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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...
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7560475 |
Phenylacetic acid derivative, process for producing the same, and use
The present invention relates to the compound represented by formula (I)
(wherein R 1 and R 2 is hydrogen atom, C1-8 alkyl etc.; R 3 is C1-8 alkyl which may be substituted with 1 to 3...
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7557095 |
Therapeutic compounds
Disclosed herein is a compound having a structure
or a pharmaceutically acceptable salt thereof, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are...
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7550448 |
Therapeutic compounds
Disclosed herein is a compound having a structure
or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also...
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7528160 |
Fused heterocyclic derivatives as PPAR modulators
The present invention is directed to a method of treatment by modulating a peroxisome proliferator activated receptor by employing a compound of Structural Formula (I). The variables in I are...
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7511149 |
Process for the oxidation of certain substituted sulfilimines to insecticidal sulfoximines
Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.
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7504431 |
Sulfonyl amide inhibitors of calcium channel function
Compounds of formula I
its stereoisomers, solvates, and salts, thereof, wherein: a, b, c, d, f, n, m and Ra are defined herein are are inhibitors of calcium channel function, and are useful in...
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7476742 |
Indane acetic acid derivatives and their use as pharmaceutical agents
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 and to...
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7456210 |
Benzyloxy derivatives
The present invention relates to compounds of formula I
wherein R 1 and R 2 are as defined in the specification and to pharmaceutically acceptable salts thereof for the treatment of diseases,...
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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...
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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...
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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 Ar 1 , and Ar 2 ...
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7355049 |
Biaryloxymethylarenecarboxylic acids as glycogen synthase activator
The present invention relates to compounds of formula (I)
wherein R 1 , R 2 , R 3 , R 4 , m, n, p and s are as defined in the description and claims, and pharmaceutically acceptable salts...
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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...
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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,...
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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...
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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...
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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 ...
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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.
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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 R 1 and R 8 each are...
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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...
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7241755 |
Epothilone derivatives
The present invention relates to compounds of the formula
in which the variables G, W, Q, X, Y, B 1 , B 2 , Z 1 , Z 2 , and R 1 –R 7 are as defined herein, methods for the preparation of the...
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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,...
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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...
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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...
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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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7138406 |
Modulators of the glucocorticoid receptor
The present invention provides compounds of the formula
wherein A is of the formula
and X, Y, n, R 1 –R 25 are as described in the specification which are modulators of the...
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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...
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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...
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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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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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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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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.
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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
R 1 , R 2 , R 4 and Het are as...
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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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6949536 |
Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
This invention provides a compound of the formula:
or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially...
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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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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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6927227 |
Heterocyclic containing biphenyl aP2 inhibitors and method
aP2 inhibiting compounds are provided having the formula
wherein R 1 , R 2 , R 3 , R 4 , X—Z and
are as described herein.
A method is also provided for treating diabetes and related...
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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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6875873 |
1,4-Diamino-2-(thiazol-2-yl)benzene derivatives, and dyes containing said compounds
1,4-Diamino-2-(thiazol-2-yl)benzene derivatives of general formula (I) and the physiologically tolerated, water-soluble salts thereof:
and agents containing these compounds, for oxidative...
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6867224 |
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...
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6849636 |
Triazole derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as...
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6723740 |
Activator of PPAR delta
Compounds of Formula (I) are disclosed. These compounds selected activators of human PPAR delta.
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6713498 |
Method for treating glaucoma VI
Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the...
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6617460 |
Process for preparing toluenesulfinates
A process for preparing novel compounds useful in the preparation of 1H-indole-3-glyoxamides.
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6603015 |
Synthesis of epothilones
Commercially feasible methods for synthesizing various epothilones precursors needed for the preparation of final epothilones are provided, including techniques for the synthesis of epothilone...
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6586464 |
Artemisinin analogs having antimalarial, antiproliferative, and antitumor activities and chemoselective methods of making the same
Methods for producing novel artemisinin analogs and artemisinin dimers having antimalarial, antiproliferative and antitumor activities are described herein. These novel artemisinin analogs and...
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6583163 |
Agent for inhibition of cytokine production and agent for inhibition of cell adhesion
The present invention provides an agent for inhibiting cytokine production or cell adhesion, comprising at least one compound selected from the group consisting of thiazole derivatives represented...
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