Oxy In Acid Moiety Patents (Class 560/42)
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Patent number: 5045567Abstract: Propanolamine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen or a group of formula ##STR2## n is the number 0 or 1; R.sup.2 and R.sup.5 are phenyl, m-halophenyl, m-trifluoromethylphenyl, thienyl or pyridyl;R.sup.3 is hydrogen or methyl;R.sup.4 is hydrogen, --CH.sub.2 COOH, --CH.sub.2 COO--C.sub.1-4 -alkyl, --(CH.sub.2).sub.2 O--C.sub.1-4 -alkyl or --(CH.sub.2).sub.2 O(CH.sub.2).sub.1-4 --C.sub.6 H.sub.5 ;and a physiologically compatible salt thereof.The invention also relates to processes for the preparation of these propanolamine derivatives, pharmaceutical preparations and feedstuffs containing them, and methods of using the propanolamine derivatives.Type: GrantFiled: October 31, 1990Date of Patent: September 3, 1991Assignee: Hoffmann-La Roche Inc.Inventor: Frank Kienzle
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Patent number: 5025017Abstract: Seco-mevinic acid derivatives are provided which has the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## R is H, alkali metal or lower alkyl, R.sup.1 is H, lower alkyl, aryl, lower alkoxy, cycloalkyl, heteroaryl, aralkyl, heteroaralkyl or heterocyclic; R.sup.2 is lower alkyl, cycloalkyl or aralkyl, and X is O or NR.sup.5 wherein R.sup.5 is H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis. New intermediates for preparing the above seco-mevinic acid derivatives are also provided.Type: GrantFiled: September 28, 1989Date of Patent: June 18, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Donald S. Karanewsky
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Patent number: 5010104Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formul (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.Type: GrantFiled: June 29, 1989Date of Patent: April 23, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Patent number: 5001156Abstract: Lipophilic quaternary ammonium salicylate, characterized in that it corresponds to the formula: ##STR1## in which: (i) R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote an alkyl or alkylcycloalkyl radical, optionally substituted or interrupted;(ii) R.sub.3 and/or R.sub.4 denote(s) a group:R.sub.8 [OC.sub.2 H.sub.3 R.sub.7 ].sub.n [OCH.sub.2 CHOH--CH.sub.2 ].sub.pin which 0.ltoreq.n.ltoreq.4 and p denotes 0 or 1; R.sub.8 denotes H or an alkyl, alkenyl, alkylcycloalkyl or alkylaryl radical;(iii) R.sub.4 denotes an alkylphenyl radical;(iv), (v) R.sub.1 and R.sub.2 can form a saturated or unsaturated aromatic or non-aromatic heterocycle;(vi) R.sub.1, R.sub.2 and R.sub.3 form polycyclic derivatives with the nitrogen atoms; R.sub.5 denotes a group corresponding to the formula: ##STR2## in which n is an integer varying between 0 and 10.Type: GrantFiled: December 1, 1987Date of Patent: March 19, 1991Assignee: L'OrealInventors: Michel Philippe, Henri Sebag, Michel Hocquaux, Bernard Jacquet, Jean P. Laugier
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Patent number: 4994495Abstract: Fungicidal compounds having the formula: ##STR1## and stereoisomers thereof, wherein R.sup.1 is optionally substituted C.sub.2-10 alkenyl, optionally substituted C.sub.5-6 cycloalkenyl, optionally substituted C.sub.2-10 alkynyl, or C.sub.1-10 alkyl substituted with --CN, --NC, --COR.sup.2, --CO.sub.2 R.sup.2, --NO.sub.2 or --SCN; X is O, S(O)n or NR.sup.2 and is attached to the 3- or the 4-position of the phenyl ring; Y and Z, which may be the same or different, are H, halogen, --CH.sub.3, --C.sub.2 H.sub.5, or --OCH.sub.3 ; R.sup.2 is H, C.sub.1-4 alkyl, C.sub.1-4 alkenyl, or, when R.sup.2 is C.sub.1-4 alkyl in the group --COR.sup.2, it joins with the alkyl group to which --COR.sup.2 is attached to form a 5- or 6-membered aliphatic ring; and n is 0, 1 or 2.Type: GrantFiled: May 11, 1989Date of Patent: February 19, 1991Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Paul J. de Fraine, Michael G. Hutchings, Ian Ferguson
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Patent number: 4992558Abstract: Novel disperse dyes particularly suitable for dyeing textile material made of polyester fibers, said dyes being of the formula ##STR1## wherein X is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen,Y is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkoxy,R is hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkenyl or phenyl, or Y and R, when taken together with the nitrogen atom and the two carbon atoms linking them, form a 5- or 6-membered ring,B is straight-chain or branched C.sub.2 -C.sub.6 alkylene,A is a radical of formula ##STR2## in which W is C.sub.1 -C.sub.9 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl, halogen or C.sub.1 -C.sub.4 alkoxy,n is 0, 1, 2, or 3,Q is hydrogen or C.sub.1 -C.sub.4 alkyl,V is halogen, andm is 0, 1, 2, 3 or 4.Type: GrantFiled: July 7, 1989Date of Patent: February 12, 1991Assignee: Ciba-Geigy CorporationInventors: Peter Liechti, Antoine Clement
