Patents Examined by Henry R. Jiles
  • Patent number: 4705865
    Abstract: 1-Aminoalkyl-imidazolium compounds which contain in the 3-position and on the terminal amino group fibre-reactive groupings which have been formed by the addition of an epihalohydrin.These bireactive imidazolium salts are suitable in particular for improving the dye yield and fastness to wet processing of dyeings and printings which have been produced on cellulose fibre materials with anionic dyes, for example with reactive or direct dyes.
    Type: Grant
    Filed: November 4, 1985
    Date of Patent: November 10, 1987
    Assignee: Ciba-Geigy Corporation
    Inventor: Rosemarie Topfl
  • Patent number: 4705785
    Abstract: Novel substituted thiacycloalkeno [3,2-b] pyridines are described. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstrictor activity.
    Type: Grant
    Filed: April 9, 1986
    Date of Patent: November 10, 1987
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Charles F. Schwender, John H. Dodd
  • Patent number: 4705554
    Abstract: A benzofuranyloxyphenylurea derivative having the formula: ##STR1## wherein X is a halogen atom or a trifluoromethyl group, n is an integer of from 0 to 2, Y is a hydrogen atom, a halogen atom or a trifluoromethyl group, R.sup.1 is a lower alkyl group, and R.sup.2 is a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a lower alkoxy group. The compounds are useful as herbicides.
    Type: Grant
    Filed: November 14, 1986
    Date of Patent: November 10, 1987
    Assignee: Mitsubishi Chemical Industries Limited
    Inventors: Susumu Matsumoto, Shigeru Suzuki, Hisao Watanabe, Hiroshi Hanabe
  • Patent number: 4705793
    Abstract: Novel pyrazolo[3,4-b]pyridine lactams which are useful as anxiolytics are disclosed including methods of preparation, pharmaceutical compositions containing them and intermediates used in their preparation.
    Type: Grant
    Filed: June 25, 1985
    Date of Patent: November 10, 1987
    Assignee: ICI Americas Inc.
    Inventor: James F. Resch
  • Patent number: 4704459
    Abstract: This invention relates to a process for industrially producing a 1-substituted aryl-1,4-dihydro-4-oxonaphthyridine derivative and a salt thereof which are useful as an antibacterial agent, and also to intermediates therefor and processes for producing the intermediates.
    Type: Grant
    Filed: January 17, 1986
    Date of Patent: November 3, 1987
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Yozo Todo, Tetsuo Yamafuji, Katsuyuki Nagumo, Isao Kitayama, Hideyoshi Nagaki, Mikako Miyajima, Yoshinori Konishi, Hirokazu Narita, Shuntaro Takano, Isamu Saikawa
  • Patent number: 4704462
    Abstract: Substituted 2,3,3a,6-tetrahydro-6-oxobenzofuran derivatives have been prepared. These neolignans are found to have potent and specific PAF (Platelet-Activating-Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by PAF, for example, pain, fever, inflammation, cardiovascular disorder, asthma, lung edema, allergic disorders, skin diseases, psoriasis, toxic shock syndrome and adult respiratory distress syndrome.
    Type: Grant
    Filed: August 22, 1985
    Date of Patent: November 3, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Michael N. Chang, San-Bao Hwang, Mitree M. Ponpipom, Robert L. Bugianesi
  • Patent number: 4704458
    Abstract: Disclosed herein is an improved process for preparing 1RS-3'RS epimer of aminated phthalideisoquinolines represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen atom or a lower alkoxy group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently hydrogen atom, amino group or a lower alkoxy group with at least one of R.sup.3 -R.sup.6 being amino group, and R.sup.7 is a lower alkyl group. The improvement comprises, after having reduced a mixture of epimers of corresponding nitro compounds of the general formula (I) wherein the amino group is replaced by nitro group into the amino compounds (I), treating said amino compound at a temperature in the range of 20.degree.-100.degree. C. in an aliphatic lower alcohol in the presence of an alkali to epimerize 1RS-3'SR epimer of said amino compound into said 1RS-3'RS epimer thereof.
    Type: Grant
    Filed: January 23, 1985
    Date of Patent: November 3, 1987
    Assignee: Mitsubishi Chemical Industries Limited
    Inventors: Yoshiyuki Takeda, Osamu Kawashima, Shiro Furukawa, Yasukazu Ogino
  • Patent number: 4703119
    Type: Grant
    Filed: June 4, 1985
    Date of Patent: October 27, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Egbert Wehinger, Horst Meyer
  • Patent number: 4703057
    Abstract: The invention relates to 1-tert.-butylamino-3-(4-hydroxy-8-thiochromanyloxy)-2-propanol.
