RU2020115596A - ПИРИМИДИНОВЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ TBK/IKKε И ИХ ПРИМЕНЕНИЯ - Google Patents
ПИРИМИДИНОВЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ TBK/IKKε И ИХ ПРИМЕНЕНИЯ Download PDFInfo
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- RU2020115596A RU2020115596A RU2020115596A RU2020115596A RU2020115596A RU 2020115596 A RU2020115596 A RU 2020115596A RU 2020115596 A RU2020115596 A RU 2020115596A RU 2020115596 A RU2020115596 A RU 2020115596A RU 2020115596 A RU2020115596 A RU 2020115596A
- Authority
- RU
- Russia
- Prior art keywords
- compound according
- nrc
- ring
- halogen
- pharmaceutically acceptable
- Prior art date
Links
- 102000001284 I-kappa-B kinase Human genes 0.000 title claims 3
- 108060006678 I-kappa-B kinase Proteins 0.000 title claims 3
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical class C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title claims 2
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 19
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 150000004677 hydrates Chemical class 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 5
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 5
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 239000001301 oxygen Chemical group 0.000 claims 5
- 229910052717 sulfur Chemical group 0.000 claims 5
- 239000011593 sulfur Chemical group 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 125000001931 aliphatic group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 208000007815 Acquired Hyperostosis Syndrome Diseases 0.000 claims 1
- 208000026326 Adult-onset Still disease Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010008690 Chondrocalcinosis pyrophosphate Diseases 0.000 claims 1
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- 102100026018 Interleukin-1 receptor antagonist protein Human genes 0.000 claims 1
- 101710144554 Interleukin-1 receptor antagonist protein Proteins 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000005777 Lupus Nephritis Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 201000004854 SAPHO syndrome Diseases 0.000 claims 1
- 201000010848 Schnitzler Syndrome Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 125000002527 bicyclic carbocyclic group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 208000002849 chondrocalcinosis Diseases 0.000 claims 1
- 208000022993 cryopyrin-associated periodic syndrome Diseases 0.000 claims 1
- 230000007812 deficiency Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 210000000936 intestine Anatomy 0.000 claims 1
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 1
- 206010072221 mevalonate kinase deficiency Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 125000003003 spiro group Chemical group 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Classifications
-
- 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
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- 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
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762573251P | 2017-10-17 | 2017-10-17 | |
| US62/573,251 | 2017-10-17 | ||
| PCT/US2018/056190 WO2019079373A1 (en) | 2017-10-17 | 2018-10-17 | PYRIMIDINE TBK / IKKε INHIBITORY COMPOUNDS AND USES THEREOF |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2020115596A3 RU2020115596A3 (enExample) | 2021-11-18 |
| RU2020115596A true RU2020115596A (ru) | 2021-11-18 |
Family
ID=64110185
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2020115596A RU2020115596A (ru) | 2017-10-17 | 2018-10-17 | ПИРИМИДИНОВЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ TBK/IKKε И ИХ ПРИМЕНЕНИЯ |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20230019491A1 (enExample) |
| EP (1) | EP3697772A1 (enExample) |
| JP (1) | JP7266592B2 (enExample) |
| KR (1) | KR20200072519A (enExample) |
| CN (1) | CN111247135A (enExample) |
| AU (1) | AU2018352699A1 (enExample) |
| BR (1) | BR112020007466A2 (enExample) |
