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7384940 |
Method of treating cancer using kinase inhibitors
Described herein are methods for treating cancer and other disease conditions in individuals who have either developed a resistance to conventional tyrosine kinase inhibitor (TKI) therapy or who...
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7365066 |
Pyrazolopyridine derivatives as pharmaceutical agents
Novel pyrazolopyridine derivative compounds are disclosed and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors useful in the treatment of...
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7361662 |
Pyridopyrimidinone compounds, method for production thereof and medicaments comprising the same
A compound of formula (I):
wherein:
R 1 , R 2 , R 3 , R 4 are defined in the description, its enantiomers, diastereoisomers, tautomers and also addition salts thereof with a pharmaceutically...
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7358250 |
Pyrrolo[2,3-d]pyrimidines that modulate ACK1 activity
Compounds that modulate the action of ACK1 and LCK, and related compositions methods for treating ACK1- and LCK-mediated diseases are described. In one aspect, the compounds have the general...
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7358249 |
Heterocyclic compounds having inhibitory activity against HIV integrase
A heterocyclic compound of the formula (I):
wherein B 1 is —C(R 2 )═ or —N═; R 1 ′ is H, etc.; one of R 1 and R 2 is -Z 1 -Z 2 -Z 3 -R 5 wherein Z 1 and Z 3 are independently...
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RE40245 |
Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I:
or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase...
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7332493 |
Substituted bicyclic derivatives for the treatment of abnormal cell growth
The invention relates to compounds of the formula 1
and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R 1 , R 3 , R 4 , R 5 , R 11 , m and p are as defined...
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7329659 |
Substituted-1-phthalazinamines as vr-1 antagonists
The present invention provides a compound of formula (I): in which Ar and R 1 are phenyl or a heteroaromatic group, R 2 is generally hydrogen, R 3 is hydrogen or alkyl and X, Y and Z are...
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7323460 |
N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides useful as HIV integrase inhibitors
N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I):
wherein R...
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7317009 |
Pyrrolopyridazine derivatives
The invention relates to compound of the formula (I) or its salt, in which R 1 , R 2 , R 3 and R 4 are as defined in the description, their use of as medicament, the process for their preparation...
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7314873 |
(Halo-benzo carbonyl)heterobi cyclic p38 linase inhibiting agents
Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (I) are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of...
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7312215 |
Benzimidazole C-2 heterocycles as kinase inhibitors
Benzimidazole derivatives having the general formula I
are provided. These compounds are useful as tyrosine kinase inhibitors, especially for the treatment of cancer.
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7304060 |
Indazolyl-substituted pyrroline compounds as kinase inhibitors
The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I):
useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods...
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7294633 |
Oxazolo-and furopyrimidines and their use in medicaments against tumors
The invention relates to pharmaceutically acceptable compounds of formula I, wherein the radicals have the significances given in the description. Compounds of formula I are useful against tumor...
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7294629 |
Quinazoline derivatives
A compound of the formula (I)
or a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, an optically active compound thereof, a racemate thereof or a diastereomer...
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7285557 |
Pyrimidinones as melanin concentrating hormone receptor 1
A compound of formula (Ia) comprising a pharmaceutically acceptable salt or solvate thereof, formulations, processes of preparing, and methods of administering to mammals are provided
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7282499 |
Sigma receptor inhibitors
The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to some pyrazole derivatives, to processes of preparation of such compounds, to...
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7282498 |
Substituted fused pyrroleoximes and fused pyrazoleoximes
Disclosed are compounds of the formula
and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R 1 and R 2 are defined herein. These compounds are highly selective agonists,...
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7262201 |
Quinazoline derivatives
The invention relates to the use of compounds of the formula I:
wherein: ring C is a 5-6 membered heterocyclic moiety; Z is —O—, —S—, or —CH 2 —; R 1 is hydrogen, C 1-4 alkyl, C...
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7226923 |
Phthalazinone derivatives
Compounds of formula I
their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates are disclosed. Also disclosed are methods for the preparation of the...
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7223756 |
Quinazoline compounds with therapeutic use
The invention concerns the use of the quinazoline derivatives of Formula (I) wherein each of m, R 1 , Z, n and R 3 have any of the meanings defined in the description in the manufacture of a...
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7217711 |
Piperazin-1-yl and 2-([1,4]diazepan-1-yl)-imidazo[4,5-d]-pyridazin-4-ones, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted imidazo[4,5-d]pyridazin-4-ones of general formula
wherein R 1 to R 3 and n are defined as in claims 1 to 8 , the tautomers, enantiomers,...
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7214676 |
Spirotricyclic derivatives and their use as phosphodiesterase-7 inhibitors
The invention provides compounds which are PDE7 inhibitors, having the following formula (I), (II) and (III)
in which X 1 , X 2 , X 3 , X 4 , X, Y, Z, A and Z 1 are as defined in the...
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7196090 |
Kinase inhibitors
This invention provides phenyl-substituted pyrimidopyrimidines, dihydropyrimido-pyrimidines, pyridopyrimidines, naphthyridines, and pyridopyrazines of the general formula:
that inhibit...
