JP2019527682A5 - - Google Patents
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- Publication number
- JP2019527682A5 JP2019527682A5 JP2019500570A JP2019500570A JP2019527682A5 JP 2019527682 A5 JP2019527682 A5 JP 2019527682A5 JP 2019500570 A JP2019500570 A JP 2019500570A JP 2019500570 A JP2019500570 A JP 2019500570A JP 2019527682 A5 JP2019527682 A5 JP 2019527682A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- pharmaceutically acceptable
- acceptable salt
- 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 34
- 239000000651 prodrug Substances 0.000 claims 32
- 229940002612 prodrug Drugs 0.000 claims 32
- 150000003839 salts Chemical class 0.000 claims 32
- 239000012453 solvate Substances 0.000 claims 31
- 239000013078 crystal Substances 0.000 claims 30
- 229910052739 hydrogen Inorganic materials 0.000 claims 29
- 239000001257 hydrogen Substances 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 28
- 150000002431 hydrogen Chemical class 0.000 claims 26
- 125000000623 heterocyclic group Chemical group 0.000 claims 23
- 125000001072 heteroaryl group Chemical group 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 17
- 150000002367 halogens Chemical class 0.000 claims 17
- 125000004452 carbocyclyl group Chemical group 0.000 claims 14
- 239000008194 pharmaceutical composition Substances 0.000 claims 12
- 125000003342 alkenyl group Chemical group 0.000 claims 11
- 125000000304 alkynyl group Chemical group 0.000 claims 11
- 201000010099 disease Diseases 0.000 claims 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 10
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 10
- 125000004429 atom Chemical group 0.000 claims 8
- 150000004677 hydrates Chemical class 0.000 claims 6
- 102000001253 Protein Kinase Human genes 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 108060006633 protein kinase Proteins 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 125000004193 piperazinyl group Chemical group 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000004434 sulfur atom Chemical group 0.000 claims 3
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- JGLMVXWAHNTPRF-CMDGGOBGSA-N CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O Chemical compound CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O JGLMVXWAHNTPRF-CMDGGOBGSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 230000001594 aberrant effect Effects 0.000 claims 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 238000003419 tautomerization reaction Methods 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000019838 Blood disease Diseases 0.000 claims 1
- 208000026350 Inborn Genetic disease Diseases 0.000 claims 1
- 208000023178 Musculoskeletal disease Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000034038 Pathologic Neovascularization Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 238000003556 assay Methods 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([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
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000016361 genetic disease Diseases 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 208000018706 hematopoietic system disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 208000017445 musculoskeletal system disease Diseases 0.000 claims 1
- 230000009826 neoplastic cell growth Effects 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 238000012216 screening Methods 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662358524P | 2016-07-05 | 2016-07-05 | |
