HRP20170773T1 - Novi anti-malarijski agensi - Google Patents

Novi anti-malarijski agensi Download PDF

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Publication number
HRP20170773T1
HRP20170773T1 HRP20170773TT HRP20170773T HRP20170773T1 HR P20170773 T1 HRP20170773 T1 HR P20170773T1 HR P20170773T T HRP20170773T T HR P20170773TT HR P20170773 T HRP20170773 T HR P20170773T HR P20170773 T1 HRP20170773 T1 HR P20170773T1
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HR
Croatia
Prior art keywords
pyrazole derivative
fluorophenyl
methyl
pyrazol
image
Prior art date
Application number
HRP20170773TT
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English (en)
Inventor
Jeremy Burrows
Matthew Wyvratt
Akhil VAIDYA
Sandhya Kortagere
Erkang FAN
Arnab Kumar CHATTERJEE
Advait Suresh NAGLE
Tomoyo KATO
Original Assignee
Mmv Medicines For Malaria Venture
Drexel University
University Of Washington
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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Publication date
Application filed by Mmv Medicines For Malaria Venture, Drexel University, University Of Washington filed Critical Mmv Medicines For Malaria Venture
Publication of HRP20170773T1 publication Critical patent/HRP20170773T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D231/38Nitrogen atoms
    • C07D231/40Acylated on said 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (14)

1. Derivat pirazola u skladu sa Formulom (I), [image] naznačen time što je X1 odabran od F i H; X2 je odabran od Cl i F; R1 je odabran od metila i trifluorometila; R2 je odabran od sljedećih grupa: [image] [image] kao i njegova farmaceutski prihvatljiva sol, hidrat, solvat, polimorf, tautomeri, geometrijski izomeri, ili optički aktivni izomeri.
2. Derivat pirazola prema zahtjevu 1, naznačen time što je R2: [image]
3. Derivat pirazola prema zahtjevu 1, naznačen time što je R2: [image]
4. Derivat pirazola prema zahtjevu 1 ili 2 odabran iz sljedeće grupe: N-(4-(4-kloro-2-fluorofenil)-3-(trifluorometil)-1-metil-1H-pirazol-5-il)-2-(2-izopropil-1H-benzo[d]imidazol-1-il)acetamid; N-(4-(4-kloro-2-fluorofenil)-1,3-dimetil-1H-pirazol-5-il)-2-(2-izopropil-1H-benzo[d]imidazol-1-il)acetamid; (R)-3-amino-N-(3-(trifluorometil)-4-(4-fluorofenil)-1-metil-1H-pirazol-5-il)-4-(4-fluorofenil) butanamid; i (R)-3-amino-4-(4-fluorofenil)-N-(4-(4-fluorofenil)-1,3-dimetil-1H-pirazol-5-il)butanamid; kao i bilo koja farmaceutski prihvatljiva sol, hidrat, solvat, polimorf, tautomeri, geometrijski izomeri ili njihovi optički aktivni oblici.
5. Derivat pirazola prema bilo kojem od zahtjeva od 1 do 4, za upotrebu kao lijek.
6. Farmaceutski sastav koji sadrži najmanje jedan derivat pirazola prema bilo kojem od zahtjeva od 1 do 4 ili njegovu farmaceutski prihvatljivu sol i farmaceutski prihvatljiv nosač, diluent ili ekscipijens.
7. Farmaceutski sastav prema zahtjevu 6 koji sadrži i antimalarijski ko-agens.
8. Farmaceutski sastav prema zahtjevu 7 u kojem je ko-agens odabran od artemisinina ili derivata artemisinina, klorokvina, kinina, meflohina, amodijahina, atovakvon/proguanila, doksiciklina, lumefantrina, piperakvina, pironaridina, halofantrina, pirimetamin-sulfadoksina, primakvina, kvinakrina, doksiciklina, atovakona, proguanil hidroklorida, piperakvina, ferokvina, tafenokvina, arterolana, Spiro[3H-indol-3,1'-[1H]pirido[3,4-b]indol]-2(1H)-ona (CAS Reg Br: 1193314-23-6), 5,7'-dikloro-6'-fluoro-2',3',4',9'-tetrahidro-3'-metil-, (1'R,3'S)-], Sumpora, [4-[[2-(1,1-difluoretil)-5-metil[1,2,4]triazolo[1,5-a]pirimidin-7-il]amino]fenil]pentafluoro-] (CAS Reg. Br: 1282041-94-4), Morfolina, i 4-[2-(4-cis-dispiro[cikloheksan-1,3'-[1,2,4]trioksolan-5'2"-triciklo [3.3.1.13,7]dekan]-4-ilfenoksi)etil]-] (CAS Reg. Br.: 1029939-86-3).
9. Farmaceutski sastav prema zahtjevu 7, u kojem je derivat artemisinina artemeter ili dihidroartemisinin.
10. Derivat pirazola prema bilo kojem od zahtjeva od 1 do 4 za upotrebu u prevenciji ili liječenju malarije.
11. Derivat pirazola za upotrebu prema zahtjevu 10 pri čemu derivat pirazola treba da bude administriran u kombinaciji sa ko-agensom korisnim u liječenju malarije.
12. Derivat pirazola za upotrebu prema zahtjevu 10 ili 11, naznačen time što je derivat pirazola prema zahtjevu 4.
13. Derivat pirazola za upotrebu prema zahtjevu 10 ili 11, naznačen time što je derivat pirazola N-(4-(4 kloro-2-fluorofenil)-3-(trifluorometil)-1-metil-1H-pirazol-5-il)-2-(2-izopropil-1H-benzo[d]imidazol -1-il)acetamid.
14. Postupak ex vivo za inaktivaciju parazitske infekcije u stanici koji obuhvaća korak dovođenja u kontakt ex vivo stanice sa efikasnom količinom najmanje jednog spoja prema bilo kojem od zahtjeva 1 do 4.
HRP20170773TT 2013-07-17 2017-05-23 Novi anti-malarijski agensi HRP20170773T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361847185P 2013-07-17 2013-07-17
EP14759317.2A EP3022200B1 (en) 2013-07-17 2014-07-17 New anti-malarial agents
PCT/IB2014/063180 WO2015008246A1 (en) 2013-07-17 2014-07-17 New anti-malarial agents

