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9024028 Methods and compositions for the synthesis of multimerizing agents  
The invention features methods and compositions for the synthesis of multimerizing agents. An exemplary method for producing AP20187 may comprise: (a) coupling...
9006227 Modulators of cortical dopaminergic- and NMDA-receptor-mediated glutamatergic neurotransmission  
The present invention relates to novel substituted phenoxyethylamine derivatives, useful as modulators of cortical and basal ganglia dopaminergic and N-methyl-D-aspartate (NMDA) receptor-mediated...
8980877 Spirocyclic derivatives as histone deacetylase inhibitors  
This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer...
8962835 Imidazopyrazine Syk inhibitors  
Certain imidazopyrazines of Formula (I): or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from...
8912188 Substituted quinoxaline carboxylic acids for the inhibition of PASK  
Disclosed herein are substituted quinoxaline carboxylic acids of Formula (I): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the...
8895559 Quinoxalines derivatives and pharmaceutical compositions and kits  
A variety of specific compounds within the scope of formula I which are useful as PI3K inhibitors and can be employed for the treatment of autoimmune diseases, inflammation, cardiovascular...
8877759 Aminopyrazines as ATR kinase inhibitors  
The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this...
8865715 Substituted 7-(1,2,3-Triazol-4-yl)-pyrrolo[2,3-b]pyrazines  
The invention relates to compounds the formula (I): and pharmaceutically usable salts, tautomers and stereoisomers thereof, wherein R1, R2 and R3 are defined herein. The compounds of formula (I)...
8853196 Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy  
The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention...
8846655 4-substituted-2-phenoxy-phenylamine delta opioid receptor modulators  
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows:...
8822469 Pyrrolo[2,3-B]pyrazines useful as inhibitors of ATR kinase  
The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the...
8815926 Substituted pyrrolo[3,4-D]imidazoles for the treatment of MDM2/4 mediated diseases  
The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a...
8742110 Spiroxazolidinone compounds  
Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of...
8697888 Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors  
In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as...
8680159 Bradykinin 1 receptor modulating compounds  
Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions...
8669252 Prolylcarboxypeptidase inhibitors  
Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the...
8658646 Pyrrolopyrazine kinase inhibitors  
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the...
8658794 8-methyl-1-phenyl-imidazol[1,5-a]pyrazine compounds as Lck inhibitors and uses thereof  
The present invention provides 8-methyl-1-phenyl-imidazo[1,5-a]pyrazine derivatives according to formula I or pharmaceutically acceptable salts thereof. The compounds of the current invention show...
8633182 Indanyloxyphenylcyclopropanecarboxylic acids  
The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular...
8592608 Triple reuptake inhibitors and methods of their use  
Provided herein are bicyclic compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological...
8586573 N-(Aminoheteroaryl)-1H-indole-2-carboxamide derivatives, and preparation and therapeutic application thereof  
The invention concerns compounds of general formula (I): Wherein n, X1, X2, X3, X4, Y, Z, Z1, Z2, Z3 and Z4 are as defined herein. The invention also concerns a process for the preparation of...
8575134 Aminocarboxylic acid derivative and medicinal use thereof  
The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same....
8546563 Compounds which modulate the CB2 receptor  
Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are...
8518945 Pyrrolopyrazine kinase inhibitors  
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X′ and Y are defined as described herein, which inhibit JAK and SYK...
8492371 Compounds as cannabinoid receptor ligands  
Disclosed herein are compounds of formula (I) wherein Ring A and R1 are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods for treating conditions...
8492499 Addition compounds as dispersants and dispersion stabilizers  
The invention relates to addition compounds which are obtainable by reacting a) one or more polyisocyanates containing uretdione groups withb) one or more compounds of the formula (I) Y—(XH)n (I)...
8492561 Azetidine derivatives as sphingosine 1-phosphate (S1P) receptor modulators  
The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of...
