Patents Examined by Delbert R. Phillips
  • Patent number: 5019390
    Abstract: The present invention relates to a novel antineoplastic agent, designated IMIC (Inhibitor of Mevalonate Incorporation Into Cholesterol) having the following characteristics:(a) is present in the retentate of dialyzed skim milk;(b) is non-dialyzable;(c) has general properties of pyrimidines;(d) is bound to a protein in the proteose-peptone fration of milk;(e) is soluble in water;(f) is insoluble in organic solvents;(g) is stable in acid;(h) is not bound or retained by a C.sub.18 or C.sub.8 reverse phase HPLC columns;(i) is not retained by a C.sub.18 or silica gel sep. pak;(j) has .lambda. maximum absorbance at 208 nm and 278 nm (UV) in neutral ad acidic solution and in a basic solution at 223 and 290 nm;(k) provides peaks with a retention time of 7.52 minutes upon fractionation by HFLC on a Biorad Aminex resin column (30 cm .times.7.9 nm) with 0.05 NH.sub.2 SO.sub.4 as the mobile phase and with a flow rate of 0.7 ml/minute;(l) provides peaks with a retention time of 9.
    Type: Grant
    Filed: May 29, 1987
    Date of Patent: May 28, 1991
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Robert D. McCarthy, deceased, Arun Kilara, David B. Pierce
  • Patent number: 4959354
    Abstract: The mixturex of FSH ( follicle stimulating hormone) and LH ( luteinizing horomone) being extracted from pig hypophyses in a definite ratio, improve to an optimum level the induction of super-ovulation in bred animals.
    Type: Grant
    Filed: July 14, 1987
    Date of Patent: September 25, 1990
    Assignee: Istituto Farmacologico Serono S.p.A.
    Inventor: Manlio Barbetti
  • Patent number: 4954638
    Abstract: Leukotrienes may be conjugated with various proteins such as Bovine Serum Albumin (BSA) and Hemocyanin from Giant Keyhole Limpets (KLH) using 1,5-difluoro-2,4-dinitrobenzene or 6-N-maleimidohexanoic acid chloride as coupling agents.These conjugates are useful as reagents in a newly developed immunoassay for leukotrienes, as well as having potential utility as chemical immunotherapeutic agents in the treatment of various allergic and chronic inflammatory diseases of the skin, lung, and airways, including asthma, allergic rhinitis, rheumatoid arthritis, and skin diseases such as psoriasis and eczema.
    Type: Grant
    Filed: August 1, 1988
    Date of Patent: September 4, 1990
    Assignees: Merck Frosst Canada, Inc., Merck & Co., Inc.
    Inventors: Robert N. Young, Joshua Rokach, Edward C. Hayes
  • Patent number: 4935235
    Abstract: What is disclosed is a protein immunoreactive with antibodies raised against HBsAg, which protein has the formula: X-S-Y, S represents a peptide residue of the hepatitis B virus S-protein, Y is OH or NH.sub.2 and X is selected from the pre-S1/pre-S2 peptide residue, the pre S2 peptide residue and a fragment of the pre-S1/pre-S2 peptide residue containing at least a 9 amino acid portion of the C-terminal sequence of pre-S2.
    Type: Grant
    Filed: December 1, 1987
    Date of Patent: June 19, 1990
    Assignee: The Regents of the University of California
    Inventors: William J. Rutter, Howard M. Goodman
  • Patent number: 4919930
    Abstract: Synthetic peptide segments of protein Pep M5 containing epitopes capable of evoking type specific opsonic antibodies against streptococci when covalently linked to a protein carrier.
