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| Number | Title | Issue Date |
| 8163933 | Clean, high-yield preparation of S,S and R,S amino acid isosteres The present invention provides compounds and methods that can be used to convert the intermediate halomethyl ketones (HMKs), e.g., chloromethyl ketones, to the corresponding S,S- and R,S-diastereomers. More particularly, the present invention provides: (1) reduction... | 04/24/2012 |
| 8030496 | Intermediate compound for synthesis of viridiofungin a derivative A method whereby a compound having HCV replication inhibitory activity and desired optical activity can be synthesized selectively and at high yield in a small number of steps by using a compound having a specific chiral auxiliary as a starting compound is provided.... | 10/04/2011 |
| 7700783 | Synthesis of discodermolide and variants thereof Processes for synthesizing a compound of Formula (I) are provided by reacting a compound of Formula (i) with a compound of Formula (xx). ... | 04/20/2010 |
| 7612210 | Process for selective synthesis of enantiomers of substituted 1-(2-amino-1-phenyl-ethyl)-cyclohexanols A process for the enantioselective synthesis of an (S)- or (R)-1-[2-dimethylamino)-1-(methoxyphenyl)ethyl]cyclohexanol and analogues or salt thereof are described. The method involves the steps of (a) reacting an (S) or (R) 4-benzyloxazolidinone with a mixed anhydri... | 11/03/2009 |
| 7482467 | N-thiolated 2-oxazolidinone-derived antibiotics This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit po... | 01/27/2009 |
| 7348322 | Glucocorticoid receptor modulators as antiinflammatory agents The present invention relates to compounds of formula I: wherein A, X, R1, R2 and R3 are as defined herein and pharmaceutically acceptable salts thereof. The invention also relates to method... | 03/25/2008 |
| 7342037 | Anti-inflammatory medicaments Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel com... | 03/11/2008 |
| 7332611 | N-thiolated 2 oxazolidone antibiotics This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit po... | 02/19/2008 |
| 7235675 | Conjugates of mycophenolic acid The present invention provides a method for the measurement of an analyte in biological samples whereby an uncompetitive inhibitor is coupled to a ligand and utilized in a homogeneous assay. The analyte can be a drug or drug derivative, hormone, polypeptide, or olig... | 06/26/2007 |
| 7223870 | Methods for preparing N-arylated oxazolidinones via a copper catalyzed cross coupling reaction Methods for the preparation of N-arylated oxazolidinone compounds via a copper catalyzed cross coupling reaction are disclosed. ... | 05/29/2007 |
| 7205289 | Combinations of active ingredients with insecticidal and acaricidal properties The invention relates to novel active compound combinations of certain cyclic ketoenols and certain insecticidally active compounds that together have very good insecticidal and acaricidal properties. ... | 04/17/2007 |
| 7144911 | Anti-inflammatory medicaments Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel com... | 12/05/2006 |
| 7126028 | Process for preparing chiral compounds Process for the preparation of chiral compounds of formula (I) comprising contacting a compound of formula (II) with a source of hydrogen or halide; wherein A is a chiral center; X is selected from oxygen, sulphur and nitrogen; n is selected from 0 and 1 and is equa... | 10/24/2006 |
| 6875874 | Processes for the preparation of oxo-oxazoline or alloamino acid derivatives A method for producing a compound represented by the general formula (I-A) or the general formula (I-B), comprising the following step: wherein R1 is an optionally substituted lower alkyl, and the like; R | 04/05/2005 |
| 6765100 | Method for producing epoxide crystal The invention relates to a method for industrially producing highly pure (2R, 3S)- or (2S, 3R)-N-carbamate-protected β-aminoepoxide (crystal) or (2R, 3S)- or (2S, 3R)-N-carbamate-protected β-aminoalcohol. The method for producing N-carbamate-protected β-aminoepox... | 07/20/2004 |
| 6746989 | Substituted benzoylpyrazoles as herbicides The invention relates to novel substituted benzoylpyrazoles of the general formula (I), in which n represents the numbers 0, 1, 2 or 3, A represents a single bond or represents alkanediyl(alkylene), ... | 06/08/2004 |
| 6747157 | Processes for the preparation of oxo-oxazoline or alloamino acid derivatives A method for producing a compound represented by the general formula (I-A) or the general formula (I-B), comprising the following step: wherein R1 is an optionally substituted lower alkyl, and the like; R... | 06/08/2004 |
| 6743814 | Nematicidal trifluorobutenes The present invention relates to novel trifluorobutenes of the formula (I) wherein R1 represents hydrogen; halogen; alkyl that is unsubstituted or substituted with halogen, hydroxy, alkoxy, alkylthio, a... | 06/01/2004 |
| 6660879 | 3-aryl-2-hydroxypropionic acid derivative I A novel 3-aryl-2-hydroxypropionic acid derivative, a process and intermediate for its manufacture, pharmaceutical preparations containing it and the use of the compound in clinical conditions associated with insulin resistance.... | 12/09/2003 |
| 6630602 | Propylisopropyl acetic acid and propylisopropyl acetamide stereoisomers, a method for their synthesis and pharmaceutical compositions containing them The present invention relates to racemic propylisopropyl acetic acid and propylisopropyl acetamide and their isomers in their racemic and stereospecific forms, for use in treatment of neurological and psychotic disorders, and affective disorders and to tr... | 10/07/2003 |
| 6545160 | 댚minocetic acid derivatives- 댔댧 receptor antagonists Disclosed are compounds which bind 댔ଲ.sub.7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by 댔ଲ.sub.7 integrin. Such compounds are usefu... | 04/08/2003 |
