HRP20240265T1 - Spoj izoksazola kao fxr agonist i farmaceutski pripravci koji ga sadrže - Google Patents
Spoj izoksazola kao fxr agonist i farmaceutski pripravci koji ga sadrže Download PDFInfo
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- HRP20240265T1 HRP20240265T1 HRP20240265TT HRP20240265T HRP20240265T1 HR P20240265 T1 HRP20240265 T1 HR P20240265T1 HR P20240265T T HRP20240265T T HR P20240265TT HR P20240265 T HRP20240265 T HR P20240265T HR P20240265 T1 HRP20240265 T1 HR P20240265T1
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- pharmaceutically acceptable
- agonist
- fxr
- acceptable salt
- compound
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- 239000008194 pharmaceutical composition Substances 0.000 title claims 2
- -1 Isoxazole compound Chemical class 0.000 title 1
- 239000000556 agonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 17
- 229940121360 farnesoid X receptor (fxr) agonists Drugs 0.000 claims 15
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 9
- 208000019423 liver disease Diseases 0.000 claims 8
- 102100038495 Bile acid receptor Human genes 0.000 claims 7
- 101000603876 Homo sapiens Bile acid receptor Proteins 0.000 claims 7
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 7
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 6
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 6
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 6
- 239000000825 pharmaceutical preparation Substances 0.000 claims 6
- 102000000452 Acetyl-CoA carboxylase Human genes 0.000 claims 4
- 108010016219 Acetyl-CoA carboxylase Proteins 0.000 claims 4
- 108010018763 Biotin carboxylase Proteins 0.000 claims 4
- 208000019425 cirrhosis of liver Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- 102000004217 thyroid hormone receptors Human genes 0.000 claims 4
- 108090000721 thyroid hormone receptors Proteins 0.000 claims 4
- 229940127254 ASK1 inhibitor Drugs 0.000 claims 3
- 229940123876 Thyroid hormone receptor beta agonist Drugs 0.000 claims 3
- 229940121373 acetyl-coa carboxylase inhibitor Drugs 0.000 claims 3
- 210000004185 liver Anatomy 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 3
- 108091007065 BIRCs Proteins 0.000 claims 2
- 102000055031 Inhibitor of Apoptosis Proteins Human genes 0.000 claims 2
- 108010075639 MAP Kinase Kinase Kinase 5 Proteins 0.000 claims 2
- 102100033127 Mitogen-activated protein kinase kinase kinase 5 Human genes 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 238000002441 X-ray diffraction Methods 0.000 claims 2
- 229940125388 beta agonist Drugs 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 208000006454 hepatitis Diseases 0.000 claims 2
- 230000003463 hyperproliferative effect Effects 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 230000003211 malignant effect Effects 0.000 claims 2
- 230000000414 obstructive effect Effects 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 208000007788 Acute Liver Failure Diseases 0.000 claims 1
- 206010000804 Acute hepatic failure Diseases 0.000 claims 1
- 206010052747 Adenocarcinoma pancreas Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023514 Barrett esophagus Diseases 0.000 claims 1
- 208000023665 Barrett oesophagus Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000017667 Chronic Disease Diseases 0.000 claims 1
- 206010048832 Colon adenoma Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 208000010334 End Stage Liver Disease Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 208000004930 Fatty Liver Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 206010019708 Hepatic steatosis Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 102000004895 Lipoproteins Human genes 0.000 claims 1
- 108090001030 Lipoproteins Proteins 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 102100029152 UDP-glucuronosyltransferase 1A1 Human genes 0.000 claims 1
- 101710205316 UDP-glucuronosyltransferase 1A1 Proteins 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 206010000891 acute myocardial infarction Diseases 0.000 claims 1
- 238000007707 calorimetry Methods 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 230000001587 cholestatic effect Effects 0.000 claims 1
- 208000011444 chronic liver failure Diseases 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 201000010897 colon adenocarcinoma Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000009866 extrahepatic cholestasis Diseases 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000001024 intrahepatic cholestasis Diseases 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 208000018191 liver inflammation Diseases 0.000 claims 1
- 230000007774 longterm Effects 0.000 claims 1
- 230000001613 neoplastic effect Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 201000002094 pancreatic adenocarcinoma Diseases 0.000 claims 1
- 208000015768 polyposis Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 238000001757 thermogravimetry curve Methods 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic 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 three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Claims (17)
1. Spoj, naznačen time, da je predstavljen sljedećom Formulom (I):
[image]
ili njegova farmaceutski prihvatljiva sol.
