MD3880676T2 - Derivați de 2,3-dihidro-1H-pirolo[3,4-c]piridin-1-onă în calitate de inhibitori ai HPK1 pentru tratamentul cancerului - Google Patents
Derivați de 2,3-dihidro-1H-pirolo[3,4-c]piridin-1-onă în calitate de inhibitori ai HPK1 pentru tratamentul canceruluiInfo
- Publication number
- MD3880676T2 MD3880676T2 MDE20210902T MDE20210902T MD3880676T2 MD 3880676 T2 MD3880676 T2 MD 3880676T2 MD E20210902 T MDE20210902 T MD E20210902T MD E20210902 T MDE20210902 T MD E20210902T MD 3880676 T2 MD3880676 T2 MD 3880676T2
- Authority
- MD
- Moldova
- Prior art keywords
- pyridin
- dihydro
- derivatives
- treatment
- cancer
- Prior art date
Links
- 102100028199 Mitogen-activated protein kinase kinase kinase kinase 1 Human genes 0.000 title abstract 3
- 206010028980 Neoplasm Diseases 0.000 title abstract 2
- 201000011510 cancer Diseases 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- QDSJMVZVUSYEMY-UHFFFAOYSA-N 2,3-dihydropyrrolo[3,4-c]pyridin-1-one Chemical class N1=CC=C2C(=O)NCC2=C1 QDSJMVZVUSYEMY-UHFFFAOYSA-N 0.000 title 1
- 101001059991 Homo sapiens Mitogen-activated protein kinase kinase kinase kinase 1 Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 108010002838 hematopoietic progenitor kinase 1 Proteins 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 230000010261 cell growth Effects 0.000 abstract 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Prezenta invenţie se referă la derivaţi de 2,3-dihidro-1H-pirol[3,4-c]piridin-1-onă cu formula generală (I) şi sărurile lor farmaceutic acceptabile ca inhibitori ai kinazei 1 a progenitorilor hematopoietici (HPK1), în care R1, R1a, R2, R3, R4 şi (R5)a au semnificaţiile definite în prezenta invenţie, la compoziţii farmaceutice care cuprind astfel de compuşi şi la compoziţii pentru tratamentul creşterii anormale a celulelor, inclusiv al cancerului. Un exemplu de compus specific este, de exemplu, 4-[(metilamino)metil]-6- [metil(propan-2-il)amino]-2-[6-(4-propil-4H-1,2,4-triazol-3-il) piridin-2-il]-2,3-dihidro-1H-pirol]3,4-c]piridin-1-onă. Prezenta descriere prezintă prepararea unor exemple de compuşi, precum şi datele farmacologice ale acestora(de exemplu, paginile 82-211; exemplele 1-188; tabelele 1-5).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862767602P | 2018-11-15 | 2018-11-15 | |
| US201962909970P | 2019-10-03 | 2019-10-03 | |
| PCT/IB2019/059702 WO2020100027A1 (en) | 2018-11-15 | 2019-11-12 | 2,3-dihydro-1h-pyrrolo[3,4-c]pyridin-1-one derivatives as hpk1 inhibitors for the treatment of cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MD3880676T2 true MD3880676T2 (ro) | 2023-12-31 |
Family
ID=68771726
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MDE20210902T MD3880676T2 (ro) | 2018-11-15 | 2019-11-12 | Derivați de 2,3-dihidro-1H-pirolo[3,4-c]piridin-1-onă în calitate de inhibitori ai HPK1 pentru tratamentul cancerului |
Country Status (36)
