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Class 546/133 - Quinuclidines (including unsaturated)


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the bicyclo ring system has the following
No. of patents: 308
Last issue date: 12/18/2012


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NumberTitleIssue Date
58344995-HT3 receptor agonist, novel thiazole derivative and intermediate thereof
A 5-HT3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): ##STR1## wherein the A ring is substituted or unsubstituted and represents a benzene or a heterocyclic...
11/10/1998
5830902Quinuclidine derivative having tricyclic hetero condensed ring
A quinuclidine derivative represented by the following general formula (I), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, which has strong squalene synthase inhibiting activity and is useful as a cholesterol lowering ...
11/03/1998
5807867Quinuclidine derivatives
Compounds of the formula ##STR1## wherein R1 is methoxy and R2 is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl; and the pharmaceutically acceptable salts of such compounds. These compo...
09/15/1998
5808075Process for the preparation of azabicyclic derivatives
A process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein R1 represents (a) in which r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1; R2 is a group...
09/15/1998
5795890Sulfonamide derivatives
A sulfonamide derivatives of formula (I) ##STR1## a non-toxic salts, an acid addition salts or a solvates thereof which has an inhibitory effect on elastase....
08/18/1998
5792777Biphenyl quinuclidines
Biphenylylquinuclidine compounds of the formula I: ##STR1## and pharmaceutically-acceptable salts thereof; wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 are joined together so that CR...
08/11/1998
5780466Substituted heterocyclic compounds method of preparing them and pharmaceutical compositions in which they are present
The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from: A1) --O--CO-- A2) --CH2 --O--CO-- A3) --O--CH2 --CO-- A4) --O--CH2 --CH
07/14/1998
5777122Enantiomerically pure quinuclidine derivatives and methods for their production and use
A process for cleaving cinchona alkaloids to a quinoline derivative and an enantiomerically pure, functionalized 1-azabicyclo(2.2.2)octane, includes treating a cinchona alkaloid with a complex metal hydride while simultaneously oxidizing by exposure to ai...
07/07/1998
5773619Process for the preparation of azabicycloc derivatives
A process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R1 represents ##STR2## in which r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 ...
06/30/1998
57734581-azabicycloheptane derivatives
The compound of the formula: ##STR1## where R is H, alkyl, haloalkyl, cycloalkyl, alkenyl or alkynyl; Y is oxygen, sulfur or NR2 where R2 is H or alkyl; or a pharmaceutically acceptable salt thereof, are centrally active muscari...
06/30/1998
5770608Heterocyclic derivatives
Quinuclidine compounds of the formula I: ##STR1## R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 are joined together so that CR1 --CR2 is a double bond; X is selected from --CH
06/23/1998
5767141Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseases
Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseases Propane derivatives of the formula I ##STR1## in which the radicals have the meanings stated in the description, a process for the pre...
06/16/1998
5744606Process for the preparation of optically active 3-quinuclidinol
Optically active 3-quinuclidinol is obtained by the asymmetric hydrogenation of 3-quinuclidinone, its Lewis acid adducts or its tertiary or quaternary salts, for example, 1-(diphenylmethyl)-3-oxoquinuclidinium bromide. Rhodium/chiral diphosphine complexes...
04/28/1998
5741797Heteroatom substituted alkyl benzylaminoquinuclidines
Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of the formula I and the pharmaceutically-acceptable salts thereof; ##STR1## wherein R is C1 -C6 alkyl; X is C
04/21/1998
5741819Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors
The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compoun...
04/21/1998
5731323Quinuclidine derivatives as squalene synthase inhibitors
Compounds of formula (I) and their pharmaceutically acceptable salts in which R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 are joined together so that CR1 --CR2 is a double bond; ...
03/24/1998
5726313Substituted arylaliphatic compounds, method of preparing them and pharmaceutical compositions in which they are present
Compound of Formula (I), wherein W1 is an oxygen atom; an --NR-- group wherein R is hydrogen, C1 -C7 alkyl or benzyl; and B is for example a substituted piperidine or quinuclidine. The disclosed compounds are useful as neu...
03/10/1998
5723103Substituted benzamides and radioligand analogs and methods of use
This invention provides compounds of the formula I ##STR1## wherein, R1, R2, and R3 are independently ›a first halogen atom,! fluorine, chlorine, bromine, iodine, alkyl, alkenyl, alkynyl, alkoxy, alkenoxy, or alkynox...
03/03/1998
5716965Substituted 3-aminoquinuclidines
Compounds of the formula ##STR1## wherein W, Ar1, Ar2 and Ar3 are defined as below; and the pharmaceutically acceptable salts of such compounds. These compounds are substance P antagonists and useful in the treatment of ...
02/10/1998
5714496Quinuclidine derivatives as squalene synthase inhibitors
Compounds of formula (I) and their pharmaceutically acceptable salts in which R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 are joined together so that CR1 -CR2 is a double bond; X ...
