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Class 546/126 - Additional polycyclo ring system having the additional hetero ring as one of the cyclos


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional hetero ring is one of the
No. of patents: 134
Last issue date: 04/24/2012


1        
NumberTitleIssue Date
8163920Quinolinone-carboxamide compounds as 5-HTreceptor agonists
The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 re...
04/24/2012
8153798Indole- and benzimidazole amides as hydroxysteroid dehydrogenase inhibitors
The use of substituted amides of structure (I) for modulating the activity of 11 β-hydroxysteroid dehydrogenase type 1 (11 βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in t...
04/10/2012
7994323Chromen-2-one derivatives
This invention relates to novel chromen-2-one derivatives useful as starting material for synthesis of pharmaceuticals. On other aspects the invention relates to a method of preparing the chromen-2-one derivatives of the invention. ...
08/09/2011
7982042Thiozanthene derivatives as delta-opioid modulators
The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic δ-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of ...
07/19/2011
7897773Urea derivatives of tropane, their preparation and their therapeutic application
The present invention is related to a compound of formula (I) wherein R1a, R1b, R1c, R1d, R2a, R2b, R3, R4, p, r and are as defined he...
03/01/2011
7674908Indazole-carboxamide compounds as 5-HTreceptor agonists
The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 recep...
03/09/2010
7589207Cyclohexyl compounds as CCR5 antagonists
The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an...
09/15/2009
7531661Indane compounds as CCR5 antagonists
The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an...
05/12/2009
7429601Esters of hydroxyl-substituted nitrogen heterocycles, processes for the preparation thereof as well as the use thereof as pharmaceutical compositions
The present invention relates to new compounds of general formula 1 wherein X− and the groups A, B, R, R1, R2, R3, R3′, R4, R4′, Rx
09/30/2008
7419989Indazole-carboxamide compounds
The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 recep...
09/02/2008
7405224Xanthenecarboxylates, processes for preparing them, and their use as pharmaceutical compositions
Xanthenecarboxylates of formula 1 wherein: A is a group selected from X− is an anion with a single negative charge; R is hydro...
07/29/2008
7381723Azabicyclylmethyl derivatives of 7,8-dihydro-1,6,9,-trioxa-3-aza-cyclopenta[a]naphthalene as 5-HT antagonists
Compounds of the formula are useful for treating the cognitive deficits due to aging, stroke, head trauma, Alzheimer's disease or other neurodegenerative diseases, or schizophrenia and are also useful for the treatment of d...
06/03/2008
7381733Tropane derivatives having dopamine reuptake inhibitor activity for the treatment of ischemic diseases
The present invention relates to the use of tropane derivatives having dopamine reuptake inhibitor activity for the treatment of diseases associated with reduced blood flow to the brain or with instances of a temporary break in blood supply to the brain, such as isc...
06/03/2008
7378526Azacyclic ethynyl derivatives
This invention relates to novel azacyclic ethynyl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of...
05/27/2008
7375114Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 re...
05/20/2008
7358244Azabicycloalkane compounds
This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acc...
04/15/2008
7351704Indazole-carboxamide compounds as 5-HTreceptor agonists
The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 recep...
04/01/2008
7329752Carbamate compounds as 5-HTreceptor agonists
The invention provides novel benzoimidazolone-carboxamide-derived carbamate 5-HT4 receptor agonist compounds of formula (I): wherein R1, R2, R3, R4, a, and b...
02/12/2008
7317022Benzoimidazolone-carboxamide compounds as 5-HTreceptors agonists
The invention provides novel benzoimidazolone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4
01/08/2008
7314870Compounds, their preparation and use
The present invention relates to novel compounds that are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention ...
01/01/2008
7307087Treatment of affective disorders by the combined action of a nicotinic receptor agonist and a monoaminergic substance
This invention relates to use of the combined action of a nicotinic acetylcholine receptor agonist and a monoaminergic substance for the treatment of affective disorders, as well as to pharmaceutical compositions comprising these substances and chemical substances f...
