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Class 549/341 - The spiro hetero ring is five-membered


Subclass of Class 549 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the spiro hetero ring is a five-membered
No. of patents: 100
Last issue date: 11/30/2010


1      
NumberTitleIssue Date
7842825Biaryloxymethylarenecarboxylic acids as glycogen synthase activator
The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, m, n, p and s are as defined in the description and claims, and pharmaceutically acceptable salts...
11/30/2010
7358030Process for producing ether compound
The present invention provides the following process for production of an ether compound, which is useful for chemical amplification type resist compositions, synthetic intermediates of pharmaceuticals, paints, or the like, with less side reaction and in high yield....
04/15/2008
7288665Process for selective derivatization of taxanes
Processes for the preparation of taxol and other taxanes through selective derivatization of the C(7) and C(10) hydroxyl groups of 10-DAB, particularly a novel process using a new strategy in which the C(10) hydroxyl group is protected or derivatized prior to the C(...
10/30/2007
7211694Substituted 4-aminocyclohexanols
Substituted 4-aminocyclohexanols, processes for their preparation, pharmaceutical compositions comprising these compounds and to the use of substituted 4-aminocyclohexanols in the preparation of pharmaceutical compositions for the treatment of various indications, e...
05/01/2007
7202370Semi-synthesis of taxane intermediates from 9-dihydro-13-acetylbaccatin III
A method is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel from 9-dihydro-13-acetylbaccatin III. The preparation of a suitably protected baccatin III backbone from 9-dihydro-13-acetylbaccatin III, and th...
04/10/2007
7183436Substituted 4-aminocyclohexanols
Substituted 4-aminocyclohexanols, methods of producing the same, pharmaceuticals containing these compounds, the use of substituted 4-aminocyclohexanols for producing pharmaceutical compositions for the treatment of various indications, in particular pain, and for r...
02/27/2007
7169940Compounds and pharmaceutical compositions comprising same
NST 400 compounds consisting of a unit for partial coordination of Ca2+ ions (CPCU). The NST 400 compounds are optionally conjugated to another pharmaceutically active compound. The compounds and conjugates can be used for affinity filters and for binding negative c...
01/30/2007
7049448Process for the preparation of monoketals of 1,4-cyclohexanedione including 1, 4-cyclohexanedione mono-2,2-dimethyl trimethylene ketal
There is provided a process for preparation of a monoketal compound of the structure that includes reacting 1,4-cyclohexanedione of the structure with a diol...
05/23/2006
7026279Use of 3-(methoxymethyl)-2-pentylcyclopenta derivatives in perfume compositions
3-(methoxymethyl)-2-pentylcyclopent derivative compounds having the structure set forth below are disclosed: where: the dotted line represents a potential double bond; ...
04/11/2006
7015363Process for producing ether compound
The present invention provides the following process for producing and the like, which enables the production of an ether compound, which is useful for chemical amplification type resist compositions, synthetic intermediates of pharmaceuticals, paints, or the like, ...
03/21/2006
6977270Tocotrienolquinone cyclization product with an anti-hypercholesterol effect
A description is given of the use of at least one compound of the formula I where R1, R2, R3 and R4 independently of one another are H or C1-C6
12/20/2005
6962938Spiro-cyclic β-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-α converting enzyme (TACE)
The present application describes novel spiro-cyclic β-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-13 membered carbocycle or heterocycle, ring C forms ...
11/08/2005
6906205Spiro and dispiro 1,2,4-trioxolane antimalarials
A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side ...
06/14/2005
6887700Process for the enzymatic preparation of enantiopure 1, 3-dioxolan-4-one and 1,3-oxathiolan-5-one derivatives
A process is provided for preparing an enantiopure 1,3-dioxolan-4-one or 1,3-oxathiolan-5-one derivative, which includes bringing a mixture containing enantiomeric 1,3-dioxolan-4-one or 1,3-oxathiolan-5-one derivatives and an enzyme with hydrolytic activity into con...
05/03/2005
6825230Spiro and dispiro 1,2,4-trixolane antimalarials
A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side ...
11/30/2004
6504037Process for preparing resorcinol derivatives
The present invention relates to an improved process for preparing 4-substituted resorcinol derivatives, and intermediate compounds useful in the preparation of such resorcinol derivatives....
01/07/2003
6486199Spiro and dispiro 1,2,4-trioxolane antimalarials
A means and method for treating malaria using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl or spiropiperidyl ring on the other ...
11/26/2002
6469184Total synthesis of antitumor acylfulvenes
The present invention provides a method of synthesizing compounds of formula (I): ##STR1## wherein R and R' are independently (C1 -C4)alkyl....
10/22/2002
6379590Method for making unsymmetrically substituted fluorenyl compounds for nonlinear optical applications
A new method for producing unsymmetrically substituted fluorenyl compounds, one step of which is the preparation of 2,7-disubstituted fluoren-9-one derivatives via the nucleophilic substitution of a compound of the formula D ##STR1## wherein A' is se...
04/30/2002
6342459Photochromic naphthopyrans
The present invention relates to photochromic 2H-naphtho[1,2-b]pyrans as well as their use in synthetic resins of all types, especially for ophthalmic purposes. In particular, the present invention relates to photochromic naphthopyran compounds, for which...
01/29/2002
6124479Process for the preparation of 1,3-dioxolane-4-methanols
A process for preparing a 1,3-dioxolane-3-methanol (5) in a racemic form or an optically active form involves reacting with an alcohol in a base (i) a 3-halogeno-1,2-propanediol (1a) in which X is halogen atom, or (ii) a glycidol effecting a 3-alkoxy-1,2-...
