | 2018-04-24 | Bayer Pharma Aktiengesellschaft | Benzimidazol-2-amines as MIDH1 inhibitors |
| SG11201605810WA (en) | 2014-02-11 | 2016-08-30 | Bayer Pharma AG | Benzimidazol-2-amines as midh1 inhibitors |
| CA2942072C (en) | 2014-03-14 | 2022-07-26 | Agios Pharmaceuticals, Inc. | Pharmaceutical compositions and use of (s)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-( 4-cyanopyridin-2-yl)-n-( 5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide |
| WO2015169130A1 (zh) * | 2014-05-09 | 2015-11-12 | 上海科胜药物研发有限公司 | 新的沃替西汀中间体及其合成方法 |
| ES2768694T3 (es) | 2014-09-19 | 2020-06-23 | Forma Therapeutics Inc | Composiciones de quinolinona pirimidinas como inhibidores de isocitrato dehidrogenasa mutante |
| EP3194375B1 (en) * | 2014-09-19 | 2018-11-21 | Forma Therapeutics, Inc. | Phenyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| PT3733662T (pt) * | 2014-09-19 | 2023-08-18 | Forma Therapeutics Inc | Derivados piridin-2(1h)-ona-quinolinona como inibidores de isocitrato desidrogenase mutante |
| US9771349B2 (en) | 2014-09-19 | 2017-09-26 | Forma Therapeutics, Inc. | Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| WO2016106331A1 (en) | 2014-12-22 | 2016-06-30 | The United States Of America | Mutant idh1 inhibitors useful for treating cancer |
| US10294206B2 (en) | 2015-04-21 | 2019-05-21 | Forma Tm2, Inc. | Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| US9624216B2 (en) | 2015-04-21 | 2017-04-18 | Forma Therapeutics, Inc. | Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors |
| DK3307271T3 (da) | 2015-06-11 | 2023-10-09 | Agios Pharmaceuticals Inc | Fremgangsmåder til anvendelse af pyruvatkinase-aktivatorer |
| JP2018525413A (ja) * | 2015-08-24 | 2018-09-06 | ザ メソディスト ホスピタル | ユーイングファミリー腫瘍を治療する組成物及び方法 |
| MA71411A (fr) | 2015-10-15 | 2025-04-30 | Les Laboratoires Servier | Polythérapie pour le traitement de tumeurs malignes |
| DK3362066T3 (da) | 2015-10-15 | 2021-11-22 | Les Laboratoires Servier Sas | Kombinationsterapi til behandling af maligniteter |
| EP3397625A4 (en) * | 2015-12-30 | 2019-12-25 | Agios Pharmaceuticals, Inc. | TREATMENT OF TUMORS WITH MUTANT ISOCITRATE DEHYDROGENASE |
| WO2017153952A1 (en) * | 2016-03-10 | 2017-09-14 | Glaxosmithkline Intellectual Property Development Limited | 5-sulfamoyl-2-hydroxybenzamide derivatives |
| EP3444237B1 (en) * | 2016-03-22 | 2020-10-28 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Iridinesulfonamide compound and use method thereof |
| IL270066B2 (en) * | 2017-04-24 | 2023-10-01 | Aurigene Oncology Ltd | Methods of use for trisubstituted benzotriazole derivatives as dihydroorotate oxygenase inhibitors |
| US20180369206A1 (en) | 2017-04-24 | 2018-12-27 | Aurigene Discovery Technologies Limited | Methods of Use for Trisubstituted Benzotriazole Derivatives as Dihydroorotate Oxygenase Inhibitors |
| CN109897044A (zh) * | 2017-12-07 | 2019-06-18 | 北京大学 | 抗神经病理性疼痛化合物及其制备方法 |
| KR102861339B1 (ko) | 2018-02-20 | 2025-09-19 | 르 라보레또레 쎄르비에르 | 삼치환 벤조트리아졸 유도체의 사용 방법 |
| US11311527B2 (en) | 2018-05-16 | 2022-04-26 | Forma Therapeutics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-1) |
| US10532047B2 (en) | 2018-05-16 | 2020-01-14 | Forma Therapeutics, Inc. | Solid forms of ((S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile |
| EP3720442B1 (en) | 2018-05-16 | 2022-12-28 | Forma Therapeutics, Inc. | Inhibiting mutant idh-1 |
| US11013734B2 (en) | 2018-05-16 | 2021-05-25 | Forma Therapeutics, Inc. | Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation |
| US11013733B2 (en) | 2018-05-16 | 2021-05-25 | Forma Therapeutics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mlDH-1) |
| CN108822082B (zh) * | 2018-06-06 | 2020-11-03 | 青岛科技大学 | 一种含氟吡啶哌嗪酰胺类化合物及其应用 |
| US10980788B2 (en) | 2018-06-08 | 2021-04-20 | Agios Pharmaceuticals, Inc. | Therapy for treating malignancies |
| CN114685399A (zh) * | 2022-04-26 | 2022-07-01 | 河北广祥制药有限公司 | 一种乌拉地尔中间体1-(2-甲氧基苯基)哌嗪及其盐的制备方法 |
| CN116425653A (zh) * | 2023-03-22 | 2023-07-14 | 烟台盛凯伦化学科技有限公司 | 一种n,n’-二(对乙氧基苯基)-1,4-苯二甲亚胺的制备方法 |
| AU2024271540A1 (en) * | 2023-05-18 | 2025-11-27 | Concarlo Therapeutics, Inc. | Small molecule inhibitors of p27 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2735127B1 (fr) * | 1995-06-09 | 1997-08-22 | Pf Medicament | Nouvelles piperazines heteroaromatiques utiles comme medicaments. |
| GB9602166D0 (en) * | 1996-02-02 | 1996-04-03 | Zeneca Ltd | Aminoheterocyclic derivatives |
| WO2004074438A2 (en) * | 2003-02-14 | 2004-09-02 | Smithkline Beecham Corporation | Ccr8 antagonists |
| WO2004073619A2 (en) * | 2003-02-14 | 2004-09-02 | Smithkline Beecham Corporation | Ccr8 antagonists |
| US20100160324A1 (en) * | 2004-12-30 | 2010-06-24 | Astex Therapeutics Limited | Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases |
| PL2176231T3 (pl) * | 2007-07-20 | 2017-04-28 | Nerviano Medical Sciences S.R.L. | Podstawione pochodne indazolu aktywne jako inhibitory kinazy |
| GB0722779D0 (en) | 2007-11-20 | 2008-01-02 | Sterix Ltd | Compound |
| EP2406389B1 (en) * | 2009-03-13 | 2019-05-08 | Agios Pharmaceuticals, Inc. | Methods and compositions for cell-proliferation-related disorders |
| CA2944788C (en) * | 2009-06-29 | 2023-08-22 | Agios Pharmaceuticals, Inc. | Compounds, and compositions thereof, which modulate pyruvate kinase m2, and methods of making same |
-
2010
- 2010-12-09 ES ES10796233.4T patent/ES2642109T3/es active Active
- 2010-12-09 JP JP2012543295A patent/JP5967827B2/ja not_active Expired - Fee Related
- 2010-12-09 WO PCT/US2010/059778 patent/WO2011072174A1/en not_active Ceased
- 2010-12-09 EP EP10796233.4A patent/EP2509600B1/en active Active
-
2012
- 2012-06-08 US US13/492,159 patent/US20130035329A1/en not_active Abandoned
-
2015
- 2015-06-03 JP JP2015113075A patent/JP2015193633A/ja not_active Withdrawn
-
2016
- 2016-12-13 US US15/377,485 patent/US20170166541A1/en not_active Abandoned
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