    Type: Grant
    Filed: May 1, 1986
    Date of Patent: April 24, 1990
    Assignee: University of Tennessee Research Corporation
    Inventors: Edwin H. Beachey, James B. Dale
  • Patent number: 4916119
    Abstract: Tripeptides of the general formula: ##STR1## wherein the symbols R, which may be the same or different represent hydrogen or a fatty acid residue (at least one of them representing a fatty acid residue), R.sub.1 represents hydroxy, amino or alkoxy and R.sub.2 and R.sub.3, which may be the same or different, represent hydrogen, carboxy, carbamoyl or alkoxycarbonyl radical (with the proviso that R.sub.2 and R.sub.3 cannot simultaneously represent a hydrogen atom), the alanine moiety being in the L form, the glutamic acid moiety being in the D form, the lysine moiety (when R.sub.2 or R.sub.3 =a hydrogen atom) being in the L form and the 2,6-diaminopimelic acid moiety or its derivatives (when R.sub.2 and/or R.sub.3 =carboxy, carbamoyl or alkoxycarbonyl) being in the D,D, L,L, D,D/L,L (racemic) or D,L (meso) form, and salts thereof, possess immunological adjuvant and immunostimulant activity.
    Type: Grant
    Filed: June 27, 1980
    Date of Patent: April 10, 1990
    Assignee: Rhone-Poulenc Industries
    Inventors: Jean Bouchaudon, Daniel Farge, Claude James
  • Patent number: 4914189
    Abstract: Human pancreatic GRF (hpGRF), rat hypothalamic GRF (rGRF) and porcine hypothalamic GRF (pGRF) have been earlier characterized and synthesized. The invention provides synthetic peptides which are extremely potent in stimulating the release of pituitary GH in animals, including humans, which have resistance to enzymatic degradation in the body, and which have the sequence: ##STR1## wherein Q.sup.1 is an omega or alpha-omega substituted alkyl,Q.sup.2 is a lower omega-quanidino-alkyl group.R.sub.2 is Ala, D-Ala, or D-N-Methyl-AlaR.sub.3 is Asp, D-Asp, Glu, or D-GluR.sub.8 is Asn, D-Asn, Ser, or D-SerR.sub.10 is Tyr or D-TyrR.sub.12 is Lys, D-Lys Arg or OrnR.sub.13 is Val or IleR.sub.14 is Leu or D-LeuR.sub.15 is Gly, N-Methyl-Gly, or D-AlaR.sub.17 is Leu or D-LeuR.sub.18 is Tyr or SerR.sub.23 is Leu or D-LeuR.sub.24 is Gln or HisR.sub.25 is Asp, D-Asp, Glu, or D-GluR.sub.27 is Met, D-Met, Ala, Nle, Ile, Val, Nva, LeuR.sub.
    Type: Grant
    Filed: February 5, 1987
    Date of Patent: April 3, 1990
    Assignee: The Adminstrators of the Tulane Educational Fund
    Inventors: Andrew V. Schally, Jozsef Gulyas, Sandor Bajusz
  • Patent number: 4910296
    Abstract: Fragments of Alpha-1 thymosin ranging from two to twelve peptides in length nd pharmaceutically acceptable salts thereof. These fragments possess immunostimulatory and immunoregulatory properties similar to the alpha thymosin molecule and are useful in the same fashion as in this molecule.
    Type: Grant
    Filed: June 26, 1986
    Date of Patent: March 20, 1990
    Assignee: Max-Planck-Gesellschaft zur Foederung der Wissenschaften e.V.
    Inventors: Christian Birr, Ilona Werner, Ulrich Stollenwerk, deceased, by Paul Stollenwerk, heir, by Margot Stollenwerk, heir
  • Patent number: 4910190
    Abstract: The invention concerns pharmaceutically useful trifluoromethyl ketone substituted di-, tri- and tetra-peptide derivatives of the formulae Ia, Ib, Ic set out hereinafter, and salts thereof, which are inhibitors of human leukocyte elastase. Also described herein are pharmaceutical compositions containing a peptide derivative and processes and intermediates for use in the manufacture of the peptide derivatives.
    Type: Grant
    Filed: January 20, 1987
    Date of Patent: March 20, 1990
    Assignee: ICI Americas Inc.
    Inventors: Scott H. Bergeson, Philip D. Edwards, John A. Schwartz, Andrew Shaw, Mark M. Stein, Diane A. Trainor, Richard A. Wildonger, Donald J. Wolanin
  • Patent number: 4908352
    Abstract: Maggy UI (Urotensin I) or flathead sole urotensin, obtained from Hippoglossides Elassodon has the formula: H-Ser-Glu-Glu-Pro-Pro-Met-Ser-Ile-Asp-Leu-Thr-Phe-His-Met-Leu-Arg-Asn-Met- Ile-His-Arg-Ala-Lys-Met-Glu-Gly-Glu-Arg-Glu-Gln-Ala-Leu-Ile-Asn-Arg-Asn-Leu -Leu-Asp-Glu-Val-NH.sub.2. Analogs have been synthesized that are at least as potent as Maggy UI, and Maggy UI or such an analog or a biologically active fragment of either or 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, .alpha.-lipotropin 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 distributio over an extended period of time.
