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SI9111427B - Heterociklične spojine - Google Patents

Heterociklične spojine Download PDF

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Publication number
SI9111427B
SI9111427B SI9111427A SI9111427A SI9111427B SI 9111427 B SI9111427 B SI 9111427B SI 9111427 A SI9111427 A SI 9111427A SI 9111427 A SI9111427 A SI 9111427A SI 9111427 B SI9111427 B SI 9111427B
Authority
SI
Slovenia
Prior art keywords
group
methoxy
alkyl
compound
compounds according
Prior art date
Application number
SI9111427A
Other languages
English (en)
Other versions
SI9111427A (en
Inventor
Alcide Perboni
Tino Rossi
Giorgio Tarzia
Giovanni Gaviraghi
Antonella Ursini
Original Assignee
Glaxo S.P.A.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB909018330A external-priority patent/GB9018330D0/en
Priority claimed from GB919104770A external-priority patent/GB9104770D0/en
Application filed by Glaxo S.P.A. filed Critical Glaxo S.P.A.
Publication of SI9111427A publication Critical patent/SI9111427A/sl
Publication of SI9111427B publication Critical patent/SI9111427B/sl

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D477/00Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Communicable Diseases (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heat Sensitive Colour Forming Recording (AREA)

Claims (12)

  1. Patentni zahtevki 1. Spojine s splošno formulo (I):
    označene s tem, da v formuli R; predstavlja skupino: — CH.O.C. (0 ) p. R 5 R4 0 kjer predstavlja vodik ali C; ^alkilno skupino; je p nič ali ena; R5 predstavlja skupino, ki je izbrana iz C; galkila, C5 ^cikloalkila, ki je v danem primeru substituiran s C; jalkilno skupino, fenila ali Cy^alkila, ki je substituiran s C; 5alkoksi skupino; in R2 predstavlja skupino OR5, kjer R^ predstavlja C; 5alkilno skupino.
  2. 2. Spojine po zahtevku 1, označene s tem, da imajo konfiguracijo: OH H
    (v kateri sta R; in R2 kot je definirano v zahtevku 1). • ec <* « · e r e 0 f • c <* * n e e λ r c *· r r r o r r r r r r r r c < 2
  3. 3. Spojine po zahtevku 1 ali zahtevku 2, označene s tem, da R4 predstavlja vodikov atom ali metilno skupino.
  4. 4. Spojine po kateremkoli od zahtevkov 1 do 3, označene s tem, da R2 predstavlja metoksi ali etoksi skupino.
  5. 5. Spojine po kateremkoli od zahtevkov 1 do 4, označene s tem, da R5 predstavlja metil, etil, izopropil, t-butil, 1-metoksi-l-metiletil, fenil, cikloheksil ali 4-etil-cikloheksilno skupino.
  6. 6. Spojine po zahtevku 2, označene s tem, da R^ predstavlja vodikov atom ali metilno skupino; je R5 skupina, ki je izbrana iz C/ 4alkila, C5 6cikloalkila, ki je v danem primeru substituiran s Cy 2alkilno skupino, fenila in Cy ^alkila, ki je substituiran z metoksi; in je R2 metoksi skupina.
  7. 7. Pivaloiloksimetil, 1-pivaloiloksietil, acetoksimetil, 1-acetoksietil, 1-metoksi-1-metiletilkarboniloksimetil, l-(l-metoksi-l-metiletilkarboniloksi)etil, 1-benzoil-oksietil, 1-izopropoksikarboniloksimetil in 1 - (4-etilcikloheksiloksikarboniloksi) -etiles tri (4S,8S,9R,10S,12R)-4-metoksi-10-(l-hidroksietil)-ll-okso-l-azatriciklo[7.2.0.03,s]u-ndec-2-en-2-karboksilne kisline.
  8. 8.1-cikloheksiloksikarboniloksietil (4S,8S,9R,10S,12R)-4-metoksi-10-(l-hidroksi-etil)-ll-okso-l-azatriciklo[7.2.0.0.i'5]undec-2-en-2-karboksilat.
  9. 9. Spojine po kateremkoli od zahtevkov 1 do 8 za uporabo v terapiji ali profilaksi sistemskih bakterijskih infekcij na organizmu ljudi in živali.
  10. 10. Uporaba spojine po kateremkoli od zahtevkov 1 do 8 v proizvodnji terapevtskega sredstva za zdravljenje ali profilakso sistemskih bakterijskih infekcij na organizmu ljudi ali živali.
  11. 11. Farmacevtski pripravki, označeni s tem, da obsegajo spojino po kateremkoli od zahtevkov 1 do 8 v zmesi z enim ali več fiziološko sprejemljivimi nosilci ali sestavinami. 0 * • · e r r r * «
  12. 12. Postopek za pripravo spojine s splošno formulo (I) po zahtevku 1, označen s tem, da obsega ali (a) reakcijo spojine s splošno formulo (II): 0 * • · e r r r * «
    v kateri je R2 kot je definirano v zahtevku 1 in Ra predstavlja atom vodika ali zaščitno skupino za hidroksil, ali njene soli ali njenega reaktivnega derivata s sredstvom za es-terifikacijo, ki služi za uvedbo skupine R;, kot je definirano v zahtevku 1, ali (b) cik-lizacijo spojine s splošno formulo (III):
    C 0 0 R (III) v kateri sta R; in R2 kot je definirano v zahtevku 1, je Rq zaščitna skupina za hidroksil in je Y atom kisika ali fosfinska skupina in nakar, če je potrebno ali če želimo, reakcijo produkta, da zamenjamo Rfl zaščitno skupino za hidroksil z atomom vodika in/ali ločitev določenega želenega izomera spojine s splošno formulo (I) od enega ali več njenih izomerov. Za GLAXO S.p.A.:
SI9111427A 1990-08-21 1991-08-20 Heterociklične spojine SI9111427B (sl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB909018330A GB9018330D0 (en) 1990-08-21 1990-08-21 Heterocyclic compounds
GB919104770A GB9104770D0 (en) 1991-03-07 1991-03-07 Heterocyclic compounds
YU142791A YU48079B (sh) 1990-08-21 1991-08-20 Heterociklična jedinjenja