| CA (1) | CA3078579A1 (enExample) |
| IL (1) | IL273891A (enExample) |
| MX (1) | MX2020003507A (enExample) |
| RU (1) | RU2020115596A (enExample) |
| SG (1) | SG11202003407VA (enExample) |
| TW (1) | TWI802604B (enExample) |
| WO (1) | WO2019079373A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019079375A1 (en) * | 2017-10-17 | 2019-04-25 | Merck Patent Gmbh | IN / ΙΚΚΕ PYRIMIDINE INHIBITOR COMPOUNDS AND USES THEREOF |
| WO2019236699A1 (en) | 2018-06-05 | 2019-12-12 | Crinetics Pharmaceuticals, Inc. | Melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof |
| CN112552280A (zh) * | 2019-09-25 | 2021-03-26 | 常州强力先端电子材料有限公司 | 一种高产酸的磺酰亚胺类光产酸剂 |
| JP7657792B2 (ja) * | 2019-11-07 | 2025-04-07 | クリネティックス ファーマシューティカルズ，インク． | メラノコルチンサブタイプ－２受容体（ｍｃ２ｒ）アンタゴニストおよびその使用 |
| EP4077307B1 (en) | 2019-12-18 | 2025-03-12 | Crinetics Pharmaceuticals, Inc. | Gem-disubstituted piperidine melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof |
| WO2021133563A1 (en) | 2019-12-23 | 2021-07-01 | Crinetics Pharmaceuticals, Inc. | Spirocyclic piperidine melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof |
| CA3211644A1 (en) | 2021-03-19 | 2022-09-22 | Christine FERRARA-COOK | Melanocortin subtype-2 receptor (mc2r) antagonist for the treatment of disease |
| CN117447407B (zh) * | 2023-12-19 | 2024-06-11 | 潍坊医学院 | 一种JAK2抑制剂Pacritinib及其中间体的制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2911139A1 (fr) * | 2007-01-05 | 2008-07-11 | Sanofi Aventis Sa | Nouveaux derives de phenyl-(4-phenyl-pyrimidin-2-yl)amines, leur preparation a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk |
| WO2009032861A1 (en) * | 2007-09-04 | 2009-03-12 | The Scripps Research Institute | Substituted pyrimidinyl-amines as protein kinase inhibitors |
| EP2488503A1 (en) | 2009-10-12 | 2012-08-22 | Myrexis, Inc. | Amino - pyrimidine compounds as inhibitors of tbkl and/or ikk epsilon |
| GB201012105D0 (en) | 2010-07-19 | 2010-09-01 | Domainex Ltd | Novel pyrimidine compounds |
| CA2832919A1 (en) * | 2011-04-12 | 2012-10-18 | Ryan C. Holcomb | Compounds, compositions, and therapeutic uses thereof |
| DE102011112978A1 (de) * | 2011-09-09 | 2013-03-14 | Merck Patent Gmbh | Benzonitrilderivate |
| US9988391B2 (en) | 2015-06-29 | 2018-06-05 | Merck Patent Gmbh | TBK/IKK inhibitor compounds and uses thereof |
-
2018
- 2018-10-17 MX MX2020003507A patent/MX2020003507A/es unknown
- 2018-10-17 TW TW107136567A patent/TWI802604B/zh not_active IP Right Cessation
- 2018-10-17 KR KR1020207014078A patent/KR20200072519A/ko not_active Withdrawn
- 2018-10-17 CN CN201880067979.0A patent/CN111247135A/zh active Pending
- 2018-10-17 RU RU2020115596A patent/RU2020115596A/ru unknown
- 2018-10-17 WO PCT/US2018/056190 patent/WO2019079373A1/en not_active Ceased
- 2018-10-17 SG SG11202003407VA patent/SG11202003407VA/en unknown
- 2018-10-17 CA CA3078579A patent/CA3078579A1/en active Pending
- 2018-10-17 JP JP2020521968A patent/JP7266592B2/ja active Active
- 2018-10-17 EP EP18797386.2A patent/EP3697772A1/en not_active Withdrawn
- 2018-10-17 US US16/756,769 patent/US20230019491A1/en not_active Abandoned
- 2018-10-17 BR BR112020007466-7A patent/BR112020007466A2/pt not_active IP Right Cessation
- 2018-10-17 AU AU2018352699A patent/AU2018352699A1/en not_active Abandoned
-
2020
- 2020-04-07 IL IL273891A patent/IL273891A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2019079373A1 (en) | 2019-04-25 |
| TWI802604B (zh) | 2023-05-21 |
| SG11202003407VA (en) | 2020-05-28 |
| AU2018352699A1 (en) | 2020-05-28 |
| JP7266592B2 (ja) | 2023-04-28 |
| CA3078579A1 (en) | 2019-04-25 |
| BR112020007466A2 (pt) | 2020-09-24 |
| JP2020537671A (ja) | 2020-12-24 |
| MX2020003507A (es) | 2020-07-22 |
| KR20200072519A (ko) | 2020-06-22 |
| RU2020115596A3 (enExample) | 2021-11-18 |
| US20230019491A1 (en) | 2023-01-19 |
| IL273891A (en) | 2020-05-31 |
| EP3697772A1 (en) | 2020-08-26 |
| TW201922735A (zh) | 2019-06-16 |
| CN111247135A (zh) | 2020-06-05 |
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