FI116220B - Svavel-substituerade azetidinonföreningar som är nyttiga som hypkolesterolemiska ämnen - Google Patents

Svavel-substituerade azetidinonföreningar som är nyttiga som hypkolesterolemiska ämnen Download PDF

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Publication number
FI116220B
FI116220B FI972099A FI972099A FI116220B FI 116220 B FI116220 B FI 116220B FI 972099 A FI972099 A FI 972099A FI 972099 A FI972099 A FI 972099A FI 116220 B FI116220 B FI 116220B
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Finland
Prior art keywords
phenyl
fluorophenyl
azetidinone
trans
thio
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FI972099A
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English (en)
Finnish (fi)
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FI972099A0 (sv
FI972099A (sv
Inventor
Sundeep Dugar
Duane A Burnett
Brian A Mckittrick
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Schering Corp
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Priority claimed from US08/342,197 external-priority patent/US5624920A/en
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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • 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
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • 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

Claims (9)

1. En förening med formeln R Am ' 1 1 n <y\? eller dess farmaceutiskt godtagbar sait, kännetecknad därav, att Ar1 ärfenyl, R10-substituerad fenyl, pyridyl eller tienyl;
10 Ar2 är fenyl eller R4-substituerad fenyl; Ar3 är fenyl eller R5-substituerad fenyl; X och Y är -CHr; R är -OR6 eller -0(C0)R6; R1 är väte; eller R och R1 tillsammans med är =0; q är 0 eller 1; 15 r är 0, 1, eller 2; m och n är oberoende av varandra 0, 1 eller 2; förutsatt att summan av m, n och q är 1 eller
2; R4 är 1 - 5 substituenter självständlgt valda ur gruppen, -OR6, -0(CO)R6, -0(CO)OR9 eller -0(CH2)1.50R6;
20 R5 är 1 - 5 substituenter självständigt valda ur gruppen -OR6 och halogen; : : : R6 är väte, lägre alkyl, fenyl och fenyl-substituerad lägre alkyl; och R9 är lägre alkyl, fenyl eller fenyl-substituerad lägre alkyl; och . · ·, R10 är 1 - 5 substituenter självständigt valda ur gruppen lägre alkyl, -OR6 och halo- gen. : 25 '' 2. Förening enligt patentkravet 1, kännetecknad därav, att Ar1 är fenyl, R10- v : substituerad fenyl eller tienyl, Ar2 är R4-substituerad fenyl och Ar3 är fenyl eller R5-substituerad fenyl. : ‘ “: 30
3. Förening enligt av patentkraven 1 eller 2, kännetecknad därav, att q är 0, X och Y är bäda -CH2 och summan av m och n är 2. t I
...: 4. Förening enligt av patentkraven 1 eller 2, kännetecknad därav, att q är 1, X .'. och Y är blda -CH2-, summan av m och n är 1, R1 är väte och R är -OR6, där R6 är , · , 35 väte eller där R och R1 tillsammans bildar en =0-grupp. 116220 39
5. Förening enligt patentkravet 1, kännetecknad därav, att den är vald ur gruppen trans-l-(4-fluorfenyl)-4-(4-hydroxifenyl)-3-[(2-fenyletyl)tio]-2-azetidinon; trans-4-(4-metoxifenyl)-l-fenyl-3-[(2-fenyletyl)tio]-2-azetidinon; cis-4-(4-metoxifenyl)-l-fenyl-3-[(2-fenyletyl)tio]-2-azetidinon; 5 trans-l-(4-fluorfenyl)-4-(4-hydroxifenyl)-3-[(2-fenyletyl)sulfinyl]-2-azetidinon; cis-l-(4-fluorfenyl)-4-(4-hydroxifenyl)-3-[(2-fenyletyl)sulfinyl]-2-azetidinon; trans-4-(4-metoxifenyl)-l-fenyl-3-[(2-fenyletyl)sulfinyl]-2-azetidinon; cis-4-(4-metoxifenyl)-l-fenyl-3-[(2-fenyletyl)sulfinyl]-2-azetidinon; trans-4-[l-(4-fluorfenyl)-4-oxo-3-[(2-fenyletyl)sulfinyl]-2-azetidinyl]-fenylacetat; 10 