Nitrogen In Acid Moiety Patents (Class 560/16)
  • Patent number: 4960881
    Abstract: The invention relates to carbonates of formula: ##STR1## in which X is a fluorine, chlorine or bromine atom and R.sup.1 is different from the ##STR2## group and represents: a substituted or non-substituted, saturated or unsaturated, aliphatic, araliphatic, primary, secondary, tertiary or cycloaliphatic radical. These .alpha.-chlorinated carbonates are prepared by the action of a compound of formula R.sup.1 OH on a chloroformate of formula: ##STR3## in a solvent medium in the presence of an acid scavenger which is added after the two preceding compounds. They are used to block the amine function of amino acids. The .alpha.-chlorinated carbonate and amino acid are reacted in a solvent medium at a temperature of -5.degree. to 100.degree. C. in the presence of an acid scavenger. Blocked amines are very useful in peptide synthesis.
    Type: Grant
    Filed: June 6, 1988
    Date of Patent: October 2, 1990
    Assignee: Societe Nationale des Poudres et Explosifs
    Inventors: Gerard Barcelo, Jean-Pierre Senet, Gerard Sennyey
  • Patent number: 4945106
    Abstract: Prostaglandin analogues exhibiting activity at thromboxane receptor sites have been prepared.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: July 31, 1990
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 4937253
    Abstract: This invention relates to ester prodrugs for alkanoic acid compounds useful as leukotriene antagonists, and pharmaceutical compositions containing such ester prodrug compounds. This invention also relates to methods of treating diseases in which leukotrienes are a factor by administration of an effective amount of the above compounds or compositions.
    Type: Grant
    Filed: September 23, 1988
    Date of Patent: June 26, 1990
    Assignee: SmithKline Beecham Corporation
    Inventors: John G. Gleason, Ralph F. Hall, John F. Newton, Kathleen A. Phipps, Joanne Smallheer
  • Patent number: 4933367
    Abstract: This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.
    Type: Grant
    Filed: March 12, 1987
    Date of Patent: June 12, 1990
    Assignee: Boehringer Mannheim GmbH
    Inventors: Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuhnle
  • Patent number: 4929755
    Abstract: In the process of hydrocarboxylating an .alpha.-enamide with CO and H.sub.2 O or an organic hydroxyl compound to produce an N-acyl-.alpha.-amino acid or ester, respectively, the improvement comprising using as the .alpha.-enamide reactant, an .alpha.-enamide which has a chiral center that is essentially all L or D, thereby producing a reaction mixture containing diastereomeric N-acyl-.alpha.-amino acids or esters having two chiral centers, said mixture having essentially no enantiomeric pairs.
    Type: Grant
    Filed: December 19, 1986
    Date of Patent: May 29, 1990
    Assignee: The Standard Oil Company
    Inventors: Mark C. Cesa, Robert A. Dubbert, James D. Burrington
  • Patent number: 4929641
    Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.
    Type: Grant
    Filed: May 11, 1988
    Date of Patent: May 29, 1990
    Assignee: Schering Corporation
    Inventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 4929754
    Abstract: The invention relates to new benzenesulphonamidoindanyl compounds useful in the treatment and prophylaxis of thromboembolic diseases, arteriosclerosis and tumor metastasis.
    Type: Grant
    Filed: February 1, 1989
    Date of Patent: May 29, 1990
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Josef Nickl, Armin Heckel, Erich Muller, Berthold Narr, Johannes Weisenberger, Wolfgang Eisert, Thomas Muller
  • Patent number: 4918223
    Abstract: N-acylated mercapto-.alpha.-amino acids of the general formula ##STR1## are prepared by reacting a nitrile of the general formulaR.sub.1 -CN (II)at a temperature between 0.degree. C. and 100.degree. C. in water or in a mixture of water and an organic solvent which is at least partially miscible with water, in the presence of a base with a mercapto-.alpha.-amino acid of the general formula ##STR2## and subsequently releasing the N-acylated mercapto-.alpha.-amino acid of general formula (I) with an acid. Mercapto-.alpha.-amino acids can be selectively acylated on the amino group in this manner in a relatively simple manner.
