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
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- 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 (https=) | 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 (https=) |
| EP (1) | EP2600874B1 (https=) |
| JP (1) | JP5797261B2 (https=) |
| AU (1) | AU2011253311B2 (https=) |
| CA (1) | CA2799495A1 (https=) |
| ES (1) | ES2538581T3 (https=) |
| TW (1) | TWI513694B (https=) |
| WO (1) | WO2011143033A1 (https=) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| ES2704744T3 (es) | 2012-06-13 | 2019-03-19 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| SG11201408816QA (en) | 2012-07-03 | 2015-03-30 | Aurigene Discovery Tech Ltd | 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 |
| US9611257B2 (en) | 2012-12-21 | 2017-04-04 | Epizyme, Inc. | PRMT5 inhibitors and uses thereof |
| UA118548C2 (uk) | 2012-12-21 | 2019-02-11 | Епізайм, Інк. | Тетрагідро- та дигідроізохіноліни як інгібітори prmt5 та їх застосування |
| JP2016505000A (ja) | 2012-12-21 | 2016-02-18 | エピザイム，インコーポレイティド | Ｐｒｍｔ５阻害剤およびその使用 |
| CA2894157A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| EP3406607A1 (en) | 2012-12-21 | 2018-11-28 | Epizyme, Inc. | Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| 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 |
| EP3177288A4 (en) | 2014-08-04 | 2018-04-04 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MX373169B (es) | 2015-02-20 | 2020-04-24 | Incyte Holdings Corp | Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr). |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CR20200590A (es) | 2018-05-04 | 2021-04-26 | Incyte Corp | Formas sólidas de un inhibidor de fgfr y procesos para prepararlas |
| MA52493A (fr) | 2018-05-04 | 2021-03-10 | Incyte Corp | Sels d'un inhibiteur de fgfr |
| 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 |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| TWI891666B (zh) | 2019-10-14 | 2025-08-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之雙環雜環 |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法 |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | 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 |
| TR200201431T2 (tr) * | 1999-11-30 | 2002-09-23 | Pfizer Products Inc. | İmünosupresanlar olarak faydalı 2,4-diaminopirimidin bileşikleri |
| CA2394727A1 (en) * | 1999-12-28 | 2001-07-05 | Pharmacopeia, Inc. | Pyrimidine and triazine kinase inhibitors |
| US6943161B2 (en) * | 1999-12-28 | 2005-09-13 | Pharmacopela Drug Discovery, Inc. | Pyrimidine and triazine kinase inhibitors |
| JP2005500294A (ja) | 2001-06-19 | 2005-01-06 | ブリストル−マイヤーズ スクイブ カンパニー | ホスホジエステラーゼ７に対するピリミジン阻害剤 |
| ATE407678T1 (de) | 2001-10-17 | 2008-09-15 | Boehringer Ingelheim Pharma | Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung |
| CA2547080A1 (en) | 2003-12-02 | 2005-07-28 | Vertex Pharmaceuticals, Inc. | Heterocyclic protein kinase inhibitors and uses thereof |
| EP1723728B1 (en) * | 2004-02-19 | 2019-10-16 | Texas Instruments Incorporated | Scalable, cooperative, wireless networking for mobile connectivity |
| EP1763514A2 (en) * | 2004-05-18 | 2007-03-21 | Rigel Pharmaceuticals, Inc. | Cycloalkyl substituted pyrimidinediamine compounds and their uses |
| GB0419160D0 (en) * | 2004-08-27 | 2004-09-29 | Novartis Ag | Organic compounds |
| 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 |
| US20090264415A2 (en) | 2004-12-30 | 2009-10-22 | Steven De Jonghe | Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment |
| WO2006084688A1 (en) * | 2005-02-10 | 2006-08-17 | Medivir Ab | HIV protease inhibitors |
| US8232278B2 (en) | 2005-06-24 | 2012-07-31 | 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 |
| AU2006327871A1 (en) | 2005-12-21 | 2007-06-28 | Pfizer Products Inc. | Pyrimidine derivatives for the treatment of abnormal cell growth |
| DK1984344T3 (da) | 2005-12-29 | 2013-01-14 | Lexicon Pharmaceuticals Inc | Multicykliske aminosyrederivater og fremgangsmåder til anvendelse heraf |
| 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 |
| AU2008268409B2 (en) | 2007-06-26 | 2013-12-05 | Lexicon Pharmaceuticals, Inc. | Compositions comprising tryptophan hydroxylase inhibitors |
| CN101784269A (zh) | 2007-06-26 | 2010-07-21 | 莱西肯医药有限公司 | 治疗由5-羟色胺介导的疾病和病症的方法 |
| 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 |
| NZ588830A (en) * | 2008-04-22 | 2012-11-30 | Portola Pharm Inc | Inhibitors of protein kinases |
| WO2009132202A2 (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 CA CA2799495A patent/CA2799495A1/en not_active Abandoned
- 2011-05-04 ES ES11781042.4T patent/ES2538581T3/es active Active
- 2011-05-04 JP JP2013510173A patent/JP5797261B2/ja not_active Expired - Fee Related
- 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 US US13/697,730 patent/US8716281B2/en active Active
- 2011-05-04 AU AU2011253311A patent/AU2011253311B2/en not_active Expired - Fee Related
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