AR124007A1 - Inhibidores de la kinasa ret - Google Patents
Inhibidores de la kinasa retInfo
- Publication number
- AR124007A1 AR124007A1 ARP210103078A ARP210103078A AR124007A1 AR 124007 A1 AR124007 A1 AR 124007A1 AR P210103078 A ARP210103078 A AR P210103078A AR P210103078 A ARP210103078 A AR P210103078A AR 124007 A1 AR124007 A1 AR 124007A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halogen
- substituted
- heteroalkyl
- tri
- Prior art date
Links
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- -1 dimethylphosphoryl Chemical group 0.000 abstract 9
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- BAVYZALUXZFZLV-UHFFFAOYSA-N Methylamine Chemical compound NC BAVYZALUXZFZLV-UHFFFAOYSA-N 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 2
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000004953 trihalomethyl group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 abstract 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 1
- 125000006519 CCH3 Chemical group 0.000 abstract 1
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000004951 trihalomethoxy group Chemical group 0.000 abstract 1
- GETQZCLCWQTVFV-UHFFFAOYSA-N trimethylamine Chemical compound CN(C)C GETQZCLCWQTVFV-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/38—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Reivindicación 1: Un compuesto de la fórmula (1) en donde A es arilo C₆₋₁₀ o heteroarilo C₅₋₆; cada R¹ es independientemente hidrógeno, halógeno, alquilo C₁₋₆, heteroalquilo C₁₋₆, -(alquilo C₁₋₄)(heteroalquilo C₅₋₆), -(alquilo C₀₋₄)(cicloalquilo C₃₋₇), -(heteroalquilo C₀₋₄)(cicloalquilo C₃₋₇), -(alquilo C₀₋₄)(cicloheteroalquilo C₃₋₇), -(heteroalquilo C₀₋₄)(cicloheteroalquilo C₃₋₇), -(alquilo C₀₋₄)(biciclilo C₄₋₁₀), -(alquilo C₀₋₄)(arilo C₅₋₆), -(alquilo C₀₋₄)(heteroarilo C₅₋₆), -(alquilo C₀₋₄)(heterobiciclilo C₄₋₁₀), espiranilo C₅₋₁₂, heteroespiranilo C₅₋₁₂, dimetilfosforilo, adamantilo, alcoxi C₁₋₆, -(alquilo C₁₋₄)-SO₂-(alquilo C₁₋₄), difluorometilsulfanilo, o pentafluorosulfanilo, en donde cada R¹ no se sustituye o cuando es capaz de ser sustituida, se sustituye con uno o más sustituyentes que se seleccionan independientemente del grupo que consiste en halógeno, ciano, hidroxilo, oxo, metilo, metoxi, hidroximetilo, etilo, etoxi, hidroxietilo, metilamina, N,N-dimetilmetilamina, mono-, di-, o tri-halometoxi, mono-, di-, o tri-halometilo, y alquil C₀₋₃-pirrolidinilo, donde el grupo pirrolidinilo no se sustituye o se sustituye con uno, dos o 3 átomos de halógeno seleccionados independientemente, y en donde dos grupos R¹ se pueden fusionar para formar una estructura de anillo que incluye una porción de A y es opcionalmente aromática, y n es 1, 2, 3, 4, 5, ó 6; X¹, X², X³, y X⁴ son cada uno independientemente N, CH, C-CH₃, C-CH₂-OH, COCH₃, C-CH₂-OCH₃, o C-halógeno; y R² es alquilo C₁₋₆, -(alquilo C₀₋₄)(cicloalquilo C₃₋₇), -(alquilo C₀₋₄)(heterocicloalquilo C₄₋₇), -(alquilo C₀₋₄)(bicíclico C₄₋₁₀) cada uno opcionalmente sustituido con uno o más de halógeno, ciano, hidroxilo, oxo, metilo, metoxi, hidroximetilo, etilo, etoxi, hidroxietilo, ciclopropilo, o mono-, di-, o tri-halometilo; o una sal farmacéuticamente aceptable de este.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063110643P | 2020-11-06 | 2020-11-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR124007A1 true AR124007A1 (es) | 2023-02-01 |
Family
ID=78806726
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP210103078A AR124007A1 (es) | 2020-11-06 | 2021-11-05 | Inhibidores de la kinasa ret |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US11697647B2 (es) |
| EP (1) | EP4240738A1 (es) |
| JP (2) | JP7338072B2 (es) |
| KR (1) | KR20230104146A (es) |
| CN (1) | CN116438179A (es) |
