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Class 546/230 - Cyano attached indirectly to the piperidine ring by nonionic bonding


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the -C N group is attached indirectly
No. of patents: 194
Last issue date: 06/03/2008


1          
NumberTitleIssue Date
7381721Substituted piperidine compounds
3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as anta...
06/03/2008
7259173Derivatives of 3-phenyl-n-(2-(4-benzyl)-piperidin-1-yl)-ethyl)-acrylamid with ccr-3-receptor antagonistic activity for use in the treatment of inflammations and allergic conditions
This invention relates to organic compounds of formula I, in which Ar1 is unsubstituted phenyl substituted by one or more halogen atoms; Ar2 is unsubstituted phenyl or phenyl substituted by ...
08/21/2007
7256312Method for producing aminoalkoxy benzylamines and aminoalkoxy benzonitriles as intermediates
The invention relates to a process for preparing 4-[aminoalkoxy]benzylamines of the general formula (I) by catalytically hydrogenating 4-[aminoalkoxy]benzonitriles of the general formula (II) ...
08/14/2007
7074820Amidino derivatives and their use as thrombin inhibitors
There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like protease...
07/11/2006
7015218Amide compounds and medicinal use thereof
The present invention relates to a compound of the formula wherein R1 is substituted aryl, heteroaryl and the like, R2 and R3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q...
03/21/2006
6998488Process and intermediates for the preparation of 4-aryl piperidines
A novel process is provided for the preparation of 4-aryl piperidines, and the useful intermediates obtained therein. These compounds are intermediates for the synthesis of melanocortin-4 receptor (MC-4R), which are useful for the treatment of disorders such as obes...
02/14/2006
6995283Benzophenones as inhibitors of reverse transcriptase
The present invention is directed to beazophenone compounds useful in the inhibition of HIV reverse transcriptase, particularly its resistant varieties. ...
02/07/2006
6992037Precious metal catalyst for debenzylation
One aspect of the invention relates to catalyst composite containing a metal catalyst and a specifically defined carbon support containing a carbonaceous material. For example, the carbon support may have a total pore surface area of about 800 m2/g or mor...
01/31/2006
6903120Modulators of dopamine neurotransmission
New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, O...
06/07/2005
6887889Aryl and biaryl piperdines with MCH modulatory activity
In one embodiment, this invention provides a novel class of compounds as antagonists of the MCH receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations compr...
05/03/2005
6753336Melanin concentrating hormone receptor ligands
Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds ...
06/22/2004
6642386N-(4-carbamimidoyl-phenyl)-glycine derivatives
The invention is concerned with water soluble N-(4-carbamimidoyl-phenyl)-glycine derivatives of formula (I) ##STR1## wherein R1 to R4 and n are as defined in the description and in the claims, as well as physiologically acceptable sa...
11/04/2003
6642239Dipeptide nitrile cathepsin K inhibitors
Dipeptide nitrile Cathepsin K inhibitors of formula I, and pharmaceutically acceptable salts or esters thereof: ##STR1## In which R1 and R2 are independently H or C1 -C7 lower alkyl, or R1 and R
11/04/2003
6605623N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): ##STR1## or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases....
08/12/2003
6562965Convergent synthesis of ଱-aryl-ଲ-ketonitriles
The present invention relates to processes for the production of ଱-aryl-ଲ-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) rece...
05/13/2003
6552022Benzamide derivatives and their use as ApoB-100 secretion inhibitors
The invention relates to therapeutic benzamide compounds of formula (I) ##STR1## wherein A, X, Z, R1, Y, R2, R3, are as defined herein, and physiologically acceptable salts, solvates or derivatives thereof. The present inv...
04/22/2003
6538137Cyanobiphenyl derivatives
Intermediates represented by the following formula: ##STR1## (wherein R1 is a hydrogen atom, an alkyl group, an aryl group, an aralkyl group or the like; X is a carboxyl group, an alkoxycarbonyl group, an aryloxycarbonyl group, an aralkoxycarbo...
03/25/2003
6486180N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): ##STR1## or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases....
11/26/2002
6458812Muscarinic antagonists
Amide derivatives of 1,4 di-substituted piperidine compounds of the formula: ##STR1## or a pharmaceutically acceptable salt, ester or solvate thereof, wherein R1 is optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or heteroar...
