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7625889 |
Substituted bis aryl and heteroaryl compounds as selective 5HT2A antagonists
The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I):
Wherein X, Y, Z, A, B, D, Ar, R 1 and R 2 are as defined herein. The compounds of...
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7615554 |
Erastin and erastin binding proteins, and uses thereof
The invention relates to methods of screening for binding partners, especially binding partners essential for the biological activity of erastin (e.g. VDACs such as VDAC3). The invention also...
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7612200 |
Inhibitors of protein kinases
The present invention is directed to a compound having the formula
wherein R 1 , R 2 , R 3 , R 4 , G, and Q are defined herein. The compounds of the present invention are useful as inhibitors...
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7612061 |
Piperazine compounds
A compound selected from those of formula (I):
wherein:
R 1 , R 2 , R 3 and R 4 , which may be the same or different, each represent an atom or group selected from hydrogen, halogen,...
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7605155 |
Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), methods of preparing such compounds,...
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7601713 |
Kinase inhibitors and their uses
The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein...
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7601711 |
5-amido-indole-2-carboxamide derivatives
The present invention relates to compounds of formula I
wherein G and R 1 to R 5 and R 12 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The...
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7597926 |
Electroluminescent quinolates
Lithium quinolate is an electroluminescent material which emits light in the blue region of the spectrum.
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7595314 |
Benzoyl-piperazine derivatives
A compound of formula
wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia,...
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7589087 |
Benzoimidazol-2-yl pyridines as modulators of the histamine H4receptor
Benzoimidazol-2-yl pyridines, pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H 4 receptor activity, including allergy, asthma,...
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7576088 |
Benzodioxole derivatives
The present invention relates to compounds of the general formula
and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases such...
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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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7572787 |
Substituted naphthalene sulfonamides
The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful...
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7572786 |
Substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives and their use as neurokinin antagonists
This invention concerns substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity, a combined NK 1 /NK...
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7569574 |
Purine derivatives, the preparation thereof and their use as pharmaceutical compositions
The invention relates to new purine derivatives of general formula
wherein R 1 to R 4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and...
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7569563 |
Substituted quinolones II
The invention relates to substituted quinolones of formula (I) and to methods for their preparation as well as their use for the production of medicaments for the treatment and/or prophylaxis of...
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7560547 |
Hydroxyalkyl cyclic diamine compounds
The present invention is directed to a process for producing a compound (5) from the compound (1).
By use of the compound (1), a variety of cyclic diamine derivatives (5) or salts thereof,...
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7560450 |
Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted xanthines of general formula
the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable...
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7557112 |
Aromatic-ring-fused pyrimidine derivative
There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a...
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7557098 |
1-aryl- or 1-alkylsulfonyl-heterocyclylbenzazoles as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
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7550469 |
Heterocyclic amide derivatives and their use as dopamine D3 receptor ligands
The invention relates to heterocyclic substituted amide derivatives that display selective binding to dopamine D 3 receptors. In another aspect, the invention relates to a method for treating...
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7550456 |
Substituted aryl cycloalkanoyl derivatives and methods of their use
The present invention is directed to substituted aryl cycloalkanoyl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions...
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7550455 |
8-(piperazin-1yl)- and 8-([1,4]diazepan-1yl)-xanthines, the preparation thereof and their use as pharmaceutical composition
The present invention relates to substituted xanthines of the general formula
in which R 1 to R 3 and n are as defined in claims 1 to 8, their tautomers, their enantiomers, their...
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7547691 |
[4-(Benzo[B]thiophen-2-yl) Pyrimidin-2-yl]-amine derivatives as IKK-beta inhibitors for the treatment of cancer and inflammatory diseases
The present invention provides compounds of Formula I: useful in the treatment of cancer and inflammatory diseases.
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7538114 |
Glycine transporter-1 inhibitors
The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition...
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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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7524839 |
Compounds, their use and preparation
The invention-provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I):
in which Ar, R 2 , R 3 , R 4 and R 5 are as defined in...
