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6849620 |
N-(azabicyclo moieties)-substituted hetero-bicyclic aromatic compounds for the treatment of disease
The invention provides compounds of Formula I:
wherein Azabicyclo is
W 0 is a bicyclic moiety and is
These compounds may be in the form of pharmaceutical salts or...
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6841563 |
Aryloxy propanolamines for improving livestock production
Disclosed is a compound represented by structural formula (I): R1 is a substituted or unsubstituted aryl group. R2 and R3 are independently —H, a C1-C4 straight chained or branched alkyl group....
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6835743 |
Pesticidal pyrazoles and derivatives
Process for the protection of a building that has already been built or is going to be built, whereby an effective amount of an insecticidally active compound is spread around or under the said...
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6831075 |
Heterocyclic substituted pyrazolones
The present invention is directed to novel heterocyclic substituted pyrazolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods...
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6828327 |
Macroheterocylic compounds useful as kinase inhibitors
This invention is directed to macroheterocyclic compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or...
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6825209 |
Compounds having unique CB1 receptor binding selectivity and methods for their production and use
Compounds are provided that are amide analogs of SR141716A having unique CB1 receptor selectivity and providing WIN sparing binding characteristics, pharmaceutical compositions containing the...
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6822001 |
Combination therapy using pentafluorobenzenesulfonamides and antineoplastic agents
Combination therapies are provided for the treatment of proliferative disorders which use a pentafluorobenzenesulfonamide of formula I and an antineoplastic agent such as gemcitabine or paclitaxel.
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6797712 |
Substituted amino-furan-2-yl-acetic acid and amino-thien-2-yl-acetic acid derivatives and their use in the treatment of migraine and pain
Compounds of formula I, or a pharmaceutically acceptable salt thereof, The compounds of the present invention are suitable for the treatment of pain and migraine. Also disclosed are method for...
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6770664 |
Bicyclic heterocyclic substituted phenyl oxazolidinone antibacterials, and related compositions and methods
Bicyclic heterocyclic substituted phenyl oxazolidinone compounds of the formula: wherein Y is a radical of Formulae II or III: in which the substituents have the meaning indicated in the...
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6759428 |
Indole nitriles
Compounds of the formula (I) wherein m, n, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as described herein, together with methods for making the compounds and using the compounds for treatment of...
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6743817 |
Substituted fused pyrroleimines and pyrazoleimines
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R 1 and R 2 are defined herein. These compounds are highly selective agonists,...
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6740654 |
Squaric acid derivatives
Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L 2 is a covalent bond or an atom or group —O—,...
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6740647 |
Thrombin inhibitors
Novel five-membered heterocyclic amidines, their preparation and use as competitive inhibitors of trypsin-like serine proteases, especially thrombin and kininogenases such as kallikrein....
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6730312 |
Pesticidal composition for seed treatment
The present invention provides an at least quaternary composition for controlling insects or representatives of the order Acarina and microorganisms, which composition comprises: (A) an...
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6726937 |
Antifungal composition
The present invention provides use of a composition containing 2-n-octyl-4-isothiazolin-3-one and N-n-butyl-1,2-benzisothiazolin-3-one for providing antifungal efficacy to a wood preservative...
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6716843 |
Alpha-amino acid sulphonyl compounds
Compound of formula (I): wherein: represents an optionally substituted, 5-membered, nitrogen-containing heterocycle, R 1 represents hydrogen, alkyl, acyl, prolyl, alanyl, histidylprolyl or...
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6716837 |
Heterocyclic compounds for the treatment of migraine
Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently...
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6706745 |
Biphenylamidine derivatives
The present invention relates to a biphenylamidine derivative of the general formula (1): or a pharmaceutically acceptable salt thereof, which is a novel compound functioning as a clinically...
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6689770 |
Aryl sulfonyls as factor Xa inhibitors
The present application describes aryl sulfonyls of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein D, E, and M are defined below, are effective factor Xa...
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6649645 |
Combination therapy of radiation and a COX-2 inhibitor for treatment of neoplasia
The present invention provides methods to treat or prevent neoplasia disorders in a mammal using a combination of radiation therapy and a cyclooxygenase-2 inhibitor.
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6630487 |
Treatment of insulin resistance with growth hormone secretagogues
This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, where the variables are defined in...
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6589973 |
Preparation of selective cyclooxygenase II inhibitors
A clear, stable novel pharmaceutical preparation of selective cyclooxygenase II inhibitors (COX 2) inhibitors in the parenteral form for the treatment of pain & inflammatory conditions arising...
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6589751 |
Immonological detection of the homocystamide adduct and a thiolactone immunoassay for endogeneous homocysteine
An antibody specific for homocystamide adducts is disclosed. In a preferred embodiment of the present invention, the antibody is used to evaluate the level of homocysteine in a biological sample.
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6552062 |
Indazole derivatives with 5-HT2 receptor activity
A chemical compound of formula (I) wherein R 1 to R 3 are independently selected from hydrogen and alkyl; R 4 to R 7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl,...
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6552051 |
Energetic nitramine-linked azoles and related compounds as oxidizers, initiators and gas generators
Novel compounds are provided having the structural formula R[—N(NO 2 )—L—R 1 ] n wherein R, L, R 1 and n are defined herein. The compounds are useful in a variety of contexts, but are...
