HRP20211032T1 - Postupci za uporabu agonista fxr - Google Patents

Postupci za uporabu agonista fxr Download PDF

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Publication number
HRP20211032T1
HRP20211032T1 HRP20211032TT HRP20211032T HRP20211032T1 HR P20211032 T1 HRP20211032 T1 HR P20211032T1 HR P20211032T T HRP20211032T T HR P20211032TT HR P20211032 T HRP20211032 T HR P20211032T HR P20211032 T1 HRP20211032 T1 HR P20211032T1
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Croatia
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compound
use according
dose
liver disease
unit dosage
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HRP20211032TT
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English (en)
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Bryan Laffitte
Michael BADMAN
Jin Chen
Sam LINDGREN
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Novartis Ag
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Publication of HRP20211032T1 publication Critical patent/HRP20211032T1/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
    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/468-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4748Quinolines; Isoquinolines forming part of bridged ring 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
    • A61K31/495Heterocyclic 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
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542Carboxylic acids, e.g. a fatty acid or an amino acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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

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

Claims (14)

1. Spoj, naznačen time, što je predstavljen formulom (I) [image] stereoizomer, enantiomer, njegova farmaceutski prihvatljiva sol ili njegov aminokiselinski konjugat, i što je za uporabu u liječenju ili prevenciji kronične bolesti jetre ili poremećaja jetre, pri čemu se navedeni spoj daje u dozi u rasponu od oko 3 µg do oko 120 µg.
2. Spoj za uporabu prema patentnom zahtjevu 1, naznačen time, što se navedeni spoj daje u dozi u rasponu od oko 30 µg do oko 90 µg.
3. Spoj za uporabu prema patentnom zahtjevu 1, naznačen time, što se navedeni spoj daje u dozi u rasponu od oko 60 µg do oko 120 µg.
4. Spoj za uporabu u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time, što je kronična bolest jetre nealkoholna bolest masne jetre (NAFLD), nealkoholni steatohepatitis (NASH), ozljeda žučnog kanala izazvana supstancom, žučni kamenci, ciroza jetre, alkoholom izazvana ciroza, cistična fibroza, opstrukcija žučnih kanala, kolelitijaza ili fibroza jetre.
5. Spoj za uporabu prema patentnom zahtjevu 4, naznačen time, što je kronična bolest jetre nealkoholni steatohepatitis (NASH).
6. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 1-5, naznačen time, što je doza dnevna doza.
7. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 1-5, naznačen time, što je doza, doza dva puta dnevno.
8. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 1-5, naznačen time, što se doza daje svaka dva dana.
9. Spoj za uporabu prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time, što je FXR agonistički spoj 2-[(1R,3r,5S)-3-({5-ciklopropil-3-[2-(trifluorometoksi)fenil]-1,2-oksazol-4-il}metoksi)-8-azabiciklo[3.2.1]oktan-8-il]-4-fluoro-1,3-benzotiazol-6-karboksilna kiselina, u slobodnom obliku ili njegov konjugat s aminokiselinom.
10. Pripravak farmaceutskog jediničnog oblika doziranja, naznačen time, što sadrži oko 10 µg, oko 30 µg, oko 60 µg, oko 90 µg ili oko 120 µg 2-[(1R,3r,5S)-3-({5-ciklopropil-3-[2-(trifluorometoksi)fenil]-1,2-oksazol-4-il}metoksi)-8-azabiciklo[3.2.1]oktan-8-il]-4-fluoro-1,3-benzotiazol-6-karboksilne kiseline, za oralnu primjenu do maksimalne ukupne doze od oko 120 µg dnevno.
11. Pripravak farmaceutskog jediničnog oblika doziranja prema patentnom zahtjevu 10, naznačen time, što je 2-[(1R,3r,5S)-3-({5-ciklopropil-3-[2-(trifluorometoksi)fenil]-1,2-oksazol-4-il}metoksi)-8-azabiciklo[3.2.1]oktan-8-il]-4-fluoro-1,3-benzotiazol-6-karboksilna kiselina u slobodnom obliku ili u obliku njezine farmaceutski prihvatljive soli ili je konjugat s aminokiselinom.
12. Pripravak farmaceutskog jediničnog oblika doziranja prema patentnom zahtjevu 10, naznačen time, što se nalazi u obliku odabranom od tekućine, tablete ili kapsule.
13. Pripravak farmaceutskog jediničnog oblika doziranja prema bilo kojem od patentnih zahtjeva 10-12, naznačen time, što je za uporabu u liječenju kronične bolesti jetre, npr. bolesti nealkoholne masne jetre (NAFLD), nealkoholnog steatohepatitisa (NASH), ozljede žučnog kanala uzrokovane supstancom, žučnih kamenaca, ciroze jetre, ciroze izazvane alkoholom, cistične fibroze, opstrukcije žučnih kanala, kolelitijaze, fibroze jetre.
14. Pripravak farmaceutskog jediničnog oblika doziranja prema patentnom zahtjevu 13, naznačen time, što je za uporabu u liječenju nealkoholnog steatohepatitisa (NASH).
HRP20211032TT 2016-02-22 2021-06-29 Postupci za uporabu agonista fxr HRP20211032T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201662298121P 2016-02-22 2016-02-22
US201662420661P 2016-12-12 2016-12-12
PCT/IB2017/050963 WO2017145041A1 (en) 2016-02-22 2017-02-20 Methods for using fxr agonists
EP17709189.9A EP3419625B1 (en) 2016-02-22 2017-02-20 Methods for using fxr agonists