    Type: Grant
    Filed: August 9, 1988
    Date of Patent: April 17, 1990
    Assignee: Degussa Aktiengesellschaft
    Inventors: Hans-Peter Krimmer, Karlheinz Drauz
  • Patent number: 4908383
    Abstract: Novel N-phenyl-N-carboxythioureas of the formula I ##STR1## in which R.sub.1 and R.sub.2 each represents C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.5 -C.sub.6 cycloalkenyl,R.sub.3 represents hydrogen, halogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy or C.sub.1 -C.sub.10 alkylthio,R.sub.4 represents C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl or phenyl-C.sub.1 -C.sub.7 alkyl; C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl or phenyl-C.sub.1 -C.sub.7 alkyl each mono- or poly-substituted by halogen or interrupted one or several times by oxygen and/or sulphur; C.sub.3 -C.sub.8 cycloalkyl; or C.sub.3 -C.sub.8 cycloalkyl mono- or poly-substituted by halogen or by C.sub.1 -C.sub.5 alkyl, andR.sub.5 represents C.sub.1 -C.sub.10 alkyl; phenyl-C.sub.1 -C.sub.7 alkyl; C.sub.1 -C.sub.10 alkyl or phenyl-C.sub.1 -C.sub.7 alkyl each mono- or poly-substituted by halogen or interrupted one or several times by oxygen and/or sulphur; C.
    Type: Grant
    Filed: May 23, 1989
    Date of Patent: March 13, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Jozef Drabek, Josef Ehrenfreund
  • Patent number: 4906662
    Abstract: Disclosed are phenol derivatives of the formula ##STR1## wherein R.sup.1 is a substituted phenyl group, R.sup.2 and R.sup.3 are C.sub.1 -C.sub.6 alkyl group and of the formula ##STR2## wherein R.sup.8, R.sup.9 and R.sup.10 are C.sub.1 -C.sub.6 alkyl and the like and A is H, C.sub.1 -C.sub.6 alkylsulfonyl and the like substituents. These compounds and some related compounds have anti-inflammatory activity and lipoxygenase inhibitory activity.
    Type: Grant
    Filed: January 27, 1987
    Date of Patent: March 6, 1990
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Kinji Hashimoto, Kiyoto Goto, Ken-ichi Kanai, Yoshiaki Tsuda
  • Patent number: 4898977
    Abstract: The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl or the radical of a natural amino acid, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, amino, hydroxy, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid, and R.sup.3 represents optionally substituted hydroxy or amino, by sigmatropic rearrangement of a suitable allyl ester, halolactonisation of the resulting .gamma.,.delta.-unsaturated acid or of a suitable derivative thereof, exchange of halogen for a nitrogen-containing nucleophile, opening of the lactone ring and freeing of the amino group. Compounds of the formula I are starting materials for the preparation of renin-inhibitors which have an anti-hypertensive action.
    Type: Grant
    Filed: August 13, 1987
    Date of Patent: February 6, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Herold, Christof Angst
  • Patent number: 4897109
    Abstract: A composition for protecting culture plants from the phytotoxic action of herbicidally active chloracetanilides contains as active ingredient an acylamine derivative of the formula I ##STR1## wherein X is oxygen, sulfur, --SO-- or --SO.sub.2 --,Q is an alkyl, alkenyl, alkinyl group, which may be interupted by oxygen, sulfur, sulfinyl or sulfonyul, or a test 1,3-dioxolan-2-yl-alkyl, 1,3-dioxolan-4-alkyl, 2,2-dialkyl-1,3-dioxolan-4-ylalkyl, 1,3-dioxan-2-ylalkyl, 2-benzopyranylalkyl, alkoxycarbonyl alkenyl-oxycarbonyl or tetrahydrofurylalkyl, or the groupOX represents also a halogenoalkyl radical,n is 1, 2 or 3,Z is hydrogen, halogen, alkyl or dioxymethylene,A is a C.sub.1 -C.sub.8 -hydrocarbon radical which may be staight-chained, branched or cyclic and which is unsubstituted or substituted by alkoxy, alkylthio, cyano or halogen,B is hydrogen, a C.sub.1 -C.sub.
