JP2014526549A5 - - Google Patents
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- JP2014526549A5 JP2014526549A5 JP2014531341A JP2014531341A JP2014526549A5 JP 2014526549 A5 JP2014526549 A5 JP 2014526549A5 JP 2014531341 A JP2014531341 A JP 2014531341A JP 2014531341 A JP2014531341 A JP 2014531341A JP 2014526549 A5 JP2014526549 A5 JP 2014526549A5
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- Prior art keywords
- alkyl
- compound
- methyl
- salt according
- ring
- 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.)
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- 150000003839 salts Chemical class 0.000 claims 21
- 125000000217 alkyl group Chemical group 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 18
- 125000003545 alkoxy group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 7
- -1 cyano, difluoromethyl Chemical group 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000006584 (C3-C10) heterocycloalkyl group Chemical group 0.000 claims 1
- FESKVIPHVGGMNZ-MFKMUULPSA-N 1-[(3r,4r)-3-[[5-chloro-2-[(1-methylpyrazol-4-yl)amino]-7h-pyrrolo[2,3-d]pyrimidin-4-yl]oxymethyl]-4-fluoropyrrolidin-1-yl]prop-2-en-1-one Chemical compound C1=NN(C)C=C1NC1=NC(OC[C@@H]2[C@H](CN(C2)C(=O)C=C)F)=C(C(Cl)=CN2)C2=N1 FESKVIPHVGGMNZ-MFKMUULPSA-N 0.000 claims 1
- ODMXWZROLKITMS-RISCZKNCSA-N 1-[(3r,4r)-3-[[5-chloro-2-[(1-methylpyrazol-4-yl)amino]-7h-pyrrolo[2,3-d]pyrimidin-4-yl]oxymethyl]-4-methoxypyrrolidin-1-yl]prop-2-en-1-one Chemical compound CO[C@H]1CN(C(=O)C=C)C[C@@H]1COC1=NC(NC2=CN(C)N=C2)=NC2=C1C(Cl)=CN2 ODMXWZROLKITMS-RISCZKNCSA-N 0.000 claims 1
- SXHNYSZARHNXML-JQWIXIFHSA-N 1-[(3r,4s)-3-[[5-chloro-2-[(1-methylpyrazol-4-yl)amino]-7h-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-4-(trifluoromethyl)pyrrolidin-1-yl]prop-2-en-1-one Chemical compound C1=NN(C)C=C1NC1=NC(N[C@@H]2[C@H](CN(C2)C(=O)C=C)C(F)(F)F)=C(C(Cl)=CN2)C2=N1 SXHNYSZARHNXML-JQWIXIFHSA-N 0.000 claims 1
- MKJVMRBTYPHRMX-UONOGXRCSA-N 1-[(3s,4r)-3-[[5-chloro-2-[(1-methylpyrazol-4-yl)amino]-7h-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-4-(triazol-1-yl)pyrrolidin-1-yl]prop-2-en-1-one Chemical compound C1=NN(C)C=C1NC1=NC(N[C@@H]2[C@@H](CN(C2)C(=O)C=C)N2N=NC=C2)=C(C(Cl)=CN2)C2=N1 MKJVMRBTYPHRMX-UONOGXRCSA-N 0.000 claims 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- HGINCPLSRVDWNT-UHFFFAOYSA-N Acrolein Chemical compound C=CC=O HGINCPLSRVDWNT-UHFFFAOYSA-N 0.000 claims 1
- LKVQXJRVWLXFLH-WKILWMFISA-N C1[C@@H](N(C)C(=O)C=C)C[C@@H]1OC1=NC(NC=2C(=NN(C)C=2)C)=NC2=C1C(C=1N=CC=CC=1)=CN2 Chemical compound C1[C@@H](N(C)C(=O)C=C)C[C@@H]1OC1=NC(NC=2C(=NN(C)C=2)C)=NC2=C1C(C=1N=CC=CC=1)=CN2 LKVQXJRVWLXFLH-WKILWMFISA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 230000010261 cell growth Effects 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- IKXHZNFGPFFALI-UHFFFAOYSA-N n-[3-[[5-(1-methylpyrazol-4-yl)-2-[(1-methylpyrazol-4-yl)amino]-7h-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenyl]prop-2-enamide Chemical compound C1=NN(C)C=C1NC1=NC(OC=2C=C(NC(=O)C=C)C=CC=2)=C(C(=CN2)C3=CN(C)N=C3)C2=N1 IKXHZNFGPFFALI-UHFFFAOYSA-N 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- GJVFBWCTGUSGDD-UHFFFAOYSA-L pentamethonium bromide Chemical compound [Br-].[Br-].C[N+](C)(C)CCCCC[N+](C)(C)C GJVFBWCTGUSGDD-UHFFFAOYSA-L 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161538103P | 2011-09-22 | 2011-09-22 | |
| US61/538,103 | 2011-09-22 | ||
| US201261639639P | 2012-04-27 | 2012-04-27 | |
| US61/639,639 | 2012-04-27 | ||
| PCT/IB2012/054702 WO2013042006A1 (en) | 2011-09-22 | 2012-09-10 | Pyrrolopyrimidine and purine derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014526549A JP2014526549A (ja) | 2014-10-06 |
| JP2014526549A5 true JP2014526549A5 (OSRAM) | 2015-10-29 |
| JP5914667B2 JP5914667B2 (ja) | 2016-05-11 |
Family
ID=47116127
