HRP20160465T1 - Novi supstituirani derivati izokinolina - Google Patents

Novi supstituirani derivati izokinolina Download PDF

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Publication number
HRP20160465T1
HRP20160465T1 HRP20160465TT HRP20160465T HRP20160465T1 HR P20160465 T1 HRP20160465 T1 HR P20160465T1 HR P20160465T T HRP20160465T T HR P20160465TT HR P20160465 T HRP20160465 T HR P20160465T HR P20160465 T1 HRP20160465 T1 HR P20160465T1
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Croatia
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group
groups
alkyl
amino
alkynyl
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HRP20160465TT
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English (en)
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Hiroyushi Hidaka
Kengo Sumi
Kouichi Takahashi
Yoshihiro Inoue
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D. Western Therapeutics Institute, Inc.
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Publication of HRP20160465T1 publication Critical patent/HRP20160465T1/hr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/04Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • 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
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Claims (10)

1. Izokinolin-6-sulfonamid derivat predstavljen Formulom (1), sol istog ili solvat derivata ili sol: [image] naznačen time, da R1 i R2 svaki neovisno predstavlja atom vodika, atom halogena, cijano skupinu, alkilnu skupinu, halogenoalkilnu skupinu, alkenilnu skupinu, alkinilnu skupinu, alkoksi skupinu, alkiltio skupinu, hidroksilnu skupinu, merkapto skupinu, nitro skupinu, amino skupinu, aminoalkiltio skupinu ili heteroarilnu skupinu; R3 i R4 svaki neovisno predstavlja atom vodika, alkilnu skupinu, hidroksialkilnu skupinu, dialkilaminoalkilnu skupinu ili aminoalkanoilnu skupinu; R5 predstavlja atom vodika, po izboru supstituiranu alkilnu skupinu, alkenilnu skupinu, po izboru supstituiranu alkinilnu skupinu, po izboru supstituiranu cikloalkilnu skupinu ili po izboru supstituiranu alkanoilnu skupinu ili R4 i R5 mogu tvoriti zasićeni heterociklički prsten zajedno sa susjednim atomom dušika, pri čemu je supstituent na alkilnoj skupini, alkinilna skupina, cikloalkilna skupina oili alkanoilna skupina u R5 je najmanje jedn supstituient odabran od (a) cikloalkilne skupine, arilne skupine, heteroarilne skupine, ariloksi skupine, heteroariloksi skupine, arilenske skupine ili heteroarilenske skupine koja po izboru ima, na prstenu, najmanje jedn supstituent odabran od atoma halogena, cijano skupine, alkilne skupine, halogenoalkilne skupine, alkenilne skupine, alkinilne skupine, alkoksi skupine, alkiltio skupine, hidroksilne skupine, okso skupine, skupine formula, alkanoilne skupine, karboksilne skupine, alkiloksikarbonilne skupine, merkapto skupine, nitro skupine, amino skupine, urea skupine, tiourea skupine i aminoalkilne skupine, (b) hidroksilne skupine, (c) okso skupine, (d) alkanoiloksi skupine, (e) amino skupine, (f) karboksilne skupine, (g) alkoksi skupine i (h) alkilooksikarbonilne skupine; i A predstavlja ravnu ili razgrananu alkilensku skupinu koja ima 2 do 6 ugljikovih atoma i po izboru ima najmanje jedan supstituent odabran od karboksilne skupine, atoma halogena, cijano skupine, okso skupine, alkenilne skupine, alkinilne skupine, alkoksi skupine, hidroksilne skupine, alkiloksikarbonilne skupine, aminoalkilne skupine, arilne skupine, heteroarilne skupine, po izboru supstituiranu aralkilnu skupinu i po izboru supstituiranu heteroarilakilnu skupinu, pri čemu aralkilna skupina ili heteroarilalkilna skupina u A po ziboru imaju najmanje jedan supstituent odabran od atoma halogena, cijano skupine, alkilne skupine, halogenoalkilne skupine, alkenilne skupine, alkinilne skupine, alkoksi skupine, alkiltio skupine, hidroksilne skupine, okso skupine, skupine formila, alkanoilne skupine, karboksilne skupine, alkiloksikarbonilne skupine, merkapto skupine, nitro skupine, amino skupine, urea skupine, tiourea skupine i aminoalkilne skupine.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da R1 i R2 su svaki neovisno atom vodika, atom halogena, C1-8 alkilna skupina, nitro skupina, cijano skupina, halogeno C1-8 alkilna skupina, fenilna skupina, C2-8 alkenilna skupina, C2-8 alkinilna skupina, hidroksilna skupina, amino skupina, amino C1-8 alkiltio skupina ili tienil skupina.
3. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 ili 2, naznačen time, da je supstituent na alkilnoj skupini, alkinilnoj skupini, cikloalkilnoj skupini ili alkanoilnoj skupini u R5 najmanje jedan supstituent odabran od (a) arilne skupine, heteroarilne skupine ili arilenske skupine koji po izboru ima, na prstenu, najmanje jedan supstituent odabran od atoma halogena, cijano skupine, C1-8 alkilne skupine, halogeno C1-8 alkilne skupine, C2-8 alkenilne skupine, C2-8 alkinilne skupine, C1-8 alkoksi skupine, C1-8 alkiltio skupine, hidroksilne skupine, okso skupine, skupine formila, C1-8 alkanoilne skupine, karboksilne skupine, C1-8 alkilooksikarbonilne skupine, merkapto skupine, nitro skupine, amino skupine, urea skupine, tiourea skupine i amino C1-8 alkilne skupine, (b) hidroksilne skupine, (c) okso skupine, (d) alkanoiloksi skupine, (e) amino skupine, (f) karboksilne skupine, (g) alkoksi skupine i (h) alkilooksikarbonilne skupine.
4. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time, da R5 predstavlja atom vodika, po supstituiranu C1-8 alkilnu skupin, C2-8 alkenilnu skupinu, C2-8 alkinilnu skupinu, C3-8 cikloalkilnu skupinu ili po izboru supstituiranu C1-8 alkanoilnu skupinu ili R4 i R5 mogu tvoriti zasićeni heterociklički prsten zajedno sa susjednim atomom dušika, pri čemu je supstituent na alkilnoj skupini ili alkanoilnoj skupini najmanje jedan spstituient koji je odabran od (a) arilne skupine, heteroarilne skupine ili arilen skupine koja po izboru može imati, na prstenu, jamanje jedan supstituent koji je odabran od atoma halogena, cijano skupine, C1-8 alkilne skupine, halogeno C1-8 alkilne skupine, C2-8 alkeniln skupine, C2-8 alkinilne skupine, C1-8 alkoksi skupine, C1-8 alkiltio skupine, hidroksilne skupine, okso skupine, skupine formila, C2-8 alkanoilne skupine, karboksilne skupine, C1-8 alkiloksikarbonilne skupine, nitro skupine, amino skupine i amino C1-8 alkilne skupine, (b) hidroksilne skupine, (c) okso skupine i (d) C2-8 alkanoiloksi skupine.
5. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time, da su R3 i R4 svaki neovisno atom vodika, C1-8 alkilna skupina, hidroksi C1-8 alkilna skupina, di(C1-8 alkil)amino C1-8 alkilna skupina ili amino C2-8 alkanoilna skupina.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time, da je A ravna ili razgranana alkilenska skupina koja ima 2 do 6 ugljikovih atoma i po izboru ima najmanje jedan supstituent odabran od karboksilne skupine, atoma halogena, cijano skupine, C2-8 alkenilne skupine, C2-8 alkinilne skupine, amino C1-8 alkilne skupine, po izboru supstituirane fenil C1-8 alkilne skupine i po izboru supstituirane heteroaril C1-8 alkilne skupine.
7. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time, da je A ravna ili razgranana alkilenska skupina koja ima 2 do 6 ugljikova atoma.
8. Spoj u skladu s patentnim zahtjevom 1 ili 2, naznačen time, da kada je A ravna ili razgranana alkilenska skupina supstituirana skupinom koja je odabrana po izboru od sustituirane aralkilne skupine i po izboru supstituirane heteroarilalkilne skupine, R4 i R5 su vodikov atom ili C1-3 alkilna skupina.
9. Farmaceutski pripravak, naznačen time, da se sastoji od spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 8.
10. Spoj u skladu s patentnim zahtjevima 1 do 8, naznačen time, da je za uporabu u prevenciji i/ili liječenju glaukoma, očne hipertenzije ili srčanožilnih bolesti.
HRP20160465TT 2010-12-22 2016-05-03 Novi supstituirani derivati izokinolina HRP20160465T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2010286445 2010-12-22
PCT/JP2011/079725 WO2012086727A1 (ja) 2010-12-22 2011-12-21 新たな置換イソキノリン誘導体
EP11851146.8A EP2657227B1 (en) 2010-12-22 2011-12-21 Novel substituted isoquinoline derivative

