Patents Represented by Attorney William B. Walker
  • Patent number: 4045485
    Abstract: 2-(2'-Naphthyl) acetaldehyde derivatives optionally substituted at the 2 position and/or positions C-1',4',5',7' or 8'; and/or position C-6' or positions C-5' and 7' exhibit anti-inflammatory, analgesic, antipyretic and anti-pruritic activity.
    Type: Grant
    Filed: November 5, 1976
    Date of Patent: August 30, 1977
    Assignee: Syntex Corporation
    Inventors: John H. Fried, Ian T. Harrison
  • Patent number: 4045568
    Abstract: Compounds of the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is phenyl, phenyl straight chain lower alkyl or phenyl straight chain lower alkenyl or one of the above substituted in the phenyl ring with one or more substituents independently selected from the group consisting of lower alkyl of from one to four carbon atoms, halo and trifluoromethyl; the other of R.sup.1 and R.sup.2 is alkyl, cyclohexyl, cyclohexyl lower alkyl or cyclohexyl substituted with from 1 to 3 lower alkyl groups; X is oxygen or sulfur; n is an integer of from 1 to 8 with the proviso that n is not 1 when R.sup.1 is phenyl or substituted phenyl; and the antimicrobial acid addition salts thereof are useful as antifungal, antibacterial and antiprotozoal agents.
    Type: Grant
    Filed: March 8, 1976
    Date of Patent: August 30, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Keith A. M. Walker
  • Patent number: 4044020
    Abstract: Biotin is prepared by (a) ozonizing methylcyclohexene; (b) reacting nitromethane with the methyl-6-oxohexanoate from a to form 7-nitro-6 hydroxyheptanoic acid methyl ester; (c) acylating to form the corresponding 6 acyloxy compound; (d) forming a double bond at the 6 position; (e) reacting the product of d with nitroethanethiol to form dl-7-thia-6-nitromethyl-9-nitro-nonanoic acid methyl ester; (f) forming a furoxan by cyclization; (g) reducing the furoxan and acylating to form dl-2(4-carbomethoxybutyl)-3,4-bis(acylamido)-2,5-dihydro thiophene; (h) selectively hydrogenating to form the 3,4-cis-bis(acylamido)-2,5-dihydro thiophene; and (i) hydrolyzing and cyclizing to form dl-biotin. The products formed at steps (e)-(h) are novel, as are the individual steps (e), (f), (g), and (h).
    Type: Grant
    Filed: June 30, 1975
    Date of Patent: August 23, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Michael Marx, Josef H. Reisdorff
  • Patent number: 4039677
    Abstract: Novel 1-phenethylimidazoles substituted at the position .beta. to the imidazole ring by an optionally substituted hydrocarbyl carbonate or a mono-, di-, or trithiocarbonate are useful as antimicrobial agents and as intermediates in the preparation of novel 1-phenethylimidazoles substituted at the position .beta. to the imidazole with a mercapto. Both the former and latter compounds are useful as intermediates in the preparation of certain 1-[.beta.-(R-thio)phenethyl]imidazoles.
    Type: Grant
    Filed: March 1, 1976
    Date of Patent: August 2, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Keith A. M. Walker
  • Patent number: 4038409
    Abstract: Novel 1-phenethylimidazoles substituted at the position .beta. to the imidazole ring by an optionally substituted hydrocarbyl ester, thioester, or dithioester are useful as antimicrobial agents and as intermediates in the preparation of novel 1-phenethylimidazoles substituted at the position .beta. to the imidazole with a mercapto. Both the former and latter compounds are useful as intermediates in the preparation of certain 1-[.beta.-(R-thio)phenethyl] imidazoles.
    Type: Grant
    Filed: March 1, 1976
    Date of Patent: July 26, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Keith A. M. Walker, Michael Marx
  • Patent number: 4038299
    Abstract: 2-Substituted-5-oxo-5H-dibenzo [a,d] cycloheptenes represented by the following formula: ##STR1## where one of R.sup.2 and R.sup.3 is hydrogen, and the other is hydrogen, methyl, or ethyl, or together R.sup.2 and R.sup.3 are methylene; the dotted line represents an optional, additional bond between the carbon atoms at the 10- and 11-positions; and the pharmaceutically acceptable esters and ethers thereof. The compounds have anti-inflammatory, analgesic, and antipyretic activities and, accordingly, are useful in the treatment of inflammation, pain and pyrexia.
    Type: Grant
    Filed: March 8, 1976
    Date of Patent: July 26, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Karl G. Untch
  • Patent number: 4036973
    Abstract: Compounds of the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is alkyl or the group ##STR2## IN WHICH N IS 0 TO 3 AND THE OTHER OF R.sup.1 and R.sup.2 is benzyl, substituted benzyl, phenyl or substituted phenyl, said substituted benzyl and substituted phenyl substituted on the phenyl ring with one or more substituents independently selected from the group consisting of halo, lower alkyl and trifluoromethyl; X and Y are independently oxygen or sulfur with the proviso that Y is not oxygen when R.sup.2 is phenyl or substituted phenyl; and the antimicrobial acid addition salts thereof are useful as antifungal, antibacterial and antiprotozoal agents.
