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Class 514/426 - Nitrogen bonded directly to the five-membered hetero ring by nonionic bonding


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein nitrogen is bonded directly to the
No. of patents: 271
Last issue date: 04/10/2012


1              
NumberTitleIssue Date
8153681Method of treating epilepsy by administering 5-(4{[(2-fluorophenyl)methyl]oxy}phenyl)prolinamide
The invention provides a compound of formula (I), a solvate, a salt or prodrug thereof, useful in the treatment of diseases and conditions mediated by modulation of use-dependent voltage-gated sodium channels. Methods of treating epilepsy in a mammal are also provid...
04/10/2012
8022099N-benzyl pyrrolidine derivatives
The present invention relates to a compound of formula I wherein Ar, R1, R2, R3, n, and o are as defined herein or to a pharmaceutically active salt, a racemic mixture...
09/20/2011
7919521Five-membered iminocyclitol derivatives as selective and potent glycosidase inhibitors: new structures for antivirals and osteoarthritis therapeutics
Novel 5-membered iminocyclitol derivatives were found to be a potent and selective inhibitors of the glycoprotein processing α- and β-glucosidase which were further found to be active antiviral agents against Japanese encephalitis virus, dengue virus serotype 2 (D...
04/05/2011
7879903Optically active 3-aminopyrrolidine salt, process for production thereof, and method for optical resolution of 3-aminopyrrolidine
An optically active 3-aminopyrrolidine (3AP) salt has a high optical purity which is useful as an intermediate in an industrial production method of an optically active 3AP, an efficient method for producing it, and an efficient industrial method for optical resolut...
02/01/2011
7807707Hair and/or scalp care compositions incorporating amino-oxo-indole-ylidene compounds
A hair and/or scalp treatment composition comprising an amino-oxo-indole-ylidene compound of general formula (I): (I) formula should be here in which: R1, R2, R3 and R4 are each, independently, hydrogen or a monovalent organic group selected from alkyl, alkenyl, alk...
10/05/2010
7714021Pyrrolidin-3-yl compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
The present invention is directed to pyrrolidin-3-yl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is...
05/11/2010
7541379Di(amido-substituted)heteroarene compounds as osteoblastogenesis agents
The present invention relates to di(amido-substituted)-heteroarene compounds and their use as osteoblastogenesis agents. The invention provides a method for inducing osteogenesis in a precursor cell capable of undergoing osteogenesis. ...
06/02/2009
7507760N-type calcium channel blockers
The invention relates to novel 3-amino pyrrolidine derivatives, as well as methods for modulating calcium channel activity and for treating conditions associated with calcium channel function. In particular, the compounds generally contain at least one benzhydril mo...
03/24/2009
7485665Medicinal composition
The present invention relates to an ameliorant for improving the movement of the digestive tract comprising, as an active ingredient, 4-amino-5-chloro-2-methoxy-N-[(2S,4S)-2-hydroxymethyl-4-pyrrolidinyl]benzamide or an acid addition salt thereof which is a metabolit...
02/03/2009
7399776Polyamine compounds for treating chemokine receptor mediated diseases
This invention relates to a method for treating inflammatory diseases or immune diseases, developmental or degenerative diseases, or tissue injuries. The method includes administering to a subject in need thereof an effective amount of one or more compounds of the f...
07/15/2008
7390830Remedies or prophylactics for diseases in association with chemokines
This invention provides remedies or prophylactics for diseases in association with chemokines such as MIP-1 α and/or MCP-1. Namely, remedies or prophylactics for diseases in association with the chemokines such as rheumatoid arthritis or nephritis contain, as the a...
06/24/2008
7388112Immunomodulation with novel pharmaceutical compositions
The synthesis and use of a novel class of tumor necrosis factor (TNFα) inhibitors and immunomodulators are provided. Examples are those having the structures: wherein a, b and c are integers from 0 to 12, X equals NH or CH...
06/17/2008
73817413-amino-2-phenylpyrrolidine derivatives
3-amino-2-phenylpyrrolidine compounds useful as NK-1 antagonists, with pharmaceutical compositions and methods of treatment comprising same, are disclosed. ...
06/03/2008
73484344-substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them
The invention relates to 4-substituted quinoline derivatives of general formula: which are active as antimicrobials, in which: X1, X2, X3, X4 an...
03/25/2008
73296851-Phenyl-2-oxo-3-sulfonylamino-pyrrolidine derivatives and related compounds as factor Xa inhibitors for the treatment of acute vascular diseases
The invention relates to compounds of formula (I): wherein substituents are as defined. ...
