HRP20100180T1 - Novi spoj piridazina i njegova primjena - Google Patents

Novi spoj piridazina i njegova primjena Download PDF

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Publication number
HRP20100180T1
HRP20100180T1 HR20100180T HRP20100180T HRP20100180T1 HR P20100180 T1 HRP20100180 T1 HR P20100180T1 HR 20100180 T HR20100180 T HR 20100180T HR P20100180 T HRP20100180 T HR P20100180T HR P20100180 T1 HRP20100180 T1 HR P20100180T1
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Croatia
Prior art keywords
compound according
compound
image
acid
phenyl
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HR20100180T
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English (en)
Inventor
S. Bondy Steven
C. Dahl Terrence
A. Oare David
Oliyai Reza
C. Tse Winston
Zia Vahid
Original Assignee
Gilead Sciences
K.U. Leuven Research & Development
Gerhard Puerstinger
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.)
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Application filed by Gilead Sciences, K.U. Leuven Research & Development, Gerhard Puerstinger filed Critical Gilead Sciences
Publication of HRP20100180T1 publication Critical patent/HRP20100180T1/hr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses

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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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Postupak za pripremu spoja formule (1) naznačen time što sadrži (a) reakciju 5-[6-kloro-piridazin-3-ilmetil]-2-(2-fluoro-fenil)-5H-imidazo[4,5-c]piridina sa 2,4-bis(triflurometil)fenil organobornom kiselinom u prisustvu otapala koje ima strukturu R1OR2O(R4O)aR3, pri čemu su svako R1, R2, R3 i R4 nezavisno izabran od C1-C6 alkila i a je 0 ili 1, i (b) dobijanje spoja (1). Patent sadrži još 23 patentna zahtjeva.

Claims (24)

1. Postupak za pripremu spoja formule (1) [image] naznačen time što sadrži (a) reakciju 5-[6-kloro-piridazin-3-ilmetil]-2-(2-fluoro-fenil)-5H-imidazo[4,5-c]piridina sa 2,4-bis(triflurometil)fenil organobornom kiselinom u prisustvu otapala koje ima strukturu R1OR2O(R4O)aR3, pri čemu su svako R1, R2, R3 i R4 nezavisno izabran od C1-C6 alkila i a je 0 ili 1, i (b) dobijanje spoja (1).
2. Postupak prema patentnom zahtjevu 1, naznačen time što je a jednako 0.
3. Postupak prema patentnom zahtjevu 2, naznačen time što je otapalo dimetoksietan.
4. Postupak prema patentnom zahtjevu 1, naznačen time što je a jednako 1.
5. Spoj naznačen time što ima formulu (1) [image] i njegove soli i otopine.
6. Spoj prema patentnom zahtjevu 5, naznačen time što je u obliku slobodne baze.
7. Spoj prema patentnom zahtjevu 5, naznačen time što je u obliku otopine.
8. Spoj prema patentnom zahtjevu 5, naznačen time što je u obliku suspenzije.
9. Spoj prema patentnom zahtjevu 5, naznačen time što je u obliku suspenzije u vodenom mediju.
10. Spoj prema patentnom zahtjevu 5, naznačen time što je u obliku otopine.
11. Spoj prema patentnom zahtjevu 10, naznačen time što je u otopini sa C6-C18 masnom kiselinom.
12. Spoj prema patentnom zahtjevu 11, naznačen time što je masna kiselina oleinska kiselina ili laurinska kiselina.
13. Kompozicija, naznačena time što sadrži spoj prema patentnom zahtjevu 5 i farmaceutski prihvatljiv nosač.
14. Kompozicija prema patentnom zahtjevu 13, naznačena time što je inertni punitelj C6-C18 masna kiselina.
15. Kompozicija prema patentnom zahtjevu 14, naznačena time što je to vodena otopina i masna kiselina je oleinska kiselina.
16. Spoj prema patentnom zahtjevu 5, naznačen time što je namijenjen za primjenu kao lijek.
17. Spoj prema patentnom zahtjevu 5, naznačen time što je namijenjen za primjenu u postupku za prevenciju ili liječenje HCV infekcije kod sisavaca.
18. Spoj prema patentnom zahtjevu 17, naznačen time što je sisavac čovjek.
19. Spoj prema patentnom zahtjevu 17 ili 18, naznačen time što je za primjenu u kombinaciji sa terapeutski efikasnom dozom drugog sredstva za liječenje ili prevenciju HCV infekcije.
20. Spoj prema patentnom zahtjevu 19, naznačen time što je sredstvo interferon.
21. Spoj prema patentnom zahtjevu 19 ili 20, naznačen time što je terapeutski efikasna doza od 0.5-5.0 mg/kg dva puta na dan.
22. Spoj prema patentnom zahtjevu 20, naznačen time što je doza od 0.7-2.2 mg/kg dva puta na dan.
23. Postupak za pripremu spoja (1), naznačen time što sadrži osiguranje intermedijera (2) [image] spajanje 2,4-bis(trifluorometil)fenil organoborne kiseline za 3-kloro-6-metilpiridazin da bi se proizveo spoj (2a) [image] tretman spoja (2a) sa sredstvom za kloriranje da bi se proizvelo alkilirajuće sredstvo (3) [image] i primjenu alkilirajućeg sredstva (3) za alkilaciju intermedijera (2) pod baznim uvjetima da bi se proizveo spoj (1) [image]
24. Spoj formule (3) [image] i njegovi analozi, naznačeni time što su supstituirani sa metilom prije nego sa klorometil, i bromo, fluro ili jodo umjesto kloro.
HR20100180T 2006-07-07 2010-03-29 Novi spoj piridazina i njegova primjena HRP20100180T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US81928906P 2006-07-07 2006-07-07
US83240306P 2006-07-21 2006-07-21
US83276906P 2006-07-24 2006-07-24
PCT/US2007/015553 WO2008005519A2 (en) 2006-07-07 2007-07-06 Novel pyridazine compound and use thereof