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Patent number: 4990668Abstract: Described is a process for preparing a racemic or chiral aryloxypropanolamine (1) or arylethanolamine (2) of the formula ##STR1## wherein Ar is aryl, substituted aryl, heteroaryl, or aralkyl and R is alkyl, substituted alkyl, aralkyl, or WB wherein W is a straight or branched chain alkylene of from 1 to about 6 carbon atoms and wherein B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, where R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.sub.5 are not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.3 or --NR.sub.3 COOR.sub.5, or R.sub.3 and R.sub.4 may together with N form a 5- to 7-membered heterocyclic group.The process can be used to prepare beta-blocking agents, useful in the treatment of cardiac conditions.Type: GrantFiled: December 4, 1985Date of Patent: February 5, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventors: Khuong H. X. Mai, Ghanshyam Patil, William L. Matier
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Patent number: 4990533Abstract: Novel benzoic acid or benzoic acid ester derivatives, pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headache, such as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.Type: GrantFiled: November 10, 1986Date of Patent: February 5, 1991Assignee: Warner-Lambert Co.Inventors: Michael F. Rafferty, Graham Johnson
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Patent number: 4990505Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein the substituents are defined in the specification, and physiologically acceptable salts and solvates thereof.The compounds of formula (I) have a selective stimulant action at .beta..sub.2 -adrenoreceptors and are useful, in particular in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: April 18, 1989Date of Patent: February 5, 1991Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell
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Patent number: 4980095Abstract: Novel benzoic acid or benzoic acid ester derivatives, pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headache, such as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.Type: GrantFiled: June 1, 1987Date of Patent: December 25, 1990Assignee: Warner-Lambert CompanyInventors: Michael F. Rafferty, Graham Johnson
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Patent number: 4965279Abstract: Novel cyclopropyl aza prostaglandin analogs are disclosed having the formula ##STR1## wherein A can be carbonyl, sulfonyl or a single bond. These compounds are useful, for example, as thromboxane antagonists.Type: GrantFiled: November 18, 1988Date of Patent: October 23, 1990Assignee: E. R. Squibb & Sons, Inc.Inventors: Raj N. Misra, David M. Floyd, Steven E. Hall
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Patent number: 4958045Abstract: A process for the preparation of a 1,8-bridged 4-quinolone-3-carboxylic acid of the formula ##STR1## comprising in a first reaction step reacting an enamine of the formula ##STR2## in an anhydrous, aprotic solvent with one equivalent of a base, at a temperature from 80.degree. C. to 180.degree. C., to give a 4-quinolone-3-carboxylic acid derivative of the formula ##STR3## and, in a second reaction step, reacting that with another equivalent of a base, to give the 1,8-bridged 4-quinolone-3-carboxylic acid derivative of the formula (I) and optionally converting the group Y into a carboxyl group or salt thereof. Both steps may be effected simultaneously in a one-pot process without intermediate isolation of the compound II. Some of the compounds are new. The old and new compounds are antibacterials and promote animal growth.Type: GrantFiled: March 30, 1989Date of Patent: September 18, 1990Assignee: Bayer AktiengesellschaftInventors: Klaus Grohe, Michael Schriewer
