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Class 546/226 - At 1-position


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the group is bonded directly to the piperidine
No. of patents: 576
Last issue date: 07/26/2011


1                      
NumberTitleIssue Date
7985861Piperidinyl derivatives as modulators of chemokine receptor activity
The present application describes substituted piperidinyl modulators of MIP-1α or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as wel...
07/26/2011
7943775Small molecules for imaging protein-protein interactions
A tissue is imaged to detect the presence of amyloid deposits or other target proteins prior to their aggregation into plaques, with the assistance of the administration of a labeled bifunctional compound of which one functionality binds to the target protein and th...
05/17/2011
7485728Colorant compounds
A compound of the formula wherein R1, R2, R3, R4, R5, R6, R, Y, CA, A−, m and n each, independently of the others are as defined herein. ...
02/03/2009
7435851Puleganic amides
The present invention provides substituted puleganic amides and compositions thereof, which are both useful as a topical treatment for skin, such as a repellant for insects and arthropods. ...
10/14/2008
7425641Carboxylic acid amides, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to carboxylic acid amides of general formula wherein R1 to R5, Ar, m and n are defined as in claim 1, the tautomers, stereoisomer...
09/16/2008
74109711,2-di(cyclic)substituted benzene compounds
A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and is useful as a therapeutic or prophylactic agent for various ...
08/12/2008
7390905Piperidine compound and process for preparing the same
The present invention relates to a piperidine compound represented by the formula [I]: wherein Ring A represents an optionally substituted benzene ring, Ring B represents an optionally substituted b...
06/24/2008
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
7378440Substituted benzoylureido-o-benzoylamides, process for their preparation and their use
The invention relates to substituted benzoylureido-o-benzoylamides and to their physiologically tolerated salts and physiologically functional derivatives. The invention relates to compounds of the formula I in which...
05/27/2008
7361666Heterocyclic analgesic compounds and methods of use thereof
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-couple...
04/22/2008
7358251N-sulfonylurea apoptosis promoters
Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds. ...
04/15/2008
7351742Sulfonamide derivatives for the treatment of diseases
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the ...
04/01/2008
7351721Amino acid derivatives and pharmaceutical composition comprising, as active ingredients, them
The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-...
04/01/2008
7323563Hydroxamic acid derivatives as antibacterials
A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily accepta...
01/29/2008
7309714Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved...
12/18/2007
7288676Arylphenyl-substituted cyclic ketoenols
The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulph...
10/30/2007
7285568Biaromatic compounds which activate PPARgamma type receptors and cosmetic/pharmaceutical compositions comprised thereof
Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the field...
10/23/2007
7262208Hydroxypropyl amides for the treatment of Alzheimer's disease
The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the...
08/28/2007
7259157N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain. ...
08/21/2007
7253171Urea derivatives as integrin α4 antagonists
Novel antagonists of ∝4β1 integrin and/or ∝4β7 integrin of the general Formula I: wherein R1, R2, R5, L1, L2, Rb, W and Z are as defined in any one of claims 1 to 13, A represents —CH— or a nitrogen atom, and p is from 0 to 4. ...
08/07/2007
7247730Process for the preparation of dexmethylphenidate hydrochloride
The present invention provides a new and efficient process for the preparation of the dexmethylphenidate hydrochloride with high optical purity, the process comprising: (a) reacting a solution of threo-N-Boc-ritalinic acid with (S)...
07/24/2007
7247748Amide compounds and methods of using the same
Disclosed is a compound having the formula (I) pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are ...
07/24/2007
7244766Sulfonamide derivatives for the treatment of diseases
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds accord...
07/17/2007
7241810Formamide derivatives for the treatment of diseases
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds accord...
07/10/2007
7241757Amidino derivatives and their use as thrombin inhibitors
There is provided compounds of formula I wherein R1, Rx, Y, Ry, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases...
07/10/2007
7238709Therapeutic carbamates
This invention relates to hindered carbamate derivatives that are muscarinic receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds. ...
07/03/2007
7132539Melanocortin receptor ligands
The present invention relates to compounds which comprise a nitrogen-containing ring scaffold substituted by an R1 alkyl units selected from the group consisting of C1–C12 linear or branched alkyl, C3–C8 cyc...
11/07/2006
7109243Inhibitors of cathepsin S
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present inven...
09/19/2006
7105471Arylphenyl-substituted cyclic ketoenols
The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulph...
09/12/2006
7091354Processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto
Novel processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto. The compounds prepared by the present processes may be useful, for example, as antagonists to the mu, kappa and delta opioid receptors, and thereby may be useful...
08/15/2006
7087749Substituted piperidine compounds and methods of their use
Certain 4-aryl-piperidine compounds, including N-substituted 9β-substituted-5-(3-substituted-phenyl)morphans and N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines, pharmaceutical compositions, and methods of their use, inter alia, as opi...
08/08/2006
7084138Active ingredient combinations with insecticidal and acaricidal properties
The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the gro...
08/01/2006
7060692Active ingredient combinations comprising insecticidal and acaricidal properties
The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the gro...
06/13/2006
7053057Caspase inhibitors and uses thereof
This invention provides caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CHN2
05/30/2006
7049330Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents
This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula
05/23/2006
7030115N-sulfonylurea apoptosis promoters
Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds. ...
04/18/2006
7015235Acylated piperidine derivatives as melanocortin-4 receptor agonists
Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment...
03/21/2006
7012084Acylated piperidine derivatives as melanocortin-4 receptor agonists
Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevent...
03/14/2006
7001905Substituted diarylamines as MEK inhibitors
Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are us...
02/21/2006
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
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