TWI902994B - Ｉｒａｋ４抑制劑、藥物組成物及其用途 - Google Patents
Ｉｒａｋ４抑制劑、藥物組成物及其用途Info
- Publication number
- TWI902994B TWI902994B TW110145977A TW110145977A TWI902994B TW I902994 B TWI902994 B TW I902994B TW 110145977 A TW110145977 A TW 110145977A TW 110145977 A TW110145977 A TW 110145977A TW I902994 B TWI902994 B TW I902994B
- Authority
- TW
- Taiwan
- Prior art keywords
- indazole
- methoxy
- methamide
- cyclohexyl
- mmol
- Prior art date
Links
Classifications
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- 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
-
- 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
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic 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
- A61K31/495—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- A61P37/08—Antiallergic agents
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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063199160P | 2020-12-10 | 2020-12-10 | |
| US63/199,160 | 2020-12-10 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202237612A TW202237612A (zh) | 2022-10-01 |
| TWI902994B true TWI902994B (zh) | 2025-11-01 |
Family
ID=79230946
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW110145977A TWI902994B (zh) | 2020-12-10 | 2021-12-09 | Ｉｒａｋ４抑制劑、藥物組成物及其用途 |
Country Status (33)
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7555519B2 (ja) * | 2022-02-14 | 2024-09-24 | アストラゼネカ・アクチエボラーグ | Ｉｒａｋ４阻害剤 |
| US20250326757A1 (en) * | 2022-05-26 | 2025-10-23 | Astrazeneca Ab | Solid forms of heterocyclylamides as irak4 inhibitors |
| TW202508568A (zh) | 2023-04-07 | 2025-03-01 | 瑞典商阿斯特捷利康公司 | Ｉｒａｋ４蛋白水解靶向嵌合體 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110003219A (zh) | 2010-07-13 | 2019-07-12 | 弗·哈夫曼-拉罗切有限公司 | 作为irak4调节剂的吡唑并[1,5a]嘧啶和噻吩并[3,2b]嘧啶衍生物 |
| BR112013015460B1 (pt) | 2010-12-20 | 2022-01-25 | Merck Serono S.A. | Derivados de indazolil triazol, kit, e composição farmacêutica |
| BG111378A (bg) * | 2013-01-14 | 2015-01-30 | Николай Цветков | Субституирани индазолови производни като in-vitro mao-b инхибитори |
| DK2970139T3 (en) | 2013-03-15 | 2018-08-13 | Biomarin Pharm Inc | HDAC inhibitors |
| EP3092226B1 (en) | 2014-01-10 | 2019-03-13 | Aurigene Discovery Technologies Limited | Indazole compounds as irak4 inhibitors |
| DK3126330T3 (en) | 2014-04-04 | 2019-04-23 | Pfizer | BICYCLE-FUSED HETEROARYL OR ARYL COMPOUNDS AND USE THEREOF AS IRAC4 INHIBITORS |
| JO3705B1 (ar) | 2014-11-26 | 2021-01-31 | Bayer Pharma AG | إندازولات مستبدلة جديدة، عمليات لتحضيرها، مستحضرات دوائية تحتوي عليها واستخدامها في إنتاج أدوية |
| TW201701879A (zh) | 2015-04-30 | 2017-01-16 | 拜耳製藥公司 | Ｉｒａｋ４抑制劑組合 |
| CN108024971A (zh) | 2015-07-15 | 2018-05-11 | 奥列基因发现技术有限公司 | 作为irak-4抑制剂的取代的氮杂化合物 |
| JP2018524372A (ja) | 2015-07-15 | 2018-08-30 | アウリジーン ディスカバリー テクノロジーズ リミテッド | Ｉｒａｋ−４阻害剤としてのインダゾール及びアザインダゾール化合物 |
| CN105503863A (zh) * | 2015-12-11 | 2016-04-20 | 南京华威医药科技开发有限公司 | 新型抗肿瘤化合物 |
| CN108473498B (zh) | 2015-12-22 | 2021-11-02 | 豪夫迈·罗氏有限公司 | 作为IRAK4调节剂的吡唑并[1,5a]嘧啶衍生物 |
| WO2017148902A1 (de) | 2016-03-03 | 2017-09-08 | Bayer Pharma Aktiengesellschaft | Neue 2-substituierte indazole, verfahren zu ihrer herstellung, pharmazeutische präparate die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln |
| US10059708B2 (en) | 2016-04-26 | 2018-08-28 | Northwestern University | Therapeutic targeting of the interleukin 1 receptor-associated kinase 4 (IRAK4) in leukemias characterized by rearrangements in the mixed lineage leukemia gene (MLL-r) |
