CA3236553A1 - Inhibitors of hif-2alpha and methods of use thereof - Google Patents
Inhibitors of hif-2alpha and methods of use thereof Download PDFInfo
- Publication number
- CA3236553A1 CA3236553A1 CA3236553A CA3236553A CA3236553A1 CA 3236553 A1 CA3236553 A1 CA 3236553A1 CA 3236553 A CA3236553 A CA 3236553A CA 3236553 A CA3236553 A CA 3236553A CA 3236553 A1 CA3236553 A1 CA 3236553A1
- Authority
- CA
- Canada
- Prior art keywords
- alkyl
- mmol
- compound
- formula
- halo
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- 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
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
-
- 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
- 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
- C07D405/02—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 two hetero rings
- C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D405/02—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 two hetero rings
- C07D405/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D413/06—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 carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163273283P | 2021-10-29 | 2021-10-29 | |
| US63/273,283 | 2021-10-29 | ||
| US202263345120P | 2022-05-24 | 2022-05-24 | |
| US63/345,120 | 2022-05-24 | ||
| US202263380221P | 2022-10-19 | 2022-10-19 | |
| US63/380,221 | 2022-10-19 | ||
| PCT/US2022/078842 WO2023077046A1 (en) | 2021-10-29 | 2022-10-28 | Inhibitors of hif-2alpha and methods of use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3236553A1 true CA3236553A1 (en) | 2023-05-04 |
Family
ID=84358530
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3236553A Pending CA3236553A1 (en) | 2021-10-29 | 2022-10-28 | Inhibitors of hif-2alpha and methods of use thereof |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US12071411B2 (https=) |
| EP (1) | EP4423069A1 (https=) |
| JP (1) | JP2024541969A (https=) |
| KR (1) | KR20240110814A (https=) |
| AU (1) | AU2022376961A1 (https=) |
| CA (1) | CA3236553A1 (https=) |
| IL (1) | IL312348A (https=) |
| TW (1) | TW202325279A (https=) |
| WO (1) | WO2023077046A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4558501A1 (en) | 2022-07-20 | 2025-05-28 | Arcus Biosciences, Inc. | Cbl-b inhibitors and methods of use thereof |
| EP4602041A1 (en) | 2022-10-14 | 2025-08-20 | Arcus Biosciences, Inc. | Hpk1 inhibitors and methods of use thereof |
| WO2024233360A1 (en) | 2023-05-05 | 2024-11-14 | Arcus Biosciences, Inc. | Cbl-b inhibitors and methods of use thereof |
| EP4720055A1 (en) | 2023-05-25 | 2026-04-08 | Arcus Biosciences, Inc. | Cbl-b inhibitors and methods of use thereof |
| WO2024249894A2 (en) | 2023-06-02 | 2024-12-05 | Arcus Biosciences, Inc. | Biomarkers for predicting cancer treatment efficacy |
| WO2025038857A1 (en) | 2023-08-16 | 2025-02-20 | Arcus Biosciences, Inc. | TETRALINS TARGETING MUTANT HIF-2α |
| WO2025054339A1 (en) | 2023-09-08 | 2025-03-13 | Arcus Biosciences, Inc. | Triazolopyridine compounds as inhibitors of kit |
| WO2025072330A1 (en) | 2023-09-26 | 2025-04-03 | Arcus Biosciences, Inc. | Kit inhibitor compounds and methods of use thereof |
| US20260116868A1 (en) | 2023-10-06 | 2026-04-30 | Arcus Biosciences, Inc. | Cbl-b inhibitors and methods of use thereof |
