CN111032642B - 激酶抑制剂及制造和使用方法 - Google Patents
激酶抑制剂及制造和使用方法 Download PDFInfo
- Publication number
- CN111032642B CN111032642B CN201880052620.6A CN201880052620A CN111032642B CN 111032642 B CN111032642 B CN 111032642B CN 201880052620 A CN201880052620 A CN 201880052620A CN 111032642 B CN111032642 B CN 111032642B
- Authority
- CN
- China
- Prior art keywords
- pyrazol
- piperidin
- phenyl
- carboxamide
- compound
- 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.)
- Expired - Fee Related
Links
Classifications
-
- 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
-
- 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]
-
- 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
- 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
- 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
- C07D405/02—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 two hetero rings
- C07D405/04—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 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
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pain & Pain Management (AREA)
- Pharmacology & Pharmacy (AREA)
- Rheumatology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762526838P | 2017-06-29 | 2017-06-29 | |
| US62/526,838 | 2017-06-29 | ||
| PCT/US2018/040021 WO2019006126A1 (en) | 2017-06-29 | 2018-06-28 | KINASE INHIBITORS AND METHODS OF MAKING AND USING THEM |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN111032642A CN111032642A (zh) | 2020-04-17 |
| CN111032642B true CN111032642B (zh) | 2023-07-18 |
Family
ID=62976284
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880052620.6A Expired - Fee Related CN111032642B (zh) | 2017-06-29 | 2018-06-28 | 激酶抑制剂及制造和使用方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US10590121B2 (https=) |
| EP (1) | EP3645525A1 (https=) |
| JP (2) | JP7167069B2 (https=) |
| CN (1) | CN111032642B (https=) |
| CA (1) | CA3068305A1 (https=) |
| WO (1) | WO2019006126A1 (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3068305A1 (en) * | 2017-06-29 | 2019-01-03 | Rigel Pharmaceuticals, Inc. | Kinase inhibitors and methods for making and using |
| WO2020132651A1 (en) | 2018-12-20 | 2020-06-25 | Amgen Inc. | Kif18a inhibitors |
| EP3898616B1 (en) | 2018-12-20 | 2024-10-02 | Amgen Inc. | Heteroaryl amides useful as kif18a inhibitors |
| JP7676308B2 (ja) * | 2018-12-20 | 2025-05-14 | アムジエン・インコーポレーテツド | Ｋｉｆ１８ａ阻害剤として有用なヘテロアリールアミド |
| US11390604B2 (en) * | 2019-03-08 | 2022-07-19 | Hoffmann-La Roche Inc. | Imidazole-pyrazole derivatives |
| WO2021018118A1 (en) * | 2019-07-29 | 2021-02-04 | Janssen Pharmaceutica Nv | Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 1 proteins |
| US12540129B2 (en) | 2019-08-02 | 2026-02-03 | Amgen Inc. | KIF18A inhibitors |
| WO2021026099A1 (en) | 2019-08-02 | 2021-02-11 | Amgen Inc. | Kif18a inhibitors |
| WO2021035257A1 (en) * | 2019-08-21 | 2021-02-25 | The Scripps Research Institute | Monocyclic agonists of stimulator of interferon genes sting |
| CN110592056A (zh) * | 2019-09-19 | 2019-12-20 | 昆明理工大学 | 噬菌体裂解酶复合粉剂及其制备方法和应用 |
| CN114981259B (zh) * | 2020-01-22 | 2024-06-18 | 豪夫迈·罗氏有限公司 | 新型杂环化合物 |
| AR121717A1 (es) * | 2020-04-02 | 2022-06-29 | Rigel Pharmaceuticals Inc | Inhibidores de rip1k |
| US20230295146A1 (en) * | 2020-07-24 | 2023-09-21 | The University Of Rochester | Inhibitors of interleukin-1 receptor-associated kinases 1 and 4 |
