PE20240687A1 - Compuestos de indazol como inhibidores de cinasas - Google Patents
Compuestos de indazol como inhibidores de cinasasInfo
- Publication number
- PE20240687A1 PE20240687A1 PE2023001961A PE2023001961A PE20240687A1 PE 20240687 A1 PE20240687 A1 PE 20240687A1 PE 2023001961 A PE2023001961 A PE 2023001961A PE 2023001961 A PE2023001961 A PE 2023001961A PE 20240687 A1 PE20240687 A1 PE 20240687A1
- Authority
- PE
- Peru
- Prior art keywords
- carbon atom
- membered
- alkyl
- ring
- optionally substituted
- Prior art date
Links
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical class C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 229910052799 carbon Inorganic materials 0.000 abstract 8
- 150000001721 carbon Chemical group 0.000 abstract 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000004432 carbon atom Chemical group C* 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000003453 indazolyl group Chemical class N1N=C(C2=C1C=CC=C2)* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
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- 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
- C07D401/14—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 three or more hetero 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
- A61K31/444—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
- 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
- A61K31/495—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
-
- 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
- A61K31/495—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
-
- 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
- A61K31/535—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
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- 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
- C07D417/14—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
-
- 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
- C07D471/10—Spiro-condensed systems
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- 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
- C07D487/10—Spiro-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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
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)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
La presente invencion se refiere a un compuesto de formula (I), o una sal farmaceuticamente aceptable del mismo, donde n = 1, 2 o 3; m = 0, 1, 2 o 3; cada R1 es independientemente H, CN o alquilo C1-C6 opcionalmente sustituido; cada R2 es independientemente H, CN o alquilo C1-C6 opcionalmente sustituido; o dos grupos R1 unidos al mismo atomo de carbono, junto con el atomo de carbono al que ambos estan unidos forman un anillo espirocicloalquilo de 3-7 miembros opcionalmente sustituido o un anillo espiroheterocicloalquilo de 3-7 miembros opcionalmente sustituido; o dos grupos R1 unidos al mismo atomo de carbono, junto con ese atomo de carbono, representan un grupo carbonilo (C=O); o dos grupos R2 unidos al mismo atomo de carbono, junto con el atomo de carbono al que ambos estan unidos forman un anillo espirocicloalquilo de 3-7 miembros opcionalmente sustituido o un anillo espiroheterocicloalquilo de 3-7 miembros opcionalmente sustituido; o dos grupos R2 unidos al mismo atomo de carbono, junto con ese atomo de carbono, representan un grupo carbonilo (C=O); o dos grupos R1 unidos a diferentes atomos de carbono, junto con los atomos de carbono a los que estan unidos, forman un anillo cicloalquilo de 3-7 miembros; o dos grupos R2 unidos a diferentes atomos de carbono, junto con los atomos de carbono a los que estan unidos, forman un anillo cicloalquilo de 3-7 miembros; o un grupo R1 y un grupo R2 estan unidos para formar un anillo biciclico puenteado de 6-9 miembros; A = N o CH; Z = S(O)2; S(O); O, entre otros; Y es un anillo heteroarilo de 5 o 6 miembros o un anillo arilo de 6 miembros; Q5, Q6, Q7, Q8 y Q9, son cada uno independientemente N o CR5, en donde uno o dos de Q5, Q6, Q7, Q8 y Q9 son N y el resto son CR5; R5 es H, halogeno, alquilo C1-C3, entre otros; X = O, S o NR, en donde R es H o alquilo C1-C3; R6 es alquilo C1-C6; R7 es H, halogeno, -alquilo C1-C6, entre otros; y R8 es H, halogeno, -alquilo C1-C6, entre otros. Asimismo, sus composiciones farmaceuticas que incluyen uno o mas de dichos compuestos de indazol o una sal farmaceuticamente aceptable del mismo, y un excipiente farmaceuticamente aceptable son utiles en el tratamiento del cancer.