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| Number | Title | Issue Date |
| 8173814 | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical ... | 05/08/2012 |
| 8153802 | Dyes linked to target molecules, oligonucleotides or polynucleotides comprising dye molecules, composite dyes and other compositions useful for detecting or quantifying desirable target molecules The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins and nucleic acids. Dyes are provided that may be used free in solution where the binding of th... | 04/10/2012 |
| 8022216 | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical ... | 09/20/2011 |
| 7982043 | Protein tyrosine kinase enzyme inhibitors This invention provides compounds of formula 1, having the structure wherein R1, R2, R3, R4, and R5 are described within the specification. ... | 07/19/2011 |
| 7973164 | Quinoline derivatives The invention concerns quinoline derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A... | 07/05/2011 |
| 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 —C(═O)—; R and R′ repre... | 07/14/2009 |
| 7538221 | Polymorphs of racemic, dextrorotatory, and levorotatory enantioners of 1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid hydrochloride and mesylate salts A polymorphic forms of the hydrochloride salt and mesylate salt of racemic (±)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid, dextrorotatory R-(+)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,... | 05/26/2009 |
| 7432377 | Quinoline intermediates of receptor tyrosine kinase inhibitors and the synthesis thereof This invention is directed to methods of preparing 4-substituted quinoline compounds as intermediates in the manufacture of receptor tyrosine kinase inhibitors and intermediate compounds used in the methods thereof, wherein the 4-substituted quinoline compound has t... | 10/07/2008 |
| 7399865 | Protein tyrosine kinase enzyme inhibitors This invention provides compounds of formula 1, having the structure wherein R1, R2, R3, R4, and R5 are described within the specification. ... | 07/15/2008 |
| 7381824 | Quinoline derivatives The invention relates to compounds represented by Formula (I): and to pharmaceutically acceptable salts or solvates of said compounds, wherein each of A, R3-8, X3, X5, m, and n are defined h... | 06/03/2008 |
| 7365203 | Process for the synthesis of 6-amino-4-(3-chloro-4-fluoro-phenylamino)-7-ethoxy-quinoline-3-carbonitrile The present invention provides a process for the preparation of 6-amino-4-(3-chloro-4-fluoro-phenylamino)-7-ethoxy-quinoline-3-carbonitrile comprising the steps and products disclosed within this application. ... | 04/29/2008 |
| 7297795 | Process for preparation of 4-amino-3-quinolinecarbonitriles This invention discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-su... | 11/20/2007 |
| 7223761 | Salts and polymorphs of a potent antidiabetic compound Salts and polymorphs of a compound useful in the treatment of inflammatory and metabolic conditions and diseases are provided herein. In particular, the invention provides salts and polymorphs of a compound which modulates the expression and/or function of a peroxis... | 05/29/2007 |
| 7176312 | Kinase inhibitor scaffolds and methods for their preparation General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, bor... | 02/13/2007 |
| 7173136 | 3-Cyano-quinoline derivatives The invention concerns quinoline derivatives of Formula (I) wherein each of Z1, m, R1, n, R3, Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmac... | 02/06/2007 |
| 7173135 | Substituted 3-cyanoquinolines as MEK inhibitors The invention concerns quinoline derivatives of Formula (I) wherein each of Z1, m, R1, n, R3, Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmac... | 02/06/2007 |
| 7173038 | Quinazoline derivatives as VEGF inhibitors The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C | 02/06/2007 |
| 7166612 | Methods for reducing platelet activation platelet aggregaton or thrombosis The invention provides methods and compositions for reducing platelet activation, platelet aggregation and thrombosis. The invention further provides compositions and methods for treating or preventing diseases or disorders in which the pathology of the disease or d... | 01/23/2007 |
| 7125893 | 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula I in which R1a, R1b, R2a, R3a, R3b, R4, R... | 10/24/2006 |
| 7087603 | Pyrazole compounds useful as protein kinase inhibitors This invention describes novel pyrazole compounds of formula IV: wherein Z1 or Z2 is nitrogen, Q is —S—, —O—, —N(R4)—, —C(R6′)2—, 1,2-cyclo... | 08/08/2006 |
| 7067532 | Substituted quinolines as antitumor agents The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt pro-drug or solvate thereof. The invention also provides a process for the preparation of a compound of Formula (Ia), pharmaceutical compositions of a compound of Formula (Ia) a... | 06/27/2006 |
