CN111163771B - 嘧啶并嘧啶酮类作为sik抑制剂的用途 - Google Patents
嘧啶并嘧啶酮类作为sik抑制剂的用途 Download PDFInfo
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- CN111163771B CN111163771B CN201880027619.8A CN201880027619A CN111163771B CN 111163771 B CN111163771 B CN 111163771B CN 201880027619 A CN201880027619 A CN 201880027619A CN 111163771 B CN111163771 B CN 111163771B
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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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- 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
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- 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
- A61P35/00—Antineoplastic agents
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (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)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Dermatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762464675P | 2017-02-28 | 2017-02-28 | |
| US62/464,675 | 2017-02-28 | ||
| US201762472468P | 2017-03-16 | 2017-03-16 | |
| US62/472,468 | 2017-03-16 | ||
| PCT/US2018/020335 WO2018160774A1 (en) | 2017-02-28 | 2018-02-28 | Uses of pyrimidopyrimidinones as sik inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN111163771A CN111163771A (zh) | 2020-05-15 |
| CN111163771B true CN111163771B (zh) | 2023-07-14 |
Family
ID=63370223
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880027619.8A Active CN111163771B (zh) | 2017-02-28 | 2018-02-28 | 嘧啶并嘧啶酮类作为sik抑制剂的用途 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US11285158B2 (enExample) |
| EP (1) | EP3589284A4 (enExample) |
| JP (2) | JP7296318B2 (enExample) |
| KR (1) | KR20190120331A (enExample) |
| CN (1) | CN111163771B (enExample) |
| AU (1) | AU2018226771B2 (enExample) |
| BR (1) | BR112019017741A2 (enExample) |
| CA (1) | CA3054809A1 (enExample) |
| RU (1) | RU2019129727A (enExample) |
| WO (1) | WO2018160774A1 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2015292818B2 (en) | 2014-07-21 | 2020-01-16 | Dana-Farber Cancer Institute, Inc. | Imidazolyl kinase inhibitors and uses thereof |
| CA3069016A1 (en) | 2016-07-05 | 2018-01-11 | The Broad Institute, Inc. | Bicyclic urea kinase inhibitors and uses thereof |
| WO2018053373A1 (en) | 2016-09-16 | 2018-03-22 | The General Hospital Corporation | Uses of satl-inducible kinase (sik) inhibitors for treating osteoporosis |
| AU2018226771B2 (en) * | 2017-02-28 | 2023-11-23 | Dana-Farber Cancer Institute, Inc. | Uses of pyrimidopyrimidinones as SIK inhibitors |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| US20230048132A1 (en) * | 2018-12-28 | 2023-02-16 | Spv Therapeutics Inc. | Cyclin-dependent kinase inhibitors |
| WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
| TW202100520A (zh) | 2019-03-05 | 2021-01-01 | 美商英塞特公司 | 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物 |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| WO2020223558A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | Tricyclic amine compounds as cdk2 inhibitors |
| IL287795B2 (en) | 2019-05-10 | 2025-05-01 | Deciphera Pharmaceuticals Llc | Heteroarylaminopyrimidine amides as autophagy inhibitors and methods of using them |
| CN118878519A (zh) | 2019-05-10 | 2024-11-01 | 德西费拉制药有限责任公司 | 苯基氨基嘧啶酰胺自噬抑制剂及其使用方法 |
| WO2020257180A1 (en) * | 2019-06-17 | 2020-12-24 | Deciphera Pharmaceuticals, Llc | Aminopyrimidine amide autophagy inhibitors and methods of use thereof |
| TW202115024A (zh) | 2019-08-14 | 2021-04-16 | 美商英塞特公司 | 作為cdk2 抑制劑之咪唑基嘧啶基胺化合物 |
| CN119930610A (zh) | 2019-10-11 | 2025-05-06 | 因赛特公司 | 作为cdk2抑制剂的双环胺 |
| EP3901151A1 (en) | 2020-04-21 | 2021-10-27 | iOmx Therapeutics AG | Halogenated-heteroaryl and other heterocyclic kinase inhibitors, and uses thereof |
| EP4143191A2 (en) | 2020-04-28 | 2023-03-08 | iOmx Therapeutics AG | Bicyclic kinase inhibitors and uses thereof |
