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5514654 |
N-acyldipeptides, processes for the preparation thereof and pharmaceutical compositions containing the same
N-acyldipeptides of formula I ##STR1## wherein R represents a rest of formula ##STR2## and R 4 , Y, m, n and Z have the meaning as defined in the description, R 1 represents hydrogen, a 1-10 C....
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5514694 |
Peptidyl ketoamides
A novel class of peptide α-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally...
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5512560 |
Conformationally restricted HIV-1 protease inhibitors
HIV protease inhibitors containing hydroxypyrrolidine or hydroxypiperidine with one or more basic amines are disclosed.
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5508266 |
Gem-disubstituted amino acid derivatives
Disclosed are the compounds of formula I ##STR1## wherein R represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl-lower alkyl or cycloalkyl-lower alkyl; R 1 represents hydrogen, lower...
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5504070 |
Inhibitors of the conversion of big endothelin to endothelin
Novel and known compounds are described which inhibit endothelin converting enzyme (ECE), thereby preventing the conversion of Big Endothelin (BET) to Endothelin (ET). Pharmaceutical usefulness and...
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5496805 |
Inhibitors of neutral endopeptidase
Diuresis, natriuresis, and the lowering of blood pressure are produced in a host by administering one or more neutral endopeptidase inhibitors. An additional blood pressure lowering agent such as...
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5494897 |
Endothelin antagonistic peptide
A peptide derivative of the formula: ##STR1## is a novel compound having antagonism against three endothelin isopeptides. A 2-cyanotryptophan or a protected compound thereof, is an intermediate for...
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5492910 |
Retrocarbamate protease inhibitors
The invention discloses compounds of the formula ##STR1## are disclosed as HIV protease inhibitors.
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5492896 |
Pseudopeptides having an antiviral action
The invention relates to new pseudopeptides having an antiviral action, oft he general formula (I) ##STR1## with the meanings given in the description for the substituents, to a process for their...
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5487898 |
Compositions and method for the sublingual or buccal administration therapeutic agents
Pharmaceutical compositions for the sublingual or buccal administration of therapeutic agents which are normally degraded upon oral administration comprise such a therapeutic agent, a solvent,...
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5484771 |
Antiherpes peptide derivatives having a 1,4-dioxo-C, N-terminus
Described herein are peptide derivatives of the formula R 1 NH--CO--Q--C(O)--NR 2 --CH[CH 2 C(O)--Y]--C(O)--NH--CH[CR 3 (R 4 )--COOH]--C(W)--NH--CHR 5 --Z wherein R 1 is an optionally...
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5480871 |
Peptoid α-1 adrenergic receptor ligands
Compounds of the formula: ##STR1## are useful for treating conditions modulated by α 1 -adrenergic receptors.
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5478808 |
2-amino-6,7-dihydroxy-4-thiaheptanoic acid derivatives, production and use thereof
A compound of the formula: ##STR1## wherein each of R 1 and R 2 is hydrogen or aliphatic acyl, A is amino which may be protected, X is an amino acid sequence consisting of 1 to 10 amino acid...
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5470834 |
Sulfoximine and suldodiimine matrix metalloproteinase inhibitors
Novel sulfoximine and sulfodiimine matrix metalloproteinase inhibitors of the formula, ##STR1## wherein: R 1 is selected from the group consisting of lower-alkyl, hydroxy lower-alkyl, amino...
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5470832 |
Inhibitors of geranylgeranyl-protein transferase
The compounds disclosed am analogs of the CAAX motif of proteins that can be modified by geranylgeranylation in vivo that selectively inhibit the geranylgeranylation of several proteins. The...
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5470849 |
γ-turn peptidomimetics as fibrinogen antagonists
This invention relates to a method of inhibiting platelet aggregation, and compounds which are mimics of the peptide sequence Arg-Gly-Asp.
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5470876 |
Topical sod for treating hair loss
SOD for treating hair loss is disclosed. The SOD has utility in a topical pharmaceutical formulation for the cosmetic treatment of hair loss and the cosmetic stimulation of hair growth. The SOD...
