RU2018136104A - СОЕДИНЕНИЯ, ГЕТЕРОБИЦИКЛО-ЗАМЕЩЕННЫЕ-[1,2,4]ТРИАЗОЛО[1,5- c]ХИНАЗОЛИН-5-АМИНА, ОБЛАДАЮЩИЕ СВОЙСТВАМИ A2А АНТАГОНИСТОВ - Google Patents
СОЕДИНЕНИЯ, ГЕТЕРОБИЦИКЛО-ЗАМЕЩЕННЫЕ-[1,2,4]ТРИАЗОЛО[1,5- c]ХИНАЗОЛИН-5-АМИНА, ОБЛАДАЮЩИЕ СВОЙСТВАМИ A2А АНТАГОНИСТОВ Download PDFInfo
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- RU2018136104A RU2018136104A RU2018136104A RU2018136104A RU2018136104A RU 2018136104 A RU2018136104 A RU 2018136104A RU 2018136104 A RU2018136104 A RU 2018136104A RU 2018136104 A RU2018136104 A RU 2018136104A RU 2018136104 A RU2018136104 A RU 2018136104A
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- Prior art keywords
- triazolo
- pharmaceutically acceptable
- acceptable salt
- amine
- ethyl
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- 150000001875 compounds Chemical class 0.000 title claims 17
- 239000005557 antagonist Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims 13
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- -1 2- (2-methyl-4H-pyrrolo [3,4-d] oxazole-5 (6H) -yl) propyl Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- KWHDQPVGKVPPPS-UHFFFAOYSA-N quinazolin-5-amine Chemical compound C1=NC=C2C(N)=CC=CC2=N1 KWHDQPVGKVPPPS-UHFFFAOYSA-N 0.000 claims 2
- FADASXSDYBZQQS-UHFFFAOYSA-N 2-[2-(2-cyclopropyl-4,6-dihydropyrrolo[3,4-d][1,3]oxazol-5-yl)ethyl]-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine Chemical compound N=1N2C(N)=NC=3C(OC)=CC=CC=3C2=NC=1CCN(CC=1O2)CC=1N=C2C1CC1 FADASXSDYBZQQS-UHFFFAOYSA-N 0.000 claims 1
- DOXTUZCGFXTMIQ-UHFFFAOYSA-N 2-[2-(2-cyclopropyl-4,6-dihydropyrrolo[3,4-d][1,3]thiazol-5-yl)ethyl]-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine Chemical compound N=1N2C(N)=NC=3C(OC)=CC=CC=3C2=NC=1CCN(CC=1S2)CC=1N=C2C1CC1 DOXTUZCGFXTMIQ-UHFFFAOYSA-N 0.000 claims 1
- PNHGGXHXLNUCPR-UHFFFAOYSA-N 2-[2-(2-ethyl-4,6-dihydropyrrolo[3,4-d][1,3]thiazol-5-yl)ethyl]-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine Chemical compound C12=CC=CC(OC)=C2N=C(N)N2C1=NC(CCN1CC=3N=C(SC=3C1)CC)=N2 PNHGGXHXLNUCPR-UHFFFAOYSA-N 0.000 claims 1
- DWMBNNGZDHHEAW-UHFFFAOYSA-N 7-methoxy-2-[2-(1-methyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl)ethyl]-[1,2,4]triazolo[1,5-c]quinazolin-5-amine Chemical compound C12=NC(CCN3CC=4N(C)N=CC=4C3)=NN2C(N)=NC2=C1C=CC=C2OC DWMBNNGZDHHEAW-UHFFFAOYSA-N 0.000 claims 1
- HLYUEBUGUJLIMG-UHFFFAOYSA-N 7-methoxy-2-[2-(2-methyl-4,6-dihydropyrrolo[3,4-d][1,3]oxazol-5-yl)ethyl]-[1,2,4]triazolo[1,5-c]quinazolin-5-amine Chemical compound C12=NC(CCN3CC=4OC(C)=NC=4C3)=NN2C(N)=NC2=C1C=CC=C2OC HLYUEBUGUJLIMG-UHFFFAOYSA-N 0.000 claims 1
- XBUZINXHGBWRAB-UHFFFAOYSA-N 7-methoxy-2-[2-(2-propan-2-yl-4,6-dihydropyrrolo[3,4-d][1,3]thiazol-5-yl)ethyl]-[1,2,4]triazolo[1,5-c]quinazolin-5-amine Chemical compound C12=NC(CCN3CC=4SC(=NC=4C3)C(C)C)=NN2C(N)=NC2=C1C=CC=C2OC XBUZINXHGBWRAB-UHFFFAOYSA-N 0.000 claims 1
