Quotables
"It is my heart-warmed and world-embracing Christmas hope and aspiration that all of us, the high, the low, the rich, the poor, the admired, the despised, the loved, the hated, the civilized, the savage (every man and brother of us all throughout the whole earth), may eventually be gathered together in a heaven of everlasting rest and peace and bliss, except the inventor of the telephone. "
Mark Twain ; Christmas greetings, 1890
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| Number | Title | Issue Date |
| 7982050 | Process for preparing ligands of PPARdelta and the intermediate compounds for preparing the same The present invention provides a process for preparing thiazole derivatives of formula (I), that activate the delta subtype of the human Peroxisome Proliferator Activated Receptor (hPPAR δ), and also provides compounds of formula (II), (IV), (X), (XI) and (XII), in... | 07/19/2011 |
| 7569698 | Process for the isolation and purification of epothilones The invention relates to a desorption process for epothilones, especially epothilone A and/or epothilone B, from resins and new production, work-up or purification processes or manufacturing methods for epothilones comprising said desorption process, as well as the ... | 08/04/2009 |
| 7402606 | Derivatives of 1-(oxoaminoacetyl) pentylcarbamate as cathepsin K inhibitors for the treatment of bone loss Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle ... | 07/22/2008 |
| 7384964 | Synthesis of epothilones, intermediates thereto, analogues and uses thereof The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (... | 06/10/2008 |
| 7368479 | Alpha-sulfonylamino-acetonitriles The invention relates to α-sulfonylamino-acetonitrile derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein Ar1, and Ar2 independently of each other stand for an optionally substitut... | 05/06/2008 |
| 7355049 | Biaryloxymethylarenecarboxylic acids as glycogen synthase activator The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, m, n, p and s are as defined in the description and claims, and pharmaceutically acceptable salts... | 04/08/2008 |
| 7345067 | Aniline derivatives, their manufacture and use as pharmaceutical agents This invention relates to compounds of the formula wherein X is N and Y is S or O; or X is S or O and Y is N; R1 is hydrogen or C1-7... | 03/18/2008 |
| 7332513 | Thiazole-based nitric oxide donors having acyl substituent(s) and uses thereof Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or dec... | 02/19/2008 |
| 7319096 | Thyroid hormone receptor antagonists for cardiac and metabolic disorders II This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subclinical hyperthyrodism... | 01/15/2008 |
| 7309709 | Thiazole sulfonamide compounds for the treatment of neurodegenerative disorders The present invention relates to compounds of the Formula: wherein R1 to R6, X, Z and A are as defined. These compounds have activity inhibiting production of Aβ-peptide. The invention also... | 12/18/2007 |
| 7294640 | Mitotic kinesin inhibitors The present invention relates to substituted thiazole derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin and MCAK activity, and for inhibiting KSP kinesin and MCAK. The invention also relates ... | 11/13/2007 |
| 7276526 | Substituted thiazoles and oxazoles as corticotropin releasing hormone ligands Provided herein are novel substituted thiazoles and oxazoles of the Formula (I): as well as compositions, including pharmaceutical compositions, containing the same, and the use thereof in the treatment of variou... | 10/02/2007 |
| 7265137 | Activator of peroxisome proliferator-activated re-ceptor δ A compound represented by the following general formula (I): (wherein R1 represents phenyl, etc. which can have substituents selected from the group consisting of C1-8 | 09/04/2007 |
| 7259157 | N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain. ... | 08/21/2007 |
| 7244752 | Broadspectrum 2-(substituted-amino)-benzoxazole sulfonamide HIV protease inhibitors The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are ... | 07/17/2007 |
| 7241755 | Epothilone derivatives The present invention relates to compounds of the formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1–R7 are as defined herein,... | 07/10/2007 |
| 7241899 | Methods for the preparation, isolation and purification of epothilone B, and X-ray crystal structures of epothilone B The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent pur... | 07/10/2007 |
| 7235669 | Epothilone side components The invention concerns compounds which can be obtained by fermenting DSM 6773, especially epothilones A1, A2, A8, A9, B10, C1, C2, C3, C4, C5, C6, C7, C8, C9, D1, D2, D5, G1, G2, H1, H2, I1, I2, I3, I4, I5, I6 and K and trans-epothilones C1 and C2. ... | 06/26/2007 |
| 7208623 | Process for the manufacture of HMG-CoA reductase inhibitory mevalonic acid derivatives The invention relates to a process for the manufacture of a compound of formula: (Formula I); or a salt, especially a pharmaceutically acceptable salt with a base, thereof or a lactone thereof wherein the element (a) represents —CH2—CH2— ... | 04/24/2007 |
| 7196107 | Thia-and oxazoles and their use as ppars activators A compound of formula (I) or pharmaceutically acceptable salts and solvates thereof. R1 and R2 are independently H or C1-3alkyl, m is 0–3; X1 is NH, NCH3, O, S; R3, R4 and R5 a... | 03/27/2007 |
