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Class 546/16 - The spiro includes the six-membered hetero ring


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein at least one of the rings in the spiro
No. of patents: 373
Last issue date: 02/07/2012


1                    
NumberTitleIssue Date
8110684Diaza-spiro [4.5] decanes useful as pesticides
A method of combating and controlling insects, acarines, nematodes or molluscs which comprises applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount ...
02/07/2012
80490123-aza-spiro[5.5]undecane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
This invention relates to novel 3-aza-spiro[5.5]undecane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions com...
11/01/2011
8030491Process and intermediate for preparation of donepezil
The invention relates to new compounds of formula (III): wherein R is a C1-C4 linear or branched alkyl group. The invention also relates to new compounds of formula (IV)
10/04/2011
80263654,4-disubstituted piperidine derivatives
This invention relates to 4,4-disubstituted piperidine derivatives of the formula wherein A and R1 to R5 are as defined in the specification, and pharmaceutically acceptable salts thereof. The inventio...
09/27/2011
7750158Cannabinoid receptor ligands
Compounds of Formula I: and/or pharmaceutically acceptable salts, solvates or prodrugs thereof, or pharmaceutical compositions containing such compounds exhibit anti-inflammatory and immunomodulatory activity, and can be ef...
07/06/2010
7504506Therapeutic compounds and uses thereof
Compounds of formula (I) are described herein The compounds can be used, for example, to modulate growth hormone secretagogue receptor (GHS-R). In some instances, the compounds can be used to treat obesity. ...
03/17/2009
7439251Methods and compositions for treatment of central and peripheral nervous system disorders and novel compounds useful therefor
There are provided methods for the treatment of diseases involving dysfunction of the peripheral and central nervous system comprising administering one or more spiro compounds. Also provided are pharmaceutical compositions useful in such methods, compounds for use ...
10/21/2008
7427621Cyclic sulfamides for inhibition of gamma-secretase
Compounds of formula I: inhibit the processing of AP by gamma-secretase, and hence are useful for treatment or prevention of Alzheimer's disease. ...
09/23/2008
7405332Chemical process
The invention provides a process for preparation of a fluorohaloalkane, preferably an [18F]fluorohaloalkane of formula (I) wherein X is halo and n is an integer of from 1 to 6; which comprises: reaction of the corresponding organosilicon compound of formu...
07/29/2008
7402671UV excitable fluorescent energy transfer dyes
Novel energy transfer dyes which can be used with shorter wavelength light sources are provided. These dyes include a donor dye with an absorption maxima at a wavelength between about 250 to 450 nm and an acceptor dye which is capable of absorbing energy emitted fro...
07/22/2008
7402590Spiroazacyclic compounds as monoamine receptor modulators
The present invention relates to optionally substituted 1-oxa-3,8-diaza-spiro[4.5]decan-2-one compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of trea...
07/22/2008
7393858Tetrahydropyran compounds as tachykinin antagonists
The present invention relates to compounds of formula (Ia) wherein A, B, n, m, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 ...
07/01/2008
7384929N-aryl azaspiroalkene and azaspiroalkane compounds and methods of preparation and use thereof
Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptab...
06/10/2008
7381823Process for preparing cyclohexanediacetic acid monoamide
A new process is described for synthesising cyclohexanediacetic acid monoamide, a key compound in the synthesis of grabapentin precursors. The process of the invention is characterised by reacting cyclohexanone with cynoacetamide and immediately after, with a suitab...
06/03/2008
7365196Sulphonamido-substituted bridged bicycloalkyl derivatives
A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease. ...
04/29/2008
7365070Modulators of melanocortin receptor
This invention provides compounds and methods for treating melanocortin receptor associated disorders, such as weight loss disorders including cachexia resulting from cancer and other chronic illnesses. The compounds are represented by formula I: ...
04/29/2008
7361666Heterocyclic analgesic compounds and methods of use thereof
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-couple...
04/22/2008
7297788Regioselective hydroxylation, functionalisation and protection of spirolactams
The present invention refers to highly functionalised spiro-fused azetidinones of formula I: having a cyclohexane moiety with the desired number of protected or unprotected hydroxyl groups which are introduced with high ste...
11/20/2007
7291728Spirolactams and their synthesis
The present invention is directed to a compound of formula I: wherein R1 and R2 are independently selected from H, halogen, protected or unprotected hydroxy, alkylsilyloxy, substituted or un...
