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Class 514/253.01 - The additional hetero ring is six-membered consisting of one nitrogen and five carbon atoms


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the additional hetero ring has exactly
No. of patents: 583
Last issue date: 04/10/2012


1                      
NumberTitleIssue Date
8153637Phenyl-alkyl piperazines having TNF-modulating activity, preparation method, and therapeutic use thereof
The present invention relates to phenyl-alkyl piperazines of formula (I): in which A, R1, R2 and R3 are as defined herein, having TNF-modulating activity. The invention also relates to the preparation thereof, pharmaceutica...
04/10/2012
8153636Pyridyl derivatives and their use as therapeutic agents
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): ...
04/10/2012
8138190Diaza heterocyclic amide compounds and their uses
Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7
03/20/2012
8129390Carboxamide, sulfonamide and amine compounds and methods for using the same
Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, ...
03/06/2012
8106055Substituted amide compounds
Substituted amide compounds corresponding to formula I: processes for preparing them, pharmaceutical compositions containing these compounds, and the use of substituted amide derivatives for the preparation of medicaments f...
01/31/2012
8101617Disubstituted ureas and uses thereof in treating heart failure
Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure. ...
01/24/2012
8039473Solid forms of [4-(3-fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl-[5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone
The present invention relates to four distinct crystalline forms and to an amorphous form of [4-(3-Fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-[5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone, and to their use in the preparatio...
10/18/2011
8034815Compounds and method for treatment of cancer
The present invention is directed to a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a ...
10/11/2011
8034816Hydrates and polymorphs of 4-[[(7)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy--(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament
Disclosed are hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, processes for preparing them and their use as pharmaceutical compositions. ...
10/11/2011
8030310Therapeutic agents useful for treating pain
Compounds of formulae: where X is S or O and Ar2, R1, R2, R3, R8, n, m, t, and v are disclosed herein, or a pharmaceutically acceptable salt thereof (a “3-substituted...
10/04/2011
8026242Cyclopropyl amines as modulators of the histamine Hreceptor
Certain cyclopropyl amines are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases. ...
09/27/2011
7964602Biaryl compounds useful as agonists of the Gpr38 receptor
The present invention relates to novel biaryl derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of gastrointestinal disorders....
06/21/2011
7919494Pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound
A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the pres...
04/05/2011
7858628Use of fused nicotinamides to promote neurogenesis
The present invention provides a group of compounds found to increase the number of neurons derived from stem cells for use as a therapeutic agent in neurological conditions or diseases. In one embodiment of the present invention, the compounds are used to detect th...
12/28/2010
7842695Substituted pyrazole compounds
Compounds of formula (I) and salts thereof, in which the following definitions apply: X is N or CH; R1 is H, A, Hal, (CH2)nHet, (CH2)nAr, C3-7-cycloalkyl, CF3, NO2, CN, C(NH)(OH)...
11/30/2010
7799789Heterocyclic substituted pyridine or phenyl compounds with CXCR3 antagonist activity
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general s...
09/21/2010
7795263Pharmaceutical combination for and method of anesthetizing and immobilizing non-domesticated mammals
Non-domesticated mammalian animals are anesthetized and immobilized by injecting an effective amount of an anesthetizing and immobilizing drug comprising pharmaceutically active ingredients of butorphanol tartrate, azaperone tartrate and medetomidine hydrochloride (...
09/14/2010
7776861Therapeutic agents useful for treating pain
A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an ef...
08/17/2010
7776862Pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general s...
08/17/2010
7754723Therapeutic agents useful for treating pain
Compounds of formulae: where Ar1, Ar2, R3, R4, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Nitro(cyano)vinylpiperazine Compound”); compositio...
07/13/2010
7696208Therapeutic agents useful for treating pain
Compounds of formulae: where X is S or O and Ar2, R1, R2, R3, R8, n, m, and t are disclosed herein, or a pharmaceutically acceptable salt thereof (a “3-substituted Py...
04/13/2010
7691861Indolymaleimide derivatives
A compound of formula I wherein R, Ra, Rb, Rc, Rd and Re are as defined in the specification, processes for their production, their uses, in particular in transplantati...
04/06/2010
7683065Pyridines useful as modulators of ion channels
The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of...
03/23/2010
7671055Insecticidal 3-(dihaloalkenyl) phenyl derivatives
Certain novel 3-(dihaloalkenyl)phenyl derivatives have unexpected insecticidal activity. These compounds are represented by formula (I), where R through R5, a, b, D, E, G and U are fully described herein. In addition, compositions comprising an insecticid...
03/02/2010
7648989Indolylmaleimide derivatives as PKC inhibitors
This invention relates to PKC inhibitors which are able to selectively inhibit e.g. the and optionally 0, isoforms of PKC, and their use in particular in transplantation. ...
01/19/2010
7625904Methods for the treatment of sleep disorders
The invention relates to methods for the treatment of a sleep disorder in a mammal comprising administering to said mammal an effective amount of a compound of formula (I): wherein all variables are as defined herein. ...
12/01/2009
76189703-aminocyclopentanecarboxamides as modulators of chemokine receptors
The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokin...
11/17/2009
7612076Piperazinyl-pyridine derivatives
The present invention relates to compounds of formula I wherein R1, R2, X, Y, Z and m are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceu...
11/03/2009
7566718Amine-linked pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general s...
07/28/2009
7528135Pyridine derivatives as H3 antagonists
The present invention relates to compounds of formula I wherein R1, R2 and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical com...
05/05/2009
7524848Diaza heterocyclic amide compounds and their uses
Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7
04/28/2009
7491727Arylpiperazinyl compounds
The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formula I, and synthesis and uses thereof for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclose...
02/17/2009
748564517β-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17β-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing...
02/03/2009
7449466Cyclic aminophenyl sulfamate derivative
This invention provides cyclicamino-phenyl sulfamate derivatives represented by a formula wherein each of R1 and R2 stands for hydrogen or lower alkyl; each of R3 an...
11/11/2008
74494673-aminocyclopentanecarboxamides as modulators of chemokine receptors
The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokin...
11/11/2008
7442692Indanyl-piperazine compounds
A compound selected from those of formula (I): wherein: R3 represents a hydrogen atom, and R1 and R2 together with the carbon atoms carrying them form a be...
10/28/2008
7439360Vanilloid receptor ligands and their use in treatments
Therapeutic benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, ...
10/21/2008
7432269Arylpiperaszine derivatives, to the process for the production thereof and to the use thereof as therapeutic agents
The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent having the property of being selective ligands for the dopamine D3 receptor. Th...
10/07/2008
7429599Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK
This invention generally relates to methods for treating or preventing a condition responsive to JNK inhibition, such as a metabolic condition, comprising administering to a patient in need thereof an effective amount of an Anilinopyrimidine Derivative having the fo...
09/30/2008
7427612Benzoyl-piperazine derivatives
A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in ...
09/23/2008
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