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7601729 |
Matrix metalloproteinase inhibitors
Compounds of Formula (I):
wherein:
A represents bond, C 1-6 alkyl or CH═CH—C 1-4 alkyl; B represents bond, O, S, SO, SO 2 , CO, CR 7 R 8 , CO 2 R 14 , CONR 14 R 15 , N(COR 14 )(COR 15 ),...
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7601723 |
Pyridyl substituted xanthines
The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xanthines of formula I
which are selective antagonists of A 2B adenosine receptors...
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7598392 |
2-amido-4-phenylthiazole derivatives, the preparation and the therapeutic use thereof
The disclosure relates to 2-amido-4-phenylthiazole derivatives of general formula (I) below:
in which R 1 , R 2 , R 3 , Y, m, n, and p are as defined in the disclosure; as well as to their...
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7595326 |
Synthesis of novel tubulin polymerization inhibitors: benzoylphenylurea (BPU) sulfur analogs
A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6 n and 7 d were shown to possess up to 10-fold increased potency, when...
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7589095 |
4-phenyl-pyrimidine-2-carbonitrile derivatives
The invention relates to 4-phenyl-pyrimidine-2-carbonitrile derivatives having the general formula I
wherein each of the substituents is given the definition as set forth in the specification...
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7589090 |
Diaminopyrimidines as P2X3 and P2X2/3 modulators
Compounds and methods for treating diseases mediated by a P2X 3 and/or a P2X 2/3 receptor antagonist, the compounds being of formula (I):
wherein R 1 , R 2 , R 3 and R 4 are as defined herein.
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7582646 |
Pyrimidine derivatives for treatment of hyperproliferative disorders
Pyrimidine derivatives of formula (I)
in which J and Y represent aromatic or heteroaromatic rings; R 2 , G, G′, and G″ represent substituent groups and R 2a represents H or halogen; L...
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7582645 |
Pyrimidine derivatives for treatment of hyperproliferative disorders
Pyrimidine derivatives of formula (I) in which J and Y represent aromatic or heteroaromatic rings; R 2 , G, G′, and G″ represent substituent groups and R 2a represents H or halogen; L...
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7582644 |
Pyrimidyl sulphone amide derivatives as chemokine receptor modulators
A compound of formula (I), pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof for the treatment of asthma, allergic rhinitis, COPD, inflammatory bowel disease,...
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7579357 |
Dipeptidyl peptidase inhibitors
Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV inhibitors comprising Formula I:
wherein the substituents are as described herein.
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7576076 |
Modified pyrimidine glucocorticoid receptor modulators
The present invention provides a compound having the formula:
wherein, n and m are 1 ; X 1 and X 2 are O; R 1 is a member selected from unsubstituted phenyl and substituted phenyl; R 2 is...
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7566723 |
1-phenyl1-3,4-dihydropyrimidin-2(1H)-one derivatives and their use
The invention relates to novel 1-Phenyl-3,4-dihydropyrimidin-2(1H)-one derivatives having the formula
processes for their preparation, and their use in medicaments, especially for the...
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7566710 |
Dual molecules containing a peroxide derivative, synthesis and therapeutic applications thereof
The invention relates to dual molecules formed from coupling products complying with the formula
wherein A represents a residue of molecule with anti-malarial activity, Y 1 and Y 2 ,...
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7560464 |
Polycyclic pyrimidines as potassium ion channel modulators
The present invention provides a genus of polycyclic pyrimidines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and...
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7553840 |
4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds and methods of their use
Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders:
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7547700 |
Aryl-[4-halo-4(heteroarylmethylamino)-methyl]-piperidin-1-1yl]-methanone derivatives, methods for production and use thereof as medicaments
The invention relates to compounds of general formula (1) in which X and Y=a carbon with a bonded hydrogen atom (CH) or a nitrogen atom, A=a methyl, fluoromethyl, cyano, hydroxyl, methoxy group, or...
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7544688 |
Hetereoaryl nitrile derivatives
The invention provides compounds of Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use...
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7534798 |
Vanilloid receptor ligands and their use in treatments
Compounds having the general structure
and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster...
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7531547 |
Diaminopyrimidines as P2X3 and P2X2/3 modulators
Compounds and methods for treating diseases mediated by a P2X 3 and/or a P2X 2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a...
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7531532 |
Pyridine derivative and pyrimidine derivative
A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor...
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7524874 |
Vanilloid receptor ligands and their use in treatments
Compounds having the general structure
and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster...
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7517882 |
Protein kinase inhibitors
Pyrimidine- and triazine-based chemical compounds that are useful, for example, as protein kinase inhibitors for treating cancer, neurological disorders, autoimmune disorders, and other diseases,...
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7514413 |
In-vivo energy depleting strategies for killing drug-resistant cancer cells
This invention also provides a method for treating a cancer subject comprising administering to the subject a combination of ATP-depleting agents at concentrations which deplete the ATP level to,...
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7504405 |
Mitotic kinesin inhibitors
The present invention relates to compounds that are useful for treating cellular proliferative diseases, for treating disorders mediated, at least in part, by KSP, and for inhibiting KSP. The...
