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 (enExample) | 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 (enExample) |
| EP (1) | EP2758402B9 (enExample) |
| JP (1) | JP5914667B2 (enExample) |
| KR (1) | KR20140059246A (enExample) |
| CN (1) | CN103814030A (enExample) |
| AP (1) | AP2014007475A0 (enExample) |
| AR (1) | AR088760A1 (enExample) |
| AU (1) | AU2012311184A1 (enExample) |
| BR (1) | BR112014006840A2 (enExample) |
| CA (1) | CA2847540C (enExample) |
| CL (2) | CL2014002726A1 (enExample) |
| CO (1) | CO6910196A2 (enExample) |
| CR (1) | CR20140132A (enExample) |
| DO (1) | DOP2014000055A (enExample) |
| EA (1) | EA201490673A1 (enExample) |
| ES (1) | ES2575710T3 (enExample) |
| IL (1) | IL231592A0 (enExample) |
| MA (1) | MA35451B1 (enExample) |
| MD (1) | MD20140023A2 (enExample) |
| MX (1) | MX2014003501A (enExample) |
| NI (1) | NI201400023A (enExample) |
| PE (1) | PE20141228A1 (enExample) |
| PH (1) | PH12014500638A1 (enExample) |
| SG (1) | SG2014014450A (enExample) |
| TN (1) | TN2014000115A1 (enExample) |
| TW (1) | TWI492946B (enExample) |
| UA (1) | UA110259C2 (enExample) |
| UY (1) | UY34342A (enExample) |
| WO (1) | WO2013042006A1 (enExample) |
Families Citing this family (55)
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| WO2011146313A1 (en) | 2010-05-19 | 2011-11-24 | The University Of North Carolina At Chapel Hill | Pyrazolopyrimidine compounds for the treatment of cancer |
| DK2975042T3 (en) * | 2010-06-23 | 2019-01-21 | Hanmi Science Co Ltd | Novel fused pyrimidine derivatives to inhibit tyrosine kinase activity |
| WO2012151561A1 (en) | 2011-05-04 | 2012-11-08 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| AU2012318896B2 (en) * | 2011-10-03 | 2017-03-02 | The University Of North Carolina At Chapel Hill | Pyrrolopyrimidine compounds for the treatment of cancer |
| JP6469567B2 (ja) | 2012-05-05 | 2019-02-13 | アリアド・ファーマシューティカルズ・インコーポレイテッド | Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物 |
| US9567326B2 (en) | 2012-05-22 | 2017-02-14 | The University Of North Carolina At Chapel Hill | Pyrimidine compounds for the treatment of cancer |
| WO2014062774A1 (en) | 2012-10-17 | 2014-04-24 | 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 |
| AU2014207641A1 (en) * | 2013-01-16 | 2015-08-06 | Signal Pharmaceuticals, Llc | Substituted Pyrrolopyrimidine Compounds, compositions thereof, and methods of treatment therewith |
| KR20150119210A (ko) * | 2013-03-14 | 2015-10-23 | 화이자 인코포레이티드 | 비소세포 폐암의 치료를 위한 egfr t790m 억제제와 egfr 억제제의 조합 |
| 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 |
| BR112016005881A2 (pt) * | 2013-09-18 | 2017-09-12 | Beijing Hanmi Pharmaceutical Co Ltd | composto, composição farmacêutica e uso do composto |
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| UA115388C2 (uk) * | 2013-11-21 | 2017-10-25 | Пфайзер Інк. | 2,6-заміщені пуринові похідні та їх застосування в лікуванні проліферативних захворювань |
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| US20150291606A1 (en) | 2014-04-11 | 2015-10-15 | The University Of North Carolina At Chapel Hill | Mertk-specific pyrrolopyrimidine compounds |
| US10144737B2 (en) | 2014-05-19 | 2018-12-04 | Jiangsu Hengrui Medicine Co., Ltd. | 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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| JP6854762B2 (ja) | 2014-12-23 | 2021-04-07 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | サイクリン依存性キナーゼ７（ｃｄｋ７）の阻害剤 |
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| AU2016243529B2 (en) * | 2015-03-27 | 2021-03-25 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
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| 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 |
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| KR102577241B1 (ko) * | 2017-12-28 | 2023-09-11 | 주식회사 대웅제약 | 카이네이즈 저해제로서의 아미노-플루오로피페리딘 유도체 |
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- 2012-09-10 WO PCT/IB2012/054702 patent/WO2013042006A1/en not_active Ceased
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- 2012-09-10 PE PE2014000403A patent/PE20141228A1/es not_active Application Discontinuation
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