JP2016523269A5 - - Google Patents
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- JP2016523269A5 JP2016523269A5 JP2016522232A JP2016522232A JP2016523269A5 JP 2016523269 A5 JP2016523269 A5 JP 2016523269A5 JP 2016522232 A JP2016522232 A JP 2016522232A JP 2016522232 A JP2016522232 A JP 2016522232A JP 2016523269 A5 JP2016523269 A5 JP 2016523269A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heterocyclyl
- ring
- substituted
- halogen
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 37
- 125000000623 heterocyclic group Chemical group 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 23
- 229910052736 halogen Inorganic materials 0.000 claims 23
- 150000002367 halogens Chemical class 0.000 claims 23
- 125000001072 heteroaryl group Chemical group 0.000 claims 19
- 125000001424 substituent group Chemical group 0.000 claims 19
- 125000001188 haloalkyl group Chemical group 0.000 claims 16
- 125000003342 alkenyl group Chemical group 0.000 claims 12
- 125000000304 alkynyl group Chemical group 0.000 claims 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 241000257303 Hymenoptera Species 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 230000008878 coupling Effects 0.000 claims 2
- 238000010168 coupling process Methods 0.000 claims 2
- 238000005859 coupling reaction Methods 0.000 claims 2
- 201000005787 hematologic cancer Diseases 0.000 claims 2
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- -1 pyridooxazinyl Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 102000009929 raf Kinases Human genes 0.000 claims 2
- 108010077182 raf Kinases Proteins 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims 1
- 206010004593 Bile duct cancer Diseases 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
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas 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
- 208000015634 Rectal Neoplasms Diseases 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
- 208000026900 bile duct neoplasm Diseases 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000002704 decyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 239000000539 dimer Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 201000005249 lung adenocarcinoma Diseases 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
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2013/078338 | 2013-06-28 | ||
| CN2013078338 | 2013-06-28 | ||
| PCT/CN2014/080983 WO2014206343A1 (en) | 2013-06-28 | 2014-06-27 | Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018135807A Division JP6707584B2 (ja) | 2013-06-28 | 2018-07-19 | Ｒａｆキナーゼおよび／またはＲａｆキナーゼの二量体阻害剤としての縮合三環式ウレア系化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016523269A JP2016523269A (ja) | 2016-08-08 |
| JP2016523269A5 true JP2016523269A5 (enExample) | 2017-08-10 |
| JP6380861B2 JP6380861B2 (ja) | 2018-08-29 |
Family
ID=52141106
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016522232A Active JP6380861B2 (ja) | 2013-06-28 | 2014-06-27 | Ｒａｆキナ−ゼおよび／またはＲａｆキナ−ゼの二量体阻害剤としての縮合三環式ウレア系化合物 |
| JP2018135807A Active JP6707584B2 (ja) | 2013-06-28 | 2018-07-19 | Ｒａｆキナーゼおよび／またはＲａｆキナーゼの二量体阻害剤としての縮合三環式ウレア系化合物 |
| JP2020088185A Active JP6889311B2 (ja) | 2013-06-28 | 2020-05-20 | Ｒａｆキナーゼおよび／またはＲａｆキナーゼの二量体阻害剤としての縮合三環式ウレア系化合物 |
