NO934541L - LHRH analoger - Google Patents
LHRH analogerInfo
- 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
Links
- XLXSAKCOAKORKW-UHFFFAOYSA-N gonadorelin Chemical class C1CCC(C(=O)NCC(N)=O)N1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)CNC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 XLXSAKCOAKORKW-UHFFFAOYSA-N 0.000 title abstract 2
- 125000003277 amino group Chemical group 0.000 abstract 2
- -1 aziridine-2- carbonyl Chemical group 0.000 abstract 2
- 231100000433 cytotoxic Toxicity 0.000 abstract 2
- 230000001472 cytotoxic effect Effects 0.000 abstract 2
- ODHCTXKNWHHXJC-VKHMYHEASA-N 5-oxo-L-proline Chemical compound OC(=O)[C@@H]1CCC(=O)N1 ODHCTXKNWHHXJC-VKHMYHEASA-N 0.000 abstract 1
- AHLPHDHHMVZTML-SCSAIBSYSA-N D-Ornithine Chemical compound NCCC[C@@H](N)C(O)=O AHLPHDHHMVZTML-SCSAIBSYSA-N 0.000 abstract 1
- QNAYBMKLOCPYGJ-UWTATZPHSA-N D-alanine Chemical compound C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 abstract 1
- KDXKERNSBIXSRK-RXMQYKEDSA-N D-lysine Chemical compound NCCCC[C@@H](N)C(O)=O KDXKERNSBIXSRK-RXMQYKEDSA-N 0.000 abstract 1
- COLNVLDHVKWLRT-MRVPVSSYSA-N D-phenylalanine Chemical compound OC(=O)[C@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-MRVPVSSYSA-N 0.000 abstract 1
- QIVBCDIJIAJPQS-SECBINFHSA-N D-tryptophane Chemical compound C1=CC=C2C(C[C@@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-SECBINFHSA-N 0.000 abstract 1
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 abstract 1
- 102000006771 Gonadotropins Human genes 0.000 abstract 1
- 108010086677 Gonadotropins Proteins 0.000 abstract 1
- 206010062767 Hypophysitis Diseases 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 230000001270 agonistic effect Effects 0.000 abstract 1
- 230000003042 antagnostic effect Effects 0.000 abstract 1
- 230000000118 anti-neoplastic effect Effects 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000002622 gonadotropin Substances 0.000 abstract 1
- 229940094892 gonadotropins Drugs 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 210000003635 pituitary gland Anatomy 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Landscapes
- 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.
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 (no) | 1993-12-10 |
| NO934541L true NO934541L (no) | 1994-02-07 |
Family
ID=22225603
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO934541A NO934541L (no) | 1991-06-14 | 1993-12-10 | LHRH analoger |
Country Status (2)
| Country | Link |
|---|---|
| FI (1) | FI935598A0 (no) |
| NO (1) | NO934541L (no) |
-
1993
- 1993-12-10 NO NO934541A patent/NO934541L/no unknown
- 1993-12-13 FI FI935598A patent/FI935598A0/fi not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| FI935598A7 (fi) | 1993-12-13 |
| FI935598A0 (fi) | 1993-12-13 |
| NO934541D0 (no) | 1993-12-10 |
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