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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....
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...
5512560 Conformationally restricted HIV-1 protease inhibitors  
HIV protease inhibitors containing hydroxypyrrolidine or hydroxypiperidine with one or more basic amines are disclosed.
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...
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...
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...
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...
5492910 Retrocarbamate protease inhibitors  
The invention discloses compounds of the formula ##STR1## are disclosed as HIV protease inhibitors.
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...
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,...
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...
5480871 Peptoid α-1 adrenergic receptor ligands  
Compounds of the formula: ##STR1## are useful for treating conditions modulated by α 1 -adrenergic receptors.
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...
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...
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...
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.
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...
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...
5468732 Phosphorus containing renin inhibitors  
Phosphorus containing polypeptides as renin inhibitors, useful as antihypertensive agents.
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...
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...
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...
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...
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...
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.
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...
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...
5447916 Peptoid alpha-1 adrenergic receptor ligands  
Compounds of the formula: ##STR1## are useful for treating conditions modulated by α 1 -adrenergic receptors.
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...
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...
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...
5432160 Nutrient composition  
A nutrient composition such as infusions and nutrient preparations, which contains β-alanyl-L-glutamine.
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...
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...
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...
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...
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...
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...
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 ...
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 ...
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...
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.
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...
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...
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...
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...
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,...
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...
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...
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...