| SG10202011653WA (en) | 2016-06-01 | 2020-12-30 | Bayer Pharma AG | Use of 2-substituted indazoles for the treatment and prophylaxis of autoimmune diseases |
| EP3642201A1 (en) | 2017-06-21 | 2020-04-29 | H. Hoffnabb-La Roche Ag | Isoindolinone derivatives as irak4 modulators |
| JP2020524692A (ja) | 2017-06-21 | 2020-08-20 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｉｒａｋ４調節因子としてのベンゾフラン |
| US20230002361A1 (en) | 2019-06-27 | 2023-01-05 | Biogen Ma Inc. | 2h-indazole derivatives and their use in the treatment of disease |
| JP7576581B2 (ja) | 2019-06-27 | 2024-10-31 | バイオジェン・エムエイ・インコーポレイテッド | イミダゾ［１，２－ａ］ピリジニル誘導体及び疾患の処置におけるそれらの使用 |
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2021
- 2021-12-01 US US17/457,249 patent/US11866405B2/en active Active
- 2021-12-09 PE PE2023001857A patent/PE20240684A1/es unknown
- 2021-12-09 TW TW110145977A patent/TWI902994B/zh active
- 2021-12-09 HR HRP20241312TT patent/HRP20241312T1/hr unknown
- 2021-12-09 SM SM20240417T patent/SMT202400417T1/it unknown
- 2021-12-09 KR KR1020237023107A patent/KR20230118153A/ko active Pending
- 2021-12-09 SI SI202130206T patent/SI4259632T1/sl unknown
- 2021-12-09 RS RS20241183A patent/RS66095B1/sr unknown
- 2021-12-09 IL IL303356A patent/IL303356B1/en unknown
- 2021-12-09 JP JP2023535016A patent/JP7749015B2/ja active Active
- 2021-12-09 PL PL21836097.2T patent/PL4259632T3/pl unknown
- 2021-12-09 LT LTEPPCT/EP2021/084916T patent/LT4259632T/lt unknown
- 2021-12-09 HU HUE21836097A patent/HUE068584T2/hu unknown
- 2021-12-09 MA MA62535A patent/MA62535B1/fr unknown
- 2021-12-09 DK DK21836097.2T patent/DK4259632T3/da active
- 2021-12-09 WO PCT/EP2021/084916 patent/WO2022122876A1/en not_active Ceased
- 2021-12-09 PT PT218360972T patent/PT4259632T/pt unknown
- 2021-12-09 ES ES21836097T patent/ES2989489T3/es active Active
- 2021-12-09 MX MX2023006816A patent/MX2023006816A/es unknown
- 2021-12-09 CR CR20230264A patent/CR20230264A/es unknown
- 2021-12-09 UA UAA202303173A patent/UA130417C2/uk unknown
- 2021-12-09 CN CN202180082181.5A patent/CN116583285B/zh active Active
- 2021-12-09 CA CA3203569A patent/CA3203569A1/en active Pending
- 2021-12-09 EP EP21836097.2A patent/EP4259632B1/en active Active
- 2021-12-09 FI FIEP21836097.2T patent/FI4259632T3/fi active
- 2021-12-09 AU AU2021395816A patent/AU2021395816B2/en active Active
- 2021-12-10 AR ARP210103432A patent/AR124303A1/es unknown
- 2021-12-10 UY UY0001039561A patent/UY39561A/es unknown
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2023
- 2023-06-08 CL CL2023001662A patent/CL2023001662A1/es unknown
- 2023-06-09 CO CONC2023/0007624A patent/CO2023007624A2/es unknown
- 2023-06-09 DO DO2023000119A patent/DOP2023000119A/es unknown
- 2023-07-05 ZA ZA2023/06848A patent/ZA202306848B/en unknown
- 2023-07-05 EC ECSENADI202350553A patent/ECSP23050553A/es unknown
- 2023-11-02 US US18/500,155 patent/US12448385B2/en active Active
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2025
- 2025-09-29 US US19/343,252 patent/US20260092069A1/en active Pending
Non-Patent Citations (1)
| Title |
|---|
| 期刊 Zhai W, et al. "Discovery and optimization of a potent and selective indazolamine series of IRAK4 inhibitors" Bioorganic & Medicinal Chemistry Letters 31: Elsevier 2020; 127686 |
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