Abstract: This invention relates to novel biologically active molecules which bind to and inhibit thrombin. These molecules comprise a catalytic site directed moiety (CSDM) of the formula ##STR1## wherein X is hydrogen or is characterized by a backbone chain consisting of from 1 to 100 atoms; R.sub.1 is selected from the group consisting of unsubstituted, monosubstituted, di-substituted and tri-substituted saturated ring structures; R.sub.2 is a bond or is characterized by a backbone chain consisting of from 1 to 5 atoms; R.sub.3 is a bond or is characterized by a backbone chain consisting of from 1 to 3 atoms; R.sub.4 is any amino acid; R.sub.5 is any L-amino acid which comprises a guanidinium- or amino-containing side chain group; R.sub.6 is a non-amide bond; and Y is characterized by a backbone chain consisting of from 1 to 9 atoms; or the formula: ##STR2## wherein R'.sub.1 is selected from the group consisting of unsubstituted, mono-substituted, di-substituted and tri-substituted ring structures; R'.sub.

Abstract: A method to obtain selected individual peptides or families thereof which have a target property and optionally to determine the amino acid sequence of a selected peptide or peptides to permit synthesis in practical quantities is disclosed. In general outline, the method of the invention comprises synthesizing a mixture of randomly or deliberately generated peptides using standard synthesis techniques, but adjusting the individual concentrations of the components of a mixture of sequentially added amino acids according to the coupling constants for each amino acid/amino acid coupling. The subgroup of peptides having the target property can then be selected, and either each peptide isolated and sequenced, or analysis performed on the mixture to permit its composition to be reproduced. Also included in the invention is an efficient method to determine the relevant coupling constants.

Abstract: Methods, compounds and compositions are provided for inducing natriuresis, diuresis and vasodilatation in mammalian hosts by administering atrial natriuretic/vasodilator peptides to said host. Also provided are methods for producing such peptide compounds.

Abstract: This invention relates to novel biologically active molecules which bind to and inhibit thrombin. Specifically, these molecules are characterized by a thrombin anion-binding exosite association moiety (ABEAM); a linker portion of at least 18 .ANG. in length; and a thrombin catalytic site-directed moiety (CSDM). This invention also relates to compositions, combinations and methods which employ these molecules for therapeutic, prophylactic and diagnostic purposes.

Abstract: The present invention relates to a method of treating chronic fatigue syndrome not associated with an HIV infection. In the method of the present invention patients are administered a pharmaceutically acceptable carrier together with(1) a neuropsychiatrically effective amount of a linear peptide of formula (I):R.sup.a -Ser-Thr-Thr-Thr-Asn-Tyr-R.sup.6 (I)whereinR.sup.a is Ala, D-Ala or Cys-Ala-, andR.sup.6 is Thr, Thr-amide, Thr-Cys or Thr-Cys-amide,or a derivative of the peptide or a physiologically acceptable salt thereof; or(2) a neuropsychiatrically effective amount of a linear peptide of formula (II):R.sup.1 -R.sup.2 -R.sup.3 -R.sup.4 -R.sup.5 (II)whereinR.sup.1 is X-Y or Y when Y is Thr-, Ser-, Asn-, Leu-, Ile-, Arg- or Glu-, and X is Cys;R.sup.2 is Thr-, Ser- or Asp;R.sup.3 is Thr, Ser, Asn, Arg, Gln, Lys or Trp;R.sup.4 is Tyr; andR.sup.

Abstract: The present specification describes a process by which a blood substitute (hereinafter referred to as "HemoSafe") is derived from uniformly stabilized monomers and polymers of deoxyhemoglobin in its tight (T) conformation, with oxygen affinity similar to that of human blood. Two classes of HemoSafe are derived respectively from animal-hemoglobin and human-hemoglobin. HemoSafe (animal) differs from HemoSafe (human) in that it is free of polymers in order to reduce potential immunogenicity if used in man. Both types of HemoSafe may be derived in the following manner. The stabilized deoxyhemoglobins are converted to their carbonmonoxy derivatives (CO-HemoSafe) which are then stable under pasteurization conditions to render them viral disease transmission-free. CO-HemoSafes are stable for 2 months at 56.degree. C. in either the solution or the freeze-dried state. For transfusion CO-HemoSafes are easily oxygenated under sterile conditions by photoconversion yielding oxy-HemoSafe.

Abstract: A polypeptide comprising repeated amino acid sequences of a cell-adhesive protein represented by the formula:(Arg--Gly--Asp)nor(Tyr--Ile--Gly--Ser--Arg)nwherein n is a number ranging from 2 to 20; or a pharmaceutical acceptable salt thereof, which is valuable as an antimetastatic agent for cancer.

Abstract: A method of preparing a mixture of peptides having a known composition and containing a peptide of a desired amino acid sequence is disclosed. The method involves three essential steps. First a given amount of a mixture of amino acyl or peptide derivatized resin is divided into a number of pools with each pool containing an equal molar amount of the resin mixture. Second a different single amino acid is coupled to the resin mixture in each of the pools and the coupling reaction is driven to completion. The peptide mixtures in each of the pools are then mixed together to obtain a complex peptide mixture containing each peptide in retrievable and analyzable amounts. The steps can be repeated to lengthen the peptide chains and methods can be employed to retrieve the desired peptide from the mixture and carry out analyses such as the determination of the amino acid sequence.

