EA029758B1 - Макроциклические производные пиридина - Google Patents
Макроциклические производные пиридина Download PDFInfo
- Publication number
- EA029758B1 EA029758B1 EA201692000A EA201692000A EA029758B1 EA 029758 B1 EA029758 B1 EA 029758B1 EA 201692000 A EA201692000 A EA 201692000A EA 201692000 A EA201692000 A EA 201692000A EA 029758 B1 EA029758 B1 EA 029758B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkyl
- hydrogen
- prom
- comm
- alkanediyl
- Prior art date
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- 150000003222 pyridines Chemical class 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 452
- 239000003814 drug Substances 0.000 claims abstract description 25
- 230000002401 inhibitory effect Effects 0.000 claims abstract description 23
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 23
- 239000004480 active ingredient Substances 0.000 claims abstract description 12
- 125000000217 alkyl group Chemical group 0.000 claims description 549
- -1 2,5-diazabicyclo [2.2.2] octanyl Chemical group 0.000 claims description 168
- 229910052739 hydrogen Inorganic materials 0.000 claims description 153
- 239000001257 hydrogen Substances 0.000 claims description 150
- 125000001424 substituent group Chemical group 0.000 claims description 104
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 99
- 229910052736 halogen Inorganic materials 0.000 claims description 79
- 150000002367 halogens Chemical class 0.000 claims description 79
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 76
- 150000002431 hydrogen Chemical class 0.000 claims description 66
- 229910052799 carbon Inorganic materials 0.000 claims description 61
- 125000003545 alkoxy group Chemical group 0.000 claims description 49
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 43
- 125000003342 alkenyl group Chemical group 0.000 claims description 39
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 35
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 30
- 125000004043 oxo group Chemical group O=* 0.000 claims description 24
- 125000004432 carbon atom Chemical group C* 0.000 claims description 23
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 23
- 125000000304 alkynyl group Chemical group 0.000 claims description 21
- 125000004122 cyclic group Chemical group 0.000 claims description 19
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 17
- 125000004076 pyridyl group Chemical group 0.000 claims description 9
- 239000003937 drug carrier Substances 0.000 claims description 6
- 229940079593 drug Drugs 0.000 claims description 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- 238000000034 method Methods 0.000 abstract description 54
- 150000003230 pyrimidines Chemical class 0.000 abstract description 3
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 abstract description 2
- 101000605630 Homo sapiens Phosphatidylinositol 3-kinase catalytic subunit type 3 Proteins 0.000 abstract 1
- 102100038329 Phosphatidylinositol 3-kinase catalytic subunit type 3 Human genes 0.000 abstract 1
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- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 10
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Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero rings
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D491/22—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 four 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
- C07D498/22—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 four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/582—Recycling of unreacted starting or intermediate materials
Landscapes
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- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
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- Veterinary Medicine (AREA)
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- Psychiatry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (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 (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14163442 | 2014-04-03 | ||
| EP14183823 | 2014-09-05 | ||
| PCT/EP2015/057401 WO2015150557A1 (en) | 2014-04-03 | 2015-04-02 | Macrocylic pyridine derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201692000A1 EA201692000A1 (ru) | 2017-01-30 |
