Class 546/125 - Additional hetero ring containing

Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which contain an additional hetero ring.
No. of patents: 150
Last issue date: 10/21/2008

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Number	Title	Issue Date
7439255	Muscarinic acetylcholine receptor antagonists Muscarinic Acetylcholine receptor antagonists and methods of using them are provided. ...	10/21/2008
7435822	3-(diheteroarylmethylene)-8-azabicyclo[3.2.1]octane and 3-((aryl)(heteroaryl)methylene)-8-azabicyclo[3.2.1]octane derivatives This invention is directed to 3-(diheteroarylmethylene)-8-azabicyclo[3.2.1] octane and 3-((aryl)(heteroaryl)methylene)-8-azabicyclo[3.2.1] octane derivatives useful as δ-opioid, μ-opioid, or δ-opioid and μ-opioid receptor receptor modulators. Depending on their ...	10/14/2008
7429601	Esters 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
7410961	2,6-disubstituted piperiddines as modulators The present invention is further directed to compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R16, R17, R	08/12/2008
7381733	Tropane 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
7378526	Azacyclic 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
7358244	Azabicycloalkane 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
7323474	Pyridine derivatives inhibiting angiogenesis and/or VEGF receptor tyrosine kinase The invention relates to pyridine derivatives of formula (I) wherein the substituents and symbols are defined as indicated in the description, processes for the preparation thereof, their usage in the preparation...	01/29/2008
7307087	Treatment 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
7297693	Nitrogen-containing heterocyclic compounds and their use as Raf inhibitors Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. ...	11/20/2007
7276520	Bicyclic piperidine derivatives as melanocortin-4 receptor agonists Certain novel bicyclic 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 prevention o...	10/02/2007
7276521	Muscarinic acetylcholine receptor antagonists Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided. ...	10/02/2007
RE39820	Esters of thienyl carboxylic acids and amino alcohols and their quaternization products Compounds of the formula of which, in exemplary compounds, the thienyl group is attached via the 2-position and; (a) A is 3α-(6β, 7β-epoxy)-tropanyl methobromide and R1 is 2-thieny...	09/04/2007
7241745	Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their m...	07/10/2007
7217716	N-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
7199132	Tropane analogs and methods for inhibition of monoamine transport New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-hydroxyl or ketone substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Ce...	04/03/2007
7192969	Ester 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); ...	03/20/2007
7189737	Cocaine receptor binding ligands A class of binding ligands for cocaine receptors and other receptors in the brain. Specifically, a novel family of compounds shows high binding specificity and activity, and, in a radiolabeled form, can be used to bind to these receptors, for biochemical assays and ...	03/13/2007
7183290	Fluoropyrrolidines as dipeptidyl peptidase inhibitors The present invention relates to novel compounds, their use for inhibiting post prolin/analine-cleaving proteases, such as serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV), and to methods for their production and their therap...	02/27/2007
7179826	Compositions useful as inhibitors of protein kinases The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, ...	02/20/2007
7105678	Boat tropanes Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter o...	09/12/2006
7094784	High 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
7094788	Esters 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′, ...	08/22/2006
7081238	Methods for diagnosing and monitoring treatment ADHD by assessing the dopamine transporter level A method of diagnosing attention deficient-hyperactivity disorder (ADHD) in a human patient by assessing the level of dopamine transporter in at least one region of the patient's central nervous system, where an elevated level of dopamine transporter in the patient ...	07/25/2006
7041674	Carbamic 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
7041667	CCR5 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
7011813	Cocaine receptor binding ligands Tropane derivatives having a high binding affinity and selectivity for dopamine transporters bear, on the tropane backbone either a carboxylic ester or isoxazole moiety, as well as a substituted phenyl moiety. The compounds have utility both as pharmaceutical and as...	03/14/2006
7001900	Azabicyclic compounds for the treatment of disease The invention provides compounds of Formula I: wherein Azabicyclo is W is a six-membered heterocyclic ring system having 1–2 nitrogen atoms or a 10-membered bicyclic-six-...	02/21/2006
6982271	Tropane analogs The present invention provides compounds, specifically novel tropane analogs, capable of acting as inhibitors of reuptake of monoamines. In preferred embodiments, these compositions are selective inhibitors of serotonin and/or norepinephrine reuptake. Also provided ...	01/03/2006
6964972	8-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
6951849	Benzimidazolidinone derivatives as muscarinic agents Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the s...	10/04/2005
6894041	Oxazolyl-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
6858623	Compounds useful as reversible inhibitors of cysteine proteases Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are...	02/22/2005
6727254	Heteroaryl tropane derivatives as superior ligands for nociceptin receptor ORL-1 Novel compounds of the formula wherein R is optionally substituted heteroaryl or R1 is H or C1-C6 alkyl; and R2 and ...	04/27/2004
6706880	Cocaine receptor binding ligands The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addicti...	03/16/2004
6680328	8-azabicyclo[3.2.1]oct-2-ene and -octane derivatives 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 use...	01/20/2004
6676925	Sigma-2 receptors as biomarkers of tumor cell proliferation Detectably-labeled compounds of formula (I) wherein A,B,C,D,E,F,R,X,Y and Z have any of the meanings given in the specification, and their pharmaceutically acceptable salts, are useful in competitive assays to assay for the presence of 2 receptors. Also d...	01/13/2004
6667314	Tropane derivatives useful in therapy The present invention provides compounds of the formula: ##STR1## wherein R1 is C3-6 cycloalkyl optionally substituted by one or more fluorine atoms, or C1-6 alkyl optionally substituted by one or more fluorine atoms, ...	12/23/2003
6656951	8-aza-bicyclo[3.2.1]octan-3-ol derivatives of 2,3-dihydro-1,4-benzodioxan as 5-HT1A antagonists Compounds of the formula: ##STR1## are useful for treating the cognitive deficits due to aging, stroke, head trauma, Alzheimer's disease or other neurodegenerative diseases, or schizophrenia and also treatment of disorders related to excessive seroto...	12/02/2003
6645977	8-azabicyclo(3,2,1)oct-2-ene and octane derivatives as cholinergic ligands at nicotinic ACh receptors The present invention discloses compounds of formula (1) any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein - - - - is a single or a double bond; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, #...	11/11/2003

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Class 546/125 - Additional hetero ring containing