JP2020512400A5 - - Google Patents
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- JP2020512400A5 JP2020512400A5 JP2020501434A JP2020501434A JP2020512400A5 JP 2020512400 A5 JP2020512400 A5 JP 2020512400A5 JP 2020501434 A JP2020501434 A JP 2020501434A JP 2020501434 A JP2020501434 A JP 2020501434A JP 2020512400 A5 JP2020512400 A5 JP 2020512400A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- carbon atoms
- group containing
- compounds
- solvate
- 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.)
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- 125000004432 carbon atom Chemical group C* 0.000 claims 63
- 150000001875 compounds Chemical class 0.000 claims 47
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 17
- 239000012453 solvate Substances 0.000 claims 17
- 125000003545 alkoxy group Chemical group 0.000 claims 16
- 125000000304 alkynyl group Chemical group 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 4
- 125000003368 amide group Chemical group 0.000 claims 3
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 2
- 150000004292 cyclic ethers Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 125000003884 phenylalkyl group Chemical group 0.000 claims 2
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 2
- 125000002112 pyrrolidino group Chemical group [*]N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- QMNUDYFKZYBWQX-UHFFFAOYSA-N 1H-quinazolin-4-one Chemical class C1=CC=C2C(=O)N=CNC2=C1 QMNUDYFKZYBWQX-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis 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
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 201000002287 Keratoconus Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000001826 Marfan syndrome Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 125000005036 alkoxyphenyl group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 208000026900 bile duct neoplasm Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 201000010982 kidney cancer 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
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028537 myelofibrosis Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000002611 ovarian Effects 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000002071 phenylalkoxy group Chemical group 0.000 claims 1
- 208000003476 primary myelofibrosis Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- -1 t-butoxycarbonyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- OJTAANBEAZFQQE-UHFFFAOYSA-N Fc1cc(NCc2nc(-c3n[n](C4CC4)cc3)c(-c(cc3)cc4c3nccn4)[nH]2)cc(F)c1 Chemical compound Fc1cc(NCc2nc(-c3n[n](C4CC4)cc3)c(-c(cc3)cc4c3nccn4)[nH]2)cc(F)c1 OJTAANBEAZFQQE-UHFFFAOYSA-N 0.000 description 1
- WDTSCTSIKGNYHU-UHFFFAOYSA-N Fc1cc(NCc2nc(-c3n[n](C4CC4)cc3)c(-c3c[n]4ncnc4cc3)[nH]2)cc(F)c1 Chemical compound Fc1cc(NCc2nc(-c3n[n](C4CC4)cc3)c(-c3c[n]4ncnc4cc3)[nH]2)cc(F)c1 WDTSCTSIKGNYHU-UHFFFAOYSA-N 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022205213A JP2023052027A (ja) | 2017-03-23 | 2022-12-22 | ＴＧＦβの阻害のための三置換イミダゾールおよび治療方法 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762475451P | 2017-03-23 | 2017-03-23 | |
| US62/475,451 | 2017-03-23 | ||
| PCT/US2018/024133 WO2019005241A1 (en) | 2017-03-23 | 2018-03-23 | TRI-SUBSTITUTED IMIDAZOLES FOR INHIBITION OF TGF-BETA AND METHODS OF TREATMENT |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022205213A Division JP2023052027A (ja) | 2017-03-23 | 2022-12-22 | ＴＧＦβの阻害のための三置換イミダゾールおよび治療方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020512400A JP2020512400A (ja) | 2020-04-23 |
| JP2020512400A5 true JP2020512400A5 (https=) | 2021-04-15 |
Family
ID=64741862
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020501434A Pending JP2020512400A (ja) | 2017-03-23 | 2018-03-23 | ＴＧＦβの阻害のための三置換イミダゾールおよび治療方法 |
| JP2022205213A Pending JP2023052027A (ja) | 2017-03-23 | 2022-12-22 | ＴＧＦβの阻害のための三置換イミダゾールおよび治療方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022205213A Pending JP2023052027A (ja) | 2017-03-23 | 2022-12-22 | ＴＧＦβの阻害のための三置換イミダゾールおよび治療方法 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US11124509B2 (https=) |