8460851 Salt and photoresist composition containing the same  
A salt represented by the formula (I): wherein Q1 and Q2 each independently represent a fluorine atom or a C1-C6 perfluoroalkyl group, L1 represents *—CO—O-La- or *—CH2—O-Lb-, * represents a...
8440667 Imidazopyrazine Syk inhibitors  
Certain imidazopyrazines of Formula (I): and pharmaceutical compositions thereof are provided herein. Methods of treating patients responsive to the inhibition of Syk activity, which comprises...
8431580 4-aminopyrimidine derivatives as histamine H4 receptor antagonists  
4-Aminopyrimidine derivatives of formula (I) that are useful as histamine H4 receptor antagonists.
8399451 Heterocyclic compounds  
Disclosed are compounds of Formula (I) or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein: A is Q is a substituted 5-membered monocyclic heteroaryl group;W is CH2, O, or NH;...
8389507 2-azetidinemethaneamines and 2-pyrrolidinemethaneamines as TAAR-ligands  
The present invention relates to compounds of formula I wherein R1, R2, R3, Ar, n and o are as defined herein and to their pharmaceutically acceptable active salts. Compounds of formula I have a...
8389509 Substituted pyrazole compounds  
Disclosed are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: n is zero or an integer selected from 1 through 4; R1 is cycloalkyl, aryl, heteroaryl, or...
8367654 8-AZA tetracycline compounds  
The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also...
8361998 Compounds and their use as IKACh blockers  
The invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, x and y are as defined herein. Compounds according to...
8357717 Spiro group-containing amide compounds having bradykinin 1 receptor (B1R) activity  
Substituted spiroamide compounds corresponding to formula (I): wherein A, B, Q1, Q2, Q3, Q4, R1, R8, R9a, R9b, R12, R13, R200 and R210 have defined meanings, processes for their preparation,...
8349825 Spirocyclic compounds  
The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal...
8344008 Aryl-substituted bridged or fused diamines as modulators of leukotriene A ydrolase  
Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A4...
8329700 Pyrazine compounds as phosphodiesterase 10 inhibitors  
Pyrazine compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein m, n, p, R1, R2, R3, R4, X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, Y and Z are defined in the...
8309734 Substituted pyridines as GPBAR1 agonists  
This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as...
8309597 1,1′-diadamantyl carboxylic acids, medicaments containing such compounds and their use  
The present invention relates to compounds defined by formula (I) wherein the group R is defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are...
8299054 Cyclic 11-beta hydroxysteroid dehydrogenase type 1 inhibitors  
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing...
8299067 5-demethoxyfumagillol and derivatives thereof  
Provided herein are 5-demethoxyfumagillol and its derivatives. Also provided herein are methods of making the 5-demethoxyfumagillol and derivatives. Also provided herein are biological activities...
8293929 Processes and intermediates  
The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for...
8288371 Ortho pyrrolidine, benzyl-substituted heterocycle CCR1 antagonists for autoimmune diseases and inflammation  
Compounds of the formula are disclosed. The compounds are CCR1 antagonists which are useful for the treatment and prevention of inflammatory and autoimmune diseases. Other embodiments are also...
8288370 Substituted azetidine compounds of formula (I) useful in the treatment of functional gastrointestinal disorders, IBS, and functional dyspepsia  
The present invention relates to new substituted azetidine compounds of formula (I): or pharmaceutically acceptable salts thereof, as further described herein, to pharmaceutical compositions...
8278341 Analogs of indole-3-carbinol and their use as agents against infection  
Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane,...
8263583 Hydrochloride salt of 5-[3-(3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenylhexanamide  
This invention relates to the hydrochloride salt of 5-[3-{3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenyl- hexanamide or derived form thereof and its use as a medicament.
8247401 P2X3 receptor antagonists for treatment of pain  
The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or...
8207169 Substituted [1,2,4]triazolo[4′,3′:1,6]pyrido[2,3-b]pyrazines of the formula D  
The compounds of Formula D are of the class of triazolo-pyrido-pyrazines which are inhibitors of AKT useful for the treatment of cancer

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