12/11/2007
7279488Imidazopyridine-derivatives as inducible no-synthase inhibitors
The compounds of Formula (I) in which R1, R2, R3, R4, R5 and A have the meanings as given in the description are novel effective iNOS inhibitors. ...
10/09/2007
7270932Imaging composition and method
Imaging compositions and methods of using the compositions are disclosed. The imaging compositions are sensitive to low levels of energy such that upon application of the low levels of energy the compositions change color or shade. The compositions may be used in me...
09/18/2007
7268232Androgen receptor modulators and method of treating disease using the same
Disclosed herein are bicycloaryl compounds of Formula (I) that selectively modulate nuclear receptors, preferably the androgen receptor, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, and methods of treating disease comprising administering...
09/11/2007
7223519Imaging compositions and methods
Imaging compositions and methods of using the compositions are disclosed. The imaging compositions are sensitive to low levels of energy such that upon application of the low levels of energy the compositions change color or shade. The compositions may be applied to...
05/29/2007
7217716N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists
Compounds represented by Formula (I): (I) or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain ...
05/15/2007
7217721Tropane derivatives useful in therapy
The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, espe...
05/15/2007
7148236Modulators of acetylcholine receptors
The present invention relates to compounds that modulate neurotransmission by promoting the release of neurotransmitters such as acetylcholine, dopamine and norepinephrine. More particularly, the present invention relates to thio-bridged aryl compounds that are capa...
12/12/2006
7144676Imaging compositions and methods
Imaging compositions and methods of using the compositions are disclosed. The imaging compositions are sensitive to low levels of energy such that upon application of the low levels of energy the compositions change color or shade. The compositions may be applied to...
12/05/2006
7094784High affinity ligands for nociceptin receptor ORL-1
Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1
08/22/2006
7071209Process for preparing a pharmaceutically active compound (granisetron)
The invention relates to a process for preparing granisetron, or a pharmaceutically acceptable salt thereof, which comprises: a) cyclisation of a compound of formula (I) in an inert solvent and at a temperature between 0–100° C., in the presence of a strong acid,...
07/04/2006
70455228-Azabicyclo[3.2.1]oct-2-ene and -octane derivatives technical field
The present invention relates to novel 8-azabicyclo[3.2.1]oct-2-ene and -octane derivatives which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful ...
05/16/2006
7041674Carbamic acid esters with anticholinergic activity
A compound of formula 1 wherein X−, A, R1, R2, R3, and R4 may have the meanings given in the claims and in the specification, processes for preparing them, their...
05/09/2006
7041667CCR5 modulators
Compounds of Formula 1 [Region α]—[Region β]—[Region γ]—[Region δ]  (1) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...
05/09/2006
7022259Liquid crystal compounds, preparation thereof, and composition containing the same
A liquid crystal compound with high helical twisting power, a method for preparing the same, and a liquid crystal composition containing the same. The liquid crystal compounds include cyclic group chain structures similar to the liquid crystal to serve as the core s...
04/04/2006
6979698Method of treating cognitive deficits in learning and memory
The treatment of learning, memory, and age-related memory disorders includes administration of a nicotine antagonist. The preferred nicotine antagonists are mecamylamine, a mecamylamine analog, or a mecamylamine stereoisomer. The effective amount of the nicotine ant...
12/27/2005
69649728-Azabicyclo(3,2,1)oct-2 ene and octane derivatives as cholinergic ligands at nicotinic ACh receptors
The invention disclosed herein relates to novel a 8-azabicyclo[3.2.1]oct-2-ene compound of Formula II, wherein R is hydrogen, methyl, ethyl or benzyl; and R1 is 3-thienyl, 2-thienyl...
11/15/2005
6897207Azaindoles
The invention is directed to physiologically active compounds of general formula (I): and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds...
05/24/2005
6894041Oxazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula:
05/17/2005
6855724Tropane derivatives useful in therapy
The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, especially...
02/15/2005
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