    Type: Grant
    Filed: September 30, 1986
    Date of Patent: October 27, 1987
    Assignee: ADIR Et Compagnie
    Inventors: Bernard Marchand, Yves M. Gargouil
  • Patent number: 4703122
    Abstract: The invention relates to a new process for preparing O-pyrimidinyl N,N-dimethylcarbamates of the formula (I) ##STR1## in which R stands for straight-chain or branched alkyl,R.sup.1 stands for hydrogen or optionally substituted radicals from the series alkyl, alkoxy, alkylthio, alkylsulphinyl or alkylsulphonyl,R.sup.2 stands for hydrogen or optionally substituted alkyl orR.sup.1 and R.sup.2 together can form a fused-on optionally substituted saturated or unsaturated ring,A stands for straight-chain or branched alkylene andn stands for 0, 1 or 2.Components of the above formula (I) are obtained when hydroxypyrimidines of the formula (II) ##STR2## in which R, R.sup.1, R.sup.2, A and n have the above mentioned meanings,are reacted with N,N-dimethylcarbamoyl halides of the formula (III)Hal--CO--N(CH.sub.3).sub.2 (III)in whichHal stands for chlorine or bromine, at temperatures between 0.degree. C. and 150.degree. C. and in particular between 20.degree. C. and 100.degree. C.
    Type: Grant
    Filed: September 20, 1985
    Date of Patent: October 27, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventor: Fritz Maurer
  • Patent number: 4703044
    Abstract: The invention provides novel imidazoquinolines, processes for their preparation and pharmaceutical compositions containing them. The compounds have Formula I ##STR1## wherein A is a C.sub.1 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,B is a C.sub.2 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,R.sup.1 and R.sup.2 are the same or different and are hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxyalkyl, C.sub.1-6 hydroxyalkyl, hydroxy, halogen, nitro, carboxy, carboxylic lower alkyl ester, carbamoyl, carbamoyloxy, cyano, loweralkanoyl, lower alkanoylamino or trifluoromethyl, Het is a heterocyclic group chosen from imidazolyl, imidazolinyl, benzimidazolyl, thiazolyl, thiazolinyl, quinolyl, piperidyl, pryidyl, benzothiazoly and pyrimidyl, any of which heterocyclic groups may be substituted, and x is 0 or 1, and pharmaceutically acceptable salts thereof.The compounds are anti-ulcer/anti-secretory agents.
    Type: Grant
    Filed: December 11, 1985
    Date of Patent: October 27, 1987
    Assignee: John Wyeth & Brother Limited
    Inventor: Roger Crossley
  • Patent number: 4703055
    Abstract: The invention concerns novel benzamides and their pharmacologically acceptable salts which are useful as gastromotor agents and correspond to the following general formula (I): ##STR1## in which: R.sub.1 is lower alkyl, lower alkenyl or a hydrogen atom;R.sub.2 is alkyl, lower alkenyl, benzyl, cycloalkylalkyl, cycloalkenylalkyl or a hydrogen atom;R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 each are lower alkyl or a hydrogen atom, andX is a halogen atom.
    Type: Grant
    Filed: July 7, 1986
    Date of Patent: October 27, 1987
    Assignee: Societe d'Etudes Scientifiques et Industrielles de l'Ile-de-France
    Inventors: Jacqueline Franceschini, Renee Gardaix-Luthereau, Josette Margarit
  • Patent number: 4701543
    Abstract: Oxygenated decaline derivatives of formula ##STR1## wherein X represents a COOH or a CHO group are obtained according to a process which consists in the oxidation of a ketone of formula ##STR2## by means of oxygen in a basic medium constituted by potassium tert-butoxide in 1,2-dimethoxyethane.Compounds (I) are useful starting materials for the preparation of AMBROX.RTM. (registered tradename of Firmenich SA, Geneva, Switzerland) which is an ingredient in perfumes.
    Type: Grant
    Filed: July 18, 1986
    Date of Patent: October 20, 1987
    Assignee: Firmenich S.A.
    Inventors: Ferdinand Naef, Christian Vial
  • Patent number: 4701542
    Abstract: A process for the resolution of hemiacetal compounds of the formula ##STR1## wherein A is a hydrocarbon chain containing 1 to 16 groups, the said chain optionally containing at least one heteroatom, at least one unsaturation, the assembly of the group constituting the chain may be a mono- or polycyclic system including a spiro or endosystem and the assembly of chain A and the carbon atoms attached thereto can contain at least one chiral atom or the hemiacetal moiety thereto which can present a chirality due to the dissymetric spatial configuration of the molecule and Y is selected from the group consisting of hydrogen, alkyl of 1 to 18 carbon atoms optionally substituted, --CY.sub.3 ' and the .beta.,.gamma.
