RU2019126455A - Пиридиновые соединения в качестве аллостерических ингибиторов shp2 - Google Patents
Пиридиновые соединения в качестве аллостерических ингибиторов shp2 Download PDFInfo
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- RU2019126455A RU2019126455A RU2019126455A RU2019126455A RU2019126455A RU 2019126455 A RU2019126455 A RU 2019126455A RU 2019126455 A RU2019126455 A RU 2019126455A RU 2019126455 A RU2019126455 A RU 2019126455A RU 2019126455 A RU2019126455 A RU 2019126455A
- Authority
- RU
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- Prior art keywords
- alkyl
- optionally substituted
- paragraphs
- heterocycle
- cycloalkyl
- Prior art date
Links
- 102100033019 Tyrosine-protein phosphatase non-receptor type 11 Human genes 0.000 title claims 7
- 101710116241 Tyrosine-protein phosphatase non-receptor type 11 Proteins 0.000 title claims 7
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical class C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 title claims 4
- 230000003281 allosteric effect Effects 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 27
- 150000001875 compounds Chemical class 0.000 claims 26
- 125000002950 monocyclic group Chemical group 0.000 claims 16
- 125000001072 heteroaryl group Chemical group 0.000 claims 14
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 150000002367 halogens Chemical class 0.000 claims 12
- 125000004429 atom Chemical group 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 239000000651 prodrug Substances 0.000 claims 10
- 229940002612 prodrug Drugs 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 239000012453 solvate Substances 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 201000010099 disease Diseases 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 125000004585 polycyclic heterocycle group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 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 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 229910052698 phosphorus Inorganic materials 0.000 claims 4
- 125000003367 polycyclic group Chemical group 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 239000012634 fragment Substances 0.000 claims 3
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 3
- -1 substituted Chemical class 0.000 claims 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 208000005101 LEOPARD Syndrome Diseases 0.000 claims 2
- 206010062901 Multiple lentigines syndrome Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 208000037538 Myelomonocytic Juvenile Leukemia Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 206010029748 Noonan syndrome Diseases 0.000 claims 2
- 208000010708 Noonan syndrome with multiple lentigines Diseases 0.000 claims 2
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 2
- 210000000481 breast Anatomy 0.000 claims 2
- 201000005992 juvenile myelomonocytic leukemia Diseases 0.000 claims 2
- 210000004072 lung Anatomy 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
Classifications
-
- 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
-
- 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
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4355—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
-
- 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
- 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
- C07D401/14—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
- 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
- C07D498/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762449529P | 2017-01-23 | 2017-01-23 | |
| US62/449,529 | 2017-01-23 | ||
| PCT/US2018/013018 WO2018136264A1 (en) | 2017-01-23 | 2018-01-09 | Pyridine compounds as allosteric shp2 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2019126455A true RU2019126455A (ru) | 2021-02-24 |
| RU2019126455A3 RU2019126455A3 (enExample) | 2021-05-17 |
Family
ID=61054565
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2019126455A RU2019126455A (ru) | 2017-01-23 | 2018-01-09 | Пиридиновые соединения в качестве аллостерических ингибиторов shp2 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US11673896B2 (enExample) |
| EP (2) | EP3571189B1 (enExample) |
| JP (2) | JP7240320B2 (enExample) |
| KR (1) | KR20190110588A (enExample) |
| CN (1) | CN110431134A (enExample) |
| AU (1) | AU2018210196B2 (enExample) |
| BR (1) | BR112019014527A2 (enExample) |
| CA (1) | CA3051054A1 (enExample) |
| IL (1) | IL268031B (enExample) |
| MX (1) | MX2019008696A (enExample) |
| RU (1) | RU2019126455A (enExample) |
| SG (1) | SG11201906412SA (enExample) |
| WO (1) | WO2018136264A1 (enExample) |
Families Citing this family (102)
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| US11466017B2 (en) | 2011-03-10 | 2022-10-11 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of PTPN11 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| AU2017274199B2 (en) | 2016-05-31 | 2021-09-23 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of PTPN11 |
| CN109415360B (zh) | 2016-06-14 | 2021-11-02 | 诺华股份有限公司 | 用于抑制shp2活性的化合物和组合物 |
| KR102598895B1 (ko) | 2016-07-12 | 2023-11-07 | 레볼루션 메디슨즈, 인크. | 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진 |
| US11529347B2 (en) | 2016-09-22 | 2022-12-20 | Relay Therapeutics, Inc. | SHP2 phosphatase inhibitors and methods of use thereof |
| TW202500565A (zh) | 2016-10-24 | 2025-01-01 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其使用方法 |
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| HRP20230488T1 (hr) | 2018-05-01 | 2023-08-04 | Revolution Medicines, Inc. | C40-, C28- I C-32-VEZANI ANALOZI RAPAMICINA KAO INHIBITORI mTOR |
| MX2020011564A (es) | 2018-05-01 | 2021-01-29 | Revolution Medicines Inc | Analogos de rapamicina unidos a c26 como inhibidores de mtor. |
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-
2018
- 2018-01-09 KR KR1020197024603A patent/KR20190110588A/ko not_active Ceased
- 2018-01-09 MX MX2019008696A patent/MX2019008696A/es unknown
- 2018-01-09 CN CN201880019182.3A patent/CN110431134A/zh active Pending
- 2018-01-09 EP EP18701882.5A patent/EP3571189B1/en active Active
- 2018-01-09 WO PCT/US2018/013018 patent/WO2018136264A1/en not_active Ceased
- 2018-01-09 RU RU2019126455A patent/RU2019126455A/ru unknown
- 2018-01-09 AU AU2018210196A patent/AU2018210196B2/en not_active Ceased
- 2018-01-09 CA CA3051054A patent/CA3051054A1/en not_active Abandoned
- 2018-01-09 JP JP2019539779A patent/JP7240320B2/ja active Active
- 2018-01-09 EP EP23163674.7A patent/EP4230623A3/en not_active Withdrawn
- 2018-01-09 BR BR112019014527-3A patent/BR112019014527A2/pt not_active Application Discontinuation
- 2018-01-09 SG SG11201906412SA patent/SG11201906412SA/en unknown
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2019
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2022
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2023
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| AU2018210196A1 (en) | 2019-08-15 |
| EP4230623A2 (en) | 2023-08-23 |
| RU2019126455A3 (enExample) | 2021-05-17 |
| EP3571189B1 (en) | 2023-03-29 |
| US20200017517A1 (en) | 2020-01-16 |
| WO2018136264A1 (en) | 2018-07-26 |
| CA3051054A1 (en) | 2018-07-26 |
| KR20190110588A (ko) | 2019-09-30 |
| JP2023018094A (ja) | 2023-02-07 |
| CN110431134A (zh) | 2019-11-08 |
| US11673896B2 (en) | 2023-06-13 |
| US20240092795A1 (en) | 2024-03-21 |
| EP3571189A1 (en) | 2019-11-27 |
| SG11201906412SA (en) | 2019-08-27 |
| AU2018210196B2 (en) | 2022-06-02 |
| JP7240320B2 (ja) | 2023-03-15 |
| JP2020505376A (ja) | 2020-02-20 |
| WO2018136264A9 (en) | 2018-10-25 |
| BR112019014527A2 (pt) | 2020-02-27 |
| EP4230623A3 (en) | 2023-10-11 |
| MX2019008696A (es) | 2019-09-13 |
| IL268031A (en) | 2019-09-26 |
| IL268031B (en) | 2022-06-01 |
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