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5468731 |
Peptide compounds, a process for preparation thereof and pharmaceutical composition comprising the same
A compound of the formula: ##STR1## wherein R 1 is aryl, or a group of the formula: ##STR2## wherein X is CH or N, and Z is O or N--R 5 , in which R 5 is hydrogen or lower alkyl, R 2 is...
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5468732 |
Phosphorus containing renin inhibitors
Phosphorus containing polypeptides as renin inhibitors, useful as antihypertensive agents.
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5464821 |
Small peptidic compounds useful for the treatment of glaucoma
Small peptidic compounds containing a small and branched chained amino acid residue, pharmaceutical compositions containing at least one such compound active against glaucoma and intraocular...
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5464819 |
Physiologically active peptide having immunoregulatory activities
A novel, substantially pure, physiologically active peptide is disclosed, comprising an amino acid sequence selected from Gly-Glu (SEQ ID NO. 5), Pro-Val-Val (SEQ ID NO. 6), Glu-Pro-Val-Val (SEQ ID...
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5462954 |
Substituted phenyl phenol leukotriene antagonists
Antagonists having a substituted phenyl phenol or a substituted phenolic biphenyl structure, and various derivatives thereof, are specific leukotriene antagonists. Their structures, use and...
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5459129 |
Condensed heterocyclic compounds, their production and use
A novel compound of the formula: ##STR1## wherein a ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent cyclic or chain group; either one of...
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5459131 |
Renin inhibitors
Renin inhibiting compounds of the formula: ##STR1## wherein A is a moiety selected from those of the formula: ##STR2## where Z is O, S, SO, or SO 2 , P is 1 or 2 and X is --O-- or --S--; and...
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5457114 |
Amidinophenylalanine derivatives, a process for the preparation thereof, use thereof and agents containing these as anticoagulants
Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.
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5455229 |
Method for minimizing and containing ischemic and reperfusion injury
The present invention is a method for minimizing and containing injury caused when tissue is subject to ischemia and reperfusion. The method comprises administering certain derivatized tripeptide...
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5451571 |
Process and composition for treating hypertension
The present invention is directed to a process for treating hypertension in mammals through the administration of an effective amount of a Z-Pro-prolinal (ZPP) composition. In addition, the present...
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5447916 |
Peptoid alpha-1 adrenergic receptor ligands
Compounds of the formula: ##STR1## are useful for treating conditions modulated by α 1 -adrenergic receptors.
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5447915 |
Terminally blocked antiviral peptides
This invention relates to antiviral peptide compounds and to methods of inhibiting infection of human cells by viruses. This invention pertains more specifically to peptides that are chemically...
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5444061 |
Anti-cancer compounds
Quinazolines of the formula: ##STR1## wherein R 1 -R 8 are defined as in the specification, or a pharmaceutically acceptable salt, ester or amide thereof areof therapeutic value, particularly in...
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5436229 |
Bisulfite adducts of arginine aldehydes
This invention relates to bisulfite adducts of L-Arginine aldehyde derivatives, pharmaceutical formulations containing those adducts and methods of their use as thrombin inhibitors, coagulation...
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5432160 |
Nutrient composition
A nutrient composition such as infusions and nutrient preparations, which contains β-alanyl-L-glutamine.
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5432159 |
N-(α-substituted-pyridinyl)carbonyl dipeptide antihypertensive agents
Dipeptide derivatives are taught which are of general formula (I) ##STR1## including tautomeric forms thereof, wherein: n is 0 or an integer of from 1 to 3; R is OH, SH, COOH, NH 2 , halogen, OR 4...
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5430024 |
Peptides bearing N-terminal amidino moieties and their use as inhibitors of platelet aggregation
Acetic acid derivatives of formula H 2 N(NH)C--X--Y--CO--Z--CH(Q 1 )COOQ 2 I and hydrates, solvates and physiologically acceptable salts thereof are useful to inhibit the binding of...
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5430021 |
Hydrophobic drug delivery systems
A pharmaceutical preparation including a drug incorporated into hydrophobic particles comprised of long chain carboxylic acid or ester thereof or long chain alcohol, wherein the particles are...
