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Class 546/197 - Plural ring hetero atoms in the polycyclo ring system


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the polycyclo ring system contains at
No. of patents: 520
Last issue date: 09/04/2012


1                      
NumberTitleIssue Date
8258305Dopamine transporter inhibitors for use in treatment of movement disorders and other CNS indications
The invention provides a class of dopamine transporter inhibitors of formula (I) (DAT inhibitors), packaged pharmaceuticals comprising such inhibitors, and their uses in treating, or manufacturing medicaments for treating disease conditions including Parkinson's dis...
09/04/2012
7678914Deuterated benzo[][1,3]-dioxol derivatives
The present invention relates to an isotopologue of Compound 1 substituted with deuterium at the methylene carbon of the benzodioxol ring. The isotopologues of this invention selective serotonin reuptake inhibitors (SSRIs) and possess unique biopharmaceutical and me...
03/16/2010
7408067Aza-cyclic compounds as modulators of acetylcholine receptors
Compounds comprising an aza-cyclic portion and an aromatic portion linked via a sulphur atom are disclosed. The compounds disclosed are selective modulators of beta 4 subtype nicotinic acetylcholine receptors and are useful for the treatment of dysfunctions of the c...
08/05/2008
7393861Derivatives of 4-aminopiperidine and their use as a medicament
A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic method...
07/01/2008
7388020Benzimidazol derivatives modulate chemokine receptors
The invention provides compounds of general formula (I) wherein A, X, m, R1, N, R2, Z1, Z2, Q, R3, R4, R5, R6, R7, R8, t and R16 are as defined i...
06/17/2008
7342114Podophyllotoxin derivatives
4-O esters of podophyllotoxin and 4′-demethylepipodophyllotoxin are provided. The compounds are 4-O esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4′-demethylepipodophyllotoxin. The compounds are useful for treating cancer. ...
03/11/2008
7329654Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators
The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their prepar...
02/12/2008
7294637Method of treating addiction or dependence using a ligand for a monamine receptor or transporter
One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substitute...
11/13/2007
7271264Pentacyclic oxepines and derivatives thereof, compositions and methods
The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6
09/18/2007
7220862Calcitonin gene related peptide receptor antagonists
The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying th...
05/22/2007
72054104-(aminomethyl)-piperidine benzamides for treating gastrointestinal disorders
The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, —R1—R2— is a ...
04/17/2007
7176236Water-soluble etoposide analogs and methods of use thereof
Etoposide analogs with improved water-solubility such as 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4β-(4″-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4β-(4″-fluoroanilino)-4-desoxy-podophyllotoxin (9) ...
02/13/2007
7144883Bicyclic sulfonamide compounds
The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obe...
12/05/2006
7144890Spiro-pentacyclic compounds
The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof, for use as therapeutically active substances. The compounds are useful for the treatment and/or prophyl...
12/05/2006
7138523Preparation of 4-(4-fluorophenyl)-N-alkylnipecotinate esters, 4-(4-fluorophenyl)-N-arylnipecotinate esters and 4-(4-fluorophenyl)-N-aralkylnipecotinate esters
A process for the industrial scale manufacture of 4-(4-fluorophenyl)-N-alkylnipecotinate esters by the addition of 4-fluorophenylmagnesium halide in tetrahydrofuran to 3,4-unsaturated-3-piperidine esters. ...
11/21/2006
7122675Gamma secretase inhibitors
Novel aryl and heteroaryl sulfonamides are disclosed. The sulfonamides, which are gamma secretase inhibitors, are represented by the formula: wherein Ar1 and Ar2 independently represent aryl or he...
10/17/2006
71156344-aminopiperidine and their use as a medicine
A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic m...
10/03/2006
7115632Sulfonyl aryl or heteroaryl hydroxamic acid compounds
A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid ...
10/03/2006
7105679Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators
The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their prepar...
09/12/2006
7084144Sulfonyl group containing compounds and their use for the treatment of erectile dysfunction
A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl ...
