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7378440 Substituted benzoylureido-o-benzoylamides, process for their preparation and their use  
The invention relates to substituted benzoylureido-o-benzoylamides and to their physiologically tolerated salts and physiologically functional derivatives. The invention relates to compounds of...
7354905 Prodrugs of thrombin inhibitors  
There is provided compounds of formula I, R 1 O(O)C—CH 2 —(R)Cgl-Aze-Pab-R 2 I
7309714 Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes  
The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or...
7273858 Salts  
There is provided pharmaceutically-acceptable acid addition salts of compounds of formula I, wherein R 1 represents C 1-2 alkyl substituted by one or more fluoro substituents; R 2 ...
7241757 Amidino derivatives and their use as thrombin inhibitors  
There is provided compounds of formula I wherein R 1 , R x , Y, R y , n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such...
7238683 Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes  
The present invention is directed to fused phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-RV inhibitors”) and which are useful in the treatment or...
7232812 Substituted azetidine compounds, their preparation and use as medicaments  
The present invention relates to substituted Azetidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the...
7220734 1-(amino)indanes and (1,2-dihydro-3-amino)-benzofurans, benzothiophenes and indoles as Edg receptor agonists  
The present invention encompasses compounds of Formula (I): as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and...
7202236 Modified release pharmaceutical formulation  
A modified release pharmaceutical composition comprising, as active ingredient, a compound of formula (I), wherein R 1 represents C?1-2#191 alkyl substituted by one or more fluoro substituents; R...
7160874 Phenylalanine derivatives  
Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
7129233 Mandelic acid derivatives and their use as thrombin inhibitors  
There is provided a compound of formula I wherein R a , R 1 , R 2 , Y and R 3 have meanings given in the description and pharmaceutically-acceptable derivatives (including prodrugs) thereof,...
7087594 Alkyl ether derivatives or salts thereof  
An alkyl ether represented by the general formula: or its salt. This compound has activity to protect neurons, activity to accelerate nerve regeneration and activity to accelerate neurite...
7084120 Prodrugs of DP IV-inhibitors  
Prodrug compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The Prodrug compounds...
7060697 Immunosuppressant compounds and compositions  
The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds...
7056907 Mandelic acid derivatives and their use as thrombin inhibitors  
There is provided a compound of formula (1) and pharmaceutically-acceptable derivatives (including prodrugs) thereof. Which compound and derivatives are useful as, or are as useful as prodrugs of,...
7030147 Combinations comprising an antidiarrheal agent and an epothilone or an epothilone derivative  
Epothilone derivatives are co-administered with an antidiarrheal agent, e.g., a DPP-IV inhibitor, in the treatment of a proliferative disease.
6921758 Amino acid derivatives  
There is provided amino acid derivatives of formula I, wherein p, q, R 1 , R 2 , R 3 , R 4 , Y, n and B have meanings given in the description which are useful as competitive inhibitors of...
6872717 Pharmacological uses of azetidine derivatives  
A method of treating or preventing obesity, this method comprising administering to a patient in need of such treatment an effective amount of a compound of formula in which R, R 3 and R 4 ...
6864249 Piperidine and azetidine thrombin inhibitors  
The present invention relates to a compound having formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I and pharmaceutical compositions containing them are of...
6831078 Azetidinecarboxamide derivatives for treating CNS disorders  
A compound of formula (1) wherein R 1 is aryl; and R 2 is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and their use in therapy, particularly for the treatment and...
6803370 Alpha amino acid derivatives—inhibitors of leukocyte adhesion mediated by VLA-4  
Disclosed are certain alpha amino acid compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such...
6710040 Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors  
The invention relates to new therapeutically active and selective inhibitors of the enzyme dipeptidyl peptidase-IV, pharmaceutical compositions comprising the compounds and the use of such...
6599894 Amidinobenzylamine derivatives and their use as thrombin inhibitors  
There is provided compounds of formula I wherein R 1 , R 2 , Y, R 3 and R 4 have meanings given in the description which are useful as, or as prodrugs of, competitive inhibitors of...
6596716 2-propane-sulphonamide derivatives  
The present invention relates to the potentiation of glutamate receptor function using certain 2-propane-sulphonamide derivatives. It also relates to novel 2-propane-sulphonamide derivatives, to...
6528503 Thrombin inhibitors  
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g....
6521619 Aryl phenylcyclopropyl sulfide derivatives and their use as cell adhesion inhibiting anti-inflammatory and immune suppressive agents  
The present invention relates to novel cyclopropane-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising...