| WO2022061312A1 (en) * | 2020-09-21 | 2022-03-24 | Soltego, Inc. | Sik inhibitors and methods of use thereof |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| US20250296928A1 (en) | 2021-10-19 | 2025-09-25 | Iomx Therapeutics Ag | A synthesis scheme and procedures for preparing a sik3 inhibitor and intermediates thereof |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| CN114414681B (zh) * | 2021-12-30 | 2024-10-11 | 珠海天祥粤澳质量技术服务有限公司 | 一种同时测定化妆品中的多种色素的方法 |
| EP4257132A1 (en) | 2022-04-08 | 2023-10-11 | iOmx Therapeutics AG | Sik3 inhibitors for treating diseases resistant to death receptor signalling |
| JP2025517351A (ja) * | 2022-05-17 | 2025-06-05 | ソルテゴ, インコーポレイテッド | ピリミドピリミドン化合物およびその使用方法 |
| WO2025059216A1 (en) * | 2023-09-12 | 2025-03-20 | Dana-Farber Cancer Institute, Inc. | Treatment of high-grade serous carcinoma |
| WO2025157389A1 (en) | 2024-01-22 | 2025-07-31 | Iomx Therapeutics Ag | Combinations of halogenated heterocyclic kinase inhibitors and vegfr inhibitors |
| CN118546871B (zh) * | 2024-05-10 | 2025-05-06 | 未来智人再生医学研究院(广州)有限公司 | 一种人多能干细胞分化为间充质干细胞的方法 |
Citations (2)
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| WO2014093383A1 (en) * | 2012-12-14 | 2014-06-19 | Arrien Pharmaceuticals Llc | Substituted 1h-pyrrolo [2,3-b] pyridine and 1h-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (sik2) inhibitors |
| WO2016023014A2 (en) * | 2014-08-08 | 2016-02-11 | Dana-Farber Cancer Institute, Inc. | Uses of salt-inducible kinase (sik) inhibitors |
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| JP4231559B2 (ja) | 1997-04-23 | 2009-03-04 | オリザ油化株式会社 | リポキシゲナーゼ阻害剤 |
| EE200000706A (et) | 1998-05-26 | 2002-06-17 | Warner-Lambert Company | Bitsüklilised pürimidiinid ja bitsüklilised 3,4-dihüdropürimidiinid kui rakkude proliferatsiooni inhibiitorid |
| EP1123295B1 (en) * | 1998-10-23 | 2004-09-29 | F. Hoffmann-La Roche Ag | Bicyclic nitrogen heterocycles |
| CZ20021744A3 (cs) | 1999-10-21 | 2002-08-14 | F. Hoffmann-La Roche Ag | Bicyklické dusíkové heterocykly substituované heteroalkylaminoskupinou jako inhibitory P38 proteinkinázy |
| US20050202001A1 (en) | 2002-04-24 | 2005-09-15 | Han-Mo Koo | Enhancement of human epidermal melanogenesis |
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| DE10239042A1 (de) | 2002-08-21 | 2004-03-04 | Schering Ag | Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel |
| CA2496234A1 (en) | 2002-08-21 | 2004-03-04 | Protein Express Co., Ltd. | Salt-inducible kinases 2 and use thereof |
| US7129351B2 (en) | 2002-11-04 | 2006-10-31 | Hoffmann-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
| BR0316680A (pt) | 2002-11-28 | 2005-10-18 | Schering Ag | Pirimidinas inibidoras de chk, pdk e akt, sua produção e uso como agentes farmacêuticos |
| KR20050111636A (ko) | 2003-04-10 | 2005-11-25 | 에프. 호프만-라 로슈 아게 | 피리미도 화합물 |
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| RU2401265C2 (ru) | 2004-06-10 | 2010-10-10 | Айрм Ллк | Соединения и композиции в качестве ингибиторов протеинкиназы |
| GB0512324D0 (en) | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| DE602005013248D1 (de) | 2004-08-31 | 2009-04-23 | Hoffmann La Roche | Amidderivate von 3-phenyldihydropyrimidoä4,5-düpyrimidinonen, deren herstellung und verwendung als pharmazeutische mittel |
| WO2006024545A1 (en) | 2004-09-03 | 2006-03-09 | Stichting Voor De Technische Wetenschappen | Fused bicyclic natural compounds and their use as inhibitors of parp and parp-mediated inflammatory processes |
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| WO2007071752A2 (en) | 2005-12-21 | 2007-06-28 | Novartis Ag | Pyrimidinyl aryl urea derivatives being fgf inhibitors |
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| CN102816162B (zh) | 2011-06-10 | 2016-04-27 | 中国科学院广州生物医药与健康研究院 | 嘧啶并嘧啶酮类化合物及其药用组合物和应用 |
| EA025881B1 (ru) | 2011-09-30 | 2017-02-28 | Онкодизайн С.А. | Макроциклические ингибиторы flt3-киназы |
| EP3569598A1 (en) | 2011-11-17 | 2019-11-20 | Dana Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| GB201204384D0 (en) | 2012-03-13 | 2012-04-25 | Univ Dundee | Anti-flammatory agents |