08/01/2006
7084140Arylglycinamide derivatives, method of producing said derivatives and pharmaceutical compositions containing these compounds
The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound...
08/01/2006
70814662-aroylimidazole compounds for treating cancer
Disclosed is a compound represented by Structural Formula (I): R1 is a substituted or unsubstituted 2-imidazolyl group which is optionally fused to a substituted or unsubstitut...
07/25/2006
7071201Quinoline derivatives
A novel compound of the formula: wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; R1, R2, R3, R4, and R5 represent each a substituent; n represe...
07/04/2006
7060725Substituted sulfamate anticonvulsant derivatives
The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as descr...
06/13/2006
70530864-heteroaryl-3-heteroarylidenyl-2-indolinones and their use as protein kinase inhibitors
The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases (“PKs”), in particular CDK2. The compounds of the present invention are the...
05/30/2006
7041683Antidepressant azaheterocyclylmethyl derivatives of 2,3-dihydro-1, 4-benzodiozan
Compounds of the formula useful for the treatment of depression and other conditions such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, sexual dysfunction, eating disorders, addictive di...
05/09/2006
6987117Antidepressant azaheterocyclylmethyl derivatives of 1,4-dioxino[2,3-b]pyridine
Compounds of the formula useful for the treatment of depression, obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder, sexual dysfunction, eating disorders, obesity, addict...
01/17/2006
6984651Piperidine amides 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 asthma and other allergic diseases. ...
01/10/2006
6956121Preparation of paroxetine involving novel intermediates
Disclosed are processes for preparing novel carbamate intermediates of paroxetine comprising dealkylating N-alkylparoxetine by reaction thereof with a haloalkyl ester of a haloformic acid, in a suitable organic solvent. Also disclosed are processes for preparing par...
10/18/2005
6953806Substituted cyclohexane derivatives
The present invention provides compounds of formula (I) wherein A1, A2, A3, A4, A5, A6, A7, A8, A9, A10, U, ...
10/11/2005
6951849Benzimidazolidinone 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
6949650Process for the racemization of 1-benzyl-4-(4-fluorophenyl)-3-hydroxymethyl-1,2-3,6-tetrahydropyridine to be used as intermediate in the synthesis of paroxetine
A process for the racemization of enantiomerically enriched 1-benzyl-4-(4-fluorophenyl)-3-hydroxymethyl-1,2,3,6-tetrahydropyridine which is a useful intermediate in the preparation of paroxetine. Formula (A) means that the compound (I) has an enantiomeric excess of ...
09/27/2005
6949546N-ureidoheterocycloalkyl-piperidines 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 asthma and other allergic diseases. ...
09/27/2005
6943178Antidepressant azaheterocyclylmethyl derivatives of 1,4,5-trioxa-phenanthrene
Compounds of the formula useful for the treatment of diseases such as depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic str...
09/13/2005
6930186Process for the preparation of paroxetine substantially free of alkoxy impurities
The present invention is directed to methods for preparing intermediates useful in the synthesis of paroxetine wherein the intermediates are substantially free of alkoxy impurities as well as to methods for preparing paroxetine and pharmaceutically acceptable salts ...
08/16/2005
6916802Amino ceramide-like compounds and therapeutic methods of use
The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer sy...
07/12/2005
6906098Mixed steroidal 1,2,4,5-tetraoxane compounds and methods of making and using thereof
Disclosed herein are mixed steroidal tetraoxanes having the following structural formula 1 wherein n is 0, 1, 2, or 3; R is H; ethanoyl, propanoyl, or benzoyl; R1 is H, methyl, ethyl, or isopropyl; R2 is H, methyl, or ...
06/14/2005
6903116Methods of treating cancer using a heat shock factor activity inhibitor
A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, whi...
06/07/2005
6900227Benzodioxole derivatives
The present invention relates to compounds of the general formula and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases such as obesity by selective mo...
05/31/2005
6900222Pyrrolidinyl, piperdinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2
05/31/2005
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