CN111542520A - 作为a2a受体抑制剂的并环类衍生物 - Google Patents
作为a2a受体抑制剂的并环类衍生物 Download PDFInfo
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- CN111542520A CN111542520A CN201880062761.6A CN201880062761A CN111542520A CN 111542520 A CN111542520 A CN 111542520A CN 201880062761 A CN201880062761 A CN 201880062761A CN 111542520 A CN111542520 A CN 111542520A
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- -1 1, 2, 3, 4-tetrahydroquinolyl Chemical group 0.000 claims description 96
- 125000005842 heteroatom Chemical group 0.000 claims description 35
- 125000000217 alkyl group Chemical group 0.000 claims description 19
- 125000003118 aryl group Chemical group 0.000 claims description 17
- 229910052717 sulfur Inorganic materials 0.000 claims description 16
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- 229910052801 chlorine Inorganic materials 0.000 claims description 12
- 229910052740 iodine Inorganic materials 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 7
- 125000004076 pyridyl group Chemical group 0.000 claims description 7
- 125000005493 quinolyl group Chemical group 0.000 claims description 7
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- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 4
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- 125000000623 heterocyclic group Chemical group 0.000 description 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 11
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- PCLIMKBDDGJMGD-UHFFFAOYSA-N N-bromosuccinimide Chemical compound BrN1C(=O)CCC1=O PCLIMKBDDGJMGD-UHFFFAOYSA-N 0.000 description 10
- 125000004432 carbon atom Chemical group C* 0.000 description 10
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- BEOOHQFXGBMRKU-UHFFFAOYSA-N sodium cyanoborohydride Chemical compound [Na+].[B-]C#N BEOOHQFXGBMRKU-UHFFFAOYSA-N 0.000 description 1
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- RMBAVIFYHOYIFM-UHFFFAOYSA-M sodium methanethiolate Chemical compound [Na+].[S-]C RMBAVIFYHOYIFM-UHFFFAOYSA-M 0.000 description 1
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- AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 description 1
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- ISIJQEHRDSCQIU-UHFFFAOYSA-N tert-butyl 2,7-diazaspiro[4.5]decane-7-carboxylate Chemical compound C1N(C(=O)OC(C)(C)C)CCCC11CNCC1 ISIJQEHRDSCQIU-UHFFFAOYSA-N 0.000 description 1
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- WMXCDAVJEZZYLT-UHFFFAOYSA-N tert-butylthiol Chemical compound CC(C)(C)S WMXCDAVJEZZYLT-UHFFFAOYSA-N 0.000 description 1
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- WLPUWLXVBWGYMZ-UHFFFAOYSA-N tricyclohexylphosphine Chemical compound C1CCCCC1P(C1CCCCC1)C1CCCCC1 WLPUWLXVBWGYMZ-UHFFFAOYSA-N 0.000 description 1
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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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
- A61K31/435—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
- A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- 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
- C07D417/02—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 two hetero rings
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- 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
- C07D417/02—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 two hetero rings
- C07D417/10—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 two hetero rings linked by a carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- 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
- C07D471/02—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 system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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
- C07D513/02—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 two hetero rings
- C07D513/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
公开了式(Ⅰ)所示化合物或其药学上可接受的盐,并涉及其在制备治疗与A2A受体相关疾病药物中的应用。
Description
PCT国内申请,说明书已公开。
Claims (17)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201710900542 | 2017-09-28 | ||
CN2017109005428 | 2017-09-28 | ||
CN2018102398242 | 2018-03-21 | ||
CN201810239824 | 2018-03-21 | ||
PCT/CN2018/107899 WO2019062803A1 (zh) | 2017-09-28 | 2018-09-27 | 作为a2a受体抑制剂的并环类衍生物 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN111542520A true CN111542520A (zh) | 2020-08-14 |
CN111542520B CN111542520B (zh) | 2022-04-15 |
Family
ID=65900821
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201880062761.6A Active CN111542520B (zh) | 2017-09-28 | 2018-09-27 | 作为a2a受体抑制剂的并环类衍生物 |
Country Status (16)
Country | Link |
---|---|
US (1) | US11312715B2 (zh) |
EP (1) | EP3686199B9 (zh) |
JP (1) | JP6836693B2 (zh) |
KR (1) | KR102254660B1 (zh) |
CN (1) | CN111542520B (zh) |
AU (1) | AU2018341781B2 (zh) |
BR (1) | BR112020006185A2 (zh) |
CA (1) | CA3077267C (zh) |
ES (1) | ES2927086T3 (zh) |
