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7625909 Substituted quinazolinone compounds  
A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to...
7625908 Quinazoline derivatives  
A quinazoline derivative of the Formula (I): wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part...
7618975 4-arylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof  
Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of...
7612094 Tri-substituted heteroaryls and methods of making and using the same  
Compounds of formula (I) possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic...
7608643 Compounds for inhibiting KSP kinesin activity  
The present invention relates to compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: The present invention provides compositions comprising these compounds that are...
7605165 Phenylalanine derivatives  
The present invention relates to the following phenylalanine derivatives or analogues thereof having an antagonistic activity to α4 integrin and therapeutic agents for various diseases concerning...
7598255 Pyrimidine compounds as serotonin receptor modulators  
Certain pyrimidine-containing compounds are serotonin receptor modulators useful in the treatment of serotonin-mediated diseases.
7579465 Antiviral agents  
This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the...
7576074 Receptor-type kinase modulators and methods of use  
The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the...
7572798 Combi-molecules having signal transduction inhibitory properties and DNA damaging properties  
The present invention relates to a series of new chemical agents that demonstrate anti-tumor activity. More particularly, the present invention relates to molecules, referred to as...
7566732 Rhodanine compositions for use as antiviral agents  
This invention describes compounds and pharmaceutical compositions useful as inhibitors of ubiquitination. The compounds and compositions of the invention are useful as inhibitors of the...
7560558 Compound having TGFβ inhibitory activity and medicinal composition containing the same  
The present invention provides compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein X represents CH or N; Z represents —O—, —NH— or...
7560461 Quinazoline derivatives as kinase inhibitors  
The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which...
7528121 Phosphonooxy quinazoline derivatives and their pharmaceutical use  
Quinazoline derivatives of formula (I) wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their...
7514460 Benzazole analogues and uses thereof  
The present invention relates to N 2 -heteroaryl-benzazole-2,(5 or 6)-diamine derivatives and compositions thereof as protein kinase inhibitors for the treatment of e.g. cancer.
7501428 Quinazoline thiazolinones  
Quinazoline thiazolinone derivatives which demonstrate CDK1 antiproliferative activity and are useful as anti-cancer agents.
7491728 Pyrimidinone compounds as calcilytics  
The pyrimidinone compounds are disclosed. Methods of preparing the pyrimidinone compounds are also disclosed.
7488823 Cyanoguanidines and cyanoamidines as ErbB2 and EGFR inhibitors  
Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Methods of treating hyperproliferative diseases...
7482352 Chemical derivatives and their application as antitelomerase agents  
The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which is quite specific. It also relates to novel chemical compounds as well as their...
7465738 Compounds useful as promoters of SMN2  
The present invention relates to compounds useful as promoters of the SMN2 gene. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using...
7462623 Quinazoline derivatives as Src tyrosine kinase inhibitors  
The invention concerns quinazoline derivatives of Formula (I): (A chemical formula should be inserted here—please see paper copy enclosed herewith) wherein Z is an O, S, SO, SO 2 , N(R 2 ) or C(R...
7456188 C-5 substituted quinazolinone derivatives as selective estrogen receptor beta modulators  
The present application describes compounds according to Formula I, wherein Q, R 1 , R 2 and X are described herein, that are useful as Estrogen Receptor Beta (ERβ) modulators. Additionally, the...
7439249 Inhibitors of phosphatases  
The present invention relates to compounds that inhibit phosphatases, compositions thereof, and methods of using those compounds and compositions for treating diseases.
7429597 Substituted nitrogen-containing heterobicycles, the preparation thereof and their use as pharmaceutical compositions  
The present invention relates to new substituted nitrogen-containing heterobicyclic compounds of general formula wherein B, X 1 to X 3 and R 1 to R 5 are defined as in claim 1, the...
7417041 Imidazopyrimidines as transforming growth factor (TGF) inhibitors  
Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described....
7410975 Small molecule toll-like receptor (TLR) antagonists  
The invention provides methods and compositions useful for modulating signaling through Toll-like receptors. The methods involve contacting a TLR-expressing cell with a small molecule having a core...