| US62/358,524 | 2016-07-05 | ||
| PCT/US2017/040722 WO2018009544A1 (en) | 2016-07-05 | 2017-07-05 | Bicyclic urea kinase inhibitors and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019527682A JP2019527682A (ja) | 2019-10-03 |
| JP2019527682A5 true JP2019527682A5 (enExample) | 2020-08-13 |
| JP7277357B2 JP7277357B2 (ja) | 2023-05-18 |
Family
ID=59351134
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019500570A Active JP7277357B2 (ja) | 2016-07-05 | 2017-07-05 | 二環式尿素キナーゼインヒビターおよびそれらの使用 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US10954242B2 (enExample) |
| EP (2) | EP3481830B1 (enExample) |
| JP (1) | JP7277357B2 (enExample) |
| KR (1) | KR20190075043A (enExample) |
| CN (1) | CN110225914A (enExample) |
| AU (1) | AU2017291812B2 (enExample) |
| CA (1) | CA3069016A1 (enExample) |
| ES (1) | ES2920823T3 (enExample) |
| IL (1) | IL264106B (enExample) |
| WO (1) | WO2018009544A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2015292818B2 (en) | 2014-07-21 | 2020-01-16 | Dana-Farber Cancer Institute, Inc. | Imidazolyl kinase inhibitors and uses thereof |
| JP7277357B2 (ja) | 2016-07-05 | 2023-05-18 | ザ ブロード インスティテュート,インコーポレーテッド | 二環式尿素キナーゼインヒビターおよびそれらの使用 |
| US11241435B2 (en) | 2016-09-16 | 2022-02-08 | The General Hospital Corporation | Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis |
| KR20190120331A (ko) * | 2017-02-28 | 2019-10-23 | 더 제너럴 하스피탈 코포레이션 | Sik 억제제로서의 피리미도피리미디논의 용도 |
| UA127059C2 (uk) * | 2018-03-30 | 2023-03-29 | Ле Лаборатуар Сервьє | Гетеробіциклічні інгібітори mat2a і способи використання для лікування злоякісної пухлини |
| WO2020027200A1 (ja) * | 2018-08-01 | 2020-02-06 | 小野薬品工業株式会社 | 軟骨関連疾患治療剤 |
| US20230027026A1 (en) * | 2019-09-27 | 2023-01-26 | Jubilant Biosys Limited | Fused pyrimidine compounds, compositions and medicinal applications thereof |
| GB201915829D0 (en) | 2019-10-31 | 2019-12-18 | Cancer Research Tech Ltd | Compounds, compositions and therapeutic uses thereof |
| GB201915828D0 (en) | 2019-10-31 | 2019-12-18 | Cancer Research Tech Ltd | Compounds, compositions and therapeutic uses thereof |
| GB201915831D0 (en) | 2019-10-31 | 2019-12-18 | Cancer Research Tech Ltd | Compounds, compositions and therapeutic uses thereof |
| US12195490B2 (en) * | 2020-01-30 | 2025-01-14 | The Regents Of The University Of California | STRAD-binding agents and uses thereof |
| CA3177164A1 (en) * | 2020-04-28 | 2021-11-04 | Peter Sennhenn | Bicyclic kinase inhibitors and uses thereof |
| EP4149629B1 (en) | 2020-05-14 | 2025-06-04 | Rhizen Pharmaceuticals AG | Purine derivatives as sik-3 inhibitors |
| EP4215533A4 (en) * | 2020-09-16 | 2024-12-18 | Axceso Biopharma Co., Ltd. | Pyrimidopyrimidinone compound and pharmaceutical composition comprising same |
| US20230265099A1 (en) * | 2020-09-21 | 2023-08-24 | Soltego, Inc. | Sik inhibitors and methods of use thereof |
| CN116801878A (zh) * | 2020-10-05 | 2023-09-22 | 达纳-法伯癌症研究所股份有限公司 | Her2的有效和选择性抑制剂 |
| US20240100177A1 (en) * | 2020-12-04 | 2024-03-28 | Dyne Therapeutics, Inc. | Antibody-oligonucleotide complexes and uses thereof |
| WO2022165530A1 (en) * | 2021-02-01 | 2022-08-04 | Janssen Biotech, Inc. | Small molecule inhibitors of salt inducible kinases |
| KR20230053049A (ko) * | 2021-10-13 | 2023-04-21 | 서울대학교산학협력단 | 류마티스 관절염 예방 또는 치료용 약학적 조성물 및 건강기능식품 |
| CN116813608B (zh) * | 2023-06-08 | 2024-03-22 | 英矽智能科技(上海)有限公司 | 噻唑类化合物及其应用 |
| CN117547615B (zh) * | 2023-09-26 | 2024-12-06 | 首都医科大学宣武医院 | 一种纳米囊泡及其制备方法和应用 |
