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4528189 Urotensin peptides
268
PATENT
spectrum: Maximum absorption is not recognized in the range of 240-400 nm: 8. Outward form: White or faint brown, amorphous powder; 9. Solubility: (a) Soluble in water: (b) Insoluble in methanol, ethanol, acetone, ethyl acetate, diethyl ether, hexane and chloroform: I0. Color reactions: Positive to the following reactions: (a) anthrone-sulfuric acid reaction: (b) Molisch's reaction; (c) skatol reaction: and (d) Bial's reaction; Negative to the follov.ing reactions: (a) ninhydrin reaction: (b) 2A-DNP reaction; (c) SelivanofFs reaction: (d) naphthoresorcinol reaction: and (e) carbazolsulfuric acid reaction; I I Component sugars: Arabinose and galactose: 12. ttomogeneity: Homogeneity is proved according to uhracentrifugation, electrophoresis and gel filtration.
4528189 UROTENSIN PEPTIDES Karl P Lederis, Keith L MacCannell. Jean E Rivier, Calgary, Canada assigned to The Salk Institute For Biological Studies UI (Urotensin I) or white sucker urotensin, obtained from Catostomus commersoni, has the formula: H-Asn-Asp-Asp-Pro-Pro-lle-Ser-lleAsp-Leu-Thr-Phe-His-Leu-Leu-Arg-Asn-Metlle-Glu-Met-Ala-Arg-lle-Glu-Asn-Glu-ArgGId-GIn-Ala-Gly-Leu-Asn-Arg-Lys-Ty r-LeuAsp-GIu-VaI-NH2. Analogs have been synthesized that are at least as potent as UI. and UI or such an analog or a fragment of either or a pharmaceutically acceptable salts of any of the foregoing, dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals to achieve a substantial elevation of ACTH, beta-endorphin, betalipotropin and corticosterone levels and or an increase in intestinal blood flow and or a lowering of systemic blood pressure and or a changing of regional blood distribution over an extended period of time. In the analogs, one or more of the first three N-terminal residues is deleted and substituted by a peptide fragment up to 5 amino acids long and/or an aeylating agent containing up to 7 carbon atoms is added at the N-terminal.
ABSTRACTS
pituitary GH in animals, including humans, which have resistance to enzymatic degradation in the body, and which have the sequence: R IR2-R3-Ala-lle-Phe-Thr-R°-Ser- R I 0-Arg- R 12 R 13-RI4-R 15-GIn-R 17-R 18-Ala-Ar g-LysLeu-R23-R24- R25-1te- R27- R28- R29-Gln-GInGly-Glu-R34-Asn-GIn-GIu-R38R39-R40Arg-R42-R43-R44 wherein RI is Tyr, D-Tyr, Met, Phe, D-Pbe, pCI-Phe, Leu, His or D-His having either a C alphaMe or N alphaMe substitution or being unsubstituted: R2 is Ala. DAla or D-NMA; R3 is Asp or D-Asp; R8 is Ser, Asn, D-Set or D-Asn; RI0 is Tyr or D-Tyr: RI2 is A rg or Lys; R 13 is lie or Val: R 14 is Leu or DLeu; R15 is Gly or D-AIa; RI7 is Leu or D-Leu; RI8 is Tyr or Ser; R23 is Leu or D-Leu; R24 is His or Gin; R25 is Glu, Asp, D-Glu or D-Asp; R27 is Met, D-Met, Ala, Nle, lie, Leu, Nva or Val; R28 is Asn or Ser; R29 is Arg or D-Arg: R34 is Arg or Ser; R38 is Gln or Arg; R39 is Arg or Gly; R40 is Ser or Ata; R42 is Phe, Ala or Val; R43 is Asn or Arg; R44 is a natural amino acid; provided however that any or all of the residues between R28 and R44, inclusive, may be deleted and provided also that R2 is D-NMA and/or R14 is D-Leu and/or R29 is D-Arg. These peptides as well as their nontoxic salts may also be used diagnostically.
4529542 PROTEINOUS S U B S T A N C E KUD-PC AND ITS PRODUCTION Iwao Umezawa, Kanki Komiyama, Tokyo. Japan assigned to The Kitasato Institute
i °i L WAV[
NUMBER
{ C m "l ]
A novel proteinous substance KUP-PC, which is produced by culturing proteinous substance KUD-PC producing organisms belonging to the genus Streptosporangium. KUD-PC increases the antitumor activity of the anti-tumor substance, sporamyein.