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Patent number: 4943591Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein X represents a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain andY represents a bond, or a C.sub.1-4 alkylene, C.sub.2-4 alkenylene or C.sub.2-4 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 8;Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups C.sub.1-3 alkyl, nitro, --(CH.sub.2).sub.q R [where R is hydroxy, C.sub.1-3 alkoxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represent a hydrogen atom, or a C.sub.1-4 alkyl group, or --NR.sup.3 R.sup.4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from --O-- or --S-- or a group --NH-- or --N(CH.sub.3)--), --NR.sup.5 COR.sup.6 (where R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.6 represents a hydrogen atom or a C.sub.Type: GrantFiled: October 14, 1986Date of Patent: July 24, 1990Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell
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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: 4933369Abstract: The present invention relates to new compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof and the enantiomers thereof, wherein R.sup.1 is H, lower alkyl, alkenyl, aralkyl, or C(O)R.sup.2 wherein R.sup.2 is lower alkyl, alkenyl, alkoxy, or aralkyl; n is an integer of from 2-4; m is an integer of from 0-4; A is S(O).sub.x wherein x is an integer of from 0-2; and Ar is phenyl or thienyl. These compounds are useful as analgesics.Type: GrantFiled: September 30, 1988Date of Patent: June 12, 1990Assignee: G. D. Searle & Co.Inventors: Barnett S. Pitzele, Nizal S. Chandrakumar, Donald W. Hansen, Jr., Gilbert W. Adelstein
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Patent number: 4929751Abstract: A vinyl tricarbonyl compound of the formula ##STR1## or its monohydrate of the formula ##STR2## wherein R.sub.1 is a hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, and cycloalkyl with 3 to 7 carbon atoms,R.sub.2 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic,R.sub.3 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic, andR.sub.4 is unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl are 3 to 7 carbon atoms. Such vinyl tricarbonyl compound is effective against tumor cells.Type: GrantFiled: October 19, 1987Date of Patent: May 29, 1990Assignee: Yale UniversityInventors: Harry H. Wasserman, Natesan Murugesan, John H. Van Duzer
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Patent number: 4927958Abstract: Styryl ketones of the formula ##STR1## wherein R.sup.8 and R.sup.9 are independently hydrogen or lower alkyl or together represent an additional carbon-carbon bond andR.sup.10 is a group of the formula ##STR2## as well as corresponding compounds of the formula ##STR3## wherein R.sup.10' is a group of formula (a), (b), (d) or (e) or a group of the formula--C(R.sup.18)(R.sup.19)OR.sup.20' ; (f')have mucosa-protective and/or gastric acid secretion-inhibiting properties, such that they can be used for the control or prevention of illnesses of the gastrointestinal tract, especially against gastric ulcers or duodenal ulcers.Type: GrantFiled: March 17, 1988Date of Patent: May 22, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Albert Fischli, Eva-Maria Gutknecht, Daniel Obrecht
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Patent number: 4927955Abstract: A process for the preparation of a compound of formula ##STR1## wherein X represents hydrogen, halogen, trifluoromethyl or lower alkyl group; W represents methyl, Q represents hydrogen or W and Q, together, form an ethylene group and R' represents a lower alkyl group which comprises protecting the amino group of the phenol corresponding to the compound of formula I, submitting the compound thus obtained to an alkylation (with a compound of formula Hal--CH.sub.2 --COOR', wherein R' is as defined hereinabove for the formula I and Hal is chlorine, bromine or iodine) and then releasing the amino group of the product thus obtained.Type: GrantFiled: August 11, 1988Date of Patent: May 22, 1990Assignee: SanofiInventors: Robert Boigegrain, Roberto Cecchi, Sergio Boveri
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Patent number: 4922015Abstract: The invention relates to new compounds of the formula ##STR1## in which R.sup.1 denotes (C.sub.1 -C.sub.8)-alkyl or optionally substituted (C.sub.6 -C.sub.14)-aryl, R.sup.2 denotes hydrogen or an amino acid residue which is protected by an amino protective group which can be cleaved off with weak acid or base, R.sup.3 denotes hydrogen or (C.sub.1 -C.sub.4)-alkyl, and Y.sup.1 -Y.sup.9 denote identical or different radicals hydrogen, (C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy or -O-(CH.sub.2).sub.n -COOH (with n=1 to 6), one of these radicals being -O-(CH.sub.2).sub.n -COOH. A process for the preparation thereof and the synthesis of peptide amides by means of a solid phase method using these new compounds (spacers) are described.Type: GrantFiled: April 6, 1988Date of Patent: May 1, 1990Assignee: Hoechst AktiengesellschaftInventors: Gerhard Breipohl, Jochen Knolle, Werner Stuber
