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| Number | Title | Issue Date |
| 8183383 | Protein tyrosine phosphatase 1B inhibitor, preparation methods and uses thereof PTP1B inhibitors with the following structure (formula I). Experiments indicate that these inhibitors can effectively inhibit the activity of protein tyrosine phosphatase 1B (PTP1B). They can be used as insulin sensitisers. They can be used to prevent, delay or trea... | 05/22/2012 |
| 8076490 | 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. ... | 12/13/2011 |
| 7795444 | Human protein tyrosine phosphatase inhibitors and methods of use The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPT... | 09/14/2010 |
| 7763733 | Ritonavir analogous compound useful as retroviral protease inhibitor, preparation of the ritonavir analogous compound and pharmaceutical composition for the ritonavir analogous compound The present invention describes a new one ritonavir analogous compound that presents significantly superior activity in inhibition of HIV protease. There are also described the usage of the ritonavir analogous compound of the present invention or salt, ester or prod... | 07/27/2010 |
| 7750164 | Synthesis of epothilones, intermediates thereto, analogues and uses thereof The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention furth... | 07/06/2010 |
| 7659405 | Polymorph of a pharmaceutical A new crystalline polymorph of ritonavir and methods for its use and preparation are disclosed. ... | 02/09/2010 |
| 7622593 | Human protein tyrosine phosphatase inhibitors and methods of use The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPT... | 11/24/2009 |
| 7407959 | Cathepsin cysteine protease inhibitors This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, s... | 08/05/2008 |
| 7407975 | Epothilone derivatives, method for producing same and their pharmaceutical use This invention relates to the new epothilone derivatives of general formula I, in which substituents Y, Z, R2a, R2b, R3, R4a, R4b, D-E, R5, R6 | 08/05/2008 |
| 7375134 | Cathepsin cysteine protease inhibitors This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, s... | 05/20/2008 |
| 7361769 | Heterocyclyls as selective melanin concentrating hormone receptor antagonists for the treatment of obesity and related disorders The present invention discloses compounds of formula I wherein m, n, p, R1, R2 and X, are herein defined, the compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as metho... | 04/22/2008 |
| 7358266 | Cyclopropyl and cyclobutyl epothilone analogs The invention relates to cis- and trans-12, 13-cyclopropyl and 12,13-cyclobutyl epothilones of formula I to IV wherein Ar is a radical represented by the following structure: and ... | 04/15/2008 |
| 7351825 | Cyclopropane compounds and pharmaceutical use thereof The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): | 04/01/2008 |
| 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 |
| 7332608 | Anthranilamides and methods of their use The present invention is related to a process for preparing anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and p... | 02/19/2008 |
| 7323573 | Production of polyketides Recombinant Myxococcus host cells can be used to produce polyketides, including epothilone and epothilone analogs that can be purified from the fermentation broth and crystallized. ... | 01/29/2008 |
| 7312211 | Pryanone compounds useful as reversible inhibitors of cysteine proteases Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and othe... | 12/25/2007 |
| 7312237 | Combination of epothilone analogs and chemotherapeutic agents for the treatment of prolilferative diseases Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders. ... | 12/25/2007 |
| 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 |
| 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 |
| 7250412 | PH sensitive prodrugs of 2,6-Diisopropylphenol The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby providing an alternative to the water-insoluble 2,6-diisopropylpheno... | 07/31/2007 |
| 7244594 | Microbial transformation method for the preparation of an epothilone A microbial method for the preparation of an epothilone containing a terminal hydroxyalkyl group, comprising contacting at least one epothilone having a terminal alkyl group with an enzyme or microorganism capable of catalyzing the selective hydroxylation of said al... | 07/17/2007 |
| 7244725 | Acetyl 2-hydroxy-1, 3-diaminoalkanes Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and RC are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase en... | 07/17/2007 |
| 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 |
| 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 |
| 7241801 | Viral polymerase inhibitors A compound, represented by formula (I): wherein A, B, R1, R2, R3, R5, R6, R7, R9, and R10 are as defined herein, or an enant... | 07/10/2007 |
| 7241901 | Process for preparing thiazole derivative and the intermediate compounds for preparing the same The present invention provides a process for preparing thiazole derivatives of formula (XI), that activate the delta subtype of the human Peroxisome Proliferator Activated Receptor (hPPARδ), and also provides processes for compounds of formula (VI), (VII), (VIII) a... | 07/10/2007 |
| 7235690 | Anthranilamides and methods of their use The present invention is related to anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations con... | 06/26/2007 |
| 7229998 | Thiazole and oxazole derivatives as activators of human peroxisome proliferator activated receptors The present invention provides a compound of formula (I): wherein R1–R5, R25, R26, Y and X2 are as defined herein. The compounds a... | 06/12/2007 |
| 7220752 | Compounds active at the glucocorticoid receptor II This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose ... | 05/22/2007 |
| 7217832 | 5-amidino-2-hydroxybenzenesulfonamide derivatives, pharmaceutical compositions containing the same and intermediates for their preparation The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; | 05/15/2007 |
| 7214802 | Anti-cytokine heterocyclic compounds Disclosed compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chr... | 05/08/2007 |
| 7214678 | Arylsulfanyl and heteroarylsulfanyl derivatives for treating pain According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification. | 05/08/2007 |
| 7211593 | C12-cyano epothilone derivatives The present invention relates to compounds useful in the treatment of cancer or other proliferative diseases represented by the formula wherein: R1, R2 | 05/01/2007 |
| 7211668 | PNA monomer and precursor This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: | 05/01/2007 |
| 7208506 | Heteroarylethenyl derivatives, their manufacture and use as pharmaceutical agents The present invention relates to compounds of formula I wherein R1, R2 and R3 are defined herein, their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and... | 04/24/2007 |
| RE39575 | Substituted thioacetamides The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases. ... | 04/17/2007 |
| 7205413 | Solvates and polymorphs of ritonavir and methods of making and using the same Novel solvates and crystal polymorphs of Ritonavir are disclosed, as well as methods of making them. Specific solvates of the compound include a formamide solvate and a partially desolvated solvate. Also disclosed are methods of making previously known forms of Rito... | 04/17/2007 |
