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5736509 |
Cyclic peptide surface feature mimics of endothelin
Cyclic peptides and pharmaceutically acceptable salts and esters thereof are provided. The cyclic peptides and pharmaceutically acceptable salts and esters thereof mimic surface features of the...
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5734012 |
Cyclic motilin-like polypeptides with gastrointestinal motor stimulating activity
This invention pertains to cyclic polypeptides having gastrointestinal motor stimulating activity which may be represented by formula (1): ##STR1## including optically active isomeric forms and the...
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5734013 |
Peptides having farnesyl transferase inhibiting properties and strain of genus streptomyces for producing same
A Steptomyces No. CBS 154.94 strain, mutants or derivatives thereof, and a method for preparing peptides using said strain, are disclosed. Novel peptides of general formula (1), pharmaceutical...
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5731286 |
Cyclic neurokinin A antagonists
Antagonists of neurokinin A which are derivatives of naturally occurring neurokinin A in which the amide bond connecting the two amino acids on the carboxy terminal end is modified are described....
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5731285 |
Tachiquinine antagonist tricyclic compounds, preparation of same and pharmaceutical compositions containing such compounds
Tachyikinin antagonist compounds of the general formula: ##STR1## are described where: X1, X2, X3, X4, X5, and X6 are identical or different and are --NR'--CO-- or --CO--NR"--, where R' is H or C 1...
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5731408 |
Peptides having potent antagonist and agonist bioactivities at melanocortin receptors
Cyclic lactam peptides, seven amino acids in length, having D-2'-naphthylalanine (D-2'-Nal) or D-para-iodo-phenylalanine D-(p-I)Phe at position 4 of the peptide provided potent and specific...
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5726151 |
Purified form of streptogramins, its preparation and pharmaceutical compositions containing it
This invention relates to a purified form of streptogramins, having of a combination of one or more group B components of streptogramins, of general formula: ##STR1## in which A 1 is a radical of...
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5726156 |
Cytokine regulatory agents and methods of use in pathologies and conditions associated with altered cytokine levels
The present invention relates to novel peptides that are potent cytokine regulatory agents. In addition, the present invention relates to pharmaceutical compositions comprising a pharmaceutically...
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5723575 |
Process for the preparation of backbone cyclic peptides
Biologically active, backbone-cyclized peptides of the formula: ##STR1## wherein AA! or A 1 A 1 ! is a naturally occurring or synthetic amino acid residue, n or e is an integer of 1-10, m or d...
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5721209 |
Iron chelator and inhibitor of iron-mediated oxidant injury
Exochelins can be used to prevent damage to living tissue from the formation or presence of the (OH) radical. In particular, the invention is directed to the administration of exochelins to...
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5721210 |
Cyclic cell adhesion modulation compounds
Cyclized integrin receptor antagonist compounds useful in modulating cell adhesion, including adhesion related to fibronectin, as well as leukocyte adhesion to endothelial cells, are disclosed....
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5719121 |
Use of balhimycin as production promoter in animals, and production promoter compositions
Balhimycin, where appropriate in combination with one or more of its derivatives, is suitable for promoting production in monogastric or polygastric animals.
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5717062 |
Cyclic analogs of PTH and PTHrP
Cyclic analogs of PTH and PTHrP wherein a disulfide or amide bond links the side chains of residues A 13 and A 17 , A 26 and A 30 , or A 13 and A 17 and A 26 and A 30 .
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5709797 |
Method of isolating cyclosporins
The present invention provides a method for isolating cyclosporin by adsorption chromatography. The method comprises the steps of: (a) loading a crude solution containing a cyclosporin onto...
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5710123 |
Peptide inhibitors of selectin binding
The present invention provides novel peptides having as their core region portions of the 109-118 amino acid sequence of P-selectin, E-selectin or L-selectin. The invention also provides...
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5705481 |
Cyclopeptides
The invention relates to novel cyclopeptides of the formula I cyclo-(A-B-C-D-Arg) I in which A and B are each independently of one another Ala, Asn, Asp,...
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5698670 |
Aureobasidins
This invention relates to Aureobasidins useful as an antifungal agent having broader spectrum. The compound according to this invention includes a cyclic depsipeptide consisting of one hydroxy acid...
