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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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6407088 |
Method of analgesia
This invention relates to a method of producing analgesia in a mammal experiencing pain by systemically administering an effective amount of a composition comprising essentially of a sodium channel...
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6391872 |
Indazole bioisostere replacement of catechol in therapeutically active compounds
Therapeutically active compositions of matter and member species thereof are described which comprise indazole-containing compounds, said compounds and their therapeutic activity resulting directly...
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6380193 |
Fused tricyclic compounds, methods and compositions for inhibiting PARP activity
A compound of formula I: or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof.
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6342499 |
Parasitic and saprophagous mite control in beneficial insects
The present invention provides a method to control parasitic and saprophagous mites on beneficial insects such as honeybees via the application of a parasiticidally or saprophagouscidally effective...
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6337331 |
Triazolo-pyrimidine as ligands for GABA receptors
Substituted or 6,7-ring fused 1,2,3-triazolo[1,5-α]-pyrimidine derivatives are selective ligands for GABA A receptors useful in the treatment of disorders of the central nervous system, including...
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6291453 |
4-amino-phenylalanine type 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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6288094 |
Polycyclic thiazol-2-ylidene amines, processes for their preparation and their use as medicaments
The invention relates to polycyclic thiazolidin-2-ylidene amines and their physiologically tolerated salts and physiologically functional derivatives. Polycyclic thiazolidin-2-ylidene amines of the...
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6214831 |
Pharmaceutical composition containing evodiamine compound and method for improving lipid metabolism or antiobesity
The present invention relates to a food and a feed having lipid metabolism improving activity or anti-obesity activity, and a lipid metabolism improving agent or an anti-obesity agent for humans or...
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6211189 |
Amino-spiro-quinazoline compounds
There are provided novel compounds of formula (I) ##STR1## wherein A represents an aromatic carbocyclic ring or a 5- or 6-membered heterocyclic aromatic ring containing 1 to 3 heteroatoms which may...
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6210687 |
Fat emulsion containing xanthine derivative
An oil-in-water emulsion containing a xanthine derivative represented by ##STR1## or its pharmacologically acceptable salt, wherein the xanthine derivative or salt is present within an oil phase of...
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6207701 |
Urokinase inhibitors
Compounds having formula I ##STR1## are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions and...
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6184221 |
Sulfonamide-substituted compounds, processes for their preparation, their use as a medicament or diagnostic, and medicament comprising them
Compounds of the formula I ##STR1## having the meanings of the substituents indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and for...
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6159996 |
Polycyclic thiazolidin-2-ylidene amines, process for their preparation, and their use as pharmaceuticals
Polycyclic thiazolidin-2-ylidene amines and their physiologically tolerable salts and physiologically functional derivatives of the formula I ##STR1## in which the radicals have the meanings...
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6124306 |
Thioalkyl alpha substituted pyrimidine compounds
The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula I ##STR1## and pyrimidine-thioalkyl and alkylethers of Formula I, where R 4 is selected from the group...
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6114339 |
Derivatives of pyrido [2,3-D] and [3,2-D] pyrimidine method of using these derivatives
The invention also discloses compounds and pharmaceutically acceptable salts having the generic formula (2) ##STR1## wherein X and Y may be the same or different and are selected from the group...
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6107304 |
Thieno[2,3-b]pyrazolo[3,4-d]pyridine-3-ones to enhance erythropoiesis
Invented are substituted thieno (2,3-b)pyrazolo(3,4-d)pyridin-3-ones, pharmaceutical compositions containing these compounds, and methods of using these compounds to enhance erythropoiesis. Also...
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6083952 |
Compounds
There are provided novel compounds of formula (I) ##STR1## wherein A represents an aromatic carbocyclic ring or a 5- or 6-membered heterocyclic aromatic ring containing 1 to 3 heteroatoms which may...
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6046183 |
Method of synergistic treatment for benign prostatic hyperplasia
Disclosed is an improved treatment for men with benign prostatic hyperplasia (BPH), involving combination therapy of a 5α-reductase inhibitor, e.g. a 17β-substituted 4-azasteroid, a...
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6030972 |
Dipeptide amidines as thrombin inhibitors
Compounds of the formula ##STR1## where A, B, D, R 1 and R 2 have the meanings stated in the description, are described. The compounds are suitable for controlling diseases. The novel compounds...
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6028077 |
Crambescidin compounds
The present invention is directed to the isolation and characterization of six new crambescidin compounds, the structures of which are shown below: ##STR1## .
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6022895 |
Substituted amino compounds and their use as substances having an analgesic effect
Substituted amino compounds of general formula (I) ##STR1## are described, as are a method of preparing them and their use as drugs, especially as analgesics.
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5998421 |
Lipid metabolism ameliorants
The present invention relates to a food and a feed having lipid metabolism improving activity or anti-obesity activity, and a lipid metabolism improving agent or an anti-obesity agent for humans or...
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5952332 |
Antiviral and cytotoxic compounds from the sponge crambe crambe
The present invention is directed to several novel compounds isolated from the sponge Crambe crambe, and designated herein as Crambescidin 816 (Compound 1), Crambescidin 830 (Compound 2),...
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5952331 |
Aryl pyrimidine derivatives
The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT 2B -antagonists.
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5939419 |
2-benzyl-polycyclic guanine derivatives and process for preparing them
Antihypertensive and bronchodilating compounds of the formula or a pharmaceutically acceptable salt thereof, and a process for preparing them are disclosed, wherein: R 1 , R 2 , R 3 , R a , R b ...