Publications (1)

Publication Number Publication Date
HRP20100180T1 true HRP20100180T1 (hr) 2010-06-30

Family

ID=38814329

Family Applications (2)

Application Number Title Priority Date Filing Date
HR20090078A HRP20090078A2 (hr) 2006-07-07 2009-02-06 Novi piridazinski spojevi i njihova upotreba
HR20100180T HRP20100180T1 (hr) 2006-07-07 2010-03-29 Novi spoj piridazina i njegova primjena

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HR20090078A HRP20090078A2 (hr) 2006-07-07 2009-02-06 Novi piridazinski spojevi i njihova upotreba

Country Status (28)

Country Link
US (3) US7754720B2 (hr)
EP (1) EP2038275B1 (hr)
JP (1) JP4958974B2 (hr)
KR (1) KR101143596B1 (hr)
CN (1) CN102617571B (hr)
AP (1) AP3430A (hr)
AR (1) AR061969A1 (hr)
AT (1) ATE454384T1 (hr)
AU (1) AU2007269614B2 (hr)
CA (1) CA2656415C (hr)
CY (1) CY1112107T1 (hr)
DE (1) DE602007004220D1 (hr)
DK (1) DK2038275T3 (hr)
EA (1) EA019452B1 (hr)
ES (1) ES2339298T3 (hr)
HK (1) HK1123803A1 (hr)
HR (2) HRP20090078A2 (hr)
IL (1) IL195528A (hr)
MX (1) MX2009000235A (hr)
NO (1) NO20090595L (hr)
NZ (1) NZ574312A (hr)
PL (1) PL2038275T3 (hr)
PT (1) PT2038275E (hr)
RS (1) RS51336B (hr)
SG (1) SG175604A1 (hr)
SI (1) SI2038275T1 (hr)
TW (1) TWI360549B (hr)
WO (1) WO2008005519A2 (hr)

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NO20090595L (no) 2009-04-07
AP3430A (en) 2015-09-30
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RS51336B (en) 2011-02-28
CY1112107T1 (el) 2015-11-04
US20100152444A1 (en) 2010-06-17
JP2009542692A (ja) 2009-12-03
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AP2008004717A0 (en) 2008-12-31
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US20100063059A1 (en) 2010-03-11
EA019452B1 (ru) 2014-03-31
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