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7192949 |
Substituted bicyclic pyrimidinones as a mitotic kinesin KSP inhibitors
The present invention relates to cycloalkylpyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for...
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7186710 |
Phthalazinones
The compounds of formula I
in which R1, R2, R3, R4 and R5 have the meanings as given in the description are PDE4/7 inhibitors.
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7169778 |
Pteridinones as kinase inhibitors
Disclosed are compounds of Formulae (Ia), (Ib), (Ic), (Id) wherein: W is NH, S, SO, or SO 2 ; R 2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle;...
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7163948 |
Heterocyclic substituted 1,4-dihydri-4ox9-1,8-naphthyridine analogs
The present invention relates to 1,4-dihydro-4-oxo-1,8-napthpyridine analogs of the formula
and pharmaceutically acceptable salts, esters, and prodrugs thereof, wherein A, X, W and Y are...
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7138420 |
Substituted benzimidazole compounds
Disclosed are substituted benzimidazole compounds of formula (I):
wherein R 1 , R 2 , R 3 , R 4 and X a are defined herein. The compounds of the invention inhibit Itk kinase and are therefore...
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7138398 |
Substituted 4-amino-2-arylcyclopenta[d]pyrimidines, their preparation, their use and pharmaceutical preparations comprising them
The present invention relates to compounds of formula (I) wherein R 1 , R 2 and R 3 have the meanings given in the claims. Said compounds are valuable active agents in medicaments for the...
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7132438 |
Benzimidazole derivatives
Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related conditions or disorders. In particular, the invention provides...
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7115644 |
Heterocyclic compounds
Disclosed are benzimidazolone compounds of formulas (I) & (II): wherein R 1 , R 2 , R 3 , R 4 , R 5 , X, L, m, n and t are defined herein. The compounds inhibit production of cytokines...
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7115615 |
Quinazoline derivatives
The invention concerns quinazoline derivatives of Formula (I)
wherein each of m, R 1 , n, R 2 and R 3 have any of the meanings defined in the description; processes for their preparation,...
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7112600 |
Fused-ring compounds and use thereof as drugs
The present invention provides a fused ring compound of the following formula [I]
wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a...
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7101879 |
Treatments for neurotoxicity in Alzheimer's Disease
The invention involves identification of a mechanism of β-amyloid peptide cytotoxicity, which enables treatment of conditions caused by β-amyloid peptide aggregates by administration of compounds...
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RE39265 |
Heteroarylpiperidines, and their use as antipsychotics and analgetics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a...
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7094780 |
3-aminoquinazolin-2,4-dione antibacterial agents
Antibacterial 3-aminoquinazolin-2,4-diones have formula (I) wherein: R 1 and R 3 include alkyl, alkenyl, cycloalkyl, aryl, hetero-cyclic, and heteroaryl; R 5 , R 6 , and R 8 include H, alkyl,...
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7091219 |
Bis-sulfonamide hydroxyethyl-amino retroviral protease inhibitors
Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease...
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7091207 |
Method of treating myocardial infarction with PDE-5 inhibitors
A method is provided for the prevention of ischemia/reperfusion injury, for example, in patients undergoing heart surgery, and involves the administration of a phosphodiesterase-5 (PDE-5) inhibitor...
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7087602 |
Cinnoline derivatives and use as medicine
The invention relates to the use of cinnoline derivatives of formula (I)
wherein Z represents —O—, —NH—, —S— or —CH 2 —; m is an integer from 1 to 5; R 1 represents hydrogen,...
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7081461 |
Quinazoline compounds and pharmaceutical compositions containing them
The use of a compound of formula (I)
or a salt, ester or amide thereof;
where X is O, or S, S(O) or S(O) 2 , NH or NR 8 where R 8 is hydrogen or C 1-6 alkyl;
R a is a 3-quinoline group...
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7071182 |
Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or...
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7064123 |
Compounds and compositions as cathepsin inhibitors
The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
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7064119 |
Fused bicyclic pyrimidine derivatives
A novel fused bicyclic pyrimidine derivative or a salt thereof that acts as a tachykinin receptor antagonist and, in particular, as an NK1 receptor antagonist is represented by the following...
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7056918 |
Benzimidazole anti-inflammatory compounds
The present invention relates to novel triazolo-pyridines of the formula I
wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from...
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7049307 |
Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or...
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7030150 |
Benzimidazole compounds and antiviral uses thereof
The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion...
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7030113 |
Aminobenzimidazoles as selective melanin concentrating hormone receptor antagonists for the treatment of obesity and related disorders
The present invention discloses compounds of formula I
wherein Ar, Z, m, n, p, R 1 and R 8 are herein defined, said compounds being novel antagonists for melanin-concentrating hormone (MCH),...
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7001904 |
Guanidine derivatives quinazoline and quinoline for use in the treatment of autoimmune diseases
The invention concerns quinazoline and quinoline derivatives of Formula (I) wherein Q 1 includes a quinazoline or quinoline ring optionally substituted with a group such as halogeno,...
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6998391 |
Method for treating diseases associated with abnormal kinase activity
Methods are provided for treating diseases associated with abnormal activity of kinases. The method comprises: administering a DNA methylation inhibitor to the patient in therapeutically effective...
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