| JP2024506021A (ja) * | 2021-02-07 | 2024-02-08 | エフ． ホフマン－ラ ロシュ アーゲー | 新規ヘテロアリール置換イミダゾール誘導体 |
| WO2022197575A1 (en) * | 2021-03-17 | 2022-09-22 | Merck Sharp & Dohme Llc | Heteroaroyl amides as lrrk2 inhibitors, pharmaceutical compositions, and uses thereof |
| WO2023088435A1 (zh) * | 2021-11-19 | 2023-05-25 | 成都奥睿药业有限公司 | 三取代吡啶衍生物的制备及作为芳香烃受体调节物的应用 |
| JP2025513716A (ja) | 2022-03-23 | 2025-04-30 | ライジェル・ファーマシューティカルズ・インコーポレイテッド | Ｉｒａｋ阻害剤としてのピリミド－２－イル－ピラゾール化合物 |
| AU2024214768A1 (en) * | 2023-01-30 | 2025-08-07 | The Johns Hopkins University | 18 f-labeled pet radiotracers for imaging macrophage colony stimulating factor 1 receptor |
| CN118027009B (zh) * | 2024-04-15 | 2024-07-12 | 北京师范大学 | 一类靶向于csf1r激酶的苯基酰胺类化合物及其应用 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015089481A2 (en) * | 2013-12-13 | 2015-06-18 | Dana-Farber Cancer Institute, Inc. | Methods to treat lymphoplasmacytic lymphoma |
| WO2017023941A1 (en) * | 2015-08-04 | 2017-02-09 | Rigel Pharmaceuticals, Inc. | Benzazole compounds and methods for making and using the compounds |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5087240A (en) | 1983-08-18 | 1992-02-11 | Drug Delivery Systems Inc. | Transdermal drug patch with conductive fibers |
| US4921475A (en) | 1983-08-18 | 1990-05-01 | Drug Delivery Systems Inc. | Transdermal drug patch with microtubes |
| US4738851A (en) | 1985-09-27 | 1988-04-19 | University Of Iowa Research Foundation, Inc. | Controlled release ophthalmic gel formulation |
| US5163899A (en) | 1987-03-20 | 1992-11-17 | Drug Delivery Systems Inc. | Transdermal drug delivery system |
| US5312325A (en) | 1987-05-28 | 1994-05-17 | Drug Delivery Systems Inc | Pulsating transdermal drug delivery system |
| GB8804164D0 (en) | 1988-02-23 | 1988-03-23 | Tucker J M | Bandage for administering physiologically active compound |
| US4882150A (en) | 1988-06-03 | 1989-11-21 | Kaufman Herbert E | Drug delivery system |
| US5008110A (en) | 1988-11-10 | 1991-04-16 | The Procter & Gamble Company | Storage-stable transdermal patch |
| US5088977A (en) | 1988-12-21 | 1992-02-18 | Drug Delivery Systems Inc. | Electrical transdermal drug applicator with counteractor and method of drug delivery |
| US5521222A (en) | 1989-09-28 | 1996-05-28 | Alcon Laboratories, Inc. | Topical ophthalmic pharmaceutical vehicles |
| EP0431519B1 (en) | 1989-12-04 | 1994-06-15 | G.D. Searle & Co. | System for transdermal albuterol administration |
| US5077033A (en) | 1990-08-07 | 1991-12-31 | Mediventures Inc. | Ophthalmic drug delivery with thermo-irreversible gels of polxoxyalkylene polymer and ionic polysaccharide |
| ATE141502T1 (de) | 1991-01-15 | 1996-09-15 | Alcon Lab Inc | Verwendung von karrageenan in topischen ophthalmologischen zusammensetzungen |
| US5352456A (en) | 1991-10-10 | 1994-10-04 | Cygnus Therapeutic Systems | Device for administering drug transdermally which provides an initial pulse of drug |
| DE69228827T2 (de) | 1991-12-18 | 1999-10-21 | Minnesota Mining And Mfg. Co., Saint Paul | Mehrschichtige sperrstrukturen |
| EP0553769B1 (de) | 1992-01-29 | 1996-01-03 | FRANZ VÖLKL GmbH & CO. SKI UND TENNIS SPORTARTIKELFABRIK KG | Ballspielschläger, insbesondere Tennisschläger |
| IL114193A (en) | 1994-06-20 | 2000-02-29 | Teva Pharma | Ophthalmic pharmaceutical compositions based on sodium alginate |
