RU2020115095A - Пиридиновые, пиразиновые и триазиновые соединения в качестве аллостерических ингибиторов shp2 - Google Patents
Пиридиновые, пиразиновые и триазиновые соединения в качестве аллостерических ингибиторов shp2 Download PDFInfo
- Publication number
- RU2020115095A RU2020115095A RU2020115095A RU2020115095A RU2020115095A RU 2020115095 A RU2020115095 A RU 2020115095A RU 2020115095 A RU2020115095 A RU 2020115095A RU 2020115095 A RU2020115095 A RU 2020115095A RU 2020115095 A RU2020115095 A RU 2020115095A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- optionally substituted
- heterocycle
- heteroaryl
- halogen
- Prior art date
Links
- 102100033019 Tyrosine-protein phosphatase non-receptor type 11 Human genes 0.000 title claims 3
- 101710116241 Tyrosine-protein phosphatase non-receptor type 11 Proteins 0.000 title claims 3
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 title 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 title 2
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 title 1
- 230000003281 allosteric effect Effects 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 title 1
- 150000003918 triazines Chemical class 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 25
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- 229910052736 halogen Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000002950 monocyclic group Chemical group 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 9
- 239000012453 solvate Substances 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 229910052698 phosphorus Inorganic materials 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 5
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 5
- 125000004585 polycyclic heterocycle group Chemical group 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 claims 2
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000003367 polycyclic group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000005101 LEOPARD Syndrome Diseases 0.000 claims 1
- 206010062901 Multiple lentigines syndrome Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000037538 Myelomonocytic Juvenile Leukemia Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010029748 Noonan syndrome Diseases 0.000 claims 1
- 208000010708 Noonan syndrome with multiple lentigines Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 201000005992 juvenile myelomonocytic leukemia Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000006578 monocyclic heterocycloalkyl group Chemical group 0.000 claims 1
- -1 substituted Chemical class 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- 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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762571760P | 2017-10-12 | 2017-10-12 | |
| US62/571,760 | 2017-10-12 | ||
| US201862615353P | 2018-01-09 | 2018-01-09 | |
| US62/615,353 | 2018-01-09 | ||
| US201862678889P | 2018-05-31 | 2018-05-31 | |
| US62/678,889 | 2018-05-31 | ||
| PCT/US2018/055502 WO2019075265A1 (en) | 2017-10-12 | 2018-10-11 | PYRIDINE, PYRAZINE AND TRIAZINE COMPOUNDS AS ALLOSTERIC INHIBITORS OF SHP2 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2020115095A true RU2020115095A (ru) | 2021-11-12 |
| RU2020115095A3 RU2020115095A3 (https=) | 2022-01-31 |
Family
ID=64049755
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2020115095A RU2020115095A (ru) | 2017-10-12 | 2018-10-11 | Пиридиновые, пиразиновые и триазиновые соединения в качестве аллостерических ингибиторов shp2 |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US11702411B2 (https=) |
| EP (1) | EP3694848A1 (https=) |
| JP (1) | JP2020536881A (https=) |
| KR (1) | KR20200070295A (https=) |
| CN (1) | CN111212834B (https=) |
