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Class 514/429 - Carbocyclic ring bonded directly to the five-membered hetero ring


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein a carbocyclic ring is bonded directly
No. of patents: 232
Last issue date: 05/08/2012


1            
NumberTitleIssue Date
8173695Kappa selective opioid receptor antagonist
A selective kappa opioid receptor antagonist useful for treating ethanol use disorder withdrawal and anxiety, and/or depression, or schizophrenia as independent comorbid conditions. ...
05/08/2012
7709522Kappa selective opioid receptor antagonist
A selective kappa opioid receptor antagonist, (S)-3-Fluoro-4-[4-[2-(3,5-dimethylphenyl)pyrrolidin-1-yl-methyl]phenoxy]benzamide or a pharmaceutically acceptable salt thereof, useful for treating ethanol use disorder withdrawal, and anxiety and/or depression, or schi...
05/04/2010
7687536Aminocycloalkyl cinnamide compounds for arrhythmia and as analgesics and anesthetics
Aminocycloalkyl cinnamide compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the trea...
03/30/2010
7569599Intermediates for the production of optically active cyclopropylamine derivatives and process for the production of the intermediates
A process for producing an optically active compound represented by formula (4), or a salt thereof, wherein R1 represents a protecting group. ...
08/04/2009
7504432Ester derivatives
This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); ...
03/17/2009
7423059Pharmaceutically active compounds and methods of use
The present invention relates to certain imine-substituted heterocyclic compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or p...
09/09/2008
7419936Optically active 2,5-bisaryl-Δ-pyrrolines and their use as pest control agents
Novel optically active Δ1-pyrrolines of the formula (I) in which R1, R2, R3, R4, and m are each as defined in the description, a plurality of...
09/02/2008
7408071N-aryl pyrrolidine derivatives as beta-secretase inhibitors
There is provided a series of substituted N-aryl pyrrolidine derivatives of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R...
08/05/2008
7399773Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1-pyrrole-3-carboxylic acid and phenylamide
An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight ...
07/15/2008
7396828PI-3 kinase inhibitor prodrugs
The invention provides prodrugs of inhibitors of PI-3 kinase. The compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine. ...
07/08/2008
7368462Melanin concentrating hormone antagonists
The present invention relates to compounds capable of serving as moderators of human and mammalian appetite and as such provide a means for reducing body mass and controlling obesity. ...
05/06/2008
7348356Phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
Disclosed are compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's dis...
03/25/2008
7345082Phosphinic acids
The present invention relates to phosphinic acid derivatives of formula I wherein R1, R2, R3 and R4 are described hereinabove. These compounds can be used in the treatment or prev...
03/18/2008
7332516Geminally di-substituted NSAID derivatives as Aβ42 lowering agents
The present invention encompasses compounds of Formula I (I) or pharmaceutically acceptable salts thereof, wherein A is the base molecule of a propionic acid or acetic acid NSAID, or a derivative thereof, X is â€...
02/19/2008
7329762Prodrugs of mitotic kinesin inhibitors
The present invention relates to phosphate ester prodrugs of dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relate...
02/12/2008
7323490Pyrrole compounds and uses thereof
The invention provides pyrrole-containing compounds and methods of use thereof. Kits and pharmaceutical compositions comprising the pyrrole compounds of the invention are also provided. The compounds and compositions disclosed herein are preferably used in the treat...
01/29/2008
73234927-pyrollyl 9-aminoacyl tetracycline compounds and methods of use thereof
A compound of formula (I): wherein: A represents an aromatic 5 membered heterocycle, optionally containing, in addition to the nitrogen atom indicated in formula (I), one to thr...
01/29/2008
7294647Kappa agonist compounds and pharmaceutical formulations thereof
Compounds having kappa opioid agonist activity, compositions containing them and 5 method of using them as analgesics and pruritic agents are provided. The compounds of formulae I, II, III and IV have the structure: ...
11/13/2007
72562107-amido-isoindolyl compounds and methods of their use
The invention encompasses 7-amido-isoindolyl compounds and methods of using these compounds and compositions in mammals for treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel di...
