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7166593 |
Glucocorticoid receptor modulators
The present invention provides non-steroidal compounds of formula I which are selective modulators (i.e., agonist and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor....
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7166609 |
Pyrimidine-4,6-dicarboxylic acid diamides for selectively inhibiting collagenases
Pyrimidine-4,6-dicarboxylic acid diamides of the formula I
are suitable for selectively inhibiting collagenase (MMP 13). The pyrimidine-4,6-dicarboxylic acid diamides can therefore be used for...
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7163951 |
N-biarylmethyl aminocycloalkanecarboxamide derivatives
N-Biarylmethylaminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated...
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7160890 |
Compounds specific to adenosine A3 receptor and uses thereof
This invention pertains to compounds which specifically inhibit the adenosine A 3 receptor and the use of these compounds to treat a disease associated with A 3 adenosine receptor in a subject,...
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7160876 |
Fused bicycloheterocycle substituted quinuclidine derivatives
Compounds of formula (I)
wherein n is 0, 1, or 2; X is O, S, —NH—, and —N-alkyl-; Ar 1 is a 6-membered aromatic ring; and Ar 2 is a fused bicycloheterocycle. The compounds are useful in...
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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...
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7153860 |
5-Phenylpyrimidines, methods and intermediate products for the production thereof and use of the same for controlling pathogenic fungi
The invention relates to 5-phenylpyrimidine of formula (I) wherein the substituents have the following designations: R 1 represents a five to ten-membered saturated, partially unsaturated or...
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7153868 |
N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises...
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7148219 |
Biaryl heterocyclic compounds and methods of making and using the same
The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of...
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7144878 |
Method for treating roundworm infestations in animals
A formulation for treating and preventing roundworm infestations in horses, dogs, cats, and other animals is provided. This formulation includes an agent effective against nematodes, wherein the...
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7141567 |
Polysubstituted imidazopyridines as gastric secretion inhibitors
The invention relates to imidazopyridines of a certain formula 1, in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric...
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7141596 |
Inhibitors of proteins that bind phosphorylated molecules
The present invention provides compounds that can modulate the activity of a target protein, such as a phosphatase, that selectively binds phosphorylated peptides or proteins. The present compounds...
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7135474 |
Derivatives of 2-(1-benzyl-1H-pyrazolo(3,4-B)pyridine-3-yl)-5(-4-pyridinyl)l-4-pyrimidinamines and the use thereof as quanylate cyclase stimulators
This application relates to compounds of the formula (I)
in which R 1 is chlorine, cyano, trifluoromethyl or methoxy and R 2 is hydrogen or flurorine; or R 1 and R 2 are both fluorine;...
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7135472 |
3-Heterocyclic benzylamide derivatives as potassium channel openers
The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A and Het are as defined in the...
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7132413 |
Anticoagulant/sterilizing compositions and methods
Compositions and methods are provided for preventing formation of thrombosis on a liquid-contacting surface of a liquid delivery system, such as a port, catheter or port-catheter system. The liquid...
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7132409 |
Adenosine derivatives and use thereof
2-(6-Cyano-1-hexyn-1-yl)adenosine, 2-(6-cyano-1-hexyn-1-yl)adenosine 5′-monophosphate, or salts thereof; and drugs containing the same as an active ingredient. The compounds have excellent...
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7132420 |
Aspartic protease inhibitors
The present invention provides an aspartic proteinase-inhibiting compound of the formula:
wherein a, b, c, d, and e, can be the same or different and each are R 7 , OR 7 , SR 7 , NR 7 R 8 ,...
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7129242 |
Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto
Compounds having activity as inhibitors of the JNK pathway are disclosed. The compounds of this invention are anilinopyrimidine derivatives having the following structure:
wherein R 1 through...
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7129235 |
Amides useful for treating pain
The present invention relates to compounds of formula (I-VII)
or a pharmaceutically acceptable salt or prodrug thereof, in which A, L, R 6 , R 7 and R 8 are defined herein. The present...
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7125879 |
HIV inhibiting pyrimidines derivatives
This invention concerns HIV replication inhibitors of formula (I) the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms...
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7125865 |
Therapeutic compounds for treating dyslipidemic conditions
The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic...
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7125881 |
Use of pyrimidine—or triazine—2 carbonitiles for treating diseases associated with cysteine prostease activity and novel pyrimidine-2-carbonitile derivatives
The present invention therefore provides use of a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors...
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7122547 |
Anthranilic acid amides and the use thereof as medicaments
The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products...
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7122551 |
Metalloproteinase inhibitor compounds
Compounds of the formula I
useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.
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7119102 |
Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses
Disclosed are compounds of formula (I):
wherein the variables R 1 , R 2 , R 3 and Z are described herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK)...
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7119096 |
Uracil reductase inactivators
Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-flourouracil and find use particularly in the treatment of cancer. The 5-substituent...