2. Farmaceutski pripravak, naznačen time, da sadrži spoj prema patentnom zahtjevu 1, ili njegovu farmaceutski prihvatljivu sol, te farmaceutski prihvatljiv nosač.
3. Spoj ili njegova farmaceutski prihvatljiva sol prema patentnom zahtjevu 1, ili farmaceutski pripravak prema patentnom zahtjevu 2, naznačen time, da je za uporabu u liječenju stanja posredovanog farnesoid X receptorom (FXR), pri čemu se stanje posredovano putem FXR bira iz skupine koju čine:
kronično stanje intrahepatičke ili ekstrahepatičke kolestaze;
fibroza jetre;
kronični ili opstrukcijski upalni poremećaj jetre;
ciroza jetre;
steatoza jetre ili pridruženi sindrom;
kolestazni ili fibrozni efekt koji je povezan s alkoholno induciranom cirozom ili s virusno nošenim oblikom hepatitisa;
akutno ili kronično zatajenje jetre;
ishemija jetre nakon značajnog odstranjenja dijela jetre;
steatohepatitis povezan s kemoterapijom (CASH);
primarna bilijarna ciroza (PBC);
primarni sklerozirajući kolangitis (PSC);
neoplastična bolest gastrointestinalnog trakta ili jetre; i
upalna bolest crijeva (IBD);
poremećaj lipida ili poremećaj lipoproteina;
dijabetes tipa I;
dijabetes tipa II;
kliničke komplikacije kod dijabetesa tipa I i tipa II, odabrane iz skupine koju čine dijabetička nefropatija, dijabetička neuropatija, dijabetička retinopatija, i ostali uočeni efekti kliničke pojavnosti dugotrajnog dijabetesa;
nealkoholna bolest masne jetre (NAFDL);
nealkoholni steatohepatitis (NASH);
pretilost;
metabolički sindrom odabran iz skupine koju čine kombinirana stanja dislipidemije, dijabetesa i abnormalno visokog indeksa tjelesne mase;
akutni infarkt miokarda;
akutni moždani udar; i
tromboza koja se pojavljuje kao krajnja točka kronične opstrukcijske ateroskleroze;
nemaligni hiperproliferativni poremećaj;
maligni hiperproliferativni poremećaj odabran iz skupine koju čine hepatocelularni karcinom, adenom debelog crijeva, i polipoza;
adenokarcinom debelog crijeva;
rak dojke;
adenokarcinom gušterače; i
Barettov ezofagus.
4. Spoj ili njegova farmaceutski prihvatljiva sol prema patentnom zahtjevu 1, ili farmaceutski pripravak prema patentnom zahtjevu 2, naznačen time, da je za uporabu u liječenju stanja posredovanog farnesoid X receptorom (FXR), pri čemu stanje posredovano putem FXR je bolest jetre ili upalna bolest crijeva (IBD), gdje opcionalno bolest jetre je nealkoholni steatohepatitis (NASH), primarni sklerozirajući kolangitis (PSC), primarna bilijarna ciroza (PBC) ili fibroza jetre.
5. Agonist farnesoid X receptora (FXR), naznačen time, da je za uporabu u kombinaciji s inhibitorom signalno-regulacijske kinaze 1 apoptoze (ASK1) za liječenje i/ili prevenciju bolesti jetre ili upalne bolesti crijeva (IBD), pri čemu FXR agonist je spoj u skladu s patentnim zahtjevom 1,
ili njegova farmaceutski prihvatljiva sol; i
pri čemu ASK1 inhibitor je spoj Formule (II):
[image]
ili njegova farmaceutski prihvatljiva sol, njegov stereoizomer, mješavina stereoizomera, ili tautomer.