Publications (2)

Publication Number Publication Date
SI9111427A SI9111427A (en) 1996-12-31
SI9111427B true SI9111427B (sl) 2000-10-31

Family

ID=26297540

Family Applications (1)

Application Number Title Priority Date Filing Date
SI9111427A SI9111427B (sl) 1990-08-21 1991-08-20 Heterociklične spojine

Country Status (32)

Country Link
US (1) US5587374A (sl)
EP (1) EP0495953B1 (sl)
JP (2) JP3151215B2 (sl)
KR (1) KR0169147B1 (sl)
CN (1) CN1030917C (sl)
AP (1) AP238A (sl)
AT (1) ATE106887T1 (sl)
AU (1) AU647178B2 (sl)
CA (1) CA2067741C (sl)
CY (1) CY2037A (sl)
CZ (1) CZ280942B6 (sl)
DE (1) DE69102415T2 (sl)
DK (1) DK0495953T3 (sl)
ES (1) ES2054502T3 (sl)
FI (1) FI97136C (sl)
HK (1) HK19495A (sl)
HR (1) HRP940556B1 (sl)
HU (2) HUT61024A (sl)
IE (1) IE66122B1 (sl)
IL (1) IL99248A (sl)
MX (1) MX9100743A (sl)
MY (1) MY106997A (sl)
NO (1) NO300176B1 (sl)
NZ (1) NZ239474A (sl)
OA (1) OA09578A (sl)
PL (1) PL169425B1 (sl)
PT (1) PT98729B (sl)
SG (1) SG169494G (sl)
SI (1) SI9111427B (sl)
SK (1) SK278470B6 (sl)
WO (1) WO1992003437A1 (sl)
YU (1) YU48079B (sl)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9104838D0 (en) * 1991-03-07 1991-04-17 Glaxo Spa Heterocyclic compounds
AP294A (en) * 1992-08-31 1993-12-28 Glaxo Spa "10-(1-Hydroxyethyl)-11-oxo-1-azatricyclo-(7.2.0.0.3.8) undec-2-ene-2-carboxylic acid derivatives".
GB9218781D0 (en) * 1992-09-04 1992-10-21 Glaxo Spa Heterocyclic derivatives
IN188720B (sl) * 1997-11-06 2002-11-02 Panacea Biotec Ltd
CA2465336C (en) 2001-11-05 2009-04-28 Sumitomo Pharmaceuticals Co., Ltd. Novel carbapenem compounds
JPWO2004089954A1 (ja) * 2003-04-08 2006-07-06 大日本住友製薬株式会社 新規なカルバペネム化合物
WO2006025475A1 (ja) * 2004-09-03 2006-03-09 Dainippon Sumitomo Pharma Co., Ltd. 新規なカルバペネム化合物
US20090029964A1 (en) * 2005-03-25 2009-01-29 Makoto Sunagawa Novel carbapenem compound
EP2085084A1 (en) * 2008-01-29 2009-08-05 LEK Pharmaceuticals D.D. Use of inhibitor of beta-lactamases and its combination with beta-lactam antibiotics
EP2135871A1 (en) * 2008-06-18 2009-12-23 LEK Pharmaceuticals D.D. New trinem antibiotics and inhibitors of beta-lactamases
PL3621609T3 (pl) 2017-05-08 2022-11-14 Glaxosmithkline Intellectual Property Development Limited Sanfetrinem lub jego sól lub ester do stosowania w leczeniu zakażenia prątkami