    Type: Grant
    Filed: March 8, 1976
    Date of Patent: July 19, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Keith A. M. Walker, Michael Marx
  • Patent number: 4036176
    Abstract: This invention is an apparatus and process for culturing aquatic animals. The apparatus comprises a container suitable for retaining water; a plurality of platforms vertically spaced from each other located in said container, the platforms being substantially parallel to each other and being designed to allow water to circulate therethrough while at the same time allowing solid food particles when dropped into the platform area to pass therethrough; and a feeding station placed on each of the platforms in a manner so that each feeding station is vertically and horizontally spaced from each adjacent station, has a structure such that the solid food particles are retained on the feeding station, and is substantially the same area as the adjacent feeding station.
    Type: Grant
    Filed: November 20, 1975
    Date of Patent: July 19, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: James C. McCarty, Dominick Mendola
  • Patent number: 4036970
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently benzyl substituted benzyl, phenyl or substituted phenyl, said substituted benzyl and substituted phenyl substituted on the phenyl ring with one or more substituents independently selected from the group consisting of halo, lower alkyl and trifluoromethyl; X and Y are independently oxygen or sulfur with the proviso that Y is not oxygen when R.sup.2 is phenyl or substituted phenyl; and the antimicrobial acid addition salts thereof are useful as antifungal, antibacterial and antiprotozoal agents.
    Type: Grant
    Filed: March 8, 1976
    Date of Patent: July 19, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Keith A. M. Walker, Michael Marx
  • Patent number: 4036975
    Abstract: Compounds of the formula ##STR1## wherein R is alkyl, cycloalkyl, cycloalkyl lower alkyl, phenyl or phenyl lower alkyl, said phenyl and phenyl lower alkyl optionally substituted on the phenyl ring with one or more substituents independently selected from the group consisting of halo, lower alkyl and trifluoromethyl; and X is oxygen or sulfur with the proviso that X is not oxygen when R is phenyl or substituted phenyl; and the antimicrobial acid addition salts thereof are useful as antifungal, antibacterial and antiprotozoal agents.
    Type: Grant
    Filed: March 8, 1976
    Date of Patent: July 19, 1977
    Assignee: Xyntex (U.S.A) Inc.
    Inventors: Keith A. M. Walker, Stefan Howard Unger
  • Patent number: 4036876
    Abstract: Novel 18.xi.-hydroxylated and 19.xi.-hydroxylated prostaglandins and novel microbiological process for the production thereof.
    Type: Grant
    Filed: July 13, 1973
    Date of Patent: July 19, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Raymond P. Lanzilotta
  • Patent number: 4036974
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently alkyl or the group ##STR2## IN WHICH N IS 0 TO 3; X and Y are independently oxygen or sulfur; and the antimicrobial acid addition salts thereof are useful as antifungal, antibacterial and antiprotozoal agents.
    Type: Grant
    Filed: March 8, 1976
    Date of Patent: July 19, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Keith A. M. Walker, Michael Marx
  • Patent number: 4035509
    Abstract: 2-Substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes represented by the following formula: ##STR1## where R' is hydrogen, alkyl having 1 to 12 carbon atoms, or ##STR2## where n is an integer from 2 to 4, inclusive, and R.sup.4 and R.sup.5 are independently lower alkyl having 1 to 6 carbon atoms or together R.sup.4 and R.sup.5 and the nitrogen atom to which they are attached form a heterocyclic ring having 5 or 6 total ring atoms; and the pharmaceutically acceptable salts thereof. The compounds are useful in the treatment of auto-immune diseases and allergic reactions.
    Type: Grant
    Filed: March 31, 1975
    Date of Patent: July 12, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Karl G. Untch
  • Patent number: 4033978
    Abstract: 3-Carboxy-5-substituted-thiacycl[2.2.2]azines of the formula: ##STR1## wherein R is phenyl or phenyl monosubstituted in the meta or para position with fluoro, chloro, lower alkyl of from 1 to 4 carbon atoms or lower alkoxy of from 1 to 4 carbon atoms, and the pharmaceutically acceptable salts thereof.These compounds are useful as anticomplimentary agents, specifically for the treatment of inflammatory conditions, auto-immune diseases, allergic reactions and vascular diseases.
