HRP20130144T4 - Inhibitori renina - Google Patents

Inhibitori renina Download PDF

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Publication number
HRP20130144T4
HRP20130144T4 HRP20130144TT HRP20130144T HRP20130144T4 HR P20130144 T4 HRP20130144 T4 HR P20130144T4 HR P20130144T T HRP20130144T T HR P20130144TT HR P20130144 T HRP20130144 T HR P20130144T HR P20130144 T4 HRP20130144 T4 HR P20130144T4
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Croatia
Prior art keywords
image
compound according
alkyl
compound
pharmaceutically acceptable
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HRP20130144TT
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English (en)
Inventor
John J. Baldwin
David A. Claremon
Colin M. Tice
Salvacion Cacatian
Lawrence W. Dillard
Alexey V. Ishchenko
Jing Yuan
Zhenrong Xu
Gerard Mcgeehan
Wei Zhao
Robert D. Simpson
Suresh B. Singh
Lanqi Jia
Patrick T. Flaherty
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Vitae Pharmaceuticals, Inc.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38786973&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20130144(T4) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Vitae Pharmaceuticals, Inc. filed Critical Vitae Pharmaceuticals, Inc.
Publication of HRP20130144T1 publication Critical patent/HRP20130144T1/hr
Publication of HRP20130144T4 publication Critical patent/HRP20130144T4/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/04Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • 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
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26Androgens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/42Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of mineralocorticosteroids
    • 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
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Claims (20)

