JP2016523270A5 - - Google Patents
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- Publication number
- JP2016523270A5 JP2016523270A5 JP2016522233A JP2016522233A JP2016523270A5 JP 2016523270 A5 JP2016523270 A5 JP 2016523270A5 JP 2016522233 A JP2016522233 A JP 2016522233A JP 2016522233 A JP2016522233 A JP 2016522233A JP 2016523270 A5 JP2016523270 A5 JP 2016523270A5
- Authority
- JP
- Japan
- Prior art keywords
- heterocyclyl
- alkyl
- cycloalkyl
- heteroaryl
- aryl
- 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
- 125000000623 heterocyclic group Chemical group 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 23
- 125000001072 heteroaryl group Chemical group 0.000 claims 20
- 125000000217 alkyl group Chemical group 0.000 claims 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims 16
- 125000003118 aryl group Chemical group 0.000 claims 15
- 125000001188 haloalkyl group Chemical group 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 11
- 125000003342 alkenyl group Chemical group 0.000 claims 10
- 125000000304 alkynyl group Chemical group 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 7
- 125000004429 atom Chemical group 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- -1 1,4-dihydro-2H-pyrido [2,3-d] [1,3] oxazinyl Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000005936 piperidyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- LVZWSLJZHVFIQJ-UHFFFAOYSA-N Cyclopropane Chemical compound C1CC1 LVZWSLJZHVFIQJ-UHFFFAOYSA-N 0.000 claims 1
- 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 102100027103 Serine/threonine-protein kinase B-raf Human genes 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 210000000013 bile duct Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 125000004966 cyanoalkyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 125000005347 halocycloalkyl group Chemical group 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 102200048955 rs121434569 Human genes 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013078317 | 2013-06-28 | ||
| CNPCT/CN2013/078317 | 2013-06-28 | ||
| PCT/CN2014/080986 WO2014206344A1 (en) | 2013-06-28 | 2014-06-27 | Fused tricyclic amide compounds as multiple kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018135872A Division JP2018184439A (ja) | 2013-06-28 | 2018-07-19 | 複数種類のキナーゼの阻害剤としての縮合三環式アミド系化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016523270A JP2016523270A (ja) | 2016-08-08 |
| JP2016523270A5 true JP2016523270A5 (cg-RX-API-DMAC10.html) | 2017-08-10 |
| JP6380862B2 JP6380862B2 (ja) | 2018-08-29 |
Family
ID=52141107
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016522233A Expired - Fee Related JP6380862B2 (ja) | 2013-06-28 | 2014-06-27 | 複数種類のキナーゼの阻害剤としての縮合三環式アミド系化合物 |
| JP2018135872A Pending JP2018184439A (ja) | 2013-06-28 | 2018-07-19 | 複数種類のキナーゼの阻害剤としての縮合三環式アミド系化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018135872A Pending JP2018184439A (ja) | 2013-06-28 | 2018-07-19 | 複数種類のキナーゼの阻害剤としての縮合三環式アミド系化合物 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US9670231B2 (cg-RX-API-DMAC10.html) |
| EP (1) | EP3013797B1 (cg-RX-API-DMAC10.html) |
| JP (2) | JP6380862B2 (cg-RX-API-DMAC10.html) |
| WO (1) | WO2014206344A1 (cg-RX-API-DMAC10.html) |
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 |
| CN107652289B (zh) | 2012-06-13 | 2020-07-21 | 因塞特控股公司 | 作为fgfr抑制剂的取代的三环化合物 |
| 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 |
| JP6449244B2 (ja) | 2013-04-19 | 2019-01-09 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｆｇｆｒ抑制剤としての二環式複素環 |
| SG11201600147TA (en) | 2013-06-28 | 2016-02-26 | Beigene Ltd | Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitors |
| WO2014206344A1 (en) | 2013-06-28 | 2014-12-31 | Beigene, Ltd. | Fused tricyclic amide compounds as multiple kinase inhibitors |
| WO2015177193A1 (en) * | 2014-05-21 | 2015-11-26 | Solvay Specialty Polymers Usa, Llc | Stabilizer compounds |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| ES2751669T3 (es) | 2015-02-20 | 2020-04-01 | Incyte Corp | Heterociclos bicíclicos como inhibidores FGFR |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| WO2017111076A1 (ja) * | 2015-12-24 | 2017-06-29 | 協和発酵キリン株式会社 | α、β不飽和アミド化合物 |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CA3091142C (en) | 2018-02-26 | 2023-04-11 | Gilead Sciences, Inc. | Substituted pyrrolizine compounds and uses thereof |
| US11266624B2 (en) * | 2018-04-03 | 2022-03-08 | Texas Tech University System | CRM1 inhibitors reduce primary and acquired resistance of EGFR inhibitors in lung cancer cells |
