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| Number | Title | Issue Date |
| 8188102 | Amide derivative for inhibiting the growth of cancer cells The present invention provides a novel amide derivative of formula (I) and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising same as an active ingredient. ... | 05/29/2012 |
| 8183249 | Inhibitors of AKT/PKB with anti-tumor activity The subject invention concerns materials and methods for inhibiting the Akt/PKB pathway. In one embodiment, a compound of the invention inhibits kinase activity and/or phosphorylation levels of Akt proteins. The subject invention also concerns methods for inhibiting... | 05/22/2012 |
| 8168645 | Arylsulfonamide compounds The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biol... | 05/01/2012 |
| 8153642 | Quinazolines useful as modulators of ion channels The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the composition... | 04/10/2012 |
| 8008311 | Methods and compostions utilizing quinazolinones Quinazolinones of formulae (a, b, c and d) are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity. ... | 08/30/2011 |
| 8003659 | Macrocyclic serine protease inhibitors Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection i... | 08/23/2011 |
| 7994181 | 6-1H-imidazo-quinazoline and quinolines derivatives, new potent analgesics and anti-inflammatory agents The present invention is directed to novel 6-1H-imidazo-2-aryl and 2-heteroaryl quinazoline and quinoline of formula I, corresponding salts and solvates thereof, to a process for their preparation and to the use of this compounds and corresponding pharmaceutical com... | 08/09/2011 |
| 7989461 | Substituted quinazolinamine compounds for the treatment of cancer The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I | 08/02/2011 |
| 7939539 | Quinazolinone compounds as anticancer agents Quinazolinone compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the quinazolinone compounds, either alone or in combination with at least one additional therapeutic ... | 05/10/2011 |
| 7893071 | Synthesis and evaluation of novel phthalimide mimics as anti-angiogenic The present invention is directed to novel thalidomide derivative compounds that have activity as anti-angiogenic compounds. More particularly the compounds have the general structure: where R1 is selected from the group consisting of H, halo, alkyl, halo... | 02/22/2011 |
| 7829573 | Therapeutic combinations of antihypertensive and antiangiogenics agents The invention concerns the use of a combination of an anti-angiogenic agent and an anti-hypertensive agent for use in the manufacture of a medicament for the treatment of a disease state associated with angiogenesis in a warm-blooded mammal, such as a human being. T... | 11/09/2010 |
| 7790731 | Crystal form of 2-methyl-3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone The present invention is directed to a form I crystal of 2-methyl 3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone that is useful for example in the treatment of sleep disorders or various sleep disorder-associated diseases. ... | 09/07/2010 |
| 7763627 | Tie-2 modulators and methods of use A compound according to Formula IV: or a pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof, wherein R1, R2, R3, R4, R... | 07/27/2010 |
| 7687508 | Cyclic derivatives as modulators of chemokine receptor activity This invention relates generally to modulators of chemokine receptor activity having unexpected combination of desirable pharmacological properties. Pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and prevention... | 03/30/2010 |
| 7678803 | Quinazoline derivatives for the treatment of cancer The current invention is directed toward compounds and pharmaceutically acceptable salts of Formula I wherein Q1 is CR1, Q2 is N, Q4 and Q5 are each CR1, Q | 03/16/2010 |
| 7678802 | Quinazolines useful as modulators of ion channels The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the composition... | 03/16/2010 |
| 7671062 | Modulators of chemokine receptor activity, crystalline forms and process The present invention provides a novel antagonist or partial agonists/antagonists of MCP-1 receptor activity: N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, | 03/02/2010 |
| 7659279 | Quinazoline derivatives and their use in the treatment of cancer The invention concerns quinazoline derivatives of the formula: (I); wherein X1, Q1, Z, R1, R2, Y, a and m are as defined in the description, which are erbB tyrosine kinase inhibitors, particularly EGFR tyrosine kinase inhi... | 02/09/2010 |
| 7655666 | Substituted 1H-quinazoline-2,4-diones useful as AMPA receptor ligands The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical comp... | 02/02/2010 |
| 7629351 | N-((1R,2S,5R)-5-(-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino) pyrrolidin-1-yl)cyclohexyl)acetamide and other modulators of chemokine receptor activity, crystalline forms and process The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, | 12/08/2009 |
| 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 by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal... | 12/01/2009 |
| 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 subjects. The compounds have the structure IA, IB, and IC where the values... | 12/01/2009 |
| 7589098 | Methods and compositions utilizing quinazolinones Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity. ... | 09/15/2009 |
| 7501428 | Quinazoline thiazolinones Quinazoline thiazolinone derivatives which demonstrate CDK1 antiproliferative activity and are useful as anti-cancer agents. ... | 03/10/2009 |
| 7498335 | Method of producing an antiangiogenic or vascular permeability reducing effect The invention concerns the use of a quinazoline derivative of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— w... | 03/03/2009 |
| 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 the compositions in the treatment of Spinal Muscular Atrophy. ... | 12/16/2008 |
| 7452895 | Quinazoline analogs as receptor tyrosine kinase inhibitors This invention provides quinazoline analogs of Formula I: where A is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to two independent R3 | 11/18/2008 |
| 7442699 | Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6 are... | 10/28/2008 |
| 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. ... | 10/21/2008 |
| 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, X1 to X3 and R1 to R5 are defined as in claim 1,... | 09/30/2008 |
| 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. The compounds of the present invention are potent inhibitors of tran... | 08/26/2008 |
| 7410974 | Halogenated Quinazolinyl nitrofurans as antibacterial agents The present invention includes novel compounds of the formula (I) wherein X is absent or trans or cis CHCH, R1 is (C1-C10) alkyl unsubstituted or substituted by one to three hydroxy, (C1-C10) alkenyl unsubstitut... | 08/12/2008 |
| 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 structure including at least two rings. Certain of the compounds are... | 08/12/2008 |
| 7388014 | Quinazoline derivatives and therapeutic use thereof Quinazoline derivatives represented by the general formula pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for using the compounds for treatment of hyperprolifer... | 06/17/2008 |
| 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 cycle of the hepatitis C virus and are also useful as antiviral agents.... | 05/27/2008 |
| 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 subjects. The compounds have the formula IA and IB. IA and IB have the fol... | 05/06/2008 |
| 7361663 | N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions cont... | 04/22/2008 |
| 7361662 | Pyridopyrimidinone compounds, method for production thereof and medicaments comprising the same A compound of formula (I): wherein: R1, R2, R3, R4 are defined in the description, its enantiomers, diastereoisomers, tautomers and also addition salts thereof with a phar... | 04/22/2008 |
| 7358253 | Indolylmaleimide derivatives Provided are compounds of formula (I) which are useful in the treatment and/or prevention of diseases or disorders mediated by T lymphocytes and/or PKC, e.g. acute or chronic rejection of organ or tissue allo- or xenografts... | 04/15/2008 |
| 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 -Z1-Z2- is... | 04/15/2008 |
