NO324694B1 - Anvendelse av endotelinreseptor-antagonister for fremstilling av medikamenter for a kontrollere hyperlipidemi. - Google Patents

Anvendelse av endotelinreseptor-antagonister for fremstilling av medikamenter for a kontrollere hyperlipidemi. Download PDF

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Publication number
NO324694B1
NO324694B1 NO20002777A NO20002777A NO324694B1 NO 324694 B1 NO324694 B1 NO 324694B1 NO 20002777 A NO20002777 A NO 20002777A NO 20002777 A NO20002777 A NO 20002777A NO 324694 B1 NO324694 B1 NO 324694B1
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Prior art keywords
receptor antagonists
endothelin receptor
medications
manufacture
endothelin
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NO20002777A
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English (en)
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NO20002777D0 (no
NO20002777L (no
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Michael Kirchengast
Klaus Muenter
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Abbott Gmbh & Co Kg
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Publication of NO20002777D0 publication Critical patent/NO20002777D0/no
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Publication of NO324694B1 publication Critical patent/NO324694B1/no

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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
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (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)
  • Medicines Containing Plant Substances (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Description

Foreliggende oppfinnelse angår anvendelse av endotelinreseptor-antagonister for fremstilling av medikamenter for å kontrollere hyperlipidemi.
Peptidhormonet endotelin er kjent for sin sterke vasokonstriktoregenskap. Endotelin- reseptor-antagonister testes derfor hovedsakelig i kardiovaskulære patologier.
Endotelinreseptor-antagonister som kan anvendes er både endotelinA- og blandet endotelinA/B reseptor-antagonister.
Spesielt egnede endotelinreseptor-antagonister er:
1. TBC-11251 (J. Med. Chem., 40, No. 11, 1690-97, 1997), 2. BMS-193884 (EP 558,258)
3. BMS-207940 (Pharmaprojects (13,06,97)),
4. BQ-123 (Exp. Opin. Invest.Drugs, 1997, 6, No. 5, 475-487),
5. SB-209670 (Exp. Opin. Invest.Drugs, 1997, 6, No. 5, 475-487),
6. SB-217242 (Exp. Opin. Invest.Drugs, 1997, 6, No. 5, 475-487),
7. SB-209598 (Trends in Pharmacol. Sei., 17,177-81, 1996),
8. TAK-044 (Exp. Opin. Invest.Drugs, 1997, 6, No. 5, 475-487),
9. Bosentan (Trends in Pharmacol. Sei., 18, 408-12, 1997),
10. PD-156707 (J. Med. Chem., 40, No. 7,1063-74, 1997),
11. L-749329 (Bioorg. Med. Chem. Lett., 7, No. 3, 275-280,1997),
12. L-754142 (Exp. Opin. Invest.Drugs, 1997, 6, No. 5, 475-487),
13. ABT-627 (J. Med. Chem., 40, No. 20, 3217-27, 1997), 14. A-127772 (J. Med. Chem., 39, No. 5, 1039-1048, 1996), 15. A-206377 (213th American Chemical Society National Meeting, San Francisco,
California, USA, 13 - 17 April, 1997, Poster, MED1193),
16. A-182086 (J. Med. Chem., 40, No. 20, 3217-27, 1997), 17. EMD-93246 (211th American Chemical Society National Meeting, Ny Orleans,
USA, 1996, Poster, MED1143),
18. EMD-122801 (Bioorg. Med. Chem. Lett., 8, No. 1,17-22,1998),
19. ZD-1611 (Trends in Pharmacol. Sei., 18, 408-12,1997),
20. AC-610612 (R&D Focus Drugs News (18.05.98)),
21. T-0201 (70th Annual Meeting of the Japanese Pharmacological Society,
Chiba, Japan, 22-25 March 1997, Lecture, 0-133),
22. J-104132 (R&D Focus Drugs News (15,12,97)) og, spesielt,
Fedme er betegnelsen anvendt når kroppsvekten er minst 20% over normalvekten. Årsakene til fedme er overspising eller gal utnyttelse av maten, for eksempel familiær hyperkolesterolemi. Sykdommer forårsaket av eller ofte forbundet med fedme som kan nevnes er hypertensjon, type 2 diabetes, hyperlipidemi, kronisk nyresvikt og arteriosklerose og muligens også gikt.
Det har hittil vært mulig bare med store vanskeligheter å simulere patologisk tilstand av fedme i dyreforsøk (administrering av ekstremt høye kolesteroldoser). Imidlertid, har nylig, "knockout" mus som mangler genet for apolipoprotein E blitt avlet og kan anvendes for testing av forbindelser mot fedme.
