NO934541L - LHRH analogues - Google Patents

LHRH analogues

Info

Publication number
NO934541L
NO934541L NO934541A NO934541A NO934541L NO 934541 L NO934541 L NO 934541L NO 934541 A NO934541 A NO 934541A NO 934541 A NO934541 A NO 934541A NO 934541 L NO934541 L NO 934541L
Authority
NO
Norway
Prior art keywords
rer
moiety
methotrexoyl
trp
arg
Prior art date
Application number
NO934541A
Other languages
Norwegian (no)
Other versions
NO934541D0 (en
Inventor
Andrew V Schally
Tamas Janaky
Atilla Juhasz
Sandor Bajusz
Original Assignee
Univ Tulane
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 PCT/US1991/004264 external-priority patent/WO1992022322A1/en
Application filed by Univ Tulane filed Critical Univ Tulane
Publication of NO934541D0 publication Critical patent/NO934541D0/en
Publication of NO934541L publication Critical patent/NO934541L/en

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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

LHRH analoger som inneholder cytotoksiske deler, har innvirkning på frigjøring av gonadotropiner fra hypofysen i pattedyr (har høy agonistisk eller antagonistisk aktivitet) og har antineoplastisk virkning, er beskrevet. Forbindelsene er representert ved formelen (I): X .R1,R2,R3-Ser-R5-R6(0)-Leu-Arg-Pro-1NH2, hvorer pGlu eller D-Nal(2), Rer His eller D-Phe(4Cl), Rer Trp, D-Trp, D-Pal(3), Rer Tyr. eller Arg, R*> er D-Lys eker D-Orn, Rer Gly eller D-Ala. X er hydrogen eller en lavere alkanoylgruppe med 2-5 karbonatomer, 0 er en cytotoksisk del med formelen -eller -() eller -B(0)ekker -B(A), hvor A er -NH-(CH2 )n-C0 eller -0C-(CH2 )n-C0 hvor n er 2-6, B er -NH-CH-(C)-CH(NH)-(C)-C0 hvor m er 0 eller 1, j n er 0 eller 1, -CO delen til A- og B- er bundet til en aminogruppe på Rog i gruppen B(A0)er -CO delen til A- bundet til en aminogruppe på B, Qer D eller L-Mel,cyklopropanalkanoyl, aziridin-2-karbonyl, epoksyalkyl eller 1,4-naftoquinon-5-oksykarbonyl-etyl , 0er Q, anthraquinonylalkoksy ellerdeoksorubicinyl, 0er 0, mitomicinyl, esperamycinyl eller methotreksoyl, Qer 0ekker methotreksoyl og farmasøytiske akseptable salter derav og fremgangsmåter for anvendelse av disse forbindelsene er beskrevet.LHRH analogs that contain cytotoxic moieties, have an effect on the release of gonadotropins from the pituitary gland in mammals (have high agonistic or antagonistic activity) and have antineoplastic activity have been described. The compounds are represented by the formula (I): X, R1, R2, R3-Ser-R5-R6 (O) -Leu-Arg-Pro-1NH2, wherein pGlu or D-Nal (2), Rer His or D-Phe (4Cl), Rer Trp, D-Trp, D-Pal (3), Rer Tyr. or Arg, R *> is D-Lys or D-Orn, Rer Gly or D-Ala. X is hydrogen or a lower alkanoyl group having 2-5 carbon atoms, 0 is a cytotoxic moiety of the formula -or - () or -B (0) or -B (A), where A is -NH- (CH 2) n -CO or -OC- (CH 2) n -CO where n is 2-6, B is -NH-CH- (C) -CH (NH) - (C) -CO where m is 0 or 1, jn is 0 or 1 , -CO moiety to A- and B- is attached to an amino group on Rog in group B (A0) is -CO moiety to A- attached to an amino group on B, Qer D or L-Mel, cyclopropanalkanoyl, aziridine-2- carbonyl, epoxyalkyl or 1,4-naphthoquinone-5-oxycarbonyl-ethyl, or Q, anthraquinonyl alkoxy or deoxorubicinyl, or Q, mitomicinyl, esperamycinyl or methotrexoyl, Qs or methotrexoyl and pharmaceutically acceptable salts are described therein.

NO934541A 1991-06-14 1993-12-10 LHRH analogues NO934541L (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US1991/004264 WO1992022322A1 (en) 1990-04-06 1991-06-14 Lhrh analogs

Publications (2)

Publication Number Publication Date
NO934541D0 NO934541D0 (en) 1993-12-10
NO934541L true NO934541L (en) 1994-02-07

Family

ID=22225603

Family Applications (1)

Application Number Title Priority Date Filing Date
NO934541A NO934541L (en) 1991-06-14 1993-12-10 LHRH analogues

Country Status (2)

Country Link
FI (1) FI935598A0 (en)
NO (1) NO934541L (en)

Also Published As

Publication number Publication date
FI935598A (en) 1993-12-13
NO934541D0 (en) 1993-12-10
FI935598A0 (en) 1993-12-13

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