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8163749 |
Six-membered heterocycles useful as serine protease inhibitors
The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, R3 and R11 are as defined...
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8143255 |
Heteroalkyl linked pyrimidine derivatives
The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to heteroalkyl linked and substituted pyrimidine...
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8129386 |
Fused azole-pyrimidine derivatives
The present invention relates to novel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the...
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8124608 |
Stable pharmaceutical composition of freeze-dried tetrodotoxin powder
This invention relates to a stable pharmaceutical composition of freeze-dried tetrodotoxin powder which contains trace amount of tetrodotoxin, substances which can stabilizes tetrodotoxin,...
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8093254 |
Aspartyl protease inhibitors
Disclosed are compounds of formula I (Chemical formula should be inserted here as it appears on abstract in paper form) Formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or...
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8093246 |
O-linked pyrimidin-4-amine-based compounds, compositions comprising them, and methods of their use to treat cancer
O-linked pyrimidin-4-amine-based compounds, pharmaceutical compositions comprising them, and methods of their use are described. Particular compounds of the invention are of formula I:
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8088788 |
Substituted fused[1,2] imidazo[4,5-c] ring compounds and methods
[1,2]Imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) substituted with a fused ring containing an oxygen and/or nitrogen...
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8067401 |
Compounds and compositions for treating infection
Compounds from 14 Kenyan plants, including from the root of Dovyalis abyssinica and Clutia robusta have been characterized and isolated, and their uses are disclosed.
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8030304 |
Thiazole pyrazolopyrimidines CRF1 receptor antagonists
The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of...
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8022047 |
Combination anticancer agents
A cancer therapeutic agent comprising a combination of compound A described below, or a pharmaceutically acceptable salt thereof, and compound B described below, or a pharmaceutically acceptable...
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8012987 |
Indolo[2,1-b] quinazole-6,12-dione antimalarial compounds and methods of treating malaria therewith
Compounds, compositions and methods are provided for treating malaria parasites in vitro and in vivo by administering indolo [2,1-b]quinazoline-6,12-dione compounds of Formula I. wherein A, B, C,...
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7994187 |
HIV inhibiting 3,4-dihydro-imidazo[4,5-B]pyridin-5-ones
HIV inhibitory compounds of formula: salts, hydrates, solvates, N-oxides, or stereoisomers thereof, wherein A forms pyridine, pyrimidine, pyrazine, pyridazine, triazine, imidazole, pyrazole,...
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7977378 |
Compositions and methods for enhancing weight-loss by cyclical administration of compounds
Compositions and methods are provided for the treatment of obesity in a human in need of such treatment which comprises administration to the human of a therapeutically effective amount of a...
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7956060 |
Pyrimidine derivative compound
The present invention provides an antitumor agent and the like, which comprises as an active ingredient, a pyrimidine derivative represented by Formula (I): [wherein —X—Y—Z— represents —O—CR3═...
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7943615 |
Fused aminopiperidines as dipeptidyl peptidase-4 inhibitors for the treatment or prevention of diabetes
The present invention is directed to novel substituted fused aminopiperidines of structural formula (I) which are inhibitors of the dipeptidyl peptidase-4 enzyme and which are useful in the...
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7910586 |
Compositions and methods for prevention and treatment of amyloid-β peptide-related disorders
The present invention provides methods and compositions for modulating levels of amyloid-β peptide (Aβ) exhibited by cells or tissues. The invention also provides pharmaceutical compositions and m...
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7910593 |
Water-soluble prodrugs
An objective of the present invention is to provide water-soluble prodrugs that can be administered parenterally, and which show excellent water solubility and small interspecies or individual...
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7855214 |
Fused cyclic systems useful as inhibitors of TEC family protein kinases
The present invention relates to compounds useful as inhibitors of Tec family protein kinases. These compounds have the general formula I: or a pharmaceutically acceptable salt thereof, wherein R1,...
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7820663 |
Substituted enaminones, their derivatives and uses thereof
The present invention is related substituted enaminones represented by a compound of Formula I that are novel allosteric modulators of α7 nAChRs. The invention also discloses the treatment of ...
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7776864 |
Fused bicyclic pyrimidines
Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6 and R7 have the meanings as given in the...
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7713954 |
Compositions and methods for treating cognitive disorders
Methods and pharmaceutical compositions relating to selective antagonists of the 5-HT6 receptor and 5-HT2A receptor useful for the treatment of cognitive disorders are presented.
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7691864 |
Anti-hypertensive composition and methods of treatment
Pharmaceutical compositions for the treatment of hypertension comprising an effective anti-hypertensive amount of at least one compound in association with a pharmaceutically acceptable,...
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7642265 |
Benzimidazoles and analogs thereof as antivirals
Provided are compounds of the formula: wherein RN1 is a substituent of formula G1—NX1X2, wherein G1 is an optionally further substituted alkylene, which optionally forms, together with RN2, a c...
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7625888 |
Fused triazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
The present invention is directed to novel fused triazole derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or pre...
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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) or...
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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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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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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 R1 represents hydrogen, an aliphatic hydrocarbon group which may have a substituent(s) or a cyclic...
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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 R4 and R5 are hydrogen, halogen, cyano, haloalkyl, or haloalkoxy, but are not both hydrogen; R6 and R7 are optional...
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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 (R1, R2, Hal and L1 through L5 are defined in the specification) show selective fungicidal activity. The new compounds may be processed with carriers and...
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7312225 |
Macrocyclic pyrimidines, their production and use as pharmaceutical agents
Macrocyclic pyrimidine derivatives of general formula I in which R1 to R5, X, Y, A, B, m and n have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinase,...
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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 the...
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7160890 |
Compounds specific to adenosine A3 receptor and uses thereof
This invention pertains to compounds which specifically inhibit the adenosine A3 receptor and the use of these compounds to treat a disease associated with A3 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 R1 is generally hydrogen or CF3, R2 is generally hydrogen, W is a cyclic amine, a heterocycle or a group L-Y—X where L-Y is a l...
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7109195 |
Hexacyclic compounds and their therapeutic use
The present invention relates to hexacyclic compound of the formula [1], wherein Z, R3 and R4 are as identified therein, and pharmaceutically acceptable salts thereof. These compounds are useful in...
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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, Y1, Y2, and R2-4 are as defined in the...
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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, R1, R2, R3, R4, R5, R6, X, Y, R1′, R2′, R3′, R4′, R5′, R6′, ring A′, ring B′ and X′ are as defin...
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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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