    Type: Grant
    Filed: October 5, 1987
    Date of Patent: January 30, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Henry Martin
  • Patent number: 4882341
    Abstract: The invention relates to amino substituted propenoates and their use against fungi.
    Type: Grant
    Filed: September 9, 1988
    Date of Patent: November 21, 1989
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Ian T. Kay
  • Patent number: 4879309
    Abstract: Novel mercapto-acylamino acids useful as analgesic, as well as in the treatment of hypertension and congestive heart failure and combinations of mercapto acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension and congestive heart failure are disclosed.
    Type: Grant
    Filed: January 30, 1989
    Date of Patent: November 7, 1989
    Assignee: Schering Corporation
    Inventors: Ronald J. Doll, Bernard R. Neustadt
  • Patent number: 4877824
    Abstract: Compounds of the formula (I) ##STR1## in which the Rs independently of one another are H, phenyl, naphthyl or C.sub.7 -C.sub.30 alkaryl and R.sup.1 is H, C.sub.1 -C.sub.8 alkyl, C.sub.7 -C.sub.9 aralkyl, C.sub.5 -C.sub.12 cycloalkyl, phenyl, naphthyl, C.sub.7 -C.sub.30 alkaryl or a group of the formula (II)--(CH.sub.2).sub.a --SR.sup.3 (II)R.sup.2 is C.sub.7 -C.sub.30 alkaryl, phenyl, naphthyl or phenyl containing, in the para-position, an HO or C.sub.1 -C.sub.18 alkoxy group or a group of the formulae ##STR2## or R.sup.1 and R.sup.2, together with the nitrogen atom to which they are attached, are a radical of the formula (III) ##STR3## R.sup.3 is a radical of the formulae --(CH.sub.2).sub.b --COOR.sup.6 or --(CH.sub.2).sub.2 OCOR.sup.7, a is the number 1, 2 or 3 and b is the number 1 or 2, and R.sup.4 is phenyl or a group of the formula (II), the two R.sup.5 s independently of one another are H, C.sub.1 -C.sub.24 alkyl, C.sub.5 -C.sub.12 cycloalkyl or C.sub.7 -C.sub.9 aralkyl, and R.sup.6 is H, C.sub.1 -C.
    Type: Grant
    Filed: January 25, 1989
    Date of Patent: October 31, 1989
    Assignee: Ciba-Geigy Corporation
    Inventor: Samuel Evans
  • Patent number: 4873327
    Abstract: Compounds of the general formula ##STR1## in which each of A and B independently represents a halogen atom or an alkyl group; m is 0 or 1; Q represents a group of general formula ##STR2## in which R is as defined, or Q represents a group of general formula --CR.sup.2 R.sup.3 R.sup.4 in which R.sup.2, R.sup.3 and R.sup.4 are as defined; together with processes for the preparation of such compounds, pesticidal compositions containing them and their pesticidal use, and certain novel intermediates.
    Type: Grant
    Filed: March 8, 1988
    Date of Patent: October 10, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Martin Anderson, Anthony G. Brinnand
  • Patent number: 4868210
    Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.
    Type: Grant
    Filed: March 30, 1988
    Date of Patent: September 19, 1989
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 4859689
    Abstract: There is disclosed a fungicidal composition comprising (A) a fungicidal compound selected from the group consisting of (i) benzimidazole compounds of the formula ##STR1## wherein W is H, or alkyl carbamoyl; Y is thiazolyl, dihydrothiazolyl, tetrahydrothiazolyl or furyl; Z is H, halogen or alkyl and (ii) benzimidazole related compounds of the formula ##STR2## wherein R.sub.3 is C.sub.1-2 alkyl, and Z is as defined above, and (B) a synergist alkyl pyridinium salt of the formula ##STR3## wherein R is an alkyl containing 8 to 20 carbon atoms; and X is a monovalent anion.
    Type: Grant
    Filed: October 31, 1986
    Date of Patent: August 22, 1989
    Assignee: Safer, Inc.
