MD4516B1 - Derivaţi noi de tienopirimidină, procedeu de preparare a acestora, compoziţii farmaceutice care îi conţin şi utilizările lor în calitate de agenţi proapoptotici - Google Patents

Derivaţi noi de tienopirimidină, procedeu de preparare a acestora, compoziţii farmaceutice care îi conţin şi utilizările lor în calitate de agenţi proapoptotici Download PDF

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Publication number
MD4516B1
MD4516B1 MDA20140137A MD20140137A MD4516B1 MD 4516 B1 MD4516 B1 MD 4516B1 MD A20140137 A MDA20140137 A MD A20140137A MD 20140137 A MD20140137 A MD 20140137A MD 4516 B1 MD4516 B1 MD 4516B1
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MD
Moldova
Prior art keywords
preparation
pharmaceutical compositions
compositions containing
proapoptotic agents
thienopyrimidine derivatives
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MDA20140137A
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English (en)
Russian (ru)
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MD20140137A2 (ro
MD4516C1 (ro
Inventor
Котцки АНДРАС
Славик ЗОЛТАН
Чекей МАРТОН
Пацал АТТИЛА
Цабо ЗОЛТАН
Сипос ЦАБОЛЧ
Радич ГАБОР
Проценьяк АГНЕС
Балинт БАЛАЖ
Бруно АЛЕН
Дженест ОЛИВЕР
Джеймс Эдвард Пол Дэвидсон
Джеймс Брук МЮРРЕЙ
Ай-Джен ЧЕНЬ
Франсуаза ПЕРРОН-СЬЕРРА
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Les Laboratoires Servier
Vernalis (R&D) Ltd
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Publication of MD20140137A2 publication Critical patent/MD20140137A2/ro
Publication of MD4516B1 publication Critical patent/MD4516B1/ro
Publication of MD4516C1 publication Critical patent/MD4516C1/ro

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    • 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
    • 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
    • A61K31/535—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
    • 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
    • A61K31/535—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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Radiology & Medical Imaging (AREA)
  • Pathology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Invenţia se referă la derivaţi noi de tienopirimidină cu formula (I):în care R1, R2, R3, R4, R5, R6, R7, R12, X, A şi n au semnificaţiile definite în descriere. Invenţia se mai referă la un procedeu de preparare a acestora şi la compoziţii farmaceutice care îi conţin.Compoziţiile menţionate pot fi utilizate în calitate de agenţi proapoptotici în tratamentul cancerelor, maladiilor autoimune şi ale sistemului imun.
MDA20140137A 2013-12-23 2014-12-22 Derivaţi noi de tienopirimidină, procedeu de preparare a acestora, compoziţii farmaceutice care îi conţin şi utilizările lor în calitate de agenţi proapoptotici MD4516C1 (ro)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR1363500A FR3015483B1 (fr) 2013-12-23 2013-12-23 Nouveaux derives de thienopyrimidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent

Publications (3)

Publication Number Publication Date
MD20140137A2 MD20140137A2 (ro) 2015-06-30
MD4516B1 true MD4516B1 (ro) 2017-09-30
MD4516C1 MD4516C1 (ro) 2018-04-30

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MDA20140137A MD4516C1 (ro) 2013-12-23 2014-12-22 Derivaţi noi de tienopirimidină, procedeu de preparare a acestora, compoziţii farmaceutice care îi conţin şi utilizările lor în calitate de agenţi proapoptotici

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US (3) US9670227B2 (ro)
EP (1) EP2886545B1 (ro)
JP (1) JP5922215B2 (ro)
KR (1) KR101636401B1 (ro)
CN (1) CN104725397B (ro)
AP (1) AP2014008127A0 (ro)
AR (1) AR098906A1 (ro)
AU (1) AU2014274644B2 (ro)
BR (1) BR102014032336B1 (ro)
CA (1) CA2875226C (ro)
CL (1) CL2014003444A1 (ro)
CO (1) CO7210068A1 (ro)
CR (1) CR20140569A (ro)
CU (1) CU24309B1 (ro)
CY (1) CY1118058T1 (ro)
DK (1) DK2886545T3 (ro)
DO (1) DOP2014000282A (ro)
EA (1) EA029601B1 (ro)
ES (1) ES2594377T3 (ro)
FR (1) FR3015483B1 (ro)
GE (1) GEP201706619B (ro)
GT (1) GT201400297A (ro)
HK (1) HK1209750A1 (ro)
HR (1) HRP20161203T8 (ro)
HU (1) HUE029654T2 (ro)
IL (1) IL236143A (ro)
JO (1) JO3193B1 (ro)
LT (1) LT2886545T (ro)
MD (1) MD4516C1 (ro)
ME (1) ME02521B (ro)
MX (1) MX351581B (ro)
MY (1) MY185221A (ro)
NI (1) NI201400150A (ro)
PE (1) PE20151064A1 (ro)
PH (1) PH12014000375B1 (ro)
PL (1) PL2886545T3 (ro)
PT (1) PT2886545T (ro)
RS (1) RS55213B1 (ro)
RU (1) RU2605403C2 (ro)
SA (1) SA114360144B1 (ro)
SG (1) SG10201408563UA (ro)
SI (1) SI2886545T1 (ro)
TN (1) TN2014000516A1 (ro)
TW (1) TWI508969B (ro)
UA (1) UA120341C2 (ro)
UY (1) UY35915A (ro)
WO (1) WO2015097123A1 (ro)
ZA (1) ZA201409365B (ro)

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