"What, sir, would you make a ship sail against the wind and currents by lighting a bonfire under her deck? I pray you, excuse me, I have not the time to listen to such nonsense."
Napoleon Bonaparte ; When told of the Robert Fulton steamboat
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| Number | Title | Issue Date |
| 7928230 | Method for modulating GPR119 G protein-coupled receptor and selected compounds A method of modulating the activity of the GPR119 G protein-coupled receptor comprising administering to a mammalian patient in need thereof a therapeutically effective amount of at least one compound of Formula I or Formula IA and, optionally, an additional therape... | 04/19/2011 |
| 7442705 | HIV replication inhibiting pyrimidines and triazines This invention concerns HIV replication inhibitors of formula (I), The N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, their use as a medicine, their processes for preparation and pharm... | 10/28/2008 |
| 7435814 | 2,4-Pyrimidinediamine compounds and their uses The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a... | 10/14/2008 |
| 7427681 | Pyrazole compounds useful as protein kinase inhibitors This invention describes novel pyrazole compounds of formula II: wherein Z1 is nitrogen or CR8; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, whe... | 09/23/2008 |
| 7419984 | Pyrimidines and uses thereof The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase β (LPAAT-β) activity and/or proliferation of cells such as tumor-cells. ... | 09/02/2008 |
| 7414046 | Gyrase inhibitors and uses thereof The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also re... | 08/19/2008 |
| 7405221 | Substituted pyrimidines Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are... | 07/29/2008 |
| RE40245 | Gyrase inhibitors and uses thereof The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates ... | 04/15/2008 |
| 7351712 | Pyrimidine derivatives for the treatment of abnormal cell growth The present invention relates to a compound of the formula 1 wherein R1-R4 are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell... | 04/01/2008 |
| 7345048 | Heterocyclic compounds and uses thereof as D-alanyl-D-alanine ligase inhibitors The invention relates to D-Ala-D-Ala ligase inhibitors having the formula: wherein R1 is NH2; R2 is NH2; R3 is selected from hydrogen, alkyl, amino, hydroxy, alkoxy, an... | 03/18/2008 |
| 7338959 | Diamino-pyrimidines and their use as angiogenesis inhibitors Benzimidazole derivatives, which are useful as TIE-2 and/or VEGFR-2 inhibitors are described herein. The described invention also includes methods of making such benzimidazole derivatives as well as methods of using the same in the treatment of hyperproliferative di... | 03/04/2008 |
| 7335672 | Vanilloid receptor ligands and their use in treatments Substituted pyridines and pyrimidines and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inf... | 02/26/2008 |
| 7332484 | 2,4-pyrimidinediamine compounds and their uses The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a... | 02/19/2008 |
| 7288547 | CDK-inhibitory 2-heteroaryl-pyrimidines, their production and use as pharmaceutical agents This invention relates to 2-heteroaryl-pyrimidine derivatives of general formula I or If as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases. ... | 10/30/2007 |
| 7282504 | Kinase inhibitors The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention... | 10/16/2007 |
| 7262200 | Indazolinone compositions useful as kinase inhibitors The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK... | 08/28/2007 |
| 7262203 | Pyrimidineamines as angiogenesis modulators Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases. ... | 08/28/2007 |
| 7253174 | N-heterocyclic inhibitors of TNF-α expression N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharm... | 08/07/2007 |
| 7241769 | Pyrimidines as PLK inhibitors The present invention comprises compounds of general formula (1) wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2 and R3 are defined as in clai... | 07/10/2007 |
| 7235562 | Pyrimidine derivatives for the treatment of abnormal cell growth The present invention relates to a compound of the formula 1 wherein R1-R4 and Ar are as defined herein. Such novel pyrimidine derivatives are useful in the treatmen... | 06/26/2007 |