Family Cites Families (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4231559B2 (ja) | 1997-04-23 | 2009-03-04 | オリザ油化株式会社 | リポキシゲナーゼ阻害剤 |
| IL139599A0 (en) | 1998-05-26 | 2002-02-10 | Warner Lambert Co | Bicyclic pyrimidines and bicyclic 3,4-dihydropyrimidines as inhibitors of cellular proliferation |
| CA2347474C (en) | 1998-10-23 | 2008-08-26 | F. Hoffmann-La Roche Ag | Bicyclic nitrogen heterocycles |
| WO2003090688A2 (en) | 2002-04-24 | 2003-11-06 | Van Andel Research Institute | Enhancement of human epidermal melanogenesis |
| US7084270B2 (en) | 2002-08-14 | 2006-08-01 | Hoffman-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
| DE10239042A1 (de) | 2002-08-21 | 2004-03-04 | Schering Ag | Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel |
| US20060094013A1 (en) | 2002-08-21 | 2006-05-04 | Hiroshi Takemori | Salt-inducible kinases 2 and use thereof |
| US7112676B2 (en) | 2002-11-04 | 2006-09-26 | Hoffmann-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
| MXPA05005547A (es) | 2002-11-28 | 2005-07-26 | Schering Ag | Pirimidinas inhibidoras de chk, pdk y akt, su produccion y uso como agentes farmaceuticos. |
| EP1615928A1 (en) | 2003-04-10 | 2006-01-18 | F.Hoffmann-La Roche Ag | Pyrimido compounds |
| US7504396B2 (en) | 2003-06-24 | 2009-03-17 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| US7442698B2 (en) | 2003-07-24 | 2008-10-28 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| AU2004260689B8 (en) * | 2003-07-29 | 2008-05-15 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| US7745437B2 (en) | 2004-06-10 | 2010-06-29 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| GB0512324D0 (en) | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| BRPI0514738A (pt) | 2004-08-31 | 2008-06-24 | Hoffmann La Roche | derivados de amida de 3-fenil-diidropirimido[4,5-d]pirimidinonas, sua fabricação e aplicação como agentes farmacêuticos |
| WO2006024545A1 (en) | 2004-09-03 | 2006-03-09 | Stichting Voor De Technische Wetenschappen | Fused bicyclic natural compounds and their use as inhibitors of parp and parp-mediated inflammatory processes |
| WO2006074057A2 (en) | 2004-12-30 | 2006-07-13 | Exelixis, Inc. | Pyrimidine derivatives as kinase modulators and method of use |
| JP2008537937A (ja) | 2005-03-25 | 2008-10-02 | グラクソ グループ リミテッド | ピリド[2,3−d]ピリミジン−7−オンおよび3,4−ジヒドロピリミド[4,5−d]ピリミジン−2(1H)−オン誘導体の製造方法 |
| MX2007015610A (es) * | 2005-06-10 | 2008-02-21 | Irm Llc | Compuestos que mantienen la fluripotencia de las celulas totipotentes embrionarias. |
| EA016438B1 (ru) | 2005-12-21 | 2012-05-30 | Новартис Аг | Производные пиримидиниларилмочевины в качестве ингибиторов фактора роста фибробластов (fgf-фактора) |
| MX2008014618A (es) * | 2006-05-15 | 2008-11-28 | Irm Llc | Composiciones y metodos para inhibidores de cinasas del receptor fgf. |
| WO2008060248A1 (en) | 2006-11-15 | 2008-05-22 | S*Bio Pte Ltd. | Indole sustituted pyrimidines and use thereof in the treatment of cancer |
| WO2009073153A2 (en) | 2007-11-28 | 2009-06-11 | Dana Farber Cancer Institute | Small molecule myristate inhibitors of bcr-abl and methods of use |
| WO2009122180A1 (en) | 2008-04-02 | 2009-10-08 | Medical Research Council | Pyrimidine derivatives capable of inhibiting one or more kinases |
| WO2009152027A1 (en) | 2008-06-12 | 2009-12-17 | Merck & Co., Inc. | 5,7-dihydro-6h-pyrrolo[2,3-d]pyrimidin-6-one derivatives for mark inhibition |
| US8455477B2 (en) | 2008-08-05 | 2013-06-04 | Merck Sharp & Dohme Corp. | Therapeutic compounds |
