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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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7585866 |
Protein tyrosine kinase inhibitors
The present invention relates to compounds of the Formula I, the pharmaceutically acceptable salts and stereoisomers thereof, which inhibit, regulate and/or modulate tyrosine kinase signal...
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7582641 |
Gyrase inhibitors and uses thereof
The present invention relates to methods of treating, preventing, or lessening the severity of resistant bacterial infections in mammals, utilizing compounds of formula I or formula VII or...
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7579349 |
4-(pyrazol-3-ylamino) pyrimidine derivatives for use in the treatment of cancer
A compound of Formula (I); wherein the substituents are as defined in the text for use in modulating insulin-like growth factor 1 receptor activity in a warm blooded animal such as man.
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7572793 |
3-Substituted-4-pyrimidone derivatives
A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1:
wherein R 1 represents...
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7528157 |
EP4 receptor antagonists
Compounds of formula (I):
wherein: R 2 is H or an optionally substituted C 1-4 alkyl group; Y is either —(CH 2 ) n —X—, where n is 1 or 2 and X is O, S, S(═O), S(═O) 2 , or NR N1 ,...
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7504502 |
Guanidinopyrimidinone compounds and phase change inks containing same
Compounds of the formula
wherein, provided that at least one of R 1 , R 2 , and R 3 is not hydrogen, R 1 , R 2 , and R 3 each, independently of the other, is hydrogen, alkyl, aryl, arylalkyl,...
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7501415 |
Selective inhibitors of ERK protein kinase and uses thereof
Described herein are compounds that are useful as ERK2 inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a...
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7470686 |
Method of inhibiting the expression and/or the activity of JNK
The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said...
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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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7442699 |
Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure:
wherein R 1 ...
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7329749 |
Piperazinylcarbonylquinolines and -isoquinolines
Compound of the formula (I) in which R 1 , R 2 and alk are as defined in Claim 1, are potent 5-HT 2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression,...
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7326793 |
Process for the preparation of diketopyrrolopyrroles
The present invention relates to a process for the preparation of diketopyrrolopyrroles of the formula (I), wherein A1, A2, A3 and A4 are as defined in the description of the present invention, to...
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7323465 |
Alkansulfonamides as endothelin antagonists
The invention relates to novel alkansulfonamides of structure (I), wherein R 1 is a lowel alzyl group and the other variables are as defined in the description, and their use as active ingredients...
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7285663 |
β-Isoindigo coloring agent
The invention relates to a compound of general formula (I) in which C represents an alicyclic or heterocyclic group having C 2v symmetry, and B represents ortho-C 6 -C 18 -arylene. The invention...
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7285560 |
Indole derivatives or benzimidazole derivatives for modulating IκB kinase
The present invention relates to indole derivatives or benzimidazole derivatives, to processes for preparing such compounds, to pharmaceutical compositions comprising such compounds, and methods...
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7285549 |
Sulfamides and their use as endothelin receptor antagonists
The invention relates to novel sulfamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for...
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7259162 |
Benzazole derivatives and their use as JNK modulators
The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said...
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7232904 |
Crystal of arylethenesulfonamide derivative and preparation process thereof
Novel crystals of a potassium salt of (E)-N-[6-methoxy-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl)pyri
midin-4-yl]-2-phenylethenesulfonamide, a preparation process thereof, and novel solvates of...
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7226919 |
Compositions useful as inhibitors of protein kinases
The present invention provides a compound of formula (I):
or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of...
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7220736 |
Pyrimidine compounds
A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof,
wherein X is ═CH— or ═N—, Y is —NH—, —NR 4 —, —S—, —O—, —CH═N—,...
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7196089 |
EP4 receptor antagonists
Compounds of formula (I):
wherein: R 2 is H or an optionally substituted C 1-4 alkyl group; Y is either —(CH 2 ) n —X—, where n is 1 or 2 and X is O, S, S(═O), S(═O) 2 , or NR N1 ,...
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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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7122551 |
Metalloproteinase inhibitor compounds
Compounds of the formula I
useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.
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7122544 |
Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure:
wherein R 1 ...
