CA3252016A1 - HETEROBORCTIONAL TETROHYDROISOQUINOLINE-BASED BCL-XL DEGRADING AGENTS - Google Patents
HETEROBORCTIONAL TETROHYDROISOQUINOLINE-BASED BCL-XL DEGRADING AGENTSInfo
- Publication number
- CA3252016A1 CA3252016A1 CA3252016A CA3252016A CA3252016A1 CA 3252016 A1 CA3252016 A1 CA 3252016A1 CA 3252016 A CA3252016 A CA 3252016A CA 3252016 A CA3252016 A CA 3252016A CA 3252016 A1 CA3252016 A1 CA 3252016A1
- Authority
- CA
- Canada
- Prior art keywords
- compound
- cancer
- group
- alkyl
- inhibitor
- 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
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four 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
- A61K31/495—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
- A61K31/495—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
- 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
- A61K31/529—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring systems
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202263339308P | 2022-05-06 | 2022-05-06 | |
| US63/339,308 | 2022-05-06 | ||
| US202263398752P | 2022-08-17 | 2022-08-17 | |
| US63/398,752 | 2022-08-17 | ||
| US202263429834P | 2022-12-02 | 2022-12-02 | |
| US63/429,834 | 2022-12-02 | ||
| US202363449728P | 2023-03-03 | 2023-03-03 | |
| US63/449,728 | 2023-03-03 | ||
| US202363454486P | 2023-03-24 | 2023-03-24 | |
| US63/454,486 | 2023-03-24 | ||
| PCT/US2023/020956 WO2023215449A1 (en) | 2022-05-06 | 2023-05-04 | Tetrahydroisoquinoline heterobifunctional bcl-xl degraders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3252016A1 true CA3252016A1 (en) | 2023-11-09 |
Family
ID=86609470
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3252016A Pending CA3252016A1 (en) | 2022-05-06 | 2023-05-04 | HETEROBORCTIONAL TETROHYDROISOQUINOLINE-BASED BCL-XL DEGRADING AGENTS |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20250288683A1 (https=) |
| EP (1) | EP4519272A1 (https=) |
| JP (1) | JP2025516359A (https=) |
| AU (1) | AU2023264537A1 (https=) |
| CA (1) | CA3252016A1 (https=) |
| MX (1) | MX2024013312A (https=) |
| WO (1) | WO2023215449A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4401729A4 (en) * | 2021-09-17 | 2025-10-01 | Kymera Therapeutics Inc | BCL-XL DEGRADING AGENTS AND THEIR USES |
| WO2025036119A1 (zh) * | 2023-08-11 | 2025-02-20 | 北京三秀生物医药科技有限公司 | 靶向Bcl-xL蛋白的PROTAC及其应用 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1888550B1 (en) | 2005-05-12 | 2014-06-25 | AbbVie Bahamas Ltd. | Apoptosis promoters |
| US8546399B2 (en) | 2009-05-26 | 2013-10-01 | Abbvie Inc. | Apoptosis inducing agents for the treatment of cancer and immune and autoimmune diseases |
| TWI571466B (zh) * | 2011-10-14 | 2017-02-21 | 艾伯維有限公司 | 用於治療癌症及免疫與自體免疫疾病之細胞凋亡誘發劑 |
| CN103987711B (zh) | 2011-10-14 | 2016-08-24 | 艾伯维公司 | 作为用于治疗癌症和免疫性和自身免疫性疾病的凋亡诱导剂的8-氨基甲酰基-2-(2,3-二取代吡啶-6-基)-1,2,3,4-四氢异喹啉衍生物 |
| JP6936498B2 (ja) | 2016-04-21 | 2021-09-15 | バイオベンチャーズ・リミテッド・ライアビリティ・カンパニーBioVentures, LLC | 抗アポトーシス性Bcl−2ファミリータンパク質の分解を誘導する化合物及びその使用 |
| EP3743069B1 (en) | 2018-01-22 | 2025-08-06 | BioVentures, LLC | Bcl-2 proteins degraders for cancer treatment |
| WO2020163823A2 (en) | 2019-02-08 | 2020-08-13 | University Of Florida Research Foundation, Incorporated | Therapeutic agents and methods of treatment |
| WO2021007307A1 (en) | 2019-07-10 | 2021-01-14 | Recurium Ip Holdings, Llc | Bcl-2 protein inhibitors |
| WO2021078301A1 (zh) | 2019-10-24 | 2021-04-29 | 上海科技大学 | 蛋白降解剂及其在疾病治疗中的应用 |
| AU2021207672A1 (en) | 2020-01-15 | 2022-07-14 | University Of Florida Research Foundation, Incorporated | Therapeutic agents and methods of treatment |
| MX2022010512A (es) | 2020-04-28 | 2022-11-16 | Recurium Ip Holdings Llc | Inhibidores de proteína bcl-2. |
| CN117794929A (zh) | 2021-02-02 | 2024-03-29 | 法国施维雅药厂 | 选择性bcl-xl protac化合物及使用方法 |
| EP4401729A4 (en) | 2021-09-17 | 2025-10-01 | Kymera Therapeutics Inc | BCL-XL DEGRADING AGENTS AND THEIR USES |
-
2023
- 2023-05-04 JP JP2024565274A patent/JP2025516359A/ja active Pending
- 2023-05-04 WO PCT/US2023/020956 patent/WO2023215449A1/en not_active Ceased
- 2023-05-04 AU AU2023264537A patent/AU2023264537A1/en active Pending
- 2023-05-04 EP EP23727754.6A patent/EP4519272A1/en active Pending
- 2023-05-04 CA CA3252016A patent/CA3252016A1/en active Pending
- 2023-05-04 US US18/858,971 patent/US20250288683A1/en active Pending
-
2024
- 2024-10-28 MX MX2024013312A patent/MX2024013312A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2025516359A (ja) | 2025-05-27 |
| US20250288683A1 (en) | 2025-09-18 |
| WO2023215449A1 (en) | 2023-11-09 |
| MX2024013312A (es) | 2025-02-10 |
| AU2023264537A1 (en) | 2024-11-14 |
| EP4519272A1 (en) | 2025-03-12 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A00 | Application filed |
Free format text: ST27 STATUS EVENT CODE: A-0-1-A10-A00-A101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: APPLICATION RECEIVED - PCT Effective date: 20241104 |
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