Patents by Examiner Henry R. Jiles

Patent number: 4851552
Abstract: 13-oxabicyclo[10.3.0]pentadecane, a valuable ambergris fragrance, is prepared by reacting cyclododecanone with cyanoacetic acid in the presence of a Knoevenagel catalyst to form cyclododecenylacetonitrile, the nitrile is hydrolyzed to cyclododecenylacetic acid, and the acid is cyclized to the lactone, and the lactone is reduced to the corresponding diol which is cyclized to 13-oxabicyclo[10.3.0]pentadecane.
Type: Grant
Filed: January 10, 1985
Issued: July 25, 1989
Assignee: Huels Aktiengesellschaft
Inventor: Manfred Kaufhold
Patent number: 4766217
Abstract: 5,6,-dihydro-pyrrolo[2,1-a]isoquinolines of the formula ##STR1## are prepared by heating a 1-(3-furyl)-3,4-dihydro-isoquinoline of the formula ##STR2## in a primary or secondary amine to at least 80.degree. C. for several hours, the amine is removed, the reaction product is treated with dilute acid, and the reaction product is purified and isolated.
Type: Grant
Filed: June 16, 1987
Issued: August 23, 1988
Assignee: Boehringer Ingelheim KG
Inventors: Walter Losel, Otto Roos, Gerd Schnorrenberger
Patent number: 4760072
Abstract: There are described new forms of nedocromil sodium, methods of producing these new forms and pharmaceutical formulations, especially pressurized inhalation aerosol formulations, containing finely divided nedocromil sodium. The formulations are indicated for the treatment of reversible obstructive conditions of the airways.
Type: Grant
Filed: April 8, 1985
Issued: July 26, 1988
Assignee: Fisons, plc
Inventors: Kenneth Brown, Andrew R. Clark, Richard Salliss
Patent number: 4754033
Abstract: A process for producing pyridine-2,3-dicarboxylic acid derivatives of the formula ##STR1## is described. The process is based on the cleavage of HNR.sub.10 R.sub.11 from 1-amino-1,2,3,4-tetrahydropyridine-2,3-dicarboxylic acid derivatives of the formula II ##STR2## to give 1,4-dihydropyridine-2,3-dicarboxylic acid derivatives of the formula III ##STR3## and subsequent oxidation of these compounds to obtain pyridine-2,3-dicarboxylic acid derivatives of the formula I. According to one variant of the process, the 1,4-dihydropyridine-2,3-dicarboxylic acid derivatives of the formula III are obtained directly, without isolation of the intermediately formed 1-amino-1,2,3,4-tetrahydropyridine-2,3-dicarboxylic acid derivatives of the formula II, by reaction of .alpha.,.beta.-unsaturated hydrazones of the formula IV ##STR4## with ethene-1,2-dicarboxylic acid derivatives of the formula V ##STR5## and subsequently oxidized to pyridine-2,3-dicarboxylic acid derivatives of the formula I. In the above formulae, R.sub.1, R.
Type: Grant
Filed: August 2, 1985
Issued: June 28, 1988
Assignee: Ciba-Geigy Corporation
Inventor: Adrian Waldner
Patent number: 4754032
Abstract: Compounds of formula I ##STR1## can be used as optical brighteners.
Type: Grant
Filed: February 26, 1986
Issued: June 28, 1988
Assignee: Sandoz Ltd.
Inventors: David L. Connell, John M. Farrar, Jurg Heller, Hans-Rudolf Schmid
Patent number: 4751227
Abstract: 5-(6-Imidazo[1,2-a]pyridyl)pyridine derivatives represented by general formula: ##STR1## wherein X represents hydrogen atom or methyl group; Y represents cyano group, carboxamido group, hydrogen atom, amino group or a halogen atom; Z represents hydrogen atom or a lower alkyl group; W represents hydrogen atom or a lower alkyl group; R.sup.1 represents hydrogen atom, a lower alkyl group, phenyl group, a group shown by formula: --CH.sub.2 R.sup.4 in which R.sup.4 is a lower alkoxy group, or a group shown by formula: ##STR2## in which R.sup.5 and R.sup.6 are hydrogen atom or a lower alkyl group R.sup.2 represents hydrogen atom or a halogen atom; and R.sup.3 represents hydrogen atom, a lower alkyl group or a halogen atom; or a tautomer thereof; and pharmacologically acceptable salts thereof are disclosed. The 5-(6-imidazo[1,2-a]pyridyl)pyridine derivatives are effective for treating congestive heart failures.
Type: Grant
Filed: March 26, 1986
Issued: June 14, 1988
Assignee: Eisai Co., Ltd.