    Inventors: George S. Puritch, Edward S. Kondo
  • Patent number: 4843070
    Abstract: Anti-bacterial and anti-fungal compounds of formula I and pharmaceutically acceptable salts thereof: ##STR1## in which R.sup.1 is hydrogen, alkyl or substituted or unsubstituted phenyl; R.sup.2 is hydrogen, alkyl, alkoxy, hydroxy, halgen, nitro or substituted or unsubstituted amino; R.sup.3 is hydrogen or substituted or unsubstituted alkyl; R.sup.4 and R.sup.5 are the same or different and are alkyl or hydroxyalkyl or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form an unsubstituted or substituted heterocyclic ring having the depicted nitrogen atom as the sole heteroatom or which may have nitrogen, oxygen or sulphur atoms as additional heteroatoms; and X is halogen.
    Type: Grant
    Filed: May 13, 1987
    Date of Patent: June 27, 1989
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Masahiro Kise, Masahiko Kitano, Masakuni Ozaki, Kenji Kazuno, Ichiro Shirahase, Yoshifumi Tomii, Jun Segawa
  • Patent number: 4837234
    Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxycyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.
    Type: Grant
    Filed: July 22, 1986
    Date of Patent: June 6, 1989
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 4827016
    Abstract: Dermal inflammations which are induced and propagated by leukotrienes are treated by topically applying to the inflamed dermis the following compound: ##STR1## wherein R.sup.3 is H or a thiol; n is 1 to 12; p is 0 to 12; X is a substituted carbonyl, such as an ester or a carboxylic acid; and Y is an aliphatic or branched hydrocarbon, aromatic ring, carbonyl or substituted amide.
    Type: Grant
    Filed: July 20, 1987
    Date of Patent: May 2, 1989
    Inventor: Lee R. Morgan
  • Patent number: 4826528
    Abstract: This invention relates to sulfonylureas of the formula ##STR1## These compounds are useful in killing weeds and in regulating the growth of cultivated plants.
    Type: Grant
    Filed: June 20, 1985
    Date of Patent: May 2, 1989
    Assignee: Celamerck GmbH & Co. KG.
    Inventors: Rudolf Mengel, W. Pfleiderer, Gerbert Linden, Gerhart Schneider
  • Patent number: 4808572
    Abstract: Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: a is an integer of from 1 to 7,R.sup.o represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted at the terminal carbon atom by a free or acylated hydroxy group, by a halogen atom having an atomic number of at most 17, or by methoxy, or represents C.sub.1-3 -perfluoroalkyl,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene or alternatively, if R.sup.1 represents a halogenated radical and/or B represents phenylene or ethylene, a single bond or vinylene,B represents a single bond, ethynylene or phenylene,R.sup.3 represents hydroxy, C.sub.
    Type: Grant
    Filed: December 1, 1986
    Date of Patent: February 28, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Andreas Beck, Werner Breitenstein, Andreas von Sprecher, Robert W. Lang, Konrad Oertle
  • Patent number: 4801609
    Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic peptides useful for treating hypertension are disclosed.
    Type: Grant
    Filed: March 27, 1987
    Date of Patent: January 31, 1989
    Assignee: Schering Corporation
    Inventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 4798905
    Abstract: The new sulphenylated carbamic acid esters of the formula ##STR1## in which R.sup.1 to R.sup.3 are identical or different and denote hydrogen, halogen, nitro, cyano, alkyl, alkoxy, alkylmercapto, trihalogenomethyl, trihalogenomethoxy or trihalogenomethylmercapto,R.sup.4 represents an optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl or aralkyl radical andn represents one of the numbers 0, 1, 2 or 3, can be prepared by reacting the corresponding N-substituted carbamic acid fluorides with an alcohol. They are active compounds for combating microorganisms.
    Type: Grant
    Filed: August 18, 1987
    Date of Patent: January 17, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Engelbert Kuhle, Wilfried Paulus, Hermann Genth, Paul Reinecke, Gerd Hanssler, Wilhelm Brandes
  • Patent number: 4769325
    Abstract: 2-(Allenyl)penicillins antibiotics and intermediates thereto are disclosed. A process for making the 2-(allenyl)penicillins and the starting materials for the process are also disclosed.
