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7601723 |
Pyridyl substituted xanthines
The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xanthines of formula I
which are selective antagonists of A 2B adenosine receptors...
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7534859 |
Protein kinase C epsilon as modulator of anxiety, alcohol consumption and self-administration of drugs of abuse
The present invention is directed to the production of PKC isozyme ε (PKCε)-deficient cells and non-human animals. The present invention is further directed to the identification of PKCε as a...
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7354943 |
Statine derivatives for the treatment of Alzheimer's disease
The present invention relates to compounds of formula (I):
useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme...
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7288546 |
Method and compound for inhibition of cell death
This invention relates to a chemical compound that inhibits the apoptotic activity of the protease Omi/HtrA2 and homologous proteins. This protease Omi/HtrA2 is present in all mammalian cells so...
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7166610 |
Method of treating movement disorders using barbituric acid derivatives
A method of treating movement disorders comprises administering to a human or animal subject in need of treatment a therapeutically effective amount of at least one compound according to the...
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7041673 |
Ultrashort acting hypnotic barbiturates
The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are...
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RE38934 |
Method and reagents for N-alkylating ureides
A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I
with an alkylating agent of structure III
in the presence of a basic catalyst...
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6939873 |
Non-sedating barbituric acid derivatives
The present invention relates to novel non-sedating barbituric acid derivatives, pharmaceutical compositions containing them and methods of neuroprotection in cases of cerebral ischemia, head...
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6919332 |
N-substituted-heteroaryloxy-aryloxy-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula
wherein X, A, Y, B, G, and R 1 are as defined in the...
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6833372 |
Non-peptide GnRH agents, Pharmaceutical compositions, and methods for their use
Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing hormone are described. Such agents are useful for treating mammalian reproductive disorders and steroid hormone-dependent...
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6756379 |
Non-sedating barbiturate compounds as neuroprotective agents
Methods of providing neuroprotection are disclosed comprising administering a non-sedative barbiturate compound in an amount sufficient to achieve neuroprotection in a mammalian subject. Preferred...
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6716845 |
Barbituric acid derivatives
The present invention pertains to derivatives of 5,5-disubstituted pyrimidine-2,4,6,-trianones having the formula: wherein R 1 , R 2 , R 3 , and R 4 are described herein. These compounds have...
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6706723 |
Pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, A, B and R 1 are as defined in the specification, and to pharmaceutical...
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6664262 |
N-methoxymethyl-5,5-diphenylbarbituric acid
A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I: with an alkylating agent of structure III: in the presence of a basic catalyst in...
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6649614 |
Use of a NK-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent for treatment of depression or anxiety
The present invention relates to the treatment of depression and/or anxiety by the administration of a combination of a specific class of NK-1 receptor antagonists and an antidepressant or...
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6573269 |
Pyrimidine-2,4,6-trione light screening compositions
The present invention provides compounds of formula I, which are effective in absorbing ultraviolet radiation and can be used as sunscreen agents: wherein R 1 and R 2 are each independently C...
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6559136 |
Fungicidal active substance combinations
Novel active compound combinations of compounds of the formula (I) in which Z, X and A are each as defined in the description with known active compounds and their use for controlling...
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6545006 |
Process for obtaining L-dihydroorotic acid and use thereof
The invention relates to a process for obtaining L-dihydroorotic acid by chromatography on an anionic exchange material in a base water mixture under a pressure from about 1.1 MPa to about 40 MPa....
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6541523 |
Methods for treating or preventing fibromyalgia using very low doses of cyclobenzaprine
The present invention relates to methods and compositions comprising a very low dose of cyclobenzaprine or metabolite thereof for preventing and treating sleep disturbances and illnesses manifested...
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6509343 |
Fungicidal active substance combinations
Active compound combinations comprising a compound of the formula (I) and known fungicidally active compounds, and their use for controlling phytopathogenic fungi, are described.
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6498164 |
Barbituric acid derivative and preventive and therapeutic agent for bone and cartilage containing the same
A compound of the formula wherein the substituents are as defined in the specification and solvates and salts thereof useful for treating bone and cartilage diseases.
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6472396 |
Barbituric acid derivatives, processes for their production and pharmaceutical agents containing these compounds
Compounds of formula I, useful as matrix metalloprotease inhibitors, wherein X, Y and Z are each oxygen; R 1 is selected from the group consisting of (a) n-octyl, (b) n-decyl, (c) biphenyl and...
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6469017 |
Method of inhibiting interleukin-12 signaling
A method for blocking IL-12 signaling by administration of the following compound: wherein, R 1 is H, CH 3 , sulfate, phosphate, or salt thereof; R 2 is alkyl (C 1-12 ), alkoxyalkyl (C 1-11 ),...
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6440985 |
Methods for treating viral infections
Methods are provided for the treatment and prophylaxis of viral infection and disease associated with such infection.
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RE37623 |
Enzyme inhibitors, their synthesis, and methods for use
Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula where X is S or Se; Y is H, I, F, Cl, Br, methoxy,...
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6335332 |
Barbituric acid derivatives with antimetastatic and antitumor activity
The invention is directed to barbituric acid derivatives having inhibitory activity for matrix maetalloproteases comprised of formula (I): pharmaceutical compositions thereof, processes for...