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Patent number: 4921997Abstract: The present invention is concerned with a process for the synthesis of substituted arylureidophenexymethyl propionic acids and an analogous benzamides series of compounds which have activity in the dissociation of oxygen from hemoglobin. In addition, the process may be utilized to prepare compounds which are known.Type: GrantFiled: June 15, 1988Date of Patent: May 1, 1990Assignee: Montefiore Medical CenterInventors: Iraj Lalezari, Parviz Lalezari
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Patent number: 4908386Abstract: The present invention provides compounds of general formula (I) ##STR1## wherein Ar represents an unsubstituted or substituted phenyl gorup;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group;X represents a bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene chain;Y represents a bond or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain;Q represents a substituted phenyl or pyridyl ring;and physiologically acceptable salts and solvates thereof useful as stimulants of .sub.2 -adrenoreceptors and particularly in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: December 20, 1988Date of Patent: March 13, 1990Assignee: Glaxo Group LimitedInventors: Harry Finch, Lawrence H. C. Lunts, Alan Naylor, Ian F. Skidmore, Ian B. Campbell, David Middlemiss, Charles Willbe
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Patent number: 4895842Abstract: A phenylalanine derivative having the formula (I): ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen provided that both R.sup.1 and R.sup.2 are not hydrogen at the same time;C.sub.1 -C.sub.8 alkyl which may be substituted with hydroxy, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.1 -C.sub.4 alkylmercapto, C.sub.1 -C.sub.4 alkoxy, carbamoyl, sulfamoyl, pyridyl, or phenyl which may further be substituted with nitro, C.sub.1 -C.sub.4 alkoxy, or halogen;C.sub.6 -C.sub.8 cycloalkyl which may be substituted with hydroxy, C.sub.1 -C.sub.4 alkoxy, hydroxylcarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, or C.sub.1 -C.sub.4 alkyl;phenyl which may be substituted with halogen, nitro, trifluoromethyl, C.sub.1 -C.sub.4 alkoxy C.sub.1 C.sub.4 alkylmercapto, C.sub.1 -C.sub.4 alkylcarbonyl, phenylcarbonyl, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, carbamoyl, sulfamoyl, amidino, pyridylcarbonyl, or C.sub.1 -C.sub.6 alkyl which may further be substituted with C.sub.1 -C.sub.Type: GrantFiled: September 29, 1986Date of Patent: January 23, 1990Assignees: Shosuke Okamoto, Showa Denko Kabushiki KaishaInventors: Shosuke Okamoto, Yoshio Okada, Akiko Okunomiya, Taketoshi Naito, Yoshio Kimura, Morihiko Yamada, Norio Ohno, Yasuhiro Katsuura, Yumi Seki
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Patent number: 4892886Abstract: [p-[2-[[(S)-2-hydroxy-3-phenoxypropyl]amino]-ethyl]phenoxy]acetic acid and its physiologically compatible salts, which have catabolic activity and can be used for the treatment of obesity, of diabetes and of conditions which are associated with increased protein breakdown or as feed additives for fattening animals, as described. The compounds are prepared starting from esters corresponding to the aforementioned acid.Type: GrantFiled: May 10, 1989Date of Patent: January 9, 1990Assignee: Hoffman-La Roche Inc.Inventors: Leo Alig, Marcel Muller
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Patent number: 4889947Abstract: Sunscreen compositions are described which contain certain substituted naphthalenylidenes which act as UV filters when incorporated in a carrier in amounts ranging from 0.1-50% by weight.Type: GrantFiled: July 28, 1988Date of Patent: December 26, 1989Assignee: ICI Americas Inc.Inventors: Charalambos J. Phalangas, Thomas P. Cleary
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Patent number: 4886898Abstract: Certain intermediate aminomethyl-5,6,7,8-tetrahydronaphthyl-oxyacetic acid derivatives of the formula ##STR1## in which R.sup.2 is hydroxyl, alkoxy, phenoxy, benzoxy or NR.sup.4 R.sup.5, andR.sup.4 and R.sup.5 each independently is hydrogen or alkyl, or one of the radicals R.sup.4 or R.sup.5 is benzyl,which are useful in preparing the corresponding aryl-sulfonamides which in-turn have antithrombotic, antiatherosclerotic and antiischaemic properties.Type: GrantFiled: May 16, 1989Date of Patent: December 12, 1989Assignee: Bayer AktiengesellschaftInventors: Ulrich Niewohner, Franz-Peter Hoever, Folker Lieb, Ulrich Rosentreter, Elisabeth Perzborn, Volker-Bernd Fiedler, Friedel Seuter