    Type: Grant
    Filed: July 28, 1986
    Date of Patent: September 6, 1988
    Inventors: Jack E. Baldwin, Amit Basak
  • Patent number: 4769484
    Abstract: Herbicidally active phenoxybenzoic acid esters of the formula ##STR1## in which X represents hydrogen or halogen,A represents optionally branched C.sub.2 -C.sub.6 -alkanediyl,Q represents oxygen, sulphur, sulphinyl (SO) or sulphonyl (SO.sub.2),R.sup.1 represents hydrogen or methyl,R.sup.2 represents hydrogen or C.sub.1 -C.sub.4 -alkyl, andR.sup.3 and R.sup.4 are identical or different and represent hydrogen, halogen, cyano, nitro, C.sub.1 -C.sub.4 -alkyl, halogeno-C.sub.1 -C.sub.2 -alkyl, C.sub.1 -C.sub.4 -alkoxy, halogeno-C.sub.1 -C.sub.2 -alkoxy and C.sub.1 -C.sub.2 -alkoxycarbonyl.
    Type: Grant
    Filed: August 4, 1987
    Date of Patent: September 6, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz Forster, Theodor Pfister, Hans-Joachim Santel, Robert R. Schmidt, Robert H. Strang
  • Patent number: 4767879
    Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: X is selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkynyl, alkenyloxy, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, amino, substituted amino, and the groups formyl and alkanoyl and the oxime, imine and Schiff base derivatives thereof;R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, alkylsulfonyl, arylsulfonyl, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl;m is an integer chosen from 3 to 5.
    Type: Grant
    Filed: December 17, 1986
    Date of Patent: August 30, 1988
    Assignee: ICI Australia Limited
    Inventors: Keith G. Watson, Lynette A. Garson, Graham J. Bird, Lindsay E. Cross, Graeme J. Farquharson
  • Patent number: 4748274
    Abstract: The present invention relates to compounds which are 4-hydroxy-4-alkenylcyclohexanecarboxylic acid derivatives possessing leukotriene antagonist activity. The compounds are useful in the treatment of allergic diseases, particularly in the treatment of human asthma. They are prepared by the reaction of an appropriate oxaspiro compound with a mercaptoalkanoic acid derivative.
    Type: Grant
    Filed: November 7, 1986
    Date of Patent: May 31, 1988
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Robert J. Cregge, Nelsen L. Lentz
  • Patent number: 4744812
    Abstract: Substituted diphenyl ethers of the formula ##STR1## where Z.sub.1, Z.sub.2 and Z.sub.3 are hydrogen, halogen, nitro, cyano, carboxyl, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylmercapto, haloalkylmercapto, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl or haloalkylsulfonyl, Z.sub.4 is hydrogen, cyano, alkyl, alkoxy, acetoxy or alkylmercapto, Y is hydrogen, halogen, cyano or nitro, X is oxygen, sulfur, sulfinyl or sulfonyl, and A is hydrogen, unsubstituted or substituted alkyl ##STR2## and can also be sulfonyl ##STR3## when X is oxygen, and, when Z.sub.4 is alkoxy or alkylmercapto, can also be a methylene chain --(CH.sub.2).sub.m -- by which the radicals Z.sub.4 --CH--X-- are bonded to form a ring, R.sub.1 is hydrogen, methyl, ethyl or n-propyl, R.sub.2 is cyano, methoxy, ethoxy or ##STR4## where B is OH, ONa, O--alkyl, unsubstituted or substituted phenoxy, --NH.sub.2, --NH--alkyl or --N(alkyl).sub.2, n is 1, 2 or 3, R.sub.3 and R.sub.
    Type: Grant
    Filed: March 4, 1985
    Date of Patent: May 17, 1988
    Assignee: BASF Aktiengesellschaft
    Inventors: Adolf Parg, Bruno Wuerzer, Gerhard Hamprecht
  • Patent number: 4745128
    Abstract: The present invention relates to pesticides containing carbamic acid ester derivatives of the formula (I), ##STR1## to pesticide compositions containing these compounds and to a process for their preparation.In the general formulaR.sup.1 is alkyl of from one to four carbon atoms;R.sup.2 represents alkyl of from one to four carbon atoms or (when X is alkyl of from one to twelve carbon atoms) alkyl of from one to twelve carbon atoms;R.sup.3 is H, methyl or ethyl;R.sup.4 and R.sup.5 are, independently from each other, H or halogen atoms;n=0, 1 or 2;X represents alkyl of from one to twelve carbon atoms or an 4-aryloxyphenoxyalkyl group of formula (II). ##STR2## The pesticide of the invention can be used for controlling insects and mites.
