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HRP20220263T1 - Fenil-2-hidroksi-acetilamino-2-metil-fenil spojevi - Google Patents

Fenil-2-hidroksi-acetilamino-2-metil-fenil spojevi Download PDF

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Publication number
HRP20220263T1
HRP20220263T1 HRP20220263TT HRP20220263T HRP20220263T1 HR P20220263 T1 HRP20220263 T1 HR P20220263T1 HR P20220263T T HRP20220263T T HR P20220263TT HR P20220263 T HRP20220263 T HR P20220263T HR P20220263 T1 HRP20220263 T1 HR P20220263T1
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HR
Croatia
Prior art keywords
compound
image
pharmaceutically acceptable
phenyl
methyl
Prior art date
Application number
HRP20220263TT
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English (en)
Inventor
Marta Maria CIFUENTES-GARCIA
Maria Cristina GARCIA-PAREDES
Original Assignee
Eli Lilly And Company
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Publication date
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Publication of HRP20220263T1 publication Critical patent/HRP20220263T1/hr

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    • 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
    • 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
    • A61K31/4418Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • A61K31/4965Non-condensed pyrazines
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C07D241/28Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)

Claims (11)

1. Spoj formule [image] naznačen time što R je odabran iz grupe koja se sastoji od [image] X je CH ili N; R1 je vodik ili fluoro; i R2 je C1 do C3 alkil; ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema patentnom zahtjevu 1, formule [image] naznačen time što R je odabran iz grupe koja se sastoji od [image] X je CH ili N; R1 je vodik ili fluoro; i R2 je C1 do C3 alkil; ili njegova farmaceutski prihvatljiva sol.
3. Spoj ili sol prema bilo kojem od patentnih zahtjeva 1 ili 2 naznačen time što, R je [image]
4. Spoj ili sol prema bilo kojem od patentnih zahtjeva 1 ili 2 naznačen time što, X je CH ili N; R1 is vodik ili fluoro; i R2 je metil ili izopropil.
5. Spoj ili sol prema bilo kojem od patentnih zahtjeva 1 ili 2 naznačen time što, R je [image]
6. Spoj prema bilo kojem od patentnih zahtjeva 1 ili 2 koji je 3-amino-6-[4-[[(2R)-2-(3,5-difluorofenil)-2-hidroksi-acetil]amino]-2-metil-fenil]-N-metilpirazin-2-karboksamid, koji je predstavljen formulom [image] ili njegova farmaceutski prihvatljiva sol.
7. Spoj prema bilo kojem od patentnih zahtjeva 1 ili 2 koji je 2-amino-5-[4-[[(2R)-2-(3,5-difluorofenil)-2-hidroksi-acetil]amino]-2-metil-fenil]-N-izopropil-piridin-3-karboksamid, koji je predstavljen formulom [image] ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema bilo kojem od patentnih zahtjeva 1 ili 2 koji je (2R)-N-[4-(4-amino-7-metil-pirolo[2,3-d]pirimidin-5-il)-3-metil-fenil]-2-(3-fluorofenil)-2-hidroksi-acetamid, koji je predstavljen formulom [image] ili njegova farmaceutski prihvatljiva sol.
9. Farmaceutska kompozicija koja sadrži spoj ili njegovu farmaceutski prihvatljivu sol prema bilo kojem od patentnih zahtjeva 1-8, sa jednim ili više farmaceutski prihvatljivih nosača, razblaživača ili ekscipijenasa.
10. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1-8, za uporabu u terapiji.
11. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1-8, za uporabu u liječenju raka gušterače.
HRP20220263TT 2017-04-18 2018-04-11 Fenil-2-hidroksi-acetilamino-2-metil-fenil spojevi HRP20220263T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP17382207 2017-04-18
EP18718570.7A EP3612519B1 (en) 2017-04-18 2018-04-11 Phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds
PCT/US2018/027005 WO2018194885A1 (en) 2017-04-18 2018-04-11 Phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds

Publications (1)