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7514436 |
Pyridazine derivatives and their use as therapeutic agents
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula...
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7514424 |
Substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives and their use as neurokinin antagonists
The invention concerns substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives having neurokinin antagonistic activity, in particular NK˜antagonistic activity, their preparation,...
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7501407 |
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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7479559 |
Benzyl(idene)-lactam derivatives
The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula I
wherein R 1 is a group of the formula G 1 or G 2 depicted below,
wherein R 1 , R 3 , R...
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7465733 |
Piperazine compounds
A compound selected from those of formula (I):
wherein:
R 1 , R 2 , R 3 and R 4 , which may be the same or different, each represent an atom or group selected from hydrogen, halogen,...
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7465726 |
Substituted pyrrolo[2.3-B]pyridines
Compounds represented by Formula (I):
or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3,...
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7456168 |
2-(pyridin-2-ylamino)-pyrido[2,3, d]pyrimidin-7-ones
The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent...
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7449477 |
7-phenyl-isoquinoline-5-sulfonylamino derivatives as inhibitors of akt (protein kinase B)
The present invention relates to compounds Formula (I) as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.
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7449456 |
Diaminopyrimidinecarboxamide derivative
A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is...
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7442791 |
Aminoalkylamide substituted cyclohexyl derivatives
The present invention relates to compounds of formula I
wherein R 1 , R 2 , R 3 , R 4 , R 5 , U, V, W, k and m are as defined in the description and claims, and pharmaceutically acceptable...
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7442692 |
Indanyl-piperazine compounds
A compound selected from those of formula (I):
wherein:
R 3 represents a hydrogen atom, and R 1 and R 2 together with the carbon atoms carrying them form a benzene, naphthalene or...
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7439245 |
Compounds
Disclosed is a method for use of phenyl sulfone compounds of formula (I) in the treatment of anxiety.
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7439244 |
Quinoline compounds and pharmeceutical compositions containing them
Disclosed are quinoline compounds of formula (I) having pharmacological activity, processes for their preparation, compositions containing them, and methods for the treatment of CNS and other...
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7439243 |
Piperazinyl-quinoline derivatives useful for the treatment of CNS disorders
Disclosed are quinoline compounds of formula (I) having pharmacological activity, processes for their preparation, compositions containing them, and methods for the treatment of CNS and other...
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7429659 |
Furan compounds as histamine H3 modulators
Certain furan compounds are histamine H 3 modulators useful in the treatment of histamine H 3 receptor mediated diseases.
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7423048 |
Compounds for treating fundic disaccomodation
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -a...
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7407971 |
Substituted pyrrolo-pyrazole derivatives as kinase inhibitors
A new class of pyrazolo derivative compounds having the formula
where R and R 1 have the meanings given herein. The pyrazolo derivative compounds are useful in treating cell proliferative...
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7393845 |
Heteroaryl derivates, their preparation and use
A heteroaryl derivative having the formula (I). The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder,...
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7378413 |
2-amino-3-(alkyl)-pyrimidone derivatives
A pyrimidone derivative represented by formula (I) or a salt thereof:
Wherein:
R1 represents a hydrogen atom or a C 1-6 alkyl group which may be substituted by a C 6,10 aryl group; R2...
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7378411 |
Substituted thienopyrimidinones as a mitotic kinesin inhibitor
The present invention relates to thienopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for...
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7371753 |
Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
Disclosed are new dihydropteridinones of general formula (I)
wherein the groups R 1 to R 5 , R a to R c , W, Q 1 and Q 2 have the meanings given in the claims and specification, the isomers...
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7358239 |
Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z...
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7351700 |
Aminomethylpyrimidines as allosteric enhancers of the GABAB receptors
The present invention relates to compounds of formula
wherein
X is —S— or —NH—; R 3 /R 4 together with the N-atom to which they are attached form a non aromatic 5, 6 or 7...
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