HRP20190808T1 - Spiro-indolini za liječenje i profilaksu infekcije respiratornim sincicijskim virusom (rsv) - Google Patents

Spiro-indolini za liječenje i profilaksu infekcije respiratornim sincicijskim virusom (rsv) Download PDF

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Publication number
HRP20190808T1
HRP20190808T1 HRP20190808TT HRP20190808T HRP20190808T1 HR P20190808 T1 HRP20190808 T1 HR P20190808T1 HR P20190808T T HRP20190808T T HR P20190808TT HR P20190808 T HRP20190808 T HR P20190808T HR P20190808 T1 HRP20190808 T1 HR P20190808T1
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Croatia
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compound
membered
substituted
unsubstituted
atom
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HRP20190808TT
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Stuart Cockerill
Neil Mathews
Simon Ward
Graham Lunn
Michael PARADOWSKI
Jose Miguel Gascon Simorte
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ReViral Limited
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=51946966&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20190808(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by ReViral Limited filed Critical ReViral Limited
Publication of HRP20190808T1 publication Critical patent/HRP20190808T1/hr

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    • 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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 the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • 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
    • 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
    • C07D403/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems

Claims (15)

1. Spoj koji je benzimidazol formule (I): naznačen time, što: - jedan od X i Y je N atom ili supstituirani C atom, a drugi je CH; - L je jednostruka veza ili C1-3 alkilen; - R1 je C1-6 alkil, C2-6 alkenil, C2-6 alkinil, 3-člani do 10-člani cikloalkil, 5-člani do 10-člani heterociklil ili 5-člani do 12-člani heteroaril, a svaki je nesupstituiran ili supstituiran; - Z je -N(R2)2; - svaki R2 je zasebno vodik, C1-6 alkil, C2-6 alkenil ili C2-6 alkinil, pri čemu su spomenute alkenilne i alkinilne grupe nesupstituirane ili supstituirane; i - m je 1; ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema patentnom zahtjevu 1, naznačen time, što je jedan od X i Y N atom ili C atom supstituiran atomom halogena, a drugi je CH.
3. Spoj prema patentnom zahtjevu 1, naznačen time, što je L jednostruka veza ili C1 alkilen.
4. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time, što je R1 C3-6 alkil, C3-6 alkenil, 5-člani ili 6-člani cikloalkil, 5-člani ili 6-člani heterociklil ili 5-člani ili 6-člani heteroaril, a svaki je nesupstituiran ili supstituiran.
5. Spoj prema patentnom zahtjevu 4, naznačen time, što je R1 C5-6 alkil koji je nesupstituiran ili supstituiran s jednim, dva, tri ili četiri atoma halogena, R1 je 6-člani cikloalkil supstituiran s jednom, dvije, tri ili četiri -OH grupe ili R1 je nesupstituirani 6-člani heterociklil.
6. Spoj prema patentnom zahtjevu 1, naznačen time, što je Z NH2.
7. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, što je svaki R2 zasebno vodik ili C1-4 alkil.
8. Spoj prema patentnom zahtjevu 1, naznačen time, što u formuli (I): - jedan od X i Y je N atom ili C supstituiran atomom fluora, a drugi je CH; - R1 je C5-6 alkil, koji je nesupstituiran ili supstituiran s jednim, dva, tri ili četiri atoma fluora, R1 je cikloheksil koji je nesupstituiran ili supstituiran s jednom ili dvije -OH grupe ili R1 je nesupstituirani tetrahidropiran; - m je 1 - L je jednostruka veza ili C1 alkilen; i - Z je NH2.
9. Spoj prema patentnom zahtjevu 1 koji je odabran iz: - 1’-{[5-(aminometil)-1-(4,4,4-trifluorobutil)-1H-1,3-benzodiazol-2-il]metil}-6’-fluoro-1’,2’-dihidrospiro[ciklopropan-1,3’-indol]-2’-ona; - 1’-((5-(aminometil)-1-(4,4,4-trifluorobutil)-1H-benzo[d]imidazol-2-il)metil)spiro[ciklopropan-1,3’-pirolo[2,3-b]piridin]-2’(1’H)-ona; - 1’-((5-(aminometil)-1-izopentil-1H-benzo[d]imidazol-2-il)metil)spiro[ciklopropan-1,3’-pirolo[2,3-b]piridin]-2’(1’H)-ona; - 1’-((5-(aminometil)-1-izopentil-1H-benzo[d]imidazol-2-il)metil)spiro[ciklopropan-1,3’-pirolo[2,3-c]piridin]-2’(1’H)-ona; i - 1’-((5-(aminometil)-1-(tetrahidro-2H-piran-4-yl)-1H-benzo[d]imidazol-2-il)metil)-6’-fluorospiro[ciklopropan-1,3’-indolin]-2’-ona; - 1’-((5-(aminometil)-1-((1R,4R)-4-hidroksicikloheksil)-1H-benzo[d]imidazol-2-il)metil)-6’-fluorospiro[ciklopropan-1,3’-indolin]-2’-ona i njihovih farmaceutski prihvatljivih soli.
10. Farmaceutski pripravak koji sadrži spoj kako je definirano prema bilo kojem patentnom zahtjevu od 1 do 9 i farmaceutski prihvatljivi nosač ili otapalo.
11. Spoj kako je definirano prema bilo kojem patentnom zahtjevu od 1 do 9, za primjenu u liječenju čovjeka ili životinje pomoću terapije.
12. Spoj kako je definirano prema bilo kojem patentnom zahtjevu od 1 do 9 za primjenu u liječenju ili sprječavanju infekcije RSV-om.
13. Proizvod koji sadrži: (a) spoj kako je definirano prema bilo kojem patentnom zahtjevu od 1 do 9; i (b) jedno ili više dodatnih terapijskih sredstava; za istovremenu, odvojenu ili sekvencijalnu primjenu u liječenju subjekta koji pati od ili je podložan infekciji RSV-om.
14. Proizvod za primjenu prema patentnom zahtjevu 13, naznačen time, što je dodatno terapijsko sredstvo: (i) inhibitor proteina nukleokapsida(N) RSV-a; (ii) drugi inhibitor proteina, primjerice neki koji inhibira fosfoprotein (P) i/ili veliki (L) protein; (iii) anti-RSV monoklonalno antitijelo, kao što je antitijelo na F-protein; (iv) spoj imunomodulirajućeg toličnog receptora; (v) drugi resipratorni, protuvirusni spoj, kao što je spoj protiv gripe i/ili rinovirusa; i/ili (vi) protuupalni spoj.
15. Farmaceutski pripravak koji sadrži (a) spoj kako je definirano prema bilo kojem patentnom zahtjevu od 1 do 9 i (b) jedno ili više dodatnih terapijskih sredstava, kako je definirano u patentnom zahtjevu 14, zajedno s farmaceutski prihvatljivim nosačem ili otapalom.
HRP20190808TT 2014-10-07 2019-04-30 Spiro-indolini za liječenje i profilaksu infekcije respiratornim sincicijskim virusom (rsv) HRP20190808T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1417707.5A GB201417707D0 (en) 2014-10-07 2014-10-07 Pharmaceutical compounds
PCT/GB2015/052920 WO2016055780A1 (en) 2014-10-07 2015-10-06 Spiro-indolines for the treatment and prophylaxis of respiratory syncytial virus infection (rsv)
EP15782033.3A EP3204375B1 (en) 2014-10-07 2015-10-06 Spiro-indolines for the treatment and prophylaxis of respiratory syncytial virus infection (rsv)