| TW202523302A (zh) | 2023-11-02 | 2025-06-16 | 美商阿克思生物科學有限公司 | 噻唑化合物及其使用方法 |
Family Cites Families (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9716101D0 (en) | 1997-07-30 | 1997-10-01 | Pharmacia & Upjohn Spa | Fused heterocyclic compounds |
| US5914405A (en) | 1997-10-07 | 1999-06-22 | Eli Lilly And Company | Process for preparing 3-substituted indazoles |
| GB9911053D0 (en) | 1999-05-12 | 1999-07-14 | Pharmacia & Upjohn Spa | 4,5,6,7-tetrahydroindazole derivatives process for their preparation and their use as antitumour agents |
| JP2004508359A (ja) | 2000-09-06 | 2004-03-18 | ニューロゲン コーポレイション | アリール置換テトラヒドロインダゾール、及び、ｇａｂａ−ａ受容体に対するリガンドとしてのそれらの使用 |
| PT2343320T (pt) | 2005-03-25 | 2018-01-23 | Gitr Inc | Anticorpos anti-gitr e as suas utilizações |
| EP1987839A1 (en) | 2007-04-30 | 2008-11-05 | I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale | Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease |
| US8591886B2 (en) | 2007-07-12 | 2013-11-26 | Gitr, Inc. | Combination therapies employing GITR binding molecules |
| EP2044949A1 (en) | 2007-10-05 | 2009-04-08 | Immutep | Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response |
| AR072999A1 (es) | 2008-08-11 | 2010-10-06 | Medarex Inc | Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos |
| JP2012506848A (ja) | 2008-10-27 | 2012-03-22 | グラクソ グループ リミテッド | グルタミン酸受容体モジュレーターとしての三環式化合物 |
| EP2202232A1 (en) | 2008-12-26 | 2010-06-30 | Laboratorios Almirall, S.A. | 1,2,4-oxadiazole derivatives and their therapeutic use |
| KR101790802B1 (ko) | 2009-09-03 | 2017-10-27 | 머크 샤프 앤드 돔 코포레이션 | 항-ｇｉｔｒ 항체 |
| ES2722300T3 (es) | 2009-12-10 | 2019-08-09 | Hoffmann La Roche | Anticuerpos que se unen preferentemente al dominio extracelular 4 de CSF1R y su uso |
| EP2542256B1 (en) | 2010-03-04 | 2019-05-22 | MacroGenics, Inc. | Antibodies reactive with b7-h3, immunologically active fragments thereof and uses thereof |
| US9169323B2 (en) | 2010-03-05 | 2015-10-27 | Hoffmann-La Roche Inc. | Antibodies against human CSF-1R |
| JP5989547B2 (ja) | 2010-03-05 | 2016-09-07 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | ヒトｃｓｆ−１ｒに対する抗体及びその使用 |
| HRP20190047T1 (hr) | 2010-05-04 | 2019-02-22 | Five Prime Therapeutics, Inc. | Protutijela koja se vežu na csf1r |
| MX337040B (es) | 2010-09-09 | 2016-02-09 | Pfizer | Moleculas de union a 4-1bb. |
| WO2012087782A1 (en) | 2010-12-23 | 2012-06-28 | Boehringer Ingelheim International Gmbh | Pyrazolopiperidine compounds as ccr1 receptor antagonists |
| JP6072771B2 (ja) | 2011-04-20 | 2017-02-01 | メディミューン，エルエルシー | Ｂ７−ｈ１およびｐｄ−１に結合する抗体およびその他の分子 |
| RU2658603C2 (ru) | 2011-12-15 | 2018-06-21 | Ф.Хоффманн-Ля Рош Аг | Антитела против человеческого csf-1r и их применения |
| KR20140127855A (ko) | 2012-02-06 | 2014-11-04 | 제넨테크, 인크. | Csf1r 억제제를 사용하는 조성물 및 방법 |
| AR090263A1 (es) | 2012-03-08 | 2014-10-29 | Hoffmann La Roche | Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma |
| RU2670743C9 (ru) | 2012-05-11 | 2018-12-19 | Файв Прайм Терапьютикс, Инк. | Способы лечения состояний антителами, которые связывают рецептор колониестимулирующего фактора 1 (csf1r) |
| UY34887A (es) | 2012-07-02 | 2013-12-31 | Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware | Optimización de anticuerpos que se fijan al gen de activación de linfocitos 3 (lag-3) y sus usos |