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1425571A (en) * 1972-03-13 1976-02-18 Astra Laekemedel Ab Penicillins and cephaosporins
GB1433131A (en) * 1972-03-13 1976-04-22 Astra Laekemedel Ab Penicillins
DE2811514A1 (de) * 1977-03-19 1978-09-21 Beecham Group Ltd Ester der 7-oxo-1-azabicyclo eckige klammer auf 3.2.0 eckige klammer zu hept- 2-en-2-carbonsaeure und deren derivate, verfahren zur herstellung dieser verbindungen und diese verbindungen enthaltende pharmazeutische zubereitungen
US4374849A (en) * 1981-09-14 1983-02-22 Merck & Co., Inc. 6-Amidocyclonocardicins
US4374848A (en) * 1981-09-14 1983-02-22 Merck & Co., Inc. 6-(1-Hydroxyethyl)cyclonocardicin
CZ285778B6 (cs) * 1989-09-08 1999-11-17 Glaxo S.P.A. Kyselina 10-(1-hydroxyethyl)-11-oxo-1-azatricyklo/7,2,0,03,8/-undec-2en-2-karboxylová a její deriváty, způsob jejich výroby, použití pro výrobu farmaceutických prostředků a farmaceutické prostředky s jejich obsahem
AU636913B2 (en) * 1989-10-11 1993-05-13 Takeda Chemical Industries Ltd. Tricyclic carbapenem compounds
GB9104832D0 (en) * 1991-03-07 1991-04-17 Glaxo Spa Heterocyclic compounds
GB9104838D0 (en) * 1991-03-07 1991-04-17 Glaxo Spa Heterocyclic compounds

Also Published As

Publication number Publication date
PT98729B (pt) 1999-01-29
NZ239474A (en) 1994-06-27
IE66122B1 (en) 1995-12-13
HUT61024A (en) 1992-11-30
MX9100743A (es) 1992-04-01
ES2054502T3 (es) 1994-08-01
CZ121392A3 (en) 1993-04-14
YU142791A (sh) 1994-01-20
EP0495953A1 (en) 1992-07-29
HRP940556B1 (en) 2000-06-30
FI921717A0 (fi) 1992-04-16
OA09578A (en) 1993-01-31
AP9100320A0 (en) 1991-10-31
SK121392A3 (en) 1997-06-04
SG169494G (en) 1995-04-28
SI9111427A (en) 1996-12-31
WO1992003437A1 (en) 1992-03-05
HU211584A9 (en) 1995-12-28
IL99248A (en) 1996-01-31
NO921521L (no) 1992-06-22
PL169425B1 (pl) 1996-07-31
AU8421291A (en) 1992-03-17
IE912944A1 (en) 1992-02-26
YU48079B (sh) 1997-01-08
IL99248A0 (en) 1992-07-15
CN1030917C (zh) 1996-02-07
JP3151215B2 (ja) 2001-04-03
KR0169147B1 (en) 1999-01-15
DK0495953T3 (da) 1994-07-18
DE69102415T2 (de) 1994-10-13
CZ280942B6 (cs) 1996-05-15
AU647178B2 (en) 1994-03-17
NO921521D0 (no) 1992-04-15
EP0495953B1 (en) 1994-06-08
JP3461786B2 (ja) 2003-10-27
ATE106887T1 (de) 1994-06-15
SK278470B6 (en) 1997-06-04
HK19495A (en) 1995-02-17
PT98729A (pt) 1992-07-31
HRP940556A2 (en) 1996-06-30
FI921717L (fi) 1992-04-16
US5587374A (en) 1996-12-24
JPH05502044A (ja) 1993-04-15
JP2000351730A (ja) 2000-12-19
CA2067741A1 (en) 1992-02-22
HU9201303D0 (en) 1992-07-28
FI97136B (fi) 1996-07-15
CY2037A (en) 1998-02-20
MY106997A (en) 1995-08-30
KR920702361A (ko) 1992-09-03
CN1060094A (zh) 1992-04-08
AP238A (en) 1993-02-04
DE69102415D1 (de) 1994-07-14
NO300176B1 (no) 1997-04-21
CA2067741C (en) 2002-01-01
FI97136C (fi) 1996-10-25

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