ME02434B - Nova jedinjenja koja moduliraju fxr (nr1h4) - Google Patents
Nova jedinjenja koja moduliraju fxr (nr1h4)Info
- Publication number
- ME02434B ME02434B MEP-2016-81A MEP201681A ME02434B ME 02434 B ME02434 B ME 02434B ME P201681 A MEP201681 A ME P201681A ME 02434 B ME02434 B ME 02434B
- Authority
- ME
- Montenegro
- Prior art keywords
- liver
- alkyl
- compound according
- group
- disease
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims 15
- 102100038495 Bile acid receptor Human genes 0.000 title claims 4
- 101000603876 Homo sapiens Bile acid receptor Proteins 0.000 title claims 4
- 230000000694 effects Effects 0.000 title claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 18
- 201000010099 disease Diseases 0.000 claims 12
- 210000004185 liver Anatomy 0.000 claims 8
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- 230000001684 chronic effect Effects 0.000 claims 6
- 208000019425 cirrhosis of liver Diseases 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 230000001587 cholestatic effect Effects 0.000 claims 4
- 206010012601 diabetes mellitus Diseases 0.000 claims 4
- 230000003176 fibrotic effect Effects 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 230000003463 hyperproliferative effect Effects 0.000 claims 4
- 150000002632 lipids Chemical group 0.000 claims 4
- 230000003211 malignant effect Effects 0.000 claims 4
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 4
- 230000000414 obstructive effect Effects 0.000 claims 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 208000007788 Acute Liver Failure Diseases 0.000 claims 2
- 206010000804 Acute hepatic failure Diseases 0.000 claims 2
- 206010052747 Adenocarcinoma pancreas Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 208000023514 Barrett esophagus Diseases 0.000 claims 2
- 208000023665 Barrett oesophagus Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010048832 Colon adenoma Diseases 0.000 claims 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 2
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 208000004930 Fatty Liver Diseases 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 206010019663 Hepatic failure Diseases 0.000 claims 2
- 206010019708 Hepatic steatosis Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- 102000004895 Lipoproteins Human genes 0.000 claims 2
- 108090001030 Lipoproteins Proteins 0.000 claims 2
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 208000007536 Thrombosis Diseases 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 2
- 238000009825 accumulation Methods 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 2
- 231100000836 acute liver failure Toxicity 0.000 claims 2
- 206010000891 acute myocardial infarction Diseases 0.000 claims 2
- 238000002512 chemotherapy Methods 0.000 claims 2
- 208000037976 chronic inflammation Diseases 0.000 claims 2
- 208000037893 chronic inflammatory disorder Diseases 0.000 claims 2
- 230000007882 cirrhosis Effects 0.000 claims 2
- 201000010897 colon adenocarcinoma Diseases 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 230000007850 degeneration Effects 0.000 claims 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 2
- 208000006454 hepatitis Diseases 0.000 claims 2
- 231100000283 hepatitis Toxicity 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 208000028867 ischemia Diseases 0.000 claims 2
- 231100000835 liver failure Toxicity 0.000 claims 2
- 208000007903 liver failure Diseases 0.000 claims 2
- 230000007774 longterm Effects 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 230000001613 neoplastic effect Effects 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 201000002094 pancreatic adenocarcinoma Diseases 0.000 claims 2
- 230000037361 pathway Effects 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 208000015768 polyposis Diseases 0.000 claims 2
- 230000002206 pro-fibrotic effect Effects 0.000 claims 2
- 238000011321 prophylaxis Methods 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 238000002271 resection Methods 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 238000011282 treatment Methods 0.000 claims 2
- 150000003626 triacylglycerols Chemical class 0.000 claims 2
