KR20190136028A - Hpk1 억제제로서의 나프티리딘 - Google Patents
Hpk1 억제제로서의 나프티리딘 Download PDFInfo
- Publication number
- KR20190136028A KR20190136028A KR1020197031494A KR20197031494A KR20190136028A KR 20190136028 A KR20190136028 A KR 20190136028A KR 1020197031494 A KR1020197031494 A KR 1020197031494A KR 20197031494 A KR20197031494 A KR 20197031494A KR 20190136028 A KR20190136028 A KR 20190136028A
- Authority
- KR
- South Korea
- Prior art keywords
- alkyl
- independently
- amino
- heteroaryl
- cycloalkyl
- 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.)
- Ceased
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- YOWJPYWJTNQLOS-UHFFFAOYSA-N N#Cc1c(N(C2)CC2(C2)C2C(Nc2ncc3c(Cl)nc(Cl)cc3c2)=O)nccc1 Chemical compound N#Cc1c(N(C2)CC2(C2)C2C(Nc2ncc3c(Cl)nc(Cl)cc3c2)=O)nccc1 YOWJPYWJTNQLOS-UHFFFAOYSA-N 0.000 description 1
- AOMAJCKOWLJRAN-RISCZKNCSA-N Nc1nc(-c2c(CCN3)c3cnc2)cc2c1cnc(NC([C@H](C1)[C@H]1F)=O)c2 Chemical compound Nc1nc(-c2c(CCN3)c3cnc2)cc2c1cnc(NC([C@H](C1)[C@H]1F)=O)c2 AOMAJCKOWLJRAN-RISCZKNCSA-N 0.000 description 1
- RQRDBUMONSULAO-UHFFFAOYSA-N Nc1nc(Cl)cc2c1cnc(NC(C(C1)C1(F)F)=O)c2 Chemical compound Nc1nc(Cl)cc2c1cnc(NC(C(C1)C1(F)F)=O)c2 RQRDBUMONSULAO-UHFFFAOYSA-N 0.000 description 1
- UUMTVTPPLGBCCL-NWDGAFQWSA-N O=C([C@H](C1)[C@@H]1c1cccnc1)Nc1ncc2c(Cl)nc(Cl)cc2c1 Chemical compound O=C([C@H](C1)[C@@H]1c1cccnc1)Nc1ncc2c(Cl)nc(Cl)cc2c1 UUMTVTPPLGBCCL-NWDGAFQWSA-N 0.000 description 1
- IAYGKSGKXUGKAS-SVRRBLITSA-N O=C([C@H](C1)[C@H]1F)Nc(nc1)cc2c1c(Cl)nc(Cl)c2 Chemical compound O=C([C@H](C1)[C@H]1F)Nc(nc1)cc2c1c(Cl)nc(Cl)c2 IAYGKSGKXUGKAS-SVRRBLITSA-N 0.000 description 1
- JGPKEAXWRNIQLO-UHFFFAOYSA-N O=C1NCCc2cc(Br)n[n]2C1 Chemical compound O=C1NCCc2cc(Br)n[n]2C1 JGPKEAXWRNIQLO-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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- A—HUMAN NECESSITIES
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- A—HUMAN NECESSITIES
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A—HUMAN NECESSITIES
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
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- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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- A—HUMAN NECESSITIES
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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- A—HUMAN NECESSITIES
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- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
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- A—HUMAN NECESSITIES
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D497/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
- C07D497/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D497/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2017078792 | 2017-03-30 | ||
| CNPCT/CN2017/078792 | 2017-03-30 | ||
| CNPCT/CN2018/076909 | 2018-02-15 | ||
| CN2018076909 | 2018-02-15 | ||
| PCT/US2018/025562 WO2018183956A1 (en) | 2017-03-30 | 2018-03-30 | Naphthyridines as inhibitors of hpk1 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20190136028A true KR20190136028A (ko) | 2019-12-09 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197031494A Ceased KR20190136028A (ko) | 2017-03-30 | 2018-03-30 | Hpk1 억제제로서의 나프티리딘 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US10407424B2 (enExample) |
| EP (1) | EP3601284B1 (enExample) |
| JP (1) | JP7154221B2 (enExample) |
| KR (1) | KR20190136028A (enExample) |
| CN (1) | CN110678466B (enExample) |
| AU (1) | AU2018244935A1 (enExample) |
| BR (1) | BR112019018093A2 (enExample) |
| CA (1) | CA3052492A1 (enExample) |
| IL (1) | IL268262A (enExample) |
| MX (1) | MX2019011511A (enExample) |
| TW (1) | TW201904964A (enExample) |
