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7615549 |
Substituted pyrrolidinones, their manufacture and their use as medicaments
The present invention relates to new substituted pyrrolidinones of general formula
wherein A, X, B and R 1 to R 9 are as defined above, or a tautomer or salt thereof, particularly the...
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7612060 |
Triazoles and methods of use
Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically...
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7605154 |
Substituted Thiazolo [4,5-d]pyrimidines as protein kinase inhibitors
The present invention is directed to novel thiazolopyrimidine compounds of Formula (I) or a form or composition thereof
and the use thereof as inhibitors of ATP-protein kinase interactions.
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7598237 |
7-aryl 1,5-dihydro-4,1-benzoxazepin-2(3H)-one derivatives and their use as progesterone receptor modulators
This invention provides progesterone receptor modulators having the structure:
wherein R 1 to R 7 , X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.
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7595312 |
Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions
The present invention relates to CGRP antagonists of general formula
wherein A, U, V, W, X and R 1 to R 3 are defined as in claim 1,
the tautomers, diastereomers, enantiomers, hydrates,...
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7589121 |
Use of furan alkyls for preparing a drug for treating obesity and cosmetically treating overweight
The invention relates to the use of one or several synthetic or natural furan alkyls for preparing a drug preventing and/or treating obesity or overweight. The use of one or several synthetic or...
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7589086 |
Substituted pyrazolo[3,4-D]pyrimidines as anti-tumor agents
The present invention provides a compound of pyrazolo[3,4-d]pyrimidine having the formula
wherein:
X=N; R=H, alkylthio, or aminoalkylthio; R 1 =NHcyclopropyl, NHC 3 H 7 , NHC 4 H 9 , N(CH 2 CH...
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7589085 |
Tetrahydropyran heterocyclic cyclopentyl heteroaryl modulators of chemokine receptor activity
The present invention is further directed to compounds of the formulas: (I) (II) (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 15 , R 16 , R 17 , R 18 , R 19 , R 24 and R...
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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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7572785 |
Substituted imidazoles as cannabinoid receptor modulators
The use of compounds of the present invention as antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor particularly in the treatment, prevention and suppression of diseases...
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7569604 |
Heterocyclic derivatives for modulation of calcium channels
Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.
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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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7566707 |
Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula
wherein Y and R 1 to R 4 are defined as in claim 1 , the tautomers, enantiomers,...
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7560481 |
Indoles are cannabinoid receptor ligands
The present invention provides novel compounds of Formula (I)
which are CB 2 selective ligands useful for the treatment of pain.
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7560453 |
6-(2, 3, 4, 5-tetrahydro-1H-benzo [D] azepin-7-yloxy) -nicotamide derivatives as radio labelled ligands
The present invention relates to radiolabelled compounds of formula (I), which are useful for the labelling and diagnostic imaging of histamine H 3 receptor functionality.
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7560452 |
Benzazepine derivatives for the treatment of neurological disorders
The present invention relates to benzazepine derivatives of formula (I) wherein: R 1 represents —C 3-7 cycloalkyl optionally substituted by C 1-3 alkyl; having pharmacological activity,...
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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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7544677 |
Inhibitors of Akt activity
The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further...
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7544675 |
Chemical compounds with dual activity, processes for their preparation and pharmaceutical compositions
The present invention concerns chemical compounds combining affinity and antagonism against the human m3 muscarinic receptor with activity as selective phosphodiesterase IV (PDE IV) inhibitors,...
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7524838 |
Pyrazolyl derivatives, preparation process and intermediates of this process as medicinal products and pharmaceutical compositions containing them
The present invention relates to the novel derivatives of formula (I) in which
A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7)...
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7514425 |
Short-acting sedative hypnotic agents for anesthesia and sedation
The invention provides compounds compositions and methods useful for inducing or maintaining general anesthesia or sedation in mammals.
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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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7514422 |
5HT2c receptor modulators
The present invention relates to novel compounds of Formula (I):
which act as 5HT 2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the...
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7504394 |
Bazedoxifene ascorbate
The present invention is directed to bazedoxifene ascorbate, compositions containing the same, dispersions thereof, preparations thereof, and uses thereof.
