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    New peptide(s) of TNF agonists and antagonists - used for treating neoplastic and autoimmune disease, infection, inflammation and transplant rejection
    17.
    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.

    18.
    发明专利
    未知

    公开(公告)号：DE3866686D1

    公开(公告)日：1992-01-16

    申请号：DE3866686

    申请日：1988-12-15

    Applicant: BASF AG

    Inventor： HERR DIETER DR ,  DOERPER THOMAS DR ,  DAUM LOTHAR DR ,  GEISS KARL-HEINZ DR ,  MOELLER ACHIM DR

    IPC: C08B37/10 ,  A61K20060101 ,  A61K31/715 ,  A61P31/12 ,  A61K31/725

    Abstract: Polysulphated heparins (I) are used to prepare medicaments for prophylaxis and therapy of diseases caused by retroviruses. (I) have an S content of 13-15% and a molecular wt. of 2000-20,000 (esp. 2000-9000 for oral admin). They may be prepd. by converting heparin to the pyridinium salt and reacting this with ClSO3H in pyridine. The medicaments may be formulated for oral or parenteral admin., or as sprays. The daily dose is 10-1000 mg/kg oral or 0.1-10 mg/kg parenteral.

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