KR20190120331A - Sik 억제제로서의 피리미도피리미디논의 용도 - Google Patents
Sik 억제제로서의 피리미도피리미디논의 용도 Download PDFInfo
- Publication number
- KR20190120331A KR20190120331A KR1020197028441A KR20197028441A KR20190120331A KR 20190120331 A KR20190120331 A KR 20190120331A KR 1020197028441 A KR1020197028441 A KR 1020197028441A KR 20197028441 A KR20197028441 A KR 20197028441A KR 20190120331 A KR20190120331 A KR 20190120331A
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- Prior art keywords
- substituted
- unsubstituted
- pharmaceutically acceptable
- certain embodiments
- acceptable salt
- Prior art date
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- 0 CCC1**CC1 Chemical compound CCC1**CC1 0.000 description 31
- HEGPEXRCAPJWOZ-UHFFFAOYSA-N CCCCNC(C1CCC1)=O Chemical compound CCCCNC(C1CCC1)=O HEGPEXRCAPJWOZ-UHFFFAOYSA-N 0.000 description 1
- JDQNYWYMNFRKNQ-UHFFFAOYSA-N CCc1c(C)ccnc1 Chemical compound CCc1c(C)ccnc1 JDQNYWYMNFRKNQ-UHFFFAOYSA-N 0.000 description 1
- OSNMRWURXNWCGA-UHFFFAOYSA-N Cc(c(OC)c1)ccc1OC Chemical compound Cc(c(OC)c1)ccc1OC OSNMRWURXNWCGA-UHFFFAOYSA-N 0.000 description 1
- VZFQJLBLKCGKLU-CQIPHJFXSA-N Cc(cccc1C)c1N(Cc1cnc(N2)nc1N1C/C=C\COCc3cc2ccc3-c2cccc(C)c2N(Cc2c(N3C/C=C/C(Cc4cccc(C)c4N(Cc4cnc(N5)nc4N4C/C=C\COc6cc5ccc6N5CCN(C)CC5)C4=O)OCc4cc(N5)ccc4)nc5nc2)C3=O)C1=O Chemical compound Cc(cccc1C)c1N(Cc1cnc(N2)nc1N1C/C=C\COCc3cc2ccc3-c2cccc(C)c2N(Cc2c(N3C/C=C/C(Cc4cccc(C)c4N(Cc4cnc(N5)nc4N4C/C=C\COc6cc5ccc6N5CCN(C)CC5)C4=O)OCc4cc(N5)ccc4)nc5nc2)C3=O)C1=O VZFQJLBLKCGKLU-CQIPHJFXSA-N 0.000 description 1
- REWJTILYPJSFSB-GUBXDBFYSA-N Cc(cccc1C)c1N(Cc1cnc(Nc2cccc3c2)nc1N1C/C=C\C[O]3c(cc2)c(C)c(N(Cc3cnc(N4)nc3N3C/C=C/COCc5cccc4c5)C3=O)c2Cl)C1=O Chemical compound Cc(cccc1C)c1N(Cc1cnc(Nc2cccc3c2)nc1N1C/C=C\C[O]3c(cc2)c(C)c(N(Cc3cnc(N4)nc3N3C/C=C/COCc5cccc4c5)C3=O)c2Cl)C1=O REWJTILYPJSFSB-GUBXDBFYSA-N 0.000 description 1
- AITBCKULROBTPQ-UHFFFAOYSA-N Cc(cccc1C)c1OC=O Chemical compound Cc(cccc1C)c1OC=O AITBCKULROBTPQ-UHFFFAOYSA-N 0.000 description 1
- UYZTUKMKOIQWKQ-DVZJXXBHSA-N Cc(cccc1C/C(/COc2cc(Nc3nc4c(CN5c6c(Cc(c(COC/C=C\CN7C(N(C8)c9c(C)cccc9Cl)=O)c9)ccc9Nc9ncc8c7n9)cccc6Cl)cn3)ccc2)=C/CN4C5=O)c1N(Cc1cnc(N2)nc1N1C/C=C/COc3cc2ccc3N2CCN(C)CC2)C1=O Chemical compound Cc(cccc1C/C(/COc2cc(Nc3nc4c(CN5c6c(Cc(c(COC/C=C\CN7C(N(C8)c9c(C)cccc9Cl)=O)c9)ccc9Nc9ncc8c7n9)cccc6Cl)cn3)ccc2)=C/CN4C5=O)c1N(Cc1cnc(N2)nc1N1C/C=C/COc3cc2ccc3N2CCN(C)CC2)C1=O UYZTUKMKOIQWKQ-DVZJXXBHSA-N 0.000 description 1
- SLIYMEVBEFGQOE-NSCUHMNNSA-N Cc(cccc1Cl)c1N(Cc1c(N2C/C=C/COc3cc(N4)ccc3)nc4nc1)C2=O Chemical compound Cc(cccc1Cl)c1N(Cc1c(N2C/C=C/COc3cc(N4)ccc3)nc4nc1)C2=O SLIYMEVBEFGQOE-NSCUHMNNSA-N 0.000 description 1
- NVLHGZIXTRYOKT-UHFFFAOYSA-N Cc1cccc(Cl)c1C Chemical compound Cc1cccc(Cl)c1C NVLHGZIXTRYOKT-UHFFFAOYSA-N 0.000 description 1
- YXFVVABEGXRONW-UHFFFAOYSA-N Cc1ccccc1 Chemical compound Cc1ccccc1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- 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
- 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
- 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)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (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 (1)
| Publication Number | Publication Date |
|---|---|
| KR20190120331A true KR20190120331A (ko) | 2019-10-23 |
Family
ID=63370223
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197028441A Ceased KR20190120331A (ko) | 2017-02-28 | 2018-02-28 | Sik 억제제로서의 피리미도피리미디논의 용도 |
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) |
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| EP3171874B1 (en) | 2014-07-21 | 2020-11-18 | Dana-Farber Cancer Institute, Inc. | Imidazolyl kinase inhibitors and uses thereof |
| JP7277357B2 (ja) | 2016-07-05 | 2023-05-18 | ザ ブロード インスティテュート,インコーポレーテッド | 二環式尿素キナーゼインヒビターおよびそれらの使用 |