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6294520 |
Material for passage through the blood-brain barrier
A material which has the ability to effect it's passage, at least in part, and the ability to transport other materials through the blood-brain barrier which includes any one or more pure sugars or...
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6288071 |
1-ethylene-2-alkylene-1,4-cyclohexadiene pesticides
Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in...
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6242455 |
Pyrimidin-2,4,6-trion derivatives, method for producing the same and medicinal products containing these compounds
Compounds of formula I ##STR1## wherein R1, R2, R3 and R4 have the meanings indicated in the specification. The compounds are useful as inhibitors of metalloproteases of the M2, M3 family and...
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6174890 |
Anti-stress, anti-impairment and anti-aging drug and process for manufacturing thereof
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6133276 |
Compounds and methods for increasing endogenous levels of corticotropin-releasing factor
Ligand inhibitors for increasing levels of free corticotropin-releasing factor (CRF) in the brain are disclosed. Such ligand inhibitors cause release of CRF from the CRF/CRF-bind protein complex....
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6087356 |
Rapid narcotic detoxification
Methods for rapid detoxification of patients addicted to opioid narcotics are provided. The methods include administering nalmefene to induce acute withdrawal, and administering dextromethorphan...
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6028073 |
N-substituted 3-azabicyclo (3.2.0)heptane derivatives useful as neuroleptics
N-substitued 3-azabicyclo[3.2.0]heptane derivatives of formula (I) ##STR1## in which R 1 , R 2 , A, X, Y and Z have the meanings given in the description, their method of preparation and their use...
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6013626 |
Cryptophycins from synthesis
A cryptophycin compound is provided having the structure: ##STR1## Further provided are methods of producing cryptophycins by total synthesis and methods of using cryptophycins in pharmaceuticals....
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5965564 |
Enantiomerically pure hydroxylated xanthine compounds
There is disclosed compounds and pharmaceutical compositions that are a resolved R or S (preferably R) enantiomer of an ω-1 alcohol of a straight chain alkyl (C 5 -8) substituted at the 1-position...
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5958946 |
Modulation of hair growth
Mammalian hair growth may be modulated by applying to the skin a compound that induces or activates the conjugation of an androgen.
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5942497 |
Purine compound and catecholamine compound containing compositions and methods for administration
A purine compound, which has a desired and an undesired effect when a dosage sufficient to induce the desired effect is administered to a mammal, is combined with a counteracting agent, wherein the...
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5889013 |
Pyrimidine acyclonucleoside derivatives
The present invention relates to novel pyrimidine acyclonucleoside derivatives represented by the following general formula (I), antiviral agents containing the derivatives as the active...
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5869494 |
Uses for barbituric acid analogs
Previously unknown anti-tumor, anti-infectious, immune system modulatory and anti-depressive properties of a family of barbituric acid derivatives are provided herein. Preferred derivatives are...
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5837703 |
Amino-alcohol substituted cyclic compounds
Therapeutic compounds have the formula: (X)j-(core moiety), j being an integer from one to three, the core moiety comprising a core moiety, the core moiety being a heterocycle having one ring or...
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5834465 |
Treatment with combined NMDA and non-NMDA antagonists to reduce excitotoxic CNS damage
This invention involves a pharmaceutical mixture for preventing or reducing excitotoxic brain damage caused by hypoxia/ischemia (such as stroke) and various other factors. This mixture comprises an...
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5763476 |
Sublingual or buccal pharmaceutical composition
The invention relates to a sublingual or buccal pharmaceutical composition comprising trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz 2,3:6,7!oxepino- 4 ,5-c!pyrrole or a pharmaceutically...
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5731337 |
Conformationally rigid bicycle and adamantane derivatives useful as α 2
A compound of formula I ##STR1## in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond...
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5696125 |
Substance abuse-induced hemorrhagic stoke in an animal model
The present invention is an substance-induced-hemorrhagic stroke animal model. The substance-induced-hemorrhagic stroke animal model is useful in screening therapeutics for the prevention and/or...
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5679650 |
Pharmaceutical compositions including mixtures of an adenosine compound and a catecholamine
A purine compound, which has a desired and an undesired effect when a dosage sufficient to induce the desired effect is administered to a mammal, is combined with a counteracting agent, wherein the...
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5674870 |
Anti-cancer uses for barbituric acid analogs
Previously unknown anti-tumor, anti-infectious, immune system modulatory and anti-depressive properties of a family of barbituric acid derivatives are provided herein. Preferred derivatives are...
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5614541 |
Pharmacologically active catechol derivatives
New catechol derivatives and pharmaceutically acceptable salts and esters thereof useful as pharmaceutical antioxidants are disclosed. Cellular damage by oxygen derived radicals is a significant...
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5543147 |
Crystalline modification of 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine, a method for the preparation thereof and a medicinal preparation based on it
A crystalline modification of 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine prepared by cooling a solution of 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine in water, an organic solvent or in a...
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5489590 |
Method of treating with therapeutic composition comprising photoactive compound
A therapeutic composition derived from a pre-activated photoactive compound and a conveyor for destroying tumor or other pathogenic biological contaminants infecting animal body tissues. The...
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5474996 |
Pyrimidine derivatives
Novel pyrimidine derivatives of the formula ##STR1## represents: either a group: ##STR2## or a group: ##STR3## having angiotensin II inhibiting activity.
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