| 6541641 | Processes for the preparation of oxo-oxazoline or alloamino acid derivatives A method for producing a compound represented by the general formula (I-A) or the general formula (I-B), comprising the following step: ##STR1## wherein R1 is an optionally substituted lower alkyl, and the like; R2 is a lower alkyl o... | 04/01/2003 |
| 6455529 | Adhesion receptor antagonists Compounds of the formula I ##STR1## in which R1, R2 and R3 have the stated meanings, and their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be used for the treat... | 09/24/2002 |
| 6444826 | Processes and intermediates for preparing substituted chromanol derivatives The invention relates to processes for preparing a compound of the formula ##STR1## and the enantiomer of said compound, wherein the benzoic acid moiety is attached at position 6 or 7 of the chroman ring, and R1, R2, and R3 | 09/03/2002 |
| 6444825 | Process for the preparation of an oxazolidinecarboxylic acid which is useful for preparing therapeutically active taxoids A method for preparing an oxazolidinecarboxylic acid of general formula (I), which is useful for preparing therapeutically active taxoids of general formula (III), from an oxazolidinecarboxylic acid of general formula (II). In formulae (I), (II) and (III)... | 09/03/2002 |
| 6403612 | Thrombin receptor antagonists A thrombin receptor antagonist having the formula ##STR1## or a pharmaceutically acceptable salt thereof, useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises ad... | 06/11/2002 |
| 6399783 | Methods for the esterification of alcohols and compounds useful therefor as potential anticancer agents The invention relates to a method for preparing an ester, by admixing a compound having the structure I or IV: ##STR1## with a base and an alcohol to produce an ester, wherein the alcohol is a precursor to Taxol and its analogs. The present invention also... | 06/04/2002 |
| 6395282 | Immunogenic conjugates of Gram-negative bacterial autoinducer molecules The present invention relates to an immunogenic conjugate comprising a carrier molecule coupled to an autoinducer of a Gram negative bacteria. The immunogenic conjugate, when combined with a pharmaceutically acceptable carrier, forms a suitable vaccine fo... | 05/28/2002 |
| 6362166 | Antipicornaviral compounds and methods for their use and preparation Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating p... | 03/26/2002 |
| 6358983 | Heterocyclically substituted -hydroxycarboxylic acid derivatives, method for producing the same and their use as endothelin receptor antagonists The present invention relates to carboxylic acid derivatives of the formula I ##STR1## the substituents having the meanings explained in the description, preparation and use as endothelin receptor antagonists.... | 03/19/2002 |
| 6340751 | Process for the preparation of 4-substituted azetidinone derivatives Disclosed is a process for the preparation of a 4-substituted azetidinone derivative, which comprises reacting an azetidinone derivative and an amide compound in the presence of a magnesium compound such as those represented by the following formulas (II)... | 01/22/2002 |
| 6329418 | Substituted pyrrolidine hydroxamate metalloprotease inhibitors The invention provides compounds which are potent inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to compounds having a structure... | 12/11/2001 |
| 6316633 | Process for manufacture of chiral succinic acid derivatives The present invention is concerned with a process for the manufacture of chiral succinic acid derivatives of formula (I) ##STR1## wherein R1 is (C1 -C6) alkyl or benzyl, and the novel intermediates used therein.... | 11/13/2001 |
| 6306892 | Metalloproteinase inhibitors, pharmaceutical compositions containing them, and their use The present invention is directed to compound of the formula I: ##STR1## wherein R1, R2, R3, R4, R 5, X, Y, and ##STR2## are as defined herein. These compounds are useful for inhibiting the activity of a ... | 10/23/2001 |
| 6265614 | Optically active intermediates for the preparation of optically active substituted oximes, hydrazones and olefins useful as neurokinin antagonists Intermediates having the formula ##STR1## wherein BI is --CH2 OH or --CH2 ORP, and RP is an alcohol protecting group; a is 1, 2, or 3; ##STR2## TI is --OH or QI is phenyl, naphth... | 07/24/2001 |
| 6265587 | Intermediary compounds for the hemisynthesis of taxanes and preparation processes therefor The present invention relates to new intermediates for the semisynthesis of taxanes and their preparation processes. It relates to derivatives of oxazolidines or oxazolidinones, as well as to new derivatives of baccatine III. The general process for the s... | 07/24/2001 |
| 6214799 | Antipicornaviral compounds and methods for their use and preparation Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating p... | 04/10/2001 |
| 6207822 | Process for the synthesis of azetidinones This invention provides a process for preparing the hypocholesterolemic compound ##STR1## comprising: (a) reacting p-fluorobenzoylbutyric acid with pivaloyl chloride and acylating the product with a chiral auxiliary to obtain a ketone of formula IV: ... | 03/27/2001 |
| 6201124 | Process for production of piperidine derivatives The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: ##STR1## and where m is an integer from 1 to 6; Q and Y are the same or different and ... | 03/13/2001 |
| 6194582 | Taxoids, their preparation and pharmaceutical compositions containing them New taxoids of general formula (I), their preparation, and pharmaceutical compounds containing them. ##STR1## In general formula (I), for example, Ar represents an aryl radical, R represents an alkoxyacetyl radical, R1 represents a benzoyl radical o... | 02/27/2001 |