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Patent number: 4883815Abstract: Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy carbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxy carbonyl-C.sub.2 -C.sub.5)-alky, piperidino-C.sub.2 -C.sub.Type: GrantFiled: July 5, 1988Date of Patent: November 28, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwenden, Rene Imhof, Roland Jakob-Roetne, Emilio Kyburz
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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: 4880840Type: GrantFiled: June 30, 1987Date of Patent: November 14, 1989Assignee: Bayer AktiengesellschaftInventors: Hans Lindel, Axel Ingendoh, Friedrich Berschauer, Anno de Jong, Martin Scheer
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Patent number: 4845127Abstract: Optically active N-3-(4-substituted phenyl)propyl-.beta.-phenethanolamines are provided as well as pharmaceutical compositions containing such compounds. A method for effecting weight control in obese animals utilizing optically active phenethanolamine is disclosed. Novel intermediates useful in the preparation of optically active .beta.-phenethanolamines are provided.Type: GrantFiled: December 14, 1984Date of Patent: July 4, 1989Assignee: Eli Lilly and CompanyInventors: Jack Mills, Klaus K. Schmiegel, Walter N. Shaw
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Patent number: 4831055Abstract: Compounds of formula (I) ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is hydrogen, halogen or alkyl and R.sup.2 is hydrogen or alkyl are useful to reduce serum lipids in animals, including humans.Type: GrantFiled: June 8, 1987Date of Patent: May 16, 1989Assignee: Nippon Shinyaku Co., Ltd.Inventors: Yoshiaki Yoshikuni, Shoichi Chokai, Takayuki Ozaki, Hirotsugu Yoshida, Haruo Tanaka, Jun Segawa
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Patent number: 4829086Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p -- or C.sub.6 C.sub.12 cycloalkenyl-C.sub.p H.sub.2p -- (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.Type: GrantFiled: October 23, 1986Date of Patent: May 9, 1989Inventor: Nicholas S. Bodor
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Patent number: 4826982Abstract: Quinolonecarboxylic acid derivatives of the following formula, ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen atom or lower alkyl group; the hydrates or the pharmaceutically acceptable acid addition or alkali salts thereof are useful as an antibacterial agent.Type: GrantFiled: September 2, 1986Date of Patent: May 2, 1989Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Kuniyoshi Masuzawa, Seigo Suzue, Keiji Hirai, Takayoshi Ishizaki
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Patent number: 4803293Abstract: Compounds of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof,in whichR.sup.1 is hydrogen, halogen, or trifluoromethyl,R.sup.2 is hydrogen or halogen,R.sup.3 is hydroxyl, C.sub.1-6 alkoxy or ##STR2## where R.sup.8 and R.sup.9 are each hydrogen or C.sub.1-6 alkyl; R.sup.4 is hydrogen or C.sub.1-6 alkyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyl optionally substituted by hydroxy; cyano, C.sub.1-6 alkenyl or C.sub.1-6 alkynyl optionally substituted by carboxy or esters and amides thereof, phenyl, C.sub.1-6 alkyl phenyl or a group ##STR3## wherein R.sup.12 and R.sup.13 are each hydrogen or C.sub.1-6 alkyl or together, along with the nitrogen to which they are attached, form a 5- or 6-membered ring and m is 1 or 2;R.sup.6 is hydrogen or methyl:R.sup.7 is --O(CH.sub.2).sub.a CO.sub.2 H, --O(CH.sub.2).sub.b M, --CO.sub.2 H; or amide thereof in whicha is an integer from 1 to 6,b is an integer from 2 to 7, andM is hydroxy, C.sub.1-6 alkoxy or ##STR4## in which R.sup.10 and R.sup.Type: GrantFiled: February 18, 1987Date of Patent: February 7, 1989Assignee: Beecham Group plcInventors: John Berge, Richard M. Hindley
