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Class 540/596 - Additional hetero ring attached directly or indirectly to the hetero ring by nonionic bonding


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein an additional hetero ring is attached
No. of patents: 454
Last issue date: 07/29/2008


1                      
NumberTitleIssue Date
7405209Protease inhibitors
The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such co...
07/29/2008
7365077Piperazine bis-amide derivatives and their use as antagonists of the orexin receptor
Disclosed are piperazine bis-amide derivatives useful as antagonists of the orexin receptor and pharmaceutical compositions containing the same. ...
04/29/2008
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
73070791,3,5-Triazine derivatives as ligands for human adenosine-A3 receptors
The invention relates to a group of novel triazine derivatives which are ligands for human adenosine-A3 receptors, as well as to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingre...
12/11/2007
7268134Medical devices employing triazine compounds and compositions thereof
The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced...
09/11/2007
7238713Muscarinic agonists
Compounds and methods are provided for the treatment of disease conditions in which modification of cholinergic, especially muscarinic m1, m4, or both m1 and m4, receptor activity has a beneficial effect. In the method, an effective amount of a compound is administe...
07/03/2007
7202237Pyridylether derivatives, their preparation and use
The present invention relates to novel pyridylether derivatives which are cholinergic ligands at nicotinic Ach receptors. The compounds of the invention are useful for the treatment of conditions, disorders, or diseases involving the cholinergic system of the centra...
04/10/2007
7202020Compositions, methods and apparatuses for preserving platelets
A platelet composition suitable for direct transfusion into a patient is provided. The platelet composition includes a preservation medium comprising plasma and a gel-forming material in a concentration relative to the plasma such that the medium is in a sufficientl...
04/10/2007
7169774Cephalotaxane derivatives and their processes of preparation and purification
The present invention concerns a new general process for asymmetric hemisynthesis of harringtonines and their analogs, that are alkaloids used in chemotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constit...
01/30/2007
7148221Vanilloid receptor ligands and their use in treatments
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular an...
12/12/2006
7122561Treatment of skin conditions
The present invention provides piperine and analogues or derivatives thereof for the treatment of skin conditions treatable by stimulation of melanocyte proliferation, such as vitiligo, and also for treating skin cancer. The piperine and analogues or derivatives the...
10/17/2006
7105556Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2
09/12/2006
70784074-hydroxycinnamamide derivatives as antioxidants and pharmaceutical compositions containing them
The present invention relates to 4-hydroxycinnamamide derivatives as antioxidants and pharmaceutical compositions containing them. More particularly, it relates to 4-hydroxycinnamamide derivatives showing superior antioxidant activity compared to the known antioxida...
07/18/2006
7071338Process for the synthesis of bis-aryl diamidoxime compounds
Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl] furans, can be prepared from 2,5-bis tri-alkylstannanes via a one step palladium-catalyzed cross reaction. Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkyl...
07/04/2006
7071184Protease inhibitors
The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel int...
07/04/2006
7057040Substituted aryl alkenoic acid heterocyclic amides
The present invention relates to novel compounds possessing specific hot, pungent and spicy taste when subjected to direct pungency evaluation, which may be useful as food additives and anti-oxidants, however the said compounds do not add to any nutritional value bu...
06/06/2006
7012153Process for preparing benzoic acids
An improved process for the preparation of 4[(2-piperidin-1-yl)ethoxy]benzoic acid derivatives, comprising reacting a haloalkyl amine of formula (III) with a compound of formula (IV) in the presence of a hydrated inorganic base in an appropriate solvent. ...
03/14/2006
6969730Amines as histamine-3 receptor ligands and their therapeutic applications
Compounds of formula (I) or a pharmaceutically acceptable salts or prodrug thereof which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders amelior...
11/29/2005
6964963Preparation of 4-amino-1-naphthol ethers
The present invention describes a process for preparing 4-amino-1-naphthol ethers which is characterized in that naphthol ethers are first prepared from 1-naphthols, the former are then converted to the corresponding 4-acetamino-1-naphthol ethers and then the acyl g...
11/15/2005
69272095-thio-β-D-xylopryanoside derivatives, preparation, method, pharmaceutical compositions containing them and their therapeutic use
The present invention relates to novel compounds of formula (I): in which: R1, R2 and R3, which are identical or different, are each independently: a (...
