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7595324 |
Substituted thieno[3,2-D]pyrimidines as HIV inhibitors
This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I
where the dashed line represents a double bond that may be located either between A and C(V)...
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7511048 |
Pyrimidothienoindazoles
The invention relates to novel pyrimidothienoindazoles of formula (I)
processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders,...
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7511041 |
Fused azole-pyrimidine derivatives
The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the...
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7498332 |
Therapy for cerebral vasospasm
The present invention relates to a method of treating or preventing cerebral vasospasm that accompanies sub-arachnoid hemorrhage.
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7498323 |
Spiro-piperidine compounds and medicinal use thereof
The present invention relates to a spiro-piperidine compound represented by formula (I):
wherein R 1 represents hydrogen, an aliphatic hydrocarbon group which may have a substituent(s) or a...
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7495104 |
Quinoline or quinazoline derivatives inhibiting auto-phosphorylation of fibroblast growth factor receptors
An objective of the present invention is to provide novel compounds which have inhibitory activity against autophosphorylation of an FGF receptor family and, when orally or intraveneously...
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7476676 |
Methods for increasing bone formation using inhibitors of glycogen synthase kinase-3β
This invention relates to the use of inhibitors of glycogen synthase kinase-3β to increase bone formation.
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7470690 |
4-(2-Fluorophenyl)-6-methyl-2-(1-piperazinyl)thieno[2,3-D)pyrimidine in the treatment of functional bowel disorder
Use of 4-(2-Fluorophenyl)-6-Methyl-2-(1-Piperazinyl)Thieno[2,3-D]Py
rimidine or a salt thereof for the manufacture of a medicament for the treatment of functional bowel disorder.
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7456185 |
Substituted quinazoline compounds useful as p38 kinase inhibitors
Compounds having the formula (I),
are useful as p38 kinase inhibitors, wherein R 4 and R 5 are hydrogen, halogen, cyano, haloalkyl, or haloalkoxy, but are not both hydrogen; R 6 and R 7 are...
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7439249 |
Inhibitors of phosphatases
The present invention relates to compounds that inhibit phosphatases, compositions thereof, and methods of using those compounds and compositions for treating diseases.
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7427616 |
Condensed pyridines and pyrimidines with tie2 (TEK) activity
A compound of the Formula (I), wherein A together with the carbon atoms to which it is attached forms a fused 5-membered heteroaryl ring, wherein said heteroaryl ring contains 1 or 2 heteroatoms...
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RE40332 |
Fungicidal trifluoromethylalkylamino-triazolopyrimidines
The novel compounds of formula I:
wherein (R 1 , R 2 , Hal and L 1 through L 5 are defined in the specification) show selective fungicidal activity. The new compounds may be processed with...
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7312225 |
Macrocyclic pyrimidines, their production and use as pharmaceutical agents
Macrocyclic pyrimidine derivatives of general formula I
in which R 1 to R 5 , X, Y, A, B, m and n have the meanings that are contained in the description, as inhibitors of the cyclin-dependent...
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7273871 |
Phenyl-5,6,6A,7,8,9-hexahydro-4H-1,4,9-triaza-phenalene derivatives as CRF antagonists
The present invention relates to tricyclic pyridines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof:
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7259167 |
Antimalarial and antiproliferative pharmacophore models, novel tryptanthrin compounds having increased solubility, and methods of making and using thereof
Disclosed herein is a pharmacophore model for antimalarial activity and methods of making and using thereof. The pharmacophore comprises two hydrogen bond acceptor (lipid) functions and two...
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7217717 |
Phenalene derivatives
Novel 1,3,4-triaza-phenalene and 1,3,4,6-tetraazaphenalene derivatives are disclosed. These compounds inhibit epidermal growth factor receptor (“EGFR”) tyrosine kinase. These compounds and...
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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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7144887 |
Substituted 1,2,3-triazolo[1,5-a]quinazolines for enhancing cognition
The present invention provides a compound of formula (I) in which R 1 is generally hydrogen or CF 3 , R 2 is generally hydrogen, W is a cyclic amine, a heterocycle or a group L-Y—X where L-Y is...
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7109195 |
Hexacyclic compounds and their therapeutic use
The present invention relates to hexacyclic compound of the formula [1],
wherein Z, R 3 and R 4 are as identified therein, and pharmaceutically acceptable salts thereof. These compounds are...
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7067519 |
7,8,9,10-tetrahydro-6H-azepino, 6,7,8,9-tetrahydro-pyrido and 2,3-dihydro-2H-pyrrolo[2,1-b]-quinazolinone derivatives
The invention relates to novel 7,8,9,10-tetrahydro-6H-azepino, 6,7,8,9-tetrahydro-pyrido and 2,3-dihydro-2H-pyrrolo[2,1-b]-quinazolinone derivatives and their use as active ingredients in the...
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6995163 |
Tricyclic fused heterocyclic compound, process for preparing it and medicament comprising it
The present invention provides a novel compound having an excellent corticotrophin-releasing-factor receptor antagonistic activity. That is, it provides a compound represented by the following...
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6969719 |
Polycyclic guanine phosphodiesterase V inhibitors
A polycyclic guanine phosphodiesterase V inhibitor having the formula (I.1) or (II.1), with the variables defined herein, which is useful for treating sexual dysfunction and other physiological...
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6967203 |
Use of pyridoindolone derivatives for preparing anticancer medicines
The invention relates to a novel use of compounds of formula:
for the preparation of medicinal products that are useful as anticancer agents.
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6964960 |
Indoloquinazolinones
The invention provides compounds of formula (I) wherein R is as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals, for use in the...
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6960585 |
Amino-substituted tetracyclic compounds useful as anti-inflammatory agents and pharmaceutical compositions comprising same
Compounds of formula (I), or pharmaceutically-acceptable salts thereof, are useful in treating inflammatory and immune diseases and disorders,
wherein X, Y 1 , Y 2 , and R 2- 4 are as...
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6946472 |
Polycyclic compounds exhibiting anti-tumor activities
This invention is concerned with novel polycyclic compounds of formula [I],
wherein ring A, ring B, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X, Y, R 1′ , R 2′ , R 3′ , R 4′ , R 5′ , R 6...
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6943171 |
Polycyclic guanine derivative phosphodiesterase V inhibitors
A compound having the formula (Ia) or (b), salt or solvate thereof, with the variables as defined herein, which can inhibit selectively phosphodiesterase V and can be useful for treating sexual...
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6916811 |
Adenosine A2a receptor antagonists
Disclosed herein are compounds having the structural formula A
including pharmaceutically acceptable salts or solvates of said compound, wherein X, Y, Q and R are as defined in the...
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6894055 |
Thieno-2′,3′ -5,6pyrimido[3,4-A]-1,2,4-triazole derivatives as modulators of phoshoinositide 3-kinase
Compounds of formula 1 are effective modulators of PI3 kinase:
wherein X is CR 9 R 10 , O, NR 11 (where R 9 and R 10 are each independently H, lower alkyl, lower alkoxy, or halo, and R...
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6878701 |
Potassium channel blocking agents
Compounds of Formula I:
wherein A and B are linking groups; R 1 , R 2 , R 3 and R 4 are defined moieties. An exemplary compound is:
These compounds function as potassium channel...
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6831074 |
Pharmaceutically active compounds
The present invention provides a compound of formula (I): where Q is a group of formula: These compounds inhibit cyclic guanosine 3′,5′-monophosphate phosphodiesterases (cGMP PDEs). More...
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6825194 |
Hexacyclic compounds
The present invention relates to hexacyclic compound of the formula [1], wherein Z, R 3 and R 4 are as identified therein, and pharmaceutically acceptable salts thereof. These compounds are...
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6825184 |
1,4-Disubstituted benzo-fused urea compounds
Disclosed are compounds of the formulas (I) & (II) shown below which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds. wherein G, X, A and Q...
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6809090 |
Derivatives of N-(iminomethy)amines, their preparation, their use as medicaments and the pharmaceutical compositions containing them
N-(imino)amines and their preparation and their use as NO synthase inhibitors and selective or non-selective traps for a reactive oxygen species.
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6797694 |
Chemical compounds having ion channel blocking activity for the treatment of immune dysfunction
The present invention relates to chemical compounds having inhibitory activity on an intermediate conductance Ca 2+ activated potassium channel (IK Ca ), and the use of such compounds for the...
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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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6787128 |
Structure-improving hair care agents
There are provided topical hair care compositions for improving the structure and strength of hair keratin and the fastness to washing of hair colors which contain vitamin B6 derivatives of the...
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6750214 |
Quinoline and quinazoline compounds useful in therapy
The invention provides compounds of formula (I), wherein R 1 represents C 1-4 alkoxy optionally substituted by one or more fluorine atoms; R 2 represents H or C 1-6 alkoxy optionally...
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6730681 |
Triazolo-pyrimidine derivatives as ligands for gaba receptors
A class of substituted or 6,7-ring fused [1, 2, 3]triazolo[1,5-α]-pyrimidine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and an...
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6686388 |
Regulators of the hedgehog pathway, compositions and uses related thereto
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function...
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6680326 |
Polycyclic compounds
Novel polycyclic compounds of the formula [I], wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , ring A, ring B, X, Y and Z are as defined herein and the pharmaceutically acceptable salts...
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6605627 |
Modulators of peroxisome proliferator activated receptor-gamma, and methods for the use thereof
In accordance with the present invention, there is provided a class of compounds which are capable of modulating processes mediated by peroxisome proliferator activated receptor-gamma (PPAR-γ)....
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6599906 |
Method of local anesthesia and analgesia
The present invention provides a method of producing local analgesia and anesthesia in a mammal experiencing pain in a nerve tissue region. The method includes topically administrating to the...
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6537974 |
Method of treating arrhythmias
A method for treating arrhythmia in mammals is provided comprising administering a low dose of an adenosine receptor agonist of the Formula I: wherein R 1 is an optionally substituted...
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6524625 |
Physiologically active extract obtained from indigo plant polygonum tinctorium
A physiologically active extract comprising an ethyl acetate-soluble ingredient of an indigo plant, which is obtainable by soaking a raw indigo plant in an organic solvent used for extraction. The...
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6518274 |
Use of cyclopentabenzofuran-derivatives for combating (NF-&kgr B)-dependent diseases
The invention relates to the use of cycloventabenzofuran derivatives for the production of a medicament for the treatment of nuclear factor of κB-dependent diseases.
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6458523 |
Hydroquinone derivatives as scavengers for oxidized developer
New compounds of the formula I are described, wherein n is >1 X is O or NR 4 ; L is a n-valent linking group defined in claim 1 and R 1 is H, halogen, C 1 -C 25 -alkyl, C 3 -C 25 -alkenyl,...
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6436949 |
Heterocyclically substituted benzamides and their use
Heterocyclically substituted benzamides of the formula I are described, where R 1 , R 2 , R 3 , R 4 , R 5 , X, m and n have the meanings given in the description. The novel compounds are useful...
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6426349 |
Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes for neoplasia
Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell...
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6420365 |
Imidazopyridines and related derivatives as selective modulators of bradykinin B2 receptors
Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein A, B, C, D, Y, R 1 , R 3 , R 4 , R 5 , and R 6 are variables defined herein, which...
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