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    New peptide(s) of TNF agonists and antagonists - used for treating neoplastic and autoimmune disease, infection, inflammation and transplant rejection
    3.
    发明专利
    New peptide(s) of TNF agonists and antagonists - used for treating neoplastic and autoimmune disease, infection, inflammation and transplant rejection 未知

    公开(公告)号：DE4041188A1

    公开(公告)日：1992-06-25

    申请号：DE4041188

    申请日：1990-12-21

    Applicant: BASF AG

    Inventor： BOEHM HANS-JOACHIM DR ,  DAUM LOTHAR DR ,  HAUPT ANDREAS DR ,  PETTIG DAGMAR DR ,  WALKER NIGEL DR ,  MAENNEL DANIELA DR ,  FRANK REINER DR ,  STIEHNER RAINER DR

    IPC: A61K38/00 ,  C07K14/525

    Abstract: Peptides of formula X-Leu-A-B-Asn- E-Leu-F-K-Pro-L-Y (I), derived from tumour necrosis factor (TNF), and their salts with physiologically tolerable acids are new: (where A = Arg, Glu, Thr, Lys or Ser; B = Asp or Asn; E = Gln or Ser; F = Val, Leu or NH-CHT-CO; T = HS(CH2)b, NH2(CH2)b or HOOC(CH2)b; b = 1-6; K = Val or Ile; L = Ser, Ala or Thr; X = G, GNH-CHM-CO or GNH-CHM-COW-; Y = Z, NH-CHQ-COZ, -V-NH-CHQ-COZ; NH-CHQ-CO-V-Z or V-NH-CHQ-CO-V-Z; G = H or amino-protecting gp.; Z = OH, NH2 or carboxy-protecting gp.; or G and Z are together a covalent bond or CO-(CH2)a-NH; a = 1-12; U, V and W = peptide chain with 1-4 naturally occurring amino acids; M and Q = H, CHMe2, CHMe-Et, phenyl, CHOH-Me, (3-indolyl)methyl, (imidazolyl-4-yl)methyl or (CH2)bT; b = 1-6; T = H, OH, MeO, MeS, Me2CH, phenyl (opt. 4-OH substd.), HS, NH2, COOH, CONH2 or guanidino; or M and Q or M and T are together a (CH2)c-S-S-(CH2)d-, (CH2)e-CONH-(CH2)f or (CH2)e-NHCO(CH2)gNH bridge; c and d = 1-4; e and f = 1-6; g = 1-12). (I) are obtd. by standard (chemical or enzymatic) peptide synthesis, initially as linear peptides, opt. followed by appropriate cyclisation reaction under very dilute conditions. USE/ADVANTAGE - Some (I) are TNF agonists, others are TNF antagonists (these have high affinity for cellular receptors but no activity). They are used for treating neoplastic and autoimmune diseases, and for treating or preventing infections, inflammation and transplant rejection. They have significantly lower mol. wt. than TNF.

    New peptides as TNF agonists and antagonists - for treatment of neoplastic and auto:immune disease, infection, inflammation and transplant rejection
    4.
    发明专利
    New peptides as TNF agonists and antagonists - for treatment of neoplastic and auto:immune disease, infection, inflammation and transplant rejection 未知

    公开(公告)号：DE4041189A1

    公开(公告)日：1992-06-25

    申请号：DE4041189

    申请日：1990-12-21

    Applicant: BASF AG

    Inventor： BOEHM HANS-JOACHIM DR ,  DAUM LOTHAR DR ,  HAUPT ANDREAS DR ,  PETTIG DAGMAR DR ,  WALKER NIGEL DR ,  MAENNEL DANIELA DR ,  FRANK REINER DR ,  STIEHNER RAINER DR

    IPC: A61K38/00 ,  C07K14/525

    Abstract: Peptides of formula X-Ala-A-B-E-Y (I), derived from tumour necrosis factor (TNF), and their salts with physiologically tolerable acids are new. A is Leu or Phe; B is Leu or Met; X is GNH-CHM-CO, GNH-CHM-CO-W, G-RNH-CHM-CO or G-R-NH-CHM-CO-W; Y is Z, NH-CHQ-COZ, V-NH-CHQ-COZ, NH-CHQ-CO-U-Z or V-NH-CHQ-U-Z; G is H or amino protecting gp.; Z is OH, NH2 or carboxy-protecting gp.; or G and Z together are a covalent bond or CO(CH2)aNH; a is 1-12; R,U,V and W are each peptide chains of 1-4 naturally occurring amino acids; M and Q = H, CHMe2, CHMe-Et, phenyl, CHOH-Me, 3-indolylmethyl, (imidazol-4-yl)methyl or (CH2)bT; b is 1-6; T is H, OH, MeO, MeS, Me2CH, phenyl (opt. 4-OH substd.), SH, NH2, COOH, CONH2, or guanidino; M and Q can together be (CH2)c-S-S-(CH2)-d, (CH2)e-CONH-(CH2)f, or (CH2)e-NH.CO-(-CH2-)-g-NH.CO-(CH2)-f; c and d = 1-4; e and f = 1-6; g = 1-22. (I) are made by standard (chemical or enzymatic) methods of peptide synthesis, initially as linear peptides, opt. followed by an appropriate cyclisation reaction under very dil. conditions. USE/ADVANTAGE - Some (I) are TNF agonists, others are TNF antagonists (these have high affinity for cellular receptors but no activity). Useful for treating neoplastic and autoimmune disorders, and for treating or preventing infections, inflammation and transplant rejection. (I) have a significantly smaller mol. wt. than TNF.

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