08/14/2007
7235580Mitotic kinesin inhibitors
The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which c...
06/26/2007
7223744Pharmaceutical formulation comprising dinucleoside polyphosphates and salts thereof
The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a pharmaceutical formulation comprising a hydrolysis-resistant P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from...
05/29/2007
7214701Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ...
05/08/2007
7199081Aqueous compositions for seed treatment
An aqueous composition suitable for applying fungicides to plant propagation materials is provided, comprising water and a blend of the following components, by weight: a) 2–10% of a surface-active agent comprising a1) at least one anionic surfactant;...
04/03/2007
7176229Cyclic AMP-specific phosphodiesterase inhibitors
Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as c...
02/13/2007
7173058Fluoroalkoxy-substituted 1,3-dihydro-isoindolyl compounds and their pharmaceutical uses
The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these comp...
02/06/2007
7160902Amide derivatives and methods of their use
Amide derivatives of the general formulae Ia and Ib: are disclosed. Pharmaceutical compositions containing these compounds, and methods for their use, inter alia, for treating and/or preventing gastrointestinal d...
01/09/2007
7144881Arylcyclopropylcarboxylic amides as potassium channel openers
The present invention provides novel arylcyclopropylcarboxylic amides and related derivatives having the general Formula I wherein R, R1, R2, R3, R4, R5, R
12/05/2006
7105507Cyclohexane derivatives and their use as therapeutic agents
The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R
09/12/2006
7074785Δ-pyrrolines used as pesticides
Novel Δ1-pyrrolines of the formula (I) in which R1, R2, R3, A, R4 and m have the meanings given in the description, a number of proce...
07/11/2006
7056945Selective inhibition of neuronal nitric oxide synthase
Compositions, prodrugs and methods for inhibiting neural Nitric Oxide Synthase (nNOS). By inhibiting nNOS, the compounds, prodrugs and methods of the presnet invention are useable to treat or prevent disorders in human or veterinary patients that are caused, mediate...
06/06/2006
7057053Ion channel modulating compounds and uses thereof
Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatme...
06/06/2006
7053087Aminocycloalkyl cinnamide compounds for arrhythmia and analgesics and anesthetics
Aminocycloalkyl cinnamide compounds (I) are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the ...
05/30/2006
7034051Fused bicyclic carboxamide derivatives and methods of their use
Fused bicyclic carboxamide derivatives are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed. ...
04/25/2006
7034045Monofluoroalkyl derivatives
The present invention provides certain monofluoroalkyl derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders. ...
04/25/2006
70340527-Amido-isoindolyl compounds and their pharmaceutical uses
The invention encompasses 7-amido-isoindolyl compounds and methods of using these compounds and compositions in mammals for treatment, prevention or management of various diseases and disorders. Examples inlcude, but are not limited to, cancer, inflammatory bowel di...
04/25/2006
7026440Branched polymers and their conjugates
The present invention is directed to branched reactive water-soluble polymers comprising at least two polymer arms, such as poly(ethylene glycol), attached to a central aliphatic hydrocarbon core molecule through heteroatom linkages. The branched polymers bear at le...
04/11/2006
6995185Δ1-pyrrolines used as pesticides
Novel Δ1-pyrrolines of the formula (I) in which Ar1, Ar2 and Q are each as defined in the description, a plurality of processes for preparing these substances...
02/07/2006
6992193Sulfonylamino phenylacetamide derivatives and methods of their use
Sulfonylamino phenylacetamide derivatives of the general formula are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed. In certain embodiments, the compounds o...
01/31/2006
6989088Perfluorocyclicamine, constant boiling composition and process for producing the same
A process for producing a perfluorocyclicamine which includes electrolytically fluorinating a triallylamine in anhydrous liquid hydrogen fluoride. A constant boiling composition and process for producing the same is also described. ...
01/24/2006
6960612Kappa agonist compounds, pharmaceutical formulations and method of prevention and treatment of pruritus therewith
Methods for prevention or treatment of pruritus are provided. The methods comprise administering to a patient an effective amount of a kappa opioid receptor agonist compound. The involved kappa opioid receptor agonist compounds are of the type represented by the fol...
11/01/2005
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