FI105817B - Förfarande för framställning av terapeutiskt användbara peptidföreningar - Google Patents

Förfarande för framställning av terapeutiskt användbara peptidföreningar Download PDF

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Publication number
FI105817B
FI105817B FI935191A FI935191A FI105817B FI 105817 B FI105817 B FI 105817B FI 935191 A FI935191 A FI 935191A FI 935191 A FI935191 A FI 935191A FI 105817 B FI105817 B FI 105817B
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Finland
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group
neu
formula
acid
preparation
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FI935191A
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English (en)
Finnish (fi)
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FI935191A0 (fi
FI935191A (fi
Inventor
Ursula Habenicht
Paul Thamm
Alessandro Lobbia
Thomas Brumby
Johann Mulzer
Fridtjofy Schroeder
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Schering Ag
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Publication of FI935191A publication Critical patent/FI935191A/fi
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Publication of FI105817B publication Critical patent/FI105817B/sv

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/23Luteinising hormone-releasing hormone [LHRH]; Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Endocrinology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (7)

1 I 15 kännetecknat av att peptidisyntesen utförs genom användning en fastfas- eller lösningsteknik pä ett i och för sig känt sätt.
1. Förfarande för framställning av terapeutiskt an-vändbara peptidföreningar med formeln 5 X-Xi-X2-X3_L-Ser-L-Tyr-X6-L-Leu-X8-L-Pro-Xio (I) 1234 56 78 9 10 väri
10 X är en naftoyl-, naftylacetyl-, naftylpropionyl- eller bensoylgrupp eller en acylgrupp med 1-7 kolatomer, Xi är D-(1)-Nai, D-(2)-Nal, D-Phe, D-(4-Y)-Phe, D-(3)-Qal eller en direkt bindning, varvid Y är en F-, Br- eller Cl-grupp,
15 X2 är D-Phe, D-(4-Y)-Phe eller en direkt bindning, varvid Y är ovan definierad, X3 är D-Trp, D-Phe, D-(4-Y)-Phe, D-(3)-Pal, D-(2)-Nai eller en direkt bindning, varvid Y betecknar detsairana som Xi ovan, 20 Χβ är D-Cit, D-Hci, D-Orn, D-Lys eller D-Neu, X8 är L-Orn, L-Arg, L-Lys eller L-Neu, varvid ät-minstone en av rester Χβ och X8 är Neu, och X10 är D-Ala-NH2, Gly-NH2, azaglysin, -NHEt eller -NH(CO)NH2, varvid Neu är en grupp med formeln IX eller IV 25 _/2|\ |H2 fH2 W CH«S /CH2 ICH J r . N ΠΧ) (IV) »o cch.j , il jU i 2 nl I 0 VV I o H väri Ζχ är en grupp 40 105817 XCH X / ! ' / ' \ \ \ 5 /S ' /”« eller en direkt bindning, n är 1 - 8, ni är 3 - 6 och 10 W är en rest O* eller On
2. Förfarande enligt patentkrav 1, kanne-20 tecknat av att Neu är en grupp raed formeln X: 0 / \ |H2 fH2 c\ /CH^ - 25 Γ 1X1 lCH,l , '/y I 0 H väri ni är 3 - 6. . 30
3. Förfarande enligt patentkrav 2, kanne- ·’ tecknat av att Neu är en rest med formeln 41 O / fH2 fH2 CV /CH* } YY I o H 10
4. Förfarande enligt patentkrav 3, kännetecknat av att Neu är eller Xs-
5. Förfarande enligt patentkrav 1, kännetecknat av att Neu är en grupp med for-meln XIII: 15 „_ O J (XIII) 20 f yV H
6. Förfarande enligt nägot av patentkraven 1-5, 25 kännetecknat av att X är en etanoylgrupp, Xi är D-Nal, X2 är D-Cpa, * X3 är D-Pal och
30 Xio är D-Ala-NH2.
7. Förfarande enligt patentkrav 1-4, kännetecknat av att peptiden Ac-D-Nal-D-Cpa-D-Pal-Ser-Tyr-D-Cit-Leu-Ahx(Mor)-Pro-D-AlaNH2 framställs.
FI935191A 1991-05-24 1993-11-23 Förfarande för framställning av terapeutiskt användbara peptidföreningar FI105817B (sv)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE4117507 1991-05-24
DE4117507A DE4117507A1 (de) 1991-05-24 1991-05-24 Verfahren zur herstellung von n(pfeil hoch)6(pfeil hoch)-substituierten lysin-derivaten
DE9200427 1992-05-22
PCT/DE1992/000427 WO1992020711A2 (de) 1991-05-24 1992-05-22 Lhrh-antagonisten und zwischenprodukte