| ES2094688B1 (es) | 1994-08-08 | 1997-08-01 | Cusi Lab | Manoemulsion del tipo de aceite en agua, util como vehiculo oftalmico y procedimiento para su preparacion. |
| IT1283911B1 (it) | 1996-02-05 | 1998-05-07 | Farmigea Spa | Soluzioni oftalmiche viscosizzate con polisaccaridi della gomma di tamarindo |
| US5800807A (en) | 1997-01-29 | 1998-09-01 | Bausch & Lomb Incorporated | Ophthalmic compositions including glycerin and propylene glycol |
| US6261547B1 (en) | 1998-04-07 | 2001-07-17 | Alcon Manufacturing, Ltd. | Gelling ophthalmic compositions containing xanthan gum |
| US6197934B1 (en) | 1998-05-22 | 2001-03-06 | Collagenesis, Inc. | Compound delivery using rapidly dissolving collagen film |
| JP2016505012A (ja) * | 2013-01-10 | 2016-02-18 | ニンバス アイリス， インコーポレイテッド | Ｉｒａｋ阻害剤およびその使用 |
| EA039043B1 (ru) * | 2015-04-22 | 2021-11-25 | Райджел Фармасьютикалз, Инк. | Пиразольные соединения и способ получения и применения данных соединений |
| BR112018000624A2 (pt) * | 2015-07-15 | 2018-09-18 | Aurigene Discovery Technologies Limited | compostos de indazol e azaindazol como inibidores de irak-4 |
| CA3068305A1 (en) * | 2017-06-29 | 2019-01-03 | Rigel Pharmaceuticals, Inc. | Kinase inhibitors and methods for making and using |
-
2018
- 2018-06-28 CA CA3068305A patent/CA3068305A1/en active Pending
- 2018-06-28 EP EP18743281.0A patent/EP3645525A1/en not_active Withdrawn
- 2018-06-28 US US16/022,323 patent/US10590121B2/en active Active
- 2018-06-28 WO PCT/US2018/040021 patent/WO2019006126A1/en not_active Ceased
- 2018-06-28 CN CN201880052620.6A patent/CN111032642B/zh not_active Expired - Fee Related
- 2018-06-28 JP JP2019572355A patent/JP7167069B2/ja active Active
-
2020
- 2020-02-12 US US16/789,131 patent/US11059814B2/en active Active
-
2021
- 2021-06-08 US US17/341,817 patent/US20210309655A1/en not_active Abandoned
-
2022
- 2022-10-26 JP JP2022171152A patent/JP7379639B2/ja active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015089481A2 (en) * | 2013-12-13 | 2015-06-18 | Dana-Farber Cancer Institute, Inc. | Methods to treat lymphoplasmacytic lymphoma |
| WO2017023941A1 (en) * | 2015-08-04 | 2017-02-09 | Rigel Pharmaceuticals, Inc. | Benzazole compounds and methods for making and using the compounds |
Non-Patent Citations (2)
| Title |
|---|
| IRAK-4 inhibitors. Part 1: A series of amides;George M. Buckley等;《Bioorg. Med. Chem. Lett.》;20080601;第18卷(第11期);第3211-3214页，尤其是第3213页Table 3，第3212页Table 1，第3213页Table 2 * |
| Quantitative structure-activity relationship (QSAR) study of interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor activity by the genetic algorithm and multiple linear regression (GA-MLR) method;Eslam Pourbashee等;《Journal of Enzyme Inhibition and Medicinal Chemistry》;20100430;第25卷(第6期);第844-853页，尤其是第846页Table 1 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US11059814B2 (en) | 2021-07-13 |
| US20190002455A1 (en) | 2019-01-03 |
| EP3645525A1 (en) | 2020-05-06 |
| JP2020526498A (ja) | 2020-08-31 |
| JP7379639B2 (ja) | 2023-11-14 |
| US20200181135A1 (en) | 2020-06-11 |
| WO2019006126A1 (en) | 2019-01-03 |
| CN111032642A (zh) | 2020-04-17 |
| JP2023011726A (ja) | 2023-01-24 |
| US10590121B2 (en) | 2020-03-17 |
| US20210309655A1 (en) | 2021-10-07 |
| JP7167069B2 (ja) | 2022-11-08 |
| CA3068305A1 (en) | 2019-01-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20230718 |