| JP2021085486A Active JP7207629B2 (ja) | 2013-06-28 | 2021-05-20 | Ｒａｆキナーゼおよび／またはＲａｆキナーゼの二量体阻害剤としての縮合三環式ウレア系化合物 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018135807A Active JP6707584B2 (ja) | 2013-06-28 | 2018-07-19 | Ｒａｆキナーゼおよび／またはＲａｆキナーゼの二量体阻害剤としての縮合三環式ウレア系化合物 |
| JP2020088185A Active JP6889311B2 (ja) | 2013-06-28 | 2020-05-20 | Ｒａｆキナーゼおよび／またはＲａｆキナーゼの二量体阻害剤としての縮合三環式ウレア系化合物 |
| JP2021085486A Active JP7207629B2 (ja) | 2013-06-28 | 2021-05-20 | Ｒａｆキナーゼおよび／またはＲａｆキナーゼの二量体阻害剤としての縮合三環式ウレア系化合物 |
Country Status (18)
| Country | Link |
|---|---|
| US (4) | US9670203B2 (enExample) |
| EP (1) | EP3013798B1 (enExample) |
| JP (4) | JP6380861B2 (enExample) |
| KR (1) | KR102272606B1 (enExample) |
| CN (2) | CN109369671B (enExample) |
| AU (1) | AU2014301816B2 (enExample) |
| BR (1) | BR112015032539B1 (enExample) |
| CA (1) | CA2916543C (enExample) |
| DK (1) | DK3013798T3 (enExample) |
| EA (1) | EA029412B1 (enExample) |
| ES (1) | ES2686821T3 (enExample) |
| IL (1) | IL242973A0 (enExample) |
| MX (1) | MX362582B (enExample) |
| NZ (1) | NZ716392A (enExample) |
| PT (1) | PT3013798T (enExample) |
| SG (1) | SG11201600147TA (enExample) |
| WO (1) | WO2014206343A1 (enExample) |
| ZA (1) | ZA201600513B (enExample) |
Families Citing this family (49)
| 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 |
| US9611267B2 (en) | 2012-06-13 | 2017-04-04 | Incyte Holdings Corporation | Substituted tricyclic compounds as FGFR 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 |
| TWI649318B (zh) | 2013-04-19 | 2019-02-01 | 英塞特控股公司 | 作為ｆｇｆｒ抑制劑之雙環雜環 |
| KR102272606B1 (ko) | 2013-06-28 | 2021-07-05 | 베이진 엘티디 | Raf 키나아제 및/또는 raf 키나아제 이량체 저해제로서 융합 트리시클릭 우레아 화합물 |
| WO2014206344A1 (en) | 2013-06-28 | 2014-12-31 | Beigene, Ltd. | Fused tricyclic amide compounds as multiple kinase inhibitors |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | 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 |
| AU2016219822B2 (en) | 2015-02-20 | 2020-07-09 | Incyte Holdings Corporation | Bicyclic heterocycles as FGFR inhibitors |
| ES2950348T3 (es) | 2015-12-09 | 2023-10-09 | Novartis Ag | Moduladores de receptores NMDA de tienopirimidinona y usos de los mismos |
| PL3386591T3 (pl) | 2015-12-09 | 2021-02-22 | Novartis Ag | Heteroaromatyczne modulatory receptorów nmda i ich zastosowania |
| EP3558318B1 (en) | 2016-12-22 | 2023-12-20 | Novartis AG | Nmda receptor modulators and uses thereof |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| TW201946630A (zh) | 2018-05-04 | 2019-12-16 | 美商英塞特公司 | Fgfr抑制劑之鹽 |
| ES2991427T3 (es) | 2018-05-04 | 2024-12-03 | Incyte Corp | Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas |
| RS64359B1 (sr) | 2018-08-03 | 2023-08-31 | Novartis Ag | Heteroaromatični modulatori nmda receptora i njihove upotrebe |
| JP2022500385A (ja) | 2018-09-10 | 2022-01-04 | ミラティ セラピューティクス， インコーポレイテッド | 組み合わせ療法 |
| CN111484490B (zh) * | 2019-01-25 | 2024-07-09 | 百济神州有限公司 | 适合大规模生产b-raf激酶二聚体抑制剂的方法 |
| 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 |
| CN116715662A (zh) * | 2019-01-25 | 2023-09-08 | 百济神州(北京)生物科技有限公司 | 无定形的b-raf激酶二聚体抑制剂 |
