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5831000 |
Hybrid calcitonin
The improved hybrid calcitonin has a peptide segment in human calcitonin and a peptide segment in calcitonin derived from animals other than humans, such as eel, salmon and chicken. Each of the...
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5830855 |
Lipodepsipeptides as antifungal and fungicidal agents
Lipodepsipeptides from Pseudomonas syringae pv. syringae were evaluated for antifungal activity. Specifically, the in vitro antifungal and fungicidal activities of three cyclic...
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5830431 |
Radiolabeled peptide compositions for site-specific targeting
This invention relates to radiolabeled peptide compositions for radiopharmaceutical use and, more specifically, to radiolabeled peptides for diagnostic or therapeutic use having an unmodified...
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5821222 |
Cyclic depsipeptides having 18 ring atoms for combating endoparasites
The present invention relates to the use of cyclic depsipeptides having 18 ring atoms of the general formula (I) ##STR1## in which R 1 to R 6 have the meaning given in the description, and to...
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5821329 |
Cyclic peptide inhibitors of β.sub.1 and β.sub.2 integrin-mediated adhesion
The present invention describes cyclic peptide compounds which modulate integrin mediated adhesion. These compounds can inhibit both β 1 and β 2 mediated adhesion. The invention further relates...
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5817749 |
Processes and intermediate compounds for the preparation of platelet glycoprotein IIb/IIIa inhibitors
This invention provides processes for the synthesis of platelet glycoprotein IIb/IIIa inhibitors and intermediate compounds useful in said processes. The compounds afforded by this invention have...
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5817751 |
Method for synthesis of diketopiperazine and diketomorpholine derivatives
The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of...
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5807979 |
Synthetic, three-dimensionally stabilized polypeptide mimics of HIV
Methods for synthesizing three-dimensional stabilized peptides which mimic the three-dimensional configuration of the active site of a natural, biologically active protein are carried out by (1)...
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5807820 |
Cyclosporin compositions for topical application
Pharmaceutical compositions comprising a cyclosoporin, e.g. Ciclosporin, and a mono- or poly-unsaturated fatty acid or alcohol, e.g. oleic acid or oleyl alcohol. The compositions are suitable for...
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5801222 |
Isolation and structure of the human cancer cell growth inhibitory cyclic octapeptides phakellistatin 10 and 11
Two new compounds which may be useful in the treatment of one or more neoplastic diseases through chemotherapy have been isolated from the Western Pacific Ocean marine sponge Phakellia sp. The...
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5801143 |
Cyclic depsipeptides useful for treatment of hyperlipemia
A cyclic depsipeptide having the general formula (I) ##STR1## (wherein n is an integer of 5-15) or a pharmacologically acceptable salt thereof. The present compound can be prepared by cultivation...
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5792746 |
Aza cyclohexapeptide compounds
Ceretain aza cyclohexapeptide compounds have been found to have superior antibiotic properties. Novel processes for their preparation are also described.
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5789537 |
Method for preparing streptogramins
A method for preparing streptogramins of the formula (I): ##STR1## wherein R 1 is methyl or ethyl, R 2 is H and X and Y together form an oxo radical, or R 1 is ethyl, R 2 and X are H and Y is H...
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5786449 |
Streptogramin derivatives, their preparation and pharmaceutical compositions which contain them
Streptogramine derivatives of general formula (I) below, wherein the radical R 1 is a methyl or ethyl radical, the radical R 2 is a bromine or chlorine atom, or is an alkenyl radical with 3 to 5...
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5786447 |
Opioid peptide analogs
Compounds of the formula I as well as methods for their preparation, their pharmaceutical preparations and their use as analgesics. ##STR1##
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5786332 |
Cytokine restraining 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 restraining agents. In addition, the present invention relates to pharmaceutical compositions comprising a pharmaceutically...
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5786325 |
Cyclic peptide antifungal agents and methods of making and using
Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I ##STR1## where: R', R", R'", R x1 , R x2 , R y1 , R y2 , R y3 , R y4...
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5786448 |
Combinatorial libraries of cyclic urea and cyclic thiourea derivatives and compounds therein
The invention provides a rapid approach for combinatorial synthesis and screening of libraries of cyclic urea and cyclic thiourea compounds. The present invention further provides the compounds...