- 230000003612 virological effect Effects 0.000 claims 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- -1 SO2NR7R8 Chemical group 0.000 claims 1
- 229910006069 SO3H Inorganic materials 0.000 claims 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 1
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- 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
- A61K31/41—Heterocyclic 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
- A61K31/42—Oxazoles
-
- 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
- A61K31/41—Heterocyclic 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
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further 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
- A61K31/435—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
-
- 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
-
- 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
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Claims (17)
1. Jedinjenje prema sledećoj formuli (1), njegov enantiomer, diastereomer, tautomer ili farmaceutski prihvatljiva so u komeR je izabran iz grupe koja se sastoji od COOR6, CONR7R8, tetrazolil, SO2NR7R8, C1-6 alkil, SO2-C1-6 alkil i H, pri čemu je R6 nezavisno izabran iz grupe koja se sastoji od H ili C1-6alkil, i R7 i R8 međusobno nezavisno su izabrani iz grupe koja se sastoji od H, C1-6alkil, halo-C1-6 alkil, C1-6 alkilen-R9, SO2-C1-6, alkil, gde je R9 izabran iz grupe koja se sastoji od COOH, OH i SO3H;A je izabran iz grupe koja se sastoji od: fenil, piridil, pirimidil, pirazolil, indolil, tienil, benzotienil, indazolil, benzizoksazolil, benzofuranil, benzotriazolil, furanil, benzotiazolil, tiazolil, oksadiazolil, svaki izborno supstituisan sa jednom ili dve grupe nezavisno izabrane iz grupe koja se sastoji od OH, O-C1-6 alkil, O-halo-C1-6 alkil, alkil, halo-C1-6 alkil, C3-6 cikloalkil i halogen;Q je izabran iz grupe koja se sastoji od fenil, piridil, tiazolil, tiofenil, pirimidil, svaka izborno supstituisana sa jednom ili dvegrupe nezavisno izabrane iz grupe koja se sastoji od C1-6alkil, halo-C1-6 alkil, halogen i CF3;Y je izabran od N ili CH;Z je izabran od ili u komeX = CH, N, NO;R1 je izabran iz grupe koja se sastoji od vodonika, C1-3 alkil, C3-6 cikloalkil, C4-5 alkilcikloalkil, gde je C1-3 alkil izborno supstituisan sa 1 do 3 supstituenta nezavisno izabrana od halogena, hidroksi ili C1-6alkoksi;R2 i R3 su nezavisno izabrani iz grupe koja se sastoji od vodonika, C1-3 alkil, C1-3 haloalkil, C1-3 alkoksi, C1-3 haloalkoksi i halogen.
2. Jedinjenje prema patentnom zahtevu 1 naznačeno time što R-A je izabran od ili
3. Jedinjenje prema patentnom zahtevu 1 ili 2 naznačeno time što Q je
4. Jedinjenje prema bilo kom od patentnih zahteva 1 do 3 naznačeno time što Z je
5. Jedinjenje prema bilo kom od patentnih zahteva 1 do 4 izabrano od ili ili njegova farmaceutski prihvatljiva so.
6. Jedinjenje prema bilo kom od patentnih zahteva 1 do 5 koje ima sledeću strukturu ili njegova farmaceutski prihvatljiva so.
7. Jedinjenje prema bilo kom od patentnih zahteva 1 do 5 koje ima sledeću strukturu ili njegova farmaceutski prihvatljiva so.
8. Farmaceutska kompozicija koja sadrži jedinjenje prema bilo kom od patentnih zahteva 1 do 7, ili njegovu farmaceutski prihvatljivu so, i farmaceutski prihvatljiv nosač.
9. Jedinjenje prema bilo kom od patentnih zahteva 1 do 7 za upotrebu kao lek.
10. Jedinjenje prema bilo kom od patentnih zahteva 1 do 7 za upotrebu u profilaksi i/ili lečenju bolesti posredovanih preko FXR.
11. Jedinjenje za upotrebu prema patentnom zahtevu 10 naznačeno time što je bolest izabrana od hroničnog intrahepatičnog ili izvesnih oblika ekstrahepatičnih holestatičkih stanja; fibroze jetre; opstruktivnih ili hroničnih inflamatornih poremećaja jetre; ciroze jetre; steatoze jetre i srodnih sindroma, holestatičkih ili fibrotičkih efekata koji su povezani sa cirozom koja je indukovana alkoholom ili sa virusnim oblicima hepatitisa; insuficijencije jetre ili ishemije jetre posle velike resekcije jetre; steatohepatitisa povezanog sa hemoterapijom (CASH); akutne insuficijencije jetre; i/ili inflamatornih bolesti creva.