| 7009053 | Quinoline derivatives as caspase-3 inhibitor, preparation for producing the same and pharmaceutical composition comprising the same The present invention relates to new quinoline derivatives of formula (1) or their pharmaceutically acceptable salts with caspase-3 inhibitory activity and their preparation methods, wherein R2 is H; halogen; C1-6alkyl; C1-6 alkoxy; ... | 03/07/2006 |
| 7009054 | Quinolines and uses thereof This invention relates to compounds of the general formula: in which RA, RB, RC and RD are as defined herein, and to their preparation and use. ... | 03/07/2006 |
| 6995174 | Hepatitis C virus inhibitors Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R′, B, Y and X are described in the description. Composit... | 02/07/2006 |
| 6987187 | Process for preparation of amidine derivatives A process for producing amidine derivatives represented by the following reaction scheme, characterized in that the reactions of steps 1 and 3 are conducted in acetonitrile and the reaction of step 2 is conducted in acetone. ... | 01/17/2006 |
| 6972288 | 4-amino-quinazoline and quinoline derivatives having an inhibitory effect on signal transduction mediated by tyrosine kinases The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rd, A to G and X are defined as in claim 1, the tautomers, the steroisome... | 12/06/2005 |
| 6969723 | Aminoquinoline and aminopyridine derivatives and their use as adenosine a3 ligands Compounds of general formula (I), wherein R4 and R5 stand for hydrogen atom or form together an 1,3-butadienyl group, optionally substituted by a methylenedioxy group or one or more straight or branched C1-4 alkyl group, straight or ... | 11/29/2005 |
| 6964973 | Bicyclic androgen and progesterone receptor modulator compounds and methods The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agon... | 11/15/2005 |
| 6946474 | Nitrogen-containing compounds and their use as glycine transport inhibitors The present invention provides trichloroethyl-sulfonylurea-containing compounds that inhibit glycing transporters, pharmaceutical compositions comprising such compounds, methods for using such compounds for inhibiting glycine transporters and methods for using such ... | 09/20/2005 |
| 6933388 | Process for the synthesis of 3-cyano-6-alkoxy-7-nitro-4-quinolones There is provided a process for the preparation of 3-cyano-6-alkoxy-7-nitro-4-quinolone intermediates useful for the preparation of protein tyrosine kinase (PTK) inhibitors which are useful in the treatment of cancer of the formula: | 08/23/2005 |
| 6864265 | Chemokine receptor binding heterocyclic compounds Compounds that bind to chemokine receptors such as CXCR4 and CCR5 demonstrate protective effects against infection of cells by human immunodeficiency virus are disclosed. These compounds contain a tertiary amine[[s]] linked to a core nitrogen via an ar... | 03/08/2005 |
| 6858611 | Potassium channel inhibitors Compounds which are useful as potassium channel inhibitors and which because of their slow off-rates are especially useful for the treatment of cardiac arrhythmias are described. ... | 02/22/2005 |
| 6855512 | Methods for identifying inhibitors of cytochrome P450RAI A method of identifying a compound which is an inhibitor of the enzyme cytochrome P450RAI is performed by selecting a compound that has retinoid activity in an art recognized assay and includes a benzoic acid, benzoic acid ester, naphthoic acid ester or heteroaryl c... | 02/15/2005 |
| 6841680 | N-type calcium channel antagonists for the treatment of pain Compounds having selective action at neuronal N-type calcium channels useful for the treatment of pain in accord with the following structural diagram, wherein R1, R2 and R3 are a varie... | 01/11/2005 |
| 6821988 | 3-cyanoquinolines as inhibitors of EGF-R and HER2 kinases This invention provides compounds of Formula (I), represented by the structure wherein G1, G2, G3, G4, Z, X and n are defined herein, or a pharmaceutically acceptable salt th... | 11/23/2004 |
| 6818772 | Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in repro... | 11/16/2004 |
| 6809097 | Quinoline derivatives inhibiting the effect of growth factors such as VEGF Compounds of the formula (I): wherein: R2 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; n is an integer from 0... | 10/26/2004 |
| 6800644 | Nitrogen-containing heterocyclic compounds and medicaments containing the compounds The present invention provides a novel nitrogen-containing heterocyclic compound useful as a phosphodiesterase-4 inhibitor, and a medicament comprising the same. Further, the present invention provides a nitrogen-containing heterocyclic compound represented by the f... | 10/05/2004 |
| 6780996 | Process for the preparation of 7-substituted-3 quinolinecarbonitriles There is provided a process for the preparation of 7-substituted-3-quinolinecarbonitriles and intermediates useful in a process to prepare 7-substituted-3-quinolinecarbonitriles and pharmaceutically acceptable salts is described. Where 7-fluoro-4-oxo-1,4-dihydro-3-q... | 08/24/2004 |
| 6770648 | Compounds for the modulation of PPARγ activity 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. ... | 08/03/2004 |
