Nitrogen In Acid Moiety Patents (Class 560/16)
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Patent number: 4960881Abstract: 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: GrantFiled: June 6, 1988Date of Patent: October 2, 1990Assignee: Societe Nationale des Poudres et ExplosifsInventors: Gerard Barcelo, Jean-Pierre Senet, Gerard Sennyey
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Patent number: 4945106Abstract: Prostaglandin analogues exhibiting activity at thromboxane receptor sites have been prepared.Type: GrantFiled: July 6, 1989Date of Patent: July 31, 1990Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 4937253Abstract: 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: GrantFiled: September 23, 1988Date of Patent: June 26, 1990Assignee: SmithKline Beecham CorporationInventors: John G. Gleason, Ralph F. Hall, John F. Newton, Kathleen A. Phipps, Joanne Smallheer
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Patent number: 4933367Abstract: 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: GrantFiled: March 12, 1987Date of Patent: June 12, 1990Assignee: Boehringer Mannheim GmbHInventors: Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuhnle
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Patent number: 4929754Abstract: The invention relates to new benzenesulphonamidoindanyl compounds useful in the treatment and prophylaxis of thromboembolic diseases, arteriosclerosis and tumor metastasis.Type: GrantFiled: February 1, 1989Date of Patent: May 29, 1990Assignee: Dr. Karl Thomae GmbHInventors: Josef Nickl, Armin Heckel, Erich Muller, Berthold Narr, Johannes Weisenberger, Wolfgang Eisert, Thomas Muller
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Patent number: 4929755Abstract: 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: GrantFiled: December 19, 1986Date of Patent: May 29, 1990Assignee: The Standard Oil CompanyInventors: Mark C. Cesa, Robert A. Dubbert, James D. Burrington
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Patent number: 4929641Abstract: 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: GrantFiled: May 11, 1988Date of Patent: May 29, 1990Assignee: Schering CorporationInventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
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Patent number: 4918223Abstract: 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: GrantFiled: August 9, 1988Date of Patent: April 17, 1990Assignee: Degussa AktiengesellschaftInventors: Hans-Peter Krimmer, Karlheinz Drauz
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Patent number: 4908383Abstract: 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: GrantFiled: May 23, 1989Date of Patent: March 13, 1990Assignee: Ciba-Geigy CorporationInventors: Jozef Drabek, Josef Ehrenfreund
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Patent number: 4906662Abstract: 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: GrantFiled: January 27, 1987Date of Patent: March 6, 1990Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Kinji Hashimoto, Kiyoto Goto, Ken-ichi Kanai, Yoshiaki Tsuda
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Patent number: 4898977Abstract: 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: GrantFiled: August 13, 1987Date of Patent: February 6, 1990Assignee: Ciba-Geigy CorporationInventors: Peter Herold, Christof Angst
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Patent number: 4897109Abstract: 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: GrantFiled: October 5, 1987Date of Patent: January 30, 1990Assignee: Ciba-Geigy CorporationInventor: Henry Martin
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Patent number: 4882341Abstract: The invention relates to amino substituted propenoates and their use against fungi.Type: GrantFiled: September 9, 1988Date of Patent: November 21, 1989Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Ian T. Kay
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Patent number: 4879309Abstract: 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: GrantFiled: January 30, 1989Date of Patent: November 7, 1989Assignee: Schering CorporationInventors: Ronald J. Doll, Bernard R. Neustadt
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Patent number: 4877824Abstract: 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: GrantFiled: January 25, 1989Date of Patent: October 31, 1989Assignee: Ciba-Geigy CorporationInventor: Samuel Evans
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Patent number: 4873327Abstract: 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: GrantFiled: March 8, 1988Date of Patent: October 10, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Martin Anderson, Anthony G. Brinnand
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Patent number: 4868210Abstract: 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: GrantFiled: March 30, 1988Date of Patent: September 19, 1989Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 4859689Abstract: 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: GrantFiled: October 31, 1986Date of Patent: August 22, 1989Assignee: Safer, Inc.Inventors: George S. Puritch, Edward S. Kondo
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Patent number: 4843070Abstract: 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: GrantFiled: May 13, 1987Date of Patent: June 27, 1989Assignee: Nippon Shinyaku Co., Ltd.Inventors: Masahiro Kise, Masahiko Kitano, Masakuni Ozaki, Kenji Kazuno, Ichiro Shirahase, Yoshifumi Tomii, Jun Segawa
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Patent number: 4837234Abstract: 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: GrantFiled: July 22, 1986Date of Patent: June 6, 1989Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 4826528Abstract: 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: GrantFiled: June 20, 1985Date of Patent: May 2, 1989Assignee: Celamerck GmbH & Co. KG.Inventors: Rudolf Mengel, W. Pfleiderer, Gerbert Linden, Gerhart Schneider
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Patent number: 4827016Abstract: 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: GrantFiled: July 20, 1987Date of Patent: May 2, 1989Inventor: Lee R. Morgan
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Patent number: 4808572Abstract: 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: GrantFiled: December 1, 1986Date of Patent: February 28, 1989Assignee: Ciba-Geigy CorporationInventors: Andreas Beck, Werner Breitenstein, Andreas von Sprecher, Robert W. Lang, Konrad Oertle
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Patent number: 4801609Abstract: 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: GrantFiled: March 27, 1987Date of Patent: January 31, 1989Assignee: Schering CorporationInventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
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Patent number: 4798905Abstract: 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: GrantFiled: August 18, 1987Date of Patent: January 17, 1989Assignee: Bayer AktiengesellschaftInventors: Engelbert Kuhle, Wilfried Paulus, Hermann Genth, Paul Reinecke, Gerd Hanssler, Wilhelm Brandes
