Class 540/578 - Three or more hetero atoms in the polycyclo ring system

Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the polycyclo ring system contains at
No. of patents: 170
Last issue date: 05/08/2012

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Number	Title	Issue Date
8173804	Process for production of mirtazapine The invention provides a process for production of mirtazapine as a convenient process for obtaining mirtazapine from a reaction mixture obtained by cyclization of 2-(4-methyl-2-phenylpiperazin-1-yl)pyridine-3-methanol with concentrated sulfuric acid, at high purity...	05/08/2012
7915404	Methods for the preparation of pyrazole-containing compounds The present invention is directed to novel processes for the preparation of fused pyrazole compounds, useful for the treatment of disorders and conditions mediated by serotonin receptor activity. ...	03/29/2011
7414046	Gyrase inhibitors and uses thereof The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also re...	08/19/2008
7407949	Benzamide derivatives as oxytocin agonists and vasopressin antagonists Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds ...	08/05/2008
7390797	Fused indazole compounds The present invention provides a novel fused indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. ...	06/24/2008
7390798	Carboxamide spirolactam CGRP receptor antagonists The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in...	06/24/2008
RE40245	Gyrase inhibitors and uses thereof The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates ...	04/15/2008
7358238	Pharmaceutical use of fused 1,2,4-triazoles The use of fused 1,2,4-triazoles for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of fused 1,2,4-triazoles, their use in therapy, p...	04/15/2008
7329653	Cyclohexylphenyl vasopressin agonists The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic rin...	02/12/2008
7297790	Anhydrous mirtazapine crystals and process for preparing the same Low-hygroscopic anhydrous mirtazapine crystals having a hygroscopic degree of not more than 0.6% by weight when the crystals are stored in the air having a relative humidity of 75% at 25° C. under atmospheric pressure for 500 hours; a process for preparing anhydrou...	11/20/2007
7262189	Benzothiazine and benzothiadiazine derivatives, method for preparing same and pharmaceutical compositions containing same Compounds of formula (I): wherein: R1 represents aryl or heteroaryl, R2 represents hydrogen, halogen or hydroxy, X represents oxygen or sulphur, ...	08/28/2007
7262190	Benzothiazine and benzothiadiazine compounds The invention relates to compounds of formula (I): wherein: R1 represents hydrogen, alkyl or cycloalkyl, R2 represents hydrogen, halogen or hydroxy, A ...	08/28/2007
7262302	1-thia-3-aza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof The present invention relates to derivatives of 1-thia-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the in...	08/28/2007
7253161	Benzothiazine and benzothiadiazine derivatives method for preparing same and pharmaceutical compositions containing same Compounds of formula (I): wherein: R1 represents aryl or heteroaryl, R2 represents hydrogen, halogen or hydroxy, A represents CR4R5	08/07/2007
7253163	Benzothiazine and benzothiadiazine compounds Compounds of formula (I): wherein: R1 represents a heterocycle, R2 represents hydrogen, a halogen or hydroxy, A represents CR4R5 ...	08/07/2007
7211574	Selective D1/D5 receptor antagonists for the treatment of obesity and CNS disorders The present invention provides compounds, which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/...	05/01/2007
7192951	Treatment of congestive heart failure Combinations of diuretics and vasopressin antagonists are useful to slow and reverse the symptoms and process of congestive heart failure, to increase the excretion of water in the urine, and to decrease the excretion of sodium and potassium ions in urine. Preferred...	03/20/2007
7176195	Fused azepine derivatives and their use as antidiuretic agents Compounds according to general formulae (1 and 2), wherein G1 is an azepine derivative and G2 is a group according to general formulae (9–11) are new. Compounds according to the invention are vasopressin V2 receptor agonists. Pharm...	02/13/2007
7122545	Imidazo-benzothiazoles The invention relates to 2-imidazo-benzothiazoles of general formula wherein R1, R2, R3, R4, R5, R6, R7, R′, R″, X, R′″ and n a...	10/17/2006
7105667	Fused heterocyclic compounds and use thereof Fused heterocylic compounds of the following Formula wherein R1, R2, R5, Z, J1 and J2 are described herein which are useful in treating leukocyte activation-...	09/12/2006
7105506	Tetracyclic compounds as PDE5-inhibitors Compounds of structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents. ...	09/12/2006