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Patent number: 4797493Abstract: Disclosed herein are benzylidene compounds represented by the formula (I): ##STR1## wherein A represents ##STR2## (wherein B represents hydrogen atom or an acetyl group, W represents hydrogen atom or --CH.sub.2 --CH.sub.2 --CO--O--R, X.sup.1, X.sup.2 and X.sup.3 represent independently hydrogen atom, a hydroxyl group or a methoxyl group (two or three of them may be the same or all of them may be different), Y represents oxygen atom or imino group (--NH--), Z represents a methyl group or a phenyl group, and R represents a straight chain alkyl group having 1 to 18 carbon atoms, or branched or cyclic alkyl group having 3 to 18 carbon atoms, provided that when A is ##STR3## R is not an alkyl group having 1 to 2 carbon atoms, and when A is ##STR4## and X.sup.1, X.sup.2 and X.sup.3 are hydrogen atom, R is not an alkyl group having 1 to 2 carbon atoms), a cosmetic composition containing the same and an ultraviolet absorber comprising the same.Type: GrantFiled: April 14, 1987Date of Patent: January 10, 1989Assignee: Ajinomoto Co., Inc.Inventors: Kazuhiro Matsuno, deceased, Toru Kobayashi, Takeshi Miyoshi, Hideaki Kawashima
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Patent number: 4795819Abstract: There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.Type: GrantFiled: July 22, 1987Date of Patent: January 3, 1989Assignee: Bristol-Myers CompanyInventors: Dolatrai M. Vyas, Paul M. Skonezny
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Patent number: 4791216Abstract: There are provided paraethylamine phenol compounds of formula I, ##STR1## and pharmaceutically acceptable derivatives thereof. There are also described the use of the compounds of formula I as pharmaceuticals, methods for making the compounds and pharmaceutical, e.g. cardiac, compositions containing the compounds.Type: GrantFiled: December 5, 1986Date of Patent: December 13, 1988Assignee: Fisons plcInventors: Francis Ince, Alan C. Tinker
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Patent number: 4780550Abstract: Compounds of the formula ##STR1## wherein R is hydrogen; halogen; C.sub.1 -C.sub.2 alkyl; C.sub.1 -C.sub.2 alkoxy; nitro; cyano; C.sub.1 -C.sub.2 haloalkyl; or R.sup.a SO.sub.m -- wherein m is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are methyl or ethyl;R.sup.5 and R.sup.6 independently are (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.4 alkyl; (4) C.sub.1 -C.sub.4 alkoxy; (5) trifluoromethoxy; (6) cyano; (7) nitro; (8) C.sub.1 -C.sub.4 haloalkyl; (9) R.sup.b SO.sub.n -- wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10) --NR.sup.c R.sup.d wherein R.sup.c and R hu d independently are hydrogen or C.sub.1 -C.sub.4 alkyl; (11) R.sup.e C(O)-- wherein R.sup.e is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; or (12) --SO.sub.2 NR.sup.c R.sup.d wherein R.sup.c and R.sup.d are as defined; and (13) --N(R.sup.c)C(O)R.sup.d wherein R.sup.c and R.sup.Type: GrantFiled: September 17, 1987Date of Patent: October 25, 1988Assignee: Stauffer Chemical CompanyInventor: Charles G. Carter
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Patent number: 4772631Abstract: The invention concerns a series of novel phenoxyacetic acid ethers (and pharmaceutically acceptable salts thereof) of the formula I in which R.sup.1 is H or F, R.sup.2 and R.sup.3 are H or (1-3C)alkyl, Z is CH.sub.2 OH or a group --CO.R.sup.4 in which R.sup.4 is OH, NH.sub.2 or (1-6C)alkoxy. The invention also includes pharmaceutical compositions for use in treating obesity and related conditions and provides processes for the manufacture of the novel ethers.Type: GrantFiled: July 28, 1986Date of Patent: September 20, 1988Assignee: Imperial Chemical Industries PlCInventors: Brian R. Holloway, Ralph Howe, Balbir S. Rao, Donald Stribling
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Patent number: 4764619Abstract: An optically active compound having the formula: ##STR1## wherein each of Z and Z' is a single bond, --COO--, --OCO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 -- or --CH.sub.2 O--, R is an alkyl group having from 1 to 12 carbon atoms, an alkoxyl group having from 1 to 12 carbon atoms, a cyano group or a halogen atom, each of rings A and B is a 1,4-di-substituted phenylene group or a trans-1,4-di-substituted cyclohexylene group, n is 0 or 1, X is ##STR2## wherein * indicates an optical center, and R' is an alkyl group having from 2 to 12 carbon atoms or ##STR3## where R" is a hydrogen atom, an alkyl or alkoxy group having from 1 to 12 carbon atoms, provided that when X is ##STR4## R is the alkyl group or the alkoxy group.Type: GrantFiled: March 21, 1986Date of Patent: August 16, 1988Assignee: Asahi Glass Company Ltd.Inventors: Tomoki Gunjima, Ryutaro Takei, Eriko Aoyama