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7115616 |
Pyrimidinone compounds
Pyrimidinone compounds of formula (10 are inhibitors of the enzyme Lp-PLA 2 and of use in therapy, in particular for treating atherosclerosis.
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7112674 |
Organic electroluminescent device based on 2,5-diaminoterephthalic acid derivatives
The invention relates to an organic electroluminescent device which contains 2,5-diaminoterephthalic acid derivatives of formula 1a as emitter substances in one or several emitter layers in a pure...
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7112585 |
Pyrimidine derivatives as corticotropin releasing factor inhibitors
The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF...
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7101873 |
Pyrimidinedione derivatives
Pyrimidinedione derivatives of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and...
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7094781 |
Sulfamides and their use as endothelin receptor antagonists
The invention relates to novel sulfamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for...
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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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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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7045519 |
Inhibitors of glycogen synthase kinase 3
New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are...
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6995148 |
Adenosine cyclic ketals: novel adenosine analogues for pharmacotherapy
The present invention relates to novel compounds that are novel adenosine receptor analogues. Specifically, the compounds of the present invention preferably function as both adenosine receptor...
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6992044 |
Substituted phenyluracils
The invention relates to novel substituted phenyl uracils of the formula (I)
in which
R 1 represents hydrogen, amino or in each case optionally substituted alkyl, alkenyl or alkynyl, R 2 ...
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6953803 |
Pyrimidine compounds
Pyrmidinone compounds of formula (I)
are inhibitors of the enzyme Lp-PLA 2 and of use in therapy, in particular for treating atherosclerosis.
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6951856 |
Arylethene-sulfonamides
The invention relates to novel aryl-ethene-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including...
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6949567 |
Compounds for the treatment of protozoal diseases
The invention relates to new diphenylurea having the formula (I)
or a salt thereof, where
Y is C═O, C═S, C═NH, (C═O) 2 or SO 2 ; and to processes for the preparation of these...
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6949544 |
Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
The present invention provide a compound of formula I or II:
or a pharmaceutically acceptable derivative thereof, wherein R 1 , R 2 , R 3 , and R 4 are as described in the specification....
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6936607 |
2,4,6-Triaminopyrimidines for the treatment of depression and/or anxiety
This invention is directed to pyrimidine derivatives which are selective antagonists for the GalR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically...
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6919332 |
N-substituted-heteroaryloxy-aryloxy-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula
wherein X, A, Y, B, G, and R 1 are as defined in the...
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6916804 |
Pyrimidine A2b selective antagonist compounds, their synthesis and use
The subject invention provides compounds having the structure:
wherein R 1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5...
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6887875 |
2,5-diarypyrimidine compounds
Diarylpyrimidine compounds of Formula I are provided, wherein.
or a pharmaceutically acceptable salt thereof, wherein:
Ar 1 and Ar 2 are independently chosen from:
phenyl...
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6861417 |
Pyridin-4-YL or pyrimidin-4-YL substituted pyrazines
Novel pyridin-4-yl or pyrimidin-4-yl substituted pyrazine compounds and compositions for use in therapy.
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6849622 |
Aliphatic nitrogenous five-membered ring compounds
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]:
wherein
A represents —CH 2 — or —S—, R 1 ...
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6838461 |
N-(indolcarbonyl-)piperazine derivatives
Compounds of the formula I
in which R 1 , R 2 , R 4 and R 5 have the meanings indicated in claim 1 , are potent 5-HT 2A antagonists and are suitable for the treatment of psychoses,...
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6833364 |
Substituted pyrazole derivatives
The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which the substituents R 1 , R 2 , R 3 , A, X and Y are each as defined, and to processes...
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6821971 |
Fused pyrazolone compounds which inhibit the release of inflammatory cytokines
The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms...
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6794386 |
β-amino acid compounds as integrin antagonists
The present invention relates to a compound of the general formula (I), wherein R 1 together with the C atom to which it is attached, and R 2 together with the N atom to which it is attached,...
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6787546 |
Heterocycle derivatives and drugs
The object of the invention is to provide an excellent compound as a drug. The invention relates to a heterocyclic compound shown by the following formula: A—B—D—E [ 1] wherein A is...
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