EA201791021A1 - 1-[2-(АМИНОМЕТИЛ)БЕНЗИЛ]-2-ТИОКСО-1,2,3,5-ТЕТРАГИДРО-4H-ПИРРОЛО[3,2-d]ПИРИМИДИН-4-ОНЫ КАК ИНГИБИТОРЫ МИЕЛОПЕРОКСИДАЗЫ - Google Patents
1-[2-(АМИНОМЕТИЛ)БЕНЗИЛ]-2-ТИОКСО-1,2,3,5-ТЕТРАГИДРО-4H-ПИРРОЛО[3,2-d]ПИРИМИДИН-4-ОНЫ КАК ИНГИБИТОРЫ МИЕЛОПЕРОКСИДАЗЫInfo
- Publication number
- EA201791021A1 EA201791021A1 EA201791021A EA201791021A EA201791021A1 EA 201791021 A1 EA201791021 A1 EA 201791021A1 EA 201791021 A EA201791021 A EA 201791021A EA 201791021 A EA201791021 A EA 201791021A EA 201791021 A1 EA201791021 A1 EA 201791021A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- thioxo
- pyrrolo
- pyrimidin
- aminomethyl
- tetrahydro
- Prior art date
Links
Classifications
-
- 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
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
В данном документе раскрываются некоторые 1-[2-(аминометил)бензил]-2-тиоксо-1,2,3,5-тетрагидро-4H-пирроло[3,2-d]пиримидин-4-оновые соединения формулы (I), a также их фармацевтически приемлемые соли вместе с композициями, содержащими их, и их применение в терапии. Соединения представляют собой ингибиторы фермента МРО и таким образом особенно пригодны для лечения или профилактики сердечно-сосудистых нарушений, таких как состояния, связанные с сердечной недостаточностью и ишемической болезнью сердца.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462085722P | 2014-12-01 | 2014-12-01 | |
| US201562166808P | 2015-05-27 | 2015-05-27 | |
| PCT/EP2015/077998 WO2016087338A1 (en) | 2014-12-01 | 2015-11-30 | 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4h-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201791021A1 true EA201791021A1 (ru) | 2017-11-30 |
| EA030805B1 EA030805B1 (ru) | 2018-09-28 |
Family
ID=54754631
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201791021A EA030805B1 (ru) | 2014-12-01 | 2015-11-30 | 1-[2-(АМИНОМЕТИЛ)БЕНЗИЛ]-2-ТИОКСО-1,2,3,5-ТЕТРАГИДРО-4H-ПИРРОЛО[3,2-d]ПИРИМИДИН-4-ОНЫ КАК ИНГИБИТОРЫ МИЕЛОПЕРОКСИДАЗЫ |
Country Status (38)
| Country | Link |
|---|---|
| US (5) | US9616063B2 (ru) |
| EP (1) | EP3227294B1 (ru) |
| JP (1) | JP6616417B2 (ru) |
| KR (1) | KR102543404B1 (ru) |
| CN (1) | CN107001374B (ru) |
| AU (1) | AU2015357290B2 (ru) |
| BR (1) | BR112017011124B1 (ru) |
| CA (1) | CA2968449C (ru) |
| CL (1) | CL2017001380A1 (ru) |
| CO (1) | CO2017006658A2 (ru) |
| CY (1) | CY1122587T1 (ru) |
| DK (1) | DK3227294T3 (ru) |
| DO (1) | DOP2017000129A (ru) |
| EA (1) | EA030805B1 (ru) |
| ES (1) | ES2751690T3 (ru) |
| GT (1) | GT201700114A (ru) |
| HK (1) | HK1245270A1 (ru) |
| HR (1) | HRP20191744T1 (ru) |
| HU (1) | HUE045606T2 (ru) |
| IL (1) | IL252436B (ru) |
| LT (1) | LT3227294T (ru) |
| ME (1) | ME03568B (ru) |
| MX (1) | MX370492B (ru) |
| MY (1) | MY195816A (ru) |
| NI (1) | NI201700065A (ru) |
| NZ (1) | NZ732164A (ru) |
| PE (1) | PE20170914A1 (ru) |
| PH (1) | PH12017500977A1 (ru) |
| PL (1) | PL3227294T3 (ru) |
| PT (1) | PT3227294T (ru) |
| RS (1) | RS59375B1 (ru) |
| SG (1) | SG11201703961UA (ru) |
