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7528173 |
Plasma carboxypeptidase B inhibitors
Compounds of the following formula (I), for example: (1), wherein R 1 , R 2 , R 3 , and R 4 are described herein, are useful as inhibitors of plasma carboxypeptidase B. Pharmaceutical compositions...
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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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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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7432292 |
Sulfhydantoins as phosphate isosteres
The present invention relates to novel phosphate isosteres. The invention relates to compounds having a sulfhydantoin or a reverse sulfhydantoin moiety, uses thereof, and related methods. The...
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7427621 |
Cyclic sulfamides for inhibition of gamma-secretase
Compounds of formula I:
inhibit the processing of AP by gamma-secretase, and hence are useful for treatment or prevention of Alzheimer's disease.
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7396838 |
Use of 1H-indol-3-yl-2-oxoacetamide compounds
A method of treating cancer including administering to a subject in need thereof an effective amount of a compound of the formula 1:
wherein R 1 , R 2 , R 3 , R 4 , and n are as defined herein.
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7388006 |
Non-steroidal progesting
The present invention relates to non-steroidal progestins of the general formula (I)
wherein
R 1 and R 2 are independently of each other —H or —F, R 3 is —CH 3 or —CF 3 , and Ar is...
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7368479 |
Alpha-sulfonylamino-acetonitriles
The invention relates to α-sulfonylamino-acetonitrile derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein Ar 1 , and Ar 2 ...
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7358239 |
Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z...
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7354941 |
Nicotinamide benzofused-heterocyclyl derivatives useful as selective inhibitors of PDE4 isozymes
Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructive...
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7338968 |
Thiadiazoles AS CXC- and CC- chemokine receptor ligands
Disclosed are novel compounds of the formula:
and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl,...
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7335653 |
Bis-aryl sulfonamides
Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the...
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7307078 |
Polycyclic compounds which modulate PPARγ type receptors and cosmetic/pharmaceutical compositions comprised thereof
Novel polycyclic compounds having the structural formula (I) below:
are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology,...
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7291635 |
5-substituted 1,1-dioxo-1,2,5,-thiadiazolidin-3-one derivatives
Compounds of the formula
provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the...
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7282513 |
Heteroaryl substituted spirocyclic sulfamides for inhibition of gamma secretase
Compounds of formula I are disclosed:
in which X is a 5-membered heteroaryl ring and R is as defined herein. The compounds are inhibitors of the processing of APP by gamma-secretase, and hence...
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7282512 |
Cycloalkyl ketoamides derivatives useful as cathepsin K inhibitors
Cycloalkyl ketoamide derivatives, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such cycloalkyl ketoamide derivatives as...
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7230019 |
Imidazo [2,1-b]-1,3,4-thiadiazole sulfonamides
This invention relates to compounds of Formula (I) and the use of compounds of Formula (I) as neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous...
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7186743 |
Substituted pyrazolyl compounds for the treatment of inflammation
The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating...
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7183299 |
Tetrazoyl oxime derivative and agricultural chemical containing the same as active ingredient
The present invention provides a tetrazoyloxime derivative which is less likely to cause chemical injury to useful plants and is also superior in chemical efficacy to a conventional hetero...
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7169797 |
Protein-tyrosine phosphatase inhibitors and uses thereof
The present invention is directed to compounds of formula (I),
or a pharmaceutically suitable salt or prodrug thereof, which are useful for the selective inhibition of protein tyrosine...
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7160909 |
Cyclopenta[b]indole derivatives as sPLA2 inhibitors
A novel class of tricyclic compounds of the following formula (I) is disclosed together with the use of such compounds for inhibiting sPLA 2 mediated release of fatty acids for treatment of...
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7157478 |
Oxadiazole derivatives for inhibition of gamma secretase
Compounds of formula I: wherein X represents a 5-(R-substituted)-1,2,4-oxadiazole-3-yl moiety are inhibitors of gamma-secretase, and hence useful for treating Alzheimer's disease
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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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7125887 |
Pyrrolidine modulators of CCR5 chemokine receptor activity
Pyrrolidine compounds of Formula (I), (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6a , R 6b , R 7 and R 8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor...
