|
Match
|
Document |
Document Title |
|
|
7598250 |
Cyclic amine BACE-1 inhibitors having a heterocyclic substituent
Disclosed are novel compounds of the formula
or a pharmaceutically acceptable salt or solvate thereof, wherein
R 1 is
X is —O—, —C(R 14 ) 2 — or —N(R)—; Z is...
|
|
|
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...
|
|
|
7566730 |
Substituted aminoethers for the treatment of Alzheimer's disease
The invention provides compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful...
|
|
|
7563902 |
Chemiluminescent compounds and their use
The present invention relates to novel chemiluminescent compounds, to a method for synthesizing these compounds, to derivatives and conjugates comprising these compounds, to the use of these...
|
|
|
7553859 |
Macrocycles for the treatment of cancer
The present invention relates to new Macro-cycles of Formula (I), and their use for the treatment of cancer.
|
|
|
7547701 |
Haloalkyl containing compounds as cysteine protease inhibitors
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these...
|
|
|
7541472 |
3-Aryl-3-hydroxy-2-methylenepropionic acid esters as fungicides
Compounds of formula I are described:
along with compositions thereof, methods of use thereof (particularly as fungicides), and methods of making the same.
|
|
|
7504420 |
Compounds which inhibit beta-secretase activity and methods of use
The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.
|
|
|
7468360 |
Therapeutic amides and related compounds
Disclosed herein is a compound having a structure:
Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.
|
|
|
7465804 |
Compounds, pharmaceutical compositions and methods for their use in treating metabolic disorders
The present invention provides compounds useful, for example, for modulating insulin levels in a subject, having the general formula I:
wherein Q is an optionally substituted phenyl; L is a...
|
|
|
7449468 |
Thiazole and oxazole derivatives as activators of human peroxisome proliferator activated receptors
The present invention provides a compound of formula (I):
wherein R 1 -R 5 , R 25 , R 26 , Y, y, and X 2 are as defined herein. The compounds activate human peroxisome proliferater...
|
|
|
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, R 2a , R 2b , R 3 , R 4a , R 4b , D-E, R 5 , R 6 , R 7 , R 8 and X have the meanings...
|
|
|
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...
|
|
|
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, R 1 , R 2 and X, are herein defined, the compounds being novel antagonists for melanin-concentrating hormone (MCH), as...
|
|
|
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 the other...
|
|
|
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...
|
|
|
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; R 1 is hydrogen or C 1-7 -alkyl; R 2 and R 3 independently from each...
|
|
|
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...
|
|
|
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.
|
|
|
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 R 2 , R 3 , R 4 , R 6 , R 8 and Y are defined herein. The compounds are useful for...
|
|
|
7309709 |
Thiazole sulfonamide compounds for the treatment of neurodegenerative disorders
The present invention relates to compounds of the Formula:
wherein R 1 to R 6 , X, Z and A are as defined. These compounds have activity inhibiting production of Aβ-peptide. The invention...
|
|
|
7265137 |
Activator of peroxisome proliferator-activated re-ceptor δ
A compound represented by the following general formula (I):
(wherein R 1 represents phenyl, etc. which can have substituents selected from the group consisting of C 1-8 alkyl, C 1-8 ...
|
|
|
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.
|
|
|
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...
|
|
|
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...
|
|
|
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...
|
|
|
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...
|
|
|
7229998 |
Thiazole and oxazole derivatives as activators of human peroxisome proliferator activated receptors
The present invention provides a compound of formula (I):
wherein R 1 –R 5 , R 25 , R 26 , Y and X 2 are as defined herein. The compounds activate human peroxisome proliferator...
|
|
|
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...
|
|
|
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 R 1 is a hydrogen atom or an optionally substituted lower alkyl...
|
|
|
7214678 |
Arylsulfanyl and heteroarylsulfanyl derivatives for treating pain
According to the invention there is provided a compound the formula I;
wherein A, X, B, R 1 , R 2 , R 3 and R 4 are as defined in the specification.
|
|
|
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: R 1 , R 2 , R 3 , R 4 , R 5 are hydrogen...
|
|
|
7208506 |
Heteroarylethenyl derivatives, their manufacture and use as pharmaceutical agents
The present invention relates to compounds of formula I
wherein R 1 , R 2 and R 3 are defined herein, their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and...
|
|
|
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...
|
|
|
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.
|
|
|
7196107 |
Thia-and oxazoles and their use as ppars activators
A compound of formula (I) or pharmaceutically acceptable salts and solvates thereof. R 1 and R 2 are independently H or C 1-3 alkyl, m is 0–3; X 1 is NH, NCH 3 , O, S; R 3 , R 4 and R 5 are...
|
|
|
7192979 |
EP4 receptor selective agonist in the treatment of osteoporosis
This invention is directed to EP4 receptor selective prostaglandin agonists of the Formula I,
wherein R 2 , X, Z and Q are as defined in the specification. This invention is also directed to...
|
|
|
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.
|
|
|
7189857 |
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 R 1 is an optionally substituted lower alkyl,...
|
|
|
7183294 |
Indole derivatives useful for the treatment of diseases
The invention relates to indole derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole...
|
|
|
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...
|
|
|
7169930 |
Analogs of epothilone
Designed epoxide and cyclopropane epothilone analogs with substituted side-chains are disclosed and characterized with respect to their biological activities against a series of human cancer cell...
|
|
|
7153946 |
Molecular conjugates for use in treatment of cancer
A molecular conjugate is provided having the formula:
wherein R 1 is a de-hydroxyl or de-amino moiety respectively of a hydroxyl-bearing or amino-bearing biologically active molecule or an...
|
|
|
7153878 |
Peroxisome proliferator activated receptor modulators
The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I. (Formula I); wherein: (a) R5 is selected...
|
|
|
7153815 |
Insecticide containing hydrazone derivative as the active ingredient and novel hydrazone derivative
A insecticide characterized by containing as active ingredient a hydrazone derivative of formula (I)
wherein A and Q are an aryl or a heterocyclic group, W is oxygen atom, an aminylene, an...
|
|
|
7148359 |
Polymorph of a pharmaceutical
A new crystalline polymorph of ritonavir and methods for its use and preparation are disclosed.
|
|
|
7144904 |
Iron binding agents
Composition, article of manufacture for and method of treating malaria in a human having an infestation of Plasmodium protozoans are described. The method comprises administering a...
|
|
|
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...
|
|
|
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...
|
|
|
7125863 |
Inhibitors of dipeptidyl peptidase IV
Compounds according to formula (1), wherein R 1 is H or CN, X 1 is S, O, SO 2 or CH 2 , X 2 is CO, CH 2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The...
|