Inventors: Motosuke Yamanaka, Kazutoshi Miyake, Shinji Suda, Hideto Ohhara, Toshiaki Ogawa
Patent number: 4747867
Abstract: Herbicidally active 1-aryl-4-cyano-5-halogenopyrazoles of the formula ##STR1## in which R is hydrogen or alkyl,Hal is halogen, andAr is substituted phenyl or represents polysubstituted pyridyl.Intermediates of the formulas ##STR2## are also disclosed.
Type: Grant
Filed: May 22, 1986
Issued: May 31, 1988
Assignee: Bayer Aktiengesellschaft
Inventors: Reinhold Gehring, Uta Jensen-Korte, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt
Patent number: 4747866
Abstract: A pirimidinyloxyalkanamide derivative of Formula 1: ##STR1## wherein R.sub.1 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkylthio group, a lower alkenylthio group, a lower alkynylthio group, a halogenated lower alkenylthio group, a cycloalkylthio group, an aroxyalkylthio group, a lower alkoxyl group, an amino group, a methanesulfonyl group, a trifluoromethyl group, an anilino group which may be substituted with a halogen atom or a benzylthio group which may be substituted with a halogen atom; R.sub.2 represents a hydrogen atom, a halogen atom, a lower alkyl group, a trifluoromethyl group, an amino group, a lower alkoxy group or a lower alkylthio group; R.sub.3 represents an ethyl group or an n-propyl group; and R.sub.
Type: Grant
Filed: August 15, 1986
Issued: May 31, 1988
Assignee: Ube Industries, Ltd.
Inventors: Tetsuo Takematsu, Yasutomo Takeuchi, Mitsuaki Takenaka, Seiji Takamura, Hiroshi Hase
Patent number: 4747868
Abstract: The new compounds of the formula I or salts thereof ##STR1## in which R denotes a (substituted) cyclohexyl radical or a (substituted) cyclohexenyl radical; and Y denotes cyano, a (substituted) (di)(thio)carboxylic acid (ester), carboxamide or acetal radical, a keto or oxime radical or a heterocyclic radical, possess an advantageous action as plant growth-regulators and, in addition, have favorable herbicidal and fungicidal properties.
Type: Grant
Filed: April 17, 1986
Issued: May 31, 1988
Assignee: Hoechst Aktiengesellschaft
Inventors: Roland Schmierer, Hilmar Mildenberger, Reinhard Handte, Helmut Burstell, Burkhard Sachse, Klaus Bauer, Hermann Bieringer
Patent number: 4748244
Abstract: The invention relates to a process for the preparation of pyridine-2,3-dicarboxylic acid derivatives of formula ##STR1## which process comprises reacting a hydrazone of formula II ##STR2## with a maleic acid derivative of formula III ##STR3## to give a 1-amino-1,4-dihydropyridine-2,3-dicarboxylic acid derivative of formula IV ##STR4## and subsequently removing R.sub.9 R.sub.10 NH. In the above formulae, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.9, R.sub.10 and X are as defined in claim 1. The pyridine-2,3-dicarboxylic acid derivatives of formula I are intermediates for the preparation of herbicidal compounds.
Type: Grant
Filed: May 3, 1985
Issued: May 31, 1988
Assignee: Ciba-Geigy Corporation
Inventors: Adrian Waldner, Achim Roloff, Daniel Bellus
Patent number: 4748258
Abstract: A mixture of cafestol and kahweol is obtained from coffee oil by treating coffee oil with anhydrous methanol in the presence of a basic catalyst, dissolving methyl esters which are formed by the reaction and then extracting the cafestol and kahweol from the reaction medium with aqueous methanol and then with a low-boiling chlorinated hydrocarbon. A process for the preparation of cafestol from kahweol is also disclosed.
Type: Grant
Filed: April 23, 1987
Issued: May 31, 1988
Assignee: Nestec S.A.
Inventor: Raymond Bertholet
Patent number: 4748182
Abstract: This invention relates to aromatic 2-aminoalkyl derivatives of 1,2-benzoisothiazol-3(2H)one-1,1-dioxides, processes for the preparation of same, and to their use as anxiolytic and antihypertensive agents.
Type: Grant
Filed: March 5, 1986
Issued: May 31, 1988
Assignee: Merrell Dow Pharmaceuticals Inc.
Inventors: Marcel Hibert, Maurice W. Gittos
Patent number: 4746354
Abstract: Herbicidally and insecticidally active 4-nitro-1-phenylpyrazoles of the formula ##STR1## in which R.sup.1 and R.sup.2 each independently is hydrogen, alkyl, cycloalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl or halogenoalkyl,R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently is hydrogen, halogen, cyano, nitro, alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkoxycarbonyl, or --(X).sub.n --R.sup.8,X is oxygen, sulphur, sulphinyl or sulphonyl,n is 0 or 1, andR.sup.8 is halogenoalkyl.
