PE20231984A1 - Derivados de pirazol como inhibidores de la ret-cinasa - Google Patents
Derivados de pirazol como inhibidores de la ret-cinasaInfo
- Publication number
- PE20231984A1 PE20231984A1 PE2023001567A PE2023001567A PE20231984A1 PE 20231984 A1 PE20231984 A1 PE 20231984A1 PE 2023001567 A PE2023001567 A PE 2023001567A PE 2023001567 A PE2023001567 A PE 2023001567A PE 20231984 A1 PE20231984 A1 PE 20231984A1
- Authority
- PE
- Peru
- Prior art keywords
- ret
- amino
- alkyl
- cancer
- compounds
- Prior art date
Links
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical class C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 206010028980 Neoplasm Diseases 0.000 abstract 3
- 201000011510 cancer Diseases 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- GKEPAOKVEUKXHF-UHFFFAOYSA-N CC(C)N(C(N)=C1C(N)=O)N=C1C1=CC=C(CC(NC2=CC(C(C3)(C4)CC34F)=NO2)=O)C=C1 Chemical compound CC(C)N(C(N)=C1C(N)=O)N=C1C1=CC=C(CC(NC2=CC(C(C3)(C4)CC34F)=NO2)=O)C=C1 GKEPAOKVEUKXHF-UHFFFAOYSA-N 0.000 abstract 1
- GBXBLLBTMYCMRH-UHFFFAOYSA-N CC(C)N(C(N)=C1C(N)=O)N=C1C1=CC=C(CC(NC2=CC(CC3(C)CC3)=NO2)=O)C=C1 Chemical compound CC(C)N(C(N)=C1C(N)=O)N=C1C1=CC=C(CC(NC2=CC(CC3(C)CC3)=NO2)=O)C=C1 GBXBLLBTMYCMRH-UHFFFAOYSA-N 0.000 abstract 1
- 125000006519 CCH3 Chemical group 0.000 abstract 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 abstract 1
- 208000009018 Medullary thyroid cancer Diseases 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 230000004927 fusion Effects 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 201000005202 lung cancer Diseases 0.000 abstract 1
- 208000020816 lung neoplasm Diseases 0.000 abstract 1
- 208000023356 medullary thyroid gland carcinoma Diseases 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
Abstract
Esta referido a compuestos con la formula general descrita a continuacion, en donde: R1 es H, halogeno, alquilo, heteroalquilo, entre otras opciones; R2 es alquilo, alquilo-cicloalquilo, alquilo-heterociloalquilo, entre otras opciones; A es arilo o heteroarilo; X1, X2, X3 y X4 son N, CH, C-CH3, C-CH2-OH, C-OCH3, C-CH2-OCH3, o C-halogeno; y n es 1, 2, 3, 4, 5, o 6. Entre los compuestos preferidos de la invencion tenemos los siguientes: 5-Amino-1-isopropil-3-(4-(2-((3-((1-metilciclopropil)metil)isoxazol-5-il)amino)-2-oxoetil)fenil)-1H-pirazol-4-carboxamida; 5-Amino-3-(4-(2-((3-(3-fluorobiciclo[1.1.1] pentan-1-il)isoxazol-5-il)amino)-2-oxoetil)fenil)-1- isopropilo-1H-pirazol-4-carboxamida; entre otros. Estos compuestos son inhibidores de la quinasa RET y se emplean para tratar el cancer, en particular para el tratamiento del cancer con expresion anormal de RET (por ejemplo, un cancer que se asocia a RET como el cancer medular de tiroides o el cancer de pulmon de fusion de RET).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063110643P | 2020-11-06 | 2020-11-06 | |
| PCT/US2021/058206 WO2022098970A1 (en) | 2020-11-06 | 2021-11-05 | Pyrazole derivatives asr et kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20231984A1 true PE20231984A1 (es) | 2023-12-12 |
Family
ID=78806726