1. Spoj koji je prikazan sa slijedećom strukturnom formulom: [image] ili njegova farmaceutski prihvatljiva sol, naznačen time da: R1 je alkil, cikloalkil ili cikloalkilalkil; R2 je H ili alkil; R3 je F, Cl, Br, cijano, nitro, alkil, haloalkil, alkoksi, haloalkoksi, ili alkansulfonil; te n je 0, 1, 2, ili 3.
2. Spoj prema zahtjevu 1, naznačen time da: R1 je (C1-C3)alkil; R2 je H ili (C1-C3)alkil; R3 je F, Cl, Br, cijano, nitro, (C1-C3)alkil, halo(C1-C3)alkil, (C1-C3)alkoksi, halo(C1-C9)alkoksi, ili (C1-C3)alkansulfonil; te n je 0, 1, 2, ili 3.
3. Spoj prema zahtjevu 1, naznačen time da je spoj prikazan sa slijedećom strukturnom formulom: [image] ili njegova farmaceutski prihvatljiva sol, pri čemu: R1 je (C1-C3)alkil; R2 je H ili (C1-C3)alkil; R3 je F, Cl, Br, cijano, nitro, (C1-C3)alkil, halo(C1-C3)alkil, (C1-C3)alkoksi, halo(C1-C3)alkoksi, ili (C1-C3)alkansulfonil; i n je 0, 1, 2, ili 3.
4. Spoj prema bilo kojem od zahtjeva 1-3, naznačen time da R1 je metil i R2 je H ili metil.
5. Spoj prema zahtjevu 1 ili 3, naznačen time da R3 je F, Cl, ili metil i n je 1 ili 2.
6. Spoj prema zahtjevu 1, naznačen time da je spoj prikazan sa strukturnom formulom koja je odabrana od: [image] [image] [image] [image] [image] [image] [image] i [image] ili njegova farmaceutski prihvatljiva sol.
7. Spoj prema zahtjevu 1 naznačen time da je prikazan sa slijedećom strukturnom formulom: [image] ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema zahtjevu 1 koji je prikazan sa slijedećom strukturnom formulom: [image] ili njegova farmaceutski prihvatljiva sol, naznačen time da je spoj barem 90% optički čist.
9. Farmaceutski pripravak naznačen time da sadrži farmaceutski prihvatljiv nosač ili razrjeđivač i spoj prema bilo kojem od zahtjeva 1-8.
10. Farmaceutski pripravak prema zahtjevu 9, naznačen time da dodatno sadrži α-blokator, β-10.blokator, blokator kalcijevog kanala, diuretik, natriuretik, saluretik, centralno djelujući antihipertenziv, inhibitor angiotenzin konvertirajućeg enzima, dvostruki angiotenzin konvertirajući enzim i neutralni inhibitor endopeptidaze, blokator receptora angiotenzina, dvostruki blokator receptora angiotenzina i antagonista receptora endotelina, inhibitor aldosteron sintaze, antagonist receptora aldosterona, ili antagonist receptora endotelina.
11. Spoj prema bilo kojem od zahtjeva 1-8 naznačen time da je za antagoniziranje jedne ili više aspartatnih proteaza.
12. Spoj prema zahtjevu 11, naznačen time da aspartatna proteaza je renin.
13. Uporaba spoja prema bilo kojem od zahtjeva 1-8 naznačena time da je za proizvodnju lijeka za antagoniziranje jedne ili više aspartatnih proteaza kod subjekta kojemu je to potrebno.
14. Spoj prema bilo kojem od zahtjeva 1-8 naznačen time da je za liječenje poremećaja koji je posredovan sa aspartatnom proteazom.
15. Spoj prema zahtjevu 14, naznačen time da navedeni poremećaj je hipertenzija, kongestivno zatajenje srca, srčana hipertrofija, srčana fibroza, kardiomiopatija nakon infarkta, nefropatija, vaskulopatija i neuropatija, bolest koronarnih krvnih žila, postoperativna hipertenzija, restenoza nakon angioplastike, povišeni intraokularni tlak, glaukom, nenormalan vaskularni rast, hiperaldosteronizam, stanje anksioznosti, ili kognitivni poremećaj.
16. Spoj prema zahtjevu 14, naznačen time da nadalje sadrži davanje jednog ili više dodatnih sredstava koja su odabrana iz skupine koja sadrži α-blokatore, β-blokator, blokator kalcijevog kanala, diuretik, inhibitor angiotenzin konvertirajućeg enzima, dvostruki angiotenzin konvertirajući enzim i neutralni inhibitor endopeptidaze, blokator receptora angiotenzina, dvostruki blokator receptora angiotenzina i antagonist receptora endotelina, inhibitor aldosteron sintaze, antagonist receptora aldosterona, te antagonist receptora endotelina.
17. Spoj prema zahtjevu 14, naznačen time da aspartatna proteaza je β-sekretaza, plazmepsin ili HIV proteaza.
18. Uporaba spoja prema bilo kojem od zahtjeva 1-8 naznačena time da je za proizvodnju lijeka za liječenje poremećaja koji je posredovan sa aspartatnom proteazom kod subjekta.
19. Spoj koji je prikazan sa strukturnom formulom koja je odabrana od: [image] [image] [image] [image] i [image] ili njegova sol, naznačen time da: R2 je H ili alkil; te E je H ili Boc.
20. Spoj prema zahtjevu 19, naznačen time da je spoj odabran iz skupine koja sadrži: tert-butil (S)-1-amino-3-((R)-tetrahidro-2H-piran-3-il)propan-2-ilkarbamat; tert-butil (S)-1-amino-3-((R)-tetrahidro-2H-piran-3-il)propan-2-il(metil)karbamat; tert-bultil-1-amino-3-(tetrahidro-2H-piran-3-il)propan-2-ilkarbamat; te tert-butil-1-amino-3-(tetrahidro-2H-piran-3-il)propan-2-il(metil)karbamat.
HRP20130144TT 2006-09-18 2013-02-20 Inhibitori renina HRP20130144T4 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US84529106P 2006-09-18 2006-09-18
PCT/US2007/020164 WO2008036247A1 (en) 2006-09-18 2007-09-18 Renin inhibitors

Publications (2)

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HRP20130144T1 HRP20130144T1 (en) 2013-03-31
HRP20130144T4 true HRP20130144T4 (hr) 2013-10-25

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US (2) US8198453B2 (hr)
EP (2) EP2581366A1 (hr)
JP (1) JP5331695B2 (hr)
KR (1) KR20090064582A (hr)
CN (1) CN101528723B (hr)
AR (1) AR062797A1 (hr)
AU (1) AU2007297729C1 (hr)
BR (1) BRPI0718460A2 (hr)
CA (1) CA2663263A1 (hr)
CL (1) CL2007002689A1 (hr)
DK (1) DK2074108T3 (hr)
ES (1) ES2400009T7 (hr)
HK (1) HK1129115A1 (hr)
HR (1) HRP20130144T4 (hr)
MX (1) MX2009002740A (hr)
NZ (1) NZ575803A (hr)
PE (1) PE20080843A1 (hr)
PL (1) PL2074108T6 (hr)
PT (1) PT2074108E (hr)
RS (1) RS52679B (hr)
SI (1) SI2074108T1 (hr)
TW (1) TWI403510B (hr)
WO (1) WO2008036247A1 (hr)

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