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5786322 |
Peptides and compounds that bind selectins including endothelium leukocyte adhesion molecule 1
Disclosed are peptides and peptide mimetics that bind selectins, including endothelial leukocyte adhesion molecule 1 (ELAM-1). Such peptides and peptide mimetics are useful in methods for blocking...
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5780426 |
Fivemer cyclic peptide inhibitors of diseases involving α.sub.v β.sub.3
The present invention includes non-RGD cyclic peptides that inhibit the function of the integrin receptor, α v β 3 . The inventive peptides are between five to about thirty amino acids in length...
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5780585 |
Bacterial nitroreductase for the reduction of CB 1954 and analogues thereof to a cytotoxic form
A prodrug of the formula (I): ##STR1## where R 1 is a group such that the compound R--NH 2 represents actinomycin D, doxorubicin, mitomycin C, or a nitrogen mustard of the formula (IV): ##STR2##...
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5776892 |
Anti-inflammatory peptides
The present invention relates to peptides, peptide analogs and peptide derivatives related to platelet factor 4 which exhibit anti-inflammatory activity, to pharmaceutical compositions comprising...
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5776950 |
Cycloanthelmintic inhibitors
This invention comprises novel compounds that inhibit the growth of helminths. The compounds have the structure of Formula I, below. ##STR1## Where the R groups are defined according to the...
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5776894 |
Chelated somatostatin peptides and complexes thereof, pharmaceutical compositions containing them and their use in treating tumors
Somatostatin peptides bearing at least one chelating group for a detectable element, said chelating group being linked to an amino group of said peptide, and said amino group having no significant...
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5773412 |
Use of peptides for altering α.sub.V β.sub.3 -mediated binding
The present invention provides Arg--Gly--Asp peptides that can alter the binding of osteoclasts to a matrix such as bone or can selectively alter integrin receptor binding. The invention also...
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5770380 |
Synthetic antibody mimics--multiple peptide loops attached to a molecular scaffold
A synthetic antibody mimic comprising multiple peptide loops built on an organic or molecular scaffold. In a highly preferred embodiment of the invention, a calixarene unit comprises the organic...
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5770686 |
ICAM-related protein fragments
DNA sequences encoding a novel human intercellular adhesion molecule polypeptide (designated "ICAM-R") and variants thereof are disclosed along with methods and materials for production of the same...
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5770687 |
Comformationally constrained backbone cyclized somatostatin analogs
Novel peptide analogs are disclosed. The novel peptides are conformationally constrained backbone cyclized somatostatin analogs. Methods for synthesizing the somatostatin analogs and for producing...
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5767068 |
Pure biologically active colistin, its components and a colistin formulation for treatment of pulmonary infections
An anti-Pseudomonas aeruginosa agent which is substantially pure biologically active colistin, its component, a mixture thereof or a pharmaceutically acceptable salt thereof delivered as an aerosol...
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5767071 |
Sevenmer cyclic peptide inhibitors of diseases involving α.sub.v β.sub.3
The present invention includes non-RGD, nine amino acid cyclic peptides that inhibit the function of the integrin receptor, α v β 3 . These peptides display surprisingly potent antagonist...
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5766593 |
Anti-inflammatory CD14 peptides
The invention relates to anti-inflammatory peptides that are based on peptide regions 7-10, 11-14, and 57-64 of CD14.
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5763221 |
Transformant producing substance PF1022, and method for transforming microorganism belonging to the class hyphomycetes
A method for transforming strain PF1022, which produces a cyclic depsipeptide (substance PF1022) and belongs to the order Agonomycetales of the class Hyphomycetes has been established by using a...
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5763395 |
Stabilized lanthionine bacteriocin compositions
The invention concerns compositions containing a lanthionine containing bacteriocin such as nisin which are stabilized by the presence of a thioether stabilizing agent against degradation.
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5763406 |
Method for the treatment of conditions caused by herpes virus infections
Peptides of the general formula (I): I-A-B-C-D-E-F-G-H-II are disclosed as being active against Herpes virus infections in animals and human beings, wherein A is Ala, Gly, Val or absent; B is Ala,...
