RU2019129727A - Применения пиримидопиримидинонов в качестве ингибиторов sik - Google Patents
Применения пиримидопиримидинонов в качестве ингибиторов sik Download PDFInfo
- Publication number
- RU2019129727A RU2019129727A RU2019129727A RU2019129727A RU2019129727A RU 2019129727 A RU2019129727 A RU 2019129727A RU 2019129727 A RU2019129727 A RU 2019129727A RU 2019129727 A RU2019129727 A RU 2019129727A RU 2019129727 A RU2019129727 A RU 2019129727A
- Authority
- RU
- Russia
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- hydrogen
- protecting group
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 62
- 125000000623 heterocyclic group Chemical group 0.000 claims 55
- 229910052739 hydrogen Inorganic materials 0.000 claims 53
- 239000001257 hydrogen Substances 0.000 claims 51
- 125000001072 heteroaryl group Chemical group 0.000 claims 49
- 150000002431 hydrogen Chemical class 0.000 claims 44
- 125000003118 aryl group Chemical group 0.000 claims 34
- 125000004452 carbocyclyl group Chemical group 0.000 claims 34
- 125000003342 alkenyl group Chemical group 0.000 claims 33
- 125000000304 alkynyl group Chemical group 0.000 claims 33
- 229910052736 halogen Inorganic materials 0.000 claims 28
- 150000002367 halogens Chemical group 0.000 claims 28
- 150000003839 salts Chemical class 0.000 claims 27
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 26
- 239000013078 crystal Substances 0.000 claims 25
- 238000000034 method Methods 0.000 claims 25
- 239000000651 prodrug Substances 0.000 claims 25
- 229940002612 prodrug Drugs 0.000 claims 25
- 239000012453 solvate Substances 0.000 claims 25
- 125000002252 acyl group Chemical group 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 17
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 13
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 12
- 229910052717 sulfur Inorganic materials 0.000 claims 12
- 125000004430 oxygen atom Chemical group O* 0.000 claims 11
- 125000004434 sulfur atom Chemical group 0.000 claims 11
- 125000004429 atom Chemical group 0.000 claims 10
- 229910052757 nitrogen Inorganic materials 0.000 claims 10
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 4
- 230000001681 protective effect Effects 0.000 claims 4
- 208000012641 Pigmentation disease Diseases 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 102000013760 Microphthalmia-Associated Transcription Factor Human genes 0.000 claims 1
- 108010050345 Microphthalmia-Associated Transcription Factor Proteins 0.000 claims 1
- 208000009795 Microphthalmos Diseases 0.000 claims 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 1
- 102000040945 Transcription factor Human genes 0.000 claims 1
- 108091023040 Transcription factor Proteins 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 201000010478 microphthalmia Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
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
Landscapes
- 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 (2)
| Publication Number | Publication Date |
|---|---|
| RU2019129727A true RU2019129727A (ru) | 2021-03-30 |
| RU2019129727A3 RU2019129727A3 (https=) | 2021-07-02 |
Family
ID=63370223
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2019129727A RU2019129727A (ru) | 2017-02-28 | 2018-02-28 | Применения пиримидопиримидинонов в качестве ингибиторов sik |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US11285158B2 (https=) |
| EP (1) | EP3589284A4 (https=) |
| JP (2) | JP7296318B2 (https=) |
| KR (1) | KR20190120331A (https=) |
| CN (1) | CN111163771B (https=) |
| AU (1) | AU2018226771B2 (https=) |
| BR (1) | BR112019017741A2 (https=) |
| CA (1) | CA3054809A1 (https=) |
| RU (1) | RU2019129727A (https=) |
| WO (1) | WO2018160774A1 (https=) |
Families Citing this family (30)
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| AU2015292818B2 (en) | 2014-07-21 | 2020-01-16 | Dana-Farber Cancer Institute, Inc. | Imidazolyl kinase inhibitors and uses thereof |
| AU2017291812B2 (en) | 2016-07-05 | 2023-12-14 | Dana-Farber Cancer 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 |
| BR112019017741A2 (pt) * | 2017-02-28 | 2020-04-07 | Dana Farber Cancer Inst Inc | usos de pirimidopirimidinonas como inibidores de sik |