02/12/2008
7326729CXCR1 and CXCR2 chemokine antagonists
The present invention is directed to a compound having the general structure of formula (1): useful for the treatment, prevention or amelioration of a CXCR1 or CXCR2 chemokine-mediated disease. ...
02/05/2008
7267826Plant protection agents
The present invention relates to a microbicide composition for plants, containing at least two active ingredient components in an amount producing synergistic activity, together with an appropriate filler, wherein component I is the compound 2-[α-{[(α-methyl-3-tri...
09/11/2007
7262316Process for producing aromatic nitrile compound
A novel process for industrially producing an aromatic nitrile compound represented by the following general formula (3): characterized in that one of an aromatic hydroxymethyl compound, an aromatic alkoxymethyl ...
08/28/2007
7256191Materials and methods for the treatment of depression
The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are metho...
08/14/2007
7250443Pyrrole based inhibitors of glycogen synthase kinase 3
New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed al...
07/31/2007
7244750Active substance combinations having insecticidal and acaricidal properties
The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties. ...
07/17/2007
7232845Active substance combinations comprising insecticidal and acaricidal properties
The invention relates to novel active compound combinations of certain cyclic ketoenols and certain insecticidally active compounds that together have very good insecticidal and acaricidal properties. ...
06/19/2007
7223788Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have...
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
7205289Combinations of active ingredients with insecticidal and acaricidal properties
The invention relates to novel active compound combinations of certain cyclic ketoenols and certain insecticidally active compounds that together have very good insecticidal and acaricidal properties. ...
04/17/2007
7198803Sustained release oral preparations
Medicinal preparations containing a drug 2-amino-3-cyano-5-2(2-fluorophenyl) -4-methylpyrrole wherein the QOL and compliance of patients taking this drug can be improved and an unnecessary increase in the drug concentration in the plasma can be prevented by sustaini...
04/03/2007
7183298Carbamic acid compounds comprising a sulfonamide linkage as HDAC inhibitors
This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S(═O)...
02/27/2007
7126010Benzylcycloalkyl amines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic disease...
10/24/2006
7115754Pyrrolidine derivatives as oxytocin antagonists
The present invention relates to novel pyrrolidine derivative of formula (I), its geometrical isomers, its optically active forms as enantiomers, diastereomers, mixtures of these and its racemate forms, as well as salts thereof, wherein R1 is selected fro...
10/03/2006
7105565Pyrrolcarboxamides and pyrrolcarbothioamides and their agrochemical uses
The invention relates to novel pesticidal pyrrolcarboxamide of the formula (I), wherein X is oxygen or sulfur; R1 is CF3, CF2H or CFH2; R2 is C1–C3alkyl, C1–C3halo...
09/12/2006
7098225Active compound combinations having insecticidal and acaricidal properties
The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties. ...
08/29/2006
7091233Active substance combinations comprising insecticidal and acaricidal properties
The invention relates to novel active compound combinations of certain cyclic ketoenols and certain insecticidally active compounds that together have very good insecticidal and acaricidal properties. ...
08/15/2006
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
7081524O-substituted 1-[(2-carboxylato)pyrrolidin-1-yl]diazen-1-ium-1,2-diolates
The present invention provides O2-substituted 1-[(2-carboxylato)pyrrolidin-1-yl]diazen-1-ium-1,2-diolates (1-[(2-carboxylato)pyrrolidin-1-yl]diazeniumdiolates) of the formula in which R and R22
07/25/2006
7078414Derivatives of 3-guanidinocarbonyl-1-heteroaryl-pyrrole, preparation process and intermediates of this process, their use as medicaments, and pharmaceutical compositions comprising them
The present invention relates to 3-guanidinocarbonyl-1-heteroaryl-pyrrole derivatives of formula (I) wherein R1 to R3 and Ar are as defined herein, pharmaceutical compositions comprising such derivatives, methods of treatment comprising adminis...
07/18/2006
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
7045521Cyclic derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and ...
05/16/2006
7041818DDS compound and method for measurement thereof
A DDS compound comprising a carboxy(C1-4)alkyldextran polyalcohol modified with a saccharide compound and a residue of drug compound bound to the carboxy(C1-4)alkyldextran polyalcohol, and a method for measuring a DDS compound in which a polyme...
05/09/2006
7005439Compounds
The invention provides compounds of general formula (I) wherein m, n, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, process...
02/28/2006
6994866Combinations of active ingredients, which exhibit 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...
02/07/2006
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