| Country | Link |
|---|---|
| US (1) | US11142525B2 (ro) |
| EP (1) | EP3880676B1 (ro) |
| JP (1) | JP7118267B2 (ro) |
| KR (1) | KR20210090675A (ro) |
| CN (1) | CN113316576A (ro) |
| AU (1) | AU2019378184B2 (ro) |
| BR (1) | BR112021008991A2 (ro) |
| CA (1) | CA3061392A1 (ro) |
| CL (1) | CL2021001190A1 (ro) |
| CO (1) | CO2021006114A2 (ro) |
| CR (1) | CR20210251A (ro) |
| CU (1) | CU20210035A7 (ro) |
| DK (1) | DK3880676T3 (ro) |
| DO (1) | DOP2021000088A (ro) |
| EC (1) | ECSP21034668A (ro) |
| ES (1) | ES2958948T3 (ro) |
| FI (1) | FI3880676T3 (ro) |
| GE (1) | GEP20227434B (ro) |
| HR (1) | HRP20231089T1 (ro) |
| HU (1) | HUE063367T2 (ro) |
| IL (1) | IL283149A (ro) |
| LT (1) | LT3880676T (ro) |
| MD (1) | MD3880676T2 (ro) |
| MX (1) | MX2021005754A (ro) |
| PE (1) | PE20211868A1 (ro) |
| PH (1) | PH12021551117A1 (ro) |
| PL (1) | PL3880676T3 (ro) |
| PT (1) | PT3880676T (ro) |
| RS (1) | RS64655B1 (ro) |
| SG (1) | SG11202104394XA (ro) |
| SI (1) | SI3880676T1 (ro) |
| TW (1) | TWI718758B (ro) |
| UA (1) | UA127426C2 (ro) |
| UY (1) | UY38471A (ro) |
| WO (1) | WO2020100027A1 (ro) |
| ZA (1) | ZA202103099B (ro) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113227089A (zh) | 2018-10-31 | 2021-08-06 | 吉利德科学公司 | 作为hpk1抑制剂的取代的6-氮杂苯并咪唑化合物 |
| CA3116347A1 (en) | 2018-10-31 | 2020-05-07 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity |
| EP3972695A1 (en) | 2019-05-23 | 2022-03-30 | Gilead Sciences, Inc. | Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors |
| CR20220548A (es) * | 2020-05-01 | 2022-12-12 | Pfizer | Compuestos de azalactama como inhibidores de hpk1 |
| CN112409268A (zh) * | 2020-12-03 | 2021-02-26 | 西南交通大学 | 靶向Fam20C抑制剂的制备及其抗三阴性乳腺癌作用 |
| WO2022258044A1 (zh) * | 2021-06-11 | 2022-12-15 | 杭州中美华东制药有限公司 | 吡咯并吡啶酮类化合物及其制备方法和用途 |
| EP4373817A1 (en) | 2021-07-20 | 2024-05-29 | Astrazeneca AB | Substituted pyrazine-2-carboxamides as hpk1 inhibitors for the treatment of cancer |
| WO2023023942A1 (en) * | 2021-08-24 | 2023-03-02 | Biofront Ltd (Cayman) | Hpk1 inhibitors, compositions comprising hpk1 inhibitor, and methods of using the same |
| CN118103369A (zh) * | 2021-09-03 | 2024-05-28 | 浙江海正药业股份有限公司 | 吡啶并内酰胺类衍生物及其制备方法和用途 |
| WO2023057883A1 (en) * | 2021-10-05 | 2023-04-13 | Pfizer Inc. | Crystalline form of azalactam compound |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| US5243049A (en) * | 1992-01-22 | 1993-09-07 | Neurogen Corporation | Certain pyrroloquinolinones: a new class of GABA brain receptor ligands |
| GB9518953D0 (en) | 1995-09-15 | 1995-11-15 | Pfizer Ltd | Pharmaceutical formulations |
| WO2000035298A1 (en) | 1996-11-27 | 2000-06-22 | Wm. Wrigley Jr. Company | Chewing gum containing medicament active agents |
| GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| EP2178861B1 (en) * | 2007-07-19 | 2014-08-20 | Merck Sharp & Dohme Corp. | Heterocyclic amide compounds as protein kinase inhibitors |