| 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 |
| WO2020180959A1 (en) | 2019-03-05 | 2020-09-10 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| WO2020223558A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | Tricyclic amine compounds as cdk2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| MX2021013662A (es) | 2019-05-10 | 2022-03-11 | Deciphera Pharmaceuticals Llc | Inhibidores de la autofagia de heteroarilaminopirimidina amida y metodos de uso de estos. |
| EP3966207B1 (en) | 2019-05-10 | 2023-11-01 | Deciphera Pharmaceuticals, LLC | Phenylaminopyrimidine amide autophagy inhibitors and methods of use thereof |
| IL325201A (en) | 2019-06-17 | 2026-02-01 | Deciphera Pharmaceuticals Llc | Aminopyrimidine amide autophagy inhibitors and methods of using them |
| 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 |
| AU2020364007A1 (en) | 2019-10-11 | 2022-04-28 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| GB201915828D0 (en) | 2019-10-31 | 2019-12-18 | Cancer Research Tech Ltd | Compounds, compositions and therapeutic uses thereof |
| EP3901151B1 (en) | 2020-04-21 | 2026-04-01 | iOmx Therapeutics AG | Halogenated-heteroaryl and other heterocyclic kinase inhibitors, and uses thereof |
| CA3177164A1 (en) | 2020-04-28 | 2021-11-04 | Peter Sennhenn | Bicyclic kinase inhibitors and uses thereof |
| WO2022061312A1 (en) * | 2020-09-21 | 2022-03-24 | Soltego, Inc. | Sik inhibitors and methods of use thereof |
| CN116529251A (zh) * | 2020-12-02 | 2023-08-01 | 上海瑛派药业有限公司 | 取代的稠合双环化合物作为激酶抑制剂及其应用 |
| 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 |
| EP4526307A1 (en) * | 2022-05-17 | 2025-03-26 | 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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| AU2015292818B2 (en) | 2014-07-21 | 2020-01-16 | Dana-Farber Cancer Institute, Inc. | Imidazolyl kinase inhibitors and uses thereof |
| AU2015300782B2 (en) | 2014-08-08 | 2020-04-16 | 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 |
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| AU2017291812B2 (en) | 2016-07-05 | 2023-12-14 | Dana-Farber Cancer 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 |
| BR112019017741A2 (pt) * | 2017-02-28 | 2020-04-07 | Dana Farber Cancer Inst Inc | usos de pirimidopirimidinonas como inibidores de sik |
-
2018
- 2018-02-28 BR BR112019017741A patent/BR112019017741A2/pt not_active Application Discontinuation
- 2018-02-28 CA CA3054809A patent/CA3054809A1/en active Pending
- 2018-02-28 JP JP2019547113A patent/JP7296318B2/ja active Active
- 2018-02-28 CN CN201880027619.8A patent/CN111163771B/zh active Active
- 2018-02-28 WO PCT/US2018/020335 patent/WO2018160774A1/en not_active Ceased
- 2018-02-28 US US16/489,462 patent/US11285158B2/en active Active
- 2018-02-28 AU AU2018226771A patent/AU2018226771B2/en active Active
- 2018-02-28 EP EP18760857.5A patent/EP3589284A4/en active Pending
- 2018-02-28 RU RU2019129727A patent/RU2019129727A/ru unknown
- 2018-02-28 KR KR1020197028441A patent/KR20190120331A/ko not_active Ceased
-
2021
- 2021-11-22 US US17/532,215 patent/US11878019B2/en active Active
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2023
- 2023-03-17 JP JP2023043357A patent/JP2023088968A/ja active Pending
- 2023-11-29 US US18/522,929 patent/US20240245695A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| JP2020509022A (ja) | 2020-03-26 |
| CA3054809A1 (en) | 2018-09-07 |
| CN111163771B (zh) | 2023-07-14 |
| KR20190120331A (ko) | 2019-10-23 |
| EP3589284A1 (en) | 2020-01-08 |
| RU2019129727A3 (https=) | 2021-07-02 |
| JP7296318B2 (ja) | 2023-06-22 |
| US11285158B2 (en) | 2022-03-29 |
| CN111163771A (zh) | 2020-05-15 |
| US20220133736A1 (en) | 2022-05-05 |
| JP2023088968A (ja) | 2023-06-27 |
| AU2018226771A1 (en) | 2019-09-19 |
| US20240245695A1 (en) | 2024-07-25 |
| AU2018226771B2 (en) | 2023-11-23 |
| WO2018160774A1 (en) | 2018-09-07 |
| US11878019B2 (en) | 2024-01-23 |
| US20200253981A1 (en) | 2020-08-13 |
| BR112019017741A2 (pt) | 2020-04-07 |
| EP3589284A4 (en) | 2020-12-16 |
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