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8173644 |
3-substituted-[1,2,3]-benzotriazinone compound for enhancing glutamatergic synaptic responses
This invention relates to the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for higher order behaviors....
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8138180 |
Exo-selective synthesis of himbacine analogs
This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal...
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8129377 |
6-(pyridinyl)-4-pyrimidone derivates as tau protein kinase 1 inhibitors
A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R1 represents a C1-C12 alkyl; R2 represents a hydrogen atom or...
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7939526 |
Sulfone substituted imidazo ring ethers
Imidazo ring compounds (e.g., imidazoquinolines, 6,7,8,9-tetrahydroimidazoquinolines, imidazonaphthyridines, and 6,7,8,9-tetrahydroimidazonaphthyridines) with a sulfide-, sulfinyl-, or...
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7935712 |
Spirochromanone derivatives as acetyl coenzyme A carboxylase (ACC) inhibitors
The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.
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7906507 |
Oxadiazoanthracene compounds for the treatment of diabetes
The present invention provides methods of use of oxadiazoanthracene derivatives of the formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, C, R, R1, R2, R3, R4 and R5 are as...
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7838519 |
Maytansinoid analogs as antitumor agents
Ansamycin analogs, including maytansinoid analogs, and their use in treating cell proliferative diseases and conditions, and in particular, for use as antitumor agents.
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7790714 |
Oxadiazoanthracene compounds for the treatment of diabetes
The present invention provides methods of use of oxadiazoanthracene derivatives of the formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, C, R, R1, R2, R3, R4 and R5 are as...
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7772228 |
Method for treatment of bacterial infections with once or twice-weekly administered rifalazil
A method for treatment of bacterial infections with rifalazil administered once-weekly, or twice-weekly. A method for treatment of tuberculosis caused by Mycobacterium tuberculosis, infections...
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7732435 |
Chromone derivatives useful as antagonists of VR1 receptors
The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their...
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7727983 |
Oxadiazoanthracene compounds for the treatment of diabetes
The present invention provides oxadiazoanthracene derivatives of the formula (I), wherein A, B, C, R, R1, R2, R3, R4 and R5 are as herein described, pharmaceutical compositions comprising...
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7678808 |
5 HT receptor mediated neurogenesis
The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes...
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7629338 |
Substituted monocyclic CGRP receptor antagonists
Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are...
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7595063 |
Compressed tablet formulation
This invention relates to a 50% drug loaded compressed tablet formulation for efavirenz. Efavirenz is a non-nucleoside reverse trancriptase inhibitor being studied clinically for use in the...
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7550458 |
Tricycloundecane compounds useful as modulators of nuclear hormone receptor function
Tricycloundecanes compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions...
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7494992 |
Antiparasitic terpene alkaloids
The present invention relates to novel terpene alkaloids and their use as antiparasitic agents. The present invention also relates to an antiparasitic agent which comprises a terpene alkaloid...
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7479490 |
Pellet for a presurrized pipeline
A system of equipment allowing addition of solid materials to a pressurized pipeline wherein said solid material is conveyed in such a way as to be readily dissolved by the liquid in said pipeline....
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7470683 |
Tetracyclic compounds
Compounds of formula I, of trans relative configuration: wherein: X represents an oxygen atom or an NR2 group,Y represents a group selected from —CH2—, —(CH2)2— and —CH═CH—,R1 and R2, which may be ...
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7465721 |
2-hydroxytetrahydrofuran derivatives and use thereof as medicaments
A hydroxytetrahydrofuran of formula wherein A is with the substituents as defined in the specification, having a calpain inhibiting activity and/or an activity which traps the reactive oxygen...
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7439239 |
Tricyclic δ- opioid modulators
Disclosed are compounds, compositions and methods for treating various diseases and conditions, including pain. Such compounds are represented by Formula I as follows: wherein A, G, Y, R3-R5 are...
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7435733 |
Mineralocorticoid receptor modulator compounds and methods, and pharmaceutical compositions containing these compounds
This invention relates to compounds that bind to mineralocorticoid receptors and/or modulate activity of mineralocorticoid receptors, and to methods for making and using such compounds. Some...
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7432257 |
Piperdinyl-phenoxazine and phenothiazine derivatives as δ-opioid modulators
The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic δ-opioid modulators. Pharmaceutical and veterinary compositions and methods of ...
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7384933 |
Derivatives of 2-hydroxytetrahydrofuran and their use as medicaments
A hydroxytetrahydrofuran of formula wherein A is with the substituents as defined in the specification, having a calpain inhibiting activity and/or an activity which traps the reactive oxygen...
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7268131 |
Substituted [1,4]oxazino[2,3-g]indazoles for the treatment of glaucoma
Substituted [1,4]oxazino[2,3-g]indazols for lowering intraocular pressure and treating glaucoma are disclosed.