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5696084 |
Amino-lipopetide antifungal agents
Disclosed are novel antifungal agents having the formula: ##STR1## or a pharmaceutically acceptable acid, ester or prodrug thereof, wherein preferred compounds include those compounds wherein R 1 ...
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5693325 |
Peptide vaccines and methods relating thereto
There are disclosed peptide vaccines and methods related thereto for generating a protective immune response in warm-blooded animals. The peptide vaccines comprise a conformationally constrained...
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5693612 |
Cyclopeptides of the formula I
The invention relates to novel cyclopeptides of the formula I cyclo-(Arg-A-Asp-R 1 -R 2 ) I in which A, R 1 and R 2 have the meaning given in claim 1, and their...
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5693750 |
Polypeptide compound and a process for preparation thereof
A process for preparing a polypeptide compound having antimicrobial activities of the following general formula: ##STR1## wherein R 1 is hydrogen R 2 is acyl group, R 3 is hydroxy or...
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5691304 |
Improved process for preparing polymyxin B/dextran conjugates
An improved process for producing a water-soluble polymyxin B/dextran conjugate comprises the step of reacting polymyxin B or pharmaceutically acceptable salt thereof with dextran in an aqueous...
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5684128 |
Process for preparing side chain derivatives of cyclohexapeptidyl lipopeptides
An improved process for the preparation of side chain derivatives of cyclohexapeptidyl lipopeptides represented by the formula ##STR1## wherein R 1 is fully defined, is disclosed.
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5683981 |
Cyclic bridged analogs of α-MSH and methods thereof
A novel class of cyclic bridged analogs of α-MSH are described herein. With the described analogs, when administered in pharmaceutical compositions, it is now possible to achieve normalization of...
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5684127 |
Tetrapeptides deriving from dalbaheptide antibiotics
Tetrapeptides of general formula (I) deriving from dalbaheptide antibiotics ##STR1## wherein: W and Z represent the relative portions of the aglycon of an antibiotic of the dalbaheptide group...
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5677423 |
Process for performing retro-aldol reaction
A process for removing β-hydroxy groups from β-hydroxy-containing compounds is disclosed. The process involves the use of a retro-aldol-promoting reagent selected from the group of...
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5677419 |
Cyclic vasoactive peptide analogs
Analogs of porcine Vasoactive Intestinal Peptide are disclosed. The analogs have been cyclized by the covalent attachment, via an amide bond, of the side-chain carboxy terminus of one amino acid in...
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5674976 |
Conformationally restricted mimetics of gamma turns and peptides containing the same
The invention provides materials and methods for synthesizing novel beta-turn mimetics, as well as the novel beta-turn mimetics themselves, and peptides containing the same. Also provided are novel...
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5674839 |
Cyclic analogs of alpha-MSH fragments
Cyclic Alpha-MSH fragment analogues of Ac-Nle 4 -Glu 5 -His 6 -D-Phe 7 -Arg 8 -Try 9 -Gly 10 -NH 2 . The method of stimulating melanocytes by the transdermal application of these...
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5674840 |
Synthetic aglucodalbaheptide antibiotics
Synthetic aglucodalbaheptides of formula (I) wherein W and Z, each independently, represent the relative portions of the aglycon of an antibiotic of the dalbaheptide group. Y represents a...
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5672584 |
Cyclic prodrugs of peptides and peptide nucleic acids having improved metabolic stability and cell membrane permeability
Provided are cyclic prodrugs of biologically active peptides and peptide nucleic acids exhibiting improved cell membrane permeability and enzymatic stability, containing...
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5670478 |
Pharmaceutical containing N-methylated cyclic undecapeptides
Medical preparations (drugs) containing N-methylated cyclic undecapeptides, especially for internal use, characterized by the presence of 0.1 to 20 weight parts of compounds from the group of...
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5670155 |
Confomationally restricted mimetics of beta turns and beta bulges and peptides containing the same
The invention provides materials and methods for synthesizing novel reverse turn mimetics, as well as peptides containing the same. Also provided are novel synthetic nonpeptide therapeutic...
