HRP20140671T1 - Derivati tioksantena za lijeäśenje infektivnih bolesti - Google Patents

Derivati tioksantena za lijeäśenje infektivnih bolesti Download PDF

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Publication number
HRP20140671T1
HRP20140671T1 HRP20140671AT HRP20140671T HRP20140671T1 HR P20140671 T1 HRP20140671 T1 HR P20140671T1 HR P20140671A T HRP20140671A T HR P20140671AT HR P20140671 T HRP20140671 T HR P20140671T HR P20140671 T1 HRP20140671 T1 HR P20140671T1
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Croatia
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alkyl
amino
mono
substance according
group
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HRP20140671AT
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English (en)
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Birgit Kjalgaard Giwercman
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Bkg Pharma Aps
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Publication of HRP20140671T1 publication Critical patent/HRP20140671T1/hr

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    • 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
    • C07D409/06Heterocyclic 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 carbon chain containing only aliphatic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial 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
    • C07D335/00Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/04Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D335/10Dibenzothiopyrans; Hydrogenated dibenzothiopyrans
    • C07D335/12Thioxanthenes
    • C07D335/20Thioxanthenes with hydrocarbon radicals, substituted by amino radicals, directly attached in position 9

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (14)

1. Tvar opće formule (I) [image] pri čemu V je odabran iz grupe koja se sastoji od S, SO2, SO, O i NH; W je C=CH-(CHX)n-CX(Rg)(R10) ili je W C=CH-(CHX)n-1-CH=(Rg)(R10); n je cijeli broj u rasponu od 1 do 5; svaki X je zasebno odabran iz grupe koja se sastoji od vodika, halogena, hidroksi, amino, nitro, C1-6-alkil i C1-6-alkoksi; R1, R3, R4, R5, R6, R7 i R8 su svaki zasebno odabrani iz grupe koja se sastoji od vodika, halogena, hidroksi, amino, nitro, C1-6-alkil, C2-6-alkenil, C2-6-alkinil i C1-6-alkoksi, C2-6-alkeniloksi, karboksi, i C1-6-alkoksikarbonil, i C1-6-alkilkarbonil, formil, i C1-6-alkilsulfonilamino, aril, ariloksikarbonil, ariloksi, arilkarbonil, arilamino, arilsulfonilamino, heteroaril, heteroariloksikarbonil, heteroariloksi, heteroarilkarbonil, heteroarilamino, heteroarilsulfonilamino, heterociklil, heterocikloksikarbonil, heterocikliloksi, heterociklilkarbonil, heterociklilamino, heterociklilsulfonilamino, mono- i di(C1-6-alkil)amino, karbamoil, mono- i di(C1-6-alkil)aminokarbonil, amino- C1-6-alkil-aminokarbonil, mono- i di(C1-6-alkil)amino- C1-6-alkil-aminokarbonil, C1-6-alkilkarbonilamnio, amino- C1-6-alkil-karbonilamino, mono- i di(C1-6-alkil)amino- C1-6-alkil-karbonilamino, amino- C1-6-alkil-amino, mono- i di(C1-6-alkil)amino- C1-6-alkil-amino, cijano, gvanidino, karbamido, C1-6-alkanoiloksi, C1-6-alkilsulfonil, C1-6-alkilsulfinil, C1-6-alkilsulfoniloksi, aminosulfonil, mono- i di(C1-6-alkil)aminosulfonil i C1-6-alkiltio; R2 je odabran iz grupe koja se sastoji od F, Cl, Br, I, CH2Y, CHY2 i CY3, gdje je Y atom halogena; i R9 i R10 zajedno s atomom ugljika za koji su povezani tvore C3-6-cikloalkil ili C3-6-heterociklil, poželjno heterociklil koji sadrži dušik; kao i njihove soli.
2. Tvar u skladu s patentnim zahtjevom 1 pri čemu je V S.