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7115597 |
Tyrosine kinase inhibitors
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to...
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7115611 |
Phenyl derivatives, their manufacture and use as pharmaceutical agents
This invention relates to compounds of the formula
wherein one of R 5 , R 6 and R 7 is
and X 1 , X 2 , Y 1 to Y 4 , R 1 to R 13 and m and n are defined in the description,...
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7115613 |
Selected fused pyrrolocarbazoles
The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also...
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7115599 |
Sulfonamide-substituted pyrazolopyridine compounds
This invention relates to compounds of the formula
in which R 1 , R 2 , and R 3 are as defined in the claims, to a process for preparing such compounds, to pharmaceutical compositions...
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7115632 |
Sulfonyl aryl or heteroaryl hydroxamic acid compounds
A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a...
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7112589 |
Cysteine protease inhibitors with 2-cyano-4-amino-pyrimidine structure and cathepsin k inhibitory activity for the treatment of inflammations and other diseases
The invention provides compounds of formula I or a pharmaceutically acceptable salt or ester thereof (I), wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find...
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7109203 |
Sulfonamide derivatives
Sulfonamide derivitives of the formula I wherein R 1 -R 6 are as defined in the description, processes for their production, their use as pharmaceuticals, particularly for use in the treatment or...
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7105523 |
Carbamate-substituted pyrazolopyridine-derivatives
This invention relates to compounds of the formula
wherein R 1 is H or a di-C 1-6 -alkylaminocarbonyl raical, and R 2 is a radical of the formula —O—C(X)—NR 3 R 4 wherein X is O or S....
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7105520 |
Phenylalanine derivatives
Phenylalanine derivatives of the following formulae and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4...
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RE39266 |
Heterocyclic compounds, process for their preparation and pharmaceutical compositions containing them and their use in the treatment of diabetes and related diseases
The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their...
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7101875 |
Methods for treating arthritic disorders
This invention provides methods for treating in mammals arthritic or rheumatic disorders using substituted indole compounds of the general formula:
and pharmaceutically acceptable salt forms...
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7094785 |
Method of treating polycythemia vera
The invention is directed to the use of imatinib mesylate for treating polycythemia vera. Imatinib mesylate is surprisingly effective at controlling the symptoms of polycythemia vera and reducing...
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7091198 |
2,5-disubstituted pyrimidine derivatives
The present invention relates to novel 2,5-disubstituted pyrimidine derivatives which stimulate soluble guanylate cyclase, to processes for the preparation thereof, and to the use thereof for...
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7091206 |
Process for producing pyrimidine derivative and intermediate thereof
The present invention relates to a method for producing a pyrimidine derivate useful as a neurocyte neurocyte necrosis inhibitor and an intermediate thereof. Disclosed is a method for producing an...
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7091202 |
4-arylspirocycloalkyl-2-aminopyrimidine carboxamide KCNQ potassium channel modulators
The invention encompasses compounds of Formula I, which are blockers of KCNQ channels. Blockers of KCNQ channels are known to enchance cognition in laboratory animals. The invention includes,...
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7091210 |
Substituted 2-aminoacetamides and the use thereof
The invention is directed to substituted 2-aminoacetamides represented by formula (II):
and to pharmaceutically acceptable salts thereof, wherein the substituents are defined herein, for use in...
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7091201 |
Arylalkane-sulfonamides having endothelin-antagonist activity
The invention relates to novel aryl-alkane-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including...
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7091204 |
Sulfonamides
The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.
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7087599 |
Estrogen receptor modulators
The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen...
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7087598 |
Diamide invertebrate pest control agents containing a non-aromatic heterocyclic ring
This invention provides compounds of Formula I, their N-oxides and agriculturally suitable salts wherein A and B are independently O or S; J is an optionally substituted 5- or 6-memebered...
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7084144 |
Sulfonyl group containing compounds and their use for the treatment of erectile dysfunction
A compound having the general formula (I):
wherein: X is N or C; R 0 is H, a lower alkyl group, a lower O-alkyl group,
lower alkyl group, a benzyl group, a phenyl group, a heterocyclic...
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7084151 |
5-(1',1'-cycloalkyl/alkenyl)methylidene 1,2-dihydro-5H-chromeno[3,4-ƒ]quinolines as selective progesterone receptor modulator compounds
The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by Progesterone Receptor. Also provided are methods of making such...
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7084145 |
Triazole compounds useful in therapy
The invention provides compounds of formula (I),
the pharmaceutically acceptable salts and solvates thereof, wherein A, B, R 1 , R 2 , and R 7 are as defined herein; pharmaceutical...
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7078400 |
20-HETE synthase inhibitor
The present invention relates to an inhibitor for production of 20-hydroxyeicosatetraenoic acid, comprising, as an effective ingredient, specific hydroxyformamidine derivatives or...
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