CN105960404B - 布鲁顿氏酪氨酸激酶的抑制剂 - Google Patents
布鲁顿氏酪氨酸激酶的抑制剂 Download PDFInfo
- Publication number
- CN105960404B CN105960404B CN201480074736.1A CN201480074736A CN105960404B CN 105960404 B CN105960404 B CN 105960404B CN 201480074736 A CN201480074736 A CN 201480074736A CN 105960404 B CN105960404 B CN 105960404B
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- China
- Prior art keywords
- amino
- carboxamide
- phenyl
- pyrazine
- piperidin
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- 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
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- 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
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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- 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
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- 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
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- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361912483P | 2013-12-05 | 2013-12-05 | |
| US61/912,483 | 2013-12-05 | ||
| PCT/US2014/068434 WO2015084998A1 (en) | 2013-12-05 | 2014-12-03 | Inhibitors of bruton's tyrosine kinase |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105960404A CN105960404A (zh) | 2016-09-21 |
| CN105960404B true CN105960404B (zh) | 2019-09-03 |
Family
ID=52302318
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480074736.1A Expired - Fee Related CN105960404B (zh) | 2013-12-05 | 2014-12-03 | 布鲁顿氏酪氨酸激酶的抑制剂 |
Country Status (12)
| Country | Link |
|---|---|
| US (5) | US9382246B2 (OSRAM) |
| EP (1) | EP3077388A1 (OSRAM) |
| JP (3) | JP6345786B2 (OSRAM) |
| KR (1) | KR20160093675A (OSRAM) |
| CN (1) | CN105960404B (OSRAM) |
| AR (1) | AR099367A1 (OSRAM) |
| AU (3) | AU2014360446A1 (OSRAM) |
| BR (1) | BR112016012728A2 (OSRAM) |
| CA (1) | CA2932609A1 (OSRAM) |
| MX (2) | MX375752B (OSRAM) |
| TW (2) | TWI672294B (OSRAM) |
| WO (1) | WO2015084998A1 (OSRAM) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6345786B2 (ja) * | 2013-12-05 | 2018-06-20 | ファーマサイクリックス エルエルシー | ブルトン型チロシンキナーゼの阻害剤 |
| JP2018522823A (ja) * | 2015-06-02 | 2018-08-16 | ファーマサイクリックス エルエルシー | ブルトン型チロシンキナーゼの阻害剤 |
| US10954216B2 (en) | 2016-12-27 | 2021-03-23 | Riken | BMP-signal-inhibiting compound |
| CN107382836A (zh) * | 2017-08-04 | 2017-11-24 | 吴赣药业(苏州)有限公司 | 一种1‑(4‑氨基苯基)‑1h‑吡啶‑2‑酮的制备方法 |
| CN107445981B (zh) * | 2017-08-25 | 2018-06-22 | 牡丹江医学院 | 一种用于防治宫颈炎的活性化合物 |
| EP3713930A1 (en) * | 2017-11-21 | 2020-09-30 | Bristol-Myers Squibb Company | Sulfone pyridine alkyl amide-substituted heteroaryl compounds |
| US20210017174A1 (en) | 2018-03-07 | 2021-01-21 | Bayer Aktiengesellschaft | Identification and use of erk5 inhibitor |
| CA3224945C (en) | 2018-07-31 | 2025-11-18 | Loxo Oncology, Inc. | SPRAY DRIED DISPERSIONS, FORMULATIONS AND POLYMORPHIES OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)(1,1,1-TRIFLUOROPROPAN-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE |
| AU2019360928B2 (en) * | 2018-10-15 | 2023-11-09 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading BTK via ubiquitin proteosome pathway |
| FI3870579T3 (fi) * | 2018-10-22 | 2025-01-02 | Alumis Inc | Tyk2-inhibiittoreita ja niiden käyttöjä |
| KR20210142154A (ko) | 2019-03-21 | 2021-11-24 | 옹쎄오 | 암 치료를 위한 키나제 억제제와 조합된 dbait 분자 |
| WO2020210508A1 (en) | 2019-04-09 | 2020-10-15 | Nurix Therapeutics, Inc. | 3-substituted piperidine compounds for cbl-b inhibition, and use of a cbl-b inhibitor in combination with a cancer vaccine and/or oncolytic virus |