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5428021 |
Human leukocyte elastase (HLE) inhibitors, and related pharmaceutical compositions and methods of use
Novel therapeutic agents useful as inhibitors of HLE are provided. The compounds have the structural formula (I) ##STR1## wherein R 1 through R 9 , m, n and p are as defined herein. Methods of...
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5428116 |
Synthesis of complex polyamines for ampholyte production
New synthesis and analysis procedures for novel crosslinked polyamines and ampholytes. Polyamines are crosslinked with tartaric acid ester, malonic acid ester, or polycarboxylic acid esters of the...
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5424292 |
5-aminosalicylic acid derivatives for the therapy of chronic inflammatory bowel diseases
5-Aminosalicylic acid derivatives acylated at the amino group with glutamic or aspartic acid and/or having the carboxy group involved in a peptide bond with the leucyl-prolyl residue are useful as...
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5424293 |
Phenylimidazolidine derivatives and their use
Phenylimidazolidine derivatives of the general formula I ##STR1## in which, for example, Y denotes --CH 2 --CH 2 --CO-- r denotes 0 to 3 Z denotes oxygen W denotes hydroxyl R 1 ...
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5422342 |
2,3-disubstituted isoxazolidines, agents containing them and their use
The invention relates to compounds of the formula ##STR1## in which A denotes an optionally substituted radical from the series comprising alkyl, acyl, cycloalkyl, aryl and heteroaryl; A 1 ...
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5420106 |
Method and composition having enhanced alpha-hydroxy acid skin permeation and retention
Methods of enhancing skin permeation and skin retention of α-hydroxy acids for the treatment of dermatological disorders by applying a composition containing an amphoteric salt of an α-hydroxy...
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5418218 |
Histidyl-proline diketopiperazine (cyclo his-pro) a cns-active pharmacologic agent
A stable peptide with a direct effect on the central nervous system that can be administered in a general manner, such as orally, is described.
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5405835 |
Compositions for use in dietetics, reanimation and therapeutics, containing a protein fraction based on three types of minipeptides
A composition intended for use in dietetics, reanimation and therapeutics is provided. The composition includes lactoserum minipeptides, casein minipeptides, and casein minipeptides without...
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5403843 |
Pyrrolopyrimidinyalglutaminate derivatives and their use
A condensed pyrimidine derivative of the formula (I): ##STR1## wherein the ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent 5- or...
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5403824 |
Methods for the treatment of osteoporosis
Methods of treatment for osteoporosis in a human or other animal subject, comprising administering to said subject a safe and effective amount of an active selected from the group consisting of...
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5401722 |
Peptide analogues
New peptide analogues of the formula I R 1 --Z--NR 2 --CHR 3 --CR 4 --(CH 2 ) o --(CR 5 ) t --(CH 2 ) v --CE--C w H 2w --R 6 I in which R 1 to R 6 Z, E, o, t and w have the meanings...
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5399487 |
6-peptidylamino-1-naphthalenesulfonamides useful as fluorogenic proteolytic enzyme substrates
The present invention encompasses compounds of formula I: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof; wherein R 1 is hydrogen, lower alkyl, alkenyl, alkynyl, cycloalkyl,...
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5391486 |
Physiologically active substance BE-16627
The present invention relates to new stromelysin (human)-inhibitors, i.e., physiologically active substances BE-16627 represented by the general formula: ##STR1## wherein R represents a hydrogen...
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5389610 |
Carboxyalkylcarbonyl aminoacid endopeptidase inhibitors
Carboxyalkylcarbonyl aminoacid inhibitors of endopeptidases of the formula: ##STR1## or pharmaceutically acceptable salt thereof, wherein R 1 is H, alkyl, arylalkyl, aryl or aryloxyalkyl; R 2 is...
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5389614 |
Hydantoin derivatives
The invention relates to compounds of the formula I ##STR1## in which R 1 , R 2 , R 3 , R 4 and Y have the meanings indicated in Claim 1, to processes for their preparation and their use as active...
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