ME02434B - Nova jedinjenja koja moduliraju fxr (nr1h4) - Google Patents

Nova jedinjenja koja moduliraju fxr (nr1h4)

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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
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ME
Montenegro
Prior art keywords
liver
alkyl
compound according
group
disease
Prior art date
Application number
MEP-2016-81A
Other languages
German (de)
English (en)
French (fr)
Inventor
Olaf Kinzel
Christoph Steeneck
Claus Kremoser
Original Assignee
Gilead Sciences Inc
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Filing date
Publication date
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of ME02434B publication Critical patent/ME02434B/me

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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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • 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)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular 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.
MEP-2016-81A 2011-07-13 2012-07-12 Nova jedinjenja koja moduliraju fxr (nr1h4) ME02434B (me)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201161507153P 2011-07-13 2011-07-13
EP11005722A EP2545964A1 (en) 2011-07-13 2011-07-13 Novel FXR (NR1H4) binding and activity modulating compounds
PCT/EP2012/002941 WO2013007387A1 (en) 2011-07-13 2012-07-12 Novel fxr (nr1h4) binding and activity modulating compounds
EP12735100.5A EP2731676B1 (en) 2011-07-13 2012-07-12 Novel fxr (nr1h4) modulating compounds

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ME02434B true ME02434B (me) 2016-09-20

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US (5) US9139539B2 (me)
EP (5) EP2545964A1 (me)
JP (2) JP5986633B2 (me)
KR (4) KR101722410B1 (me)
CN (2) CN103702719B (me)
AR (1) AR087127A1 (me)
AU (4) AU2012283387C1 (me)
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CA (1) CA2839357C (me)
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DK (2) DK2731676T3 (me)
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ES (3) ES2978166T3 (me)
FI (1) FI3246070T3 (me)
HR (2) HRP20240422T1 (me)
HU (2) HUE066734T2 (me)
IL (1) IL229944A (me)
LT (1) LT3246070T (me)
ME (1) ME02434B (me)
MX (2) MX368371B (me)
MY (1) MY161158A (me)
PH (1) PH12014500124A1 (me)
PL (3) PL3246070T3 (me)
PT (2) PT3246070T (me)
RS (1) RS54786B1 (me)
SI (3) SI2987532T1 (me)
SM (1) SMT201600169B (me)
TW (1) TWI439455B (me)
UY (1) UY34196A (me)
WO (1) WO2013007387A1 (me)
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