Classifications
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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
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed 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
- C07D498/04—Ortho-condensed systems
-
- 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
- C07D513/02—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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- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Hydrogenated Pyridines (AREA)
Claims (44)
1. Соединение или его фармацевтически приемлемая соль, имеющая структуру
Где
каждый RGda независимо представляет собой: (а) Н; (b) метил или (с) этил;
RGe представляет собой:
2. Соединение по п.1, представляющее собой:
2-(2-(2-циклопропил-4H-пирроло[3,4-d]тиазол-5(6H)-ил)этил)-7-метокси-[1,2,4]триазоло[1,5-c]хиназолин-5-амин;
2-(2-(2-изопропил-4H-пирроло[3,4-d]тиазол-5(6H)-ил)этил)-7-метокси-[1,2,4]триазоло[1,5-c]хиназолин-5-амин;
2-(2-(2-этил-4H-пирроло[3,4-d]тиазол-5(6H)-ил)этил)-7-метокси-[1,2,4]триазоло[1,5-c]хиназолин-5-амин;
7-метокси-2-(2-(2-метил-4H-пирроло[3,4-d]оксазол-5(6H)-ил)этил)-[1,2,4]триазоло[1,5-c]хиназолин-5-амин;
2-(2-(2-циклопропил-4H-пирроло[3,4-d]оксазол-5(6H)-ил)этил)-7-метокси-[1,2,4]триазоло[1,5-c]хиназолин-5-амин;
7-метокси-2-(2-(1-метилпирроло[3,4-c]pyrazol-5(1H,4H,6H)-ил)этил)-[1,2,4]триазоло[1,5-c]хиназолин-5-амин;
(R)-7-метокси-2-(2-(2-метил-4H-пирроло[3,4-d]оксазол-5(6H)-ил)пропил)-[1,2,4]триазоло[1,5-c]хиназолин-5-амин;
(R)-7-метокси-2-(2-(2-метил-4H-пирроло[3,4-d]оксазол-5(6H)-ил)бутил)-[1,2,4]триазоло[1,5-c]хиназолин-5-амин,
или его фармацевтически приемлемую соль.
3. Соединение или его фармацевтически приемлемая соль, представляющая собой соединение структуры:
где:
каждый RGda независимо представляет собой: (а) Н; (b) метил или (с) этил; и
RGe представляет собой:
4. Фармацевтическая композиция, содержащая инертный носитель и соединение по п.3, или его фармацевтически приемлемую соль.
5. Соединение формулы:
или его фармацевтически приемлемая соль.
6. Соединение по п.5, представляющее собой:
7. Соединение по п.5 в форме фармацевтически приемлемой соли.
8. Фармацевтическая композиция, содержащая инертный носитель и соединение по п.5 или его фармацевтически приемлемую соль.
9. Соединение формулы
или его фармацевтически приемлемая соль.
10. Соединение по п.9, представляющее собой
11. Соединение по п.9 в форме фармацевтически приемлемой соли.
12. Фармацевтическая композиция, содержащая инертный носитель и соединение по п.9 или его фармацевтически приемлемую соль.
13. Соединение формулы:
или его фармацевтически приемлемая соль.
14. Соединение по п.13 в форме фармацевтически приемлемой соли.
