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7612104 |
Bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, processes for their preparation, pharmaceutical compositions and methods for their use
The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof as well as their physiologically acceptable salts and pharmaceutical...
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7592461 |
Indane modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
Novel non-steroidal compounds are provided that are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes,...
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7589212 |
Human protein tyrosine phosphatase inhibitors and methods of use
The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to...
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7585882 |
Phosphodiesterase 4 inhibitors
Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula I:
wherein R 1 , R 2 ,...
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7585460 |
Method for inhibiting the biological acidification of water in contact with materials containing sulfur
The invention relates to a method for inhibiting the biological acidification of water which is in contact with materials containing sulfur in reduced form or with elemental sulfur, susceptible to...
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7576108 |
Substituted arylcyclopropylacetamides as glucokinase activators
According to the present invention there is provided a compounds of formula (I): and pharmaceutically acceptable salts thereof.
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7557138 |
5-phenoxyalkoxypsoralens and methods for selective inhibition of the voltage gated Kv1.3 potassium channel
Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects,...
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7553973 |
Pharmaceutical compounds
The instant invention provides compounds of Formula Ia which are leukotriene biosynthesis inhibitors.
Compounds of Formula Ia are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic,...
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7524863 |
Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic...
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7459473 |
N-linked sulfonamides of N-heterocyclic carboxylic acids or carboxylic acid isosteres
This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including...
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7449486 |
Mitotic kinesin inhibitors and methods of use thereof
This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the...
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RE40558 |
Therapeutic uses of di-aryl acid derivatives
The use of diaryl acid derivatives of formula (I)
or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and...
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7439242 |
PPARγ modulators
Modulators of PPARγ activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.
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7435748 |
Gamma-secretase inhibitors
Compounds of formula I:
inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease.
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7425636 |
Thiadiazoline derivative
(wherein R 1 and R 4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or...
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7408068 |
Compounds for the treatment of neurodegenerative disorders
The present invention relates to compounds of the Formula
wherein R 3 , R 5 , R 7 , U, X, Y and Z are as defined. Compounds of the Formula I have activity inhibiting production of Aβ-peptide....
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7407976 |
Thiazoles and oxazoles useful as modulators of ATP-Binding Cassette transporters
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions...
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7402606 |
Derivatives of 1-(oxoaminoacetyl) pentylcarbamate as cathepsin K inhibitors for the treatment of bone loss
Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The...
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7399765 |
Substituted diazabicycloalkane derivatives
Compounds of formula (I)
Z-Ar 1 —Ar 2 (I)
wherein Z is a diazabicyclic...
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7387798 |
Method and composition for resuscitation
The key obstacle for current resuscitation is the acutely limited time window. The major reason for the limited time window is that the brain and spinal cord are extremely vulnerable to...
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7354944 |
Thiadiazole compounds and methods of use
The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and...
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7348345 |
Nonnucleoside reverse transcriptase inhibitors
This invention relates to methods of treating an HIV infection with novel heterocyclic compounds of formula I wherein R 1 —R 4 , X 1 and X 2 are as defined in the summary and pharmaceutically...
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7338966 |
Substituted oxindole derivatives as tyrosine kinase inhibitors
The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful...
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7326695 |
Anti-bacterial agents based upon oxoanion binding
Compounds of the structure I:
are useful for treating bacterial growth, wherein E is selected from the group consisting of B, P, and S, T 1 and T 2 are each independently selected from...
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7232820 |
Thiadiazole-amine compounds for the treatment of neurodegenerative disorders
The present invention relates to compounds of the Formula I
wherein R 1 , R 3 , R 5 , R 7 , X, Y and U are as defined. Compounds of the Formula I have activity inhibiting production of...
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7211592 |
Substituted an unsubstituted benzooxathiazoles and compounds derived therefrom
The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydro-benzo[c]isothiazole 2,2-dioxides, to...
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7183277 |
Carboxylic acid amides
Novel compounds of the formula I
in which
D, W, X, Y, T and R 1 are as defined in Patent Claim 1,
are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or...
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7153873 |
Salts of bicyclic, N-acylated imidazo-3-amines and imidazo-5-amines
Salts of a bicyclic, N-acylated imidazo-3-amine or an imidazo-5-amine of the formula:
addition products thereof with acids, and methods for preparing the salts and addition products. Also...