12. Jedinjenje za upotrebu prema patentnom zahtevu 10 naznačeno time što je bolest izabrana od poremećaja lipida i lipoproteina; dijabetesa tipa II i kliničkih komplikacija dijabetesa tipa I i tipa II, uključujući dijabetičku nefropatiju, dijabetičku neuropatiju, dijabetičku retinopatiju i druge zabeležene efekte kliničke manifestacije dugotrajnog dijabetesa; stanja i bolesti koja su rezultat hronične masne i fibrotičke degeneracije organa kao posledica pojačane akumulacije lipida i naročito triglicerida i kasnije aktivacije profibrotičkih puteva, kao što je bolest nealkoholne masne jetre (NAFLD) ili nealkoholni steatohepatitis (NASH); gojaznosti ili metaboličkog sindroma (kombinovana stanja dislipidemije, dijabetesa ili abnormalno visokog indeksa telesne mase); i/ili akutnog infarkta miokarda, akutnog šloga ili tromboze koji se javlja kao krajnja tačka hronične opstruktivne ateroskleroze.
13. Jedinjenje za upotrebu prema patentnom zahtevu 10 naznačeno time što je bolest izabrana od nemalignih hiperproliferativnih poremećaja i malignih hiperproliferativnih poremećaja, naročito hepatoćelijskog karcinoma, adenoma debelog creva i polipoza, adenokarcinoma debelog creva, kancera dojke, adenokarcinoma pankreasa, Baretovog jednjaka ili drugih oblika neoplastičnih bolesti gastrointestinalnog trakta i jetre.
14. Upotreba jedinjenja prema bilo kom od patentnih zahteva 1 do 7 za pripremu leka za profilaksu i/ili lečenje bolesti posredovanih preko FXR.
15. Upotreba prema patentnom zahtevu 14 naznačena time što je bolest izabrana od hroničnih intrahepatičnih ili izvesnih oblika ekstrahepatičnih holestatičkih stanja; fibroze jetre; opstruktivnih ili hroničnih inflamatornih poremećaja jetre; ciroze jetre; steatoze jetre i povezanih sindroma, holestatičkih ili fibrotičkih efekata koji su povezani sa cirozom koja je indukovana alkoholom ili sa virusnim oblicima hepatitisa; insuficijencije jetre ili ishemije jetre posle velike resekcije jetre; steatohepatitisa povezanog sa hemoterapijom (CASH); akutne insuficijencije jetre; i/ili inflamatornih bolesti creva.
16. Upotreba prema patentnom zahtevu 14 naznačena time što je bolest izabrana od poremećaja lipida i lipoproteina; dijabetesa tipa II i kliničkih komplikacija dijabetesa tipa I i tipa II, uključujući dijabetičku nefropatiju, dijabetičku neuropatiju, dijabetičku retinopatiju i druge zabeležene efekte kliničke manifestacije dugotrajnog dijabetesa; stanja i bolesti koji su rezultat hronične masne i fibrotičke degeneracije organa kao posledica pojačane akumulacije lipida i naročito triglicerida i kasnije aktivacije profibrotičkih puteva; kao što je bolest nealkoholne masne jetre (NAFLD) ili nealkoholni steatohepatitis (NASH); gojaznosti ili metaboličkog sindroma (kombinovana stanja dislipidemije, dijabetesa ili abnormalno visokog indeksa telesne mase); i/ili akutnog infarkta miokarda, akutnog šloga ili tromboze koja se javlja kao krajnja tačka hronične opstruktivne ateroskleroze.
17. Upotreba prema patentnom zahtevu 14 naznačena time što je bolest izabrana od nemalignih hiperproliferativnih poremećaja i malignih hiperproliferativnih poremećaja, naročito hepatoćelijskog karcinoma, adenoma debelog creva i polipoza, adenokarcinoma debelog creva, kancera dojke, adenokarcinoma pankreasa, Baretovog jednjaka ili drugih oblika neoplastičnih bolesti gastrointestinalnog trakta i jetre.
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| PCT/EP2012/002941 WO2013007387A1 (en) | 2011-07-13 | 2012-07-12 | Novel fxr (nr1h4) binding and activity modulating compounds |
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