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Patent number: 4769484Abstract: 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: GrantFiled: August 4, 1987Date of Patent: September 6, 1988Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Theodor Pfister, Hans-Joachim Santel, Robert R. Schmidt, Robert H. Strang
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Patent number: 4769325Abstract: 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: GrantFiled: July 28, 1986Date of Patent: September 6, 1988Inventors: Jack E. Baldwin, Amit Basak
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Patent number: 4767879Abstract: 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: GrantFiled: December 17, 1986Date of Patent: August 30, 1988Assignee: ICI Australia LimitedInventors: Keith G. Watson, Lynette A. Garson, Graham J. Bird, Lindsay E. Cross, Graeme J. Farquharson
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Patent number: 4748274Abstract: 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: GrantFiled: November 7, 1986Date of Patent: May 31, 1988Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Robert J. Cregge, Nelsen L. Lentz
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Patent number: 4745113Abstract: 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: GrantFiled: September 10, 1986Date of Patent: May 17, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: Martin Anderson, Anthony G. Brinnand
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Patent number: 4744812Abstract: 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: GrantFiled: March 4, 1985Date of Patent: May 17, 1988Assignee: BASF AktiengesellschaftInventors: Adolf Parg, Bruno Wuerzer, Gerhard Hamprecht
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Patent number: 4745128Abstract: 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: GrantFiled: January 9, 1987Date of Patent: May 17, 1988Assignee: Innofinance Altalanos Innovacios PenzintezetInventors: Istvan Ujvari, Gyorgy Matolcsy, Ivan Belai, Laszlo Varjas, Bela Darvas
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Patent number: 4742067Abstract: 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: GrantFiled: July 30, 1986Date of Patent: May 3, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: Sesha I. Natarajan, Eric M. Gordon
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Patent number: 4740611Abstract: 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: GrantFiled: October 30, 1986Date of Patent: April 26, 1988Assignee: The Standard Oil CompanyInventors: Mark C. Cesa, James E. Rinz, Gilles Klopman, Teodora T. Kopp
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Patent number: 4736056Abstract: 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: GrantFiled: December 15, 1986Date of Patent: April 5, 1988Inventors: Oliver W. Smith, Russell J. Outcalt
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Patent number: 4730053Abstract: 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: GrantFiled: November 25, 1985Date of Patent: March 8, 1988Assignee: A. Nattermann & Cie GmbHInventors: Norbert Dereu, Albrecht Wendel, Helmut Sies, Sigurd Leyck, Axel Romer, Erich Graf
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Patent number: 4721803Abstract: 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: GrantFiled: October 29, 1985Date of Patent: January 26, 1988Assignee: The Standard Oil CompanyInventors: Mark C. Cesa, Robert A. Dubbert, James D. Burrington
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Patent number: 4720569Abstract: 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: GrantFiled: July 30, 1985Date of Patent: January 19, 1988Assignee: Kansai Paint Co., Ltd.Inventor: Akira Tominaga
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3-[N-(mercaptoacyl)]amino-4-arylbutanoic acid derivatives and an analgesic agent comprising the same
Patent number: 4719231Abstract: 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: GrantFiled: May 20, 1985Date of Patent: January 12, 1988Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Tomio Takeuchi, Takaaki Aoyagi, Mitsugu Hachisu, Masao Hirayama, Shinjiro Murata, Shunzo Fukatsu -
Patent number: 4716178Abstract: 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: GrantFiled: August 27, 1986Date of Patent: December 29, 1987Assignee: Riker Laboratories, Inc.Inventors: Robert A. Scherrer, Mark A. Rustad
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Patent number: 4710515Abstract: 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: GrantFiled: March 17, 1987Date of Patent: December 1, 1987Assignee: Riker Laboratories, Inc.Inventors: Alan R. Kirk, Robert A. Scherrer
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Patent number: 4698365Abstract: 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: GrantFiled: November 25, 1986Date of Patent: October 6, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Martin Anderson
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Patent number: 4692455Abstract: 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: GrantFiled: January 25, 1985Date of Patent: September 8, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Eric M. Gordon
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Patent number: 4681973Abstract: 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: GrantFiled: February 27, 1986Date of Patent: July 21, 1987Assignee: USV Pharmaceutical CorporationInventor: Martin L. Kantor
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Patent number: 4678806Abstract: 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: GrantFiled: September 2, 1986Date of Patent: July 7, 1987Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Wasyl Halczenko, George Hartman, Steven M. Pitzenberger
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Patent number: 4673582Abstract: 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: GrantFiled: March 5, 1986Date of Patent: June 16, 1987Assignee: Universite Claude Bernard/Lyon 1Inventors: Claude Nofre, Jean M. Tinti
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Patent number: 4672139Abstract: Benzoylurea compounds of the formula ##STR1## wherein the meaning of each of the symbols is described in the specification.Type: GrantFiled: July 21, 1986Date of Patent: June 9, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Martin Anderson
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Patent number: 4665092Abstract: 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: GrantFiled: October 3, 1985Date of Patent: May 12, 1987Assignee: Ortho Pharmaceutical CorporationInventors: Michael P. Ferro, Michael P. Wachter
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Patent number: 4665193Abstract: 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: GrantFiled: June 27, 1986Date of Patent: May 12, 1987Assignee: E. R. Squibb & Sons, Inc.Inventors: Denis E. Ryono, Edward W. Petrillo, Jr.
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Patent number: 4663452Abstract: 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: GrantFiled: August 29, 1985Date of Patent: May 5, 1987Assignee: Ethyl CorporationInventor: Kenneth C. Lilje