PE20220808A1 - Derivados de benzisoxazol sulfonamida - Google Patents
Derivados de benzisoxazol sulfonamidaInfo
- Publication number
- PE20220808A1 PE20220808A1 PE2021002180A PE2021002180A PE20220808A1 PE 20220808 A1 PE20220808 A1 PE 20220808A1 PE 2021002180 A PE2021002180 A PE 2021002180A PE 2021002180 A PE2021002180 A PE 2021002180A PE 20220808 A1 PE20220808 A1 PE 20220808A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- halogen
- membered heteroaryl
- sulfonamide derivatives
- methoxy
- Prior art date
Links
- OIFAKIJHBGJKLD-UHFFFAOYSA-N 1,2-benzoxazole-3-sulfonamide Chemical class C1=CC=C2C(S(=O)(=O)N)=NOC2=C1 OIFAKIJHBGJKLD-UHFFFAOYSA-N 0.000 title abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 2
- 229910052731 fluorine Inorganic materials 0.000 abstract 2
- 239000011737 fluorine Substances 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- -1 -OH Chemical group 0.000 abstract 1
- 101100439664 Arabidopsis thaliana CHR8 gene Proteins 0.000 abstract 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- 102000007077 Lysine Acetyltransferases Human genes 0.000 abstract 1
- 108010033293 Lysine Acetyltransferases Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000010261 cell growth Effects 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 239000003085 diluting agent Substances 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
- 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
- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic rings
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Referido a un compuesto de la Formula I, o una sal farmaceuticamente aceptable del mismo, en donde R1 es un H o heteroarilo de 5-6 miembros opcionalmente sustituido por metilo; R2 es un H o -(CHR8)n-(heteroarilo de 5-9 miembros) opcionalmente sustituido por halogeno, alquilo de C1-C3, entre otros; R3 es H, halogeno, alquilo de C1-C3, entre otros; R4 es H, halogeno, alquilo de C1-C3, ciclopropilo, entre otros; Anillo A es arilo de C6-C10 o heteroarilo de 9-10 miembros; R5 es H, fluor, ciano, alquilo de C1-C3, entre otros; R6 es H, fluor, metilo, -OH, o metoxi; R7 es H, bromo, cloro, fluor, o metoxi; R8 es un H o -OH; y n es 0 o 1. Estos compuestos son derivados de benzisoxazol sulfonamida actuan como inhibidores de Lisina Acetil Transferasa (KAT) y son utiles para el tratamiento de crecimiento celular anormal, tal como cancer. Tambien se refiere a una composicion farmaceutica que comprende dicho compuesto, y un portador farmaceuticamente aceptable o diluyente.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962863199P | 2019-06-18 | 2019-06-18 | |
| US201962953223P | 2019-12-24 | 2019-12-24 | |
| US202063025278P | 2020-05-15 | 2020-05-15 | |
| PCT/IB2020/055589 WO2020254946A1 (en) | 2019-06-18 | 2020-06-16 | Benzisoxazole sulfonamide derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20220808A1 true PE20220808A1 (es) | 2022-05-20 |
Family
ID=71738189
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021002180A PE20220808A1 (es) | 2019-06-18 | 2020-06-16 | Derivados de benzisoxazol sulfonamida |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US11492346B2 (es) |
| EP (2) | EP3986890B9 (es) |
| JP (2) | JP7352662B2 (es) |
| KR (1) | KR102823056B1 (es) |
| CN (1) | CN114364672B (es) |
| AU (2) | AU2020296361A1 (es) |
| BR (1) | BR112021025528A2 (es) |
| CA (1) | CA3143666C (es) |
| CL (1) | CL2021003372A1 (es) |
| CO (1) | CO2021017504A2 (es) |
| CR (1) | CR20210627A (es) |
| DK (2) | DK3986890T3 (es) |
| EC (1) | ECSP21091615A (es) |
| ES (2) | ES2969616T3 (es) |
| FI (2) | FI3986890T3 (es) |
| HR (2) | HRP20231501T1 (es) |
| HU (1) | HUE064683T2 (es) |
| IL (1) | IL288802B2 (es) |
| LT (2) | LT3986890T (es) |
| MA (1) | MA67365B1 (es) |