| WO2015188369A1 (en) | 2014-06-13 | 2015-12-17 | Merck Sharp & Dohme Corp. | Purine inhibitors of human phosphatidylinositol 3-kinase delta |
| WO2016109684A2 (en) | 2014-12-30 | 2016-07-07 | Novira Therapeutics, Inc. | Derivatives and methods of treating hepatitis b infections |
| WO2016144825A1 (en) | 2015-03-11 | 2016-09-15 | Peloton Therapeutics, Inc. | Aromatic compounds and uses thereof |
| WO2017120508A1 (en) | 2016-01-08 | 2017-07-13 | Arcus Biosciences, Inc. | Modulators of 5'-nucleotidase, ecto and the use thereof |
| EP3518934A4 (en) | 2016-10-03 | 2020-06-24 | Arcus Biosciences, Inc. | Inhibitors of adenosine 5'-nucleotidase |
| WO2018094148A1 (en) | 2016-11-18 | 2018-05-24 | Arcus Biosciences, Inc. | Inhibitors of cd73-mediated immunosuppression |
| HUE064141T2 (hu) | 2017-01-20 | 2024-02-28 | Arcus Biosciences Inc | Azolopirimidin rákkal összefüggõ rendellenességek kezelésére |
| ES2953349T3 (es) | 2017-05-05 | 2023-11-10 | Arcus Biosciences Inc | Derivados de quinazolina-piridina para el tratamiento de trastornos relacionados con el cáncer |
| PL3634417T3 (pl) | 2017-05-17 | 2023-09-25 | Arcus Biosciences, Inc. | Pochodne chinazolino-pirazolowe do leczenia chorób związanych z nowotworem |
| AU2019229978B2 (en) | 2018-03-05 | 2024-05-30 | Arcus Biosciences, Inc. | Arginase inhibitors |
| PL3829581T3 (pl) | 2018-07-27 | 2024-07-01 | Arcus Biosciences, Inc. | Antagoniści pirydonu a2r |
| WO2020046813A1 (en) | 2018-08-27 | 2020-03-05 | Arcus Biosciences, Inc. | Cd73 inhibitors |
| TWI828800B (zh) | 2018-11-16 | 2024-01-11 | 美商阿克思生物科學有限公司 | Arg1及/或arg2之抑制劑 |
| CN114206332B (zh) | 2019-06-04 | 2024-08-23 | 艾库斯生物科学有限公司 | 2,3,5-三取代吡唑并[1,5-a]嘧啶化合物 |
| AU2020312800B2 (en) | 2019-07-17 | 2026-04-23 | Zomagen Biosciences Ltd | N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4,5,6,7-tetrahydrobenzofuran -2-sulfonamide derivatives and related compounds as NLPR3 modulators for the treatment of multiple sclerosis (ms) |
| CN119118872A (zh) * | 2020-03-19 | 2024-12-13 | 艾库斯生物科学有限公司 | 作为HIF-2α抑制剂的四氢化萘和四氢喹啉化合物 |
| MX2022015157A (es) | 2020-06-02 | 2023-01-16 | Arcus Biosciences Inc | Anticuerpos para tigit. |
| CA3186769A1 (en) * | 2020-06-11 | 2021-12-16 | Betta Pharmaceuticals Co., Ltd | Bicyclic compounds and use thereof |
| WO2022063115A1 (zh) * | 2020-09-24 | 2022-03-31 | 贝达药业股份有限公司 | 双环化合物及其应用 |
-
2022
- 2022-10-28 WO PCT/US2022/078842 patent/WO2023077046A1/en not_active Ceased
- 2022-10-28 TW TW111141151A patent/TW202325279A/zh unknown
- 2022-10-28 KR KR1020247017707A patent/KR20240110814A/ko active Pending
- 2022-10-28 JP JP2024525262A patent/JP2024541969A/ja active Pending
- 2022-10-28 IL IL312348A patent/IL312348A/en unknown
- 2022-10-28 CA CA3236553A patent/CA3236553A1/en active Pending
- 2022-10-28 AU AU2022376961A patent/AU2022376961A1/en active Pending
- 2022-10-28 EP EP22803462.5A patent/EP4423069A1/en active Pending
- 2022-10-28 US US18/050,557 patent/US12071411B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US20230159466A1 (en) | 2023-05-25 |
| AU2022376961A1 (en) | 2024-05-16 |
| JP2024541969A (ja) | 2024-11-13 |
| IL312348A (en) | 2024-06-01 |
| EP4423069A1 (en) | 2024-09-04 |
| KR20240110814A (ko) | 2024-07-16 |
| TW202325279A (zh) | 2023-07-01 |
| US12071411B2 (en) | 2024-08-27 |
| WO2023077046A1 (en) | 2023-05-04 |
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