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 |
|---|---|---|---|
| CN2013078338 | 2013-06-28 | ||
| CNPCT/CN2013/078338 | 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) | CN105452223B (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) |
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| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
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| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| KR102269032B1 (ko) | 2013-04-19 | 2021-06-24 | 인사이트 홀딩스 코포레이션 | Fgfr 저해제로서 이환식 헤테로사이클 |
| WO2014206344A1 (en) * | 2013-06-28 | 2014-12-31 | Beigene, Ltd. | Fused tricyclic amide compounds as multiple kinase inhibitors |
| KR102272606B1 (ko) * | 2013-06-28 | 2021-07-05 | 베이진 엘티디 | Raf 키나아제 및/또는 raf 키나아제 이량체 저해제로서 융합 트리시클릭 우레아 화합물 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
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| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
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| CN111484489B (zh) * | 2019-01-25 | 2023-05-23 | 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 |
| 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 |
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| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
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| WO2021072028A1 (en) * | 2019-10-08 | 2021-04-15 | The Brigham And Women's Hospital, Inc. | Activators of heme regulated inhibitor kinase (hri) |
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| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
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2014
- 2014-06-27 KR KR1020167001854A patent/KR102272606B1/ko active Active
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2015
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2016
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2017
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2018
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2019
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2020
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2021
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