| MD (2) | MD3986890T3 (es) |
| MX (1) | MX2021016085A (es) |
| MY (1) | MY210207A (es) |
| PE (1) | PE20220808A1 (es) |
| PH (1) | PH12021553107A1 (es) |
| PL (2) | PL4299135T3 (es) |
| PT (2) | PT4299135T (es) |
| RS (2) | RS67276B1 (es) |
| SI (2) | SI3986890T1 (es) |
| TW (1) | TWI787620B (es) |
| UA (1) | UA129891C2 (es) |
| UY (1) | UY38752A (es) |
| WO (1) | WO2020254946A1 (es) |
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| GB201810092D0 (en) * | 2018-06-20 | 2018-08-08 | Ctxt Pty Ltd | Compounds |
| TW202108559A (zh) | 2019-05-31 | 2021-03-01 | 美商醫肯納腫瘤學公司 | Tead抑制劑及其用途 |
| AU2020296361A1 (en) | 2019-06-18 | 2022-01-06 | Ctxt Pty Ltd | Benzisoxazole sulfonamide derivatives |
| US20220024919A1 (en) * | 2020-07-15 | 2022-01-27 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
| EP4667055A2 (en) * | 2020-07-15 | 2025-12-24 | Pfizer Inc. | Kat6 inhibitor methods and combinations for cancer treatment |
| WO2022187693A1 (en) * | 2021-03-05 | 2022-09-09 | Umbra Therapeutics Inc. | Covalent cdk2-binding compounds for therapeutic purposes |
| WO2022187688A1 (en) * | 2021-03-05 | 2022-09-09 | Umbra Therapeutics Inc. | Covalent kras-binding compounds for therapeutic purposes |
| CA3221048A1 (en) * | 2021-05-21 | 2022-11-24 | Aurigene Oncology Limited | Fused isoxazolyl compounds as kat6a inhibitors |
| CA3225068A1 (en) | 2021-07-05 | 2023-01-12 | Hangzhou Innogate Pharma Co., Ltd. | Compound serving as kat6 inhibitor |
| JP2024529068A (ja) * | 2021-08-10 | 2024-08-01 | 江蘇恒瑞医薬股▲ふん▼有限公司 | スルファミド誘導体、その調製方法及びその医薬的使用 |
| CA3237830A1 (en) * | 2021-11-16 | 2023-05-25 | Insilico Medicine Ip Limited | Lysine acetyltransferase 6a (kat6a) inhibitors and uses thereof |
| EP4448109A1 (en) * | 2021-12-13 | 2024-10-23 | Aurigene Oncology Limited | Fused benzoisoxazolyl compounds as kat6a inhibitors |
| CN116621859A (zh) * | 2022-02-18 | 2023-08-22 | 山东轩竹医药科技有限公司 | 三并环类kat6抑制剂 |
| IL315930A (en) * | 2022-03-28 | 2024-11-01 | Isosterix Inc | Inhibitors of the myst family of lysine acetyl transferases |
| JP2025525339A (ja) * | 2022-06-16 | 2025-08-05 | プレリュード・セラピューティクス・インコーポレイテッド | ビキチンリガーゼ結合部分を有するｋａｔ６標的化合物 |
| CN119604288A (zh) | 2022-07-29 | 2025-03-11 | 辉瑞大药厂 | 用于治疗癌症的包含kat6抑制剂的给药方案 |
| WO2024131772A1 (zh) * | 2022-12-20 | 2024-06-27 | 杭州中美华东制药有限公司 | 具有sting抑制作用的含肟化合物及其药物组合物和用途 |
| EP4663635A1 (en) | 2023-02-10 | 2025-12-17 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Crystalline form of sulfonamide derivative and preparation method therefor |
| KR20250155594A (ko) | 2023-03-16 | 2025-10-30 | 올레마 파마슈티컬스 인코포레이티드 | 아실설폰아마이드 kat6a 억제제 |
| WO2024199254A1 (zh) * | 2023-03-27 | 2024-10-03 | 北京康辰药业股份有限公司 | 磺酰胺化合物、其药物组合物和应用 |
| WO2024201334A1 (en) | 2023-03-30 | 2024-10-03 | Pfizer Inc. | Kat6a as a predictive biomarker for treatment with a kat6a inhibitor and methods of treatment thereof |
| KR20250172879A (ko) * | 2023-04-19 | 2025-12-09 | 인실리코 메디신 아이피 리미티드 | 리신 아세틸트랜스퍼라제 6a (kat6a) 억제제, 그의 조합 및 용도 |
| AU2024262206A1 (en) * | 2023-04-25 | 2025-12-04 | Insilico Medicine Ip Limited | Crystalline lysine acetyltransferase 6a (kat6a) inhibitor and uses thereof |
| WO2025007873A1 (zh) * | 2023-07-04 | 2025-01-09 | 上海齐鲁制药研究中心有限公司 | Kat6抑制剂 |
| WO2025036382A1 (zh) * | 2023-08-14 | 2025-02-20 | 上海复宏汉霖生物医药有限公司 | 一种磺酰胺类化合物、其制备方法及用途 |
| US20250122182A1 (en) * | 2023-09-27 | 2025-04-17 | Isosterix, Inc. | MYST Inhibitors |
| WO2025098417A1 (zh) * | 2023-11-08 | 2025-05-15 | 再和医药科技（苏州）有限公司 | 磺酰胺类化合物及其应用 |
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| WO2026003716A1 (en) | 2024-06-27 | 2026-01-02 | Pfizer Inc. | Process for preparing n-(6-((1h-pyrazol-1-yl)methyl)-4-methoxybenzo[d]isoxazol- 3-yl)-2-methoxybenzenesulfonamide |
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