Alan D Hutchison

48016055, Jan 31, 1989

Feb 27, 1987

7/020054

Alan J. Hutchison - Verona NJ

Ciba-Geigy Corporation - Ardsley NY

A61K 3138
C07D33506
C07D40902

514432

##STR1## wherein Z represents O or S; R represents hydrogen or lower alkyl; R. sub. 1 represents hydrogen, lower alkyl or aryl-lower alkyl; R. sub. 2 represents hydrogen, lower alkyl or aryl-lower alkyl; or R. sub. 1 and R. sub. 2 together represent alkylene of 4 to 6 carbon atoms; R. sub. 3 represents hydrogen, hydroxy, lower alkoxy, aryl-lower alkoxy, acyloxy or aryloxy in compounds wherein Z represents S; or R. sub. 3 represents hydroxy, lower alkoxy, aryl-lower alkoxy, acyloxy or aryloxy, and is attached only at the 5- or 8- position in compounds wherein Z represents O; R. sub. 4 and R. sub. 5 represent independently hydrogen, lower alkyl or halogen; and pharmaceutically acceptable salts thereof; and mono or di- S-oxides of compounds of formula I wherein Z represents S and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof; and use thereof as central nervous system active agents for the treatment of central nervous system disorders.

44643802, Aug 7, 1984

May 25, 1983

6/497962

Alan J. Hutchison - Verona NJ

Pfizer Inc. - New York NY

A61K 31435
C07D40114

424263

A series of novel spiro-oxindole imidazolidinedione derivatives have been prepared, including their pharmaceutically acceptable salts. These compounds are useful in therapy as aldose reductose inhibitors for the control of certain chronic diabetic complications. Preferred compounds include 6'-amino-spiro-[imidazolidine-4,3'-indoline]-2,2',5-trione, 5'-chloro-7'-amino-spiro-[imidazolidine-4,3'-indoline]-2,2',5-trione, 1'-(3-pyridylmethyl)-5'-fluoro-spiro-[imidazolidine-4,3'-indoline]-2,2',5- trione, 1'-(3-pyridylmethyl)-5',7'-dichloro-spiro-[imidazolidine-4,3'-indoline]-2, 2',5-trione and spiro-[imidazolidine-4,3'-(6-azaindoline)]-2,2',5-trione. Methods for preparing these compounds from known starting materials are provided.

50343815, Jul 23, 1991

May 13, 1988

7/193968

Alan J. Hutchison - Verona NJ
John E. Francis - Basking Ridge NJ

Ciba-Geigy Corporation - Ardsley NY

A61K 3170
C07H 19167

514 26

Disclosed are 2-substituted adenosine derivatives of the formula ##STR1## in which R represents a substituted amino grouping of the formula ##STR2## as defined herein; pharmaceutically acceptable ester derivatives thereof in which free hydroxy groups are esterified in the form of a pharmaceutically acceptable prodrug ester; and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for their preparation; and their use in mammals as therapeutically effective adenosine-2 (A-2) agonists.

49924656, Feb 12, 1991

Feb 16, 1990

7/481770

Alan J. Hutchison - Verona NJ

Ciba-Geigy Corporation - Ardsley NY

A61K 3135
A61K 31395
C07D31158

514456

##STR1## wherein Z represents O or S; R represents hydrogen or lower alkyl; R. sub. 1 represents hydrogen, lower alkyl or aryl-lower alkyl; R. sub. 2 represents hydrogen, lower alkyl or aryl-lower alkyl; or R. sub. 1 and R. sub. 2 together represent alkylene of 4 to 6 carbon atoms; R. sub. 3 represents hydrogen, hydroxy, lower alkoxy, aryl-lower alkoxy, acyloxy or aryloxy in compounds wherein Z represents S; or R. sub. 3 represents hydroxy, lower alkoxy, aryl-lower alkoxy, acyloxy or aryloxy, and is attached only at the 5- or 8- position in compounds wherein Z represents O; R. sub. 4 and R. sub. 5 represent independently hydrogen, lower alkyl or halogen; and pharmaceutically acceptable salts thereof; and mono or di- S-oxides of compounds of formula I wherein Z represents S and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof; and use thereof as central nervous system active agents for the treatment of central nervous system disorders.