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7125869 |
Polycyclic compounds which modulate PPARγ type receptors and cosmetic/pharmaceutical compositions comprised thereof
Novel polycyclic compounds having the structural formula (I) below:
are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology,...
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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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7078418 |
1-aziridino-1-hydroxyiminomethyl-derivates, method for the production thereof and medicaments containing said compounds
Described are new 1-aziridino-1-hydroxyiminomethyl derivatives with the general formula (I), wherein R is able to is a single bond or a linker moiety capable of covalently bonding two aziridine...
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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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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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7041689 |
Heteroaryl substituted spriocyclic sulfamides for inhibition of gamma secretase
Compounds of formula I are disclosed: in which X is a 5-membered heteroaryl ring and R is as defined herein. The compounds are inhibitors of the processing of APP by gamma-secretase, and hence are...
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7041688 |
Alkynly-substituted spirocyclic sulfamides for the treatment of alzheimer's disease
Compounds of formula (I) are disclosed. The compounds inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease
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7030119 |
Method for treating chronic pain using MEK inhibitors
The invention features a method for treating chronic pain using a compound of formula (I).
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7022721 |
Method and composition for rejuvenating cells, tissues, organs, hair and nails
In one embodiment, the present invention relates to compounds and compositions including pharmaceutical compositions containing the compounds and associated methods that uncouple sugar-mediated...
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6974829 |
Succinoyl aminopyrazoles and related compounds
This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl...
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6927215 |
Heterocyclic fluoroalkenyl thioethers and the use thereof as pesticides (I)
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 2 to 10, n...
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6911457 |
Diabetes imaging probes
The present invention relates to novel imaging probes and methods for using the probes in diagnostic imaging processes and other imaging processes to determine physiological functions.
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6858607 |
7,8-fused 4H-chromene and analogs as activators of caspases and inducers of apoptosis and the use thereof
The present invention is directed to substituted 4H-chromene and analogs thereof, represented by the general Formula I:
or pharmaceutically acceptable salts or prodrugs thereof, wherein:
...
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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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6743817 |
Substituted fused pyrroleimines and pyrazoleimines
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R 1 and R 2 are defined herein. These compounds are highly selective agonists,...
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6720342 |
Heterocyclic compounds and their preparation and use
The present invention relates to therapeutically active azabicyclic compounds, a method of preparing the same and to pharmaceutical or veterinary compositions comprising the compounds. The novel...
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6706743 |
β3 adrenergic receptor agonists and uses thereof
The instant invention provides β 3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds,...
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6686363 |
Cyclopropyl containing oxazolidinone antibiotics and derivatives thereof
This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and...
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6677360 |
Biphenyl and biphenyl-analogous compounds as integrin antagonists
The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of...
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6617339 |
Oxazolidinone derivatives, process for their preparation and pharmaceutical compositions containing them
Compounds of formula (I) as defined herein, or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, are useful as antibacterial agents. Processes for their manufacture and...
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6559171 |
7-oxo-2-azabicyclo&lsqb 2.2.1&rsqb heptanes as selective muscarinic receptor antagonist
The present invention relates to muscarinic receptor modulators, specifically, 7-oxo-2-azabicyclo[2.2.1]heptanes of formula (I) which are useful for the treatment of various diseases and...
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6555576 |
Method for treating exercise induced asthma
Methods of treating exercise-induced asthma using a PDE-4 inhibitor are disclosed.
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6552031 |
Synergistic analgesic combination of oxycodone and rofecoxib
Disclosed is a pharmaceutical composition, comprising a combination of a dose of rofecoxib or a pharmaceutically acceptable salt thereof and a dose of oxcodone or a pharmaceutically acceptable salt...
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6537549 |
Cytokine antagonists for the treatment of localized disorders
Cytokine antagonists for use in localized clinical disorders are provided for the treatment and prevention of damage to the optic nerve, other cranial nerves, spinal cord, nerve roots, peripheral...
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