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Class 544/138 - Oxadiazole ring (including hydrogenated)


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the five-membered hetero ring consists
No. of patents: 81
Last issue date: 01/27/2009


1      
NumberTitleIssue Date
7482448Compounds and compositions as cathepsin inhibitors
Novel inhibitors of cathepsin S, K, B, and L, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making. ...
01/27/2009
7390804N-containing five-membered ring compounds and pharmaceutical agents comprising the same as active ingredient
An N-containing five-membered ring compound of formula (I) wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity aga...
06/24/2008
7348427Antipathogenic benzamide compounds
Antipathogenic benzamide compounds having the formula wherein at least one of the R1 groups is F, Cl, CN or CF3 and R2, R3, Y, Z, m, and n are as defined herein. ...
03/25/2008
7226921Compounds and compositions as cathepsin S inhibitors
The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making. ...
06/05/2007
7220745Heterocyclic compounds useful to treat HCV
The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication a...
05/22/2007
72146943-ox(adi)azolylpropanohydroxamic acids useful as procollagen C-proteinase inhibitors
Compounds of formula (I): wherein the substituents are as defined herein, and their salt, solvates, and prodrugs are procollagen C-proteinase (PCP) inhibitors useful in treating conditions mediated by PCP. ...
05/08/2007
7151175Propenecarboxylic acid amidoxime derivatives, a process for the preparation thereof, and pharmaceutical compositions containing the same
The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suit...
12/19/2006
7148219Biaryl heterocyclic compounds and methods of making and using the same
The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety th...
12/12/2006
7064123Compounds and compositions as cathepsin inhibitors
The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making. ...
06/20/2006
7041685Substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present i...
05/09/2006
7030116Compounds and compositions as cathepsin inhibitors
The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making. ...
04/18/2006
6992083Benzoxazol derivatives
The invention relates to compounds of formula wherein R is phenyl, unsubstituted or substituted by halogen or —CH2N(CH3)(CH2)nOCH3
01/31/2006
6977256Compounds and compositions as cathepsin S inhibitors
The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making. ...
12/20/2005
68973063-heterocyclylpropanohydroxamic acids
Compounds of formula (I): and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by P...
05/24/2005
6852719Glucocorticoid receptor modulators
The present invention provides non-steroidal compounds of Formula I, including prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocor...
02/08/2005
6730671Compounds useful as reversible inhibitors of cathespin S
Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.
05/04/2004
6617323Amino-substituted compounds useful as inhibitors of IMPDH enzyme
The present invention discloses compounds useful in treating or preventing IMPDH-associated disorders, such as transplant rejection and autoimmune diseases, having the formula (I), ##STR1## wherein X is --C(O)--, --C(S)--, or --S(O)2 --; A is a...
09/09/2003
6608057Compounds useful as reversible inhibitors of cathepsin S
Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds ##STR1##...
08/19/2003
6576630Compounds and compositions as protease inhibitors
The present invention relates to novel alkanoyl-substituted heterocyclic derivatives which are cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making....
06/10/2003
6566509Multivalent macrolide antibiotics
Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptogramins, tetracycline and/or other compounds at which bind to bacterial ribosomal RNA and/or to one or more proteins involved i...
05/20/2003
6395897Nitrile compounds useful as reversible inhibitors of #9 cathepsin 5
Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds. ##STR1##...
05/28/2002
6277872Oxadiazoles, processes for their preparation and their use as medicaments
The invention relates to oxadiazole derivatives of general formula (I) ##STR1## wherein X, Y, Z and R1 are defined as described in the specification and claims, processes for preparing them and their use as pharmaceutical compositions....
08/21/2001
6255304Oxazolidinone antibacterial agents having a thiocarbonyl functionality
The present invention provides compounds of Formula 1 ##STR1## or pharmaceutical acceptable salts thereof wherein A, G and R, are as defined in the claims which are antibacterial agents....
07/03/2001
6100259Cannabinoid receptor modulators
Novel pyrazole derivatives are provided which are cannabinoid receptor modulators. ##STR1##...
08/08/2000
6087359Thioaryl sulfonamide hydroxamic acid compounds
A thioaryl sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated thioaryl sulfonamide hydroxamic acid compound in a MMP enzyme-inhi...