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5939442 |
Modulations of peroxisome proliferator activated receptor-γ, 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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5880135 |
Substituted 4-phenylaminothiazoles, their process of preparation and the pharmaceutical compositions containing them
A compound, as well as its stereoisomers and addition salts, possssing antagonist activity with respect to corticotropin releasing hormone (CRF) has the formula: ##STR1## in which R 1 , and R 21 ...
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5874451 |
Propanolamine derivatives, processes for their preparation, pharmaceuticals comprising these compounds, and their use
The invention relates to substituted propanolamine derivatives and their acid addition salts. Propanolamine derivatives of formula I, ##STR1## in which R 1 to R 8 have the meanings indicated in...
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5859016 |
Memory enhancing and anti-dementia agent containing dehydroevodiamine HC1 as active ingredient
Dehydroevodiamine-HCl, a constituent of Evodia rutaecarpa Benth. (DHED) exhibits anti-AChE activity and improves the memory impairment of animals produced by scopolamine in the passive avoidance...
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5856322 |
Unsaturated hydroxyalkylquinoline acids as leukotriene antagonists
Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and...
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5824683 |
2'- 4'-h alo- 1,1'-biphenyl!-4-yl!methyl!-5'-methyl-spiro cyclopentane-1,7' (8'H)- 3H! imidazo 2,1-b!purin!-4' (5'H)-ones
Antihypertensive and bronchodilating phosphoclusterose inhibitory compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein X is fluoro, chloro or bromo.
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5786361 |
Pyridazino-, pyrimido-, pyrazino- and triazinoindoles, -pyrrolocycloalkenes or pyrrolooxocycloalkenes, or pyridopyrrolylpyrido compounds, compositions containing them, and use thereof to treat atherosclerosis
Compounds of the formula (I): ##STR1## are prepared by reaction of the phenylacetic acid derivatives substituted by the appropriate heterocycles, optionally in an activated form, with...
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5753663 |
Pyrimidine derivatives
The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts thereof, exhibit useful pharmacological properties, in particular use as 5HT 2C - antagonists. The invention is also...
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5728684 |
Determination of prodrugs metabolizable by the liver and therapeutic use thereof
A method of ascertaining if a prodrug is useful for treating a disease is disclosed. The prodrug is acceptable if it is metabolized in liver cells by aldehyde oxidase to produce an active drug or...
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5667792 |
Derivatives of 2,5-dihydroxyphenylcarboxylic acids, and their utilization in cosmetic or dermatological compositions with a depigmenting action
A cosmetic or dermatological composition with a depigmenting action comprises derivatives of 2,5-dihydroxyphenylcarboxylic acids, their homologs, and their salts, with the derivatives having the...
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5654310 |
Triazolopyrimidones their preparation and use
Triazolopyrimidines of the formula ##STR1## where A, D and X have the meanings stated in the description, and their preparation are described. The novel compounds are suitable for controlling...
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5646154 |
Pharmaceutical compositions for inhibiting the formation of tumor necrosis factor
Quinazoline compounds represented by general formula (1) or (2) possess an activity of significantly inhibiting the production or secretion of a tumor necrosis factor and are useful as drugs for...
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5639756 |
Benzimidazole compounds
An antidiabetic compound selected from those of formula (I): ##STR1## wherein A, B, C, D, n, R 1 , R 2 , R 3 , R 4 , X, Y and Z are as defined in the description. Medicaments containing the same.
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5631261 |
Triazoloquinazolines, their preparation and use
Novel triazoloquinazolines of the formula I ##STR1## where A, X R 1 and R 2 have the meanings stated in the description, and their preparation are described. The compounds are suitable for...
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5612344 |
Triazoloquinazolines for the treatment of central nervous disorders
The use of triazoloquinazolines for the production of drugs for controlling central nervous disorders is described. The triazoloquinazolines have the formula ##STR1## where R 1 , R 2 and X have...
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5604224 |
Substituted heterocyclylisoquinolinium salts and compositions and methods of use thereof
Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries...
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5602137 |
Pyrimidine compounds and their use as pharmaceuticals
Compounds for treating cardiovascular or circulatory disorders of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R 1 , R 2 , R 3 , R 7 , Ar 1 , Ar 2 , X, Y, and n are...
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5574039 |
Antiproliferative compounds having nitrogen-containing tricyclic ring systems and phenyl substituents
The invention relates to TS-inhibiting compounds of the formula ##STR1## where W is an alkylene group; D is a structure having two rings that are unsubstituted or substituted, where (i) one ring is...
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5574038 |
5,6-cyclicimidazo [1,5-a] Quinoxalines
The invention discloses imidazo[1,5-a]quinoxalines (I) ##STR1## which do not contain an endocyclic carbonyl group that are useful as anxiolytic and sedative/hypnotic agents.
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5571813 |
Fused pyrimidine compounds and their use as pharmaceuticals
Pharmaceutical compounds which are azolo-fused pyrimidine compounds having the formula ##STR1## in which A--B-- together with the pyrimidine ring forms a) a pyrazolo[1,5-a]pyrimidine of formula...
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5569655 |
Substituted heterocyclylisoquinolinium salts and compositions and method of use thereof
Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries...
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5565460 |
Therapeutic purine agents for parkinson's disease
The present invention relates to a therapeutic agent for Parkinson's disease containing as an active ingredient a polycyclic compound or a pharmaceutically acceptable salt thereof, the compound...
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5532366 |
Heterocyclic amides
The present invention relates to certain novel amide derivatives which are pyrido[3,4-d]pyrimidin-7-ylacetamides which are inhibitors of human leukocyte elastase (HLE), also known as human...
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5510370 |
Parathyroid hormone and raloxifene for increasing bone mass
The present invention includes a method for increasing bone mass in a subject by administration of PTH and raloxifene. Another aspect of the invention is a method for treating bone loss in a...
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