AR120684A1 - INHIBIDORES DE HIF-2a - Google Patents
INHIBIDORES DE HIF-2aInfo
- Publication number
- AR120684A1 AR120684A1 ARP200103396A ARP200103396A AR120684A1 AR 120684 A1 AR120684 A1 AR 120684A1 AR P200103396 A ARP200103396 A AR P200103396A AR P200103396 A ARP200103396 A AR P200103396A AR 120684 A1 AR120684 A1 AR 120684A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- independently selected
- alkyl
- haloalkyl
- alkoxy
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- 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
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- 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
- A61K31/4353—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
- A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines 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
- A61K31/495—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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines 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
- A61K31/495—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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
- A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- 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
-
- 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
Abstract
En el presente documento se describen compuestos que inhiben HIF-2a y composiciones que contienen los compuestos y métodos para sintetizar los compuestos. También se describe el uso de tales compuestos y composiciones para el tratamiento de una diversidad de enfermedades, trastornos y afecciones, incluidos los trastornos relacionados con el cáncer y con el sistema inmunitario que están mediados, al menos en parte, por HIF-2a. Reivindicación 1: Un compuesto representado por la fórmula (1) o una sal farmacéuticamente aceptable de este, caracterizado por que, los enlaces discontinuos son enlaces simples y dobles concordantes con los grupos proporcionados para Y¹, Y² e Y³; X¹ es CR¹ o N; X² es CR² o N; X³ es CR³ o N; Y se selecciona del grupo que consiste en -O-, -C(Rᵃ)(Rᵇ)-, -N(Rᵃ)-, -C(Rᵃ)(Rᵇ)-N(Rᵃ)-, -S- y -S(O)₂-; Y¹, Y² y Y³ se seleccionan cada uno independientemente del grupo que consiste en CR⁵, NR⁶ y N, donde uno de Y¹, Y² y Y³ es N, y uno de Y¹, Y² y Y³ es NR⁶; R¹ y R² son cada uno miembros seleccionados independientemente del grupo que consiste en H, halógeno, CN, -NO₂, alquilo C₁₋₄, haloalquilo C₁₋₄ y haloalcoxi C₁₋₄; R³ es un miembro seleccionado del grupo que consiste en H, halógeno, CN, -NO₂, -S(O)₂Rᵃ, -C(O)NRᵃRᵇ, -P(O)RᵃRᵇ, alquilo C₁₋₈, alcoxi C₁₋₈, haloalquilo C₁₋₈, haloalcoxi C₁₋₄, arilo C₆₋₁₀ y heteroarilo de 5 a 10 miembros que tiene de 1 a 4 heteroátomos en los vértices del anillo seleccionados independientemente del grupo que consiste en N, O y S; cuando cada uno de R¹, R² y R³ están presentes, al menos uno es diferente de H; R⁴ es un miembro seleccionado del grupo que consiste en alquilo C₁₋₈, alcoxi C₁₋₈, cicloalquilo C₃₋₈, arilo C₆₋₁₀ y heteroarilo de 6 miembros que tiene de 1 a 4 heteroátomos en los vértices del anillo seleccionados independientemente del grupo que consiste en N, O y S; cada R⁵ es un miembro seleccionado del grupo que consiste en H, -NO₂, -S(O)₂Rᵃ, -S(O)₂NRᵃRᵇ, -S(O)(NH)Rᵃ, -C(O)Rᵃ, -C(O)NRᵃRᵇ, CN, halógeno, -P(O)RᵃRᵇ, alquilo C₁₋₈, alcoxi C₁₋₈, alcoximetilo C₁₋₈, haloalquilo C₁₋₈, hidroxialquilo C₁₋₈, -NRᵃRᵇ, arilo C₆₋₁₀ y heteroarilo de 5 a 10 miembros que tiene de 1 a 4 heteroátomos en los vértices del anillo seleccionados independientemente del grupo que consiste en N, O y S; cada R⁶ es un miembro seleccionado del grupo que consiste en H, alquilo C₁₋₈, arilo C₆₋₁₀ y heteroarilo de 5 a 10 miembros que tiene de 1 a 4 heteroátomos en los vértices del anillo seleccionados independientemente del grupo que consiste en N, O y S; donde cada Rᵃ y Rᵇ se seleccionan independientemente del grupo que consiste en H, alquilo C₁₋₈, alcoxi C₁₋₈, haloalquilo C₁₋₈ y haloalcoxi C₁₋₈ e hidroxialquilo C₁₋₈; y para cada R⁴, R⁵ y R⁶, cada cicloalquilo C₃₋₈, arilo C₆₋₁₀ y heteroarilo esté o no sustituido con uno a cinco Rᶜ; donde cada Rᶜ se selecciona independientemente del grupo que consiste en halógeno, CN, -NO₂, alquilo C₁₋₈, alcoxi C₁₋₈, haloalquilo C₁₋₈, -S(O)₂Rᵈ, -C(O)NRᵈRᵉ y -P(O)RᵈRᵉ; y Rᵈ y Rᵉ se seleccionan cada uno independientemente del grupo que consiste en H, alquilo C₁₋₈, alcoxi C₁₋₈, haloalquilo C₁₋₈ y haloalcoxi C₁₋₈.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201962943632P | 2019-12-04 | 2019-12-04 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR120684A1 true AR120684A1 (es) | 2022-03-09 |