Publications (3)

Publication Number Publication Date
FI935191A0 FI935191A0 (fi) 1993-11-23
FI935191A FI935191A (fi) 1993-11-23
FI105817B true FI105817B (sv) 2000-10-13

Family

ID=6432667

Family Applications (2)

Application Number Title Priority Date Filing Date
FI935191A FI105817B (sv) 1991-05-24 1993-11-23 Förfarande för framställning av terapeutiskt användbara peptidföreningar
FI991441A FI114026B (sv) 1991-05-24 1999-06-24 Peptidföreningar, speciellt LHRH-antagonister, som används vid fertilitetskontroll

Family Applications After (1)

Application Number Title Priority Date Filing Date
FI991441A FI114026B (sv) 1991-05-24 1999-06-24 Peptidföreningar, speciellt LHRH-antagonister, som används vid fertilitetskontroll

Country Status (14)

Country Link
US (1) US5527777A (sv)
EP (1) EP0668874B1 (sv)
JP (1) JP3370668B2 (sv)
AT (1) ATE170190T1 (sv)
AU (1) AU667038B2 (sv)
CA (1) CA2109830C (sv)
DE (3) DE4117507A1 (sv)
DK (1) DK0668874T3 (sv)
ES (1) ES2123554T3 (sv)
FI (2) FI105817B (sv)
HU (1) HU219912B (sv)
NO (1) NO311725B1 (sv)
RU (1) RU2124023C1 (sv)
WO (1) WO1992020711A2 (sv)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4801577A (en) * 1987-02-05 1989-01-31 Syntex (U.S.A.) Inc. Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists
US5843901A (en) * 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
US5916582A (en) * 1996-07-03 1999-06-29 Alza Corporation Aqueous formulations of peptides
US5932547A (en) * 1996-07-03 1999-08-03 Alza Corporation Non-aqueous polar aprotic peptide formulations
US5981489A (en) * 1996-07-18 1999-11-09 Alza Corporation Non-aqueous protic peptide formulations
US6455499B1 (en) 1999-02-23 2002-09-24 Indiana University Foundation Methods for treating disorders associated with LHRH activity
DE19911771B4 (de) * 1999-03-17 2006-03-30 Zentaris Gmbh LHRH-Antagonist, Verfahren zu seiner Herstellung und seiner Verwendung
GB201009603D0 (en) * 2010-06-08 2010-07-21 Cambridge Entpr Ltd Anti-inflammatory agent
AR122446A1 (es) * 2020-04-29 2022-09-14 Medimmune Llc Composiciones y métodos para suministrar agentes farmacéuticamente activos

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4667014A (en) * 1983-03-07 1987-05-19 Syntex (U.S.A.) Inc. Nonapeptide and decapeptide analogs of LHRH, useful as LHRH antagonists
US4801577A (en) * 1987-02-05 1989-01-31 Syntex (U.S.A.) Inc. Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists
US4800191A (en) * 1987-07-17 1989-01-24 Schally Andrew Victor LHRH antagonists
US4935491A (en) * 1987-08-24 1990-06-19 Board Of Regents, The University Of Texas System Effective antagonists of the luteinizing hormone releasing hormone which release negligible histamine
IE902446A1 (en) * 1989-07-26 1991-02-13 Abbott Lab Peptidyl aminodiol renin inhibitors

Also Published As

Publication number Publication date
HU9303324D0 (en) 1994-03-28
FI935191A0 (fi) 1993-11-23
JPH06508115A (ja) 1994-09-14
US5527777A (en) 1996-06-18
CA2109830A1 (en) 1992-11-26
JP3370668B2 (ja) 2003-01-27
ATE170190T1 (de) 1998-09-15
CA2109830C (en) 2003-04-08
EP0668874B1 (de) 1998-08-26
EP0668874A1 (de) 1995-08-30
NO934237D0 (no) 1993-11-23
FI991441A0 (sv) 1999-06-24
DE59209476D1 (de) 1998-10-01
AU1887992A (en) 1992-12-30
DE4291426D2 (de) 1994-02-17
WO1992020711A3 (de) 1993-03-18
ES2123554T3 (es) 1999-01-16
RU2124023C1 (ru) 1998-12-27
WO1992020711A2 (de) 1992-11-26
HU219912B (hu) 2001-09-28
FI935191A (fi) 1993-11-23
HUT65732A (en) 1994-07-28
NO934237L (no) 1993-11-23
AU667038B2 (en) 1996-03-07
DK0668874T3 (da) 1999-05-25
FI114026B (sv) 2004-07-30
FI991441A (sv) 1999-06-24
NO311725B1 (no) 2002-01-14
DE4117507A1 (de) 1992-11-26

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