| CN111484488A (zh) * | 2019-01-25 | 2020-08-04 | 百济神州(北京)生物科技有限公司 | 一种b-raf激酶二聚体抑制剂的稳定结晶形式a |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| BR112021018168B1 (pt) | 2019-03-21 | 2023-11-28 | Onxeo | Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer |
| 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 |
| WO2021072028A1 (en) * | 2019-10-08 | 2021-04-15 | The Brigham And Women's Hospital, Inc. | Activators of heme regulated inhibitor kinase (hri) |
| GEAP202415945A (en) | 2019-10-14 | 2024-04-25 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CA3159348A1 (en) | 2019-11-08 | 2021-05-14 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| DK4146348T3 (da) | 2020-05-08 | 2024-09-30 | Halia Therapeutics Inc | Inhibitorer af nek7-kinase |
| BR112022024729A2 (pt) | 2020-06-05 | 2023-02-28 | Kinnate Biopharma Inc | Inibidores de quinases do receptor do fator de crescimento de fibroblastos |
| WO2022146022A1 (ko) * | 2020-12-29 | 2022-07-07 | 주식회사 티씨노바이오사이언스 | 엑토뉴클레오티드 피로포스파타아제-포스포디에스터라아제의 저해 활성을 갖는 신규한 나프티리딘온 유도체 및 이들의 용도 |
| PH12023552774A1 (en) | 2021-04-05 | 2024-04-15 | Halia Therapeutics Inc | Nek7 inhibitors |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| US20250177382A1 (en) | 2021-04-22 | 2025-06-05 | Halia Therapeutics, Inc. | Nek7 inhibitors |
| CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| AR126101A1 (es) | 2021-06-09 | 2023-09-13 | Incyte Corp | Heterociclos tricíclicos como inhibidores de fgfr |
| JP2025519981A (ja) * | 2022-06-08 | 2025-06-30 | マップキュア，エルエルシー | Ｂ－ｒａｆ阻害剤によるがんの治療方法 |
| US20240158394A1 (en) | 2022-09-14 | 2024-05-16 | Halia Therapeutics, Inc. | Nek7 inhibitors |
| IL319792A (en) * | 2022-09-26 | 2025-05-01 | Mapkure Llc | Combinations of B-RAF inhibitor and anti-EGFR antibody for cancer treatment |
| US20240122881A1 (en) * | 2022-10-14 | 2024-04-18 | Springworks Therapeutics, Inc. | Combination for use in treating cancers |
| WO2025073765A1 (en) | 2023-10-03 | 2025-04-10 | Institut National de la Santé et de la Recherche Médicale | Methods of prognosis and treatment of patients suffering from melanoma |
| TW202515875A (zh) | 2023-10-12 | 2025-04-16 | 瑞士商百濟神州瑞士有限責任公司 | 包含b-raf激酶二聚體抑制劑之固體形式、其製備方法及用途 |
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| PE20081581A1 (es) | 2006-12-21 | 2008-11-12 | Plexxikon Inc | COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA |
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| WO2011092088A1 (en) | 2010-01-27 | 2011-08-04 | Nerviano Medical Sciences S.R.L. | Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors |
| HUE029656T2 (en) | 2011-12-31 | 2017-03-28 | Beigene Ltd | Condensed tricyclic compounds as RAF kinase inhibitors |
| KR102272606B1 (ko) | 2013-06-28 | 2021-07-05 | 베이진 엘티디 | Raf 키나아제 및/또는 raf 키나아제 이량체 저해제로서 융합 트리시클릭 우레아 화합물 |
| WO2014206344A1 (en) | 2013-06-28 | 2014-12-31 | Beigene, Ltd. | Fused tricyclic amide compounds as multiple kinase inhibitors |
-
2014
- 2014-06-27 KR KR1020167001854A patent/KR102272606B1/ko active Active
- 2014-06-27 EA EA201690098A patent/EA029412B1/ru not_active IP Right Cessation
- 2014-06-27 NZ NZ716392A patent/NZ716392A/en unknown
- 2014-06-27 BR BR112015032539-4A patent/BR112015032539B1/pt active IP Right Grant
- 2014-06-27 AU AU2014301816A patent/AU2014301816B2/en active Active
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