MD20140044A2 - 2-Tiopirimidinone şi utilizarea lor pentru tratamentul afecţiunilor cardiovasculare - Google Patents

2-Tiopirimidinone şi utilizarea lor pentru tratamentul afecţiunilor cardiovasculare Download PDF

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Publication number
MD20140044A2
MD20140044A2 MDA20140044A MD20140044A MD20140044A2 MD 20140044 A2 MD20140044 A2 MD 20140044A2 MD A20140044 A MDA20140044 A MD A20140044A MD 20140044 A MD20140044 A MD 20140044A MD 20140044 A2 MD20140044 A2 MD 20140044A2
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MD
Moldova
Prior art keywords
inhibitors
thiopyrimidinones
treatment
cardiovascular diseases
prodrugs
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MDA20140044A
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English (en)
Russian (ru)
Inventor
Филипп Альберт КАПРИНО
Эдвард Ли Конн
Дэвид Хепуорт
Дэниел Вэй-Шун КУН
Бенджамин Нейл РОКИ
Роджер Бенджамин Руггери
Джозеф Скотт ВАРМУС
Янь Чжан
Роберт Ли Дау
Мэтью Скотт ДАУЛИНГ
Суви Туула Марджукка ОРР
Мэтью Форрест САММОНС
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Pfizer Inc.
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Application filed by Pfizer Inc. filed Critical Pfizer Inc.
Publication of MD20140044A2 publication Critical patent/MD20140044A2/ro

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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    • C07D239/56—One oxygen atom and one sulfur atom
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    • A61K31/365—Lactones
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    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
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    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Cardiology (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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Abstract

Prezenta invenţie se referă la compuşi care inhibă mieloperoxidaza, la compoziţii farmaceutice care conţin asemenea inhibitori şi la utilizarea lor pentru tratamentul, de exemplu, al afecţiunilor cardiovasculare, inclusiv al sindromului coronarian acut.În calitate de inhibitori se propun 2-tiopirimidinone cu formula (I), sărurile lor farmaceutic acceptabile sau promedicamentele acestora, în care R1 şi R2 sunt definiţi în descrierea invenţiei:(I).
MDA20140044A 2011-11-11 2012-10-28 2-Tiopirimidinone şi utilizarea lor pentru tratamentul afecţiunilor cardiovasculare MD20140044A2 (ro)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161558605P 2011-11-11 2011-11-11
PCT/IB2012/055949 WO2013068875A1 (en) 2011-11-11 2012-10-28 2-thiopyrimidinones

Publications (1)

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MD20140044A2 true MD20140044A2 (ro) 2014-08-31

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MDA20140044A MD20140044A2 (ro) 2011-11-11 2012-10-28 2-Tiopirimidinone şi utilizarea lor pentru tratamentul afecţiunilor cardiovasculare

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US (4) US8835449B2 (ro)
EP (1) EP2776405A1 (ro)
JP (1) JP5731718B2 (ro)
KR (1) KR101650262B1 (ro)
CN (1) CN103917529B (ro)
AP (1) AP2014007621A0 (ro)
AR (1) AR088805A1 (ro)
AU (1) AU2012335220B2 (ro)
BR (1) BR112014011254A2 (ro)
CA (1) CA2853024C (ro)
CL (1) CL2014000996A1 (ro)
CO (1) CO6960543A2 (ro)
CR (1) CR20140179A (ro)
CU (1) CU20140049A7 (ro)
DO (1) DOP2014000098A (ro)
EA (1) EA027324B1 (ro)
EC (1) ECSP14004595A (ro)
GE (1) GEP201706656B (ro)
GT (1) GT201400090A (ro)
IL (2) IL232425A (ro)
MA (1) MA35638B1 (ro)
MD (1) MD20140044A2 (ro)
MX (1) MX351299B (ro)
NI (1) NI201400042A (ro)
PE (1) PE20161219A1 (ro)
PH (1) PH12014501032A1 (ro)
SG (1) SG11201401531RA (ro)
TN (1) TN2014000195A1 (ro)
TW (2) TWI480269B (ro)
UA (1) UA108713C2 (ro)
UY (1) UY34442A (ro)
WO (1) WO2013068875A1 (ro)
ZA (1) ZA201403589B (ro)

Families Citing this family (14)

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Publication number Priority date Publication date Assignee Title
EP2386555A1 (en) 2010-05-13 2011-11-16 Almirall, S.A. New cyclohexylamine derivatives having beta2 adrenergic agonist and m3 muscarinic antagonist activities
SG11201401531RA (en) 2011-11-11 2014-07-30 Pfizer 2-thiopyrimidinones
EP2592078A1 (en) 2011-11-11 2013-05-15 Almirall, S.A. New cyclohexylamine derivatives having beta2 adrenergic agonist and M3 muscarinic antagonist activities
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