    Type: Grant
    Filed: January 9, 1987
    Date of Patent: May 17, 1988
    Assignee: Innofinance Altalanos Innovacios Penzintezet
    Inventors: Istvan Ujvari, Gyorgy Matolcsy, Ivan Belai, Laszlo Varjas, Bela Darvas
  • Patent number: 4745113
    Abstract: Compounds of the general formula ##STR1## in which each of A and B independently represents a halogen atom or an alkyl group; m is 0 or 1; Q represents a group of general formula ##STR2## in which R is as defined, or Q represents a group of general formula --CR.sup.2 R.sup.3 R.sub.4 in which R.sup.2, R.sup.3 and R.sup.4 are as defined; together with processes for the preparation of such compounds, pesticidal compositions containing them and their pesticidal use, and certain novel intermediates.
    Type: Grant
    Filed: September 10, 1986
    Date of Patent: May 17, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Martin Anderson, Anthony G. Brinnand
  • Patent number: 4742067
    Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
    Type: Grant
    Filed: July 30, 1986
    Date of Patent: May 3, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Sesha I. Natarajan, Eric M. Gordon
  • Patent number: 4740611
    Abstract: Disclosed are new compounds ##STR1## where each of R and R' have zero to 10 C atoms; R is H or hydrocarbyl; R' is H, hydrocarbyl, or hydrocarbyl substituted with hydrocarbylcarbonylamino, di(hydrocarbylcarbonyl)amino, hydrocarbylcarbonyl(hydrocarbyl)amino, formylamino, diformylamino and formyl(hydrocarbyl)amino, hydrocarbyloxy, hydrocarbylthio, formylthio, hydrocarbylcarbonylthio, hydrocarbyloxycarbonyl, hydrocarbyl carboxyl, hydrocarbylamino, dihydrocarbylamino, formyl, 3-indolyl, 3-(1-hydrocarbyl)indolyl, 3-(1-hydrocarbylcarbonyl)indolyl, 3-(1-formyl)indolyl, carbamoyl, hydrocarbylcarbamoyl, dihydrocarbylcarbamoyl, 5-imidazolyl, 5-(3-hydrocarbyl)imidazolyl, 5-(3-hydrocarbylcarbonyl)imidazolyl, or 5-(3-formyl)imidazolyl, and R" is phenyl or a C.sub.1 to C.sub.6 alkyl group; and methods of making such compounds.
    Type: Grant
    Filed: October 30, 1986
    Date of Patent: April 26, 1988
    Assignee: The Standard Oil Company
    Inventors: Mark C. Cesa, James E. Rinz, Gilles Klopman, Teodora T. Kopp
  • Patent number: 4736056
    Abstract: This invention relates to a process for preparing a malonic acid derivative compound of formula (i) depicted herein in high yield and high purity by reacting a malonic acid derivative compound of formula (ii) depicted herein with an alkylating agent of formula (iii) depicted herein in the presence of a solvent and a base.
    Type: Grant
    Filed: December 15, 1986
    Date of Patent: April 5, 1988
    Inventors: Oliver W. Smith, Russell J. Outcalt
  • Patent number: 4730053
    Abstract: The present invention is related to new S-(Carbamoyl-phenylselenyl) derivatives of mercaptanes of the general formula (I) ##STR1## and to a process for the treatment of diseases caused by cell injury due to the increased formation of active oxygen metabolites.
    Type: Grant
    Filed: November 25, 1985
    Date of Patent: March 8, 1988
    Assignee: A. Nattermann & Cie GmbH
    Inventors: Norbert Dereu, Albrecht Wendel, Helmut Sies, Sigurd Leyck, Axel Romer, Erich Graf
  • Patent number: 4721803
    Abstract: In the process of hydrocarboxylating an .alpha.-enamide with CO and an organic hydroxyl compound to produce a N-acyl-.alpha.-amino acid ester, the improvement comprising using as the organic hydroxyl compound reactant, an organic hydroxyl compound which has a chiral center that is essentially all L or D, thereby producing a reaction mixture having essentially no enantiomeric pairs and containing diastereomeric N-acyl-.alpha.-amino acid esters having two chiral centers.