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063132031P | 2020-12-30 | 2020-12-30 | |
| US202163216879P | 2021-06-30 | 2021-06-30 | |
| PCT/US2021/065679 WO2022147246A1 (en) | 2020-12-30 | 2021-12-30 | Indazole compounds as kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20240687A1 true PE20240687A1 (es) | 2024-04-10 |
Family
ID=80168316
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2023001961A PE20240687A1 (es) | 2020-12-30 | 2021-12-30 | Compuestos de indazol como inhibidores de cinasas |
Country Status (16)
| Country | Link |
|---|---|
| US (3) | US12264149B2 (es) |
| EP (1) | EP4271673A1 (es) |
| JP (1) | JP7791196B2 (es) |
| KR (1) | KR20230152654A (es) |
| AU (1) | AU2021411587B2 (es) |
| CA (1) | CA3205986A1 (es) |
| CL (1) | CL2023001951A1 (es) |
| CO (1) | CO2023008689A2 (es) |
| CR (1) | CR20230325A (es) |
| EC (1) | ECSP23048136A (es) |
| IL (1) | IL304014A (es) |
| MX (1) | MX2023007793A (es) |
| PE (1) | PE20240687A1 (es) |
| TW (1) | TW202241906A (es) |
| WO (1) | WO2022147246A1 (es) |
| ZA (1) | ZA202306559B (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021138391A1 (en) | 2019-12-30 | 2021-07-08 | Tyra Biosciences, Inc. | Indazole compounds |
| MX2023007793A (es) | 2020-12-30 | 2023-09-22 | Tyra Biosciences Inc | Compuestos de indazol como inhibidores de cinasas. |
| JP2025525433A (ja) * | 2022-06-29 | 2025-08-05 | タイラ・バイオサイエンシーズ・インコーポレイテッド | インダゾール化合物 |
| TW202408493A (zh) * | 2022-06-29 | 2024-03-01 | 美商泰拉生物科學公司 | 多晶形化合物及其用途 |
| JP2025529161A (ja) | 2022-08-30 | 2025-09-04 | タイラ・バイオサイエンシーズ・インコーポレイテッド | 活性化fgfr3遺伝子変化を有する固形腫瘍を処置する方法 |
| WO2024104922A1 (en) | 2022-11-14 | 2024-05-23 | Ascendis Pharma Growth Disorders A/S | Method of improving skeletal muscle function |
| WO2024137742A1 (en) | 2022-12-20 | 2024-06-27 | Blueprint Medicines Corporation | Compounds and compositions as fgfr3 degraders and uses thereof |
| WO2024138112A1 (en) * | 2022-12-22 | 2024-06-27 | Tyra Biosciences, Inc. | Indazole compounds |
| IL321294A (en) * | 2022-12-30 | 2025-08-01 | Jiangsu Yahong Meditech Co Ltd | A compressed pyrazole ring compound, a method for its preparation and use |
| KR20250162619A (ko) | 2023-03-20 | 2025-11-18 | 아센디스 파마 그로우쓰 디스오더스 에이/에스 | 연골무형성증을 가진 인간 대상에서의 흉요추 변형의 치료 방법 |
| CN119306723A (zh) * | 2023-07-13 | 2025-01-14 | 长春金赛药业有限责任公司 | 吲唑类fgfr2/3选择性抑制剂、药物组合物及其应用 |
| CN121013846A (zh) * | 2023-07-21 | 2025-11-25 | 长春金赛药业有限责任公司 | 成纤维细胞生长因子受体抑制剂、药物组合物及其应用 |
| WO2025021997A1 (en) | 2023-07-27 | 2025-01-30 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | New map4k1 inhibitors |
| WO2025061029A1 (en) * | 2023-09-18 | 2025-03-27 | 3H Pharmaceuticals Co., Ltd. | Fgfr inhibitors and methods of use thereof |
| TW202519212A (zh) | 2023-09-22 | 2025-05-16 | 美商泰拉生物科學公司 | 組合治療療法 |
| WO2025129014A1 (en) * | 2023-12-15 | 2025-06-19 | Tyra Biosciences, Inc. | Indazole compounds for the treatment of cancer |
| WO2025170959A1 (en) | 2024-02-05 | 2025-08-14 | Tyra Biosciences, Inc. | Combination of the fgfr 3 inhibitor tyra-300 and a nectin-4 targeting agent-drug conjugate for use in the treatment of cancer |
| WO2025199217A1 (en) | 2024-03-19 | 2025-09-25 | Tyra Biosciences, Inc. | Pharmaceutical compositions |
| WO2026020109A1 (en) * | 2024-07-19 | 2026-01-22 | Tyra Biosciences, Inc. | Combination treatment comprising a fgfr3 inhibitor and a pd-1/pd-l1 inhibitor for use in the treatment of cancer |
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