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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...
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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...
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RE39356 |
Process for the preparation of epothilone analogs
The present invention relates to a process for the preparation of epothilone analogs by initially forming novel ring-opened epothilones and carrying out a macrolactamization reaction thereon. The...
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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, X 1 is C or N, and R 1 , R 2 , R 2a , R 2b , R 2c , R 3 , Y, A, m, n, X 2 , X 3 and X 4 are as defined herein, which...
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7105564 |
Pharmaceutical composition comprising a dual antagonist against PGD2/TXA2 receptors having a [2.2.1] or [3.1.1] bicyclic skeleton
The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D 2 receptor and pharmaceutical compositions comprising them. ...
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7105551 |
Thiazole derivatives for treating PPAR related disorders
The present invention provides compounds of formula (I). These compounds are used for the treatment of PPAR related diseases
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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...
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7098228 |
Indolyl derivatives
The present invention provides compounds of formula I
as well as pharmaceutically acceptable salts and esters thereof, wherein R 1 to R 4 , A and n have the significance given in the...
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7094792 |
Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
The present invention relates to compounds with the formula (I)
and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for...
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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...
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7053069 |
Pharmaceutical compositions and methods of using C-21 modified epothilone derivatives
Pharmaceutical compositions containing C-21 modified epothilone derivatives, methods for their preparation and dosing regimen for administration of these epothilone compounds are provided. The...
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7045532 |
ACE-2 modulating compounds and methods of use thereof
ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include...
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7041690 |
Inhibitors of HCV NS5B polymerase
The present invention provides compounds of Formula I, compositions and methods that are useful for treating viral infections and associated diseases, particularly HCV infections and associated...
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7030139 |
Compounds
Compounds of general formula (I), are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in...
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7030239 |
Compounds to treat Alzheimer's disease
The present invention is directed toward substituted hydroxyethylene compounds of formula (XII)
useful in treating Alzheimer's disease and other similar diseases.
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7022719 |
Preventing and reversing the formation of advance glycosylation endproducts
The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent...
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7001916 |
Epothilon derivatives, method for the production and the use thereof as pharmaceuticals
Disclosed are epothilone compounds of formula I,
which are useful as pharmaceutical compounds for treating, for example, malignant tumors and chronic inflammatory diseases and are useful in...
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6998256 |
Methods of obtaining epothilone D using crystallization and /or by the culture of cells in the presence of methyl oleate
Methods are provided for purification of epothilone D and epothilone D analogs from epothilone producing cells such as, for example, Sorangium cellulosum and Myxococcus xanthus (recombinant)....
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6989450 |
Synthesis of epothilones and related analogs
The present invention relates to methods for use in producing epothilones and analogs and derivatives thereof. A general method according to the present invention broadly comprises performing an...
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6958401 |
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...
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6949566 |
Thiazole and oxazole derivatives
A compound of the formula (I):
wherein R 1 is hydroxy and the like; R 2 is optionally substituted lower alkyl and the like; R 3 is hydrogen atom and the like; R 4 is optionally...
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6946561 |
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...
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6936602 |
Benzazepine derivatives, process for the preparation of the same and uses thereof
Compounds of the general formula (I):
or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R 1 is a 5- to 6-membered...
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6936719 |
Biaryl compounds as serine protease inhibitors
Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat...
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6936628 |
Oral administration of epothilones
The invention relates to methods of increasing the bioavailability of orally administered epothilones. Epothilones administered by the methods of the invention are sufficiently bioavailable to have...
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6930187 |
Method of preparation of 21-amino epothilone derivatives
An improved method of synthesis of 21-amino epothilone derivatives which provides a one-pot conversion of 21-hydroxy epothilones to highly desirable 21-amino epothilones in high yield.
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6924300 |
Oxyiminoalkanoic acid derivatives
To provide a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the prevention or treatment of diabetes mellitus, hyperlipemia,...
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6916813 |
(1-phenyl-2-heteoaryl)ethyl-guanidine compounds as inhibitors of mitochondrial F1F0 ATP hydrolase
Compounds having the formula (I), and pharmaceutically acceptable salts thereof,
are useful for modulating mitochondrial F 1 F 0 ATPase activity and treating ischemic conditions including...
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6903119 |
Amino acid derivatives and drugs containing the same as the active ingredient
The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification).
The compounds of the formula (I)...
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6903131 |
3,4-di-substituted maleimide compounds as CXC chemokine receptor antagonists
Disclosed are compounds of the formula (I)
or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the treatment of chemokine-mediated diseases such as acute and...
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6900331 |
Derivatives of epothilone B and D and synthesis thereof
The present invention provides the following new compounds: (R)-C14-methyl-epothilone B, (S)-C14-methyl-epothilone B, (S)-C14-methyl-epothilone D, and (R)-C14-methyl-epothilone D and methods for...
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6894171 |
Polymorph of a pharmaceutical
A new crystalline polymorph of ritonavir and methods for its use and preparation are disclosed.
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6884821 |
Carboxylic acid derivatives and drugs containing the same
Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the...
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6875765 |
Arylsulfonamide ethers, and methods of use thereof
The novel arylsulfonamide ether compounds, pharmaceutical compositions and uses thereof as inhibitors of interleukin-1β converting enzyme and other cysteine proteases in the ICE family are...
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6869967 |
Peroxisome proliferator-activated receptor (PPAR) active vinyl carboxylic acid derivatives
Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these...
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6864270 |
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...
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6858611 |
Potassium channel inhibitors
Compounds which are useful as potassium channel inhibitors and which because of their slow off-rates are especially useful for the treatment of cardiac arrhythmias are described.
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6838474 |
Sulphonamide derivatives as prodrugs of aspartyl protease inhibitors
The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl...
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6831076 |
Epothilons C and D, preparation and compositions
The present invention relates to epothilon derivatives and to their use.
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6818635 |
7-substituted tetracycline compounds
The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states,...
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6812229 |
Carbamate derivative and agricultural/horticultural fungicide
It is to provide a novel fungicide having high controlling effects on plant diseases particularly on wheat powdery mildew and cucumber gray mold, without ill effects on crops. A carbamate...
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6809110 |
Thiazole derivatives
The present invention provides compounds of formula (I) wherein R 1 to R 10 , X, Y and n are indicated in the specification, and pharmaceutically acceptable salts and esters thereof. The...
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6803466 |
HIV/FIV protease inhibitors having a small P3 residue
With the help of X-ray structural analyses of drug-resistant HIV proteases and molecular modeling, a new type of inhibitor with a small P3 residue has been developed. These inhibitors are effective...
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6800653 |
Epothilone derivatives
The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives, and intermediates therefor.
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6787552 |
PPAR delta activators
Compounds of the general formula (I) or salts thereof and activators of PPARδ (peroxisome proliferator activated receptor δ) containing the compounds or the salts as the active ingredient:...
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6784167 |
17-beta-hydroxysteroid dehydrogenase-II inhibitors
17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula wherein the phenyl group labeled A and the group —C(R 4 )(R 6 )Y are oriented cis to each other; W represents O...
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6780995 |
Activated iododerivatives for the treatment of cancer and aids
A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an...
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6777418 |
Retinoid compounds (I)
The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical...
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6743810 |
Indol-3-yl derivatives
Indol-3-yl derivatives of the general formula I in which A, B, X, R 1 , R 2 , R 3 , R 4 , R 5 , n and m are as defined in patent claim 1 , and their physiologically acceptable salts or solvates...
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6737418 |
Aryl substituted pyrazoles, imidazoles, oxazoles, thiazoles and pyrroles, and the use thereof
This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R 5 -R 13 are set in the specification. The...
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