Abstract: A medical device is provided which is coated with a polypeptide which can bind heparin and promote cellular adhesion and neurite outgrowth is provided of the formula:lys-asn-asn-gln-lys-ser-glu-pro-leu-ile-gly-arg-lys-lys-thr,leu-ile-gly-arg-lys-lys-thr,tyr-arg-val-arg-val-thr-pro-lys-glu-lys-thr-gly-pro-met-lys-glu,ser-pro-pro-arg-arg-ala-arg-val-thr,trp-gly-pro-pro-arg-ala-arg-ile, or mixtures thereof.

Abstract: The present invention relates to a human SP18 monomer protein-related polypeptide useful in forming a synthetic pulmonary surfactant. The present invention also relates to a method of treating neonatal respiratory distress syndrome comprising adminstering a therapeutically effective amount of synthetic pulmonary of the present invention. Further contemplated by the present invention is a composition containing human SP18 monomer and human SP18 dimer but no other pulmonary surfactant proteins. A recombinant DNA molecule capable of expressing, without post-translational proteolytic processing, mature human SP18 monomer, and methods of using the recombinant DNA molecule are also contemplated.

Abstract: The present invention relates to novel human insulin analogues exhibiting a low ability to associate in solution, a method for the preparation of such insulin analogues, insulin preparations containing the human insulin analogues of the invention and a method of treating Diabetes Mellitus using these human insulin analogues.

Abstract: A peptide derivative of the formula ##STR1## wherein A is hydrogen or a hydrocarbon acyl having 2 to 18 carbon atoms which is substituted by an amino group at the .alpha.-position; B is F-Gly wherein F is a neutral .alpha.-amino acid residue, or NH-(CH.sub.2)nCO wherein n is an integer of 1 to 4; C is a neutral .alpha.-amino acid residue; and E is L-Arg or D-Arg; when A, B and C are hydrogen, Gly-Gly, and Met or Ile, respectively, E is D-Arg, or its pharmacologically acceptable salt has strong hypotensive and natriuretic activity; therefore it is useful as a therapeutic drug for hypertension, a diuretic, and a therapeutic drug for cardiac and cerebral circulatory diseases.

Abstract: A novel pentadecapeptide is disclosed which is useful for the control of intestinal fluid absorption and that has the following amino acid sequence ##STR1##

Abstract: The present invention relates to novel LHRH analogs. The LHRH analogs include "pseudo" hexapeptide, heptapeptide, octapeptide and nonapeptide analogs of LHRH, wherein all or some of the amino acids, 1, 2 and 3 have been eliminated and the remaining (2-9), (2-10), (3-9), (3-10), (4-9) or (4-10) peptide is linked to various carboxylic acids which take the place of amino acids 1, 2 or 3 in LHRH.

Abstract: The present invention relates to a process for preparing optically active synthons, in which an oxygen-silylated amino acid or peptide having a protected nitrogenous group, is activated by a non-coordinated halogenated phosphorus derivative and is condensed with an N-silyl amino acid or peptide in which the acid group is protected.

Abstract: Novel protein partial degradation products obtainable from grain proteins such as wheat protein, maize protein, soya bean protein, etc., by specific degradation treatments, which are useful as a quality-improving agent for various food stuffs, a surface active agent, a dispersing agent for particles, etc.

Abstract: The present invention provides both agonist and antagonist nerve growth factor peptides. The NGF blocking peptides can be used to inhibit the expression of mRNA and their encoded proteins whose expression is stimulated by NGF, such as .beta.-protein precursor and prion proteins, which proteins or their products are associated with neurodegenerative disorders, whereas the NGF agonist peptides can be used to treat neoplastic disorders such as neuroblastomas.

Abstract: The cDNA sequence encoding porcine brain natriuretic peptide and related genes encoding canine and human peptides with natriuretic activity are disclosed. The gene is shown to make accessible the DNAs encoding analogous natriuretic peptides in other vertebrate species. The genes encoding these NPs can be used to effect modifications of the sequence to produce alternate forms of the NPs and to provide practical amounts of these proteins. The NPs of the invention can also be synthesized chemically. The invention peptides have the formula: ##STR1## wherein R.sup.1 is selected from the group consisting of: ##STR2## or a 10- to 109-amino acid sequence shown as the native upstream sequence for porcine, canine or human NP in FIG. 6, or a composite thereof;R.sup.2 is (OH), NH.sub.2, or NR'R" wherein R' and R" are independently lower alkyl (1-4C) or is ##STR3## or the amides (NH.sub.2 or NR'R") thereof, with the proviso that if formula (1) isR.sup.

Abstract: Analogs of CRF are disclosed that can be administered to achieve a substantial elevation of ACTH, .beta.-endorphin, .beta.-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone levels and/or a lowering of blood pressure over an extended period of time. One analog which has been found to be particularly preferred is: [His.sup.20, Nle.sup.21, Leu.sup.38 ]-rCRF. In the analogs, one or more of the first five N-terminals residues may be deleted or may be substituted by a peptide up to 10 amino acids long and/or by an acylating agent containing up to 7 carbon atoms. A number of other substitutions may also be made throughout the chain. These analogs or pharmaceutically or veterinarily acceptable salts thereof, dispersed in a pharmaceutically or veterinarily acceptable liquid or solid carrier, can be administered to mammels, including humans. These analogs may also be used as stimulants to elevate mood and improve memory and learning.