RS54743B1 - Agonisti adenozina a1 za tretman glaukoma i očnog pritiska - Google Patents

Agonisti adenozina a1 za tretman glaukoma i očnog pritiska

Info

Publication number
RS54743B1
RS54743B1 RS20160304A RSP20160304A RS54743B1 RS 54743 B1 RS54743 B1 RS 54743B1 RS 20160304 A RS20160304 A RS 20160304A RS P20160304 A RSP20160304 A RS P20160304A RS 54743 B1 RS54743 B1 RS 54743B1
Authority
RS
Serbia
Prior art keywords
hydrogen
methyl
group
pyrrolidine
piperidine
Prior art date
Application number
RS20160304A
Other languages
English (en)
Inventor
Jürgen Klar
Degenfeld Georges Von
Hans-Georg Lerchen
Barbara Albrecht-Küpper
Andreas Knorr
Peter Sandner
Daniel Meibom
Original Assignee
Bayer Ip Gmbh
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 Bayer Ip Gmbh filed Critical Bayer Ip Gmbh
Publication of RS54743B1 publication Critical patent/RS54743B1/sr

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • 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
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Ophthalmology & Optometry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)

Abstract

Jedinjenje, naznačeno time, što je predstavljeno formulom (I)u kojojA je kiseonik ili sumpor,R1 je vodonik ili grupa sa formulomu kojima# je veza prema atomu kiseonika,L1 je linearni (C2-C4)-alkandiil,L2 je linearni (C1-C3)-alkandiil,R3 i R8 su identični ili različiti i nezavisno izabrani iz grupe koja obuhvata vodonik, metil, propan-2-il, propan-1-il, 2-metilpropan-1-il, 1-metilpropan-1-il, butan-1-il, tert-butil, fenil, benzil, p-hidroksibenzil, indol-3-ilmetil, imidazol-4-ilmetil, hidroksimetil, 2-hidroksietil, 1-hidroksietil, merkaptometil, metiltiometil, 2-merkaptoetil. 2-metiltioetil, karbamoilmetil, 2-karbamoiletil, karboksimetil, 2-karboksietil, 4-aminobutan-1-il, 4-amino-3-hidroksibutan-1-il, 3-aminopropan-1-il, 2-aminometil, aminometil, 3-gvanidinopropan-1-il, 3-ureidopropan-1-il,R6 i R9 su nezavisno izabrani iz vodonika ili metila,R7 je vodonik ili (C1-C4)-alkil, iliR7 i R3 formiraju, zajedno sa atomima na kojima su spojeni, pirolidin- ili piperidin-prsten,R10 i R11 su identični ili različiti i su nezavisno izabrani iz vodonika ili (C1-C4)-alkila, pri čemu (C1-C4)-alkil može da bude supstituisan sa jednom grupom koja je izabrana iz hidroksi, (C1-C4)-alkoksi, amino, mono-(C1-C4)-alkilamino ili di-(C1-C4)-alkilamino, iliR10 i R8 formiraju, zajedno sa atomima na kojima su spojeni, pirolidin- ili piperidin-prsten, aR12 je vodonik ili hidroksikarbonil,R2 je vodonik ili grupa sa formulom -CH2OR1, pri čemu je R1 definisan kao malopre,R3 je vodonik, metil ili etil,R4 je vodonik, metil ili etil,iliR3 i R4 formiraju, zajedno sa atomom azota na kojeg su spojeni, azetidin-, pirolidin- ili piperidin-prsten, pri čemu pomenuti azetidin-, pirolidin- ili piperidin-prsten može da bude supstituisan sa jednim ili 2 supstituenta nezavisno izabrana iz grupe koja obuhvata fluoro, trifluorometil, metil, etil, metoksi i etoksi, ili njegove soli, solvati i solvati pomenutih soli za upotrebu u postupku za tretman i/ili profilaksu glaukoma, normotenzivnog glaukoma, očnog pritiska i/ili njihovih kombinacija.Prijava sadrži još 11 patentnih zahteva.
RS20160304A 2010-09-02 2011-08-29 Agonisti adenozina a1 za tretman glaukoma i očnog pritiska RS54743B1 (sr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10175151 2010-09-02
PCT/EP2011/064829 WO2012028585A1 (en) 2010-09-02 2011-08-29 Adenosine a1 agonists for the treatment of glaucoma and ocular hypertension
EP11752517.0A EP2611415B1 (en) 2010-09-02 2011-08-29 Adenosine a1 agonists for the treatment of glaucoma and ocular hypertension

Publications (1)

Publication Number Publication Date
RS54743B1 true RS54743B1 (sr) 2016-10-31

Family

ID=44582992

Family Applications (1)

Application Number Title Priority Date Filing Date
RS20160304A RS54743B1 (sr) 2010-09-02 2011-08-29 Agonisti adenozina a1 za tretman glaukoma i očnog pritiska

Country Status (30)

Country Link
US (3) US20120058983A1 (sr)
EP (1) EP2611415B1 (sr)
JP (1) JP5875585B2 (sr)
KR (1) KR20140091457A (sr)
CN (1) CN103249400B (sr)
AP (1) AP3413A (sr)
AU (1) AU2011298430B2 (sr)
BR (1) BR112013005224A2 (sr)
CA (1) CA2809700A1 (sr)
CL (2) CL2013000599A1 (sr)
CR (1) CR20130094A (sr)
CY (1) CY1117458T1 (sr)
DK (1) DK2611415T3 (sr)
EA (1) EA028411B1 (sr)
ES (1) ES2570659T3 (sr)
HK (1) HK1188138A1 (sr)
HR (1) HRP20160532T1 (sr)
HU (1) HUE027295T2 (sr)
MA (1) MA34489B1 (sr)
MX (1) MX2013002396A (sr)
MY (1) MY160383A (sr)
NZ (1) NZ607624A (sr)
PL (1) PL2611415T3 (sr)
RS (1) RS54743B1 (sr)
SG (1) SG187974A1 (sr)
SI (1) SI2611415T1 (sr)
TW (1) TWI516266B (sr)
UA (1) UA111947C2 (sr)
WO (1) WO2012028585A1 (sr)
ZA (1) ZA201302340B (sr)

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DE102009006602A1 (de) * 2009-01-29 2010-08-05 Bayer Schering Pharma Aktiengesellschaft Alkylamino-substituierte Dicyanopyridine und deren Aminosäureester-Prodrugs
ES2554684T3 (es) 2009-05-01 2015-12-22 Inotek Pharmaceuticals Corporation Método de reducción de la presión intraocular en humanos

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BR112013005224A2 (pt) 2016-05-03
EP2611415B1 (en) 2016-02-24
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JP2013536819A (ja) 2013-09-26
CN103249400A (zh) 2013-08-14
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