Publications (1)

Publication Number Publication Date
HRP20170773T1 true HRP20170773T1 (hr) 2017-08-11

Family

ID=51492402

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20170773TT HRP20170773T1 (hr) 2013-07-17 2017-05-23 Novi anti-malarijski agensi

Country Status (17)

Country Link
US (1) US9464057B2 (hr)
EP (1) EP3022200B1 (hr)
JP (1) JP2016527228A (hr)
CN (1) CN105377838A (hr)
CA (1) CA2918290A1 (hr)
CY (1) CY1118913T1 (hr)
ES (1) ES2625160T3 (hr)
HK (1) HK1219728A1 (hr)
HR (1) HRP20170773T1 (hr)
HU (1) HUE033124T2 (hr)
LT (1) LT3022200T (hr)
ME (1) ME02724B (hr)
PL (1) PL3022200T3 (hr)
PT (1) PT3022200T (hr)
RS (1) RS55998B1 (hr)
SI (1) SI3022200T1 (hr)
WO (1) WO2015008246A1 (hr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107149604A (zh) * 2017-03-17 2017-09-12 高雪亚 一种治疗非酒精性脂肪肝的药物组合物
PL233259B1 (pl) * 2017-07-10 2019-09-30 Politechnika Poznanska Indolilooctany 1-alkilochininy, sposób ich otrzymywania oraz zastosowanie jako środki bakteriostatyczne i bakteriobójcze
EP3710492B1 (en) 2017-11-13 2021-08-11 INEOS Styrolution Group GmbH Thermoplastic molding composition and articles made thereof having improved surface quality

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009065096A1 (en) 2007-11-16 2009-05-22 University Of Medicine And Dentistry Of New Jersey Mechanism-based small-molecule parasite inhibitors

Also Published As

Publication number Publication date
EP3022200A1 (en) 2016-05-25
SI3022200T1 (sl) 2017-06-30
CA2918290A1 (en) 2015-01-22
ME02724B (me) 2017-10-20
PT3022200T (pt) 2017-06-12
WO2015008246A1 (en) 2015-01-22
CN105377838A (zh) 2016-03-02
US20160194286A1 (en) 2016-07-07
PL3022200T3 (pl) 2017-08-31
ES2625160T3 (es) 2017-07-18
EP3022200B1 (en) 2017-03-01
HUE033124T2 (en) 2017-11-28
LT3022200T (lt) 2017-06-12
CY1118913T1 (el) 2018-01-10
HK1219728A1 (zh) 2017-04-13
US9464057B2 (en) 2016-10-11
RS55998B1 (sr) 2017-09-29
JP2016527228A (ja) 2016-09-08

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