cis-4-[l-(4-fluorfenyl)-4-oxo-3-[(2-fenyletyl)sulfinyl]-2-azetidinyl]-fenyl-acetat; (+/-)-trans-4-(4-metoxifenyl)-l-fenyl-3-[(2-fenyletyl)sulfonyl]-2-azetidinon; trans-l-(4-fluorfenyl)-3-[[2-(4-fluorfenyl)-2-oxoetyl]tio]-4-(4-hydroxifenyl)-2-azetidinon; trans-l-(4-fluorfenyl)-3-[[2-(4-fluorfenyl)-2-hydroxietyl]tio]-4-(4-hydroxifenyl)-2-15 azetidinon; (3R,4R)-l-(4-fluorfenyl)-3-[[2-(4-fluorfenyl)-2-oxoetyl]sulfinyl]-4-(4-hydroxifenyl)-2- azetidinon; 1- (4-fluorfenyl)-3(R)-[[2-(4-fluorfenyl)-2(R)-hydroxietyl]sulfinyl]-4(R)-(4-hydroxi-fenyl)-2-azetidinon; 20 l-(4-fluorfenyl)-3(R)-[[2-(4-fluorfenyl)-2(S)-hydroxietyl]sulfinyl]-4(R)-(4-hydroxi- fenyl)-2-azetidinon; (3R,4R)-trans-l-(4-fluorfenyl)-3-[[2-(2-tienyl)-2-oxoetyl]tio]-4-(4-hydroxi-fenyl)-2- azetidinon; (3R,4R)-trans-l-(4-fluorfenyl)-3-[[2-(3-tienyl)-2-oxoetyl]tio]-4-(4-hydroxi-fenyl)-2- • »» v : 25 azetidinon; :,: ; (3R/4R)-trans-l-(4-fluorfenyl)-3-[[2-(3-pyridnyl)-2-oxoetyl]tio]-4-(4-hydroxi-fenyl)- 2- azetidinon; . ·. : (3R,4R)-trans-l-(4-fIuorfenyl)-3-[[2-(4-pyridnyl)-2-oxoetyl]tio]-4-(4-hydroxi-fenyl)- 2-azetidinon; 30 (3R/4R)-trans-l-(4-fluorfenyl)-3-[[2-(2-pyridnyl)-2-oxoetyl]tio]-4-(4-hydroxi-fenyl)- 2-azetidinon; (3R,4R)-trans-l-(4-fluorfenyl)-3-[[2-hydroxi-2-(3-tienyl)etyl]tio]-4-(4-hyd-roxifenyl)-i 2-azetidinon; : ’'': (3R,4R)-trans-l-(4-fluotfenyl)-3-[[2-hydroxi-2-(4-pyridnyl)etyl]tio]-4-(4-hydroxi- 35 fenyl)-2-azetidinon; ‘. (3S,4R)-cis-l-(4-fluorfenyl)-3-[[2-(4-fluorfenyl)-2-oxoetyl]tio]-4-(4-hydroxi-fenyl)-2- azetidinon; ‘ : (3S,4R)-cis-l-(4-fluorfenyl)-3-[[2-(4-fluorfenyl)-2-hydroxietyl]tio]-4-(4-hydroxifenyl)- :"'; 2-azetidinon. 116220 40
6. Farmaceutiskt blandning för profylax och skötsel av ateroskleros, eller för sänk-ning av plasmans kolesterolnivler, kännetecknad därav, att den innehäller en förening enligt vilket som heist av patentkraven 1, 2, 3, 4 eller 5 ensam eller i kom-bination med en biosyntesinhibitor för kolesterol, och en farmaceutiskt godtagbar 5 bärare.
7. Förfarande för framställning av en farmaceutisk blandning enligt patentkravet 6, kännetecknad därav, att en förening enligt vilket som heist av patentkraven 1, 2, 3, 4 eller 5 blandas ensam eller i kombination med en biosyntesinhibitor för koleste- 10 rol, med en farmaceutiskt godtagbar bärare.
8. Användningen av en förening enligt vilket som heist av patentkraven 1, 2, 3, 4 eller 5 för framställning av ett läkemedel för skötsel och profylax av ateroskleros, eller sänkning av plasmans kolesterolniväer, kännetecknad därav, att den omfat- 15 tar en förening enligt vilket som heist av patentkraven 1, 2, 3, 4 eller 5 ensam eller i kombination med en biosyntesinhibitor för kolesterol och en farmaceutiskt godtagbar bärare.
9. Kitt, som innehäller i separata behällare en enskilda förpackning av farmaceutiska 20 blandningar för skötsel och profylax av ateroskleros eller sänkning av plasmans ko- lesterolniväer, kännetecknad därav, att i en behällare finns en effektiv mängd av en biosyntesinhibitor för kolesterol i en farmaceutiskt godtagbar bärare, och i den andra behällaren en effektiv mängd av en förening enligt vilket som heist av patentkraven 1, 2, 3, 4 eller 5 i en farmaceutiskt godtagbar bärare. v : 25
FI972099A 1994-11-18 1997-05-16 Svavel-substituerade azetidinonföreningar som är nyttiga som hypkolesterolemiska ämnen FI116220B (sv)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US08/342,197 US5624920A (en) 1994-11-18 1994-11-18 Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents
US34219794 1994-11-18
US46361995 1995-06-05
US08/463,619 US5633246A (en) 1994-11-18 1995-06-05 Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents
US9514134 1995-11-15
PCT/US1995/014134 WO1996016037A1 (en) 1994-11-18 1995-11-15 Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents

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FI972099A0 FI972099A0 (sv) 1997-05-16
FI972099A FI972099A (sv) 1997-05-16
FI116220B true FI116220B (sv) 2005-10-14

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US (2) US5633246A (sv)
EP (1) EP0792264B1 (sv)
JP (1) JP2908031B2 (sv)
KR (1) KR100235806B1 (sv)
CN (1) CN1083833C (sv)
AT (1) ATE213726T1 (sv)
AU (1) AU698750B2 (sv)
BR (1) BR9509669A (sv)
CA (1) CA2205202C (sv)
CZ (1) CZ289033B6 (sv)
DE (1) DE69525643T2 (sv)
DK (1) DK0792264T3 (sv)
ES (1) ES2169162T3 (sv)
FI (1) FI116220B (sv)
HK (1) HK1002558A1 (sv)
HU (1) HU227672B1 (sv)
MX (1) MX9703577A (sv)
NO (1) NO308468B1 (sv)
NZ (1) NZ296720A (sv)
PL (1) PL184310B1 (sv)
PT (1) PT792264E (sv)
RU (1) RU2159243C2 (sv)
SK (1) SK283860B6 (sv)
UA (1) UA54381C2 (sv)
WO (1) WO1996016037A1 (sv)

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KR100235806B1 (ko) 2000-02-01
JPH09512833A (ja) 1997-12-22
DE69525643T2 (de) 2002-09-26
DE69525643D1 (de) 2002-04-04
KR970707092A (ko) 1997-12-01
UA54381C2 (uk) 2003-03-17
SK283860B6 (sk) 2004-03-02
PT792264E (pt) 2002-07-31
HU227672B1 (en) 2011-11-28
RU2159243C2 (ru) 2000-11-20
EP0792264B1 (en) 2002-02-27
US5633246A (en) 1997-05-27
ES2169162T3 (es) 2002-07-01
NO972272D0 (no) 1997-05-16
BR9509669A (pt) 1997-10-28
NZ296720A (en) 1999-03-29
NO972272L (no) 1997-05-16
CZ289033B6 (cs) 2001-10-17
US5744467A (en) 1998-04-28
AU4140196A (en) 1996-06-17
EP0792264A1 (en) 1997-09-03
CA2205202C (en) 2002-01-08
FI972099A0 (sv) 1997-05-16
DK0792264T3 (da) 2002-04-22
NO308468B1 (no) 2000-09-18
ATE213726T1 (de) 2002-03-15
AU698750B2 (en) 1998-11-05
WO1996016037A1 (en) 1996-05-30
PL184310B1 (pl) 2002-09-30
CN1174548A (zh) 1998-02-25
FI972099A (sv) 1997-05-16
SK61697A3 (en) 1997-12-10
CN1083833C (zh) 2002-05-01
HK1002558A1 (en) 1998-09-04
CZ148697A3 (en) 1997-11-12
PL320092A1 (en) 1997-09-15
CA2205202A1 (en) 1996-05-30
HUT77088A (hu) 1998-03-02
MX9703577A (es) 1997-08-30
JP2908031B2 (ja) 1999-06-21

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