DOP2017000129A - 1-[2-(aminometil)bencil]-2-tioxo-1,2,3,5-tetrahidro-4h-pirrolo[3,2-d]pirimidin-4-onas como inhibidores de mieloperoxidasa - Google Patents

1-[2-(aminometil)bencil]-2-tioxo-1,2,3,5-tetrahidro-4h-pirrolo[3,2-d]pirimidin-4-onas como inhibidores de mieloperoxidasa

Info

Publication number
DOP2017000129A
DOP2017000129A DO2017000129A DO2017000129A DOP2017000129A DO P2017000129 A DOP2017000129 A DO P2017000129A DO 2017000129 A DO2017000129 A DO 2017000129A DO 2017000129 A DO2017000129 A DO 2017000129A DO P2017000129 A DOP2017000129 A DO P2017000129A
Authority
DO
Dominican Republic
Prior art keywords
thioxo
pyrimidin
tetrahydro
aminometil
bencil
Prior art date
Application number
DO2017000129A
Other languages
English (en)
Inventor
Bertil Inghardt Tord
Tomkinson Nicholas
Gan Li-Ming
Paul Stonehouse Jeffrey
Johannesson Petra
Jurva Ulrik
Michaëlsson Erik
Lindstedt-Alstermark Eva-Lotte
Original Assignee
Astrazeneca Ab
Astrazeneca Uk Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Astrazeneca Ab, Astrazeneca Uk Ltd filed Critical Astrazeneca Ab
Publication of DOP2017000129A publication Critical patent/DOP2017000129A/es

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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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Se dan a conocer determinados compuestos de 1-[2-(aminometil)bencil]-2-tioxo-1,2,3,5-tetrahidro-4H-pirrolo[3,2-d]pirimidin-4-ona de fórmula (I), y sales farmacéuticamente aceptable de los mismos, junto con composiciones que los contienen y su uso en terapia. Los compuestos son inhibidores de la enzima MPO y de este modo son particularmente útiles en el tratamiento o profilaxis de trastornos cardiovasculares tales como insuficiencia cardíaca y estados relacionados con arteriopatía coronaria.
DO2017000129A 2014-12-01 2017-05-30 1-[2-(aminometil)bencil]-2-tioxo-1,2,3,5-tetrahidro-4h-pirrolo[3,2-d]pirimidin-4-onas como inhibidores de mieloperoxidasa DOP2017000129A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462085722P 2014-12-01 2014-12-01
US201562166808P 2015-05-27 2015-05-27

Publications (1)

Publication Number Publication Date
DOP2017000129A true DOP2017000129A (es) 2017-09-15

Family

ID=54754631

Family Applications (1)

Application Number Title Priority Date Filing Date
DO2017000129A DOP2017000129A (es) 2014-12-01 2017-05-30 1-[2-(aminometil)bencil]-2-tioxo-1,2,3,5-tetrahidro-4h-pirrolo[3,2-d]pirimidin-4-onas como inhibidores de mieloperoxidasa

Country Status (38)

Country Link
US (5) US9616063B2 (es)
EP (1) EP3227294B1 (es)
JP (1) JP6616417B2 (es)
KR (1) KR102543404B1 (es)
CN (1) CN107001374B (es)
AU (1) AU2015357290B2 (es)
BR (1) BR112017011124B1 (es)
CA (1) CA2968449C (es)
CL (1) CL2017001380A1 (es)
CO (1) CO2017006658A2 (es)
CY (1) CY1122587T1 (es)
DK (1) DK3227294T3 (es)
DO (1) DOP2017000129A (es)
EA (1) EA030805B1 (es)
ES (1) ES2751690T3 (es)
GT (1) GT201700114A (es)
HR (1) HRP20191744T1 (es)
HU (1) HUE045606T2 (es)
IL (1) IL252436B (es)
LT (1) LT3227294T (es)
ME (1) ME03568B (es)
MX (1) MX370492B (es)
MY (1) MY195816A (es)
NI (1) NI201700065A (es)
NZ (1) NZ732164A (es)
PE (1) PE20170914A1 (es)
PH (1) PH12017500977A1 (es)
PL (1) PL3227294T3 (es)
PT (1) PT3227294T (es)
RS (1) RS59375B1 (es)
SG (1) SG11201703961UA (es)
SI (1) SI3227294T1 (es)
SM (1) SMT201900572T1 (es)
SV (1) SV2017005451A (es)
TN (1) TN2017000208A1 (es)
TW (1) TWI681963B (es)
UY (1) UY36416A (es)
WO (1) WO2016087338A1 (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
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
SG11202000086PA (en) * 2017-07-17 2020-02-27 Astrazeneca Ab Mpo inhibitors for use in medicine
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
TW202426450A (zh) 2022-08-18 2024-07-01 瑞典商阿斯特捷利康公司 髓過氧化物酶抑制劑
US20240092787A1 (en) 2022-08-24 2024-03-21 Astrazeneca Ab Pharmaceutical process and intermediates
CN119789849A (zh) 2022-08-31 2025-04-08 阿斯利康(瑞典)有限公司 药物制剂
CN120265633A (zh) * 2022-12-09 2025-07-04 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
JP2026513871A (ja) * 2023-04-06 2026-05-01 アストラゼネカ・アクチエボラーグ Mpo阻害剤による治療方法
WO2025172474A1 (en) 2024-02-15 2025-08-21 Astrazeneca Ab Inhibitors of myeloperoxidase
CN121378265B (zh) * 2025-10-30 2026-07-24 乐平市康鑫医药化工有限公司 一种吡唑类化合物及其制备方法和用途