    Type: Grant
    Filed: September 28, 1987
    Date of Patent: March 13, 1990
    Assignee: The Salk Institute for Biological Studies
    Inventors: Karl P. Lederis, Denis McMaster, Jean E. F. Rivier
  • Patent number: 4906615
    Abstract: A method for inhibiting the action of enkephalinases in a mannal to thereby elicit an analgesic effect in said mammal is described.Novel compounds and compositions useful for accomplishing the method of the invention are also described.
    Type: Grant
    Filed: October 26, 1987
    Date of Patent: March 6, 1990
    Assignee: Schering Corporation
    Inventor: Joel G. Berger
  • Patent number: 4906614
    Abstract: A method of preventing or treating posttraumatic nervous injuries by administering a compound of the formula: ##STR1## wherein R.sub.1 is hydrogen, a lower alkyl group, cyclohexyl or benzyl; Z is one of the groups ##STR2## if Z is a group (a), R.sub.2 and R.sub.3 together represent an additional bond between the carbon atoms bearing them, or if Z represents a group (b), R.sub.2 is hydrogen; R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl or phenyl, and R.sub.6 is hydrogen or methyl. Hydrates or pharmaceutically acceptable acid addition salts may also be used in the method. Pharmaceutical compositions used in this method containing such compounds in a prophylactically or therapeutically effective amount may be administered by infusion, injection, orally, perorally, rectally, percutaneously or other route.
    Type: Grant
    Filed: June 14, 1988
    Date of Patent: March 6, 1990
    Assignee: Gruenenthal GmbH
    Inventors: Hubert Giertz, Hans Barth, Leopold Flohe
  • Patent number: 4904642
    Abstract: An octapeptide of the formula: ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl), or R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H; A.sub.3 is CH.sub.2 -A.sub.6 (where A.sub.6 is pentafluorophenyl, naphthyl, pyridyl, or phenyl); A.sub.4 is o- m- or p-substituted X-Phe (where X is a halogen, H, NO.sub.2, OH, NH.sub.2, or C.sub.1-3 alkyl), pentafluoro-Phe, or .beta.-Nal; A.sub.5 is Thr, Ser, Phe, Val, .alpha.-aminobutyric acid, or Ile, provided that when A.sub.3 is phenyl, A.sub.1 is H, and A.sub.2 is H, A.sub.5 cannot be Val; and A.sub.7 is Thr, Trp, or .beta.-Nal; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 17, 1989
    Date of Patent: February 27, 1990
    Assignee: The Administrators of the Tulane Educational Fund
    Inventors: David H. Coy, William A. Murphy, Mark L. Heiman
  • Patent number: 4904643
    Abstract: Thymolymphotropin, a thymus derivative able to stimulate the differentiation and the function of T-lymphycytes, is active after oral administration and can be prepared through a process of partial acid lysis of mammal thymuses. Pharmaceutical compositions containing thymolymphotropin are utilized in the treatment of primary and secondary immunodeficiencies.
    Type: Grant
    Filed: June 11, 1987
    Date of Patent: February 27, 1990
    Assignee: Ellem Industria Farmaceutica, s.r.l.
    Inventors: Brunetto Brunetti, Marco Prada
  • Patent number: 4900811
    Abstract: Synthetic polypeptides whose sequences correspond substantially to amino acid residue sequences of at least portions of naturally occurring proteinoids translated from brain-specific mRNAs are disclosed as are receptors, methods and diagnostics that utilize those synthetic polypeptides. The synthetic polypeptides have molecular weights less than those of their corresponding proteinoids, and induce the production of antibodies that bind to the naturally occurring proteinoid, or a derivative thereof when bound to a carrier as a conjugate and are introduced into an animal.