6479479 Azetidine derivatives, their preparation and pharmaceutical compositions containing them  
Compounds of formula: in which R represents a CR 1 R 2 , C═C(R 5 )SO 2 R 6 or C═C(R 7 )SO 2 alk radical, their preparation and the pharmaceutical compositions containing them.
6462021 Use of low molecular weight thrombin inhibitor  
According to the invention there is provided the use of melagatran, or a pharmaceutically-acceptable derivative thereof, for the manufacture of a medicament for the treatment of ischemic disorders...
6455531 Hydroxamic acid derivatives  
Compounds having therapeutic utility are of the formula wherein NB 2 is heterocycloalkyl and R 1 and R 2 are each various substituents or a cyclic group.
6417229 α-sulfonylamino hydroxamic acid inhibitors of matrix metalloproteinases for the treatment of peripheral or central nervous system disorders  
The present invention relates to a method of using a compound of the formula (I): wherein A, X 1 , X 2 and Q are as defined herein, a pharmaceutically acceptable salt thereof, or a...
6306880 Triazole antifungal agent  
A triazole compound having the formula: ##STR1## wherein Ar 1 represents a phenyl group which may be substituted; Ar 2 represents a phenyl group which may be substituted; R 0 represents a...
6303636 Arylsulfonylamino hydroxamic acid derivatives  
A compound of the formula ##STR1## wherein R 1 , R 2 and Q are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration,...
6251949 Oxime derivatives, hydrazone derivatives and use thereof  
Compounds having fungicidal activities and represented by general formula (I) and salts and hydrates thereof ##STR1## wherein R 1 represents an optionally substituted aryl, an optionally...
6239175 Carbamoyloxy derivatives of mutiline and their use as antibacterials  
Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R 1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is...
6191168 Methods for the use of nonprotein amino acids as therapeutic agents  
Provided are compositions comprising nonprotein amino acids and modified amino acids, as well as methods for the use of nonprotein amino acids and modified amino acids in inhibiting the growth of...
6051568 Thrombin inhibitors, their preparation and use  
6034067 Serine protease inhibitors  
The invention relates to a compound having formula (I), wherein A, B, X, N, Z and Q are defined as described in the description. The compounds of the invention have anticoagulant activity and can...
5932567 Thrombin inhibitors  
Thrombin inhibitors of the formula ##STR1## where R 1 , A, B and D have the meaning indicated in the description, and intermediates for the preparation thereof are described. The compounds I are...
5932196 Buffered emulsion compositions containing actives subject to acid or base hydrolysis  
The present invention are for emulsion compositions and the process for making such compositions containing biological and cosmetic actives subject to hydrolysis of actives during processing and...
5877203 Treatment for atherosclerosis and other cardiovascular and inflammatory diseases  
Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of...
5859002 HIV protease inhibitors  
HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These...
5798360 N-(aminoalkyl)- and/or N-(amidoalkyl)- dinitrogen heterocyclic compositions  
Compositions are provided comprising novel di-nitrogen heterocycle compounds containing N-(aminoalkyl) and/or N-(amidoalkyl) groups. An additional situs of functionality is also provided. The...
5776927 Methionine sulfone and S-substituted cysteine sulfone derivatives as enzyme inhibitors  
This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The...
5747522 Amino acid derivatives  
N-Acyl-α-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R"' and Q have the significance given in the description, can be used for the treatment or prophylaxis of...
5719141 2,9-diamino- and 2-amino-8-carbamoyl-4-hydroxy-alkanoic acid amide derivatives  
Compounds of the formula I ##STR1## in which R 1 is arylamino, N-aryl-N-(lower alkoxy-lower alkyl)-amino, N-aryl-N-aryl-lower alkyl-amino or heterocyclyl bonded via a ring carbon atom, X is a...
5691329 Compounds containing basic and acidic termini useful as fibrinogen receptor antagonists  
This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using...
5639746 Hydroxamic acid-containing inhibitors of matrix metalloproteases  
The invention provides hydroxamic acid-containing compounds which are useful as inhibitors of matrix metalloproteases and which are effective in treating conditions associated with excess activity...
5622984 Amidinophenol derivatives  
Amidinophenol derivatives of the formula (I): ##STR1## wherein R 1 and R 2 are (i) H, (ii) C1-4 alkoxy, (iv) C2-5 acyl, (v) halogen, (vi) NO 2 , (vii) benzoyl, (viii) COOR 4 (in which R 4 is...
5476849 Methods for glycosylation inhibition using amino-benzoic acids and derivatives  
The present invention relates to compounds, compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent...
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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