EA201891599A1 - Новые производные фосфинанов и азафосфинанов, способ их получения и содержащие их фармацевтические композиции - Google Patents

Новые производные фосфинанов и азафосфинанов, способ их получения и содержащие их фармацевтические композиции

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Publication number
EA201891599A1
EA201891599A1 EA201891599A EA201891599A EA201891599A1 EA 201891599 A1 EA201891599 A1 EA 201891599A1 EA 201891599 A EA201891599 A EA 201891599A EA 201891599 A EA201891599 A EA 201891599A EA 201891599 A1 EA201891599 A1 EA 201891599A1
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EA
Eurasian Patent Office
Prior art keywords
azaphosphinanes
phosphinanes
receiving
pharmaceutical compositions
new derivatives
Prior art date
Application number
EA201891599A
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English (en)
Other versions
EA035072B1 (ru
Inventor
Филипп Глоанек
Арно-Пьер Шаффнер
Патрисия Сансильвестри-Морель
Ален Рупен
Филипп Маннесье
Мари-Одиль Валлез
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Ле Лаборатуар Сервье
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Application filed by Ле Лаборатуар Сервье filed Critical Ле Лаборатуар Сервье
Publication of EA201891599A1 publication Critical patent/EA201891599A1/ru
Publication of EA035072B1 publication Critical patent/EA035072B1/ru

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6568Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • C07F9/65842Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • C07F9/65842Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring
    • C07F9/65846Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring the phosphorus atom being part of a six-membered ring which may be condensed with another ring system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

Соединения формулы (I)в которой Akпредставляет собой алкильную цепь, X представляет собой -(CH)-, -CH(R)-, -N(R)-, -CH-N(R)-, -N(R)-CH- или -CH-N(R)-CH-, m и R имеют значения, определенные в описании, Rи Rкаждый представляет собой H, когда X представляет собой -(CH)-, -CH(R)-, -N(R)-, -CH-N(R)- или -N(R)-CH-, или вместе образуют связь, когда X представляет собой -CH-N(R)-CH-, Rпредставляет собой NH, Cy-NH, Cy-Ak-NHили пиперидин-4-ил, Cy и Akимеют значения, определенные в описании, Rи R, которые могут быть одинаковыми или разными, каждый представляют собой H или F, их оптические изомеры, а также их соли присоединения к фармацевтически приемлемой кислоте. Лекарственные средства.
EA201891599A 2016-01-14 2017-01-13 НОВЫЕ ПРОИЗВОДНЫЕ ФОСФИНАНОВ И АЗАФОСФИНАНОВ, КОТОРЫЕ ЯВЛЯЮТСЯ ИНГИБИТОРАМИ TAFIa, И СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ EA035072B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR1670004A FR3046793B1 (fr) 2016-01-14 2016-01-14 Nouveaux derives de phosphinanes et azaphosphinanes, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
PCT/FR2017/050075 WO2017121969A1 (fr) 2016-01-14 2017-01-13 Nouveaux derives de phosphinanes et azaphosphinanes, leur procede de preparation et les compositions pharmaceutiques qui les contiennent

Publications (2)

Publication Number Publication Date
EA201891599A1 true EA201891599A1 (ru) 2019-01-31
EA035072B1 EA035072B1 (ru) 2020-04-23

Family

ID=55752640

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201891599A EA035072B1 (ru) 2016-01-14 2017-01-13 НОВЫЕ ПРОИЗВОДНЫЕ ФОСФИНАНОВ И АЗАФОСФИНАНОВ, КОТОРЫЕ ЯВЛЯЮТСЯ ИНГИБИТОРАМИ TAFIa, И СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

Country Status (47)

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US (2) US10138260B2 (ru)
EP (1) EP3271368B1 (ru)
JP (1) JP2019504070A (ru)
KR (1) KR20180101522A (ru)
CN (1) CN108495857A (ru)
AR (1) AR107433A1 (ru)
AU (1) AU2017207003B2 (ru)
BR (1) BR112018014020A2 (ru)
CA (1) CA3011184C (ru)
CL (1) CL2018001862A1 (ru)
CO (1) CO2018007271A2 (ru)
CU (1) CU20180072A7 (ru)
CY (1) CY1121154T1 (ru)
DK (1) DK3271368T3 (ru)
DO (1) DOP2018000165A (ru)
EA (1) EA035072B1 (ru)
EC (1) ECSP18051972A (ru)
ES (1) ES2709376T3 (ru)
FR (1) FR3046793B1 (ru)
GE (1) GEP20207092B (ru)
HK (1) HK1244283B (ru)
HR (1) HRP20190193T1 (ru)
HU (1) HUE042924T2 (ru)
IL (1) IL260425B (ru)
JO (1) JO3660B1 (ru)
LT (1) LT3271368T (ru)
MA (1) MA41798B1 (ru)
MD (1) MD3271368T2 (ru)
ME (1) ME03305B (ru)
MX (1) MX367319B (ru)
NI (1) NI201800073A (ru)
PE (1) PE20181503A1 (ru)
PH (1) PH12018501373A1 (ru)
PL (1) PL3271368T3 (ru)
PT (1) PT3271368T (ru)
RS (1) RS58338B1 (ru)
RU (1) RU2729641C2 (ru)
SG (1) SG11201805757WA (ru)
SI (1) SI3271368T1 (ru)
SV (1) SV2018005721A (ru)
TN (1) TN2018000226A1 (ru)
TR (1) TR201820430T4 (ru)
TW (1) TWI625334B (ru)
UA (1) UA121275C2 (ru)
UY (1) UY37072A (ru)
WO (1) WO2017121969A1 (ru)
ZA (1) ZA201804391B (ru)