| 7189858 | N-phenyl substituted carbamoyloxyalkyl-azolium derivatives N-substituted carbamoyloxyalkyl-azolium derivatives Which have antifungal activity and are useful for the treatment of fungal diseases. ... | 03/13/2007 |
| 7173137 | Epothilone analogs Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of micro... | 02/06/2007 |
| 7166726 | Aryl substituted 3,4-dihydroanthracene derivatives having retinoid antagonist or retinoid inverse agonist type biological activity Disclosed herein are compounds of the formula wherein R1 is independently H or alkyl of 1 to 6 carbons; R2 is optional and is defined as lower alkyl of 1 to 6 carbons, F, Cl, Br... | 01/23/2007 |
| 7151182 | Intermediates for N-substituted carbamoyloxyalkyl-azolium derivatives N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases. ... | 12/19/2006 |
| 7145018 | Method for synthesizing epothilones and epothilone analogs A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. One embodiment of the method was used to synthesize epothilone B by a convergent approach that entailed Wittig coupling of an ylide derived from phosphoni... | 12/05/2006 |
| 7141533 | Hetaryl-substituted heterocycles The present invention relates to novel compounds of the formula (I) in which A, B, W, G and Het are each as defined in the description, to a plurality of processes for their preparation a... | 11/28/2006 |
| 7141672 | Oxazole-aryl-carboxylic acids useful in the treatment of insulin resistance and hyperglycemia This invention provides compounds of Formula I having the structure or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia. ... | 11/28/2006 |
| 7138406 | Modulators of the glucocorticoid receptor The present invention provides compounds of the formula wherein A is of the formula and X, Y, n, R1–R25 are as described in the speci... | 11/21/2006 |
| 7129071 | Recombinant methods and materials for producing epothilone and epothilone derivatives Recombinant nucleic acids that encode all or a portion of the epothilone polyketide synthase (PKS) are used to express recombinant PKS genes in host cells for the production of epothilones, epothilone derivatives, and polyketides that are useful as cancer chemothera... | 10/31/2006 |
| 7112597 | Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic d... | 09/26/2006 |
| 7109222 | Compounds that modulate PPAR activity and methods of preparation This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic a... | 09/19/2006 |
| 7105556 | Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2 | 09/12/2006 |
| 7101702 | Fermentative preparation process for and crystal forms of cytostatics The invention relates to a new process for concentrating epothilones in culture media, a new process for the production of epothilones, a new process for separating epothilones A and B and a new strain obtained by mutagenesis for the production of epothilones, as we... | 09/05/2006 |
| 7091226 | Cancer treatment with epothilones The invention relates to the treatment of a proliferative disease, especially according to certain treatment regimens, with an epothilone, especially with epothilone A and more preferably epothilone B; as well as to the treatment of certain cancers with such an epot... | 08/15/2006 |
| 7091225 | Substituted oxazoles and thiazoles as hPPAR alpha agonists Compounds of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof wherein X is O or S X1 is O or S; X is S or O; R1 and R2 are independently H, methyl, or halogen; R4 and R5 are independently H or C1-3 alkyl or R4 and R5 may, t... | 08/15/2006 |
| 7070964 | Epothilone compounds and methods for making the same The present invention provides bioconversion methods for making epothilone analogs. These analogs differ from the starting material by the addition of one or more hydroxyl groups or by the addition of an epoxide. These compounds, in turn, can be further modified by ... | 07/04/2006 |
| 7067544 | Epothilones C, D, E and F, preparation and compositions The present invention relates to epothilones C, D, E and F, their preparation and their use for the production of therapeutic compositions and compositions for plant protection. ... | 06/27/2006 |
| 7056954 | Means for the modulation of processes mediated by retinoid receptors and compounds useful therefor In accordance with the present invention, there are provided methods to modulate processes mediated by retinoid receptors, employing high affinity, high specificity ligands for such receptors. In one aspect of the present invention, there are provided ligands which ... | 06/06/2006 |
| 7034165 | Protected 3,-5-dihydroxy-2,2-dimethyl-valeronitriles for the synthesis of epothilones and epothilone derivatives and process for the production The invention relates to 3,5-dihydroxy-2,2-dimethyl-valeronitriles for the synthesis of epothilones and epothilone derivatives and process for the production of these new intermediate products in the synthesis and the use for the production of epothilones or epothil... | 04/25/2006 |
| 7026307 | Method for producing 1,3-disubstituted 2-nitroguanidines The present invention relates to a process for the preparation of compounds of the formula (I) by reacting compounds of the formula (II) in which ... | 04/11/2006 |