| AU (1) | AU2018347516A1 (https=) |
| BR (1) | BR112020007058A2 (https=) |
| CA (1) | CA3078565A1 (https=) |
| CO (1) | CO2020003714A2 (https=) |
| IL (1) | IL273756A (https=) |
| MX (1) | MX2020003579A (https=) |
| PH (1) | PH12020550216A1 (https=) |
| RU (1) | RU2020115095A (https=) |
| SG (1) | SG11202002941WA (https=) |
| TW (1) | TW201930292A (https=) |
| WO (1) | WO2019075265A1 (https=) |
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| WO2017210134A1 (en) | 2016-05-31 | 2017-12-07 | Board Of Regents, University Of Texas System | Heterocyclic inhibitors of ptpn11 |
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| JP2022508651A (ja) | 2018-10-08 | 2022-01-19 | レヴォリューション・メディスンズ，インコーポレイテッド | 癌を処置するためのｓｈｐ２阻害剤組成物および方法 |
| JP2022506887A (ja) | 2018-11-07 | 2022-01-17 | シャンハイ リンジーン バイオファーマ カンパニー リミテッド | 窒素含有縮合複素環系ｓｈｐ２阻害剤化合物、製造方法及び使用 |
| JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法 |
| EP3889153A4 (en) | 2018-11-30 | 2022-09-07 | Tuojie Biotech (Shanghai) Co., Ltd. | PYRIMIDINE AND FIVE-MEMBERED HETEROCYCLIC NITROGEN DERIVATIVE, METHOD OF MANUFACTURE THEREOF AND MEDICAL USES THEREOF |
| US20220073521A1 (en) | 2018-11-30 | 2022-03-10 | Tuojie Biotech (Shanghai) Co., Ltd. | Pyrimidine and five-membered nitrogen heterocycle derivative, preparation method therefor, and medical uses thereof |
| BR112021012057A2 (pt) | 2018-12-21 | 2021-10-19 | Revolution Medicines, Inc. | Compostos que participam de ligação cooperativa e usos dos mesmos |
| IL322454A (en) | 2019-11-04 | 2025-09-01 | Revolution Medicines Inc | ras inhibitors |
-
2018
- 2018-10-11 TW TW107135797A patent/TW201930292A/zh unknown
- 2018-10-11 KR KR1020207013076A patent/KR20200070295A/ko not_active Ceased
- 2018-10-11 AU AU2018347516A patent/AU2018347516A1/en not_active Abandoned
- 2018-10-11 WO PCT/US2018/055502 patent/WO2019075265A1/en not_active Ceased
- 2018-10-11 CA CA3078565A patent/CA3078565A1/en not_active Abandoned
- 2018-10-11 SG SG11202002941WA patent/SG11202002941WA/en unknown
- 2018-10-11 JP JP2020519790A patent/JP2020536881A/ja active Pending
- 2018-10-11 MX MX2020003579A patent/MX2020003579A/es unknown
- 2018-10-11 RU RU2020115095A patent/RU2020115095A/ru unknown
- 2018-10-11 BR BR112020007058-0A patent/BR112020007058A2/pt not_active Application Discontinuation
- 2018-10-11 EP EP18795913.5A patent/EP3694848A1/en not_active Withdrawn
- 2018-10-11 CN CN201880066291.0A patent/CN111212834B/zh not_active Expired - Fee Related
-
2020
- 2020-03-27 CO CONC2020/0003714A patent/CO2020003714A2/es unknown
- 2020-03-31 PH PH12020550216A patent/PH12020550216A1/en unknown
- 2020-04-01 IL IL273756A patent/IL273756A/en unknown
- 2020-04-10 US US16/845,539 patent/US11702411B2/en active Active
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2023
- 2023-04-05 US US18/131,226 patent/US20240067636A1/en not_active Abandoned
Also Published As
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|---|---|
| TW201930292A (zh) | 2019-08-01 |
| SG11202002941WA (en) | 2020-04-29 |
| US20240067636A1 (en) | 2024-02-29 |
| CN111212834B (zh) | 2024-01-19 |
| EP3694848A1 (en) | 2020-08-19 |
| CA3078565A1 (en) | 2019-04-18 |
| RU2020115095A3 (https=) | 2022-01-31 |
| AU2018347516A1 (en) | 2020-05-07 |
| CN111212834A (zh) | 2020-05-29 |
| US11702411B2 (en) | 2023-07-18 |
| US20200339552A1 (en) | 2020-10-29 |
| JP2020536881A (ja) | 2020-12-17 |
| KR20200070295A (ko) | 2020-06-17 |
| IL273756A (en) | 2020-05-31 |
| MX2020003579A (es) | 2020-07-22 |
| PH12020550216A1 (en) | 2021-02-15 |
| BR112020007058A2 (pt) | 2020-10-06 |
| CO2020003714A2 (es) | 2020-04-24 |
| WO2019075265A1 (en) | 2019-04-18 |
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