| SI (1) | SI3227294T1 (ru) |
| SV (1) | SV2017005451A (ru) |
| TN (1) | TN2017000208A1 (ru) |
| TW (1) | TWI681963B (ru) |
| UY (1) | UY36416A (ru) |
| WO (1) | WO2016087338A1 (ru) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9616063B2 (en) | 2014-12-01 | 2017-04-11 | Astrazeneca Ab | 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase |
| BR112019026270A2 (pt) * | 2017-07-17 | 2020-06-30 | Astrazeneca Ab | inibidores de mpo para uso em medicina |
| CN112151111B (zh) * | 2020-08-27 | 2022-10-11 | 上海大学 | 基于多元线性回归快速预测黄嘌呤衍生物抑制活性的qsar方法 |
| CN115403584B (zh) * | 2021-05-26 | 2024-04-02 | 长春金赛药业有限责任公司 | 2-硫代-2,3-二氢嘧啶-4-酮衍生物、药物组合物及其制备方法和应用 |
| WO2024038131A1 (en) | 2022-08-18 | 2024-02-22 | Astrazeneca Ab | Inhibitors of myeloperoxidase |
| US20240092787A1 (en) | 2022-08-24 | 2024-03-21 | Astrazeneca Ab | Pharmaceutical process and intermediates |
| WO2024047094A1 (en) | 2022-08-31 | 2024-03-07 | Astrazeneca Ab | Pharmaceutical formulation |
| WO2024120457A1 (zh) * | 2022-12-09 | 2024-06-13 | 深圳信立泰药业股份有限公司 | 一种吡咯并[3,2-d]嘧啶-4-酮类衍生物及其制备方法和医药用途 |
| WO2024209075A1 (en) * | 2023-04-06 | 2024-10-10 | Astrazeneca Ab | Method of treatment with mpo inhibitors |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR039385A1 (es) | 2002-04-19 | 2005-02-16 | Astrazeneca Ab | Derivados de tioxantina como inhibidores de la mieloperoxidasa |
| US20050130983A1 (en) * | 2002-05-02 | 2005-06-16 | Dae-Kee Kim | Pyrrolopyrimidinone derivatives, process for preparation thereof, and method of using and composition comprising them |
| SE0302756D0 (sv) | 2003-10-17 | 2003-10-17 | Astrazeneca Ab | Novel Compounds |
| GB0401269D0 (en) * | 2004-01-21 | 2004-02-25 | Astrazeneca Ab | Compounds |
| MY140748A (en) | 2004-12-06 | 2010-01-15 | Astrazeneca Ab | Novel pyrrolo [3,2-d] pyrimidin-4-one derivatives and their use in therapy |
| WO2006064196A1 (en) * | 2004-12-14 | 2006-06-22 | Astrazeneca Ab | Pyrazolopyrimidine compounds as antitumor agents |
| TW200806667A (en) | 2006-04-13 | 2008-02-01 | Astrazeneca Ab | New compounds |
| JP2009533426A (ja) | 2006-04-13 | 2009-09-17 | アストラゼネカ・アクチエボラーグ | チオキサンチン誘導体およびそれらのｍｐｏ阻害剤としての用途 |
| TW200804383A (en) | 2006-06-05 | 2008-01-16 | Astrazeneca Ab | New compounds |
| JP2009539829A (ja) | 2006-06-05 | 2009-11-19 | アストラゼネカ・アクチエボラーグ | ミエロペルオキシダーゼ阻害剤としてのピロロ［３，２−ｄ］ピリミジン−４−オン誘導体 |
| US20090054468A1 (en) * | 2007-08-23 | 2009-02-26 | Astrazeneca Ab | New Use 938 |
| WO2012106343A2 (en) | 2011-02-01 | 2012-08-09 | The Board Of Trustees Of The University Of Illinois | Hdac inhibitors and therapeutic methods using the same |
| AU2012335220B2 (en) | 2011-11-11 | 2017-06-01 | Pfizer Inc. | 2-thiopyrimidinones |
| US9616063B2 (en) * | 2014-12-01 | 2017-04-11 | Astrazeneca Ab | 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase |
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2015
- 2015-11-25 US US14/951,979 patent/US9616063B2/en active Active
- 2015-11-30 WO PCT/EP2015/077998 patent/WO2016087338A1/en active Application Filing