| CA3041033A1 (en) | 2016-09-12 | 2018-03-15 | Numerate, Inc. | Monocyclic compounds useful as gpr120 modulators |
| CN110402248B (zh) | 2017-03-15 | 2023-01-06 | 豪夫迈·罗氏有限公司 | 作为hpk1抑制剂的氮杂吲哚类 |
| TW201908306A (zh) | 2017-07-18 | 2019-03-01 | 大陸商南京聖和藥業股份有限公司 | 作為ask抑制劑的雜環化合物及其應用 |
| WO2019148005A1 (en) | 2018-01-26 | 2019-08-01 | Nurix Therapeutics, Inc. | Inhibitors of cbl-b and methods of use thereof |
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2019
- 2019-11-11 US US16/679,820 patent/US11142525B2/en active Active
- 2019-11-12 HR HRP20231089TT patent/HRP20231089T1/hr unknown
- 2019-11-12 CR CR20210251A patent/CR20210251A/es unknown
- 2019-11-12 MD MDE20210902T patent/MD3880676T2/ro unknown
- 2019-11-12 PE PE2021000685A patent/PE20211868A1/es unknown
- 2019-11-12 CA CA3061392A patent/CA3061392A1/en active Pending
- 2019-11-12 JP JP2021525702A patent/JP7118267B2/ja active Active
- 2019-11-12 WO PCT/IB2019/059702 patent/WO2020100027A1/en active Application Filing
- 2019-11-12 ES ES19813943T patent/ES2958948T3/es active Active
- 2019-11-12 CU CU2021000035A patent/CU20210035A7/es unknown
- 2019-11-12 UA UAA202102538A patent/UA127426C2/uk unknown
- 2019-11-12 HU HUE19813943A patent/HUE063367T2/hu unknown
- 2019-11-12 LT LTEPPCT/IB2019/059702T patent/LT3880676T/lt unknown
- 2019-11-12 SI SI201930620T patent/SI3880676T1/sl unknown
- 2019-11-12 BR BR112021008991-8A patent/BR112021008991A2/pt unknown
- 2019-11-12 RS RS20230847A patent/RS64655B1/sr unknown
- 2019-11-12 PL PL19813943.8T patent/PL3880676T3/pl unknown
- 2019-11-12 DK DK19813943.8T patent/DK3880676T3/da active
- 2019-11-12 FI FIEP19813943.8T patent/FI3880676T3/fi active
- 2019-11-12 CN CN201980089161.3A patent/CN113316576A/zh active Pending
- 2019-11-12 EP EP19813943.8A patent/EP3880676B1/en active Active
- 2019-11-12 MX MX2021005754A patent/MX2021005754A/es unknown
- 2019-11-12 GE GEAP201915630A patent/GEP20227434B/en unknown
- 2019-11-12 KR KR1020217017777A patent/KR20210090675A/ko active IP Right Grant
- 2019-11-12 AU AU2019378184A patent/AU2019378184B2/en active Active
- 2019-11-12 SG SG11202104394XA patent/SG11202104394XA/en unknown
- 2019-11-12 PT PT198139438T patent/PT3880676T/pt unknown
- 2019-11-14 UY UY0001038471A patent/UY38471A/es unknown
- 2019-11-14 TW TW108141429A patent/TWI718758B/zh active
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2021
- 2021-05-06 CL CL2021001190A patent/CL2021001190A1/es unknown
- 2021-05-07 DO DO2021000088A patent/DOP2021000088A/es unknown
- 2021-05-07 ZA ZA2021/03099A patent/ZA202103099B/en unknown
- 2021-05-11 CO CONC2021/0006114A patent/CO2021006114A2/es unknown
- 2021-05-12 IL IL283149A patent/IL283149A/en unknown
- 2021-05-14 PH PH12021551117A patent/PH12021551117A1/en unknown
- 2021-05-14 EC ECSENADI202134668A patent/ECSP21034668A/es unknown
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