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7504392 |
2,3,4,5-tetrahydro-1H-3-benzazepines and their medical use
The invention provides compounds of the formula
or a pharmaceutically acceptable salts thereof. The compounds are useful in therapy, in particular as antipsychotic agents.
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7504391 |
Selective D1/D5 receptor antagonists for the treatment of obesity and CNS disorders
The present invention provides compounds, which, are novel antagonists for D 1 /D 5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides...
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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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7498334 |
Pyrrolopyrimidines as phosphodiesterase VII inhibitors
Pyrrolopyrimidine derivatives of the formula I
in which R 3 , R 4 , R 5 , R 6 and X are as defined in claim 1 , act as phosphodiesterase VII inhibitors and can be employed for the treatment...
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7494990 |
2-(piperidin-4-yl)-4,5-dihydro-2H-pyridazin-3-one derivatives as PDE4 inhibitors
The compounds of a certain formula (1),
in which R1, R2, R3 and R9 have the meanings as given in the description, are novel effective PDE4 inhibitors.
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7494989 |
Pyridine compounds useful as N-type calcium channel antagonists
Achiral pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when...
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7476663 |
Substituted thiophene carboxamides
The present invention relates to new substituted thiophene-2-carboxylic acid amides of general formula
wherein A, and R 1 to R 8c are defined as in claim 1, the tautomers, the enantiomers,...
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7468363 |
Methods for treatment of cancers using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione
Methods of treating a specific cancer or amyloidosis are disclosed. Specific methods encompass the administration of 3-(4-amino-1 oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione alone or in...
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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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7465723 |
Use of carboxamides for the treatment of tinnitus
The present invention relates to the use of carbamazepine derivatives in treating tinnitus.
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7462717 |
C6-and C9-substituted chromeno[4,3-c]isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and...
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7456195 |
Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants
The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV):
or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein...
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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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7446103 |
Bicyclic benzamide compound as histamine H3 receptor ligand useful in the treatment of neurological diseases
The present invention relates to novel bicyclic benzamide derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the...
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7435833 |
Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme
A compound of formula (I):
or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Methods of inhibiting 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme....
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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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7432255 |
1H-indol-5-yl-piperazin-1-yl-methanone derivatives
The present invention relates to compounds of formula I and their pharmaceutically acceptable salts wherein in formula I is:
wherein R 1 to R 4 are as defined in the description and claims....
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7429607 |
5-HT2B receptor antagonists
The present invention relates to compounds of formula I:
wherein one of R 1 and R 4 is selected from the group consisting of H, and optionally substituted C 1-6 alkyl, C 3-7 cycloalkyl, C...
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7429579 |
Tetrahydrobenzazepine derivatives useful as modulators of dopamine D3 receptors (antipsychotic agents)
The invention provides compounds of formula (I): wherein: R 2 and R 3 independently represent various substituents; R 1 and R 4 independently represent H, F, Cl, Br, C 1-2 alkyl, C 1 alkoxy,...
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7427612 |
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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7423030 |
1-amino-phthalazine derivatives, the preparation and the therapeutic use thereof
A 1-amino-phthalazine derivative of general formula (I)
wherein the substituents are as defined herein. Also disclosed are a method for preparing such compounds, intermediates for use in such...
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7414048 |
4,5-dihydro-isoxazole derivatives and their pharmaceutical use
The present invention is concerned with the compounds of formula
wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; -A 1 =A 2 -A 3 =A 4 - is a pyridinylidene,...
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7414047 |
Piperazinyl and diazapanyl benzamides and benzthioamides
Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
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7407950 |
N-(heteroaryl)-1H-indole-2-carboxamide derivatives and their use as vanilloid TRPV1 receptor ligands
The invention concerns compounds of general formula (I), wherein n, X 1 , X 2 , X 3 , X 4 , Z 1 , Z 2 , Z 3 , Z 4 , Z 5 and W are as defined herein.
Said compounds are ligands of the TRPV 1 ...
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7407949 |
Benzamide derivatives as oxytocin agonists and vasopressin antagonists
Novel compounds according to general formula 1, wherein G 1 is NR 5 R 6 or a fused polycyclic group that are specific OT receptor agonists and/or V 1a receptor antagonists. Pharmaceutical...
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