3. Tvar u skladu s bilo kojim od patentnih zahtjeva 1 ili 2, pri čemu je n 2, 3 ili 4.
4. Tvar u skladu s bilo kojim od patentnih zahtjeva 1-3, pri čemu R9 i R10 zajedno s atomom ugljika za kojeg su vezani tvore piperidinil ili piperazinil, poželjno piperidinil.
5. Tvar u skladu s bilo kojim od patentnih zahtjeva 1-4, pri čemu R9 i R10 zajedno s atomom ugljika za kojeg su vezani tvore heteroaril ili heterociklil koji sadrži dušik gdje je atom dušika odvojen dvjema atomima ugljika od atoma ugljika za koji su R9 i R10 vezani.
6. Tvar opće formule [image] pri čemu V je odabran iz grupe koja se sastoji od S, SO2, SO, O i NH; W' je C=CH; n je cijeli broj u rasponu od 1 do 6; svaki X je zasebno odabran iz grupe koja se sastoji od vodika, halogena, hidroksi, amino, nitro, C1-6-alkil i C1-6-alkoksi; Z je odabran između C, N, S ili O; R1, R3, R4, R5, R6, R7, R8 R11, R12, R14 i R15 su svaki zasebno odabrani iz grupe koja se sastoji od vodika, halogena, hidroksi, amino, nitro, C1-6-alkil, C2-6-alkenil, C2-6-alkinil i C1-6-alkoksi, C2-6-alkeniloksi, karboksi, i C1-6-alkoksikarbonil, i C1-6-alkilkarbonil, formil, i C1-6-alkilsulfonilamino, aril, ariloksikarbonil, ariloksi, arilkarbonil, arilamino, arilsulfonilamino, heteroaril, heteroariloksikarbonil, heteroariloksi, heteroarilkarbonil, heteroarilamino, heteroarilsulfonilamino, heterociklil, heterocikloksikarbonil, heterocikliloksi, heterociklilkarbonil, heterociklilamino, heterociklilsulfonilamino, mono- i di(C1-6-alkil)amino, karbamoil, mono- i di(C1-6-alkil)aminokarbonil, amino- C1-6-alkil-aminokarbonil, mono- i di(C1-6-alkil)amino- C1-6-alkil-aminokarbonil, C1-6-alkilkarbonilamnio, amino- C1-6-alkil-karbonilamino, mono- i di(C1-6-alkil)amino- C1-6-alkil-karbonilamino, amino- C1-6-alkil-amino, mono- i di(C1-6-alkil)amino- C1-6-alkil-amino, cijano, gvanidino, karbamido, C1-6-alkanoiloksi, C1-6-alkilsulfonil, C1-6-alkilsulfinil, C1-6-alkilsulfoniloksi, aminosulfonil, mono- i di(C1-6-alkil)aminosulfonil i C1-6-alkiltio; i R2 je odabran iz grupe koja se sastoji od F, Cl, Br, I, CH2Y, CHY2 i CY3, gdje je Y atom halogena; i R13 je vodik, halogen, hidroksi, amino, nitro, C1-6-alkil ili C1-6-alkoksi; ili njihove soli.
7. Tvar u skladu s bilo kojim od patentnih zahtjeva 1-6 za uporabu u tretmanu liječenja.
8. Tvar u skladu s bilo kojim od patentnih zahtjeva 1-7 za uporabu u liječenju infektivne bolesti.
9. Tvar u skladu s bilo kojim od patentnih zahtjeva 1-8 za uporabu u liječenju infektivne bolesti u kombinaciji s dodatnim antiinfektivnim agensom.
10. Tvar u skladu s bilo kojim od patentnih zahtjeva 1-9 gdje je infektivna bolest uzrokovana infektivnim agensom otpornim na lijekove.
11. Uporaba tvari definirane u bilo kojem od prethodnih patentnih zahtjeva 1-10 za proizvodnju lijeka za liječenje ili profilaksu infektivne bolesti.
12. Uporaba u skladu s patentnim zahtjevom 11, pri čemu je navedena tvar korištena ili dana u klinički značajnoj količini.
13. Farmaceutski sastav sadrži tvar u skladu s bilo kojim od patentnih zahtjeva 1-6 i najmanje jedan farmaceutski prihvatljivi nosač ili ekscipijens.
14. Farmaceutski sastav u skladu s patentnim zahtjevom 13, sadrži klinički značajnu količinu tvari u skladu s bilo kojim od patentnih zahtjeva 1-6.
HRP20140671AT 2009-04-20 2014-07-14 Derivati tioksantena za lijeäśenje infektivnih bolesti HRP20140671T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US20291809P 2009-04-20 2009-04-20
EP09158229A EP2246349A1 (en) 2009-04-20 2009-04-20 Treatment of infectious diseases
PCT/EP2010/055176 WO2010122012A1 (en) 2009-04-20 2010-04-20 Thioxanthene derivatives for the treatment of infectious diseases