08/09/2005
6921822Process for stereoselectively reducing 4-aryl-4-oxobutanoic acid derivatives
The present invention relates to a process for preparing stereoisomerically enriched 4-aryl-4-hydroxybutanoic acid derivatives by reducing 4-aryl-4-ketobutanoic acid derivatives in the presence of ruthenium-containing catalysts. ...
07/26/2005
6919456Catalytic compositions and methods for asymmetric aldol reactions
Methods and compositions are provided for the direct catalytic asymmetric aldol reaction of aldehydes with donor molecules selected from ketones and nitroalkyl compounds. The reactions employ as catalyst a Group 2A or Group 2B metal complex of a ligand of formula I,...
07/19/2005
6916899Polycarbonates, polyester carbonates and polyesters having lateral, cycloalkyl-substituted phenols
A process of using of a particularly substituted phenol as a chain terminator of a polymeric resin is disclosed. The chain terminator is a member selected from among ortho-substituted phenol, metha-substituted phenol, and their corresponding coupled esters. The poly...
07/12/2005
6914140Asymmetric synthesis process
A novel process for the manufacture of compounds of the formula wherein R1 and R2 independently represent aroyl. The present invention also concerns novel intermediates used in the novel p...
07/05/2005
6908914Antipsychotic cyclic N-aralkylamines
The invention relates to benzene derivatives, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment of psychotic disorders. ...
06/21/2005
6887864Azepane derivatives
This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their ...
05/03/2005
6881733Serotonergic benzofurans
The present invention provides serotonergic benzofurans of Formula (I): where A, R, R1, R2, R3, and R4 are as described in the specification. ...
04/19/2005
6849619Substituted pyridoindoles as serotonin agonists and antagonists
The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, ...
02/01/2005
68443364-fluoroalkyl-2h-benzopyrans with anti-estogenic activity
This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I, in which Z is a straight-chain or branched-chain alkyl group with up to 5 carbon atoms that is fluo...
01/18/2005
6831180Cephalotaxane derivatives and process for their preparation
The present invention concerns a new general process for asymetric hemisynthesis of harringtonines and their analogs, that are alcaloids used in chimiotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constit...
12/14/2004
6825217Carbinols for the treatment of neuropathic dysfunction
Compositions and methods are provided for treating neuropathic pain or neuropathic dysfunction that include the administration of an effective amount of a defined carbinol or a pharmaceutically acceptable salt or prodrug thereof. ...
11/30/2004
6750213Estrogen receptor modulators
The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a v...
06/15/2004
6720317Inhibitors of factor Xa
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders. ...
04/13/2004
6717014Processes for preparing haloamines and tertiary aminoalkylorganometallic compounds
Processes for the preparation of haloalkylamines and tertiary aminoalkylorganometallic compounds are disclosed. The haloalkylamines can be prepared by direct reaction of an amine with an α,ω-dihaloalkane or an α,ω-dihaloalkene. Tertiary aminoalkylorganometallic ...
04/06/2004
6699852Substituted pyridoindoles as serotonin agonists and antagonists
The present invention is directed to certain novel compounds represented by structural Formula (I) ##STR1## or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9...
03/02/2004
6680314Azacyclooctane and heptane derivatives, their preparation and use in therapy
Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: ##STR1## wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 ...
01/20/2004
6667303Aryl substituted 1,4-diazepanes and method of use thereof
Aryl substituted 1,4-diazepanes are provided such as derivatives of 6-(1,4-diazepan-1-yl)benzo[cd]indol-2(1H)-one, 6-(1,4-diazepan-1-yl)acenaphthylen-1(2H)-one and 5-(1,4-diazepan-1-yl)-2H-naphtho[1,8-cd]isothiazole-1,1-dioxide. Also provided are pha...
12/23/2003
66533283-benzyl-benzothiophenes
This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzothiophenes which are ଱-substituted with ether, thioether amino, cyano or halo that are useful for the treatment of the various medical indi...
11/25/2003
6653302Quinoline and quinazoline compounds useful in therapy
Compounds of formula I, ##STR1## wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atom...
11/25/2003
6617329Aminoquinazolines and their use as medicaments
Compounds of the formula ##STR1## having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and air-ways, and the preparation thereof...
09/09/2003
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