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8178539 |
Substituted 3,4,6,7-tetrahydro-5H-1,2a,4a,8-tetraazacyclopenta[cd]phenalenes and methods
Substituted 3,4,6,7-tetrahydro-5H-1,2a,4a,8-tetraazacyclopenta[cd]phenal
ene-9-amines, pharmaceutical compositions containing the compounds or salts thereof, intermediates, methods of making the...
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8173157 |
Pharmaceutical composition comprising phenylamidine derivative and method of using the pharmaceutical composition in combination with antifungal agent
A pharmaceutical composition comprising a phenylamidine derivative or a salt thereof, represented by a general formula, wherein R1 and R2 may be same or different, and represent an optionally...
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8168638 |
Pyrazinecarboxamide derivatives and plant disease controlling agents containing the same
The present invention provides the compounds represented by the general formula (I): [wherein X is a halogen atom or an (C1-C3)alkyl group which may be substituted with a halogen atom(s); Y is a...
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8158631 |
Heterocyclic antiviral compounds
Compounds having the formula I wherein R1, R2, R3, R4, and R5 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV...
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8158630 |
Application of 2,5 -dihydroxymethyl-3,6-dimethyl pyrazine and its derivates in pharmacy
An application of 2,5-dihydroxymethyl-3,6-dimethyl pyrazine and its derivatives in the preparation of drugs for the treatment of, prevention of, and/or protection from heart failure wherein the...
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8138189 |
Substituted benzene compounds as modulators of the glucocorticoid receptor
The present invention relates to compounds of formula I wherein R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds...
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8114898 |
Compositions and methods for treating purpura
Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an α adrenergic receptor agonist selected from selective ...
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8110577 |
Histone deacetylase inhibitors
The present invention provides histone deacetylase inhibitors of general formula (I), a process for the preparation of such compounds and uses of the compounds in medicine, especially in the...
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8097625 |
Combination of sedative and a neurotransmitter modulator, and methods for improving sleep quality and treating depression
One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and/or depression. The...
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8076341 |
Compounds and use thereof
A compound of formula (I) wherein R1 is selected from H, F, Cl, Br, CF3, C1-C6 alkoxy and OH; R2 is selected from H and C1-C6 alkyl; n is 1-12; m is O or 1; Y is selected from CH2, NR3, (NR3R4)+X,...
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8071594 |
Substituted diketopiperazines and their use as oxytocin antagonists
Compounds of formula (1) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is 2-methyl-1,3-oxazol-4-yl and R4 and R5 together with the notrogen atom to which they are attached represents...
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8067418 |
Tricyclic angiotensin II agonists
There is provided compounds of formula I, wherein the dotted line, X1, X2, X3, A, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts...
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8048884 |
Substituted piperazinyl pyrazines and pyridines as 5-HT7 receptor antagonists
The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is —C(H)═ or —N═; m is 0, 1 or 2; R1 is optiona...
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8044053 |
Sulfonamide substituted pyrazoline compounds, their preparation and use as CB1 modulators
The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the...
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8030313 |
Controlled release sterile injectable aripiprazole formulation and method
A controlled release sterile freeze-dried aripiprazole formulation is provided which is formed of aripiprazole of a desired mean particle size and a vehicle therefor, which upon constitution with...
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7981894 |
Polymorphic forms of 1-′4-(5-cyanoindol-3-yl) butyl-4-(2-carbamoylbenzofuran-5-yl)piperazine hydrochloride
The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl) butyl]-4-(2-carbomyl-benzofuran-5-yl)-piperazine, crystaline modification of the...
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7981436 |
Hydrogels for the controlled release of bioactive materials
The present invention relates to the formation of hydrogels based on guanosine hydrazide derivatives in the presence of cations. The hydrogels can be used as a carrier/delivery system for...
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7977332 |
Insecticidal N-(heteroarylalkyl)alkanediamine derivatives
Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb,...
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7968547 |
Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
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7964606 |
Therapeutic agents useful for treating pain
The present invention discloses compounds of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Phenylene Compound”); compositions com...
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7960384 |
Dipeptidyl peptidase inhibitors
Compounds, pharmaceutical compositions, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound of the formula: wherein the substituents are as defined...
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7951830 |
Compounds effecting glucokinase
The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a...
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7947684 |
1-aroyl-piperidinyl benzamidines
This invention relates to compounds of formula which inhibit Factor Xa or tryptase, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of...
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7947685 |
Pyrazine-2-carboxyamide derivatives
The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I) wherein R1, R2 and R3 are as defined in the specification. These compounds are useful for the...
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7923446 |
Biaryl sulfonamides and methods for using same
The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.
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7851501 |
Aromatic nitrocatechol compounds and their use for modulating processes mediated by cell adhesion molecules
Pharmaceutical compositions comprising at least one compound of e.g. the formulas (Ie) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents...
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7851475 |
Substituted pyrrole-2, 5-diones as protein kinase C inhibitors
A compound of formula I wherein R, Ra and Rb are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions...
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7838520 |
Inhibitors of histone deacetylase
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides...
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7829563 |
Aminoamides as orexin antagonists
The present invention relates to compounds of formula I wherein Ar1, Ar2, Ar3, n, and R1 to R8 are as defined herein and to pharmaceutically suitable acid addition salts, optically pure...
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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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7820671 |
Peptidomimetic protease inhibitors
The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors;...
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7812017 |
4-substituted indole and indoline compounds
The present invention relates to novel compounds of formula (I): wherein m, n, R0, R1, R2, R3 and R4 are as described herein, to pharmaceutical compositions comprising the compounds, to processes...
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7807680 |
Controlled release sterile injectable aripiprazole formulation and method
A controlled release sterile freeze-dried aripiprazole formulation is provided which is formed of aripiprazole of a desired mean particle size and a vehicle therefor, which upon constitution with...
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7807677 |
HIV protease inhibitors
Compounds of the formula I: wherein R1, R2, X and N are as defined in the specification;E is N, CH;A′ and A″ are terminal groups as defined in the specification. The compounds have utility as HIV...
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7803802 |
Substituted amide beta secretase inhibitors
Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are...
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7799786 |
Therapeutic agents useful for treating pain
A compound of formula: wherein A, Ar, R3, R6, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Cyanoiminopiperazine Compound”), compositions comprising an effective amo...
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7795302 |
Use of compositions for treating rosacea
Rosacea is treated with a composition comprising an antimicrobial and at least one of an anti-inflammatory and a non-retinoid inhibitor of at least one of NF-KB, AP-1, MMPs, adhesion molecules,...
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7780986 |
Method of preparing sustained-release preparations of quinolone antibiotics
The present invention relates to an orally administrable preparation comprising a quinolone antibiotic which releases the active compound with a delay.
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7732450 |
Antifungal ketoconazole composition for topical use
A pharmaceutical composition suitable for topical application comprising ketoconazole in a solution which comprises: (i) 13 to 50 wt % water; (ii) 45 to 85 wt % of an alcohol having a boiling point...
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7718668 |
Salts of 6-heterocycle substituted hexahydrophenanthridine derivatives
The invention relates to salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4-inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical...
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7696191 |
Crystalline compound
A novel crystalline form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-[(1-methyle
thyl)oxy]-N-1H-pyrazol-3-ylbenzamide is described in the specification. This compound is a glucokinase (GLK...
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7687067 |
2-pyridinylcycloalkylcarboxamide derivatives useful as fungicides
A compound of general formula (I): A process for preparing this compound.An intermediate of general formula (II) for the preparation of a compound of general formula (I). A fungicidal composition...
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7625949 |
Methods for treating retroviral infections
The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to formula I where Ar, R1-R5, R11c and X1...
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7622471 |
Pyrazole derivatives having a pyridazine and pyridine functionality
The present invention is directed to a strong platelet aggregation-inhibiting agent which does not inhibit COX-1 or COX-2. Further, the present invention provides compounds represented by formula...
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7622472 |
Combination of Src kinase inhibitors and chemotherapeutic agents for the treatment of proliferative diseases
Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders.
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7612074 |
Diazabicyclic aryl derivatives as cholinergy ligands
This invention relates to novel diazabicyclic aryl compounds of the formula wherein: R′ represents hydrogen or alkyl; A represents an aromatic monocyclic or bicyclic carbocyclic or heterocyclic; a...
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7598248 |
Certain 1H-imidazo[4,5-b]pyrazin-2(3H)-ones and 1H-imidazo[4,5-b]pyrazin-2-ols, compositions thereof, and methods for their use
Provided is at least one chemical entity chosen from compounds of Formula I and compounds of Formula II: and pharmaceutically acceptable salts thereof, compositions thereof, and methods for their...
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7595318 |
Polyethylene glycol conjugates of heterocycloalkyl carboxamido propanoic acids
Disclosed are conjugates which bind VLA-4. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such conjugates are useful in the...
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7566716 |
Imidazopyrazines as Raf inhibitor compounds
Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, tautomers, solvates and...
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7547701 |
Haloalkyl containing compounds as cysteine protease inhibitors
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these...
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