| PE20210919A1 (es) | 2018-05-04 | 2021-05-19 | Incyte Corp | Sales de un inhibidor de fgfr |
| CN119241541A (zh) | 2018-05-04 | 2025-01-03 | 因赛特公司 | Fgfr抑制剂的固体形式和其制备方法 |
| TWI849043B (zh) * | 2019-01-25 | 2024-07-21 | 英屬開曼群島商百濟神州有限公司 | B-raf激酶二聚體抑制劑之穩定固體分散體、製備方法及其用途 |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | 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 |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| IL293001A (en) | 2019-12-04 | 2022-07-01 | Incyte Corp | Derivatives of fgfr repressors |
| CN114746417B (zh) * | 2019-12-06 | 2023-12-08 | 齐鲁制药有限公司 | Pan-RAF激酶抑制剂的联芳基化合物 |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2022125971A1 (en) * | 2020-12-11 | 2022-06-16 | Erasca, Inc. | Combination therapies for the treatment of cancer |
| JP2024513575A (ja) | 2021-04-12 | 2024-03-26 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤及びネクチン－４標的化剤を含む併用療法 |
| AR126101A1 (es) | 2021-06-09 | 2023-09-13 | Incyte Corp | Heterociclos tricíclicos como inhibidores de fgfr |
| WO2022261160A1 (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 |
|---|---|---|---|---|
| SE0100733D0 (sv) | 2001-03-05 | 2001-03-05 | Medivir Ab | Non-nucleoside reverse transcriptase inhibitors |
| AU2003245700A1 (en) | 2002-02-12 | 2003-09-04 | Glaxo Group Limited | Pyrazolopyridine derivatives |
| EP1534276B1 (en) * | 2002-09-05 | 2008-11-05 | Medivir AB | Non-nucleoside reverse transcriptase inhibitors |
| SI1696920T1 (sl) | 2003-12-19 | 2015-02-27 | Plexxikon Inc. | Spojine in postopki za razvoj modulatorjev ret |
| EP1833829A2 (en) | 2004-12-23 | 2007-09-19 | F. Hoffmann-Roche AG | Benzamide substituted imidazo- and pyrrolo-pyridines as protein kinase inhibitors |
| TW200639163A (en) | 2005-02-04 | 2006-11-16 | Genentech Inc | RAF inhibitor compounds and methods |
| WO2007013896A2 (en) | 2005-05-17 | 2007-02-01 | Plexxikon, Inc. | Pyrrol (2,3-b) pyridine derivatives protein kinase inhibitors |
| EP1902056A2 (en) | 2005-05-20 | 2008-03-26 | Array Biopharma, Inc. | Raf inhibitor compounds and methods of use thereof |
| MY153898A (en) | 2005-06-22 | 2015-04-15 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| BRPI0615781A2 (pt) | 2005-09-01 | 2009-06-16 | Array Biopharma Inc | compostos inibidores de raf e métodos de uso destes |
| AU2006322094A1 (en) * | 2005-12-08 | 2007-06-14 | Millennium Pharmaceuticals, Inc. | Bicyclic compounds with kinase inhibitory activity |
| ATE552245T1 (de) | 2006-05-15 | 2012-04-15 | Merck Sharp & Dohme | Antidiabetische bicyclische verbindungen |
| MX2009002010A (es) | 2006-09-06 | 2009-03-05 | Hoffmann La Roche | Derivados de heteroarilo como inhibidores de la proteina cinasa. |
| WO2008079909A1 (en) | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2,3-b] pyridines as kinase modulators |
| PE20121126A1 (es) | 2006-12-21 | 2012-08-24 | Plexxikon Inc | Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa |
| MX2010000617A (es) | 2007-07-17 | 2010-05-17 | Plexxikon Inc | Compuestos y metodos para modulacion de cinasa, e indicaciones de estos. |
| JO3101B1 (ar) | 2008-12-02 | 2017-09-20 | Takeda Pharmaceuticals Co | مشتقات بنزوثيازول كعوامل مضادة للسرطان |
| US20100197924A1 (en) | 2008-12-22 | 2010-08-05 | Millennium Pharmaceuticals, Inc. | Preparation of aminotetralin compounds |
| AU2011209234B2 (en) | 2010-01-27 | 2015-05-07 | Nerviano Medical Sciences S.R.L. | Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors |
| JP5728499B2 (ja) | 2010-02-05 | 2015-06-03 | アイアールエム・リミテッド・ライアビリティ・カンパニーＩｒｍ，Ｌｌｃ | タンパク質キナーゼ阻害剤としての化合物および組成物 |
| EP2552907B1 (en) | 2010-03-26 | 2014-10-22 | Boehringer Ingelheim International GmbH | Pyridyltriazoles |
| WO2012118492A1 (en) | 2011-03-01 | 2012-09-07 | Array Biopharma Inc. | Heterocyclic sulfonamides as raf inhibitors |
| SI2797888T1 (sl) * | 2011-12-31 | 2017-01-31 | BeiGene, Ltd. Mourant Ozannes Corporate Services (Cayman) Limited | Zlite triciklične spojine kot inhibitorji kinaze raf |
| WO2014206344A1 (en) | 2013-06-28 | 2014-12-31 | Beigene, Ltd. | Fused tricyclic amide compounds as multiple kinase inhibitors |
| SG11201600147TA (en) | 2013-06-28 | 2016-02-26 | Beigene Ltd | Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitors |
-
2014
- 2014-06-27 WO PCT/CN2014/080986 patent/WO2014206344A1/en not_active Ceased
- 2014-06-27 US US14/901,556 patent/US9670231B2/en not_active Expired - Fee Related
- 2014-06-27 JP JP2016522233A patent/JP6380862B2/ja not_active Expired - Fee Related
- 2014-06-27 EP EP14816633.3A patent/EP3013797B1/en not_active Not-in-force
-
2018
- 2018-07-19 JP JP2018135872A patent/JP2018184439A/ja active Pending
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