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Class 514/374 - 1,3-oxazoles (including hydrogenated)


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the five-membered hetero ring is
No. of patents: 1171
Last issue date: 04/10/2012


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NumberTitleIssue Date
6767918N-(aryl/heteroarylacetyl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or i...
07/27/2004
6762182Converting cox inhibition compounds that are not COX-2 selective inhibitors to derivatives that are COX-2 selective inhibitors
A method of altering specificity of cyclooxygenase-inhibiting compounds that have a COOH moiety by changing the various COOH containing compounds, such as indomethacin, into ester derivatives or into secondary amide derivatives. ...
07/13/2004
6759407Acyclic and cyclic guanidine- and acetamidine derivatives, their preparation and their use as pesticides, ESP as parasiticides
Novel pesticides of formula (I) wherein the substituents, R, R1, R2, R2′, T, U, X and Y are as defined in claim 1, are described. Also described are compositions suitable for use as par...
07/06/2004
6759402Cyclic felbamate derived compounds
The present invention relates to novel felbamate derivatives and their use to treat neurological diseases such as epilepsy and to treat tissue damage resulting form ischemic events. The felbamate derivatives are modified to prevent the formation of metabolites that ...
07/06/2004
6750236Propionic acid derivatives
This invention relates to novel potent PPAR-alpha-activating compounds which are useful in the treatment of diseases such as coronary heart disease. The invention also relates to methods of preparation of PPAR-alpha-activating compounds. ...
06/15/2004
6747049Oxazole derivatives
Compounds of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 and n have the significance given in the specification can be used to treat non-...
06/08/2004
6747047Insecticidal anthranilamides
This invention provides compounds of Formula (1), their N-oxides and agriculturally suitable salts wherein A, B, J, R1, R2, R3 and R4 and n are as defined in the disclosure. Also disclosed are methods for controlling arthr...
06/08/2004
6747028Respiratory syncytial virus replication inhibitors
This invention concerns compounds of formula (I) prodrugs, addition salts, or stereochemically isomeric forms thereof for use as, inter alia, respiratory syncytial virus replication inhibitors; their preparation, composi...
06/08/2004
6743817Substituted fused pyrroleimines and pyrazoleimines
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists...
06/01/2004
6737418Aryl substituted pyrazoles, imidazoles, oxazoles, thiazoles 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 R5-R13 are set in the specification. The invention also i...
05/18/2004
6727238Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated fi...
04/27/2004
6727271Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
Compounds are provided which have the structure wherein Q is C or N, A is O or S, Z is O or a bond, X is CH or N and R1, R2, R2a, R2b, R2c, R3, Y, x, m, a...
04/27/2004
6723740Activator of PPAR delta
Compounds of Formula (I) are disclosed. These compounds selected activators of human PPAR delta. ...
04/20/2004
6716881Carbanilides used as pesticides
The present invention provides carbanilides of formula (I), wherein A, Q, R, X, Z and m are as defined herein. A plurality of processes for preparing these compounds is provided, along with methods of using the compounds...
04/06/2004
6716864Interheteroaryl 7-oxabicyclic [2.2.1]heptane oxazoles as prostaglandin F2α antagonists
The present invention provides novel compounds represented by the general formula I. wherein m, n, X, Y, Z, R, R1 and R2 are as defined in the specification or a pharmaceutically acceptable salt the...
04/06/2004
6716863Heterocyclic compounds their production and use
A compound represented by the formula: wherein m is 1 or 2, R1 is a halogen or an optionally halogenated C1-2 alkyl; one of R2 and R3 is a hydrogen atom and the other is a grou...
04/06/2004
6710063Activators of PPAR delta
Compounds of Formula (1) are disclosed. These compounds include selective activators of human PPAR delta. ...
03/23/2004
6706743β3 adrenergic receptor agonists and uses thereof
The instant invention provides β3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and ...
03/16/2004
6706724Substituted aryl compounds as novel cyclooxygenase-2 selective inhibitors, compositions and methods of use
The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfer...