09/26/2000
5962704Production of amide derivatives and intermediate compounds therefor
A method for producing an amide derivative of the formula ›XV! ##STR1## wherein each symbol is as defined in the specification, and an enantiomer thereof, a novel intermediate useful for producing said compound and a production method thereof. The p...
10/05/1999
5616609Carcinostatic compound and production thereof
Described are stelleramacrin A and stelleramacrin B represented by the following formulas (I) and (II), respectively: ##STR1## a process for the preparation thereof; and anticancer agents containing either of them as an active ingredient. Therapeutic...
04/01/1997
5585490Certain cycloalkyl and azacycloalkyl pyrrolopyrimidines; a new class of GABA brain receptor ligands
This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: n is 0, 1 or 2, and R1, R2, X, Y and W are variables. These compounds are highly selective agonists, antag...
12/17/1996
5576355Diamondoid derivatives for pharmaceutical use
A method of inhibiting viruses in which a virus is contacted with diamondoid alcohol, ketone, ketone derivative, adamantyl amino acid, quaternary salt or combinations thereof which have antiviral properties. These diamondoid derivatives are shown to have ...
11/19/1996
5493034Intermediate for pesticidal aminomethylheterocyclic compounds
Fungicidally active compounds of the formula ##STR1## in which X represents oxygen or sulphur, R represents cycloalkyl, or represents optionally substituted aryl, or represents the radical ##STR2## R1 and R2 each independen...
02/20/1996
5416225Total synthesis of taxol
The present invention provides two basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as w...
05/16/1995
5387593Piperazinyl-and piperidinyl-cyclohexanols
Novel piperazinyl- and piperidinyl-cyclohexanols of the following formula are useful as anxiolytic agents and have other psychotropic properties ##STR1##...
02/07/1995
5352678Antiischemic piperazinyl- and piperidinyl-cyclohexanes
Certain piperazinyl- and piperidinyl-substituted cyclohexanes have anti-ischemic properties....
10/04/1994
5300705Process for the preparation of 1଱,25,26-trihydroxy-22-ene-cholecalciferol
A process for preparing 1଱,25(R),26-trihydroxy-22E-ene-cholecalciferol and 1଱,25(S),26-trihydroxy-22E-ene-cholecalciferol....
04/05/1994
5286860Certain aryl substituted pyrrolopyrazines; a new class of GABA brain receptor ligands
This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## represents: ##STR3## where n is 0, 1, or 2; R1 and R2 are hydrogen or straight o...
02/15/1994
5283346Dioxolanes
Alcohols of the formula ##STR1## wherein R1 and R2 are each independently methyl or ethyl or together signify pentamethylene, formed by the enzymatic hydrolysis of a corresponding (RS) alkanoic acid ester are intermediates for V...
02/01/1994
5260472Efficient chemoenzymatic synthesis of D-myo-inositol 1,4,5-triphosphate, D-myo-inositol 1,3,4-triphosphate, and D-myo-inositol 1,3,4,5-tetraphosphate
Multigram quantities of Ins(1,4,5) P3, Ins(1,3,4) P3, and Ins(1,3,4,5)P4 are prepared in their enantiomerically pure forms from the two enantiomers of 1,2:5,6-di-O-cyclohexylidene myo-inositol. Also, a facile enzymatic pre...
11/09/1993
5235057Aminodiol derivatives
The invention relates to compounds of the formula ##STR1## in which R1 and R2 are identical or different and are hydrogen or aralkyl, R3 is alkyl, cycloalkyl or cycloalkylalkyl, R4 and R5 are ide...
08/10/1993
5202444Optically isomeric inositol and process for making optically active compound
Optically active diols and hydroxycarboxylic acids and their esters are produced by deriving 1L-1,2:5,6-di-O-cyclohexylidene-chiro-inositol from 1L-chiro-inositol as an asymmetric source, followed by introduction of a selected class of sterically hinderin...
04/13/1993
5192798Lipophilic polyamines useful for treating hypercholesterolemia
This invention relates to novel lipophilic polyamines of formula I, the method of using these compounds to treat hypercholesterolemia, and intermediates thereto. Z1 --(CH2)n --Y1 --X1 --R1 I...
03/09/1993
5110958Compounds, process and intermediates
The claimed invention relates to intermediate compounds of the formula ##STR1## wherein R is hydrogen or methyl, R1 and R2 each, independently, is hydrogen, lower alkyl or aryl, or taken together are lower alkylene of from 3 to ...
05/05/1992
5098932Cyclic ether derivatives
The invention concerns a cyclic ether derivative of the formula I, ##STR1## wherein Ar1 is optionally substituted phenyl or naphthyl; A1 is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene; Ar2 is ...
03/24/1992
5093490Process for optical resolution of bicyclo[3.3.0]octane-3,7-dione-2 carboxylic acid esters and their 7-monoketals
The invention relates to a process for the production of (+)-bicyclo[3.3.0]octan-3-one-2 carboxylic acid steroid esters of formula I ##STR1## in which X means oxygen or the radicals --O--(CH2)n --O-- or --O--CH2 ...
03/03/1992
5089629Fluorine-substituted cyclohexylcyclohexene derivative
A compound represented by formula (I): ##STR1## wherein wherein R represents a straight chain alkyl group having from 1 to 9 carbon atoms; ##STR2## represents ##STR3## X represents a hydrogen atom or a fluorine atom; and ##STR4## ...
02/18/1992
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