    Type: Grant
    Filed: October 29, 1985
    Date of Patent: January 26, 1988
    Assignee: The Standard Oil Company
    Inventors: Mark C. Cesa, Robert A. Dubbert, James D. Burrington
  • Patent number: 4720569
    Abstract: A polycarbamic acid ester-type curing agent for thermosetting resin paints, said curing agent containing per molecule at least two groups represented by the following formula ##STR1## wherein Y represents ##STR2## --O--, or --S--; R.sub.1 represents a direct bond, or a divalent aliphatic hydrocarbon group having 1 to 6 carbon atoms which may be substituted by a hydroxyl group or an alkoxy group, provided that when Y is ##STR3## R.sub.1 represents a direct bond; R.sub.2 and R.sub.4, independently from each other, represent a hydrogen atom, or an aliphatic hydrocarbon group having 1 to 6 carbon atoms which may be substituted by an amino group, a hydroxyl group or an alkoxy group, or a group of the formula ##STR4## and R.sub.3 represents a hydrogen atom or a monovalent aliphatic hydrocarbon group having 1 to 6 carbon atoms which may be substituted by a hydroxyl group or an alkoxy group.
    Type: Grant
    Filed: July 30, 1985
    Date of Patent: January 19, 1988
    Assignee: Kansai Paint Co., Ltd.
    Inventor: Akira Tominaga
  • Patent number: 4719231
    Abstract: New 3-[N-(mercaptoacyl)]amino-4-arylbutanoic acid derivatives are now provided, which exhibit analgesic activity and are effective to enhance the analgesia induced by a known analgesic compound, ]D-ala.sup.2,met.sup.5 ]-enkephalin (DAME).
    Type: Grant
    Filed: May 20, 1985
    Date of Patent: January 12, 1988
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Tomio Takeuchi, Takaaki Aoyagi, Mitsugu Hachisu, Masao Hirayama, Shinjiro Murata, Shunzo Fukatsu
  • Patent number: 4716178
    Abstract: Novel compounds which are 2,6-di-t-butylphenols substituted on the 4 position by an anilino group, which anilino group is substituted by a group which includes carboxyl, tetrazolyl or N-methyltetrazolyl are useful as inhibitors of leukotriene synthesis and as antiallergic agents. Pharmaceutical compositions containing such compounds and pharmacological methods for use of such compounds are also disclosed.
    Type: Grant
    Filed: August 27, 1986
    Date of Patent: December 29, 1987
    Assignee: Riker Laboratories, Inc.
    Inventors: Robert A. Scherrer, Mark A. Rustad
  • Patent number: 4710515
    Abstract: Novel compounds which are 2,6-di-tertiary-butylphenols substituted in the 4 position by an acylaminophenyl group, which acylaminophenyl group is substituted by a moiety which includes a carboxyl group, are useful as inhibitors of leukotriene biosynthesis and as antiallergic agents.
    Type: Grant
    Filed: March 17, 1987
    Date of Patent: December 1, 1987
    Assignee: Riker Laboratories, Inc.
    Inventors: Alan R. Kirk, Robert A. Scherrer
  • Patent number: 4698365
    Abstract: Compounds of the formula ##STR1## in which "halogen" represents chlorine or fluorine and n is zero, one, two or three, that have useful pesticidal activity.
    Type: Grant
    Filed: November 25, 1986
    Date of Patent: October 6, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Martin Anderson
  • Patent number: 4692455
    Abstract: Compounds of the formula ##STR1## wherein Y is oxygen or sulfur are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of R.sub.1 may also be useful as analgesics due to their enkepahlinase inhibition activity.
    Type: Grant
    Filed: January 25, 1985
    Date of Patent: September 8, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Eric M. Gordon
  • Patent number: 4681973
    Abstract: Acylated amino acids having the general formula ##STR1## are prepared by reacting a compound of formula II ##STR2## with a compound of formula IIIROCOClwherein R, R.sub.1, R.sub.2 and R.sub.3 are as defined herein.