| EP (1) | EP3600294B1 (https=) |
| JP (2) | JP2020512400A (https=) |
| ES (1) | ES3053505T3 (https=) |
| WO (1) | WO2019005241A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11124509B2 (en) | 2017-03-23 | 2021-09-21 | Clavius Pharmaceuticals, LLC. | Tri-substituted imidazoles for the inhibition of TGF beta and methods of treatment |
| US12077548B2 (en) | 2018-08-22 | 2024-09-03 | Clavius Pharmaceuticals, LLC. | Substituted imidazoles for the inhibition of TGF-β and methods of treatment |
| SG11202104331YA (en) | 2018-12-11 | 2021-05-28 | Theravance Biopharma R&D Ip Llc | Naphthyridine and quinoline derivatives useful as alk5 inhibitors |
| CN114728941A (zh) | 2019-11-22 | 2022-07-08 | 施万生物制药研发Ip有限责任公司 | 作为alk5抑制剂的经取代的1,5-萘啶或喹啉 |
| KR102509625B1 (ko) * | 2022-03-25 | 2023-03-14 | 주식회사 메드팩토 | TGF-β 저해제의 합성에 유용한 중간체 및 이를 이용한 TGF-β 저해제 제조방법 |
| EP4717694A1 (en) * | 2023-05-22 | 2026-04-01 | Iregene Therapeutics Co., Ltd. | Pyrazolformyl piperazinone compound, pharmaceutical composition and use thereof |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2001163861A (ja) * | 1999-12-07 | 2001-06-19 | Nippon Soda Co Ltd | ジフェニルイミダゾール化合物および農園芸用殺菌剤 |
| NZ549003A (en) * | 2004-03-05 | 2009-07-31 | Taisho Pharmaceutical Co Ltd | Thiazole derivative as an ALK5 inhibitor |
| US8188113B2 (en) * | 2006-09-14 | 2012-05-29 | Deciphera Pharmaceuticals, Inc. | Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| EP2108017A2 (en) * | 2007-01-30 | 2009-10-14 | Biogen Idec MA, Inc. | Imidazolone compounds as tgf-beta family type i receptors, alk5 and/or alk4 antagonists |
| SI2947072T1 (sl) * | 2008-03-17 | 2017-03-31 | Ambit Biosciences Corporation | 1-(3-(6,7-dimetoksikinazolin-4-iloksi)fenil)-3-(5-1,1,1-trifluoro-2- metilpropan-2-il)izoksazol-3-il)urea kot modulator raf kinaze pri zdravljenju rakavih bolezni |
| AU2009227013B2 (en) * | 2008-03-21 | 2013-01-10 | Novartis Ag | Novel heterocyclic compounds and uses therof |
| CN102131801B (zh) * | 2008-06-25 | 2015-04-08 | 福拉姆医药股份有限公司 | 1,2-二取代的杂环化合物 |
| WO2010078408A1 (en) * | 2008-12-30 | 2010-07-08 | Biogen Idec Ma Inc. | Heteroaryl compounds useful as raf kinase inhibitors |
| US8080568B1 (en) | 2010-06-29 | 2011-12-20 | Ewha University - Industry Collaboration Foundation | 2-pyridyl substituted imidazoles as therapeutic ALK5 and/or ALK4 inhibitors |
| US20120252721A1 (en) | 2011-03-31 | 2012-10-04 | Idenix Pharmaceuticals, Inc. | Methods for treating drug-resistant hepatitis c virus infection with a 5,5-fused arylene or heteroarylene hepatitis c virus inhibitor |
| DK2731949T3 (en) | 2011-07-13 | 2018-06-14 | Tiumbio Co Ltd | 2-PYRIDYL-SUBSTITUTED IMIDAZOLS AS ALK5 AND / OR ALK4 INHIBITORS |
| JO3336B1 (ar) * | 2014-10-07 | 2019-03-13 | Lilly Co Eli | مركبات أمينو بيريديلوكسي بيرازول |
| EP3221318B1 (en) | 2014-11-21 | 2021-08-25 | Rigel Pharmaceuticals, Inc. | Fused imidazole derivatives as tgf-beta inhibitors |
| ES2789331T3 (es) | 2015-03-02 | 2020-10-26 | Rigel Pharmaceuticals Inc | Inhibidores de TGF-beta |
| EP3527570A4 (en) | 2016-10-14 | 2020-04-15 | Jiangsu Hengrui Medicine Co., Ltd. | FIVE-LINKED HETERARYARYLE CYCLE BRIDGE DERIVATIVE, METHOD FOR PREPARING SAME, AND MEDICAL USE THEREOF |
| US11124509B2 (en) | 2017-03-23 | 2021-09-21 | Clavius Pharmaceuticals, LLC. | Tri-substituted imidazoles for the inhibition of TGF beta and methods of treatment |
-
2018
- 2018-03-23 US US16/496,703 patent/US11124509B2/en active Active
- 2018-03-23 ES ES18823320T patent/ES3053505T3/es active Active
- 2018-03-23 EP EP18823320.9A patent/EP3600294B1/en active Active
- 2018-03-23 WO PCT/US2018/024133 patent/WO2019005241A1/en not_active Ceased
- 2018-03-23 JP JP2020501434A patent/JP2020512400A/ja active Pending
-
2021
- 2021-09-16 US US17/476,943 patent/US11845745B2/en active Active
-
2022
- 2022-12-22 JP JP2022205213A patent/JP2023052027A/ja active Pending
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