    Type: Grant
    Filed: March 31, 1986
    Date of Patent: October 20, 1987
    Assignee: Roussel Uclaf
    Inventors: Jean Tessier, Jean-Pierre Demoute
  • Patent number: 4701459
    Abstract: Novel series of 2,3-dihydro-2-oxo-1H-imidazo[4,5-b]quinolinyl amine derivatives of Formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl; R.sub.2 is hydrogen, lower alkyl, lower alkoxy, halogen; R.sub.3 is hydrogen, lower alkyl; R.sub.4 is hydrogen, lower alkyl, alkanoyl, phenylalkanoyl wherein phenyl is optionally substituted with halogen, lower alkyl, lower alkoxy; R.sub.3 and R.sub.4 are joined together to form morpholinyl, piperidinyl or pyrrolidinyl optionally substituted with --CO.sub.2 R.sub.5 or ##STR2## wherein R.sub.5 is hydrogen or lower alkyl, and R.sub.6 is hydrogen, lower alkyl, cycloalkyl; 4-R.sub.7 -piperazinyl wherein R.sub.7 is --CO.sub.2 R.sub.8 wherein R.sub.8 is lower alkyl, phenyl optionally substituted with up to 2 halogen, lower alkyl or lower alkoxy; phenylalkanoyl of 7 to 10 carbon wherein phenyl is unsubstituted or independently substituted with up to 2 halogen, lower alkyl, lower alkoxy.
    Type: Grant
    Filed: July 8, 1986
    Date of Patent: October 20, 1987
    Assignee: Bristol-Myers Company
    Inventors: Nicholas A. Meanwell, John J. Wright
  • Patent number: 4699985
    Abstract: An improved vanadium/phosphorus catalyst for the oxidation of n-butane to maleic anhydride is disclosed. Preferably, the catalyst contains a promoter. A process for the oxidation of n-butane to maleic anhydride using the improved catalyst is also disclosed.
    Type: Grant
    Filed: June 13, 1986
    Date of Patent: October 13, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Tom A. Bither, Jr.
  • Patent number: 4699652
    Abstract: The invention is directed to fungicidal pyridine derivatives and their N-amino salts and acid addition salts, said pyridine derivatives having the formula ##STR1## wherein R is mono-, di- or trisubstituted phenyl, wherein the substituents are the same or different and are selected from the group consisting of 1 to 3 halogen, 1 or 2 C.sub.1-3 -alkyl, 1 or 2 C.sub.1-3 -alkoxy and 1 or 2 trifluoromethyl moieties; R.sup.1 is hydrogen, C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl or C.sub.2-6 -alkynyl; R.sup.2 is hydrogen; R.sup.3 is selected from the group consisting of --CO--R.sup.4, --C(OR.sup.5).dbd.CHR.sup.6, --CH(R.sup.4)OR.sup.5, --C(R.sup.4).dbd.NOR.sup.7 and ##STR2## R.sup.4 is hydrogen or C.sub.1-5 -alkyl; R.sup.5 is C.sub.1-4 -alkyl; R.sup.6 and R.sup.7 are hydrogen or C.sub.1-4 -alkyl; n is 2 or 3; or R.sup.2 taken together with R.sup.4 is equal to the group --CH.dbd.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: October 13, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Beat Zehnder
  • Patent number: 4699917
    Abstract: Novel 6H-dibenz[b,e][1,4]oxathiepin derivatives of the formulae I and Ia are employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: January 9, 1986
    Date of Patent: October 13, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Joshua Rokach
  • Patent number: 4699984
    Abstract: Shown is the process which comprises heating 4-(2-fluorophenyl)-2,6-dimethyl-3,5-pyridinedicarboxylic acid to produce a mixture of 4-(2-fluorophenyl)-2,6-dimethylpyridine and 2,4-dimethyl-5H-[1]benzopyrano[3,4-c]pyridin-5-one, separating the components of said mixture and nitrating 4-(2-fluorophenyl)-2,6-dimethylpyridine to produce 4-(2-fluoro-5-nitrophenyl)-2,6-dimethylpyridine. Also shown are the 3-step synthesis of 4-(2-fluorophenyl)-2,6-dimethyl-3,5-pyridinedicarboxylic acid from 2-fluorobenzaldehyde and the five step synthesis of 1-ethyl-6-fluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-oxo-3-quinolin ecarboxylic acid, a highly potent antibacterial agent, starting with 4-(2-fluoro-5-nitrophenyl)-2,6-dimethylpyridine. Other intermediates shown in said five step synthesis include 3-(2,6-dimethyl-4-pyridinyl)-4-fluorobenzeneamine and diethyl 4-fluoro-3-(2,6-dimethyl-4-pyridinyl)anilinomethylenemalonate.
    Type: Grant
    Filed: February 20, 1986
    Date of Patent: October 13, 1987
    Assignee: Sterling Drug Inc.
    Inventor: Baldev Singh
  • Patent number: 4699983
    Abstract: 2-Amino-4-trichloromethylpyridine of the formula I ##STR1## The compound is an effective nitrification inhibitor.
    Type: Grant
    Filed: March 12, 1986
    Date of Patent: October 13, 1987
    Assignee: BASF Aktiengesellschaft
    Inventors: Helmut Hagen, Hans Ziegler, Rolf-Dieter Kohler, Ernst-Heinrich Pommer, Jurgen Dressel