Type: Grant
Filed: March 4, 1986
Issued: May 24, 1988
Assignee: Bayer Aktiengesellschaft
Inventors: Reinhold Gehring, Uta Jensen-Korte, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt, Wolfgang Behrenz
Patent number: 4746671
Abstract: Novel [[[(3-pyridinyl)methylen]amino]oxy]alkanoic acids and esters, compositions containing the same, and methods of treating clinical conditions related with the production of thromboxane A.sub.2, prostacyclin and/or prostaglandins D.sub.2, E.sub.2 and F.sub.2.alpha..
Type: Grant
Filed: July 23, 1986
Issued: May 24, 1988
Assignee: Janssen Pharmaceutica N.V.
Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers, Victor Sipido, Marc G. Venet
Patent number: 4745111
Abstract: Compounds of the formula ##STR1## where R and A have the meanings given in the description, and their use in the treatment of disorders are described.
Type: Grant
Filed: July 9, 1986
Issued: May 17, 1988
Assignee: BASF Aktiengesellschaft
Inventors: Gerd Steiner, Hans-Juergen Teschendorf, Liliane Unger
Patent number: 4745189
Abstract: A method of preparing N-halogenated organic heterocyclic compounds by reacting in an aqueous mixture under alkaline conditions (e.g. NaOH) and in the presence of a halogenated organic compound (e.g. methylene chloride), a N-hydrogen organic heterocyclic compound containing at least one NH group (e.g. 5,5-dimethylhydantoin) and a halogen-producing chemical (e.g. Br.sub.2).
Type: Grant
Filed: June 23, 1986
Issued: May 17, 1988
Assignee: Ethyl Corporation
Inventors: John Y. Lee, Mark A. Templeton
Patent number: 4745120
Abstract: The present invention relates to new pyridines substituted in the 3-position, of the formula ##STR1## and to a process for their preparation. The compounds bring about specific inhibition of thromboxane synthetase and can thus be used as medicaments.
Type: Grant
Filed: August 21, 1985
Issued: May 17, 1988
Assignee: Hoechst Aktiengesellschaft
Inventors: Gunther Wess, Wilhelm Bartmann, Gerhard Beck, Hans-Hermann Lau
Patent number: 4744819
Abstract: Novel pyridinecarboxamide derivatives having the general formula (I) ##STR1## or salts thereof wherein R is hydrogen atom, alkoxy group, aralkyloxy group or a group of --(CH.sub.2).sub.n --R.sub.1 wherein n is an interger from 1 to 3 and R.sub.1 is hydrogen atom, hydroxy group, lower alkoxy group, mercapto group, lower alkylthio group, amino group, di-lower alkylamino group, C.sub.3-11 alkyl group, lower alkenyl group, lower alkynyl group, cycloalkyl group, 5- or 6-membered heterocyclic group, or aryl group which may be substituted by one or two substituents of halogen, lower alkyl or lower alkoxy;R.sub.2 is halogen atom, lower alkyl group, hydroxy group, lower alkoxy group, aryloxy group, carboxy group or lower alkoxycarbonyl group;R.sub.3 is hydrogen atom, halogen atom or lower alkyl group, which possess plant growth inhibitory activities and also anti-inflammatory activity.
Type: Grant
Filed: October 21, 1985
Issued: May 17, 1988
Assignee: Daicel Chemical Industries Ltd.
Inventors: Yoichiro Ueda, Yoshiyuki Hirako, Kazuhisa Masamoto, Yukihisa Goto, Hiroshi Yagihara, Yasuo Morishima, Hirokazu Osabe
Patent number: 4744813
Abstract: An imidazolidine-2-one having the formula ##STR1## in which X, X', Y and Y' are the same or different and are selected from the group consisting of trifluoromethyl, chloro, bromo, fluoro, hydrogen, cyano, alkyl, thioalkyl, halothialkyl, alkoxy and sulfonylalkyl, wherein the alkyl groups have from one to four carbon atoms; andR is selected from the group consisting of hydrogen and alkyl wherein the alkyl groups have from one to four carbon atoms. The compounds are useful as herbicidal agents.
Type: Grant
Filed: November 24, 1986
Issued: May 17, 1988
Assignee: Stauffer Chemical Co.
Inventor: Eugene G. Teach
Patent number: 4745127
Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit the mammalian 5-lipoxygenase enzyme, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.
Type: Grant
Filed: January 7, 1987
Issued: May 17, 1988
Assignee: Merck Frosst Canada, Inc.
Inventors: Joseph G. Atkinson, Yvan Guindon, Cheuk K. Lau