- 2015-11-30 AU AU2015357290A patent/AU2015357290B2/en active Active
- 2015-11-30 HU HUE15802075A patent/HUE045606T2/hu unknown
- 2015-11-30 EA EA201791021A patent/EA030805B1/ru not_active IP Right Cessation
- 2015-11-30 MY MYPI2017701958A patent/MY195816A/en unknown
- 2015-11-30 SG SG11201703961UA patent/SG11201703961UA/en unknown
- 2015-11-30 LT LT15802075T patent/LT3227294T/lt unknown
- 2015-11-30 EP EP15802075.0A patent/EP3227294B1/en active Active
- 2015-11-30 RS RSP20191310 patent/RS59375B1/sr unknown
- 2015-11-30 PT PT158020750T patent/PT3227294T/pt unknown
- 2015-11-30 UY UY0001036416A patent/UY36416A/es not_active Application Discontinuation
- 2015-11-30 PE PE2017000940A patent/PE20170914A1/es unknown
- 2015-11-30 BR BR112017011124-1A patent/BR112017011124B1/pt active IP Right Grant
- 2015-11-30 TW TW104139983A patent/TWI681963B/zh active
- 2015-11-30 ES ES15802075T patent/ES2751690T3/es active Active
- 2015-11-30 KR KR1020177016607A patent/KR102543404B1/ko active IP Right Grant
- 2015-11-30 PL PL15802075T patent/PL3227294T3/pl unknown
- 2015-11-30 DK DK15802075.0T patent/DK3227294T3/da active
- 2015-11-30 NZ NZ732164A patent/NZ732164A/en unknown
- 2015-11-30 TN TN2017000208A patent/TN2017000208A1/en unknown
- 2015-11-30 JP JP2017528830A patent/JP6616417B2/ja active Active
- 2015-11-30 MX MX2017007322A patent/MX370492B/es active IP Right Grant
- 2015-11-30 CN CN201580065064.2A patent/CN107001374B/zh active Active
- 2015-11-30 CA CA2968449A patent/CA2968449C/en active Active
- 2015-11-30 ME MEP-2019-286A patent/ME03568B/me unknown
- 2015-11-30 SI SI201530918T patent/SI3227294T1/sl unknown
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2017
- 2017-03-09 US US15/454,318 patent/US10016430B2/en active Active
- 2017-05-22 IL IL252436A patent/IL252436B/en active IP Right Grant
- 2017-05-26 PH PH12017500977A patent/PH12017500977A1/en unknown
- 2017-05-30 CL CL2017001380A patent/CL2017001380A1/es unknown
- 2017-05-30 DO DO2017000129A patent/DOP2017000129A/es unknown
- 2017-05-31 SV SV2017005451A patent/SV2017005451A/es unknown
- 2017-06-01 GT GT201700114A patent/GT201700114A/es unknown
- 2017-06-01 NI NI201700065A patent/NI201700065A/es unknown
- 2017-06-30 CO CONC2017/0006658A patent/CO2017006658A2/es unknown
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2018
- 2018-04-12 HK HK18104749.6A patent/HK1245270A1/zh unknown
- 2018-06-15 US US16/009,590 patent/US11000525B2/en active Active
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2019
- 2019-09-26 HR HRP20191744TT patent/HRP20191744T1/hr unknown
- 2019-10-15 CY CY20191101079T patent/CY1122587T1/el unknown
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2021
- 2021-04-12 US US17/228,492 patent/US11975004B2/en active Active
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2024
- 2024-04-05 US US18/628,297 patent/US20240335446A1/en active Pending
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ KG TJ TM |