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7501429 |
Pyrimidine compounds as anti-ictogenic and/or anti-epileptogenic agents
Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and/or...
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7491728 |
Pyrimidinone compounds as calcilytics
The pyrimidinone compounds are disclosed. Methods of preparing the pyrimidinone compounds are also disclosed.
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7488733 |
6-arylamino-5-cyano-4-pyrimidinones as pde9a inhibitors
The invention relates to novel 6-arylamino-5-cyano-4-pyrimidinones of formula (I)
methods for the production thereof, and the use thereof for producing medicaments utilized for improving...
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7479495 |
N-heterocyclic inhibitors of TNF-α expression
N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I:
Methods of...
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7470714 |
GM-95-containing antitumor effect potentiator, combined antitumor preparation and antitumor agent
An antitumor effect enhancer for enhancing the antitumor effects of an antitumor substance, which comprises a compound represented by the following formula (1):
wherein each R independently...
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7470699 |
Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
The present invention relates to certain trisubstituted aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism.
Accordingly, compounds of the present invention are...
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7470685 |
Pyrimidine compounds
This invention features pyrimidine compounds of formula (I):
R 1 is
in which one of R a and R b is H or alkyl, and the other is aryl or heteroaryl optionally substituted with R d and R...
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7465736 |
Azole methylidene cyanide derivatives and their use as protein kinase modulators
An azole derivative of formula (I)
a medicament that contains the azole derivative of formula (I), a method of treating a disease with the azole derivative of formula (I), and a method of...
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7465735 |
5-Phenypyrimidines their preparation compositions comprising them and their use
5-Phenylpyrimidines, their preparation, compositions comprising them and their use 5-Phenylpyrimidines of the formula I
in which the substituents and the index are as defined below:
R 1 ,R 2 ...
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7465725 |
Pyrimidine compounds
This invention features pyrimidine compounds of formula (I):
R 1 is
aryl, or heteroaryl; each of R 2 and R 4 , independently, is R c , halogen, nitro, cyano, isothionitro, SR c , or OR c ;...
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7462625 |
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ...
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7462619 |
Pyridazine, pyrimidine and pyrazine ethyne compounds
In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring...
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7459452 |
Dihydroxypyrimidine carboxamide inhibitors of HIV integrase
4,5-Dihydroxypyrimidine-6-carboxamides of formula:
are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R 1 , R 2 , R 3 and R 4 are defined herein. These...
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7452896 |
Pyrimidine-sulfamides and their use as endothelian receptor antagonist
The invention relates to novel sulfamic acid amides of General Formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related...
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7449471 |
5-phenylpyrimidines, their preparation, compositions comprising them and their use
5-Phenylpyrimidines of the formula I
in which the substituents and the index are as defined below:
R 1 ,R 2 are hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl,...
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7442702 |
Prostaglandin agonists
This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such...
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7442701 |
Amino-heterocycles as VR-1 antagonists for treating pain
The present invention provides a compound of formula (I): wherein V represents NR 5 , O, S, SO or S(O) 2 ; W and X each independently represent CH or N; Y represents N, CH or C—Ar 2 , with the...
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7439250 |
Compositions and methods related to fatty amino acid derivatives
The present invention concerns the use of methods and/or compositions related to the synthesis and use of fatty asparagine, cysteine and/or serine derivatives. In particular, the invention concerns...
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7435741 |
2-N{5-[[4-[2-(methyl-2-pyridinylamino) ethoxy] phenyl]methyl]-2,4-thiazolidinedione} butanedioic acid, methods of preparation and compositions with rosiglitazone maleate
Disclosed is an isolated compound of the formula:
along with methods of detecting it and of minimizing it in improved pharmaceutical compositions of rosiglitazone maleate.
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7435734 |
N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula:
are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R 1 , R 2 , R 3 and R 4 are defined...
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7435729 |
Compounds and methods for modulation of estrogen receptors
Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for...
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7432272 |
Antiviral analogs
The application relates to 4′-substituted nucleoside derivatives of Formula I:
wherein B and R 1 have any of the values described in the application, as well as to compositions comprising...
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7423148 |
Small molecule PI 3-kinase inhibitors and methods of their use
Compounds having formula I are provided where the variables have the values described herein.
Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a...
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7423044 |
Pyrimidine derivatives useful in the treatment of insulin resistance and hyperglycemia
This invention provides compounds of Formula I having the structure:
wherein:
B is alkyl of 1-4 carbons or alkoxy of 1-4 carbons; R 1 is aryl or Het optionally substituted with R 6 ; R 2 and...
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7405214 |
Nucleoside derivatives and therapeutic use thereof
The present invention relates to nucleoside derivatives represented by general formulas I and II, their synthetic methods and their pharmacologically acceptable salts thereof, and compositions...
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7402587 |
Crystalline forms of a pyridinyl-sulfonamide and their use as endothelin receptor antagonists
Crystalline forms A and B of 5-methyl-pyridine-2-sulfonic acid [6-methoxy-5-(2-methoxy-phenoxy)-2-pyridin-4-yl-pyrimidin-4-
yl]-amide of formula (I) are described, whereby form B is the most stable...
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