10/01/2002
64410012-substituted-4-nitrogen heterocycles as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): ##STR1## or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases....
08/27/2002
6358979N-cyclopentyl modulators of chemokine receptor activity
The present invention is directed to compounds of the formula I: ##STR1## (wherein R1, R3, R4, R5, R6, R7, R8, X, n, x and y are defined herein) which are useful as modulators of chem...
03/19/2002
6313097Antagonists of calcitonin gene-related peptide
Compounds of the formula (I) ##STR1## wherein A, R, R1, R2, X1, X2, X3, and Y are as defined herein, and the tautomers and the pharmaceutically acceptable salts thereof, including pharmaceutical compo...
11/06/2001
6303652BTK inhibitors and methods for their identification and use
The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors....
10/16/2001
6303637Heterocyclic potassium channel inhibitors
The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like. ##STR1##...
10/16/2001
6294575BTK inhibitors and methods for their identification and use
The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors....
09/25/2001
6231786Fluorinated azoles, and their use in liquid-crystalline mixtures
In the fluorinated azoles of the formula (I) R1 (--A1)a --T--(A2 --)b (M--A3 --)c R2 (I) the symbols and indices have -the following meanings: T is undirected and is 4-fluorot...
05/15/2001
6221898Amidino derivatives and their use as thrombin inhibitors
There is provided compounds of formula I, ##STR1## wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in partic...
04/24/2001
6160010BTK inhibitors and methods for their identification and use
The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors....
12/12/2000
6143896Process for the alkylation of alkyl-or benzylcyanogen derivatives in the presence of trialkylamines or trialkylphosphines
A process for the alkylation of compounds of the formula II ##STR1## where the reaction with the alkylating agent is carried out in the presence of a base and a trialkylamine and/or trialkylphosphine....
11/07/2000
61243234-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists
Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs are selective active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such...
09/26/2000
6107508Convergent synthesis of ଱-aryl-ଲ-ketonitriles
The present invention relates to processes for the production of ଱-aryl-ଲ-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) rece...
08/22/2000
6008358Process for the preparation of piperidinylidene derivative
Disclosed is a process for economic, safe and simple production of a 2-phenyl-2-(2'-piperidinylidene)acetate derivative at a reduced number of steps in a high yield, which comprises allowing 2,3,4,5-Tetrahydro-6-methoxypyridine and a benzyl cyanide deriva...
12/28/1999
6008220Aromatic keto-acids and their derivatives as inhibitors of matrix metalloproteinases
Aromatic keto-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 metalloproteinases, particularly gelatinase A (72 kD gelatinase) and strome...
12/28/1999
6002009Di-substituted 1,4-piperidine esters and amides having 5-HT4 antagonistic activity
Pharmacologically active novel esters and amides of di-substituted 1,4 piperidine as 5-HT4 antagonists of formula (I) ##STR1## wherein A, X, Y and R have the meanings specified in the description, and a process for their preparation, are d...
12/14/1999
5977141Sulfonamide inhibitors of matrix metalloproteinases
Sulfonamide compounds are described which are inhibitors of matrix metalloproteinases, particularly stromelysin-1 and gelatinase A (72 kD gelatinase). Also described are methods for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aort...
11/02/1999
5932594Muscarinic receptor antagonists
A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein Y is a direct link, --(CH2 --, --(CH2)2 --, --CH2 O-- or CH2 S--; R is --CN or --CONH2 ; and R1 is a group...
08/03/1999
5922763Biphenyl derivatives, pharmaceutical compositions containing these compounds and processes for preparing them
The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts the...
07/13/1999
5792769Guanidino protease inhibitors
Compounds of the formula: ##STR1## wherein R1 --R4, R7 --R8, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically ...
08/11/1998
5777123Process for regioselective substitution of trifluorobenzoate or trifluorobenzonitrile
The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselective...
07/07/1998
57671513,3-(disubstituted) cyclohexan-1-ylidine acetate dimers and related compounds
The present invention relates to novel 3,3-(disubstituted)-cyclohexan-1-ylidene acetate dimers of Formula (I): ##STR1## and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammateor...
06/16/1998
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