4528190 GRF ANALOGS IV Wylie W Vale, Jean E Rivier assigned to The Salk Institute For Biological Studies Human GRF(hGRF), rat GRF(rGRF) porcine GRF(pGRF) and bovine GRF(bGRF) have been earlier characterized and synthesized. The invention provides synthetic peptides v.hich are extremely potent in stimulating the release of
4529545 ISOLATION OF CHEMICALLY UNSTABLE ANTIBIOTICS FROM FERMENTATION S O L U T I O N S Gerhard Huber, Pete Schindler. Kelkheim, Federal Republic Of Germany assigned to Hoechst Aktiengeseltschaft
PATENT
spectrum: Maximum absorption is not recognized in the range of 240-400 nm: 8. Outward form: White or faint brown, amorphous powder; 9. Solubility: (a) Soluble in water: (b) Insoluble in methanol, ethanol, acetone, ethyl acetate, diethyl ether, hexane and chloroform: I0. Color reactions: Positive to the following reactions: (a) anthrone-sulfuric acid reaction: (b) Molisch's reaction; (c) skatol reaction: and (d) Bial's reaction; Negative to the follov.ing reactions: (a) ninhydrin reaction: (b) 2A-DNP reaction; (c) SelivanofFs reaction: (d) naphthoresorcinol reaction: and (e) carbazolsulfuric acid reaction; I I Component sugars: Arabinose and galactose: 12. ttomogeneity: Homogeneity is proved according to uhracentrifugation, electrophoresis and gel filtration.
4528189 UROTENSIN PEPTIDES Karl P Lederis, Keith L MacCannell. Jean E Rivier, Calgary, Canada assigned to The Salk Institute For Biological Studies UI (Urotensin I) or white sucker urotensin, obtained from Catostomus commersoni, has the formula: H-Asn-Asp-Asp-Pro-Pro-lle-Ser-lleAsp-Leu-Thr-Phe-His-Leu-Leu-Arg-Asn-Metlle-Glu-Met-Ala-Arg-lle-Glu-Asn-Glu-ArgGId-GIn-Ala-Gly-Leu-Asn-Arg-Lys-Ty r-LeuAsp-GIu-VaI-NH2. Analogs have been synthesized that are at least as potent as UI. and UI or such an analog or a fragment of either or a pharmaceutically acceptable salts of any of the foregoing, dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals to achieve a substantial elevation of ACTH, beta-endorphin, betalipotropin and corticosterone levels and or an increase in intestinal blood flow and or a lowering of systemic blood pressure and or a changing of regional blood distribution over an extended period of time. In the analogs, one or more of the first three N-terminal residues is deleted and substituted by a peptide fragment up to 5 amino acids long and/or an aeylating agent containing up to 7 carbon atoms is added at the N-terminal.
ABSTRACTS
pituitary GH in animals, including humans, which have resistance to enzymatic degradation in the body, and which have the sequence: R IR2-R3-Ala-lle-Phe-Thr-R°-Ser- R I 0-Arg- R 12 R 13-RI4-R 15-GIn-R 17-R 18-Ala-Ar g-LysLeu-R23-R24- R25-1te- R27- R28- R29-Gln-GInGly-Glu-R34-Asn-GIn-GIu-R38R39-R40Arg-R42-R43-R44 wherein RI is Tyr, D-Tyr, Met, Phe, D-Pbe, pCI-Phe, Leu, His or D-His having either a C alphaMe or N alphaMe substitution or being unsubstituted: R2 is Ala. DAla or D-NMA; R3 is Asp or D-Asp; R8 is Ser, Asn, D-Set or D-Asn; RI0 is Tyr or D-Tyr: RI2 is A rg or Lys; R 13 is lie or Val: R 14 is Leu or DLeu; R15 is Gly or D-AIa; RI7 is Leu or D-Leu; RI8 is Tyr or Ser; R23 is Leu or D-Leu; R24 is His or Gin; R25 is Glu, Asp, D-Glu or D-Asp; R27 is Met, D-Met, Ala, Nle, lie, Leu, Nva or Val; R28 is Asn or Ser; R29 is Arg or D-Arg: R34 is Arg or Ser; R38 is Gln or Arg; R39 is Arg or Gly; R40 is Ser or Ata; R42 is Phe, Ala or Val; R43 is Asn or Arg; R44 is a natural amino acid; provided however that any or all of the residues between R28 and R44, inclusive, may be deleted and provided also that R2 is D-NMA and/or R14 is D-Leu and/or R29 is D-Arg. These peptides as well as their nontoxic salts may also be used diagnostically.
4529542 PROTEINOUS S U B S T A N C E KUD-PC AND ITS PRODUCTION Iwao Umezawa, Kanki Komiyama, Tokyo. Japan assigned to The Kitasato Institute
i °i L WAV[
NUMBER
{ C m "l ]
A novel proteinous substance KUP-PC, which is produced by culturing proteinous substance KUD-PC producing organisms belonging to the genus Streptosporangium. KUD-PC increases the antitumor activity of the anti-tumor substance, sporamyein.
4528190 GRF ANALOGS IV Wylie W Vale, Jean E Rivier assigned to The Salk Institute For Biological Studies Human GRF(hGRF), rat GRF(rGRF) porcine GRF(pGRF) and bovine GRF(bGRF) have been earlier characterized and synthesized. The invention provides synthetic peptides v.hich are extremely potent in stimulating the release of
4529545 ISOLATION OF CHEMICALLY UNSTABLE ANTIBIOTICS FROM FERMENTATION S O L U T I O N S Gerhard Huber, Pete Schindler. Kelkheim, Federal Republic Of Germany assigned to Hoechst Aktiengeseltschaft