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014531341A Active JP5914667B2 (ja) | 2011-09-22 | 2012-09-10 | ピロロピリミジンおよびプリン誘導体 |
Country Status (29)
| Country | Link |
|---|---|
| US (2) | US9040547B2 (OSRAM) |
| EP (1) | EP2758402B9 (OSRAM) |
| JP (1) | JP5914667B2 (OSRAM) |
| KR (1) | KR20140059246A (OSRAM) |
| CN (1) | CN103814030A (OSRAM) |
| AP (1) | AP2014007475A0 (OSRAM) |
| AR (1) | AR088760A1 (OSRAM) |
| AU (1) | AU2012311184A1 (OSRAM) |
| BR (1) | BR112014006840A2 (OSRAM) |
| CA (1) | CA2847540C (OSRAM) |
| CL (2) | CL2014000566A1 (OSRAM) |
| CO (1) | CO6910196A2 (OSRAM) |
| CR (1) | CR20140132A (OSRAM) |
| DO (1) | DOP2014000055A (OSRAM) |
| EA (1) | EA201490673A1 (OSRAM) |
| ES (1) | ES2575710T3 (OSRAM) |
| IL (1) | IL231592A0 (OSRAM) |
| MA (1) | MA35451B1 (OSRAM) |
| MD (1) | MD20140023A2 (OSRAM) |
| MX (1) | MX2014003501A (OSRAM) |
| NI (1) | NI201400023A (OSRAM) |
| PE (1) | PE20141228A1 (OSRAM) |
| PH (1) | PH12014500638A1 (OSRAM) |
| SG (1) | SG2014014450A (OSRAM) |
| TN (1) | TN2014000115A1 (OSRAM) |
| TW (1) | TWI492946B (OSRAM) |
| UA (1) | UA110259C2 (OSRAM) |
| UY (1) | UY34342A (OSRAM) |
| WO (1) | WO2013042006A1 (OSRAM) |
Families Citing this family (55)
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| PT2300013T (pt) | 2008-05-21 | 2017-10-31 | Ariad Pharma Inc | Derivados de fósforo como inibidores de cinases |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| WO2011146313A1 (en) | 2010-05-19 | 2011-11-24 | The University Of North Carolina At Chapel Hill | Pyrazolopyrimidine compounds for the treatment of cancer |
| CA2803056C (en) * | 2010-06-23 | 2017-05-16 | Hanmi Science Co., Ltd. | Fused pyrimidine derivatives for inhibition of tyrosine kinase activity |
| EP2704572B1 (en) | 2011-05-04 | 2015-12-30 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| BR112014007788A2 (pt) | 2011-10-03 | 2017-04-18 | Univ North Carolina Chapel Hill | compostos de pirrolopirimidina para tratamento do câncer |
| AU2013204563B2 (en) | 2012-05-05 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| MX2014013632A (es) | 2012-05-22 | 2015-02-05 | Univ North Carolina | Compuestos de pirimidina para el tratamiento de cancer. |
| US9562047B2 (en) | 2012-10-17 | 2017-02-07 | The University Of North Carolina At Chapel Hill | Pyrazolopyrimidine compounds for the treatment of cancer |
| WO2014085225A1 (en) | 2012-11-27 | 2014-06-05 | The University Of North Carolina At Chapel Hill | Pyrimidine compounds for the treatment of cancer |
| WO2017156493A1 (en) | 2016-03-11 | 2017-09-14 | Denali Therapeutics Inc. | Compounds, compositions, and methods |
| EP2945636B1 (en) | 2013-01-16 | 2017-06-28 | Signal Pharmaceuticals, LLC | Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith |
| BR112015023020A2 (pt) * | 2013-03-14 | 2017-07-18 | Pfizer | combinação de inibidor de egfr t790m e inibidor de egfr para o tratamento de câncer pulmonar de células não-pequenas |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| KR101657616B1 (ko) * | 2013-05-24 | 2016-09-19 | 주식회사유한양행 | 피리미딘 고리를 포함하는 바이사이클릭 유도체 및 그의 제조방법 |
| CN104311573B (zh) * | 2013-09-18 | 2017-12-15 | 北京韩美药品有限公司 | 抑制btk和/或jak3激酶活性的化合物 |
| CN104513229A (zh) * | 2013-09-28 | 2015-04-15 | 正大天晴药业集团股份有限公司 | 喹唑啉衍生物及其制备方法 |
| UA115388C2 (uk) * | 2013-11-21 | 2017-10-25 | Пфайзер Інк. | 2,6-заміщені пуринові похідні та їх застосування в лікуванні проліферативних захворювань |
| KR20160106622A (ko) | 2014-01-29 | 2016-09-12 | 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 | 화합물 |
| JP6474826B2 (ja) | 2014-01-29 | 2019-02-27 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | 化合物 |
| US20170137426A1 (en) * | 2014-03-28 | 2017-05-18 | Changzhou Jiekai Pharmatech Co., Ltd. | Heterocyclic compounds as axl inhibitors |
| US9603850B2 (en) | 2014-04-11 | 2017-03-28 | The University Of North Carolina At Chapel Hill | MerTK-specific pyrazolopyrimidine compounds |