| CN114206855B (zh) | 2019-05-17 | 2024-11-26 | 紐力克斯治疗公司 | 用于Cbl-b抑制的氰基环丁基类化合物及其用途 |
| EP3972963A1 (en) | 2019-05-21 | 2022-03-30 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
| CN110066259A (zh) * | 2019-05-22 | 2019-07-30 | 南京合巨药业有限公司 | 一种n-环戊基-1,1-二氧代-4-硫代吗啉甲酰胺的合成方法 |
| BR112021026241A2 (pt) | 2019-06-26 | 2022-06-07 | Nurix Therapeutics Inc | Compostos de benzil-triazol substituído para inibição de cbl-b e outros usos dos mesmos |
| AU2020353015A1 (en) | 2019-09-24 | 2022-03-31 | Nurix Therapeutics, Inc. | CBL inhibitors and compositions for use in adoptive cell therapy |
| JP2023500906A (ja) | 2019-11-08 | 2023-01-11 | インサーム(インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル) | キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法 |
| JP2023504147A (ja) * | 2019-12-04 | 2023-02-01 | ニューリックス セラピューティクス,インコーポレイテッド | ユビキチンプロテオソーム経路を介したbtkの分解のための二官能性化合物 |
| CN111018842B (zh) * | 2019-12-04 | 2021-02-12 | 宜春市人民医院 | 一种唑代嘧啶衍生物、其药物组合物和在抗肿瘤中的应用 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| WO2022032484A1 (zh) * | 2020-08-11 | 2022-02-17 | 北京诺诚健华医药科技有限公司 | 哒嗪-3-甲酰胺类化合物、其制备方法及其在医药学上的应用 |
| WO2022071772A1 (ko) * | 2020-09-29 | 2022-04-07 | (주)메디톡스 | 단백질 키나제 저해제 및 그의 용도 |
| JP2024514836A (ja) | 2021-04-08 | 2024-04-03 | ニューリックス セラピューティクス,インコーポレイテッド | Cbl-b阻害化合物との組み合わせ療法 |
| KR20240029070A (ko) * | 2021-07-01 | 2024-03-05 | 항저우 힐젠 테라퓨틱스 컴퍼니 리미티드 | 브루톤 티로신 키나아제, 이의 돌연변이체 분해제, 조성물 및 응용 |
| JP2024542984A (ja) | 2021-10-26 | 2024-11-19 | ニューリックス セラピューティクス,インコーポレイテッド | がんを治療および予防するためのピペリジニルピラジン-カルボキサミド化合物、およびbtkを分解するためのピペリジニルピラジン-カルボキサミド化合物 |
| CN118598858A (zh) * | 2021-11-22 | 2024-09-06 | 杭州和正医药有限公司 | 一种可降解btk激酶的多功能化合物、组合物及应用 |
| CN114349707B (zh) * | 2022-01-20 | 2024-01-09 | 中国医学科学院医药生物技术研究所 | 一种n-取代脲类化合物及其制备方法和应用 |
| CN115417827B (zh) * | 2022-09-30 | 2023-05-26 | 中国药科大学 | 6-氨基-1,3,5-三嗪类化合物及其合成方法和应用 |
| WO2024129395A1 (en) * | 2022-12-16 | 2024-06-20 | Gwynant Therapeutics, Inc. | Btk inhibitors |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102083800A (zh) * | 2008-06-27 | 2011-06-01 | 阿维拉制药公司 | 杂芳基化合物和其用途 |
| WO2013047813A1 (ja) * | 2011-09-30 | 2013-04-04 | 大鵬薬品工業株式会社 | 1,2,4-トリアジン-6-カルボキサミド誘導体 |
| US20130131040A1 (en) * | 2011-11-23 | 2013-05-23 | Portola Pharmaceuticals, Inc. | Pyrazine kinase inhibitors |
| WO2013108754A1 (ja) * | 2012-01-17 | 2013-07-25 | アステラス製薬株式会社 | ピラジンカルボキサミド化合物 |
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| US3710795A (en) | 1970-09-29 | 1973-01-16 | Alza Corp | Drug-delivery device with stretched, rate-controlling membrane |
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| US3731683A (en) | 1971-06-04 | 1973-05-08 | Alza Corp | Bandage for the controlled metering of topical drugs to the skin |
| US3742951A (en) | 1971-08-09 | 1973-07-03 | Alza Corp | Bandage for controlled release of vasodilators |
| US3996934A (en) | 1971-08-09 | 1976-12-14 | Alza Corporation | Medical bandage |
| BE795384A (fr) | 1972-02-14 | 1973-08-13 | Ici Ltd | Pansements |
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| US3993072A (en) | 1974-08-28 | 1976-11-23 | Alza Corporation | Microporous drug delivery device |
| US4151273A (en) | 1974-10-31 | 1979-04-24 | The Regents Of The University Of California | Increasing the absorption rate of insoluble drugs |
| US3972995A (en) | 1975-04-14 | 1976-08-03 | American Home Products Corporation | Dosage form |
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