Publication Number Publication Date
HRP20220263T1 true HRP20220263T1 (hr) 2022-04-29

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Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20220263TT HRP20220263T1 (hr) 2017-04-18 2018-04-11 Fenil-2-hidroksi-acetilamino-2-metil-fenil spojevi

Country Status (28)

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US (2) US11655214B2 (hr)
EP (2) EP4039675B1 (hr)
JP (2) JP7110232B2 (hr)
KR (2) KR20230129627A (hr)
CN (2) CN110831927B (hr)
AU (2) AU2018255191B2 (hr)
BR (1) BR112019021867A2 (hr)
CA (1) CA3060564A1 (hr)
CO (1) CO2019012767A2 (hr)
CR (1) CR20190519A (hr)
CY (1) CY1125150T1 (hr)
DK (2) DK4039675T3 (hr)
ES (1) ES2906847T3 (hr)
FI (1) FI4039675T3 (hr)
HR (1) HRP20220263T1 (hr)
HU (1) HUE057745T2 (hr)
IL (2) IL270005B (hr)
LT (2) LT4039675T (hr)
MX (2) MX2019012428A (hr)
PH (1) PH12019502363A1 (hr)
PL (1) PL3612519T3 (hr)
PT (2) PT3612519T (hr)
RS (2) RS62933B1 (hr)
SA (1) SA519410320B1 (hr)
SG (1) SG11201909680UA (hr)
SI (2) SI4039675T1 (hr)
WO (1) WO2018194885A1 (hr)
ZA (1) ZA201906811B (hr)

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Publication number Publication date
AU2018255191B2 (en) 2022-04-21
CN117510405A (zh) 2024-02-06
KR102575246B1 (ko) 2023-09-06
FI4039675T3 (fi) 2024-09-10
RS62933B1 (sr) 2022-03-31
KR20190140966A (ko) 2019-12-20
JP2021517555A (ja) 2021-07-26
SA519410320B1 (ar) 2022-05-08
CR20190519A (es) 2020-03-06
EP3612519B1 (en) 2021-12-01
AU2018255191A1 (en) 2019-11-07
HUE057745T2 (hu) 2022-06-28
EP4039675A1 (en) 2022-08-10
ES2906847T3 (es) 2022-04-20
ZA201906811B (en) 2021-01-27
MX2019012428A (es) 2022-01-28
LT3612519T (lt) 2022-03-25
RS65914B1 (sr) 2024-10-31
IL288822B2 (en) 2023-06-01
EP3612519A1 (en) 2020-02-26
PL3612519T3 (pl) 2022-05-02
JP2022141835A (ja) 2022-09-29
PT4039675T (pt) 2024-09-16
CA3060564A1 (en) 2018-10-25
PT3612519T (pt) 2022-02-22
BR112019021867A2 (pt) 2020-05-26
US11655214B2 (en) 2023-05-23
DK3612519T3 (da) 2022-03-07
CN110831927B (zh) 2023-07-14
CO2019012767A2 (es) 2020-04-01
SI3612519T1 (sl) 2022-04-29
IL288822A (en) 2022-02-01
DK4039675T3 (da) 2024-09-02
JP7331212B2 (ja) 2023-08-22
US20210114985A1 (en) 2021-04-22
MX2022001310A (es) 2022-03-02
JP7110232B2 (ja) 2022-08-01
SI4039675T1 (sl) 2024-10-30
AU2022206702A1 (en) 2022-08-11
AU2022206702B2 (en) 2024-04-11
CN110831927A (zh) 2020-02-21
WO2018194885A1 (en) 2018-10-25
LT4039675T (lt) 2024-10-10
CY1125150T1 (el) 2023-06-09
PH12019502363A1 (en) 2020-12-07
EP4039675B1 (en) 2024-06-12
SG11201909680UA (en) 2019-11-28
RU2019136694A3 (hr) 2021-05-19
IL270005B (en) 2022-01-01
KR20230129627A (ko) 2023-09-08
US20230373922A1 (en) 2023-11-23
RU2019136694A (ru) 2021-05-18

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