    Type: Grant
    Filed: June 3, 1987
    Date of Patent: February 13, 1990
    Assignee: Scripps Clinic and Research Foundation
    Inventor: J. Gregor Sutcliffe
  • Patent number: 4898930
    Abstract: Peptide ester and amide derivatives of the general formula I: ##STR1## in which X is H or an acyl, A and B are structurally defined amino acid residues, n is an integer of from 1 to 3, R.sup.1 is H or a lower alkyl and either R.sup.2 or C is a defined optionally modified amino acid residue and the other is a lower alkoxyl, an amino group or a direct chemical bond, are converted under physiologic conditions, by enzymic hydrolysis in pathologically altered tissues and subsequent spontaneous cyclization, into pharmacodynamically active spirocyclic peptide derivatives of the general formula III: ##STR2## in which R.sup.3 and R.sup.4 are H atoms, optionally substituted alkyl groups or jointly an aliphatic chain forming preferably a 2,5- piperazinedione ring, and hence can act as pro-farmaca (drug precursors) of prolonged biological effect.
    Type: Grant
    Filed: June 12, 1987
    Date of Patent: February 6, 1990
    Assignee: Spofa, spojene podniky pro
    Inventors: Evzen Kasafirek, Miroslav Rybak, Ivan Krejci, Antonin Sturc, Alena Roubalova, Jiri Vanzura, Evzen Krepela, Michal Bartik
  • Patent number: 4894436
    Abstract: Microbially produced aprotinin and aprotinin homologs used for treating patients suffering from an excess release of pancreatic elastase, serum elastase or leukocyte elastase.
    Type: Grant
    Filed: March 23, 1987
    Date of Patent: January 16, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ernst-August Auerswald, Werner Schroder, Eugen Schnabel, Wolfgang Bruns, Gerd Reinhardt, Michael Kotick
  • Patent number: 4894438
    Abstract: A synthetic peptide of the formula: ##STR1## wherein A.sub.1 is Pro or Ala, is excellent in solubility in water and substrate specificitity and is suitable as a substrate for determining trypsin and .alpha..sub.1 -antitrypsin.
    Type: Grant
    Filed: November 21, 1986
    Date of Patent: January 16, 1990
    Assignee: Nitto Boseki Co., Ltd.
    Inventors: Takeshi Nagasawa, Yuko Gemba, Yoshio Nakamura, Katsumasa Kuroiwa
  • Patent number: 4894437
    Abstract: The present invention provides novel renin-inhibiting peptides of the formula X-A.sub.6 -B.sub.5 -C.sub.8 -D.sub.9 -E.sub.10 -F.sub.11 -G.sub.12 -H.sub.13 -I.sub.14 -Z, wherein X and Z are terminal groups, C.sub.8 contains S-aryl-D- or L- or DL-cysteinyl, 3-(arylthio)lactic acid, and 3-(arylthio)alkyl moieties, and the remaining variables are amino acid residues. Such inhibitors are useful for the diagnosis and control of renin-dependent hypertension.
    Type: Grant
    Filed: June 29, 1987
    Date of Patent: January 16, 1990
    Assignee: The Upjohn Company
    Inventor: Ruth E. TenBrink
  • Patent number: 4886663
    Abstract: A synthetic polypeptide having at least about 10% of the immunological activity of biologic heat-stable enterotoxin of E. coli. The synthetic polypeptide includes at least 14 amino acids in the sequence, from amino-terminus to carboxy-terminus, represented by the formula: CysCysGluLeuCysCysTyr-(Asn)ProAlaCysAla(Thr)GlyCysAsn(Tyr) wherein the amino acid in parentheses may replace the immediately preceding amino acid residue, and at least one intramolecular disulfide bond formed between the Cys residues. The Cys residues that are not part of the intramolecular disulfide bond can be replaced by other amino acid residues or be bonded to substituent moieties. The polypeptides can be a monomeric or multimeric material containing an intramolecular, intrapolypeptide and/or an intramolecular, interpolypeptide cystine disulfide bond.
    Type: Grant
    Filed: December 12, 1983
    Date of Patent: December 12, 1989
    Assignee: Scripps Clinic and Research Foundation
    Inventor: Richard A. Houghten