7407946 Quinazoline compounds  
Quinazoline derivatives of formula (I) wherein A is 5-membered heteroaryl containing a sulphur atom and optionally containing one or more nitrogen atoms; compositions containing them, processes for...
7402585 Substituted quinazoline derivatives as inhibitors of aurora kinases  
The invention provides quinazoline derivatives of formula (I): in the preparation of a medicament for use in the inhibition of Aurora kinase and also novel quinazoline derivatives, processes for...
7381730 3-arylquinazoline derivatives as selective estrogen receptor beta modulators  
Novel quinazoline derivatives possessing activity as estrogen receptor beta (ERβ) modulators are provided which have the general formula I wherein X is O or S; A and B are each...
7378422 Inhibitors of serine proteases, particularly HCV NS3-NS4A protease  
The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life...
7378522 Quinoline, isoquinoline and phthalazine derivatives as antagonists of the gonadotropin-releasing hormone  
The invention relates to new quinoline, isoquinoline and phthalazine derivatives as antagonists of the gonadotropin-releasing hormone.
7368445 Fused pyrazole derivatives as TGF-β signal transduction inhibitors for the treatment of fibrosis and neoplasms  
The disclosed invention is directed to compounds of the formula: Formula (I) and methods of using these compounds.
7368453 Quinazolinone compounds with reduced bioaccumulation  
A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to...
7348332 (3,4-dihydro-quinazolin-2-yl)-indan-1-yl-amines  
The present invention relates to compounds of formula wherein R 1 , R 2 , and n are as defined herein and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula...
7348333 Cycloalkyl derivatives as inhibitors of bone resorption and vitronectin receptor antagonists  
There are described cycloalkyl derivatives of the formula (I) R 1 —Y-A-B-D-E-F-G (I)
7342022 Compounds in the treatment of dementia related diseases, Alzheimer's Disease and conditions associated with glycogen synthase kinase-3  
The present invention relates to new compounds of formula I wherein R 1 , R 2 , R 3 , n, m are defined as in claim 1, a process for their preparation and new intermediates used in the preparation...
7332493 Substituted bicyclic derivatives for the treatment of abnormal cell growth  
The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R 1 , R 3 , R 4 , R 5 , R 11 , m and p are as defined...
7329664 Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues  
Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and...
7329655 Nitrogenous heterocyclic compounds  
The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which...
7329665 Quinazolinone derivative  
An optically active form of the quinazolinone derivatives represented by the general formula (1): [wherein Y represents a phenyl group or C2-C7 alkyl group; E represents —CH═ or nitrogen...
7329749 Piperazinylcarbonylquinolines and -isoquinolines  
Compound of the formula (I) in which R 1 , R 2 and alk are as defined in Claim 1, are potent 5-HT 2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression,...
7326712 Substituted tricyclic compounds as protein kinase inhibitors  
Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following...
7312209 Acridone inhibitors of IMPDH enzyme  
Compounds having the formula (I), wherein R 3 is selected from H, OH and NH 2 ; R 30 is selected from ═O and ═S; W is —C(═O)—, —S(═O)—, or —S(O) 2 —; or W may be —CH 2...
7312214 1, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors  
The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
7304059 Substituted quinazolin-4-ylamine analogues  
Substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the...
7279481 Quinoline and quinazoline derivatives having affinity for 5HT1-type receptors  
Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided: wherein R 1 , m, X, R 2 , n, W, p, Y, Z, R 3 , R 4 , R 5 and q have the meanings as defined in the...
7273936 Oxazole and thiazole compounds as transforming growth factor (TGF) inhibitors  
Novel oxazole and thiazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described....
7271179 Inhibitors of JAK protein kinase  
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of...
7268142 Tetrahydroisoquinolinyl derivatives of quinazoline and isoquinoline  
The invention pertains to substituted quinazoline and isoquinoline compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which...
7268230 Quinazoline compounds  
The invention relates to compounds of the formula (I): wherein ring C is as defined herein, for example indolyl, indazolyl or azaindolyl; Z is —O—, —NH— or —S—; n is 0-5; m is 0-3; R 1 ...