Publications (1)

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HRP20211032T1 true HRP20211032T1 (hr) 2021-10-01

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US (2) US11344540B2 (hr)
EP (2) EP3848031A1 (hr)
JP (1) JP6986022B2 (hr)
KR (1) KR20180115270A (hr)
CN (2) CN108697702A (hr)
AU (1) AU2017223155B2 (hr)
BR (1) BR112018016310A2 (hr)
CA (1) CA3013186A1 (hr)
CL (1) CL2018002359A1 (hr)
CY (1) CY1124300T1 (hr)
DK (1) DK3419625T3 (hr)
ES (1) ES2878575T3 (hr)
HK (1) HK1257647A1 (hr)
HR (1) HRP20211032T1 (hr)
HU (1) HUE054819T2 (hr)
IL (1) IL260784B (hr)
LT (1) LT3419625T (hr)
MX (1) MX2018010100A (hr)
PH (1) PH12018501656A1 (hr)
PL (1) PL3419625T3 (hr)
PT (1) PT3419625T (hr)
RU (1) RU2743075C2 (hr)
SI (1) SI3419625T1 (hr)
TW (1) TWI735546B (hr)
WO (1) WO2017145041A1 (hr)

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RS62110B1 (sr) 2015-03-31 2021-08-31 Enanta Pharm Inc Derivati žučnih kiselina kao agonisti fxr/tgr5 i postupci njihove upotrebe
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WO2017201152A1 (en) 2016-05-18 2017-11-23 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
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WO2019089670A1 (en) 2017-11-01 2019-05-09 Bristol-Myers Squibb Company Alkene compounds as farnesoid x receptor modulators
KR20200083528A (ko) 2017-11-01 2020-07-08 브리스톨-마이어스 스큅 컴퍼니 파르네소이드 x 수용체 조정제로서의 스피로시클릭 화합물
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WO2019160813A1 (en) 2018-02-14 2019-08-22 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
AR118050A1 (es) 2019-02-15 2021-09-15 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x
WO2020231917A1 (en) 2019-05-13 2020-11-19 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
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WO2021044351A1 (en) * 2019-09-06 2021-03-11 Novartis Ag Methods of treating liver disease using lta4h inhibitors
CN114945361A (zh) 2020-01-15 2022-08-26 法国国家卫生及研究医学协会 Fxr激动剂在治疗丁型肝炎病毒感染中的用途
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RU2018133298A (ru) 2020-03-24
CN108697702A (zh) 2018-10-23
CA3013186A1 (en) 2017-08-31
MX2018010100A (es) 2018-11-09
SI3419625T1 (sl) 2021-08-31
CL2018002359A1 (es) 2018-12-07
ES2878575T3 (es) 2021-11-19
US11344540B2 (en) 2022-05-31
WO2017145041A1 (en) 2017-08-31
US20220313677A1 (en) 2022-10-06
EP3419625B1 (en) 2021-04-07
EP3848031A1 (en) 2021-07-14
TW201735924A (zh) 2017-10-16
US20190046519A1 (en) 2019-02-14
BR112018016310A2 (pt) 2018-12-26
JP6986022B2 (ja) 2021-12-22
RU2743075C2 (ru) 2021-02-15
HUE054819T2 (hu) 2021-10-28
KR20180115270A (ko) 2018-10-22
JP2019511478A (ja) 2019-04-25
TWI735546B (zh) 2021-08-11
EP3419625A1 (en) 2019-01-02
PH12018501656A1 (en) 2019-06-03
DK3419625T3 (da) 2021-07-12
HK1257647A1 (zh) 2019-10-25
PL3419625T3 (pl) 2021-10-25
RU2018133298A3 (hr) 2020-05-27
IL260784B (en) 2022-04-01
LT3419625T (lt) 2021-07-26
AU2017223155A1 (en) 2018-08-09
AU2017223155B2 (en) 2019-08-22
CY1124300T1 (el) 2022-07-22
PT3419625T (pt) 2021-07-07
CN113679718A (zh) 2021-11-23

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