11/06/2007
7288548Spiro compounds and methods for the modulation of chemokine receptor activity
Compounds of formula I wherein X, Y, Z, W, R1 and R2 as defined herein, or pharmaceutically acceptable salts, hydrates or solvates thereof, are useful for the modulation of CCR5 chemokine re...
10/30/2007
7279471Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP antagonists of general formula wherein A and R1 to R3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the hydra...
10/09/2007
7271172Pyrrolidine and azetidine 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...
09/18/2007
7265126Diaza-spiropiperidine derivatives
The present invention relates to compounds of formula wherein A-B, R1, R2, R3, R4, and n are as defined herein; and to pharmaceutically accept...
09/04/2007
7256291Labeling reagents comprising aphenylic analogs of rhodamine dyes
This invention provides for labeling reagents, labeled targets and processes for preparing labeling reagents. The labeling reagents can take the form of cyanine dyes, xanthene dyes, porphyrin dyes, coumarin dyes or composite dyes. These labeling reagents are useful ...
08/14/2007
7238703Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexane NMDA, 5HT, and neuronal nicotinic receptor antagonists
Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of tr...
07/03/2007
7235563Spirocyclic compounds useful as modulators of nuclear hormone receptor function
Spirocyclic compounds, methods of using such spirocyclic compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds are disclosed. ...
06/26/2007
7230125Methods of performing cycloadditions, reaction mixtures, and methods of performing asymmetric catalytic reactions
Methods of performing cycloadditions are described that include (a) combining a first reactant and a second reactant in a hydrogen bonding solvent to form a reaction mixture; and (b) reacting the first reactant and the second reactant to form a cycloadduct. Methods ...
06/12/2007
7226740Aza-benzazolium containing cyanine dyes
Unsymmetrical cyanine dyes that incorporate an aza-benzazolium ring moiety are described, including cyanine dyes substituted by a cationic side chain, monomeric and dimeric cyanine dyes, chemically reactive cyanine dyes, and conjugates of cyanine dyes. The subject d...
06/05/2007
72146912-substituted benzimidazole derivatives as selective melanin concentrating hormone receptor antagonists for the treatment of obesity and related disorders
The present invention discloses compounds of formula I wherein Ar, X, R1 and R11 are herein defined, said compounds being novel antagonists for melanin-concentrating hormone (MCH), as well a...
05/08/2007
7202254Antibacterial compounds: process for their preparation and pharmaceutical compositions containing them
The present invention relates to novel triazole compounds of formula (I), their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutic...
04/10/2007
71992454-imino-n-alkoxy or oxy-polyalkyl-piperidine compounds and their use as polymerization regulators
The present invention relates to selected 4-imino-N-alkoxy-polyalkyl-peperidine compounds preparation, a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a 4-imino-N-alkoxy-polyalkyl-piperidine compound. Further aspects o...
04/03/2007
7173133Diaza-spiropiperidine derivatives
The present invention relates to compounds of formula wherein A-B is —CH2—CH2—, —CH2—O— or —O—CH2—; X is hydrogen or hydroxy...
02/06/2007
7157454Derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and the pharmaceutical compositions containing same
The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal pr...
01/02/2007
7132540Hindered spiro-ketal nitroxides
The present invention discloses a series of novel hindered spiro-ketal nitroxides prepared by the ketalization reaction of 1,3-propanediols with triacetoneamine followed by oxidation. These novel spiro-ketals have unexpected advantages in hydrocarbon and monomer sol...
11/07/2006
7122678Cyclic amino acids and derivatives thereof useful as pharmaceutical agents
The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syn...
10/17/2006
7122677NK1 antagonists
A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5...
10/17/2006
7115635Benzylpiperidine compound
The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following ben...
10/03/2006
7105507Cyclohexane derivatives and their use as therapeutic agents
The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R
09/12/2006
7081463Hydroxy alkyl substituted 1,3,8-Triazaspiro[4.5]decan-4-one derivatives useful for the treatment of orl-1receptor mediated disorders
The present invention is directed to novel hydroxy alkyl substituted 1,3,8-triazaspiro[4.5]decan-4-one derivatives of the general formula wherein all variables are as defined herein, usef...
07/25/2006
7067501Aryloxyphenyl and arylsulfanylphenyl derivatives
The invention provides compounds of the formula wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors. ...
06/27/2006
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