| JP2012511501A (ja) * | 2008-12-12 | 2012-05-24 | Msd株式会社 | ジヒドロピリミドピリミジン誘導体 |
| EP2488526B1 (en) | 2009-10-14 | 2013-07-24 | Bristol-Myers Squibb Company | Compounds for the treatment of hepatitis c |
| CN102816162B (zh) * | 2011-06-10 | 2016-04-27 | 中国科学院广州生物医药与健康研究院 | 嘧啶并嘧啶酮类化合物及其药用组合物和应用 |
| CA2849999A1 (en) | 2011-09-30 | 2013-04-04 | Oncodesign S.A. | Macrocyclic flt3 kinase inhibitors |
| CA2856291C (en) | 2011-11-17 | 2020-08-11 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| GB201204384D0 (en) | 2012-03-13 | 2012-04-25 | Univ Dundee | Anti-flammatory agents |
| SI3459942T1 (sl) | 2012-04-24 | 2021-05-31 | Vertex Pharmaceuticals Incorporated | Inhibitorji DNA-PK |
| GB201212960D0 (en) * | 2012-07-20 | 2012-09-05 | Common Services Agency | Erythroid production |
| JP5683634B2 (ja) * | 2012-11-28 | 2015-03-11 | 株式会社ショーワ | 圧力緩衝装置 |
| US9260426B2 (en) | 2012-12-14 | 2016-02-16 | Arrien Pharmaceuticals Llc | Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors |
| WO2014138485A1 (en) * | 2013-03-08 | 2014-09-12 | Irm Llc | Ex vivo production of platelets from hematopoietic stem cells and the product thereof |
| SG11201507478VA (en) * | 2013-03-15 | 2015-10-29 | Celgene Avilomics Res Inc | Heteroaryl compounds and uses thereof |
| CN105209040A (zh) | 2013-03-15 | 2015-12-30 | 昂科迪塞恩股份有限公司 | 大环的盐可诱导的激酶抑制剂 |
| AU2014287209B2 (en) | 2013-07-09 | 2019-01-24 | Dana-Farber Cancer Institute, Inc. | Kinase inhibitors for the treatment of disease |
| CN104418860B (zh) * | 2013-08-20 | 2016-09-07 | 中国科学院广州生物医药与健康研究院 | 嘧啶并杂环类化合物及其药用组合物和应用 |
| AU2015292818B2 (en) | 2014-07-21 | 2020-01-16 | Dana-Farber Cancer Institute, Inc. | Imidazolyl kinase inhibitors and uses thereof |
| CA2954187C (en) | 2014-07-21 | 2022-08-16 | Dana-Farber Cancer Institute, Inc. | Macrocyclic kinase inhibitors and uses thereof |
| CA2955082A1 (en) | 2014-08-08 | 2016-02-11 | Dana-Farber Cancer Institute, Inc. | Uses of salt-inducible kinase (sik) inhibitors |
| KR101850282B1 (ko) | 2014-11-26 | 2018-05-31 | 한국과학기술연구원 | 단백질 키나아제 저해제로 유용한 헤테로아릴아민 유도체 |
| CN104482860B (zh) | 2014-12-05 | 2017-10-31 | 浙江大学宁波理工学院 | 鱼类形态参数自动测量装置和方法 |
| JP7277357B2 (ja) | 2016-07-05 | 2023-05-18 | ザ ブロード インスティテュート,インコーポレーテッド | 二環式尿素キナーゼインヒビターおよびそれらの使用 |
| US11241435B2 (en) | 2016-09-16 | 2022-02-08 | The General Hospital Corporation | Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis |
| KR20190120331A (ko) | 2017-02-28 | 2019-10-23 | 더 제너럴 하스피탈 코포레이션 | Sik 억제제로서의 피리미도피리미디논의 용도 |
-
2017
- 2017-07-05 JP JP2019500570A patent/JP7277357B2/ja active Active
- 2017-07-05 EP EP17740232.8A patent/EP3481830B1/en active Active
- 2017-07-05 US US16/315,438 patent/US10954242B2/en active Active
- 2017-07-05 AU AU2017291812A patent/AU2017291812B2/en active Active
- 2017-07-05 KR KR1020197003642A patent/KR20190075043A/ko not_active Withdrawn
- 2017-07-05 ES ES17740232T patent/ES2920823T3/es active Active
- 2017-07-05 EP EP21218204.2A patent/EP4047001A3/en active Pending
- 2017-07-05 CN CN201780054098.0A patent/CN110225914A/zh active Pending
- 2017-07-05 WO PCT/US2017/040722 patent/WO2018009544A1/en not_active Ceased
- 2017-07-05 CA CA3069016A patent/CA3069016A1/en active Pending
-
2019
- 2019-01-06 IL IL264106A patent/IL264106B/en unknown
-
2020
- 2020-11-20 US US16/953,984 patent/US11725011B2/en active Active
-
2023
- 2023-03-27 US US18/126,676 patent/US12398145B2/en active Active
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