Effekten av endotelinreseptor-antagonistsubstans 23 ble undersøkt i dyremodellen av apoE "knockout" mus. I kontrollrotter, som forventet, økte kroppsvekten til dyrene på en høy-fettdiett sterkt. Dette ble forbundet med en økning i størrelsen av leveren med samtidig fettdegenerasjon av leveren. I en parallel gruppe, ble dyrene behandlet med substans 23 (50 mg/kg/d). I denne gruppen, ble økningen i kropps- og levervekt fullstendig forhindret. Leveren var også histologisk uforandret.
EndotelinA- og endotelinA/B reseptor-antagonister må administreres hele livet. Deres dose er fra 50 til 500 mg pr. pasient og dag.
EndotelinA- og endotelinA/B reseptor-antagonister blir generelt administrert oralt, for eksempel i form av ubelagte, lakkerte og sukker-belagte tabletter, harde og myke gelatinkapsler, løsninger, emulsjoner eller suspensjoner. Imidlertid, kan administrering også finne sted rektalt, for eksempel i form av suppositorier eller parenteralt, for eksempel i form av injeksjonsløsninger.
For å produsere ubelagte, lakkerte og sukker-belagte tabletter, harde og myke gelatinkapsler, kan endotelinreseptor-antagonister prosesseres med farmasøytisk inerte, uorganiske eller organiske tilsetningsmidler. Tilsetningsmidler av disse typer som kan anvendes for ubelagte og sukker-belagte tabletter og harde gelatinkapsler er laktose, maisstivelse eller derivater derav, talk, stearinsyre eller dens salter. Tilsetningsmidler egnet for myke gelatinkapsler er vegetabilske oljer, vokser, fett, semifaste- og væskepolyoler.
Tilsetningsmidler egnet for å produsere løsninger og siruper er, for eksempel vann, polyoler, sukrose, invertsukker, glukose og lignende. Tilsetningsmidler egnet for injeksjonsløsninger er vann, alkoholer, polyoler, glycerol, vegetabilske oljer. Tilsetningsmidler egnet for suppositorier er naturlige eller herdede oljer, vokser, fett, semivæske eller væskepolyoler og lignende.
De farmasøytiske preparater kan dessuten inneholde konserveringsmidler, solubiliseringsmidler, stabiliseringsmidler, fuktemidler, emulgeringsmidler, søtningsmidler, farger, aromatiseringsmidler, salter for å endre det osmotiske trykket, buffere, belegningsmidler og/eller antioksydasjonsmidler.
De følgende eksempler illustrerer oppfinnelsen.
Eksempel 1
Lakkerte tabletter av de følgende preparater ble produsert:
Forbindelse 23, laktosen, cellulosen og polyvinylpyrrolidonet er våt-granulert og tørket. De siktede granuler blir blandet med magnesiumstearatet og blandingen er kompressert til ovale tablettkjerner som hver veier 390,0 mg. Kjernene blir deretter lakk-belagt inntil de lakkerte tabletter har nådd en endelig vekt på 400 mg.
Eksempel 2
Lakkerte tabletter ble produsert i analogi med Eksempel 1, men inneholdt 300 mg Forbindelse 26 istedenfor 300 mg Forbindelse 23.
Eksempel 3
Produksjon av harde gelatinkapsler av de følgende preparater:
De første fem bestanddeler er våt-granulert og tørket. Granulene blir blandet med natriumkarboksymetylstivelsen, talket og magnesiumstearatet og blandingen pakkes i størrelse 0 harde gelatinkapsler.
1. Anvendelse av endotelinreseptor-antagonister med følgende formler:
for å fremstille medikamenter for å kontrollere hyperlipidemi.
NO20002777A 1997-12-05 2000-05-30 Anvendelse av endotelinreseptor-antagonister for fremstilling av medikamenter for a kontrollere hyperlipidemi. NO324694B1 (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19754082A DE19754082A1 (de) 1997-12-05 1997-12-05 Methode zur Bekämpfung der Fettleibigkeit
PCT/EP1998/007501 WO1999029308A2 (de) 1997-12-05 1998-11-21 Methode zur bekämpfung der fettleibigkeit

Publications (3)

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NO20002777D0 NO20002777D0 (no) 2000-05-30
NO20002777L NO20002777L (no) 2000-06-02
NO324694B1 true NO324694B1 (no) 2007-12-03

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NO20002777A NO324694B1 (no) 1997-12-05 2000-05-30 Anvendelse av endotelinreseptor-antagonister for fremstilling av medikamenter for a kontrollere hyperlipidemi.
NO20074419A NO20074419L (no) 1997-12-05 2007-08-30 Anvendelse av endotelinreseptorantagonister for fremstilling av medikamenter for a bekjempe sykdom