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Patent number: 4753962Abstract: The compounds of the formula (II): ##STR1## and their pharmaceutically acceptable salts wherein R.sub.1 is a hydrogen, fluorine or chlorine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R.sub.2 is a hydrogen, fluorine or chlorine atom or a hydroxyl group; R.sub.3 is a hydrogen or chlorine atom or a hydroxyl group; R.sub.4 is a carboxylic acid group or a salt, ester or amide thereof; R.sub.5 is a hydrogen, chlorine or fluorine atom or a methyl, methoxyl or hydroxyl group or a carboxylic acid group or a salt, ester or amide thereof; R.sub.6 is a hydrogen atom or a methyl, or propyl group; X is an oxygen atom or a bond; and Y is an alkylene group of up to 6 carbon atoms or a bond have been found to possess anti-obesity and/or anti-hyperglycaemic activity.Type: GrantFiled: December 1, 1986Date of Patent: June 28, 1988Assignee: Beecham Group p.l.c.Inventors: Anthony T. Ainsworth, David G. Smith
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Patent number: 4749809Abstract: The present invention relates to an optically active borane complex represented by the general formula, ##STR1## wherein R.sup.1 represents an aryl group, R.sup.2 represents an alkyl group and a mark * means an asymmetric carbon, and a method for producing optically active alcohol derivatives by the reduction of prochiral ketones with said borane complex. The optically active alcohol derivative is useful for fungicides, herbicides or plant growth regulators.Type: GrantFiled: July 1, 1985Date of Patent: June 7, 1988Assignee: Sumitomo Chemical Company, LimitedInventors: Yukio Yoneyoshi, Gohfu Suzukamo, Kazuhiko Hamada, Toshio Nishioka
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Patent number: 4748184Abstract: The present invention relates to new compounds of the formula ##STR1## wherein X is ##STR2## wherein R.sub.1 is hydrogen, lower alkyl, phenyl, benzyl, cinnamoyl, thiophene, furan, pyrrole, imidazole, pyrazole oxazole or thiazole; W is hydrogen or hydroxy; (Y).sub.A is positioned ortho to W and is an aminoloweralkyl having the formula --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 are the same or different and may be lower alkyl or R.sub.2 and R.sub.3 may together with N form a pyrrolidine, piperidine or azepine ring, and A is 2; n and m are independently from 0 to 5; and R is straight or branched C.sub.1 -C.sub.10 alkyl, straight or branched C.sub.3 -C.sub.10 cycloalkyl, straight or branched C.sub.2 -C.sub.4 alkenyl or straight or branched C.sub.2 -C.sub.4 alkynyl, or a pharmaceutically acceptable salt thereof.These compounds are useful in the treatment of various cardiac arrhythmias.Type: GrantFiled: December 27, 1985Date of Patent: May 31, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: David M. Stout, William L. Matier, Lawrence A. Black
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Patent number: 4738787Abstract: The present application relates to cationic block polyesters useful as soil relese agents, softeners and antistatic agents. In addition to cleaning performance, laundry detergent compositions should have other benefits. One is the ability to impart soil release properties to fabrics woven from polyester fibers.Type: GrantFiled: May 26, 1987Date of Patent: April 19, 1988Assignee: Alkaril Chemicals Inc.Inventors: Anthony J. O'Lenick, Jr., Joseph J. Fanelli
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Patent number: 4735959Abstract: There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.Type: GrantFiled: May 14, 1985Date of Patent: April 5, 1988Assignee: Dr. Karl Thomae GmbHInventors: Wolfgang Grell, Gerhart Griss, Robert Sauter, Rudolf Hurnaus, Eckhard Rupprecht, Nikolaus Kaubisch, Joachim Kahling, Bernhard Eisele
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Patent number: 4730008Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein Ar, R.sup.1, R.sup.2, X, Y and Q are defined in the specification and physiologically acceptable salts and solvates thereof.The compounds have a selective stimulant action at .beta..sub.2 -adrenoreceptors and may be used, inter alia, in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: January 10, 1986Date of Patent: March 8, 1988Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Harry Finch, Alan Naylor, Lawrence H. C. Lunts, Ian B. Campbell
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Patent number: 4728740Abstract: There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.Type: GrantFiled: September 15, 1986Date of Patent: March 1, 1988Assignee: Bristol-Myers CompanyInventors: Dolatrai M. Vyas, Paul M. Skonezny
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Patent number: 4727181Abstract: Prepare esters of .alpha.-halocinnamic acid and related compounds in high yield under relatively mild conditions.Type: GrantFiled: April 21, 1986Date of Patent: February 23, 1988Assignee: The Dow Chemical CompanyInventor: William J. Kruper, Jr.