    Type: Grant
    Filed: August 15, 1975
    Date of Patent: July 5, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Karl G. Untch, John O. Gardner
  • Patent number: 4032789
    Abstract: An axial tomographic system having scanner means normally in an "off" condition where all power sources associated therewith are electrically isolated from the units driven thereby, means for activating the scanner means to establish an "on" condition, control means including means to measure one or more system parameters when the scanner means is in an "on" condition and to determine if the measured parameters are within predetermined limits therefor, and means for maintaining the "on" condition only if the control means is properly operational and all measured system parameters are within the predetermined limits therefor.
    Type: Grant
    Filed: October 28, 1975
    Date of Patent: June 28, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Samuel Thomas Workman
  • Patent number: 4031234
    Abstract: This application relates to 1,5(6)-disubstituted benzimidazole-2-carbamate derivatives represented by the following formula: ##STR1## where R is lower alkyl having 1 to 4 carbon atoms; R.sup.1 is --SOR.sup.2, --SR.sup.5, --OR.sup.5 or M'(CH.sub.2).sub.n MR.sup.7 ; R.sup.2 is lower alkyl having from 1 to 6 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, lower alkenyl or lower alkynyl having 3 to 6 carbon atoms, or aralkyl or aryl; R.sup.5 is lower alkenyl, lower alkynyl or aralkyl; R.sup.7 is lower alkyl having 1 to 4 carbon atom, or aryl; M and M' are independently O, S, ##STR2## n is 1-4; and R.sup.8 is lower alkyl having 1 to 12 carbon atoms optionally substituted with a --COOR group where R is lower alkyl having 1 to 4 carbon atoms, aryl or aralkyl. The R.sup.1 substitution is at the 5(6)-position.The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.
    Type: Grant
    Filed: June 18, 1976
    Date of Patent: June 21, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Colin C. Beard, John A. Edwards, John H. Fried
  • Patent number: 4029773
    Abstract: Compositions and method for treating, or reducing the occurrence, of stomach and duodenum ulcers. The compositions and methods are characterized by the administration of a composition containing (dry weight basis) 10 to 40% sucrose; 10 to 40% glucose; 12 to 20% amino acids and 7.5 to 12% lipids. The composition is typically administered orally as an aqueous liquid emulsion.
    Type: Grant
    Filed: May 25, 1973
    Date of Patent: June 14, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Myron A. Beigler, Ronald J. Amen
  • Patent number: 4020094
    Abstract: 2-Substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes represented by the following formula: ##STR1## where R' is hydrogen, alkyl having 1 to 12 carbon atoms, or ##STR2## where n is an integer from 2 to 4, inclusive, and R.sup.4 and R.sup.5 are independently lower alkyl having 1 to 6 carbon atoms or together R.sup.4 and R.sup.5 and the nitrogen atom to which they are attached form a heterocyclic ring having 5 or 6 total ring atoms; one of R.sup.2 and R.sup.3 is hydrogen and the other is hydrogen, methyl, or ethyl, or together R.sup.2 and R.sup.3 are methylene; and the pharmaceutically acceptable salts thereof. The compounds have anti-inflammatory, analgesic, and antipyretic activities and, accordingly, are useful in the treatment of inflammation, pain and/or pyrexia.
    Type: Grant
    Filed: March 24, 1975
    Date of Patent: April 26, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Karl G. Untch
  • Patent number: 4014336
    Abstract: An inhalation device having an elongate housing having one or more passageways for the passage of air therethrough. Each passageway, of relatively small diameter, opens into an emptying chamber, of relatively greater diameter, adjacent that end of the housing which is adapted for insertion into the mouth or nose of a user. Adjacent that end of the emptying chamber closest to the passageway(s), the housing has means for receiving or presenting a unit dose of powdered medicament for administration. Means are provided to open the medicament holder as it is being inserted into, or after it has been inserted into, the means for receiving or presenting a unit dose of powdered medicament for administration. During inhalation, the air stream passing over and directed into the powdered medicament holder entrains the powdered medicament which is then carried into the nose, throat or lungs of the user where beneficial or therapeutic action of the medicament occurs.
    Type: Grant
    Filed: November 20, 1975
    Date of Patent: March 29, 1977
    Assignee: Syntex Puerto Rico, Inc.
    Inventor: Stanley Mathes
  • Patent number: 4011320
    Abstract: 7(8)-substituted triazinobenzimidazoles represented by the formula: ##STR1## where R is a lower alkyl group having 1 to 4 carbon atoms; R' is diloweralkylaminoalkyl (C.sub.2-6) or alkyl having 1 to 18 carbon atoms; R.sup.2 is phenylsulfinyl, phenoxyethoxy, benzyloxyethoxy, methoxyethylsulfinyl, or 3-chloroprop-1-ylsulfinyl; the R.sup.2 -substitution being at the 7(8)-position; or a pharmaceutically acceptable salt thereof.The compounds are useful as pesticides, particularly as antifungal and anthelmintic agents.
    Type: Grant
    Filed: March 8, 1976
    Date of Patent: March 8, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Colin C. Beard, John A. Edwards, John H. Fried