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7141566 |
Benzoxazine and benzothiazine derivatives and the use thereof in medicaments
The invention relates to compounds of formula (I), the tautomeric and isomeric forms and salts thereof, in addition to a method for production and use thereof in medicaments.
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7135468 |
Antibacterial compounds
Bacterial protein synthesis-inhibiting compounds having formula (I) and salts, prodrugs, salts of prodrugs, and metabolites thereof, processes for making the compounds and intermediates in the...
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7115624 |
Method of inhibiting protein tyrosine phosphatase 1B and/or T-cell protein tyrosine phosphatase 4 and/or other PTPases with an Asp residue at position 48
The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTPα, PTPε, PTPμ, PTPδ, PTP...
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7084138 |
Active ingredient combinations with insecticidal and acaricidal properties
The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the groups W, X,...
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7015219 |
3-aryl-hydroxybenzoxazines and 3, 4-dihydro-3-aryl-hydroxybenzoxazines as selective estrogen receptor beta modulators
Substituted benzoxazine and 3,4-dihydrobenzoxazine derivatives possessing activity as estrogen receptor beta (ERβ) modulators are provided which have the structure of formula I wherein the ...
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6992092 |
Anti-diabetic agents
The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein R1,...
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6936606 |
Cyanoamido-containing heterocyclic compounds useful as reversible inhibitors of cysteine proteases
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful...
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6914059 |
Benzoxazine and benzothiazine derivatives and the use thereof in medicaments
Compounds of formula I, their tautomeric and isomeric forms and salts, as well as the process for their production and their use in pharmaceutical agents are described.
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6897199 |
Pharmaceutically acceptable salts of phenoxazine and phenothiazine compounds
The present invention relates to pharmaceutically acceptable salts of compound of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their...
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6861442 |
PYK2 and inflammation
The present invention relates generally to the fields of immunology and medicine, and more specifically to the field of cellular signal transduction. The present invention relates, inter alia, to...
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6858607 |
7,8-fused 4H-chromene and analogs as activators of caspases and inducers of apoptosis and the use thereof
The present invention is directed to substituted 4H-chromene and analogs thereof, represented by the general Formula I: or pharmaceutically acceptable salts or prodrugs thereof, wherein: wherein A,...
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6841550 |
Benzoxazine and benzothiazine derivatives and their use in medicines
The invention relates to compounds of formula (I) and their tautomeric and isomeric forms and salts, as well as to a method for producing said compounds and their use in medicines.
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6794384 |
Hydroxylation activated drug release
The present invention concerns prodrugs whose aromatic oxidation, particularly their enzymatic aromatic hydroxylation, results in their activation by the release of a drug moiety. It particularly...
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6630465 |
Synergistic insecticidal compositions
The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist and an arylpyrrole insecticide. Also provided...
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6610686 |
Use of pirenoxine for the protection of corneal tissues in photokeractomy
Pirenoxine or 1-hydroxy-5-oxo-5H-pyrido-[3,2a]-phenoxazin-3-carboxylic acid, also called pirfenossone and already used as anti-cataract agent, in the form of a pharmaceutically acceptable salt...
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6608055 |
Crystalline anticholinergic, processes for preparing it and its use for preparing a pharmaceutical composition
The invention relates to crystalline anhydrous (1α,2β,4β,5α,7β)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9
-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.022,4]nonane-bromide,
processes for preparing it and ...
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6528507 |
Polymorphic forms of an antidiabetic agent: process for their preparation and a pharmaceutical composition containing them
This invention relates to novel polymorphic/pseudopolymorphic forms of arginine salt of 3-[4-[2-(phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid, having the formula I shown below. The...
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6514984 |
Treatment for alzheimer's disease
A method is disclosed for the prevention and treatment of Alzheimer's disease by administering to a human in need thereof an effective amount of a substituted tricyclic sPLA2 inhibitor.
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6468996 |
Substituted hetero-polycyclic compounds as PPARα and PPAR&ggr activators
The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the...
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6462038 |
Androgen receptor modulator compounds and methods
Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions...
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6410598 |
Compositions and methods for advanced glycosylation endproduct-mediated modulation of amyloidosis
The present invention relates generally to the non-enzymatic glycosylation of amyloidogenic proteins and the consequent formation of advanced glycosylation endproducts (AGEs). It has been found...
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6410556 |
Modulators of protein tyrosine phosphateses (PTPases)
Disclosed are novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein...
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6384045 |
Tricyclic and tetracyclic pyrones
This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone...
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6380235 |
Benzimidazolones and analogues
The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein:A is O, S, or NR4;B is a...
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6365610 |
Ozonide compounds with inhibitory activity for urokinase production and angiogenesis
The invention provides a urokinase production inhibitor or angiogenesis inhibitor comprising as an active component an ozonide derivative represented by the formula (1), and method of prevention or...
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6310059 |
Fused ring calcium channel blockers
Compounds of the formula ##STR1##or salts thereof, wherein the variable are as defined herein are useful as calcium channel blockers.
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