Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R.sub.1 is hydrogen, alkyl, aryl, arylloweralkyl, naphthyl, furyl, thienyl, pyridinyl or pyrrolyl; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.2 or --NR.sub.3 R.sub.4 where R.sub.2 is hydrogen or loweralkyl, and R.sub.3 and R.sub.4 are independently hydrogen, loweralkyl or cycloalkyl; stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.
Abstract: A process for the preparation of a compound of the formula ##STR1## in which R is hydrogen, alkoxy, alkylamino, dialkylamino or an optionally substituted radical from the group consisting of alkyl, cycloalkyl, aralkyl and aryl,R.sup.1 is an optionally substituted radical from the group consisting of alkyl, alkoxy, alkylthio, mono- or dialkylamino and phenyl,R.sup.2 is optionally substituted alkyl, andY is oxygen or sulphur,comprising(a1) reacting a compound of the formula ##STR2## with ##STR3## or withR.sup.5 COOHin whichR.sup.5 is R except for hydrogen, or equivalent, to produce ##STR4## oxidizing that compound or its salt to ##STR5## and phosphorylating. Several of the intermediates are new.
Type:
Grant
Filed:
December 9, 1988
Date of Patent:
April 23, 1991
Assignee:
Bayer Aktiengesellschaft
Inventors:
Fritz Maurer, Reinhard Lantzsch, Helmut Fiege, Albert Schnatterer
Abstract: A seris of antibody-vinca drug conjugates comprise antibodies which target antigens associated with undesirable cells, so that the cells are controlled or killed by the cytotoxic vinca drug. The drug is linked to the antibody through an organic group comprising a carbonyl at the antibody end, and an alkylidene hydrazide at the vinca end.
Type:
Grant
Filed:
August 8, 1988
Date of Patent:
April 9, 1991
Assignee:
Eli Lilly and Company
Inventors:
George J. Cullinan, Bennett C. Laguzza, William L. Scott
Abstract: Water soluble camptothecin analogs, pharmaceutical compositions comprising such analogs, and a method of inhibiting the growth of tumor cells sensitive to such analogs in an animal in need thereof.
Type:
Grant
Filed:
November 2, 1988
Date of Patent:
April 2, 1991
Assignee:
SmithKline Beecham Corporation
Inventors:
Jeffrey C. Boehm, Sidney M. Hecht, Kenneth G. Holden, Randall K. Johnson, William D. Kingsbury
Abstract: 2-Alkylpyrimidines are prepared from 1,3-diaminopropane and an appropriate alkanecarboxylic acid in a continuous vapor phase process without isolating any of the reaction intermediates. Improvements in each reaction step, namely, the amidation, the cyclization/dehydration and the dehydrogenation, contribute to the overall success of the continuous vapor phase process.
Abstract: An antiviral compound of the formula: ##STR1## wherein A is selected from a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group and a heterocyclic isostere of a pyrimidin-1-yl group; andG and D are independently selected from hydrogen, C.sub.1 to C.sub.10 alkyl and substituted derivatives thereof, --OH, --C(O)H, --CO.sub.2 R.sub.1 l wherein R.sub.1 is hydrogen or C.sub.1 to C.sub.10 alkyl and --OCH.sub.2 PO.sub.3 H.sub.2, with the proviso that one of D or G is other than hydrogen or C.sub.1 to C.sub.10 alkyl; or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
May 22, 1989
Date of Patent:
January 29, 1991
Assignee:
Abbott Laboratories
Inventors:
Daniel W. Norbeck, Terry J. Rosen, Hing L. Sham
Abstract: Halogenated 9-phosphonoalkyl derivatives of guanine and hypoxanthine are inhibitors of purine nucleoside phosphorylase and are useful as immuno suppressant and antiparasitic agents as well as against T cell leukemia and antiureicopoietic agents.
Abstract: A compound selected from the group consisting of optical isomers and racemates of 4-hydroxy-3-quinoline carboxylates of the formula ##STR1## wherein X is in the 5-, 6-, 7- or 8-position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --SCF.sub.3, and OCF.sub.3, R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.2 is selected from the group consisting of thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl and tetrazolyl, all optionally substituted with alkyl of 1 to 4 carbon atoms and phenyl and phenyl substituted with at least one member of the group consisting of --OH, alkyl and alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --NO.sub.2 and halogen, A is ##STR2## in which R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl, R.sub.
Type:
Grant
Filed:
April 20, 1988
Date of Patent:
January 29, 1991
Assignee:
Roussel Uclaf
Inventors:
Francois Clemence, Odile Le Martret, Francoise Delevallee
Abstract: A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase I and show anti-leukemic and anti-tumor activity.
Type:
Grant
Filed:
September 28, 1988
Date of Patent:
January 1, 1991
Assignee:
Research Triangle Institute
Inventors:
Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
Abstract: Therapeutic compositions comprising the new derivatives of aminooxodihydroisoindolo-quinazoline of the formula ##STR1## are useful in inhibiting the growth of colon and rectal tumors.
Type:
Grant
Filed:
June 20, 1989
Date of Patent:
December 25, 1990
Assignee:
Bayer Aktiengesellschaft
Inventors:
Valentino Stella, Laman A. Al-Razzak, Hans-Joachim Kabbe
Abstract: Antihypertensive phosphodiesterase inhibitors having an optionally substituted purine derivative portion and a benzo- or cyclopenta-furan derivative portion are disclosed.
Type:
Grant
Filed:
March 23, 1989
Date of Patent:
November 20, 1990
Assignee:
Schering Corporation
Inventors:
Ronald J. Doll, Deen Tulshian, Charles V. Magatti
Abstract: Square-planar four-coordinate complexes of cis-platinum(II) with neutral bidentate aminoalkyl-substituted cycloalkylamine ligands and bromo-, chloro-, iodo-, nitrato-, oxalato-, or malanato-ligands possess antimicrobial activity as well as activity against transplanted L1210 and P388 murine leukemia cell lines.
Type:
Grant
Filed:
January 8, 1988
Date of Patent:
November 13, 1990
Inventors:
James D. Hoeschele, David A. Berry, Luigi G. Marzilli
Abstract: Disclosed are 7.beta.-arylalkyl substituted morphinan compounds characterized by the formula: ##STR1## In the above formula, R is H or methyl, R.sub.1 is methyl, cyclopropylmethyl or cyclobutylmethyl and n is 2 to 5.