    Type: Grant
    Filed: February 27, 1986
    Date of Patent: July 21, 1987
    Assignee: USV Pharmaceutical Corporation
    Inventor: Martin L. Kantor
  • Patent number: 4678806
    Abstract: Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## the amido ester moiety of which is in the L-configuration, and pharmaceutically acceptable salts thereof are disclosed.
    Type: Grant
    Filed: September 2, 1986
    Date of Patent: July 7, 1987
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Wasyl Halczenko, George Hartman, Steven M. Pitzenberger
  • Patent number: 4673582
    Abstract: Sweetening agents of general formula: ##STR1## wherein: X is a CN, COOC.sub.1 -C.sub.3 alkyl, COC.sub.1 -C.sub.3 alkyl, CONHC.sub.1 -C.sub.3 alkyl, SO.sub.2 C.sub.1 -C.sub.3 alkyl, SOC.sub.1 -C.sub.3 alkyl, SO.sub.2 NHC.sub.1 -C.sub.3 alkyl, NO.sub.2, F, Cl substituent;n is a number equal to 0 or 1;M is a hydrogen atom, or an organic or inorganic physiologically acceptable cation;Y is a COOC.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkyl, CH.sub.2 OH, CHOHCH.sub.3, CF.sub.3 substituent;Z is a C.sub.1 -C.sub.5 n-alkyl, isobutyl, isopentyl, phenyl, cyclohexyl, benzyl, cyclohexylmethyl, CH.sub.2 C.sub.6 H.sub.4 OH(p), CH.sub.2 OC.sub.1 -C.sub.4 alkyl, CH.sub.2 COOC.sub.1 -C.sub.4 alkyl, CH.sub.2 SC.sub.1 -C.sub.4 alkyl, CH.sub.2 CH.sub.2 SCH.sub.3, CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3, COOC.sub.1 -C.sub.4 alkyl, COOC.sub.3 -C.sub.7 cycloalkyl, CONHC.sub.2 -C.sub.4 alkyl, CONHC.sub.3 -C.sub.7 cycloalkyl, CONHC.sub.3 -C.sub.7 thiacycloalkyl, or CONHCH.sub.2 COOCH.sub.3 group;characterized in that A is an N--CN group.
    Type: Grant
    Filed: March 5, 1986
    Date of Patent: June 16, 1987
    Assignee: Universite Claude Bernard/Lyon 1
    Inventors: Claude Nofre, Jean M. Tinti
  • Patent number: 4672139
    Abstract: Benzoylurea compounds of the formula ##STR1## wherein the meaning of each of the symbols is described in the specification.
    Type: Grant
    Filed: July 21, 1986
    Date of Patent: June 9, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Martin Anderson
  • Patent number: 4665092
    Abstract: Alkenes of the formula (I) and epoxides (II) used to make them are useful as anti-inflammatory and antiallergic pharmaceuticals: ##STR1## wherein R.sup.1 =H or CH.sub.3 ; R.sup.2 =phenyl, substituted phenyl, benzyl or a cysteinyl moiety; R.sup.4 and R.sup.5 =alkyl; n=O or 1; and R.sup.3 is as described.
    Type: Grant
    Filed: October 3, 1985
    Date of Patent: May 12, 1987
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Michael P. Ferro, Michael P. Wachter
  • Patent number: 4665193
    Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.
    Type: Grant
    Filed: June 27, 1986
    Date of Patent: May 12, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Denis E. Ryono, Edward W. Petrillo, Jr.
  • Patent number: 4663452
    Abstract: An organic carbonyl compound is thiated to the corresponding thiono compound by reacting it with phosphorus pentasulfide in the presence of an alkali metal bicarbonate and a hydrocarbon diluent. In preferred embodiments of the invention, the carbonyl compound is an amide, especially an aromatic amide, and the diluent is an inert hydrocarbon having a boiling point in the range of about 50.degree.-150.degree. C.
    Type: Grant
    Filed: August 29, 1985
    Date of Patent: May 5, 1987
    Assignee: Ethyl Corporation
    Inventor: Kenneth C. Lilje