HUP0102840A2 - Epesav transzportot és taurokolát felvételt gátló benzotiepinszármazékok, valamint ezeket tartalmazó gyógyászati készítmények és eljárás a hatóanyagok előállítására - Google Patents

Epesav transzportot és taurokolát felvételt gátló benzotiepinszármazékok, valamint ezeket tartalmazó gyógyászati készítmények és eljárás a hatóanyagok előállítására

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Publication number
HUP0102840A2
HUP0102840A2 HU0102840A HUP0102840A HUP0102840A2 HU P0102840 A2 HUP0102840 A2 HU P0102840A2 HU 0102840 A HU0102840 A HU 0102840A HU P0102840 A HUP0102840 A HU P0102840A HU P0102840 A2 HUP0102840 A2 HU P0102840A2
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HU
Hungary
Prior art keywords
alkyl
aryl
heterocyclic
group
compounds
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HU0102840A
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English (en)
Inventor
Shyamal C. Banerjee
Horng-Chih Huang
Len F. Lee
Jinglin J. Li
Raymond E. Miller
David B. Reitz
Samuel J. Tremont
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G.D. Searle & Co.
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Application filed by G.D. Searle & Co. filed Critical G.D. Searle & Co.
Publication of HUP0102840A2 publication Critical patent/HUP0102840A2/hu

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    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D337/00—Heterocyclic compounds containing rings of more than six members having one sulfur atom as the only ring hetero atom
    • C07D337/02—Seven-membered rings
    • C07D337/06—Seven-membered rings condensed with carbocyclic rings or ring systems
    • C07D337/08—Seven-membered rings condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • 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
    • 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
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/14—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D337/00—Heterocyclic compounds containing rings of more than six members having one sulfur atom as the only ring hetero atom
    • C07D337/02—Seven-membered rings
    • C07D337/06—Seven-membered rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
    • C07F9/655381—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a seven-(or more) membered ring
    • C07F9/65539—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a seven-(or more) membered ring condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06086—Dipeptides with the first amino acid being basic
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32—Polymers modified by chemical after-treatment
    • C08G65/329—Polymers modified by chemical after-treatment with organic compounds

Abstract

A találmány tárgyát az (I) általános képletű benzotiepin-származékokképezik, amely vegyületek az ileum epesav transzport és taurokolátfelvétel inhibitorai. A találmány tárgyát képezik ezen vegyületekettartalmazó gyógyá- szati készítmények, valamint a vegyületekelőállítására szolgáló eljárás is. A találmány szerinti vegyületekettartalmazó gyógyászati készítmények eredményesen alkalmazhatókhiperlipaemiás állapotok, mint magas koleszterinszint csökkentésérevagy megelőzésére. Az (I) általános képlet a szubsztituensek jelentéseigen sokféle, többek között q értéke 1, 2, 3 vagy 4; n értéke 0, 1vagy 2; R1 és R2 jelentése egymástól függetlenül többek közötthidrogénatom, alkil-, alkenil-, alkinil-, halogén-alkil-, alkil-aril-,aril-alkil-, alkoxi-, alkoxi-alkil-, dialkil-amino-, alkil-tio-,(polialkil)-aril- vagy cikloalkilcsoport, amelyek adott esetben egyvagy több szubsztituenssel lehetnek helyettesítve vagy együttesjelentésük 3-10 szénatomos cikloalkilcsoport; R3 és R4 jelentéseegymástól függetlenül többek között hidrogénatom, alkil-, alkenil-,alkinil-, acil-oxi-, aril-, heterociklusos csoport, -OR9, -NR9R10, -SR9, -S(O)R9, -SO2R9 vagy -SO3R9; vagy R3 és R4 együttes jelentése =O,=NOR11, =S, =NNR11R12, =NR9 vagy =CR11R12 vagy R11 és R12 jelentése anitrogénatommal vagy szénatommal együtt, amelyhez kapcsolódnak egygyűrűs csoport; R5 jelentése arilcsoport, amely egy vagy több -OR13acsoporttal van helyettesítve, ahol R13a jelentése alkil-aril-alkil-,alkil-heteroaril-alkil-, alkil-heterociklusos-alkil-, heterociklusos-alkil-, heteroaril-alkil-, kvaterner heterociklusos-alkil-, alkil-ammónium-alkil- vagy karboxi-alkil-amino-karbonit-alkilcsoport; R6jelentése például adott esetben szubsztituált alkil-, alkenil-,alkinil-, aril-, cikloalkil-, heterociklusos csoport, kvaternerheterociklusos csoport; -SR9, -S(O)R9, -SO2R9 vagy -SO3R9 csoport. Ó
HU0102840A 1998-07-02 1999-06-29 Epesav transzportot és taurokolát felvételt gátló benzotiepinszármazékok, valamint ezeket tartalmazó gyógyászati készítmények és eljárás a hatóanyagok előállítására HUP0102840A2 (hu)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/109,551 US5994391A (en) 1994-09-13 1998-07-02 Benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
PCT/US1999/012828 WO2000001687A1 (en) 1998-07-02 1999-06-29 Benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake

Publications (1)

Publication Number Publication Date
HUP0102840A2 true HUP0102840A2 (hu) 2002-01-28

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Application Number Title Priority Date Filing Date
HU0102840A HUP0102840A2 (hu) 1998-07-02 1999-06-29 Epesav transzportot és taurokolát felvételt gátló benzotiepinszármazékok, valamint ezeket tartalmazó gyógyászati készítmények és eljárás a hatóanyagok előállítására

Country Status (37)

Country Link
US (1) US5994391A (hu)
EP (2) EP1466911A3 (hu)
JP (3) JP2002519418A (hu)
KR (1) KR20010083084A (hu)
CN (1) CN1312805A (hu)
AP (1) AP2001002062A0 (hu)
AR (1) AR019880A1 (hu)
AT (1) ATE256122T1 (hu)
AU (2) AU766957B2 (hu)
BG (1) BG105206A (hu)
BR (1) BR9911737A (hu)
CA (1) CA2336315A1 (hu)
CO (2) CO5080807A1 (hu)
DE (1) DE69913530T2 (hu)
DK (1) DK1091953T3 (hu)
EA (2) EA004650B1 (hu)
EE (1) EE200100002A (hu)
ES (1) ES2213373T3 (hu)
GE (1) GEP20032925B (hu)
HK (1) HK1039614A1 (hu)
HR (1) HRP20010004A2 (hu)
HU (1) HUP0102840A2 (hu)
ID (1) ID28221A (hu)
IL (1) IL140576A0 (hu)
IS (1) IS5798A (hu)
NO (1) NO20010016L (hu)
NZ (1) NZ509621A (hu)
OA (1) OA11629A (hu)
PL (1) PL346324A1 (hu)
PT (1) PT1091953E (hu)
SG (1) SG108309A1 (hu)
SK (1) SK20302000A3 (hu)
TR (1) TR200100824T2 (hu)
TW (1) TWI229670B (hu)
WO (1) WO2000001687A1 (hu)
YU (1) YU84400A (hu)
ZA (1) ZA200100028B (hu)

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