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5667991 |
Recombinant mersacidin and a method for production
The present invention refers in particular to the structural gene sequence of the peptide antibiotic mersacidin. Sequencing revealed that premersacidin consists of an unusually long 48 amino acid...
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5665703 |
GE3 compound
A GE3 compound of the formula (I) having antibacterial and antitumor properties: ##STR1##
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5663292 |
Cyclic CRF analogs
Improved CRF antagonist peptides have the formula: ##STR1## wherein R 30 is Cys or Glu; R 33 is Cys, Lys or Orn; provided that when R 30 is Cys, R 33 is Cys and when R 30 is Glu, R 33 is Lys...
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5656723 |
Analogues of hypocalcemiant polypeptide compounds sparing the calcium of the organism, their preparation, their use as medicaments and the compositions containing them
New polypeptides comprising 32 amino acids, process for preparation thereof, application thereof as drugs and pharmaceutical preparations containing, as active ingredient, one or a plurality of...
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5656602 |
PLA.sub.2 inhibitory compounds
The present invention provides peptides and compounds which inhibit the enzyme activity of Type II phospholipases A 2 . The preferred compounds are pentapeptides. Where the phospholipase is human...
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5654271 |
Fungicidally active compounds
Novel compounds of the general composition I, Lactate (1), Glycine (1), Valine (4), Isoleucine (1), pipecolic acid (1), Aspartic acid (1), Tyrosine (1), wherein each amino acid residue...
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5652211 |
Peptides for neutralizing the toxicity of Lipid A
The present invention is concerned with a peptide composition which includes a peptide having units of the formula: (a) (A) n wherein A is Lysine or Arginine and n is an integer with a minimum...
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5648456 |
Pentapeptide antibiotics
Pentapeptide antibiotics of the formula ##STR1## wherein W, Z, X 1 , X 2 and T represent the relative portions of an antibiotic of the dalbaheptide group (glyccpeptide antibiotics), Y represents a...
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5648330 |
Method and composition for treating vascular graft occlusion
The invention provides RGD containing peptides which are cyclized and contain hydrophobic moieties adjacent the carboxy terminus of the RGD sequence. Such peptides have an high affinity for the...
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5646111 |
Cyclic peptide antifungal Agents
Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I: ##STR1## wherein: R' is hydrogen, methyl or NH 2 C(O)CH 2 --; ...
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5646244 |
Cyclodepsipeptide compound
A compound of the formula: ##STR1## wherein A is benzyl group which has suitable substituent (s), A a , B and D are each lower alkyl, C is hydrogen or lower alkyl, or a salt thereof. The...
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5643871 |
Antitumor antibiotics
The present invention relates to novel antitumor depsipeptides produced by Micromonospora strain 39500, ATCC 55011, and having the structural formula ##STR1## wherein R 1 is 2-methylpropanoyl, and...
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5643869 |
Pipecolic acid-containing peptolides, their preparation and pharmaceutical compositions containing them
Pipecolic acid-containing peptolides wherein the peptidic backbone is of at least 9 α-amino acid residues joined together by peptide bonds, particularly the compounds of formula I ##STR1## wherein...
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5643870 |
O-acylated cyclosporins
A cyclosporin of the formula ##STR1## wherein A is a residue of the formula ##STR2## wherein R is hydrogen, C 1 -3 alkyl, C 1 -3 alkoxy or C 1 -3 alkylthio; halo-substituted-C 1 -3 alkyl, -C 1 -3...
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5643872 |
Cyclic anti-aggregatory peptides
This invention relates to compounds of the formula: ##STR1## wherein: A' is absent, Asn, Gln, Ala or Abu; A is absent or a D- or L-amino acid chosen from Arg, HArg, (Me 2 )Arg, (Et 2 )Arg, Abu,...
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5644024 |
Tetrahydronaphthalene derivatives
The present invention is concerned with tetrahydronaphthalene derivatives which are mimics of domains of peptides or proteins which can interact with other proteins or with DNA or RNA through...
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5639852 |
Immunostimulatory agents
Compositions and methods are described for the synthesis of novel analogs of cyclosporin A, and the use of those analogs as immunostimulatory agents.
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