6. Agonist farnesoid X receptora (FXR), naznačen time, da je za uporabu u kombinaciji s inhibitorom acetil CoA karboksilaze (ACC) za liječenje i/ili prevenciju bolesti jetre ili upalne bolesti crijeva (IBD), pri čemu FXR agonist je spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol; i pri čemu ACC inhibitor je spoj Formule (III):
[image]
ili njegova farmaceutski prihvatljiva sol, njegov stereoizomer, mješavina stereoizomera, ili tautomer.
7. Agonist farnesoid X receptora (FXR), naznačen time, da je za uporabu u kombinaciji s agonistom receptora tiroidnog hormona (THR) β za liječenje i/ili prevenciju bolesti jetre ili upalne bolesti crijeva (IBD), pri čemu FXR agonist je spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol; i pri čemu THR β agonist je spoj Formule (IV):
[image]
ili njegova farmaceutski prihvatljiva sol, njegov stereoizomer, mješavina stereoizomera, ili tautomer.
8. FXR agonist za uporabu prema bilo kojem od patentnih zahtjeva 5 do 7, naznačen time, da se FXR agonist i ASK1 inhibitor, ACC inhibitor ili THR β agonist, primjenjuju odvojeno.
9. FXR agonist za uporabu prema bilo kojem od patentnih zahtjeva 5 do 8, naznačen time, da se bolest jetre bira od nealkoholnog steatohepatitisa (NASH), primarnog sklerozirajućeg kolangitisa (PSC) i primarne bilijarne ciroze (PBC).
10. Farmaceutski pripravak, naznačen time, da sadrži terapijski učinkovitu količinu inhibitora signalno-regulacijske kinaze 1 apoptoze (ASK1) i terapijski učinkovitu količinu agonista farnesoid X receptora (FXR), pri čemu FXR agonist je spoj u skladu s patentnim zahtjevom 1,
ili njegova farmaceutski prihvatljiva sol; i
pri čemu ASK1 inhibitor je spoj Formule (II):
[image]
ili njegova farmaceutski prihvatljiva sol, njegov stereoizomer, mješavina stereoizomera, ili tautomer.
11. Farmaceutski pripravak, naznačen time, da sadrži terapijski učinkovitu količinu inhibitora acetil CoA karboksilaze (ACC) i terapijski učinkovitu količinu agonista farnesoid X receptora (FXR), pri čemu FXR agonist je spoj u skladu s patentnim zahtjevom 1,
ili njegova farmaceutski prihvatljiva sol; i
pri čemu ACC inhibitor je spoj Formule (III):
[image]
ili njegova farmaceutski prihvatljiva sol, njegov stereoizomer, mješavina stereoizomera, ili tautomer.
12. Farmaceutski pripravak, naznačen time, da sadrži terapijski učinkovitu količinu agonista receptora tiroidnog hormona (THR) β i terapijski učinkovitu količinu agonista farnesoid X receptora (FXR), pri čemu FXR agonist je spoj u skladu s patentnim zahtjevom 1,
ili njegova farmaceutski prihvatljiva sol; i
pri čemu THR β agonist je spoj Formule (IV):
[image]
ili njegova farmaceutski prihvatljiva sol, njegov stereoizomer, mješavina stereoizomera, ili tautomer.
13. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 10 do 12, naznačen time, da nadalje sadrži farmaceutski prihvatljiv nosač.
14. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u inhibiranju UGT1A1 kod pacijenta koji ima bolest jetre.
15. Kristalni oblik spoja sa sljedećom formulom:
[image]
naznačen time, da posjeduje uzorak rendgenske difrakcije koji ima 2θ-refleksije na 9,6, 19,3, i 22,6 stupnjeva 2θ, plus ili minus 0,2 stupnja 2θ.
16. Kristalni oblik prema patentnom zahtjevu 15,
naznačen time, da posjeduje uzorak rendgenske difrakcije koji nadalje sadrži 2θ-refleksije na 3,2, 6,4, i 12,8 stupnjeva 2θ, plus ili minus 0,2 stupnja 2θ, opcionalno nadalje sadrži 2θ-refleksije na 22,1, 25,8, 29,1 stupanj 2θ, plus ili minus 0,2 stupnja 2θ.