| 7230104 | Fungicidal 5-phenyl substituted 2-(cyanoamino) pyrimidines Pyrimidines of formula I in which R1 represents hydrogen or alkyl, haloalkyl, alkenyl, alkynyl, alkadienyl, alkoxy, cycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered h... | 06/12/2007 |
| 7220736 | Pyrimidine compounds A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ═CH— or ═N—, Y is —NH—, —NR4—, —S—, —O—, —CH═N—,... | 05/22/2007 |
| 7208499 | Pyrimidine derivatives for the treatment of abnormal cell growth The present invention relates to a compound of the formula 1 wherein A and Ar are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals... | 04/24/2007 |
| 7205310 | Pyrimidine hydantoin analogues which inhibit leukocyte adhesion mediated by VLA-4 Disclosed are compounds which bind VLA-4 and/or LPAM-1. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4 and/or LPAM-1. Such compounds are useful in the treatment of inflammatory diseases in a mammal... | 04/17/2007 |
| 7205307 | Pyrimidines as novel openers of potassium ion channels The present invention provides a genus of pyrimidine amides that are useful as openers of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods. ... | 04/17/2007 |
| 7179604 | Methods of use of DNA encoding a human histamine receptor of the H3 subtype DNAs encoding the human histamine H3 receptor have been cloned and characterized. The recombinant protein is capable of forming biologically active histamine H3 receptor protein. The cDNA's have been expressed in recombinant host cells which produce active recombina... | 02/20/2007 |
| 7179816 | 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 inhibits telomerase. It also relates to novel chemical compounds as well as their therapeutic application in humans. ... | 02/20/2007 |
| 7173028 | Pyrimidine derivatives The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characteri... | 02/06/2007 |
| 7166599 | Trisubstituted pyrimidines The present invention relates to trisubstituted pyrimidines of formula wherein Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses in which β-amy... | 01/23/2007 |
| 7157455 | 4-Aminopyrimidine-5-one derivatives Novel 4-aminopyrimidine-5-one derivatives are disclosed. These compounds inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are ... | 01/02/2007 |
| 7153964 | Pyrimidine compounds Pyrimidine derivatives of formula (I) wherein: Qh1 and Q2 are independently selected from aryl or carbon linked heteroaryl optionally substituted as defined within; and one of Q1 and Q2 or both Q1 and Q2 | 12/26/2006 |
| 7153860 | 5-Phenylpyrimidines, methods and intermediate products for the production thereof and use of the same for controlling pathogenic fungi The invention relates to 5-phenylpyrimidine of formula (I) wherein the substituents have the following designations: R1 represents a five to ten-membered saturated, partially unsaturated or aromatic monocyclic or bicyclic heterocycle which contains betwee... | 12/26/2006 |
| 7151106 | Crystal modification of a N-phenyl-2-pyrimidineamine derivative, processes for its manufacture and its use The invention relates to a new crystalline form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of formula 1, which may be used for example for tumor therapy. | 12/19/2006 |
| 7148219 | Biaryl heterocyclic compounds and methods of making and using the same The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety th... | 12/12/2006 |
| 7145008 | Pyrimidine derivatives for the treatment of abnormal cell growth The present invention relates to a compound of the formula 1 or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof, wherein R1–R4 and Ar are ... | 12/05/2006 |
| 7135477 | Heterocyclic compounds which inhibit leukocyte adhesion mediated by αintegrins Disclosed are compounds which bind α4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, preferably VLA-4. Such compounds are useful in the ... | 11/14/2006 |
| 7122552 | Inhibitors of JAK and CDK2 protein kinases The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of JAK and CDK2 mammalian protein ... | 10/17/2006 |
| 7122670 | Selective synthesis of CF3-substituted pyrimidines The present invention relates to a method of making a compound of the formula wherein X1, X2 and R3—R4 are as defined herein. The method includes reacting a compound ... | 10/17/2006 |
| 7115617 | Amino-substituted pyrimidinyl derivatives and methods of use The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer. ... | 10/03/2006 |
| 7109204 | Tyrosine kinase inhibitors The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen... | 09/19/2006 |