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Patent number: 4724263Abstract: Compounds of the formula ##STR1## wherein R is hydrogen; halogen; C.sub.1 -C.sub.2 alkyl; C.sub.1 -C.sub.2 alkoxy; nitro; cyano; C.sub.1 -C.sub.2 haloalkyl; or R.sup.a SO.sub.m --wherein m is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are methyl or ethyl;R.sup.5 and R.sup.6 independently are (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.4 alkyl; (4) C.sub.1 -C.sub.4 alkoxy; (5) trifluoromethoxy; (6) cyano; (7) nitro; (8) C.sub.1 -C.sub.4 haloalkyl; (9) R.sup.b SO.sub.n --wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10) --NR.sup.c R.sup.d wherein R.sup.c and R.sup.d independently are hydrogen or C.sub.1 -C.sub.4 alkyl; (11) R.sup.e C(O)--wherein R.sup.e is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; or (12) --SO.sub.2 NR.sup.c R.sup.d wherein R.sup.c and R.sup.d are as defined; and (13) --N(R.sup.c)C(O)R.sup.d wherein R.sup.c and R.sup.Type: GrantFiled: June 9, 1986Date of Patent: February 9, 1988Assignee: Stauffer Chemical CompanyInventor: Charles G. Carter
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Patent number: 4692465Abstract: Compounds of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereof, wherein: Ar is benzofuran-2-yl, or phenyl optionally substituted by groups R.sup.1 and/or R.sup.2 wherein R.sup.1 is halogen, trifluoromethyl or hydroxy and R.sup.2 is halogen;R.sup.3 is hydrogen or methyl;X is --O(CH.sub.2).sub.a CO.sub.2 H, --O(CH.sub.2)bM or --CO.sub.2 Hin whicha is an integer from 1 to 6,b is an integer from 2 to 7,M is hydroxy, C.sub.1-6 alkoxy, phenyl C.sub.1-6 alkoxy, or --NR.sup.4 R.sup.5 in which R.sup.4 and R.sup.5 are each hydrogen or C.sub.1-6 alkyl or together form a five or six membered heterocyclic ring;Y is C.sub.2-6 straight or branched alkylene, with at least two carbon atoms between the --O-- and --OH;and n is 1 or 2,having anti-obesity and/or anti-hyperglycaemic activity, processes for their preparation and their pharmaceutical use.Type: GrantFiled: August 15, 1984Date of Patent: September 8, 1987Assignee: Beecham Group PLCInventors: Richard M. Hindley, John Berge
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Patent number: 4668727Abstract: Ester substituted benzylhydroxylamine derivatives are effective in stabilizing polyolefin compositions containing a stabilizer or mixture of stabilizers selected from the group consisting of the phenolic antioxidants, the hindered amine light stabilizers, the alkylated hydroxybenzoate light stabilizers, the ultraviolet light absorbers, the organic phosphorus compounds, the alkaline metal salts of fatty acids and the thiosynergists, against degradation upon high temperature extrusion, exposure to the combustion products of natural gas, gamma irradiation or upon storage for extended periods. These ester substituted benzylhydroxylamine derivatives exhibit resistance to loss or extraction during processing and in end-use applications.Type: GrantFiled: November 21, 1985Date of Patent: May 26, 1987Assignee: Ciba-Geigy CorporationInventors: Ramanathan Ravichandran, Thomas E. Snead