JP2013527175A5 - - Google Patents
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- Publication number
- JP2013527175A5 JP2013527175A5 JP2013510173A JP2013510173A JP2013527175A5 JP 2013527175 A5 JP2013527175 A5 JP 2013527175A5 JP 2013510173 A JP2013510173 A JP 2013510173A JP 2013510173 A JP2013510173 A JP 2013510173A JP 2013527175 A5 JP2013527175 A5 JP 2013527175A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- stereoisomer
- alkyl
- acceptable salt
- mixture
- 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
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 134
- 150000003839 salts Chemical class 0.000 claims description 122
- 150000001875 compounds Chemical class 0.000 claims description 120
- 239000000203 mixture Substances 0.000 claims description 78
- 125000003118 aryl group Chemical group 0.000 claims description 46
- 125000002947 alkylene group Chemical group 0.000 claims description 40
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 36
- -1 2,3-dihydrobenzofuranyl Chemical group 0.000 claims description 32
- 206010028980 Neoplasm Diseases 0.000 claims description 25
- 201000011510 cancer Diseases 0.000 claims description 25
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 21
- 102100033793 ALK tyrosine kinase receptor Human genes 0.000 claims description 20
- 108020001507 fusion proteins Proteins 0.000 claims description 20
- 102000037865 fusion proteins Human genes 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 20
- 125000005842 heteroatom Chemical group 0.000 claims description 18
- 239000008194 pharmaceutical composition Substances 0.000 claims description 17
- 229910052760 oxygen Inorganic materials 0.000 claims description 16
- 125000001424 substituent group Chemical group 0.000 claims description 16
- 125000000623 heterocyclic group Chemical group 0.000 claims description 14
- 229910052717 sulfur Inorganic materials 0.000 claims description 14
- 125000002619 bicyclic group Chemical group 0.000 claims description 12
- 125000004076 pyridyl group Chemical group 0.000 claims description 12
- 229920006395 saturated elastomer Polymers 0.000 claims description 12
- 125000004432 carbon atom Chemical group C* 0.000 claims description 10
- 125000001041 indolyl group Chemical group 0.000 claims description 10
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 10
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 10
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 8
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 8
- 125000002883 imidazolyl group Chemical group 0.000 claims description 8
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims description 8
- 125000001624 naphthyl group Chemical group 0.000 claims description 8
- 108700009251 p80(NPM-ALK) Proteins 0.000 claims description 8
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 8
- 125000000335 thiazolyl group Chemical group 0.000 claims description 8
- 229910052799 carbon Inorganic materials 0.000 claims description 6
- 125000005946 imidazo[1,2-a]pyridyl group Chemical group 0.000 claims description 6
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims description 6
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 6
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 6
- 125000000597 dioxinyl group Chemical group 0.000 claims description 5
- 230000002401 inhibitory effect Effects 0.000 claims description 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 4
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 4
- 125000002950 monocyclic group Chemical group 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 4
- 125000002971 oxazolyl group Chemical group 0.000 claims description 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 4
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 4
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 3
- 208000026310 Breast neoplasm Diseases 0.000 claims description 3
- 206010009944 Colon cancer Diseases 0.000 claims description 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 3
- 201000003803 Inflammatory myofibroblastic tumor Diseases 0.000 claims description 3
- 206010067917 Inflammatory myofibroblastic tumour Diseases 0.000 claims description 3
