RS54752B1 - Triazolopiridini kao inhibitori fosfodiesteraze za lečenje kožnih bolesti - Google Patents

Triazolopiridini kao inhibitori fosfodiesteraze za lečenje kožnih bolesti

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Publication number
RS54752B1
RS54752B1 RS20160308A RSP20160308A RS54752B1 RS 54752 B1 RS54752 B1 RS 54752B1 RS 20160308 A RS20160308 A RS 20160308A RS P20160308 A RSP20160308 A RS P20160308A RS 54752 B1 RS54752 B1 RS 54752B1
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Serbia
Prior art keywords
alkyl
cycloalkyl
aryl
heterocycloalkyl
nr7r8
Prior art date
Application number
RS20160308A
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English (en)
Inventor
Simon Feldbæk Nielsen
Thomas Vifian
Anne Marie Horneman
Jesper Færgemann Lau
Original Assignee
Leo Pharma As
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Publication date
Application filed by Leo Pharma As filed Critical Leo Pharma As
Publication of RS54752B1 publication Critical patent/RS54752B1/sr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/08Antiseborrheics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/16Emollients or protectives, e.g. against radiation
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Toxicology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Jedinjenje opšte formule I,pri čemu R1 je C1-6 alkoksi, kao što su metoksi, mono-, di- ili trifluormetoksi, haiogen, ili hidroksi;R2 je alkil, cikloalkil, alkilcikloalkil, ili cikloalkil (C(O)NR7R8), od kojih je svaki opciono supstituisan sa jednim ili više supstituenata izabranih između R4;R3 je vodonik, halogen, aril, hetercaril, hidroksi, alkil, cikloalkil, heterocikloalkil, alkoksi, okso, cijano, amino, aminoalkil, alkilamino ili dialkilamino;R4je vodonik, halogen, hidroksi, okso, cijano, karboksi, ili trihalometil, ili R4 je NR5R6, -C(O)NR7R8, -C(O)R7, -COOR7, -NR5C(O)NR7R8, -OC(O)NR7R8, -OC(O)R3, NC(O)R7, -OR7, -NC(O)OR3, -NSO2R7, -SO2NR7R8, ili -SO2R7R8, alkil, cikloalkil, alkenil, alkinil, aril, heteroaril, cikloalkilalkil, cikloalkilalkenil, cikloalkilalkinil, cikloalkenilalkil, cikloalkenilalkenil, cikloalkenilalkinil, heterocikloalkil, heterocikloalkilalkil, heterocikioalkenil, heterocikloalkenilalkil, heterocikloalkenilalkenil, heterocikloalkenilalkinil, arilalkil, arilalkenil, arilalkinil, heteroariialkil, heteroarilalkenil, heteroarilalkinil, alkoksi, cikloalkiloksi, alkiltio, cikloalkiltio, sulfamoil, sulfinamoil, alkilamino ili cikloalkilamino, od kojih je svaki opciono supstituisan sa jednim ili više supstituenata izabranih između R9;svaki R5 i R6 nezavisno predstavlja vodonik, alkil, alkenil, cikloalkil, heterocikloalkil, -C(O)alkil, -C(O)Oalkil, -C(O)cikloalkil, -C(O)N-alkil, karboksialkil, -C(O)alkil-C(O)OH, -C(O)alkil-C(O)N-alkil, -C(O)N-aril, -S(O)2alkil, -S(O)alkil, -S(O)2aril, -S(O)2N-alkil, -S(O)aril, aril, heteroaril alkilaril ili alkilheteroaril, od kojih je svaki opciono supstituisan sa hidroksi ili jednim ili više halogena, ili R5 i R6 zajedno sa atomom azota za koji su vezani obrazuju heterocikloalkil prsten. pri čemu je pomenuti prsten opciono supstituisan sa jednom ili više alkil grupa; svaki R7 i R8 nezavisno predstavlja vodonik, alkil, cikloalkil, alkenil, heteroaril, heterocikloalkil, karboksialkil, karbamoilalkil, alkiloksialkil, alkeniloksialkil, aril, arilalkil, alkilaril, heteroaril, heteroarilalkil, ili alkilheteroaril, od kojih je svaki opciono supstituisan sa jednim ili više supstituenata izabranih iz grupe koju čine hidroksi, halogen, okso, cijano, alkil, cikloalkil, alkenil, alkoksi, aril, heteroaril, heterocikloalkil, -S(O)2-alkil, -S(O)2-NR11R12, -NC(O)-alkil, -C(O)N-alkil, -NC(O)O-alkil, -OC(O)N-alkil, -NC(O)NR11R12, -NR11SO2-alkil, -S(O)-alkil, iii R7 i R8 zajedno sa atomom azota za koji su vezani obrazuju heterocikloalkil prsten, pri čemu je pomenuti prsten opciono supstituisan sa jednom ili više alkil grupa;R9 je vodonik, halogen, hidroksi, alkoksi, karboksi ili trihalometil;X i Y su ili C i N ili N i C, respektivno;A je aril, cikloalkil, cikloalkenil, heteroaril, heterocikloalkil ili heterocikioalkenil, od kojih je svaki opciono supstituisan sa jednim ili više supstituenata izabranih iz grupe koja se sastoji od R10;R10 je vodonik, cijano, halogen, hidroksi, ili okso, ili je R10 alkil, cikloalkil, alkenil, alkinil, aril, heteroaril, cikloalkilalkil. cikloalkilalkenil, cikloalkilaikinil, cikloalkenilalkil, cikloalkenilalkenil, cikloalkenilalkinil, heterocikloalkil, heterocikloalkenil, heterocikloalkenilalkil, heterocikloalkenilalkenil, heterocikloalkenilalkinil, arilalkil, arilalkenil, arilalkinil, heteroarilalkil, heteroarilalkenii, heteroarilalkinil, alkoksi, cikloalkiloksi, alkiltio, cikloalkiltio, -S(O)alkil, -S(O)2-alkil, sulfamoil, sulfinamoil, -C(O)OR3, -C(O)R3, -NR5R6, -alkil(NR5R6), -cikloalkil(NR5R6), -cikloaikilalkil(NR5R6), -alkilcikloalkil(NR5R6), -C(O)NR7R8, -aikil(C(O)NR7R8), -cikloalkil(C(O)NR7R8), -cikloalkilalkil(C(O)NR7R8) ili -alkilcikloalkil(C(O)NR7R8), od kojih je svaki opciono supstituisan sa jednim ili više supstituenata izabranih između R4; R11 i R12 svaki nezavisno predstavlja vodonik ili alkil;i njegove farmaceutski prihvatljive soli, hidrati, N-oksidi ili solvati.Prijava sadrži još 29 patentnih zahteva.
RS20160308A 2008-12-19 2009-12-18 Triazolopiridini kao inhibitori fosfodiesteraze za lečenje kožnih bolesti RS54752B1 (sr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13944508P 2008-12-19 2008-12-19
EP09795687.4A EP2379548B1 (en) 2008-12-19 2009-12-18 Triazolopyridines as phosphodiesterase inhibitors for treatment of dermal diseases
PCT/DK2009/000262 WO2010069322A1 (en) 2008-12-19 2009-12-18 Triazolopyridines as phosphodiesterase inhibitors for treatment of dermal diseases