Family
ID=76222655
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP200103396A AR120684A1 (es) | 2019-12-04 | 2020-12-04 | INHIBIDORES DE HIF-2a |
Country Status (10)
Country | Link |
---|---|
US (1) | US20230024438A1 (es) |
EP (1) | EP4069212A4 (es) |
JP (1) | JP2023504623A (es) |
KR (1) | KR20220110524A (es) |
CN (1) | CN114760994A (es) |
AR (1) | AR120684A1 (es) |
AU (1) | AU2020395783A1 (es) |
CA (1) | CA3163338A1 (es) |
TW (1) | TW202134216A (es) |
WO (1) | WO2021113436A1 (es) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA3173831A1 (en) | 2020-03-19 | 2021-09-23 | Arcus Biosciences, Inc. | Tetralin and tetrahydroquinoline compounds as inhibitors of hif-2alpha |
TW202313603A (zh) | 2021-05-21 | 2023-04-01 | 美商阿克思生物科學有限公司 | Axl抑制劑化合物 |
CN117295741A (zh) | 2021-05-21 | 2023-12-26 | 艾库斯生物科学有限公司 | Axl化合物 |
CN116332960A (zh) * | 2021-12-23 | 2023-06-27 | 上海优理惠生医药有限公司 | 一种哒嗪类化合物、其药物组合物及应用 |
WO2023215719A1 (en) | 2022-05-02 | 2023-11-09 | Arcus Biosciences, Inc. | Anti-tigit antibodies and uses of the same |
WO2024015251A1 (en) | 2022-07-15 | 2024-01-18 | Arcus Biosciences, Inc. | Inhibitors of hpk1 and methods of use thereof |
WO2024020034A1 (en) | 2022-07-20 | 2024-01-25 | Arcus Biosciences, Inc. | Cbl-b inhibitors and methods of use thereof |
WO2024059142A1 (en) | 2022-09-14 | 2024-03-21 | Arcus Biosciences, Inc. | Dispersions of etrumadenant |
CN117800944A (zh) * | 2022-09-30 | 2024-04-02 | 苏州阿尔脉生物科技有限公司 | 吡啶酰胺类衍生物、包含其的药物组合物及其医药用途 |
WO2024081385A1 (en) | 2022-10-14 | 2024-04-18 | Arcus Biosciences, Inc. | Hpk1 inhibitors and methods of use thereof |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2645137A1 (en) * | 2006-03-07 | 2007-09-13 | James F. Blake | Heterobicyclic pyrazole compounds and methods of use |
US8314234B2 (en) * | 2006-09-25 | 2012-11-20 | Janssen Pharmaceutica N.V. | Bicyclic pyrimidine kinase inhibitors |
JPWO2008072634A1 (ja) * | 2006-12-12 | 2010-04-02 | 武田薬品工業株式会社 | 縮合複素環化合物 |
GB0704407D0 (en) * | 2007-03-07 | 2007-04-18 | Glaxo Group Ltd | Compounds |
US8188098B2 (en) * | 2008-05-19 | 2012-05-29 | Hoffmann-La Roche Inc. | GPR119 receptor agonists |
RU2509078C2 (ru) * | 2008-07-01 | 2014-03-10 | Дженентек, Инк. | Бициклические гетероциклы в качестве ингибиторов киназы мек |
AU2010224693B2 (en) * | 2009-03-19 | 2016-07-28 | Lifearc | Compounds |
KR102153772B1 (ko) * | 2013-09-09 | 2020-09-09 | 펠로톤 테라퓨틱스, 인크. | 아릴 에테르 및 이의 용도 |
US9399640B2 (en) * | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
MX2017005719A (es) * | 2014-11-03 | 2017-12-07 | Iomet Pharma Ltd | Compuesto farmaceutico. |
WO2016145045A1 (en) * | 2015-03-11 | 2016-09-15 | Peloton Therapeutics, Inc. | Compositions for use in treating glioblastoma |
WO2016168510A1 (en) * | 2015-04-17 | 2016-10-20 | Peloton Therapeutics, Inc. | Combination therapy of a hif-2-alpha inhibitor and an immunotherapeutic agent and uses thereof |
CN107033087B (zh) * | 2016-02-04 | 2020-09-04 | 西华大学 | 1h-吲唑-4-胺类化合物及其作为ido抑制剂的用途 |
CN108689937B (zh) * | 2017-04-10 | 2021-09-17 | 西华大学 | 吲唑类化合物及其在制备ido抑制剂类药物上的用途 |
TW201942115A (zh) * | 2018-02-01 | 2019-11-01 | 美商輝瑞股份有限公司 | 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物 |
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2020
- 2020-12-03 JP JP2022532743A patent/JP2023504623A/ja active Pending
- 2020-12-03 CA CA3163338A patent/CA3163338A1/en active Pending
- 2020-12-03 WO PCT/US2020/063000 patent/WO2021113436A1/en unknown
- 2020-12-03 AU AU2020395783A patent/AU2020395783A1/en active Pending
- 2020-12-03 EP EP20897463.4A patent/EP4069212A4/en active Pending
- 2020-12-03 KR KR1020227022279A patent/KR20220110524A/ko unknown
- 2020-12-03 CN CN202080083619.7A patent/CN114760994A/zh active Pending
- 2020-12-03 TW TW109142543A patent/TW202134216A/zh unknown
- 2020-12-03 US US17/777,103 patent/US20230024438A1/en active Pending
- 2020-12-04 AR ARP200103396A patent/AR120684A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
CN114760994A (zh) | 2022-07-15 |
TW202134216A (zh) | 2021-09-16 |
EP4069212A4 (en) | 2024-03-06 |
JP2023504623A (ja) | 2023-02-06 |
US20230024438A1 (en) | 2023-01-26 |
AU2020395783A1 (en) | 2022-06-09 |
KR20220110524A (ko) | 2022-08-08 |
WO2021113436A1 (en) | 2021-06-10 |
EP4069212A1 (en) | 2022-10-12 |
CA3163338A1 (en) | 2021-06-10 |
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