49066218, Mar 6, 1990

Nov 23, 1987

7/124226

Alan J. Hutchison - Verona NJ
Kenneth R. Shaw - Florham Park NJ
Josef A. Schneider - Murray Hill NJ

Ciba-Geigy Corporation - Ardsley NY

C07F 965
A61K 31445

514 89

The present invention is concerned with the phosphonic acids of formula I ##STR1## wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be functionalized in form of pharmaceutically acceptable mono- or di- esters; wherein Y represents optionally substituted 2-carboxypyrrolidinyl, 2-carboxy-2,5-dihydropyrrolyl, 2-carboxy-1,2,3,6-tetrahydropyridinyl, 2-carboxy-1,2,5,6-tetrahydropyridinyl, 2-carboxypiperidinyl, 2-carboxytetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, 2-carboxy-2,3-dihydroindolyl or 2-carboxyperhydroindolyl as described herein, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents a direct bond, lower alkenylene, lower alkylidene or lower alkylene provided that A does not represent a direct bond when Y represents 2-carboxypyrrolidinyl; and pharmaceutically acceptable salts thereof; which are useful for the treatment of nervous system disorders in mammals and as antagonists of the N-methyl-D-aspartate sensitive excitatory amino acid receptor.

48164747, Mar 28, 1989

Feb 27, 1987

7/020053

Alan J. Hutchison - Verona NJ

Ciba-Geigy Corporation - Ardsley NY

A61K 3138
C07D49504

514432

Disclosed are compounds of the formula ##STR1## wherein A represents the divalent radical --S--CR. sub. 4. dbd. CR. sub. 5 -- in which R. sub. 4 and R. sub. 5 independently represent hydrogen or lower alkyl; R. sub. 1 represents hydrogen, lower alkyl or aryl-lower alkyl; R. sub. 2 represents hydrogen, lower alkyl or aryl-lower alkyl; or R. sub. 1 and R. sub. 2 combined represent alkylene of 4 to 6 carbon atoms; R. sub. 3 represents hydrogen or lower alkyl; an S-oxide thereof; or a pharmaceutically acceptable salt thereof; which are useful as presynaptic dopamine receptor agonists for the treatment of central nervous system disorders; processes for preparing same; and pharmaceutical compositions comprising said compounds.

47217871, Jan 26, 1988

Sep 26, 1985

6/780711

Alan J. Hutchison - Verona NJ

Ciba-Geigy Corporation - Ardsley NY

C07D491052
C07D49504

546 89

A process for the preparation of a compound of the formula ##STR1## having a trans 4a,10b-ring junction wherein X represents oxygen or sulfur; ring A is substituted by lower alkoxy; R represents lower alkyl; R. sub. 1 -R. sub. 5 represent hydrogen; which comprises (a) condensing the corresponding 2H[1]-benzopyran-3-one with the corresponding carboxy protected 3-aminopropanoic acid, (b) reducing and dehydrating the resultant product, and reducing the resulting double bond to a compound of formula I.

52179630, Jun 8, 1993

Jul 30, 1991

7/738073

Alan J. Hutchison - Verona NJ
Kenneth R. Shaw - Florham Park NJ
Josef A. Schneider - Murray Hill NJ

Ciba-Geigy Corporation - Ardsley NY

C07F 960
C07F 962
A61K 3147

514 82

The present invention is concerned with the phosphonic acids of formula I ##STR1## wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be functionalized in form of pharmaceutically acceptable mono- or di- esters; wherein Y represents optionally substituted 2-carboxytetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents a direct bond, lower alkenylene, lower alkylidene or lower alkylene; and pharmaceutically acceptable salts thereof; which are useful for the treatment of nervous system disorders in mammals and as antagonists of the N-methyl-D-aspartate sensitive excitatory amino acid receptor.