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6545037 |
Benzenesulfonamide compounds
A compound of formula (I): which is useful as a TXA 2 and 5-HT 2 receptor and pharmaceutical compositions containing the same.
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6534534 |
Pharmaceutical composition active in reducing production of MCP-1 protein
The present application relates to a method of treating atherosclerosis by administering to a patient a compound of formula: and/or salts thereof with pharmaceutically acceptable organic or...
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6534504 |
Indazolyloxy propanolamines for improving livestock production
Disclosed is compound represented by Structural Formula (I), wherein Ring A, Ring B and Ring C are independently substituted or unsubstituted. R1 and R2 are independently a C1-C4 straight chained...
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6521656 |
Remedies for male sterility
Efficacious remedies for male sterility which are in the form of preparations containing as the active ingredient an adenosine A 1 antagonist.
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6518294 |
Fused pyrazolyl compounds
A fused pyrazolyl compound of the following formula: wherein each of Ar 1 , Ar 2 , and Ar 3 , independently, is phenyl, thienyl, pyrrolyl, or furyl, optionally substituted with halo, alkyl,...
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6518266 |
1- Aryl-3-thioalkyl pyrazoles, the synthesis thereof and the use thereof as insecticides
The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I: or a salt thereof, where R 1 represents R 5 O, R 5...
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6509367 |
Pyrazole cannabinoid agonist and antagonists
Disclosed are pyrazole derivatives of formula I: Where R 1 , R 2 , R 3 , and R 4 are defined as in the specification described. These compounds are antagonists of the brain cannabinoid (CB-1)...
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6486203 |
Treating inflammatory diseases of the head and neck with cyclooxygenase-2 inhibitors
A patient with an inflammatory disease of the head and neck is treated with a therapeutic amount of a selective inhibitor of cyclooxygenase-2 or a cyclooxygenase-2 inhibitor from a natural source....
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6476060 |
4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
The present invention relates, among many things, to novel 4,5-dihydro-1H-pyrazole compounds which can be potent antagonists of the cannabis CB 1 -receptor. The compounds have the formula (I) ...
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6472416 |
Sulfonylphenylpyrazole compounds useful as COX-2 inhibitors
The present invention encompasses novel sulfonylphenylpyrazole compounds useful in the treatment of cyclooxygenase-2 mediated diseases.
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6469040 |
Method of using cyclooxygenase-2 inhibitors in the treatment and prevention of neoplasia
This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing and treating neoplasia. In particular, the invention describes the method of preventing and...
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6462068 |
Heterocyclylmethyl-substituted pyrazole derivatives
The present invention relates to new heterocyclylmethyl-substituted pyrazole derivatives, processes for their preparation and their use as medicaments, in particular as medicaments for treatment of...
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6458823 |
Diaminopyrazoles
This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R 1 and R 2 are...
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6451834 |
Indeno&lsqb 1,2-c&rsqb -, naphtho&lsqb 1,2-c&rsqb - and benzo&lsqb 6,7&rsqb cyclohepta&lsqb 1,2-c&rsqb pyrazole derivatives
Chemical compounds that are derivatives of indeno[1,2-c]-, naphtho[1,2-c]- and benzo[6,7]cyclohepta[1,2-c]pyrazole are inhibitors of tyrosine kinase activity. Several of the tyrosine kinases, whose...
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6448242 |
Cyclic amide compounds
The invention relates to compounds represented by the following general formula (1): wherein A is an aromatic compound which may be substituted, or the like, B is a nitrogen atom or CH, X is a...
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6436978 |
Guanidinylamino heterocycle compounds useful as α-2 adrenoceptor agonists
This invention involves compounds having the following structure: as described in the Claims; and enantiomers, optical isomers, stereoisomers, diastereomers, tautomers, addition salts,...
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6432995 |
Aromatic heterocyclic compounds and their use as anti-inflammatory agents
Novel aromatic heterocyclic compounds inhibit cytokines production involved in immunoregulation and inflammation such as interleukin-1 and tumor necrosis factor production. The compounds are...
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6426341 |
Treatment for diabetic complications
This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or...
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6414011 |
Aryl substituted pyrazoles, and pyrroles, and the use thereof
This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R 5 -R 13 are set in the specification. The...
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6414009 |
Heterocyclylmethyl-substituted pyrazol derivatives
The present invention relates to new heterocyclylmethyl-substituted pyrazole derivatives, processes for their preparation and their use as medicaments, in particular as medicaments for treatment of...
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6413957 |
Methods of inhibiting cell proliferation using indeno &lsqb 1,2-c&rsqb pyrazol-4-ones
The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases,...
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6407103 |
Indeno &lsqb 1,2-c&rsqb pyrazol-4-ones and their uses
The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases,...
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6403630 |
Treating cancers associated with overexpression of HER-2/neu
Cancers associated with overexpression of HER-2/neu are treated with a selective inhibitor of cyclooxygenase-2 as the sole treating agent or said inhibitor in combination regimen with HERCEPTIN®...
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6399612 |
Heteroaryl butyric acids and their derivatives as inhibitors of matrix metalloproteinases
Heteroaryl butyric acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix...
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RE37729 |
4-Heteroaryl-1-piperidinealkylamines and derivatives thereof and their therapeutic utility
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a...
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