7056910	1,4,5.6-tetrahydroimidazo[4,5-d]diazepine derivatives or salts thereof To provide a compound having a superior arginine vasopressin antagonism. A novel 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or a pharmaceutically acceptable salt thereof. ...	06/06/2006
7053083	Cyclohexylphenyl vasopressin agonists The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl “Z” represents optionally substituted phenyl or a 6-membered aromatic ring...	05/30/2006
6951850	Dipeptide derivatives This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which inc...	10/04/2005
6916925	Dye labeled imidazoquinoline compounds Dye labeled imidazonaphthyridine, imidazopyridine and imidazoquinoline compounds having immune response modulating activity are disclosed. The compounds arc useful, inter alia, for determining the binding and/or receptor sites of the molecules. ...	07/12/2005
6908926	Substituted imidazoles, their preparation and use Disclosed is a novel class of substituted imidazole compounds, pharmaceutical compositions containing them and uses of these compounds in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, these compoun...	06/21/2005
6852855	Synthesis of piperazine ring A novel process for preparing a compound of the formula I: wherein R1 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy; R2 denotes substituted or unsubstit...	02/08/2005
6815440	Cyclic and heterocyclic N-substituted α-iminohydroxamic and -carboxylic acids Cyclic and heterocyclic N-substituted α-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is invol...	11/09/2004
6774230	Methods for the preparation of mirtazapine intermediates The preparation of 1-(3-carboxypyridyl-2)-4-methyl-2-phenylpiperazine dihydrate and other mirtazapine intermediates are described. These compounds are particularly useful in the preparation of mirtazapine. ...	08/10/2004
6770647	Bicyclic hydroxamates as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE) The present application describes to novel bicyclic hydroxamates derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, B1, B2, R1, and C ar...	08/03/2004
6723845	Anhydrous mirtazapine crystals and process for preparing the same Low-hygroscopic anhydrous mirtazapine crystals having a hygroscopic degree of not more than 0.6% by weight when the crystals are stored in the air having a relative humidity of 75% at 25° C. under atmospheric pressure for 500 hours; a process for preparing anhydrou...	04/20/2004
6720316	Therapeutic 5-HT ligand compounds The present invention provides compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and Z have any of the values defined ...	04/13/2004
6686352	Substituted imidazo [1,5-a] pyrimido [5,4-d] [1] benzazepine derivatives The present invention is a compound of formula ##STR1## wherein R1 is halogen or lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, --(CH2)m -phenyl, wherein the phenyl ring may be substituted by lower alkoxy, or ...	02/03/2004
6660730	Anhydrous mirtazapine and process for preparing the same Methods for producing anhydrous mirtazapine crystals that are either (1) substantially free of lower alcohol insolubles or (2) substantially free of residual solvent and have an average particle diameter of from 10 to 50 μm, are provided, and the resulti...	12/09/2003
6653471	Heterocyclic compounds as ligands of the GABAA receptor Disclosed are heterocyclic compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein the variables A, V, Y, J, E, X, T, G, Q, W, Z, b, n and m are defined herein. These compounds are highly selective agonists, antagonists...	11/25/2003
6649604	Substituted pyridone compounds and methods of use Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-଱, IL-1ଲ, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention enco...	11/18/2003
6642222	Pyrano, piperidino, and thiopyrano compounds and methods of use ##STR1## The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions....	11/04/2003
6638934	Substituted pyrazinoquinoxaline derivatives as serotonin receptor agonist and antagonists ligands The present invention is directed to novel compounds represented by structural Formulas (I) and (I-a): ##STR1## or a pharmaceutically acceptable salt thereof, wherein R1, R4a, R4b, R5, R6, R7	10/28/2003
6632809	Gyrase inhibitors and uses thereof The present invention relates to compounds of the formula I: ##STR1## or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for tr...	10/14/2003
6603003	Method for the preparation of piperazine and its derivatives A novel method for the synthesis of piperazine and its derivatives of formula 1, ##STR1## wherein R is selected from hydrogen, or a lower alkyl group having 1 to 6 carbon atoms or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms; R...	08/05/2003

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Class 540/578 - Three or more hetero atoms in the polycyclo ring system