| AR (1) | AR124007A1 (es) |
| AU (1) | AU2021376367B2 (es) |
| CA (1) | CA3197032A1 (es) |
| CL (1) | CL2023001277A1 (es) |
| CO (1) | CO2023005600A2 (es) |
| CR (1) | CR20230193A (es) |
| DO (1) | DOP2023000088A (es) |
| EC (1) | ECSP23033180A (es) |
| IL (1) | IL302542A (es) |
| MX (1) | MX2023005289A (es) |
| PE (1) | PE20231984A1 (es) |
| TW (2) | TW202315623A (es) |
| WO (1) | WO2022098970A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116438179A (zh) * | 2020-11-06 | 2023-07-14 | 伊莱利利公司 | 作为ret激酶抑制剂的吡唑衍生物 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016516026A (ja) * | 2013-03-15 | 2016-06-02 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | Ｒｅａｒｒａｎｇｅｄｄｕｒｉｎｇｔｒａｎｓｆｅｃｔｉｏｎ（ｒｅｔ）キナーゼ阻害剤としてのピリジン誘導体 |
| WO2017145050A1 (en) * | 2016-02-23 | 2017-08-31 | Glaxosmithkline Intellectual Property Development Limited | Pyridylpyridone derivative useful as a ret kinase inhibitor in the treatment of ibs and cancer |
| US10183928B2 (en) | 2016-03-17 | 2019-01-22 | Blueprint Medicines Corporation | Inhibitors of RET |
| WO2020035065A1 (zh) | 2018-08-17 | 2020-02-20 | 南京明德新药研发有限公司 | 作为ret抑制剂的吡唑衍生物 |
| TWI777509B (zh) | 2020-04-27 | 2022-09-11 | 美商美國禮來大藥廠 | 用於抑制ret激酶之化合物 |
| CN116438179A (zh) * | 2020-11-06 | 2023-07-14 | 伊莱利利公司 | 作为ret激酶抑制剂的吡唑衍生物 |
-
2021
- 2021-11-05 CN CN202180074242.3A patent/CN116438179A/zh active Pending
- 2021-11-05 TW TW111149771A patent/TW202315623A/zh unknown
- 2021-11-05 US US17/519,878 patent/US11697647B2/en active Active
- 2021-11-05 IL IL302542A patent/IL302542A/en unknown
- 2021-11-05 PE PE2023001567A patent/PE20231984A1/es unknown
- 2021-11-05 JP JP2022549002A patent/JP7338072B2/ja active Active
- 2021-11-05 TW TW110141379A patent/TWI790810B/zh active
- 2021-11-05 AR ARP210103078A patent/AR124007A1/es unknown
- 2021-11-05 KR KR1020237014916A patent/KR20230104146A/ko unknown
- 2021-11-05 WO PCT/US2021/058206 patent/WO2022098970A1/en active Application Filing
- 2021-11-05 CA CA3197032A patent/CA3197032A1/en active Pending
- 2021-11-05 EP EP21815830.1A patent/EP4240738A1/en active Pending
- 2021-11-05 CR CR20230193A patent/CR20230193A/es unknown
- 2021-11-05 MX MX2023005289A patent/MX2023005289A/es unknown
- 2021-11-05 AU AU2021376367A patent/AU2021376367B2/en active Active
-
2022
- 2022-10-19 US US18/047,794 patent/US11970485B2/en active Active
-
2023
- 2023-04-28 JP JP2023074122A patent/JP2023099116A/ja active Pending
- 2023-05-02 CO CONC2023/0005600A patent/CO2023005600A2/es unknown
- 2023-05-03 CL CL2023001277A patent/CL2023001277A1/es unknown
- 2023-05-05 DO DO2023000088A patent/DOP2023000088A/es unknown
- 2023-05-05 EC ECSENADI202333180A patent/ECSP23033180A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP4240738A1 (en) | 2023-09-13 |
| KR20230104146A (ko) | 2023-07-07 |
| TW202233180A (zh) | 2022-09-01 |
| US20220144816A1 (en) | 2022-05-12 |
| US20230265085A1 (en) | 2023-08-24 |
| PE20231984A1 (es) | 2023-12-12 |
| AU2021376367A1 (en) | 2023-05-11 |
| DOP2023000088A (es) | 2023-07-16 |
| CO2023005600A2 (es) | 2023-05-29 |
| AU2021376367A9 (en) | 2023-07-13 |
| JP2023504303A (ja) | 2023-02-02 |
| MX2023005289A (es) | 2023-07-26 |
| WO2022098970A1 (en) | 2022-05-12 |
| CN116438179A (zh) | 2023-07-14 |
| US11697647B2 (en) | 2023-07-11 |
| US11970485B2 (en) | 2024-04-30 |
| TW202315623A (zh) | 2023-04-16 |
| WO2022098970A9 (en) | 2023-04-27 |
| CA3197032A1 (en) | 2022-05-12 |
| AU2021376367B2 (en) | 2024-08-01 |
| CR20230193A (es) | 2023-07-03 |
| IL302542A (en) | 2023-07-01 |
| JP2023099116A (ja) | 2023-07-11 |
| JP7338072B2 (ja) | 2023-09-04 |
| ECSP23033180A (es) | 2023-06-30 |
| TWI790810B (zh) | 2023-01-21 |
| CL2023001277A1 (es) | 2023-12-01 |
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