03/16/2004
6699890Phosphodiesterase 4 inhibitors
PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: ##STR1## wherein R1, R2 , R3 and R4 are as defined ...
03/02/2004
6699860Di-substituted aminomethyl-chroman derivative beta-3 adrenoreceptor agonists
This invention is related to novel di-substituted aminomethyl chroman derivatives which are useful in the treatment of beta-3 receptor-mediated conditions....
03/02/2004
6699886Store operated calcium influx inhibitors and methods of use
The present invention provides store operated calcium influx inhibitor compounds, pharmaceutical compositions, and methods of use. The compounds are useful for treating an inflammatory disease or treating an inflammatory reaction. Preferably, compounds, c...
03/02/2004
6699896Oxazole-aryl-carboxylic acids useful in the treatment of insulin resistance and hyperglycemia
This invention provides compounds having the structure ##STR1## wherein A is OR5, or ##STR2## R1 is alkyl, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, pyridyl, ##STR3## R2 is H, alkyl, or aryl; R3
03/02/2004
6696437Heterocyclically substituted benzimidazoles, the production and application thereof
The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs....
02/24/2004
6696474Antidiabetic agents
Compounds of formula I: ##STR1## wherein X, Y, B, E, J, K, L, Z, and R9 -R12 have any of the meanings described herein, their pharmaceutically acceptable salts, lower blood glucose levels and are useful for treating diseases in m...
02/24/2004
6689794Aromatic sulfone hydroxamates and their use as protease inhibitors
This invention is directed to aromatic sulfone hydroxamates (also known as "aromatic sulfone hydroxamic acids") and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as "matrix metalloprotease" or "MMP") activity and/or aggrecan...
02/10/2004
6685959Pharmaceutical compositions comprising 2-isoxazoles-8-aminotetralin derivatives
The invention relates to novel pharmaceutical compositions comprising 2-isoxazole-8-aminotetralin derivatives. The invention more specifically relates to compositions in the form of a patch comprising a therapeutically efficacious amount of a derivative o...
02/03/2004
6686363Cyclopropyl containing oxazolidinone antibiotics and derivatives thereof
This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as...
02/03/2004
6683078Use of sulfonyl aryl or heteroaryl hydroxamic acids and derivatives thereof as aggrecanase inhibitors
This invention is directed to a process for inhibiting aggrecanase activity. The process comprises administering a therapeutically effective amount of a sulfonyl aromatic or heteroaromatic hydroxamic acid, a derivative thereof, or a pharmaceutically accep...
01/27/2004
6677341(R)-Chiral halogenated substituted heteroaryl benzyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and m...
01/13/2004
6677364Substituted sulfonylphenylheterocycles as cyclooxygenase-2 and 5-lipoxygenase inhibitors
This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation....
01/13/2004
6670358Substituted thioacetamides
The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases....
12/30/2003
6667331Non-peptidyl inhibitors of VLA-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases
There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.0): ##STR1## and p...
12/23/2003
6664281Carboxylic acid derivatives and drugs containing the same as the active ingredient
A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) ##STR1## (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because o...
12/16/2003
6660760Heterocyclic aromatic compounds useful as growth hormone secretagogues
Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocycl...
12/09/2003
6660758Epothilone analogs
Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilizati...
12/09/2003
66607594.5-diaryloxazole compounds with prostaglandin I2 (PGI2) agonistic activity
Heterocyclic compounds of formula (I), wherein R1 is carboxy or protected carboxy, R2 is aryl which may have suitable sustituent(s), R3 is aryl which may have suitable substituent(s), R4 is hydrogen, lower alkyl...
12/09/2003
6656954Sulfonyl divalent aryl or heteroaryl hydroxamic acid compounds
A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroa...
12/02/2003
6653314Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
Compounds are provided which have the structure ##STR1## wherein Q is C or N, A is O or S, Z is O or a bond, X is CH or N and R1, R2, R2a, R2b, R2c, R3, Y, x, m, and n are as defined herein...
11/25/2003
6653309Inhibitors of IMPDH enzyme technical field of the invention
The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for inhibit...
11/25/2003
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