17. Kristalni oblik prema patentnom zahtjevu 15 ili zahtjevu 16,
naznačen time, da posjeduje termogram diferencijalne pretražne kalorimetrije koji sadrži endotermički maksimum s početkom na oko 221°C.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201962792714P | 2019-01-15 | 2019-01-15 | |
EP20708721.4A EP3911647B1 (en) | 2019-01-15 | 2020-01-13 | Isoxazole compound as fxr agonist and pharmaceutical compositions comprising same |
PCT/US2020/013319 WO2020150136A1 (en) | 2019-01-15 | 2020-01-13 | Fxr (nr1h4) modulating compounds |
Publications (1)
Publication Number | Publication Date |
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HRP20240265T1 true HRP20240265T1 (hr) | 2024-05-10 |
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HRP20240265TT HRP20240265T1 (hr) | 2019-01-15 | 2020-01-13 | Spoj izoksazola kao fxr agonist i farmaceutski pripravci koji ga sadrže |
Country Status (29)
Country | Link |
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US (2) | US11225473B2 (hr) |
EP (2) | EP3911647B1 (hr) |
JP (2) | JP7265635B2 (hr) |
KR (1) | KR20210114457A (hr) |
CN (1) | CN113302190A (hr) |
AR (1) | AR117814A1 (hr) |
AU (2) | AU2020209564B2 (hr) |
BR (1) | BR112021011762A2 (hr) |
CA (1) | CA3124702A1 (hr) |
CL (1) | CL2021001877A1 (hr) |
CO (1) | CO2021009240A2 (hr) |
CR (1) | CR20210385A (hr) |
DK (1) | DK3911647T3 (hr) |
DO (2) | DOP2021000148A (hr) |
EA (1) | EA202191566A1 (hr) |
ES (1) | ES2973500T3 (hr) |
FI (1) | FI3911647T3 (hr) |
HR (1) | HRP20240265T1 (hr) |
IL (1) | IL284591A (hr) |
LT (1) | LT3911647T (hr) |
MX (1) | MX2021008518A (hr) |
PE (1) | PE20211907A1 (hr) |
PL (1) | PL3911647T3 (hr) |
PT (1) | PT3911647T (hr) |
SG (1) | SG11202107434PA (hr) |
SI (1) | SI3911647T1 (hr) |
TW (1) | TWI733307B (hr) |
WO (1) | WO2020150136A1 (hr) |
ZA (1) | ZA202104705B (hr) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2921432T3 (es) | 2016-06-13 | 2022-08-25 | Gilead Sciences Inc | Derivados de azetidina como moduladores de FXR (NR1H4) |
CA2968836A1 (en) | 2016-06-13 | 2017-12-13 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
ES2927019T3 (es) | 2017-03-28 | 2022-11-02 | Gilead Sciences Inc | Combinaciones terapéuticas para el tratamiento de enfermedades hepáticas |
US20210393662A1 (en) * | 2018-10-18 | 2021-12-23 | Avolynt | Use of sglt2 inhibitors to treat primary sclerosing cholangitis |
CN113439078B (zh) | 2019-02-19 | 2024-04-23 | 吉利德科学公司 | Fxr激动剂的固体形式 |
EP4090327A1 (en) | 2020-01-15 | 2022-11-23 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Use of fxr agonists for treating an infection by hepatitis d virus |
US11478533B2 (en) | 2020-04-27 | 2022-10-25 | Novo Nordisk A/S | Semaglutide for use in medicine |
IL302099A (en) * | 2020-10-15 | 2023-06-01 | Lilly Co Eli | FXR agonist polymorphs |
CN117202905A (zh) | 2021-01-14 | 2023-12-08 | 埃尼奥制药公司 | Fxr激动剂和ifn用于治疗hbv感染的协同效果 |
JP2024503861A (ja) | 2021-01-14 | 2024-01-29 | ウエヌイグレックオ・ファーマ | 慢性腎疾患を処置する方法 |
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