| WO (1) | WO2018183956A1 (enExample) |
Families Citing this family (83)
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| AU2018244935A1 (en) * | 2017-03-30 | 2019-08-15 | F. Hoffmann-La Roche Ag | Naphthyridines as inhibitors of HPK1 |
| JP6836693B2 (ja) * | 2017-09-28 | 2021-03-03 | シーストーン・ファーマスーティカルズ・(スージョウ)・カンパニー・リミテッドCstone Pharmaceuticals (Suzhou) Co., Ltd. | A2a受容体アンタゴニストとしての縮合環誘導体 |
| EP3707138B1 (en) | 2017-11-06 | 2022-07-13 | Bristol-Myers Squibb Company | Isofuranone compounds useful as hpk1 inhibitors |
| CR20200347A (es) | 2018-02-13 | 2020-09-23 | Gilead Sciences Inc | Inhibidores pd-1/pd-l1 |
| EP3765459A1 (en) | 2018-03-13 | 2021-01-20 | Shire Human Genetic Therapies, Inc. | Substituted imidazopyridines as inhibitors of plasma kallikrein and uses thereof |
| TWI712412B (zh) | 2018-04-19 | 2020-12-11 | 美商基利科學股份有限公司 | Pd‐1/pd‐l1抑制劑 |
| SG11202012425QA (en) | 2018-07-13 | 2021-01-28 | Gilead Sciences Inc | Pd-1/pd-l1 inhibitors |
| TW202012405A (zh) * | 2018-07-24 | 2020-04-01 | 瑞士商赫孚孟拉羅股份公司 | 萘啶化合物及其用途 |
| EP3856724A1 (en) * | 2018-09-30 | 2021-08-04 | F. Hoffmann-La Roche AG | Cinnoline compounds and for the treatment of hpk1-dependent disorders such as cancer |
| US11203591B2 (en) | 2018-10-31 | 2021-12-21 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds |
| WO2020092528A1 (en) | 2018-10-31 | 2020-05-07 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity |
| WO2020120257A1 (en) | 2018-12-11 | 2020-06-18 | Bayer Aktiengesellschaft | Substituted pyrrolopyridine-derivatives |
| US12492194B2 (en) | 2019-03-26 | 2025-12-09 | Janssen Pharmaceutica Nv | HPK1 inhibitors |
| US12486264B2 (en) | 2019-03-26 | 2025-12-02 | Janssen Pharmaceutica Nv | Bicyclic HPK1 inhibitors |
| EP3972695A1 (en) | 2019-05-23 | 2022-03-30 | Gilead Sciences, Inc. | Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors |
| WO2020263830A1 (en) | 2019-06-25 | 2020-12-30 | Gilead Sciences, Inc. | Flt3l-fc fusion proteins and methods of use |
| TWI848141B (zh) | 2019-07-04 | 2024-07-11 | 英屬開曼群島商百濟神州有限公司 | 及其用途 |
| TW202116753A (zh) * | 2019-07-11 | 2021-05-01 | 大陸商南京征祥醫藥有限公司 | 以噌啉作為hpk1的抑制劑 |
| US12459958B2 (en) | 2019-07-17 | 2025-11-04 | Beone Medicines I Gmbh | Tricyclic compounds as HPK1 inhibitor and the use thereof |
| CN110483402B (zh) * | 2019-08-12 | 2021-07-23 | 上海毕得医药科技股份有限公司 | 一种3-溴-5-苯基-1h-吡唑的合成方法 |
| WO2021032148A1 (en) * | 2019-08-21 | 2021-02-25 | Beigene, Ltd. | Aminopyrazine compounds as hpk1 inhibitor and the use thereof |
| MX2022002877A (es) * | 2019-09-13 | 2022-08-08 | Nimbus Saturn Inc | Antagonistas de cinasa progenitora hematopoyetica 1 (hpk1) y sus usos. |
| DK4031547T3 (da) | 2019-09-18 | 2024-09-09 | Takeda Pharmaceuticals Co | Plasmakallikreininhibitorer og anvendelser deraf |
| EP4031245A1 (en) | 2019-09-18 | 2022-07-27 | Takeda Pharmaceutical Company Limited | Heteroaryl plasma kallikrein inhibitors |
| ES2973832T3 (es) | 2019-10-18 | 2024-06-24 | Forty Seven Inc | Terapias combinadas para el tratamiento de síndromes mielodisplásicos y leucemia mieloide aguda |
| JP2022552748A (ja) | 2019-10-31 | 2022-12-19 | フォーティ セブン, インコーポレイテッド | 抗cd47及び抗cd20による血液癌の治療 |
| TWI778443B (zh) | 2019-11-12 | 2022-09-21 | 美商基利科學股份有限公司 | Mcl1抑制劑 |
| IL294032A (en) | 2019-12-24 | 2022-08-01 | Carna Biosciences Inc | Compounds that regulate diacylglycerol kinase |
| TW202140473A (zh) * | 2020-01-15 | 2021-11-01 | 美商纜圖藥品公司 | Map4k1抑制劑 |
| TWI890283B (zh) | 2020-02-14 | 2025-07-11 | 美商基利科學股份有限公司 | 結合ccr8之抗體及融合蛋白及其用途 |
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| MX2019011511A (es) | 2019-11-18 |
| EP3601284C0 (en) | 2023-12-27 |
| WO2018183956A1 (en) | 2018-10-04 |
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