| EA029758B1 true EA029758B1 (ru) | 2018-05-31 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201692000A EA029758B1 (ru) | 2014-04-03 | 2015-04-02 | Макроциклические производные пиридина |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US20170022201A1 (enExample) |
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| US10407442B2 (en) | 2015-09-24 | 2019-09-10 | Cyclenium Pharma Inc. | Libraries of heteroaryl-containing macrocyclic compounds and methods of making and using the same |
| AU2017219846B2 (en) | 2016-02-19 | 2021-05-13 | Sprint Bioscience Ab | 6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes |
| LT3416957T (lt) | 2016-02-19 | 2020-11-25 | Sprint Bioscience Ab | 6-heterociklil-4-morfolin-4-ilpiridin-2-ono junginiai, tinkami vėžio ir diabeto gydymui |
| IL316954A (en) | 2017-02-28 | 2025-01-01 | Morphic Therapeutic Inc | (Alpha-V)(beta-6)integrin inhibitors |
| EP3760202A1 (en) | 2017-02-28 | 2021-01-06 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| ES2900199T3 (es) | 2017-03-28 | 2022-03-16 | Bayer Ag | Novedosos compuestos macrocíclicos inhibidores de PTEFB |
| WO2018177889A1 (en) | 2017-03-28 | 2018-10-04 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| US20200190083A1 (en) * | 2017-06-22 | 2020-06-18 | Cyclenium Pharma Inc. | Libraries of pyridine-containing macrocyclic compounds and methods of making and using the same |
| CN116589461A (zh) | 2017-08-23 | 2023-08-15 | 思普瑞特生物科学公司 | 氮杂吲哚基吡啶酮化合物和二氮杂吲哚基吡啶酮化合物 |
| IL302293A (en) | 2017-08-23 | 2023-06-01 | Sprint Bioscience Ab | Pyridinamine-pyridone and pyrimidinamine-pyridone compounds |
| IL302077A (en) | 2017-08-23 | 2023-06-01 | Sprint Bioscience Ab | Morpholinylpyridone compounds |
| EP4056556A1 (en) | 2017-08-23 | 2022-09-14 | Sprint Bioscience AB | Pyridylpyridone compounds |
| WO2020047208A1 (en) | 2018-08-29 | 2020-03-05 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| UY38352A (es) | 2018-08-29 | 2020-03-31 | Morphic Therapeutic Inc | Inhibidores de integrina alfavbeta6 |
| UY38353A (es) | 2018-08-29 | 2020-03-31 | Morphic Therapeutic Inc | Inhibición de integrina alfavbeta6 |
| EP4013762A1 (en) * | 2019-08-16 | 2022-06-22 | Inflazome Limited | Macrocyclic sulfonylamide derivatives useful as nlrp3 inhibitors |
| CN113845521B (zh) * | 2021-08-31 | 2024-06-18 | 中原工学院 | 水相中光催化一锅法合成咪唑并含氮杂环肼类衍生物的方法 |
| CN115260128B (zh) * | 2022-09-21 | 2022-12-09 | 苏州凯瑞医药科技有限公司 | 一种新型jak抑制剂关键中间体的制备方法 |
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| MY169441A (en) | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
| JO3088B1 (ar) | 2004-12-08 | 2017-03-15 | Janssen Pharmaceutica Nv | مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف |
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| EP1951729B1 (en) * | 2005-11-16 | 2014-06-25 | Cell Therapeutics, Inc. | Oxygen linked pyrimidine derivatives |
| CA2687909C (en) | 2007-06-21 | 2015-09-15 | Janssen Pharmaceutica Nv | Indolin-2-ones and aza-indolin-2-ones |
| US8318731B2 (en) | 2007-07-27 | 2012-11-27 | Janssen Pharmaceutica Nv | Pyrrolopyrimidines |
| KR20110031318A (ko) | 2008-06-13 | 2011-03-25 | 노파르티스 아게 | Ｉａ 심부전 및 암 치료에 유용한 단백질 키나제 ｄ 억제제로서의 2,4'-비피리디닐 화합물 |
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| JP2017509685A (ja) | 2017-04-06 |
| SG11201608241UA (en) | 2016-10-28 |
| ES2665797T3 (es) | 2018-04-27 |
| BR112016022700B1 (pt) | 2022-01-11 |
| PE20161365A1 (es) | 2016-12-17 |
| JP6420362B2 (ja) | 2018-11-07 |
| MY185500A (en) | 2021-05-19 |
| PH12016501962A1 (en) | 2017-01-09 |
| EP3126365B1 (en) | 2018-01-10 |
| KR102390274B1 (ko) | 2022-04-22 |
| MX2016012994A (es) | 2016-12-07 |
| AU2015239100A1 (en) | 2016-09-29 |
| MX369799B (es) | 2019-11-21 |
| EA201692000A1 (ru) | 2017-01-30 |
| IL248001B (en) | 2018-11-29 |
| CA2942751A1 (en) | 2015-10-08 |
| US20170022201A1 (en) | 2017-01-26 |
| CA2942751C (en) | 2023-03-21 |
| BR112016022700A2 (enExample) | 2017-08-15 |
| MA39823A (fr) | 2018-01-09 |
| UA118120C2 (uk) | 2018-11-26 |
| CN106132964B (zh) | 2019-07-19 |
| ZA201606768B (en) | 2018-11-28 |
| NZ725406A (en) | 2022-08-26 |
| AU2015239100B2 (en) | 2019-06-27 |
| KR20160140739A (ko) | 2016-12-07 |
| EP3126365A1 (en) | 2017-02-08 |
| PH12016501962B1 (en) | 2017-01-09 |
| KR102390274B9 (ko) | 2023-03-03 |
| WO2015150557A1 (en) | 2015-10-08 |
| CL2016002495A1 (es) | 2017-02-24 |
| CN106132964A (zh) | 2016-11-16 |
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