"That the automobile has practically reached the limit of its development is suggested by the fact that during the past year no improvements of a radical nature have been introduced."
Scientific American ; Jan. 2 edition, 1909
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| Number | Title | Issue Date |
| 8076358 | 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE) The present invention is directed to 6-substituted-thio-2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD), mild cognitive impairment, senility and/or dementia. The compounds of the p... | 12/13/2011 |
| 7993638 | Cancer treatment combining lymphodepleting agent with CTLs and cytokines In a cancer treatment combining cell therapy with chemotherapy, autologous CD8+ T cells are obtained from a patient, activated ex vivo by contacting them with xenogenic antigen presenting cells loaded with selected peptide antigen, thereby generating anti... | 08/09/2011 |
| 7968580 | Imidazolidin-2-one derivatives as selective androgen receptor modulators (SARMS) The present invention is directed to novel imidazolidin-2-one derivatives having a structure according to Formula I wherein a, b, R1, R2, R3, and R4 are as defined above, pharmace... | 06/28/2011 |
| 7951829 | Benzimidazole modulators of VR1 The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them. ... | 05/31/2011 |
| 7947694 | Substituted pyrazolo[3,4-D]pyrimidines as cell cycle kinase inhibitors This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X1 and X2 have defined meanings, having cel... | 05/24/2011 |
| 7939052 | Method of measuring the biological activity of an urotensin II receptor Administration of U-II to rats caused an increase in the redness or the skin temperature of the ear of the rats. The increase was inhibited by compounds that decease the biological activity of the U-II/UT receptor. Thus, the present invention provides methods of mea... | 05/10/2011 |
| 7932399 | 2-substituted benzimidazoles as selective androgen receptor modulators (SARMS) The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. ... | 04/26/2011 |
| 7928246 | Dihydroisoindolones as allosteric modulators of glucokinase The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating glucokinase mediated disorders. More particularly, the c... | 04/19/2011 |
| 7928238 | 1,2,3,4-tetrahydro-quinoline derivatives as CETP inhibitors The invention is directed to compounds of Formula (I) described herein useful as CETP inhibitors, compositions containing them, and methods of using them. ... | 04/19/2011 |
| 7897781 | Cold menthol receptor-1 antagonists The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated d... | 03/01/2011 |
| 7897771 | Fused heterocyclic compounds Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases. ... | 03/01/2011 |
| 7897636 | Sulfamide derivative useful for the treatment of epilepsy The present invention is directed to novel sulfamide derivatives, pharmaceutical compositions comprising said compounds and methods for the treatment of epilepsy and related disorders comprising administering to a subject in need thereof, said compounds, either alon... | 03/01/2011 |
| 7893064 | Hydrazone derivatives as kinase inhibitors The present invention is directed to novel bicyclic pyrimidine compounds of Formula (I) or a form or composition thereof as inhibitors of ATP-protein kinase interactions, wherein substituents on each side of the iminomethyl... | 02/22/2011 |
| 7887845 | Antiviral compositions The present invention is concerned with pharmaceutical compositions of antiviral compounds which can be administered to a mammal, in particular a human, suffering from a viral infection. These compositions comprise particles obtainable by melt-extruding a mixture co... | 02/15/2011 |
| 7846930 | Diaryl-substituted tetrahydroisoquinolines as histamine Hreceptor and serotonin transporter modulators Certain diaryl-substituted tetrahydroisoquinoline compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases. ... | 12/07/2010 |
| 7879895 | Benzimidazole derivatives useful as selective androgen receptor modulators (SARMS) The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. ... | 02/01/2011 |
| 7875621 | Substituted 2-alkyl quinazolinone derivatives as PARP inhibitors The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions containing compounds of formula (I) wherein R1, R3, L, X, Y and Z have defin... | 01/25/2011 |
| 7872138 | Process for the preparation of substituted-1,2,3,4-tetrahydroisoquinoline derivatives The present invention is directed to a process for the synthesis of substituted-1,2,3,4-tetrahydroisoquinoline derivatives, useful as intermediates in the synthesis of pharmaceutical agents. ... | 01/18/2011 |