| US9296701B2 (en) | 2012-04-24 | 2016-03-29 | Vertex Pharmaceuticals Incorporated | DNA-PK inhibitors |
| KR20150133767A (ko) | 2013-03-15 | 2015-11-30 | 온코디자인 에스.에이. | 거대고리 염-유도성 키나아제 억제제 |
| SG11201507478VA (en) | 2013-03-15 | 2015-10-29 | Celgene Avilomics Res Inc | Heteroaryl compounds and uses thereof |
| AU2014287209B2 (en) * | 2013-07-09 | 2019-01-24 | Dana-Farber Cancer Institute, Inc. | Kinase inhibitors for the treatment of disease |
| AU2015292818B2 (en) | 2014-07-21 | 2020-01-16 | Dana-Farber Cancer Institute, Inc. | Imidazolyl kinase inhibitors and uses thereof |
| WO2016014551A1 (en) | 2014-07-21 | 2016-01-28 | Dana-Farber Cancer Institute, Inc. | Macrocyclic kinase inhibitors and uses thereof |
| KR101850282B1 (ko) | 2014-11-26 | 2018-05-31 | 한국과학기술연구원 | 단백질 키나아제 저해제로 유용한 헤테로아릴아민 유도체 |
| CN104482860B (zh) | 2014-12-05 | 2017-10-31 | 浙江大学宁波理工学院 | 鱼类形态参数自动测量装置和方法 |
| CA3069016A1 (en) | 2016-07-05 | 2018-01-11 | The Broad Institute, Inc. | Bicyclic urea kinase inhibitors and uses thereof |
| WO2018053373A1 (en) | 2016-09-16 | 2018-03-22 | The General Hospital Corporation | Uses of satl-inducible kinase (sik) inhibitors for treating osteoporosis |
| AU2018226771B2 (en) * | 2017-02-28 | 2023-11-23 | Dana-Farber Cancer Institute, Inc. | Uses of pyrimidopyrimidinones as SIK inhibitors |
-
2018
- 2018-02-28 AU AU2018226771A patent/AU2018226771B2/en active Active
- 2018-02-28 JP JP2019547113A patent/JP7296318B2/ja active Active
- 2018-02-28 KR KR1020197028441A patent/KR20190120331A/ko not_active Ceased
- 2018-02-28 EP EP18760857.5A patent/EP3589284A4/en active Pending
- 2018-02-28 CN CN201880027619.8A patent/CN111163771B/zh active Active
- 2018-02-28 CA CA3054809A patent/CA3054809A1/en active Pending
- 2018-02-28 US US16/489,462 patent/US11285158B2/en active Active
- 2018-02-28 RU RU2019129727A patent/RU2019129727A/ru unknown
- 2018-02-28 BR BR112019017741A patent/BR112019017741A2/pt not_active Application Discontinuation
- 2018-02-28 WO PCT/US2018/020335 patent/WO2018160774A1/en not_active Ceased
-
2021
- 2021-11-22 US US17/532,215 patent/US11878019B2/en active Active
-
2023
- 2023-03-17 JP JP2023043357A patent/JP2023088968A/ja active Pending
- 2023-11-29 US US18/522,929 patent/US20240245695A1/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014093383A1 (en) * | 2012-12-14 | 2014-06-19 | Arrien Pharmaceuticals Llc | Substituted 1h-pyrrolo [2,3-b] pyridine and 1h-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (sik2) inhibitors |
| WO2016023014A2 (en) * | 2014-08-08 | 2016-02-11 | Dana-Farber Cancer Institute, Inc. | Uses of salt-inducible kinase (sik) inhibitors |
Non-Patent Citations (3)
| Title |
|---|
| A Potent Inhibitor of SIK2, 3, 3’, 7-Trihydroxy-4’-Methoxyflavon (4’-O-Methylfisetin), Promotes Melanogenesis in B16F10 Melanoma Cells;Ayako Kumagai et al.;《PLoS ONE》;20111013;第6卷(第10期);摘要,第1页左栏第1段,图2-图4 * |
| Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function In Vivo;Thomas B. Sundberg et al.;《ACS Chemical Biology》;20160819;第11卷(第8期);表1 * |
| Downregulation of SIK2 expression promotes the melanogenic program in mice;Nanao Horike et al.;《Pigment Cell Melanoma Research》;20100831;第23卷(第6期);第809页摘要,第815页左栏第2段 * |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2023088968A (ja) | 2023-06-27 |
| AU2018226771B2 (en) | 2023-11-23 |
| CA3054809A1 (en) | 2018-09-07 |
| CN111163771A (zh) | 2020-05-15 |
| AU2018226771A1 (en) | 2019-09-19 |
| BR112019017741A2 (pt) | 2020-04-07 |
| US11285158B2 (en) | 2022-03-29 |
| JP2020509022A (ja) | 2020-03-26 |
| US20200253981A1 (en) | 2020-08-13 |
| US20240245695A1 (en) | 2024-07-25 |
| EP3589284A4 (en) | 2020-12-16 |
| JP7296318B2 (ja) | 2023-06-22 |
| KR20190120331A (ko) | 2019-10-23 |
| RU2019129727A (ru) | 2021-03-30 |
| US20220133736A1 (en) | 2022-05-05 |
| US11878019B2 (en) | 2024-01-23 |
| EP3589284A1 (en) | 2020-01-08 |
| WO2018160774A1 (en) | 2018-09-07 |
| RU2019129727A3 (enExample) | 2021-07-02 |
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