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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...
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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
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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...
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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 ...
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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...
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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...
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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...
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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...
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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...
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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.
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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,...
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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...
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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...
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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...
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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,...
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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.
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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...
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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 ...
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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...
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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...
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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...
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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...
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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...
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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...
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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....
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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...
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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.
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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...
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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.
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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...
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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...
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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,...
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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...
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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...
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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...
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6051568 |
Thrombin inhibitors, their preparation and use
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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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