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HRP20160465T1 true HRP20160465T1 (hr) 2016-06-03

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US (1) US8883792B2 (hr)
EP (1) EP2657227B1 (hr)
JP (1) JP5781093B2 (hr)
KR (1) KR101911324B1 (hr)
CN (1) CN103270024B (hr)
AU (1) AU2011345969B2 (hr)
BR (1) BR112013015604B1 (hr)
CA (1) CA2822787C (hr)
CY (1) CY1117560T1 (hr)
DK (1) DK2657227T3 (hr)
EA (1) EA022646B1 (hr)
ES (1) ES2571529T3 (hr)
HK (1) HK1185619A1 (hr)
HR (1) HRP20160465T1 (hr)
HU (1) HUE029976T2 (hr)
MX (1) MX2013007296A (hr)
NZ (1) NZ612336A (hr)
PL (1) PL2657227T3 (hr)
PT (1) PT2657227T (hr)
TW (1) TWI527799B (hr)
WO (1) WO2012086727A1 (hr)

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JP2021042126A (ja) * 2017-12-27 2021-03-18 佐藤製薬株式会社 アリールオキシ化合物
JP7425482B2 (ja) 2018-12-17 2024-01-31 株式会社デ・ウエスタン・セラピテクス研究所 イソキノリンスルホンアミドの新規な形態
JPWO2020129877A1 (ja) * 2018-12-18 2021-10-28 株式会社デ・ウエスタン・セラピテクス研究所 イソキノリンスルホニルクロリド酸付加塩及びその製造方法
WO2020172615A1 (en) 2019-02-22 2020-08-27 Glaukos Corporation Compounds for the treatment of ocular disease
CN114340740A (zh) * 2019-07-01 2022-04-12 库拉森疗法公司 β肾上腺素能激动剂及其使用方法
CN110616439B (zh) * 2019-10-31 2020-06-30 安阳师范学院 电化学氧化合成4-磺酸取代异喹啉酮衍生物的方法
AU2021331624A1 (en) * 2020-08-31 2023-05-04 Viewpoint Therapeutics, Inc. Compounds and formulations for treating ophthalmic diseases

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Also Published As

Publication number Publication date
DK2657227T3 (en) 2016-08-01
CN103270024A (zh) 2013-08-28
NZ612336A (en) 2014-05-30
CA2822787A1 (en) 2012-06-28
PT2657227T (pt) 2016-08-01
KR20130142163A (ko) 2013-12-27
MX2013007296A (es) 2013-08-26
AU2011345969A1 (en) 2013-07-11
EP2657227B1 (en) 2016-04-27
AU2011345969B2 (en) 2016-04-21
EA022646B1 (ru) 2016-02-29
JP5781093B2 (ja) 2015-09-16
CA2822787C (en) 2018-07-17
BR112013015604B1 (pt) 2021-11-03
EP2657227A1 (en) 2013-10-30
TW201305112A (zh) 2013-02-01
JPWO2012086727A1 (ja) 2014-06-05
CY1117560T1 (el) 2017-04-26
US8883792B2 (en) 2014-11-11
TWI527799B (zh) 2016-04-01
BR112013015604A2 (pt) 2018-07-24
KR101911324B1 (ko) 2018-10-25
EP2657227A4 (en) 2013-11-27
HK1185619A1 (zh) 2014-02-21
US20130274269A1 (en) 2013-10-17
EA201390939A1 (ru) 2013-12-30
PL2657227T3 (pl) 2016-09-30
WO2012086727A1 (ja) 2012-06-28
HUE029976T2 (en) 2017-04-28
CN103270024B (zh) 2015-07-08
ES2571529T3 (es) 2016-05-25

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