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7148219 |
Biaryl heterocyclic compounds and methods of making and using the same
The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of...
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7122565 |
Thiadiazoles and oxadiazoles and their use as phosphodiesterase-7 inhibitors
The invention provides 1,3,4-thiadiazoles and 1,3,4-oxadiazoles having the following Formula I:
in which,
Y is S or O, R 1 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl,...
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7119099 |
Inhibitors of papilloma virus
A compound of formula (I) or its enantiomers or diastereoisomers thereof:
wherein: A,; X, W, R 1 , Y; R 3 ; and R 4 are as defined herein.
The compounds of the invention may be used as...
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7115658 |
Inhibitors of hepatitis C virus RNA-dependent RNA polymerase
Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virus
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7115639 |
Pyrrolidine oxadiazole- and thiadiazole oxime derivatives being oxytocin receptor antagonists
The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such...
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7115624 |
Method of inhibiting protein tyrosine phosphatase 1B and/or T-cell protein tyrosine phosphatase 4 and/or other PTPases with an Asp residue at position 48
The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTPα, PTPε, PTPμ, PTPδ,...
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7105556 |
Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
Compounds are provided which have the structure
wherein Q is C or N, X 1 is C or N, and R 1 , R 2 , R 2a , R 2b , R 2c , R 3 , Y, A, m, n, X 2 , X 3 and X 4 are as defined herein, which...
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7098201 |
Heteroaromatic derivatives having an inhibitory activity against HIV integrase
A compound of the formula (I):
wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COOR A wherein R A is hydrogen or ester residue, —CONR B R C wherein R B ...
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7078403 |
Antiviral agents
Disclosed herein are compounds of formula II:
wherein Alk, Z, X 1 , X 2 , R 1 , —R 10 and R 11 are defined herein, and their salts and pharmaceutically acceptable derivatives thereof, as...
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7071217 |
Substituted oxindole derivatives as tyrosine kinase inhibitors
The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful...
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7071180 |
Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases
The invention relates to compounds of the general formula (I):
wherein
Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO 2 —, —NH—, (ii) a C 1-4...
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7060718 |
Arylsulfonanilide ureas
The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as...
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7045544 |
Substituted 2,5-diamidoindoles as ECE inhibitors for the treatment of cardiovascular diseases
The invention relates to compounds of formula (I), to a method for the production thereof, and to the use of the same as pharmaceuticals for the treatment of diseases in humans and/or animals
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7041670 |
Florfenicol-type antibiotics
The present invention relates to novel florfenicol compounds having the chemical structure:
wherein the compounds are useful for the treatment and/or prevention of bacterial infections in a...
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6908937 |
Heterocyclic fluoroalkenyl thioethers (II)
The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I)
in which
X represents hydrogen, halogen or alkyl, m represents integers from 3 to 10, n...
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6903104 |
Indol-3-YL-2-oxoacetamide compounds and methods of use thereof
The invention is based on the discovery that certain 3-oxoacetamideindolyl compounds have potent anticancer and anti-angiogenic activity. The 3-oxoacetamideindolyl compounds are of the following...
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6894054 |
Heterocyclic inhibitors of glycine transporter 2
Compounds, compositions, and methods for inhibiting the glycine transporter 2 and for inhibiting glycine transporter mediated neuronal activity. These compounds are particularly useful for...
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6890942 |
Acyl sulfonamides as inhibitors of HIV integrase
The present invention relates a series of compounds of Formula I
wherein R 1 , R 2 , R 3 , and B are as defined in the specification. The compounds are useful for the inhibition of HIV...
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6852716 |
Substituted-aryl compounds for treatment of disease
The invention provides compounds of Formula I:
These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of...
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6846839 |
Methods for treating diseases and disorders related to unregulated angiogenesis and/or vasculogenesis
The present invention relates to methods for treating diseases and disorders related to unregulated angiogenesis and/or vasculogenesis. More specifically, this invention relates to methods for...
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6800649 |
Method for inhibiting c-jun expression using JAK-3 inhibitors
The invention provides a method for inhibiting c-jun activation in mammalian or avian cells comprising contacting the cells with a substance that inhibits the activity of Janus family kinase 3...
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6777418 |
Retinoid compounds (I)
The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical...
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