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims description 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 3
- 206010025323 Lymphomas Diseases 0.000 claims description 3
- 206010027406 Mesothelioma Diseases 0.000 claims description 3
- 206010029260 Neuroblastoma Diseases 0.000 claims description 3
- 206010033128 Ovarian cancer Diseases 0.000 claims description 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 3
- 208000009956 adenocarcinoma Diseases 0.000 claims description 3
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims description 3
- 208000005017 glioblastoma Diseases 0.000 claims description 3
- 201000008298 histiocytosis Diseases 0.000 claims description 3
- 201000005202 lung cancer Diseases 0.000 claims description 3
- 208000020816 lung neoplasm Diseases 0.000 claims description 3
- 201000001441 melanoma Diseases 0.000 claims description 3
- 230000009885 systemic effect Effects 0.000 claims description 3
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 239000008177 pharmaceutical agent Substances 0.000 claims 2
- 238000000034 method Methods 0.000 description 8
- 206010041067 Small cell lung cancer Diseases 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 208000000587 small cell lung carcinoma Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33362310P | 2010-05-11 | 2010-05-11 | |
| US61/333,623 | 2010-05-11 | ||
| PCT/US2011/035186 WO2011143033A1 (en) | 2010-05-11 | 2011-05-04 | Pyrimidine compounds that inhibit anaplastic lymphoma kinase |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013527175A JP2013527175A (ja) | 2013-06-27 |
| JP2013527175A5 true JP2013527175A5 (enExample) | 2014-06-26 |
| JP5797261B2 JP5797261B2 (ja) | 2015-10-21 |
Family
ID=44914649
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013510173A Expired - Fee Related JP5797261B2 (ja) | 2010-05-11 | 2011-05-04 | 未分化リンパ腫キナーゼを阻害するピリミジン化合物 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US8716281B2 (enExample) |
| EP (1) | EP2600874B1 (enExample) |
| JP (1) | JP5797261B2 (enExample) |
| AU (1) | AU2011253311B2 (enExample) |
| CA (1) | CA2799495A1 (enExample) |
| ES (1) | ES2538581T3 (enExample) |
| TW (1) | TWI513694B (enExample) |
| WO (1) | WO2011143033A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| CA2876689C (en) | 2012-06-13 | 2022-04-26 | Incyte Corporation | Substituted tricyclic compounds as fgfr inhibitors |
| EP2867233A1 (en) | 2012-07-03 | 2015-05-06 | Aurigene Discovery Technologies Limited | 3-(PYRAZOLYL)-1H-PYRROLO[2,3-b]PYRIDINE DERIVATIVES AS KINASE INHIBITORS |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| US9908887B2 (en) | 2012-12-21 | 2018-03-06 | Epizyme, Inc. | PRMT5 inhibitors and uses thereof |
| US9604930B2 (en) | 2012-12-21 | 2017-03-28 | Epizyme, Inc. | Tetrahydro- and dihydro-isoquinoline PRMT5 inhibitors and uses thereof |
| US9365555B2 (en) | 2012-12-21 | 2016-06-14 | Epizyme, Inc. | PRMT5 inhibitors and uses thereof |
| JP2016505002A (ja) | 2012-12-21 | 2016-02-18 | エピザイム，インコーポレイティド | ジヒドロイソキノリンまたはテトラヒドロイソキノリンを含有するｐｒｍｔ５阻害剤およびその使用 |
| US10118918B2 (en) | 2012-12-21 | 2018-11-06 | Epizyme, Inc. | PRMT5 inhibitors and uses thereof |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| US10205950B2 (en) * | 2014-02-21 | 2019-02-12 | Panasonic Corporation | Image decoding method, image encoding method, image decoding apparatus, and image encoding apparatus |
| US10000469B2 (en) | 2014-03-25 | 2018-06-19 | Duke University | Heat shock protein 70 (hsp-70) receptor ligands |
| AU2015301196A1 (en) | 2014-08-04 | 2017-01-12 | Epizyme, Inc. | PRMT5 inhibitors and uses thereof |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CA2976790C (en) | 2015-02-20 | 2024-02-27 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| RS66310B1 (sr) | 2018-05-04 | 2025-01-31 | Incyte Corp | Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu |
| KR102956194B1 (ko) | 2018-05-04 | 2026-04-23 | 인사이트 코포레이션 | Fgfr 억제제의 염 |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| CN110317176A (zh) * | 2019-07-04 | 2019-10-11 | 沈阳药科大学 | 2-氨基嘧啶类化合物及其用途 |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| GEP20247679B (en) | 2019-10-14 | 2024-10-10 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021113479A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| MX2022006691A (es) | 2019-12-04 | 2022-09-19 | Incyte Corp | Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr). |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| TW202313610A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之三環雜環 |
| CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5739127A (en) | 1996-11-08 | 1998-04-14 | Bayer Aktiengesellschaft | 2,4'-bridged bis-2,4-diaminoquinazolines |
| BR0015995A (pt) * | 1999-11-30 | 2002-08-06 | Pfizer Prod Inc | Compostos 2,4-diaminopirimidina úteis como imunossupressores |
| CA2396693A1 (en) * | 1999-12-28 | 2001-07-05 | Stephen T. Wrobleski | Cytokine, especially tnf-alpha, inhibitors |
| US6943161B2 (en) * | 1999-12-28 | 2005-09-13 | Pharmacopela Drug Discovery, Inc. | Pyrimidine and triazine kinase inhibitors |
| CA2450934A1 (en) | 2001-06-19 | 2002-12-27 | Marco Dodier | Pyrimidine inhibitors of phosphodiesterase (pde) 7 |
| JP4460292B2 (ja) | 2001-10-17 | 2010-05-12 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | ピリミジン誘導体、これらの化合物を含む医薬組成物、その使用及びその調製方法 |
| CA2547080A1 (en) | 2003-12-02 | 2005-07-28 | Vertex Pharmaceuticals, Inc. | Heterocyclic protein kinase inhibitors and uses thereof |
| US20050245199A1 (en) * | 2004-02-19 | 2005-11-03 | Texas Instruments Incorporated | Scalable, cooperative, wireless networking for mobile connectivity |
| JP4812763B2 (ja) * | 2004-05-18 | 2011-11-09 | ライジェル ファーマシューティカルズ， インコーポレイテッド | シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途 |
| GB0419160D0 (en) * | 2004-08-27 | 2004-09-29 | Novartis Ag | Organic compounds |
| US20090264415A2 (en) | 2004-12-30 | 2009-10-22 | Steven De Jonghe | Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment |
| GB0428475D0 (en) | 2004-12-30 | 2005-02-02 | 4 Aza Bioscience Nv | Pyrido(3,2-D)pyrimidine derivatives and pharmaceutical compositions useful as medicines for the treatment of autoimmune disorders |
| KR20070110847A (ko) * | 2005-02-10 | 2007-11-20 | 메디비르 아베 | Ｈｉｖ 프로테아제 억제제 |
| WO2006135993A1 (en) | 2005-06-24 | 2006-12-28 | Gilead Sciences, Inc. | Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for treating hepatitis c. |
| WO2007048557A1 (en) * | 2005-10-25 | 2007-05-03 | Medivir Ab | Protease inhibitors |
| EP1966207A2 (en) | 2005-12-21 | 2008-09-10 | Pfizer Products Inc. | Pyrimidine derivatives for the treatment of abnormal cell growth |
| WO2007089335A2 (en) | 2005-12-29 | 2007-08-09 | Lexicon Pharmaceutical Inc. | Multicyclic amino acid derivatives and methods of their use |
| WO2007081978A2 (en) | 2006-01-11 | 2007-07-19 | Angion Biomedica Corporation | Modulators of hepatocyte growth factor / c-met activity |
| US8017612B2 (en) | 2006-04-18 | 2011-09-13 | Japan Tobacco Inc. | Piperazine compound and use thereof as a HCV polymerase inhibitor |
| CA2691003A1 (en) | 2007-06-26 | 2008-12-31 | Lexicon Pharmaceuticals, Inc. | Methods of treating serotonin-mediated diseases and disorders |
| US8093291B2 (en) | 2007-06-26 | 2012-01-10 | Lexicon Pharmaceuticals, Inc. | Methods of using and compositions comprising tryptophan hydroxylase inhibitors |
| CN101815534A (zh) | 2007-07-11 | 2010-08-25 | 莱西肯医药有限公司 | 用于治疗肺动脉高压以及相关疾病和病症的方法和组合物 |
| US20090029993A1 (en) | 2007-07-26 | 2009-01-29 | Qingyun Liu | Methods of affecting gastrointestinal transit and gastric emptying, and compounds useful therein |
| BRPI0910668A2 (pt) * | 2008-04-22 | 2019-09-24 | Portola Pharmaceutiacals Inc | inibidores de proteína quinases |
| CA2722326A1 (en) * | 2008-04-24 | 2009-10-29 | Incyte Corporation | Macrocyclic compounds and their use as kinase inhibitors |
-
2011
- 2011-04-20 TW TW100113777A patent/TWI513694B/zh not_active IP Right Cessation
- 2011-05-04 ES ES11781042.4T patent/ES2538581T3/es active Active
- 2011-05-04 US US13/697,730 patent/US8716281B2/en active Active
- 2011-05-04 WO PCT/US2011/035186 patent/WO2011143033A1/en not_active Ceased
- 2011-05-04 EP EP11781042.4A patent/EP2600874B1/en not_active Not-in-force
- 2011-05-04 AU AU2011253311A patent/AU2011253311B2/en not_active Expired - Fee Related
- 2011-05-04 JP JP2013510173A patent/JP5797261B2/ja not_active Expired - Fee Related
- 2011-05-04 CA CA2799495A patent/CA2799495A1/en not_active Abandoned
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