15. Фармацевтическая композиция, содержащая инертный носитель и соединение по п.13 или его фармацевтически приемлемую соль.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2012/087865 | 2012-12-28 | ||
| PCT/CN2012/087865 WO2014101120A1 (en) | 2012-12-28 | 2012-12-28 | Heterobicyclo-substituted-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties |
| CNPCT/CN2013/076853 | 2013-06-06 | ||
| PCT/CN2013/076853 WO2014101373A1 (en) | 2012-12-28 | 2013-06-06 | Heterobicyclo-substituted-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds for treatment of central nervous system disorder |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2015131148A Division RU2671628C2 (ru) | 2012-12-28 | 2013-12-20 | СОЕДИНЕНИЯ, ГЕТЕРОБИЦИКЛО-ЗАМЕЩЕННЫЕ-[1,2,4]ТРИАЗОЛО[1,5c]ХИНАЗОЛИН-5-АМИНА, ОБЛАДАЮЩИЕ СВОЙСТВАМИ А2А АНТАГОНИСТОВ |
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| Publication Number | Publication Date |
|---|---|
| RU2018136104A true RU2018136104A (ru) | 2018-11-21 |
| RU2018136104A3 RU2018136104A3 (ru) | 2022-04-05 |
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| RU2018136104A RU2018136104A (ru) | 2012-12-28 | 2013-12-20 | СОЕДИНЕНИЯ, ГЕТЕРОБИЦИКЛО-ЗАМЕЩЕННЫЕ-[1,2,4]ТРИАЗОЛО[1,5- c]ХИНАЗОЛИН-5-АМИНА, ОБЛАДАЮЩИЕ СВОЙСТВАМИ A2А АНТАГОНИСТОВ |
| RU2015131148A RU2671628C2 (ru) | 2012-12-28 | 2013-12-20 | СОЕДИНЕНИЯ, ГЕТЕРОБИЦИКЛО-ЗАМЕЩЕННЫЕ-[1,2,4]ТРИАЗОЛО[1,5c]ХИНАЗОЛИН-5-АМИНА, ОБЛАДАЮЩИЕ СВОЙСТВАМИ А2А АНТАГОНИСТОВ |
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| RU2015131148A RU2671628C2 (ru) | 2012-12-28 | 2013-12-20 | СОЕДИНЕНИЯ, ГЕТЕРОБИЦИКЛО-ЗАМЕЩЕННЫЕ-[1,2,4]ТРИАЗОЛО[1,5c]ХИНАЗОЛИН-5-АМИНА, ОБЛАДАЮЩИЕ СВОЙСТВАМИ А2А АНТАГОНИСТОВ |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US9708347B2 (ru) |
| EP (1) | EP2945632B1 (ru) |
| JP (1) | JP6306049B2 (ru) |
| KR (1) | KR102165113B1 (ru) |
| AU (1) | AU2013370977B2 (ru) |
| BR (1) | BR112015015468B8 (ru) |
| CA (1) | CA2896056C (ru) |
| CY (1) | CY1120258T1 (ru) |
| DK (1) | DK2945632T3 (ru) |
| ES (1) | ES2667477T3 (ru) |
| HR (1) | HRP20180678T1 (ru) |
| HU (1) | HUE037950T2 (ru) |
| LT (1) | LT2945632T (ru) |
| ME (1) | ME03034B (ru) |
| MX (1) | MX370017B (ru) |
| NO (1) | NO2945632T3 (ru) |
| PL (1) | PL2945632T3 (ru) |
| PT (1) | PT2945632T (ru) |
| RS (1) | RS57162B1 (ru) |
| RU (2) | RU2018136104A (ru) |
| SI (1) | SI2945632T1 (ru) |
| WO (3) | WO2014101120A1 (ru) |
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| EP3307067B1 (en) * | 2015-06-11 | 2022-11-02 | Merck Sharp & Dohme LLC | Aminopyrazine compounds with a2a antagonist properties |
| WO2017008205A1 (en) | 2015-07-10 | 2017-01-19 | Merck Sharp & Dohme Corp. | Substituted aminoquinazoline compounds as a2a antagonist |
| US10568882B2 (en) | 2015-08-21 | 2020-02-25 | Srx Cardio, Llc | Phenylpiperazine proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators and their use |
| HK1260897A1 (zh) * | 2015-08-21 | 2019-12-27 | Portola Pharmaceuticals, Inc. | 使用四氢异喹啉小分子来结合并调节pcsk9的蛋白活性的组合物和方法 |
| US10821106B2 (en) | 2015-08-21 | 2020-11-03 | Srx Cardio, Llc | Composition and methods of use of novel phenylalanine small organic compounds to directly modulate PCSK9 protein activity |
| US10329289B2 (en) | 2015-12-23 | 2019-06-25 | Merck Sharp & Dohme Corp. | 6,7-dihydro-5H-pyrrolo[3,4-B]pyridin-5-one allosteric modulators of the M4 muscarinic acetylcholine receptor |
| WO2017107087A1 (en) * | 2015-12-23 | 2017-06-29 | Merck Sharp & Dohme Corp. | 6, 7-dihydro-5h-pyrrolo [3, 4-b] pyridin-5-oneallosteric modulators of the m4 muscarinic acetylcholine receptor |
| WO2017107089A1 (en) | 2015-12-23 | 2017-06-29 | Merck Sharp & Dohme Corp. | 3- (1h-pyrazol-4-yl) pyridineallosteric modulators of the m4 muscarinic acetylcholine receptor |
| WO2017147328A1 (en) | 2016-02-23 | 2017-08-31 | Portola Pharmaceuticals, Inc. | Compounds for binding proprotein convertase subtilisin/kexin type 9 (pcsk9) |
| WO2018112842A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | 6,6-fused heteroaryl piperidine ether allosteric modulators of m4 muscarinic acetylcholine receptor |
| WO2018112843A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor |
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