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* Cited by examiner, † Cited by third party
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FR3046793B1 (fr) * 2016-01-14 2018-01-05 Les Laboratoires Servier Nouveaux derives de phosphinanes et azaphosphinanes, leur procede de preparation et les compositions pharmaceutiques qui les contiennent

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI1311488T1 (sl) * 2000-08-17 2010-01-29 Pfizer Ltd Substituirani imidazoli kot inhibitorji TAFIA
SE0103272D0 (sv) * 2001-09-28 2001-09-28 Astrazeneca Ab Chemical compounds
WO2003076416A1 (en) * 2002-03-08 2003-09-18 Warner-Lambert Company Llc Oxo azabicyclic compounds
US7420000B2 (en) * 2003-09-10 2008-09-02 University Of Southern California Amino phosphonate and amino bis-phosphonate derivatives
US20050143349A1 (en) * 2003-12-17 2005-06-30 Quatrx Pharmaceuticals Co. Phosphorus containing compounds useful for the regulation of LDL and Lp(a) levels
US20060234986A1 (en) * 2005-04-18 2006-10-19 Schering Aktiengesellschaft Use of TAFI inhibitors for enhanced myocardial reperfusion and facilitated PCI
JP5478488B2 (ja) * 2007-06-20 2014-04-23 メルク・シャープ・アンド・ドーム・コーポレーション Janusキナーゼの阻害剤
FR2920773B1 (fr) * 2007-09-11 2009-10-23 Servier Lab Derives de 1,2,4,5-tetrahydro-3h-benzazepines, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
FR2947266B1 (fr) * 2009-06-26 2011-06-17 Servier Lab Nouveaux derives d'acide 2-mercaptocyclopentanecarboxylique, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
EP2507249B1 (en) * 2009-09-09 2015-11-11 Gilead Sciences, Inc. Inhibitors of flaviviridae viruses
AU2013292950C1 (en) * 2012-07-18 2016-01-21 Sunshine Lake Pharma Co., Ltd. Nitrogenous heterocyclic derivatives and their application in drugs
FR3046793B1 (fr) * 2016-01-14 2018-01-05 Les Laboratoires Servier Nouveaux derives de phosphinanes et azaphosphinanes, leur procede de preparation et les compositions pharmaceutiques qui les contiennent

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AR107433A1 (es) 2018-05-02
MX367319B (es) 2019-08-15
TN2018000226A1 (fr) 2019-10-04
HK1244283B (zh) 2019-11-22
LT3271368T (lt) 2018-12-10
HRP20190193T1 (hr) 2019-04-05
FR3046793A1 (fr) 2017-07-21
TW201726697A (zh) 2017-08-01
KR20180101522A (ko) 2018-09-12
PT3271368T (pt) 2018-12-04
MA41798B1 (fr) 2018-11-30
HUE042924T2 (hu) 2019-07-29
EP3271368B1 (fr) 2018-10-31
SV2018005721A (es) 2018-09-06
CU20180072A7 (es) 2018-10-04
JP2019504070A (ja) 2019-02-14
WO2017121969A1 (fr) 2017-07-20
GEP20207092B (en) 2020-04-10
RS58338B1 (sr) 2019-03-29
JO3660B1 (ar) 2020-08-27
EP3271368A1 (fr) 2018-01-24
ECSP18051972A (es) 2018-07-31
EA035072B1 (ru) 2020-04-23
BR112018014020A2 (pt) 2018-12-11
CA3011184A1 (fr) 2017-07-20
RU2729641C2 (ru) 2020-08-11
US20190031693A1 (en) 2019-01-31
TWI625334B (zh) 2018-06-01
AU2017207003A2 (en) 2018-10-04
ES2709376T3 (es) 2019-04-16
FR3046793B1 (fr) 2018-01-05
US10654878B2 (en) 2020-05-19
AU2017207003B2 (en) 2020-10-08
ME03305B (me) 2019-10-20
DOP2018000165A (es) 2018-09-15
MD3271368T2 (ro) 2019-03-31
UA121275C2 (uk) 2020-04-27
RU2018129027A (ru) 2020-02-14
UY37072A (es) 2017-07-31
CA3011184C (fr) 2020-09-29
IL260425B (en) 2020-05-31
NI201800073A (es) 2018-09-06
TR201820430T4 (tr) 2019-01-21
PH12018501373B1 (en) 2019-02-27
CO2018007271A2 (es) 2018-07-19
CY1121154T1 (el) 2020-05-29
US10138260B2 (en) 2018-11-27
DK3271368T3 (da) 2019-02-25
RU2018129027A3 (ru) 2020-03-19
PL3271368T3 (pl) 2019-04-30
ZA201804391B (en) 2020-01-29
AU2017207003A1 (en) 2018-07-26
PE20181503A1 (es) 2018-09-18
PH12018501373A1 (en) 2019-02-27
MA41798A (fr) 2018-01-24
MX2018008639A (es) 2018-11-19
CN108495857A (zh) 2018-09-04
CL2018001862A1 (es) 2018-10-05
SG11201805757WA (en) 2018-08-30
US20180016288A1 (en) 2018-01-18
SI3271368T1 (sl) 2019-02-28

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