| WO2018053373A1 (en) | 2016-09-16 | 2018-03-22 | The General Hospital Corporation | Uses of satl-inducible kinase (sik) inhibitors for treating osteoporosis |
| EP3589284A4 (en) * | 2017-02-28 | 2020-12-16 | The General Hospital Corporation | 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 |
| WO2020140055A1 (en) * | 2018-12-28 | 2020-07-02 | 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 |
| US11472791B2 (en) | 2019-03-05 | 2022-10-18 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| PT3966206T (pt) | 2019-05-10 | 2023-11-10 | Deciphera Pharmaceuticals Llc | Inibidores de autofagia de heteroarilaminopirimidina amida e métodos de utilização dos mesmos |
| US11530206B2 (en) | 2019-05-10 | 2022-12-20 | Deciphera Pharmaceuticals, Llc | Phenylaminopyrimidine amide autophagy inhibitors and methods of use thereof |
| JP7626722B2 (ja) * | 2019-06-17 | 2025-02-04 | デシフェラ・ファーマシューティカルズ,エルエルシー | アミノピリミジンアミドオートファジー阻害剤およびその使用方法 |
| BR112022002698A2 (pt) | 2019-08-14 | 2022-07-19 | Incyte Corp | Compostos de imidazolil pirimidinilamina como inibidores de cdk2 |
| AU2020364007A1 (en) | 2019-10-11 | 2022-04-28 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| 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 |
| AU2021343539A1 (en) * | 2020-09-21 | 2023-05-18 | 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 |
| KR20240115232A (ko) | 2021-10-19 | 2024-07-25 | 아이오엠엑스 테라퓨틱스 아게 | Sik3 억제제 및 이의 중간체를 제조하기 위한 합성 반응식 및 과정 |
| 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 |
| WO2023225097A1 (en) * | 2022-05-17 | 2023-11-23 | Soltego, Inc. | Pyrimidopyrimidone compounds and methods of use thereof |
| 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 |
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| NZ510760A (en) | 1998-10-23 | 2003-08-29 | F | Bicyclic nitrogen heterocycles |
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| GB201204384D0 (en) | 2012-03-13 | 2012-04-25 | Univ Dundee | Anti-flammatory agents |
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| AU2014228746B2 (en) | 2013-03-15 | 2018-08-30 | Celgene Car Llc | Heteroaryl compounds and uses thereof |
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| EP3171874B1 (en) | 2014-07-21 | 2020-11-18 | Dana-Farber Cancer Institute, Inc. | Imidazolyl kinase inhibitors and uses thereof |
| CA2954187C (en) | 2014-07-21 | 2022-08-16 | Dana-Farber Cancer Institute, Inc. | Macrocyclic kinase inhibitors and uses thereof |
| EP3177295A4 (en) | 2014-08-08 | 2018-06-13 | Dana Farber Cancer Institute, Inc. | Uses of salt-inducible kinase (sik) inhibitors |
| 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 |
| JP7277357B2 (ja) | 2016-07-05 | 2023-05-18 | ザ ブロード インスティテュート,インコーポレーテッド | 二環式尿素キナーゼインヒビターおよびそれらの使用 |
| WO2018053373A1 (en) | 2016-09-16 | 2018-03-22 | The General Hospital Corporation | Uses of satl-inducible kinase (sik) inhibitors for treating osteoporosis |
| EP3589284A4 (en) * | 2017-02-28 | 2020-12-16 | The General Hospital Corporation | USES OF PYRIMIDOPYRIMIDINONES AS SIK INHIBITORS |
-
2018
- 2018-02-28 EP EP18760857.5A patent/EP3589284A4/en active Pending
- 2018-02-28 US US16/489,462 patent/US11285158B2/en active Active
- 2018-02-28 CA CA3054809A patent/CA3054809A1/en active Pending
- 2018-02-28 JP JP2019547113A patent/JP7296318B2/ja active Active
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| US20200253981A1 (en) | 2020-08-13 |
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| JP2023088968A (ja) | 2023-06-27 |
| CA3054809A1 (en) | 2018-09-07 |
| BR112019017741A2 (pt) | 2020-04-07 |
| US20220133736A1 (en) | 2022-05-05 |
| WO2018160774A1 (en) | 2018-09-07 |
| AU2018226771A1 (en) | 2019-09-19 |
| JP2020509022A (ja) | 2020-03-26 |
| EP3589284A4 (en) | 2020-12-16 |
| EP3589284A1 (en) | 2020-01-08 |
| CN111163771A (zh) | 2020-05-15 |
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