Family Cites Families (14)

* Cited by examiner, † Cited by third party
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
ATE501148T1 (de) * 2004-12-14 2011-03-15 Astrazeneca Ab Pyrazolopyrimidinverbindungen als antitumormittel
CN101472926A (zh) 2006-04-13 2009-07-01 阿斯利康(瑞典)有限公司 硫代黄嘌呤衍生物以及它们作为髓过氧化物酶抑制剂的用途
UY30267A1 (es) 2006-04-13 2007-11-30 Astrazeneca Ab Nuevos derivados de la tioxantina , composiciones farmacéuticas que los contienen, procedimientos de preparacion y aplicaciones
TW200804383A (en) 2006-06-05 2008-01-16 Astrazeneca Ab New compounds
WO2007142577A1 (en) 2006-06-05 2007-12-13 Astrazeneca Ab Pyrrolo[3,2-d]pyrimidin-4-one derivative as myeloperoxidase inhibitor
US20090054468A1 (en) * 2007-08-23 2009-02-26 Astrazeneca Ab New Use 938
USRE47009E1 (en) 2011-02-01 2018-08-28 The Children's Hospital Of Philadelphia 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

Also Published As

Publication number Publication date
TWI681963B (zh) 2020-01-11
NI201700065A (es) 2018-01-04
SG11201703961UA (en) 2017-06-29
US9616063B2 (en) 2017-04-11
BR112017011124B1 (pt) 2022-11-16
PL3227294T3 (pl) 2020-04-30
TW201639846A (zh) 2016-11-16
US20160152623A1 (en) 2016-06-02
US20240335446A1 (en) 2024-10-10
NZ732164A (en) 2018-02-23
US10016430B2 (en) 2018-07-10
JP2017535588A (ja) 2017-11-30
AU2015357290A1 (en) 2017-06-15
US11975004B2 (en) 2024-05-07
CA2968449A1 (en) 2016-06-09
EP3227294B1 (en) 2019-08-14
ES2751690T3 (es) 2020-04-01
SI3227294T1 (sl) 2019-11-29
EP3227294A1 (en) 2017-10-11
EA201791021A1 (ru) 2017-11-30
HRP20191744T1 (hr) 2019-12-27
EA030805B1 (ru) 2018-09-28
US20190076432A1 (en) 2019-03-14
RS59375B1 (sr) 2019-11-29
WO2016087338A1 (en) 2016-06-09
MX370492B (es) 2019-12-16
CN107001374A (zh) 2017-08-01
TN2017000208A1 (en) 2018-10-19
US20210228585A1 (en) 2021-07-29
UY36416A (es) 2016-06-01
DK3227294T3 (da) 2019-10-21
US11000525B2 (en) 2021-05-11
BR112017011124A2 (pt) 2017-12-26
ME03568B (me) 2020-07-20
CA2968449C (en) 2023-02-28
HUE045606T2 (hu) 2020-01-28
PH12017500977A1 (en) 2017-11-27
PT3227294T (pt) 2019-10-28
HK1245270A1 (en) 2018-08-24
SMT201900572T1 (it) 2019-11-13
MY195816A (en) 2023-02-22
IL252436A0 (en) 2017-07-31
US20170173025A1 (en) 2017-06-22
GT201700114A (es) 2019-08-12
KR20170088900A (ko) 2017-08-02
PE20170914A1 (es) 2017-07-12
KR102543404B1 (ko) 2023-06-14
MX2017007322A (es) 2018-02-19
CY1122587T1 (el) 2021-01-27
LT3227294T (lt) 2019-10-25
AU2015357290B2 (en) 2018-03-29
IL252436B (en) 2021-05-31
CO2017006658A2 (es) 2017-10-20
CN107001374B (zh) 2019-06-14
JP6616417B2 (ja) 2019-12-04
CL2017001380A1 (es) 2018-01-12
US12569489B2 (en) 2026-03-10
SV2017005451A (es) 2017-10-12

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