02/03/1998
5712288Quaternary basic amides, method of preparing them and pharmaceutical compositions in which they are present
The invention relates to quaternary basic amides of the formula ##STR1## in which Ar is an optionally substituted mono-, di- or tri-cyclic aromatic or heteroaromatic group; T is a direct bond, a hydroxymethylene group, an alkoxymethylene group in whi...
01/27/1998
57122702-arylamidothiazole derivatives with CNS activity
This invention relates to methods of treating neurological illnesses related to acetylcholine deficiency in the CNS including memory loss attending senility, Parkinson's disease, Down's syndrome or senile pugilistica by administering a therapeutically eff...
01/27/1998
5710191Hydroxymethyl quinuclidine catalyst compositions for making polyurethane foams
A method for preparing a polyurethane foam which comprises reacting an organic polyisocyanate and a polyol in the presence of a blowing agent, a cell stabilizer and a catalyst composition comprising at least one compound of either of the following formula...
01/20/1998
5691349Quinclidine derivatives as squalene synthase inhibitors
Quinuclidine derivatives of formula, and their pharmaceutically acceptable salts, in which: R1 is hydrogen or hydroxy; R2 is hydrogen; pr R1 and R2 are joined together so that CR1 -CR2 is a ...
11/25/1997
5686461Indole derivatives
The invention relates to compounds of formula (I). ##STR1## or a salt, or metabolically labile ester thereof wherein R1 represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, tri...
11/11/1997
5686463Oxadiazoles useful in the treatment of senile dementia
A class of novel oxadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring, and substituted on the other ring carbon atom with a substituent of low lipophilicity; are potent muscarinic agonists, and have go...
11/11/1997
5662828Compound having unsaturated side chain, process for preparing the same, liquid crystalline polymer prepared from the same, liquid crystal mixture and display element
A compound having an unsaturated side chain represented by the formula: ##STR1## in which A and B are the same and different and represent an aromatic or heterocyclic group or either one of A and B represents a single bond; X1, X2
09/02/1997
5658925Aminobenzoic acid derivatives
To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically accepta...
08/19/1997
5656639Heterocyclic compounds, method of preparing them and pharmaceutical compositions in which they are present
The invention relates to compounds of the formula ##STR1## in which: m is 2 or 3; n is 0, 1 or 2; Am is ##STR2## R1 is a (C1 -C4)-alkyl or a benzyl; R2 is a substituted or unsubstituted phenyl; x is ze...
08/12/1997
5654315Quinuclidine compounds useful in treating diseases
Quinuclidine compounds of the formula I: ##STR1## R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 are joined together so that CR1 --CR2 is a double bond; X is selected from --CH
08/05/1997
5643923Quinuclidinyloxy-isoxazole compounds and their therapeutic uses
Compounds of formula (I): ##STR1## wherein R1 is hydrogen, halogen or alkyl; R2 is hydrogen, alkyl, optionally substituted phenyl or a heterocycle; or R1 and R2 together form a group of formula --CR4
07/01/1997
5641777Substituted heterocyclic compounds and pharmaceutical compositions in which they are present
The invention relates to neurokinin receptor antagonist compounds of the formula ##STR1## in which: A is a divalent radical selected from: A1) --O--CO-- A2) --CH2 --O--CO-- A3) --O--CH2 --CO-- A4...
06/24/1997
5637596Azabicycloalkyl derivatives of imidazo[1,5-a]indol-3-one and process for their preparation
Novel 5-HT3 receptor antagonist compounds having the general formula (I) ##STR1## wherein each of R, R1 and R2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C1 -C6 al...
06/10/1997
5614629Benzyl quaternary tropinium compound
This invention is directed to novel benzyl quaternary ammonium compounds and their synthesis. The compounds have valuable utility as organic directing agents in the crystallization of a silicate structure which, in turn, is useful as a catalyst component,...
03/25/1997
5612352Heterocyclic compounds
Biphenylylquinuclidine derivatives of formula I, Q--Ar1 --Ar2, in which Q is of formula Ia or Ib, ##STR1## in which R1 and R2 are independently selected from hydrogen, alkyl, halogeno and hydroxy; or R...
03/18/1997
5612336Heterocyclic amide derivatives as tachykinin antagonists
Compounds of formula (I), and salts and prodrugs thereof, wherein Q1 is phenyl substituted by one or more halo; optionally substituted naphthyl, indolyl, benzothiophenyl, benzofuranyl, benzyl or fluorenyl; the dotted line represents an optional...
03/18/1997
5605908Heterocyclic compounds and their use
The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nerv...
02/25/1997
5604241Substituted benzylaminoquinuclidines as substance P antagonists
Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of the formula I ##STR1## and the pharmaceutically-acceptable salts thereof, wherein Ar1 and Ar2 are each independ...
02/18/1997
5599937Heteroaromatic quinuclidinenes, their use and preparation
The invention relates to novel compounds of general formula (I), wherein R is a group of general formula (II) or (III), where X1 represents oxygen or sulphur and Y1 and Z1 both represent carbon, or X1 represents...
02/04/1997
5591748Immunomodulatory azaspiranes
Invented are substituted azaspirane compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to induce an immunosuppressive effect in a mammal in need thereof....
01/07/1997
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