| WO2015178955A1 (en) * | 2014-05-19 | 2015-11-26 | Eternity Bioscience Inc. | Substituted ethynyl heterobicyclic compounds as tyrosine kinase inhibitors |
| NZ629796A (en) * | 2014-07-14 | 2015-12-24 | Signal Pharm Llc | Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use |
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| CN105524068B (zh) | 2014-09-30 | 2017-11-24 | 上海海雁医药科技有限公司 | 氮杂双环衍生物、其制法与医药上的用途 |
| CN105085489B (zh) | 2014-11-05 | 2019-03-01 | 益方生物科技（上海）有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| EP3236959B1 (en) | 2014-12-23 | 2025-09-24 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| JP6704422B2 (ja) | 2015-03-20 | 2020-06-03 | チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッドChia Tai Tianqing Pharmaceutical Group Co., Ltd. | キナゾリン誘導体の塩およびその製造方法 |
| CA2978518C (en) * | 2015-03-27 | 2023-11-21 | Nathanael S. Gray | Inhibitors of cyclin-dependent kinases |
| CN112932416A (zh) | 2015-06-04 | 2021-06-11 | 松下知识产权经营株式会社 | 生物体信息检测装置及生物体信息检测方法 |
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| CN114656446A (zh) * | 2015-11-25 | 2022-06-24 | R.J.雷诺兹烟草公司 | 烟碱盐、共晶体和盐共晶体配合物 |
| US10709708B2 (en) | 2016-03-17 | 2020-07-14 | The University Of North Carolina At Chapel Hill | Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor |
| PE20190395A1 (es) | 2016-06-16 | 2019-03-13 | Denali Therapeutics Inc | Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos |
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| US11208412B2 (en) | 2017-02-22 | 2021-12-28 | Daegu-Gyeongbuk Medical Innovation Foundation | Pyrrolo-pyrimidine derivative compound, preparation method therefor, and pharmaceutical composition comprising same compound as effective ingredient for preventing or treating protein kinase-related disease |
| KR102398659B1 (ko) | 2017-03-17 | 2022-05-16 | 주식회사 대웅제약 | 카이네이즈 저해제로서의 피롤로트리아진 유도체 |
| US10807951B2 (en) | 2017-10-13 | 2020-10-20 | The Regents Of The University Of California | mTORC1 modulators |
| CN111433208B (zh) * | 2017-12-05 | 2023-06-30 | 奥斯考泰克公司 | 作为lrrk2抑制剂的吡咯并(吡唑并)嘧啶衍生物 |
| PE20201146A1 (es) * | 2017-12-28 | 2020-10-26 | Dae Woong Pharma | Derivado de oxi-fluoropiperidina como inhibidor de quinasa |
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| KR102377007B1 (ko) * | 2018-09-20 | 2022-03-22 | 한미약품 주식회사 | 상피세포 성장인자 수용체 돌연변이 저해 효과를 갖는 신규 융합 피리미딘 골격 설폰아마이드 유도체 |
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| WO2021147952A1 (zh) * | 2020-01-21 | 2021-07-29 | 江苏先声药业有限公司 | 嘧啶并吡咯类化合物 |
| CN115244055B (zh) * | 2020-01-21 | 2024-09-03 | 江苏先声药业有限公司 | 嘧啶并五元环类衍生物及其应用 |
| WO2022062601A1 (zh) * | 2020-09-22 | 2022-03-31 | 江苏先声药业有限公司 | 嘧啶并吡咯类化合物 |
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| WO2023041071A1 (zh) * | 2021-09-18 | 2023-03-23 | 山东新时代药业有限公司 | 一种egfr抑制剂及其制备方法和用途 |
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2012
- 2012-09-10 CN CN201280045991.4A patent/CN103814030A/zh active Pending
- 2012-09-10 AU AU2012311184A patent/AU2012311184A1/en not_active Abandoned
- 2012-09-10 EA EA201490673A patent/EA201490673A1/ru unknown
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- 2012-09-10 JP JP2014531341A patent/JP5914667B2/ja active Active
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- 2012-09-10 PH PH1/2014/500638A patent/PH12014500638A1/en unknown
- 2012-09-10 WO PCT/IB2012/054702 patent/WO2013042006A1/en not_active Ceased
- 2012-09-10 UA UAA201402828A patent/UA110259C2/uk unknown
- 2012-09-10 KR KR20147007254A patent/KR20140059246A/ko not_active Ceased
- 2012-09-10 PE PE2014000403A patent/PE20141228A1/es not_active Application Discontinuation
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- 2012-09-10 BR BR112014006840A patent/BR112014006840A2/pt not_active IP Right Cessation
- 2012-09-10 MX MX2014003501A patent/MX2014003501A/es not_active Application Discontinuation
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