Patents Examined by M. Ambrose
  • Patent number: 5442088
    Abstract: Process for the preparation of phosphorus-containing L-amino acids, their derivatives and intermediates for this processL-amino acids of the formula I and salts thereof, ##STR1## in which R.sup.1 to R.sup.5 are defined as in claim 1 and n is 0 or 1, are obtained according to the invention bya) reacting an optically active S-homoserine lactone of the formula II, ##STR2## with hydrogen chloride in the presence of an alcohol of the formula R.sup.5 --OH to give novel compounds of the formula III, ##STR3## in which R.sup.3, R.sup.4 and R.sup.5 are defined as in formula I, except that R.sup.5 =H, andb) reacting the resulting compound of formula III with a compound of formula IV,R.sup.1 (O).sub.n -R(OR.sup.2).sub.2 (IV)and if desired, hydrolyzing the product to give a compound of formula I, in which R.sup.5 =H.
    Type: Grant
    Filed: July 7, 1994
    Date of Patent: August 15, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Michael Hoffmann
  • Patent number: 5300671
    Abstract: Diphosphonic acids of formula (I), wherein R.sub.1 and R.sub.2 are hydrogen or C.sub.1 -C.sub.4 alkyl; (A) is hydrogen, halogen, hydroxy or C.sub.1 -C.sub.12 alkyl; (B) is a bond, a C.sub.1 -C.sub.8 alkylene chain, a cycloalkylalkylene chain, an alkylene chain substituted by cyclohexyl or cyclopentyl groups, or an aralkyl chain, an alkyl chain containing an heteroatom (O, S or N--CH.sub.3) or an ureido residue --(CH.sub.2).sub.nl --NHCONH--(CH.sub.2).sub.n --with n ranging from 1 to 5, R.sub.3 is hydrogen, C.sub.1 -C.sub.9 alkyl, C.sub.3 -C.sub.6 cycloalkyl, benzyl, phenyl or p-methoxybenzyl; (C) is C.sub.1 -C.sub.5 alkyl, phenyl or an aralkyl chain; R.sub.4 is hudrogen, C.sub.1 -C.sub.5 alkyl or an amino group optionally substituted by alkyl, phenyl, benzyl, p-methoxybenzyl, acyl, amminoacidic or peptide groups; R.sub.5 and R.sub.6 are 2-haloethyl or together form a 1-aziridinyl residue, are useful as antitumor agent.
    Type: Grant
    Filed: June 9, 1992
    Date of Patent: April 5, 1994
    Assignee: Boehringer Mannheim Italia S.p.A.
    Inventors: Sergio Tognella, Valeria Livi, Ernesto Menta, Silvano Spinelli
  • Patent number: 5298500
    Abstract: Disclosed is a phosphoric acid ester derivative represented by the general formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each lower alkyl, X.sup.1 and X.sup.2 are the same or different and are each a hydrogen atom or halogen atom, and Y is an oxygen atom or sulfur atom. The phosphoric acid ester derivatives of the present invention are usable as insecticides and miticides having excellent residual activity and low toxicity to warm blooded animals.
    Type: Grant
    Filed: March 17, 1992
    Date of Patent: March 29, 1994
    Assignee: Otsuka Kagaku Kabushiki Kaisha
    Inventor: Hisashi Takao
  • Patent number: 5107011
    Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents, are provided which have the structure ##STR1## wherein R.sup.2 is a metal ion, lower alkyl or H; R.sup.3 is a metal ion or lower alkyl;R is R.sup.1 --(CH.sub.2).sub.n --, R.sup.1 --(CH.sub.2).sub.m --O-- or R.sup.1 --(CH.sub.2).sub.m --OCH.sub.2 --, wherein n is 1 to 4 and m is 0 to 3, andR.sup.1 is R.sup.5 --Q.sup.1 --Q.sup.2 --Q.sup.3 -- wherein R.sup.5, Q.sup.1, Q.sup.2 and Q.sup.3 are as defined herein.New intermediates, new methods of preparation and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.
    Type: Grant
    Filed: February 5, 1991
    Date of Patent: April 21, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Scott A. Biller