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5763397 |
Glycopeptides, a process for their preparation and their use
Desmethylbalhimycin, a compound of the formula C 65 H 71 Cl 2 N 9 O 24 , desmethylleucylbalhimycin, a compound of the formula C 59 H 60 Cl 2 N 8 O 23 , desglucobalhimycin, a compound of the...
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5759834 |
Synthetic sterically-constrained pepzyme catalysts modeled on lysozyme and ribonuclease
Pepzymes, chemically synthesized cyclic peptides, modeled on lysozyme and ribonuclease have been prepared which efficiently catalyze the same reaction as the native enzyme being modeled. The...
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5759995 |
Antiviral treatment
A method of inhibiting viral infection with a pharmaceutical composition containing cyclomarin-A.
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5756450 |
Water soluble monoesters as solubilisers for pharmacologically active compounds and pharmaceutical excipients and novel cyclosporin galenic forms
A combination of a pharmacologically active compound and a water soluble monoester of a saturated or unsaturated (C 6 -18) fatty acid and a polyol, especially a saccharide, particularly as a solid...
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5753619 |
Composition for prophylaxis or treatment of pulmonary circulatory diseases
Cyclic hexapeptides having antagonistic activity on endothelin receptors of the formula I!: ##STR1## wherein X and Y each is an α-amino acid residue having D-, L-form or DL-form, A is a...
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5753617 |
Peptide inhibitors of cellular adhesion
Novel cyclic peptides of the selectin 54-63 sequence exhibit unexpected and desired properties. Specific points of cyclization or conformational restriction in conjunction with specific...
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5753627 |
Use of certain complexed somatostatin peptides for the invivo imaging of somatostatin receptor-positive tumors and metastasis
Somatostatin peptides bearing at least one chelating group for a detectable element, said chelating group being linked to an amino group of said peptide, and said amino group having no significant...
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5750088 |
Stable hydrazones linked to a peptide moiety as reagents for the preparation of radiopharmaceuticals
This invention provides novel reagents for the preparation of radiopharmaceuticals useful as imaging agents for the diagnosis of cardiovascular disorders, infection, inflammation and cancer,...
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5750509 |
Amide derivatives of antibiotic A 40926
The present invention is directed to novel antibiotic A 40926 derivatives characterized by having a carboxy, (C 1 -C 4 ) alkoxy-carbonyl, aminocarbonyl, (C 1 -C 4 ) alkylaminocarbonyl, di (C 4 ...
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5747304 |
Fungicidal agents LL-15G256γ,δ, and ε produced by LL-15G256 (Hypoxylon oceanicum)
This invention provides new antifungal compounds of Formula I or II: ##STR1## wherein R, R 1 and R 2 are defined in the specification produced by culture LL-15G256 (Hypoxylon oceanicum), NRRL...
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5747461 |
Synergistic administration of cyclosporine and fructose diphosphate
This invention discloses a method of using fructose-1,6-diphosphate (FDP) to help suppress the rejection of internal organs such as kidneys, hearts, etc. At least three major advantages of FDP in...
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5747448 |
Derivatives of cyclodepsipeptide PF 1022
Novel PF 1022 derivatives--cyclodepsipeptides represented by the below-described formula (I)--and acid addition salts thereof, which have been synthesized according to the present invention, have...
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5741775 |
Cyclohexapeptidyl aminoalkyl ethers
There are disclosed compounds of the general formula ##STR1## wherein all substituents are defined herein. The compounds are useful as antibiotic and antifungal agents.
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5741774 |
Use of a cytokine regulatory agent to treat rheumatoid arthritis
The present invention relates to the use of a cytokine regulatory agent to reduce the severity of rheumatoid arthritis.
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5739104 |
Anti-fungal agents
Compounds of the formula ##STR1## or pharmaceutically acceptable salts thereof wherein R 1 , R 2 , X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , and X 8 , are as set forth herein are described. These...
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5736510 |
Antibiotics 10381v, w, x,y, z1, z2, pre-b and t
Antibiotics 10381v, w, x, y, z1, z2, pre-b and t are antibiotics producible by culturing the microorganism Streptomyces arginensis in an aqueous medium and isolation thereof. The structure of...
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