IL (1) | IL273606B (zh) |
MX (1) | MX2020003732A (zh) |
RU (1) | RU2748993C1 (zh) |
SA (1) | SA520411635B1 (zh) |
SG (1) | SG11202002886PA (zh) |
TW (1) | TWI788424B (zh) |
WO (1) | WO2019062803A1 (zh) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN111377873A (zh) * | 2018-12-28 | 2020-07-07 | 四川科伦博泰生物医药股份有限公司 | 氨基嘧啶化合物及其制备方法和用途 |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN110655509B (zh) * | 2018-06-29 | 2023-01-24 | 江苏恒瑞医药股份有限公司 | 2-胺基嘧啶类衍生物、其制备方法及其在医药上的应用 |
CN111094254B (zh) * | 2018-07-12 | 2022-07-26 | 江苏恒瑞医药股份有限公司 | 杂芳基类衍生物、其制备方法及其在医药上的应用 |
WO2020192762A1 (zh) * | 2019-03-28 | 2020-10-01 | 基石药业(苏州)有限公司 | 一种a2a受体拮抗剂的盐型、晶型及其制备方法 |
WO2022017434A1 (zh) * | 2020-07-23 | 2022-01-27 | 上海赛岚生物科技有限公司 | 一类具有激酶抑制活性的化合物 |
CN116514803A (zh) * | 2022-01-21 | 2023-08-01 | 上海赛岚生物科技有限公司 | 一种激酶抑制剂的盐晶型和自由碱晶型 |
Citations (3)
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CN1437471A (zh) * | 2000-06-21 | 2003-08-20 | 弗·哈夫曼-拉罗切有限公司 | 苯并噻唑衍生物 |
WO2015020565A1 (ru) * | 2013-08-05 | 2015-02-12 | Общество С Ограниченной Ответственностью "Ньювак" (Ооо "Ньювак") | Замещенные [1,2,4]триазоло[4,3-a]пиридины, проявляющие свойства антогонистов аденозиновых а2а рецепторов, и их применение |
CN105025899A (zh) * | 2012-12-28 | 2015-11-04 | 默沙东公司 | 具有A2A拮抗剂性质的杂二环取代的-[1,2,4]三唑并[1,5-c]喹唑啉-5-胺化合物 |
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AU699623B2 (en) | 1995-04-21 | 1998-12-10 | Neurosearch A/S | Benzimidazole compounds and their use as modulators of the GABAA receptor complex |
EP0976753B1 (en) * | 1997-03-24 | 2004-01-02 | Kyowa Hakko Kogyo Co., Ltd. | [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES |
EP1308441B1 (en) * | 2000-08-11 | 2009-10-07 | Eisai R&D Management Co., Ltd. | 2-aminopyridine compounds and use thereof as drugs |
ES2425476T3 (es) | 2004-04-02 | 2013-10-15 | Prana Biotechnology Limited | Compuestos neurológicamente activos |
ES2241496B1 (es) | 2004-04-15 | 2006-12-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de piridina. |
ES2274712B1 (es) | 2005-10-06 | 2008-03-01 | Laboratorios Almirall S.A. | Nuevos derivados imidazopiridina. |
EP1903044A1 (en) | 2006-09-14 | 2008-03-26 | Novartis AG | Adenosine Derivatives as A2A Receptor Agonists |
HUE025704T2 (en) * | 2009-03-20 | 2016-04-28 | Sigma Tau Ind Farmaceuti | Oxidized triazolyl purine derivatives used as adenosine A2A receptor ligands and their use as medicaments |
DE102012019369A1 (de) | 2012-10-02 | 2014-04-03 | Merck Patent Gmbh | 7-Azaindolderivat |
WO2014101120A1 (en) * | 2012-12-28 | 2014-07-03 | Merck Sharp & Dohme Corp. | Heterobicyclo-substituted-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties |
JP6275410B2 (ja) | 2013-08-06 | 2018-02-07 | 大和ハウス工業株式会社 | 固定具 |
WO2015027431A1 (en) | 2013-08-29 | 2015-03-05 | Merck Sharp & Dohme Corp. | 2,2-difluorodioxolo a2a receptor antagonists |
AU2018244935A1 (en) * | 2017-03-30 | 2019-08-15 | F. Hoffmann-La Roche Ag | Naphthyridines as inhibitors of HPK1 |
-
2018
- 2018-09-27 US US16/650,967 patent/US11312715B2/en active Active
- 2018-09-27 KR KR1020207012498A patent/KR102254660B1/ko active IP Right Grant
- 2018-09-27 JP JP2020517949A patent/JP6836693B2/ja active Active
- 2018-09-27 EP EP18861150.3A patent/EP3686199B9/en active Active
- 2018-09-27 BR BR112020006185-9A patent/BR112020006185A2/pt unknown
- 2018-09-27 SG SG11202002886PA patent/SG11202002886PA/en unknown
- 2018-09-27 CN CN201880062761.6A patent/CN111542520B/zh active Active
- 2018-09-27 MX MX2020003732A patent/MX2020003732A/es unknown
- 2018-09-27 RU RU2020114314A patent/RU2748993C1/ru active
- 2018-09-27 CA CA3077267A patent/CA3077267C/en active Active
- 2018-09-27 WO PCT/CN2018/107899 patent/WO2019062803A1/zh unknown
- 2018-09-27 ES ES18861150T patent/ES2927086T3/es active Active
- 2018-09-27 AU AU2018341781A patent/AU2018341781B2/en active Active
- 2018-09-28 TW TW107134271A patent/TWI788424B/zh active
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2020
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CN111377873B (zh) * | 2018-12-28 | 2023-03-28 | 四川科伦博泰生物医药股份有限公司 | 氨基嘧啶化合物及其制备方法和用途 |
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TWI788424B (zh) | 2023-01-01 |
CN111542520B (zh) | 2022-04-15 |
JP2020535196A (ja) | 2020-12-03 |
CA3077267C (en) | 2021-02-16 |
TW201920171A (zh) | 2019-06-01 |
IL273606B (en) | 2021-05-31 |
EP3686199B1 (en) | 2022-08-03 |
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EP3686199A4 (en) | 2021-04-07 |
US20200239465A1 (en) | 2020-07-30 |
KR102254660B1 (ko) | 2021-05-24 |
RU2748993C1 (ru) | 2021-06-02 |
CA3077267A1 (en) | 2019-04-04 |
US11312715B2 (en) | 2022-04-26 |
WO2019062803A1 (zh) | 2019-04-04 |
JP6836693B2 (ja) | 2021-03-03 |
AU2018341781A1 (en) | 2020-04-30 |
IL273606A (en) | 2020-05-31 |
BR112020006185A2 (pt) | 2020-10-13 |
MX2020003732A (es) | 2021-06-29 |
SG11202002886PA (en) | 2020-04-29 |
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