Patents Examined by Joseph Paul Brust
  • Patent number: 5418249
    Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a thiazolidinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: January 25, 1994
    Date of Patent: May 23, 1995
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5416083
    Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a benzodiazepinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: May 16, 1995
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5416112
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, Y is selected from the group consisting of ##STR2## Z.sub.1 and Z.sub.2 are individually selected from the group consisting of hydrogen, halogen, --NO.sub.2, --CN and alkyl of 1 to 3 carbon atoms, R.sub.3 is hydrogen or alkyl of 1 to 3 carbon atoms, m is an integer from 0 to 6, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are individually selected from the group consisting of hydrogen, halogen, --CN, --NO.sub.2, alkyl, alkylthio and alkoxy of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, --COR.sub.10, --(CH.sub.2).sub.n --CX.sub.3, --O--(CH.sub.2).sub.n CX.sub.3 and --S--(CH.sub.2).sub.n --CX.sub.3, R.sub.
    Type: Grant
    Filed: June 6, 1994
    Date of Patent: May 16, 1995
    Assignee: Roussel Uclaf
    Inventor: Elizabeth A. Kuo
  • Patent number: 5416084
    Abstract: Compounds characterized generally as benzo-fused thiomorpholinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is a benzo-fused thiomorpholinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sub.q --C.ident.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: May 16, 1995
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Patent number: 5416104
    Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having an oxazolidinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: January 25, 1994
    Date of Patent: May 16, 1995
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5416092
    Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a 3-azabicyclo[3.2.1]-oct-8-yl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: January 25, 1994
    Date of Patent: May 16, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5416235
    Abstract: A process for the preparation of aromatic compounds of the general formula I,Ar--X Iin which Ar represents an optionally substituted aryl group and X represents a group OH, Cl, Br or CN, by reaction of an aryl diazoniumsalt of the formula II,Ar--N.dbd.N.sup.+ Y.sup.- IIin which Ar is as defined above and Y represents a suitable counterion, with water, hydrogen chloride or a salt thereof, hydrogen bromide or a salt thereof, or a cyanide in the presence of a copper(I)salt, characterized in that the copper(I)salt is a copper(I)salt derived from an hydroxy carboxylic acid.
    Type: Grant
    Filed: November 1, 1993
    Date of Patent: May 16, 1995
    Assignee: Octel Chemicals Limited
    Inventors: Bruce C. Gilbert, Peter Hanson, Jason R. Jones, Allan W. Timms
  • Patent number: 5416111
    Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols containing a cyano group and having an N-phenyl-amino-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: May 16, 1995
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5416095
    Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a tetrahydro-quinolinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: May 16, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5416085
    Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a 3-oxa-8-azabicyclo[3.2.1]-oct-8-yl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: May 16, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5414012
    Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having an indolyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: May 9, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5413998
    Abstract: Compounds characterized generally as benzo-fused thiazopinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is a benzo-fused thiazopinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: May 9, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Patent number: 5412145
    Abstract: Compounds of general formula I: ##STR1## Wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are variables. These compounds have collagenase inhibition activity and are useful in the management of disease involving collagen degradation. Its uses include rheumatoide arthritis, corneal ulceration, osteoporosis, periodontitis, gingivitis and tumor invasion.
    Type: Grant
    Filed: December 23, 1993
    Date of Patent: May 2, 1995
    Assignee: British Bio-Technology Limited
    Inventors: M. J. Crimmin, A. H. Davidson, R. P. Beckett
  • Patent number: 5411961
    Abstract: Compounds characterized generally as benzo-fused morpholinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is a benzo-fused morpholinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: January 25, 1994
    Date of Patent: May 2, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Patent number: 5411953
    Abstract: Compounds characterized generally as oxazopinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is an oxazopinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sub.q --C.tbd.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: May 2, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Patent number: 5411962
    Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a benzomorpholinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: May 2, 1995
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5411959
    Abstract: Compounds characterized generally as 1,4-thiomorpholinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is a 1,4-thiomorpholinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: May 2, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Patent number: 5412144
    Abstract: The present invention is directed to organic materials that have the ability to double or triple the frequency of light that is directed through the materials. Particularly, the present invention is directed to the compound 4-[4-(2R)-2-cyano-7-(4'-pentyloxy-4-biphenylcarbonyloxy)phenylheptylidene) phenylcarbonyloxy]benzaldehyde, which can double the frequency of light that is directed through the compound. The invention is also directed to the compound (12-hydroxy-5,7-dodecadiynyl) 4'-[(4'-pentyloxy-4-biphenyl)carbonyloxy]-4-biphenylcarboxylate, and its polymeric form. The polymeric form can triple the frequency of light directed through it.
    Type: Grant
    Filed: January 12, 1994
    Date of Patent: May 2, 1995
    Assignee: The Board of Trustees of the Univ. of Illinois
    Inventors: Samuel I. Stupp, Sehwan Son, Hong-Cheu Lin
  • Patent number: 5412146
    Abstract: For the preparation of 2-cyanoacetoxypropionic esters, a mixture of lactic ester and cyanoacetic ester is introduced, an alkali metal alcoholate is added as catalyst and the mixture is heated while the alcohol eliminated during the course of the reaction is distilled off. The course of the reaction is followed by means of gas chromatographic analysis and the reaction is terminated prior to eliminating the theoretical amount of alcohol by destroying the catalyst by acidification. The reaction mixture is worked up by distillation and the product easily separated from the reaction mass due to the substantial absence of high boiling components.
    Type: Grant
    Filed: June 3, 1994
    Date of Patent: May 2, 1995
    Assignee: Huels Aktiengesellschaft
    Inventors: Manfred Kaufhold, Marcel Feld
  • Patent number: 5411950
    Abstract: Compounds characterized generally as benzo-fused oxazocinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is a benzo-fused oxazocinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein v is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: May 2, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning