JP2018535949A5 - - Google Patents
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- JP2018535949A5 JP2018535949A5 JP2018518629A JP2018518629A JP2018535949A5 JP 2018535949 A5 JP2018535949 A5 JP 2018535949A5 JP 2018518629 A JP2018518629 A JP 2018518629A JP 2018518629 A JP2018518629 A JP 2018518629A JP 2018535949 A5 JP2018535949 A5 JP 2018535949A5
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- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- unsubstituted
- cycloalkyl
- independently
- 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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- 150000004820 halides Chemical class 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 7
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 230000004761 fibrosis Effects 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 claims 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- -1 C 1 -C 6 alkyl Chemical group 0.000 claims 1
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 1
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010061534 Oesophageal squamous cell carcinoma 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
- 208000032056 Radiation Fibrosis Syndrome Diseases 0.000 claims 1
- 201000000582 Retinoblastoma Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 1
- 208000036765 Squamous cell carcinoma of the esophagus Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- YZCKVEUIGOORGS-NJFSPNSNSA-N Tritium Chemical compound [3H] YZCKVEUIGOORGS-NJFSPNSNSA-N 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000004442 acylamino group Chemical group 0.000 claims 1
- 125000005256 alkoxyacyl group Chemical group 0.000 claims 1
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 125000004422 alkyl sulphonamide group Chemical group 0.000 claims 1
- 125000000266 alpha-aminoacyl group Chemical group 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 229910052805 deuterium Inorganic materials 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002500 effect on skin Effects 0.000 claims 1
- 208000007276 esophageal squamous cell carcinoma Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 201000008026 nephroblastoma Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 229910052722 tritium Inorganic materials 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
Applications Claiming Priority (15)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510645986.2 | 2015-10-08 | ||
| CN201510645986.2A CN105254613A (zh) | 2015-10-08 | 2015-10-08 | 具有Wnt信号通路抑制活性的杂环化合物及其应用 |
| CN201610195731 | 2016-03-31 | ||
| CN201610195733 | 2016-03-31 | ||
| CN201610195733.4 | 2016-03-31 | ||
| CN201610195731.5 | 2016-03-31 | ||
| CN201610670828.7 | 2016-08-16 | ||
| CN201610670828.7A CN107759584B (zh) | 2016-08-16 | 2016-08-16 | 一种具有Wnt信号通路抑制活性的氨基五元杂环化合物及其应用 |
| CN201610850358.2 | 2016-09-26 | ||
| CN201610850360.XA CN106565673B (zh) | 2015-10-08 | 2016-09-26 | 具有Wnt信号通路抑制活性的5-氟嘧啶杂环化合物及其应用 |
| CN201610850358.2A CN107286136B (zh) | 2016-03-31 | 2016-09-26 | 一种3-氟吡啶杂环化合物及其应用 |
| CN201610850357.8A CN107286135B (zh) | 2016-03-31 | 2016-09-26 | 一种具有Wnt信号通路抑制活性的杂环化合物及其应用 |
| CN201610850360.X | 2016-09-26 | ||
| CN201610850357.8 | 2016-09-26 | ||
| PCT/US2016/055851 WO2017062688A1 (en) | 2015-10-08 | 2016-10-06 | Wnt signaling pathway inhibitors and therapeutic applications thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018535949A JP2018535949A (ja) | 2018-12-06 |
| JP2018535949A5 true JP2018535949A5 (enExample) | 2019-11-14 |
| JP6853819B2 JP6853819B2 (ja) | 2021-03-31 |
Family
ID=62621830
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018518629A Active JP6853819B2 (ja) | 2015-10-08 | 2016-10-06 | Wntシグナル伝達経路阻害剤およびその治療用途 |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US10450300B2 (enExample) |
| EP (1) | EP3359154B1 (enExample) |
| JP (1) | JP6853819B2 (enExample) |
| KR (1) | KR102698411B1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7421655B2 (ja) * | 2020-01-02 | 2024-01-24 | へルムホルツ-ツェントルム・フューア・インフェクツィオーンスフォルシュング・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | 新規なPqsRインバースアゴニスト |
| CN112612873B (zh) * | 2020-12-25 | 2023-07-07 | 上海德拓信息技术股份有限公司 | 一种基于nlp技术的集中性事件挖掘方法 |
| JP2024532597A (ja) * | 2021-08-27 | 2024-09-05 | 杭州阿諾生物医薬科技有限公司 | サイクリンk分解剤 |
| WO2025143733A1 (ko) * | 2023-12-26 | 2025-07-03 | (주)아이젠사이언스 | 신규한 유비퀴틴 특이적 펩티드 분해효소 1 저해제 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61205261A (ja) * | 1985-03-08 | 1986-09-11 | Sagami Chem Res Center | 6―置換―5―フルオロウラシル誘導体 |
| US4617393A (en) * | 1985-07-19 | 1986-10-14 | American Home Products Corporation | 5-substituted-6-aminopyrimidines, composition and uses as cardiotonic agents for increasing cardiac contractility |
| US7135575B2 (en) * | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| UY31048A1 (es) | 2007-04-25 | 2008-11-28 | Astrazeneca Ab | Nuevos compuestos de pirimidina y usos de los mismos |
| US20090054392A1 (en) * | 2007-08-20 | 2009-02-26 | Wyeth | Naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analogs and their use as agonists of the wnt-beta-catenin cellular messaging system |
| UY32055A (es) * | 2008-08-19 | 2010-03-26 | Astrazeneca Ab | Derivados sustituidos de la 5-Halo-N2-[sustituido](1-metil-1H-imidazol-4-il)pirimidin-2,-diamina y sus sales farmacéuticamente aceptables, procesos de preparación, composiciones y aplicaciones. |
| GB0818241D0 (en) | 2008-10-06 | 2008-11-12 | Cancer Res Technology | Compounds and their use |
| US20110189097A1 (en) * | 2009-11-09 | 2011-08-04 | Dritan Agalliu | Use of WNT inhibitor to inhibit angiogenesis in the CNS |
| WO2012149528A1 (en) * | 2011-04-29 | 2012-11-01 | Exelixis, Inc. | Inhibitors of inducible form of 6-phosphofructose-2-kinase |
| RU2014134909A (ru) | 2012-01-28 | 2016-03-20 | Мерк Патент Гмбх | Азагетероциклические соединения |
| PH12017500997A1 (en) * | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
| CA2905830C (en) * | 2013-03-12 | 2022-01-18 | Curegenix Inc. | Quinazoline and naphthyridine derivatives useful in the treatment of cancer |
| CA2905841A1 (en) | 2013-03-14 | 2014-10-02 | Curegenix, Inc. | Quinazoline and naphthyridine derivatives useful in the treatment of fibrotic disorders |
| SG11201700777VA (en) * | 2014-08-04 | 2017-02-27 | Nuevolution As | Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases |
| US9771349B2 (en) * | 2014-09-19 | 2017-09-26 | Forma Therapeutics, Inc. | Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| MX2017005346A (es) * | 2014-10-29 | 2017-08-02 | Dong A St Co Ltd | Nuevos compuestos de piridopirimidinona para modular la actividad catalitica de histona lisina desmetilasas (kdm). |
-
2016
- 2016-10-06 EP EP16854369.2A patent/EP3359154B1/en active Active
- 2016-10-06 US US15/766,799 patent/US10450300B2/en active Active
- 2016-10-06 JP JP2018518629A patent/JP6853819B2/ja active Active
- 2016-10-06 KR KR1020187013073A patent/KR102698411B1/ko active Active
-
2019
- 2019-10-15 US US16/653,217 patent/US20200048223A1/en not_active Abandoned
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