Publications (1)

Publication Number Publication Date
RS54752B1 true RS54752B1 (sr) 2016-10-31

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US (1) US8952162B2 (sr)
EP (1) EP2379548B1 (sr)
JP (2) JP5743901B2 (sr)
KR (1) KR20110094355A (sr)
CN (1) CN102317287B (sr)
AU (1) AU2009328752B2 (sr)
BR (1) BRPI0922452A2 (sr)
CA (1) CA2747022A1 (sr)
CY (1) CY1117562T1 (sr)
DK (1) DK2379548T3 (sr)
ES (1) ES2570769T3 (sr)
HK (1) HK1165791A1 (sr)
HR (1) HRP20160488T1 (sr)
HU (1) HUE027770T2 (sr)
IL (1) IL213570A (sr)
MX (1) MX2011006428A (sr)
NO (1) NO20110871A1 (sr)
NZ (1) NZ593595A (sr)
PL (1) PL2379548T3 (sr)
RS (1) RS54752B1 (sr)
RU (1) RU2544011C2 (sr)
SG (1) SG172206A1 (sr)
SI (1) SI2379548T1 (sr)
WO (1) WO2010069322A1 (sr)
ZA (1) ZA201104422B (sr)

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ME01858B (me) 2009-07-17 2014-12-20 Japan Tobacco Inc Jedinjenje triazolopiridina i njegovo dejstvo kao inhibitora prolil hidroksilaze i induktora proizvodnje eritropoetina
EP2343294A1 (en) 2009-11-30 2011-07-13 Bayer Schering Pharma AG Substituted triazolopyridines
CA2785251A1 (en) 2009-12-22 2011-06-30 Leo Pharma A/S Cutaneous composition comprising vitamin d analogue and a mixture of solvent and surfactants
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EP2515866B1 (en) 2009-12-22 2014-02-19 Leo Pharma A/S Pharmaceutical composition comprising solvent mixture and a vitamin d derivative or analogue
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WO2014083099A1 (en) * 2012-11-30 2014-06-05 Leo Pharma A/S A method of inhibiting the expression of il-22 in activated t-cells
WO2014206903A1 (en) 2013-06-25 2014-12-31 Leo Pharma A/S METHODS FOR THE PREPARATION OF SUBSTITUTED [1,2,4]TRIAZOLO[1,5-a]PYRIDINES
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JP2021155336A (ja) * 2018-06-27 2021-10-07 Meiji Seikaファルマ株式会社 新規pde4阻害剤
AR114977A1 (es) * 2018-06-27 2020-11-11 Meiji Seika Pharma Co Ltd Cristales de derivado de benzoxazol

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Publication number Publication date
EP2379548B1 (en) 2016-03-09
IL213570A (en) 2015-10-29
CN102317287A (zh) 2012-01-11
CA2747022A1 (en) 2010-06-24
EP2379548A1 (en) 2011-10-26
SI2379548T1 (sl) 2016-06-30
HRP20160488T1 (hr) 2016-06-17
CY1117562T1 (el) 2017-04-26
JP2015096535A (ja) 2015-05-21
RU2544011C2 (ru) 2015-03-10
JP5743901B2 (ja) 2015-07-01
WO2010069322A1 (en) 2010-06-24
BRPI0922452A2 (pt) 2015-12-15
PL2379548T3 (pl) 2016-08-31
HUE027770T2 (en) 2016-11-28
NZ593595A (en) 2013-07-26
MX2011006428A (es) 2011-07-28
AU2009328752B2 (en) 2015-07-16
SG172206A1 (en) 2011-07-28
DK2379548T3 (en) 2016-05-17
ES2570769T3 (es) 2016-05-20
KR20110094355A (ko) 2011-08-23
AU2009328752A1 (en) 2011-07-07
CN102317287B (zh) 2014-10-08
IL213570A0 (en) 2011-07-31
US8952162B2 (en) 2015-02-10
US20120028974A1 (en) 2012-02-02
ZA201104422B (en) 2012-09-26
JP2012512192A (ja) 2012-05-31
HK1165791A1 (en) 2012-10-12
NO20110871A1 (no) 2011-09-19

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