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2023001567A PE20231984A1 (es) | 2020-11-06 | 2021-11-05 | Derivados de pirazol como inhibidores de la ret-cinasa |
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) | AU2021376367A1 (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) | TWI790810B (es) |
| WO (1) | WO2022098970A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20230193A (es) * | 2020-11-06 | 2023-07-03 | Lilly Co Eli | Derivados de pirazol como inhibidores de la ret-cinasa |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105051027A (zh) * | 2013-03-15 | 2015-11-11 | 葛兰素史密斯克莱知识产权发展有限公司 | 作为转染期间重排(ret)激酶抑制剂的吡啶衍生物 |
| 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 |
| TW201738228A (zh) | 2016-03-17 | 2017-11-01 | 藍圖醫藥公司 | Ｒｅｔ之抑制劑 |
| 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 |
| AR121914A1 (es) * | 2020-04-27 | 2022-07-20 | Lilly Co Eli | Compuestos útiles para inhibir la quinasa ret |
| CR20230193A (es) * | 2020-11-06 | 2023-07-03 | Lilly Co Eli | Derivados de pirazol como inhibidores de la ret-cinasa |
-
2021
- 2021-11-05 CR CR20230193A patent/CR20230193A/es unknown
- 2021-11-05 CN CN202180074242.3A patent/CN116438179A/zh active Pending
- 2021-11-05 IL IL302542A patent/IL302542A/en unknown
- 2021-11-05 KR KR1020237014916A patent/KR20230104146A/ko unknown
- 2021-11-05 JP JP2022549002A patent/JP7338072B2/ja active Active
- 2021-11-05 CA CA3197032A patent/CA3197032A1/en active Pending
- 2021-11-05 PE PE2023001567A patent/PE20231984A1/es unknown
- 2021-11-05 TW TW110141379A patent/TWI790810B/zh active
- 2021-11-05 TW TW111149771A patent/TW202315623A/zh unknown
- 2021-11-05 US US17/519,878 patent/US11697647B2/en active Active
- 2021-11-05 MX MX2023005289A patent/MX2023005289A/es unknown
- 2021-11-05 AU AU2021376367A patent/AU2021376367A1/en active Pending
- 2021-11-05 EP EP21815830.1A patent/EP4240738A1/en active Pending
- 2021-11-05 AR ARP210103078A patent/AR124007A1/es unknown
- 2021-11-05 WO PCT/US2021/058206 patent/WO2022098970A1/en active Application Filing
-
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 |
|---|---|
| JP7338072B2 (ja) | 2023-09-04 |
| AU2021376367A1 (en) | 2023-05-11 |
| ECSP23033180A (es) | 2023-06-30 |
| TW202315623A (zh) | 2023-04-16 |
| EP4240738A1 (en) | 2023-09-13 |
| AR124007A1 (es) | 2023-02-01 |
| TW202233180A (zh) | 2022-09-01 |
| CN116438179A (zh) | 2023-07-14 |
| JP2023099116A (ja) | 2023-07-11 |
| MX2023005289A (es) | 2023-07-26 |
| US11697647B2 (en) | 2023-07-11 |
| TWI790810B (zh) | 2023-01-21 |
| AU2021376367A9 (en) | 2023-07-13 |
| CR20230193A (es) | 2023-07-03 |
| DOP2023000088A (es) | 2023-07-16 |
| IL302542A (en) | 2023-07-01 |
| JP2023504303A (ja) | 2023-02-02 |
| US11970485B2 (en) | 2024-04-30 |
| WO2022098970A9 (en) | 2023-04-27 |
| WO2022098970A1 (en) | 2022-05-12 |
| US20220144816A1 (en) | 2022-05-12 |
| CO2023005600A2 (es) | 2023-05-29 |
| CA3197032A1 (en) | 2022-05-12 |
| CL2023001277A1 (es) | 2023-12-01 |
| KR20230104146A (ko) | 2023-07-07 |
| US20230265085A1 (en) | 2023-08-24 |
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