07/11/2000
6051572Azetidine, pyrrolidine and piperidine derivatives
A class of azetidine, pyrrolidine and piperidine derivatives, substituted by inter alia a phenylmorpholinyl, phenylpiperidinyl or benzimidazolone moiety, are selective agonists of 5-HT1 -like receptors, being potent agonists of the human 5-HT
04/18/2000
5965579Substituted 1-phenyl-3-pyrazolecarboxamides active on neurotensin receptors, their preparation and pharmaceutical compositions containing them
The invention relates to compounds of the formula: ##STR1## Compounds of the above formula have a great affinity for the neurotensin receptors....
10/12/1999
5914351Anti-viral aromatic hydrazones
Compounds of the formula ##STR1## wherein Q is a hydrazone derivative; R1 is hydrogen, halogen, alkyl or alkoxy; R2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; a...
06/22/1999
5877316Morpholine derivatives, compositions containing them and their use as therapeutic agents
The present invention relates to compounds of formula (I), wherein R1 and R4 represent hydrogen, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkyl...
03/02/1999
5854179Sulfur-substituted phenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators
Sulfur-substituted phenylsulfonylureas; processes for their preparation and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof ##STR1## in which R*, R1, R2, R3, X, Y, Z, W, n...
12/29/1998
5852011Benzimidazole derivatives
Disclosed are compounds represented by the following chemical formula (I) and pharmacologically acceptable salts thereof which are novel compounds useful as anticancer agents, antiviral agents or antimicrobial agents. ##STR1##...
12/22/1998
5840721Imidazole derivatives as MDR modulators
The present invention relates to polysubsituted imidazole having formula 1 ##STR1## These compounds are useful for restoring the sensitivity of multidrug resistant cells to cancer chemotherapeutic agents....
11/24/1998
58377024-arylamino-benzopyran and related compounds
Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is alkyl, Y is a single bond, --CH2 --, --C(O)--, --O--, --S-- or --N(R8)-- where R8 is hydrogen, alkyl, haloalkyl, aryl, a...
11/17/1998
5801170Heterocyclic biphenylylamides useful as 5HT1D antagonists
A compound of formula (I) or a salt thereof: ##STR1## wherein P is a 5 to 7 membered heterocyclic ring selected from the group consisting of thienyl, furyl, pyrrolyl, triazolyl, diazolyl, tetrazolyl, imidazolyl, oxadiazolyl, isothiazolyl, isoxazolyl,...
09/01/1998
5665746Mono- and bicyclic DNA gyrase inhibitors
The present invention relates to a compound of the formula ##STR1## wherein X1, R1, R2, OP, R3, R4, R5, R6, and R0 are as described herein, and their pharmaceutically ...
09/09/1997
5589473Mono- and bicyclic DNA gyrase inhibitors
The present invention relates to a compound of the formula ##STR1## wherein X1, R1, R2, OP, R3, R4, R5, R6, and R0 are as described herein, and their pharmaceutically ...
12/31/1996
5403840Inclusion complexes of N-ethoxycarbonyl 1-3-morpholino-sydnonimine or salts formed with cyclodextrin-derivatives, preparation thereof and pharmaceutical compositions containing the same
The invention relates to inclusion complexes of N-ethoxycarbonyl-3-morpholino-sydnonimine or its salts formed with a cyclodextrin derivatives, preparation thereof and pharmaceutical compositions containing the same. The inclusion complex of N-ethoxycarbon...
04/04/1995
53569161,2,4-oxadiazole derivatives having monoamine oxidase B enzyme-inhibitory activity
A 1,2,4-oxadiazole derivative is represented by the following general formula (I): ##STR1## wherein R1 represents a lower alkyl or cycloalkyl group, a lower alkyl group substituted with a halogen atom, a lower alkylamino group or a ph...
10/18/1994
5332742Renin inhibitors
A renin inhibiting compound of the formula: ##STR1## wherein R1 is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-l-oxo-4-piperazinyl, 2-oxo-4-piperazinyl, 4-morpholinyl, 4-thiomorpholinyl or 1-methyl-4-homopiperazinyl; R2 is b...
07/26/1994
5225548Indophenol dyes and thermal transfer thereof
Indophenol dyes of the formula ##STR1## where X is nitrogen or the radical CH, Q is a five-membered heterocyclic radical, and K is a radical of an aniline, aminonaphthalene, aminoquinoline or aminothiazole derivative, and the radical A can be benzofused, ...
07/06/1993
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