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Country Link
US (1) US6197780B1 (no)
EP (1) EP1035851B1 (no)
JP (1) JP2002512173A (no)
KR (1) KR20010032779A (no)
CN (1) CN1152685C (no)
AT (1) ATE204172T1 (no)
AU (1) AU751053B2 (no)
BR (1) BR9815335A (no)
CA (1) CA2311423C (no)
CZ (1) CZ300442B6 (no)
DE (2) DE19754082A1 (no)
ES (1) ES2162493T3 (no)
HK (1) HK1037141A1 (no)
HU (1) HUP0100171A3 (no)
NO (2) NO324694B1 (no)
RU (1) RU2292891C2 (no)
WO (1) WO1999029308A2 (no)

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DE19533023B4 (de) 1994-10-14 2007-05-16 Basf Ag Neue Carbonsäurederivate, ihre Herstellung und Verwendung
EP1130027A1 (de) * 2000-02-29 2001-09-05 Aventis Pharma Deutschland GmbH Memno-Peptide, Verfahren zu ihrer Herstellung und Verwendung derselben
US20050175667A1 (en) * 2004-02-10 2005-08-11 Wenda Carlyle Use of endothelin antagonists to prevent restenosis
EP2190433A2 (en) 2007-08-22 2010-06-02 Gilead Colorado, Inc. Therapy for complications of diabetes
PL3628320T3 (pl) 2011-11-11 2022-07-25 Gilead Apollo, Llc Inhibitory acc i ich zastosowania
WO2016099233A2 (ru) * 2014-10-20 2016-06-23 Товарищество С Ограниченной Ответственностью "Фармацевтическая Компания "Ромат" Фармацевтическая композиция для лечения туберкулеза
AR106472A1 (es) 2015-10-26 2018-01-17 Gilead Apollo Llc Inhibidores de acc y usos de los mismos
SI3380479T1 (sl) 2015-11-25 2023-04-28 Gilead Apollo, Llc Triazolni inhibitorji ACC in uporabe le-teh
CA3004796C (en) 2015-11-25 2023-11-14 Gilead Apollo, Llc Pyrazole acc inhibitors and uses thereof
CA3004798C (en) 2015-11-25 2023-10-31 Gilead Apollo, Llc Ester acc inhibitors and uses thereof
EP3379933B1 (en) 2015-11-25 2023-02-15 Gilead Apollo, LLC Fungicidal compositions containing derivatives of 2,4-dioxo-1,4-dihydrothieno[2,3-d]pyrimidine
EP4364795A3 (en) 2016-03-02 2024-08-14 Gilead Apollo, LLC Solid forms of a thienopyrimidinedione acc inhibitor and methods for production thereof
US20180280394A1 (en) 2017-03-28 2018-10-04 Gilead Sciences, Inc. Methods of treating liver disease

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WO1994012499A1 (en) * 1992-12-01 1994-06-09 The Green Cross Corporation 1,8-naphthyridin-2-one derivative and use thereof_
WO1997008169A1 (en) 1995-08-24 1997-03-06 Warner-Lambert Company Furanone endothelin antagonists
JP3116347B2 (ja) * 1996-11-13 2000-12-11 田辺製薬株式会社 医薬組成物

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Publication number Publication date
RU2292891C2 (ru) 2007-02-10
US6197780B1 (en) 2001-03-06
KR20010032779A (ko) 2001-04-25
HK1037141A1 (en) 2002-02-01
WO1999029308A3 (de) 1999-09-30
CZ300442B6 (cs) 2009-05-20
WO1999029308A2 (de) 1999-06-17
AU2153599A (en) 1999-06-28
DE19754082A1 (de) 1999-06-10
ATE204172T1 (de) 2001-09-15
EP1035851A2 (de) 2000-09-20
ES2162493T3 (es) 2001-12-16
CA2311423A1 (en) 1999-06-17
BR9815335A (pt) 2000-10-17
CN1152685C (zh) 2004-06-09
DE59801230D1 (de) 2001-09-20
HUP0100171A2 (hu) 2003-02-28
JP2002512173A (ja) 2002-04-23
CN1301162A (zh) 2001-06-27
NO20002777D0 (no) 2000-05-30
HUP0100171A3 (en) 2003-10-28
EP1035851B1 (de) 2001-08-16
AU751053B2 (en) 2002-08-08
NO20002777L (no) 2000-06-02
CA2311423C (en) 2008-01-29
NO20074419L (no) 2000-06-02
RU2003138080A (ru) 2005-06-10
CZ20002006A3 (cs) 2000-11-15

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