| 7872044 | Inhibitors of chymase The present invention is directed to a compound of Formula (I): or an enantiomer, diastereomer, polymorph or pharmaceutically acceptable salt thereof and methods for preparing said compounds and compositions, intermediates ... | 01/18/2011 |
| 7868023 | Thiophene sulfoximines, compositions thereof, and methods of treating complement-mediated diseases and conditions Disclosed are compounds for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade. The compounds are of Formula I or a solvate, hydrate, pharmaceutically acceptabl... | 01/11/2011 |
| 7851498 | Hexahydro-cyclooctyl pyrazole cannabinoid modulators This invention is directed to a hexahydro-cyclooctyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or... | 12/14/2010 |
| 7838553 | Benzopyran derivatives as potassium channel openers The present invention is directed to novel benzopyran derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to potassium channel. ... | 11/23/2010 |
| 7825244 | Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: wherein R1, R2, R99, and X are as defined herein, the use of such compounds in the synthesis of prote... | 11/02/2010 |
| 7825151 | Hexahydro-cyclooctyl pyrazole cannabinoid modulators This invention is directed to a hexahydro-cyclooctyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or... | 11/02/2010 |
| 7825110 | Substituted spiroheterocycles The invention is directed to nonpeptide substituted spiroheterobenzazepine of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as tho... | 11/02/2010 |
| 7820650 | Antifungal 4-substituted 5,6-dihydro-4H-pyrrolo [1,2-a][1,4]benzodiazepines The present invention concerns compounds for use as a medicine having the formula the N-oxide forms, the salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 represent... | 10/26/2010 |
| 7820630 | Substituted indole-O-glucosides Substituted indole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed. ... | 10/26/2010 |
| 7816390 | N-substituted tricyclic 3-aminopyrazoles as anti-mitotic tubulin polymerization inhibitors The invention is directed to compounds having the following structures: N-(3-ethoxyphenyl)-1,4-dihydro-6-ethoxy-7-(3-hydroxypropoxy)-1-methylindeno[1,2-c]pyrazole-3-amine; 3-[3-(3... | 10/19/2010 |
| 7816331 | Substituted indazole-O-glucosides Substituted indazole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed. ... | 10/19/2010 |
| 7816330 | Substituted benzimidazole-, benztriazole-, and benzimidazolone-O-glucosides This invention relates to substituted benzimidazole-O-glucosides, benztriazole-O-glucosides, and benzimidazolone-O-glucosides, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of diabetes and Syndrome X. ... | 10/19/2010 |
| 7816328 | Substituted fused heterocyclic C-glycosides This invention relates to substituted fused heterocyclic C-glycosides, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of diabetes and Syndrome X. ... | 10/19/2010 |
| 7812183 | Benzopyran derivatives as potassium channel openers The present invention is directed to novel benzopyran derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to potassium channel. ... | 10/12/2010 |
| 7803823 | 2-amino-4,5-trisubstituted thiazolyl derivatives This invention concerns the use of a compound of formula (I′) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alky... | 09/28/2010 |
| 7803793 | Heterocyclic derived metalloprotease inhibitors This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metallop... | 09/28/2010 |
| 7799785 | Substituted tetracyclic tetahydrofuran, pyrrolidine and tetrahydrothiophene derivatives This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptor... | 09/21/2010 |
| 7795440 | N-substituted tricyclic 1-aminopyrazoles as inhibitors for the treatment of cell proliferative disorders The invention is directed to N-substituted tricyclic 3-AMINOPYRAZOLE derivatives, which are useful as inhibitors of platelet-derived growth factor receptor (PDGF-R) kinase, and methods for the preparation of said derivatives. The present invention is further directe... | 09/14/2010 |
| 7795261 | Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined N... | 09/14/2010 |
| 7790895 | Quinoline derivatives as potassium ion channel openers The present invention is directed to novel quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to ion channels such as potassium channels. ... | 09/07/2010 |
| 7790894 | Mycobacterial inhibitors The present invention relates to novel substituted quinoline derivatives according to the general Formula (I) and pharmaceutically acceptable addition salts thereof, wherein the variable moieties are as defined in the speci... | 09/07/2010 |
| 7759331 | Pyridine-containing macroheterococylic compounds as kinase inhibitors This invention is directed to pyridine-containing macroheterocyclic compounds useful as kinase inhibitors, methods for producing such compounds and methods for treating or preventing a kinase mediated disorder. ... | 07/20/2010 |