CA3124935A1 - 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof - Google Patents
3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof Download PDFInfo
- Publication number
- CA3124935A1 CA3124935A1 CA3124935A CA3124935A CA3124935A1 CA 3124935 A1 CA3124935 A1 CA 3124935A1 CA 3124935 A CA3124935 A CA 3124935A CA 3124935 A CA3124935 A CA 3124935A CA 3124935 A1 CA3124935 A1 CA 3124935A1
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- Prior art keywords
- alkyl
- optionally substituted
- heteroatoms selected
- cycloalkyl
- halogen
- Prior art date
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- CIBYAIJUOIICFR-UHFFFAOYSA-N 3-[3-oxo-6-[1-(pyrimidin-4-ylmethyl)piperidin-4-yl]-1H-isoindol-2-yl]piperidine-2,6-dione Chemical compound O=C1N(CC2=CC(=CC=C12)C1CCN(CC1)CC1=NC=NC=C1)C1C(NC(CC1)=O)=O CIBYAIJUOIICFR-UHFFFAOYSA-N 0.000 claims 1
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- VJYJJHQEVLEOFL-UHFFFAOYSA-N thieno[3,2-b]thiophene Chemical compound S1C=CC2=C1C=CS2 VJYJJHQEVLEOFL-UHFFFAOYSA-N 0.000 description 1
- GKTQKQTXHNUFSP-UHFFFAOYSA-N thieno[3,4-c]pyrrole-4,6-dione Chemical compound S1C=C2C(=O)NC(=O)C2=C1 GKTQKQTXHNUFSP-UHFFFAOYSA-N 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 208000013818 thyroid gland medullary carcinoma Diseases 0.000 description 1
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 description 1
- 201000006134 tongue cancer Diseases 0.000 description 1
- 208000025358 tongue carcinoma Diseases 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- IAQRGUVFOMOMEM-ONEGZZNKSA-N trans-but-2-ene Chemical compound C\C=C\C IAQRGUVFOMOMEM-ONEGZZNKSA-N 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- IMFACGCPASFAPR-UHFFFAOYSA-N tributylamine Chemical compound CCCCN(CCCC)CCCC IMFACGCPASFAPR-UHFFFAOYSA-N 0.000 description 1
- YNJBWRMUSHSURL-UHFFFAOYSA-N trichloroacetic acid Chemical compound OC(=O)C(Cl)(Cl)Cl YNJBWRMUSHSURL-UHFFFAOYSA-N 0.000 description 1
- 125000004784 trichloromethoxy group Chemical group ClC(O*)(Cl)Cl 0.000 description 1
- 125000003866 trichloromethyl group Chemical group ClC(Cl)(Cl)* 0.000 description 1
- 229940086542 triethylamine Drugs 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- YFTHZRPMJXBUME-UHFFFAOYSA-N tripropylamine Chemical compound CCCN(CCC)CCC YFTHZRPMJXBUME-UHFFFAOYSA-N 0.000 description 1
- 208000017997 tumor of parathyroid gland Diseases 0.000 description 1
- 208000010570 urinary bladder carcinoma Diseases 0.000 description 1
- 230000002485 urinary effect Effects 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- PXXNTAGJWPJAGM-UHFFFAOYSA-N vertaline Natural products C1C2C=3C=C(OC)C(OC)=CC=3OC(C=C3)=CC=C3CCC(=O)OC1CC1N2CCCC1 PXXNTAGJWPJAGM-UHFFFAOYSA-N 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
Classifications
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- 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
- C07D405/14—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| US201962806140P | 2019-02-15 | 2019-02-15 | |
| US62/806,140 | 2019-02-15 | ||
| PCT/IB2020/051205 WO2020165833A1 (en) | 2019-02-15 | 2020-02-13 | 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
Publications (1)
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| CA3124935A1 true CA3124935A1 (en) | 2020-08-20 |
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| EP (1) | EP3924054B1 (enExample) |
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| BR (1) | BR112021015783A2 (enExample) |
| CA (1) | CA3124935A1 (enExample) |
| EA (1) | EA202192019A1 (enExample) |
| ES (1) | ES3032659T3 (enExample) |
| MX (1) | MX2021009763A (enExample) |
| WO (1) | WO2020165833A1 (enExample) |
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| WO2020117759A1 (en) | 2018-12-03 | 2020-06-11 | Dana-Farber Cancer Institute, Inc. | Small molecule degraders of helios and methods of use |
| MX2021014443A (es) | 2019-05-31 | 2022-01-06 | Ikena Oncology Inc | Inhibidores del dominio asociado mejorador de la transcripcion (tead) y usos de los mismos. |
| AU2020282759A1 (en) | 2019-05-31 | 2021-12-23 | Ikena Oncology, Inc. | TEAD inhibitors and uses thereof |
| AU2020374957A1 (en) * | 2019-10-30 | 2022-04-28 | Dana-Farber Cancer Institute, Inc. | Small molecule degraders of Helios and methods of use |
| MX2023004374A (es) * | 2020-10-14 | 2023-07-06 | C4 Therapeutics Inc | Ligandos tricíclicos para la degradación de la familia ikaros 2 o la familia ikaros 4. |
| WO2022081976A1 (en) * | 2020-10-16 | 2022-04-21 | Dana-Farber Cancer Institute, Inc. | Piperidinyl small molecule degraders of helios and methods of use |
| CN116669769A (zh) * | 2020-10-16 | 2023-08-29 | 达纳-法伯癌症研究所公司 | Helios的哌啶基小分子降解剂和使用方法 |
| WO2022120355A1 (en) * | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Tead degraders and uses thereof |
| AU2022253242A1 (en) | 2021-04-06 | 2023-11-23 | Bristol-Myers Squibb Company | Pyridinyl substituted oxoisoindoline compounds |
| CA3209633A1 (en) * | 2021-04-29 | 2022-11-03 | Tinghu Zhang | Phthalimido cereblon complex binders and transcription factor degraders and methods of use |
| JP2024517772A (ja) * | 2021-04-29 | 2024-04-23 | ネオモルフ インコーポレイテッド | 置換された2-(2,6-ジオキソピペリジン-3-イル)-5-(1-ピペリジン-4-イル)イソインドリン-1,3-ジオン誘導体及びその使用 |
| KR20240035820A (ko) | 2021-07-09 | 2024-03-18 | 플렉시움 인코포레이티드 | Ikzf2를 조절하는 아릴 화합물 및 약학 조성물 |
| CN116003418A (zh) * | 2021-10-22 | 2023-04-25 | 标新生物医药科技(上海)有限公司 | Crbn e3连接酶配体化合物、基于该配体化合物开发的蛋白降解剂及它们的应用 |
| JP2024545193A (ja) * | 2021-12-22 | 2024-12-05 | ギリアード サイエンシーズ, インコーポレイテッド | Ikarosジンクフィンガーファミリー分解剤及びその使用 |
| CN116640122A (zh) * | 2022-02-16 | 2023-08-25 | 苏州国匡医药科技有限公司 | Ikzf2降解剂及包含其的药物组合物和用途 |
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| WO2024096753A1 (en) * | 2022-11-02 | 2024-05-10 | Captor Therapeutics S.A. | Nek7 degraders and methods of use thereof |
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| AU2020222345B2 (en) | 2022-11-17 |
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| JP7483732B2 (ja) | 2024-05-15 |
| EP3924054B1 (en) | 2025-04-02 |
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| ES3032659T3 (en) | 2025-07-23 |
| EP3924054A1 (en) | 2021-12-22 |
| WO2020165833A1 (en) | 2020-08-20 |
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