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HRP20190808T1 true HRP20190808T1 (hr) 2019-08-23

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HRP20190808TT HRP20190808T1 (hr) 2014-10-07 2019-04-30 Spiro-indolini za liječenje i profilaksu infekcije respiratornim sincicijskim virusom (rsv)

Country Status (30)

Country Link
US (1) US10106539B2 (hr)
EP (1) EP3204375B1 (hr)
JP (1) JP6695334B2 (hr)
KR (2) KR102561796B1 (hr)
CN (1) CN107108557B (hr)
AR (1) AR102181A1 (hr)
AU (1) AU2015329778B2 (hr)
BR (1) BR112017007311B1 (hr)
CA (1) CA2963740C (hr)
CL (1) CL2017000839A1 (hr)
CO (1) CO2017004603A2 (hr)
CY (1) CY1121564T1 (hr)
DK (1) DK3204375T3 (hr)
ES (1) ES2718976T3 (hr)
GB (1) GB201417707D0 (hr)
HR (1) HRP20190808T1 (hr)
HU (1) HUE043553T2 (hr)
LT (1) LT3204375T (hr)
MX (1) MX2017004425A (hr)
NZ (1) NZ731323A (hr)
PE (1) PE20170949A1 (hr)
PL (1) PL3204375T3 (hr)
PT (1) PT3204375T (hr)
RS (1) RS58706B1 (hr)
RU (1) RU2734248C2 (hr)
SG (1) SG11201702766YA (hr)
SI (1) SI3204375T1 (hr)
TR (1) TR201903362T4 (hr)
TW (1) TWI718107B (hr)
WO (1) WO2016055780A1 (hr)

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TR201903362T4 (tr) 2019-04-22
KR102561796B1 (ko) 2023-07-31
CL2017000839A1 (es) 2017-10-13
NZ731323A (en) 2022-09-30
JP2017530992A (ja) 2017-10-19
SG11201702766YA (en) 2017-05-30
RU2017113026A3 (hr) 2019-03-22
PL3204375T3 (pl) 2019-06-28
TW201625583A (zh) 2016-07-16
EP3204375A1 (en) 2017-08-16
ES2718976T3 (es) 2019-07-05
WO2016055780A1 (en) 2016-04-14
AU2015329778A1 (en) 2017-05-04
US10106539B2 (en) 2018-10-23
HUE043553T2 (hu) 2019-09-30
CA2963740A1 (en) 2016-04-14
AR102181A1 (es) 2017-02-08
AU2015329778B2 (en) 2020-04-23
RU2017113026A (ru) 2018-11-13
TWI718107B (zh) 2021-02-11
CN107108557A (zh) 2017-08-29
JP6695334B2 (ja) 2020-05-20
SI3204375T1 (sl) 2019-05-31
MX2017004425A (es) 2017-10-11
RS58706B1 (sr) 2019-06-28
DK3204375T3 (en) 2019-04-01
LT3204375T (lt) 2019-05-10
US20170305908A1 (en) 2017-10-26
CY1121564T1 (el) 2020-05-29
CA2963740C (en) 2022-11-29
AU2015329778A8 (en) 2017-05-18
GB201417707D0 (en) 2014-11-19
PE20170949A1 (es) 2017-07-13
CN107108557B (zh) 2020-11-10
KR20230116097A (ko) 2023-08-03
EP3204375B1 (en) 2019-02-13
BR112017007311A2 (pt) 2017-12-19
PT3204375T (pt) 2019-04-01
KR20170066577A (ko) 2017-06-14
BR112017007311B1 (pt) 2022-11-22
CO2017004603A2 (es) 2017-10-31
RU2734248C2 (ru) 2020-10-13

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