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HRP20140671T1 true HRP20140671T1 (hr) 2014-10-10

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US (2) US8604059B2 (hr)
EP (3) EP2246349A1 (hr)
JP (2) JP5854987B2 (hr)
CN (1) CN102459245B (hr)
AU (1) AU2010240999B2 (hr)
CA (1) CA2759364A1 (hr)
DK (1) DK2421858T3 (hr)
EA (1) EA022060B1 (hr)
ES (1) ES2484016T3 (hr)
HK (1) HK1170733A1 (hr)
HR (1) HRP20140671T1 (hr)
MX (1) MX2011011062A (hr)
NZ (1) NZ596158A (hr)
PL (1) PL2421858T3 (hr)
SI (1) SI2421858T1 (hr)
WO (1) WO2010122012A1 (hr)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2009007235A (es) * 2007-01-05 2009-10-16 Bkg Pharma Aps "derivados de tioxanteno utiles para el tratamiento de enfermedades infecciosas.".
EP2246349A1 (en) * 2009-04-20 2010-11-03 BKG Pharma ApS Treatment of infectious diseases
RU2019101646A (ru) * 2016-06-23 2020-07-23 Биоимикс Аб Противоинфекционные гетероциклические соединения и варианты их применения
RU2738405C1 (ru) * 2020-05-26 2020-12-11 Федеральное государственное бюджетное образовательное учреждение высшего образования "Пермский государственный национальный исследовательский университет" АМИД (Е)-2-АМИНО-4-ОКСО-5-(2-ОКСО-2-ФЕНИЛЭТИЛИДЕН)-1-(3-ЭТОКСИКАРБОНИЛ)-4,5,6-7-ТЕТРАГИДРОБЕНЗО[b]ТИОФЕН-2-ИЛ)4,5-ДИГИДРО-1Н-ПИРРОЛ-3-КАРБОНОВОЙ КИСЛОТЫ, ОБЛАДАЮЩИЙ ПРОТИВОМИКРОБНОЙ АКТИВНОСТЬЮ

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CN102459245A (zh) 2012-05-16
EA022060B1 (ru) 2015-10-30
MX2011011062A (es) 2011-11-18
NZ596158A (en) 2013-02-22
US20120122880A1 (en) 2012-05-17
EP2778166A1 (en) 2014-09-17
PL2421858T3 (pl) 2014-10-31
EP2421858A1 (en) 2012-02-29
AU2010240999B2 (en) 2012-09-20
JP2012524118A (ja) 2012-10-11
DK2421858T3 (en) 2014-07-14
JP2014240401A (ja) 2014-12-25
US8604059B2 (en) 2013-12-10
US20140066451A1 (en) 2014-03-06
WO2010122012A1 (en) 2010-10-28
JP5854987B2 (ja) 2016-02-09
CA2759364A1 (en) 2010-10-28
ES2484016T3 (es) 2014-08-08
SI2421858T1 (sl) 2014-09-30
EP2421858B1 (en) 2014-04-30
CN102459245B (zh) 2015-01-28
HK1170733A1 (en) 2013-03-08
EP2246349A1 (en) 2010-11-03
EA201171269A1 (ru) 2012-03-30
AU2010240999A1 (en) 2011-11-10

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