Ureido, Guanido Or Hydrazino In Acid Moiety Patents (Class 560/34)
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Patent number: 4956460Abstract: A process for the preparation of 1-alkyl-3-carboxy-4-cinnolones of formula I ##STR1## wherein R and R.sub.1 are electron donor groups and R.sub.3 is an alkyl group, starting from an amine of formula II ##STR2## which is subjected to the following transformations; (1) diazotation;(2) coupling with a cyanoacetic ester;(3) alkylation of the arylhydrazone obtained in (2);(4) hydrolysis of the ester and conversion into acyl chloride;(5) intramolecular cyclization;(6) hydrolysis of the nitrile residue.Type: GrantFiled: March 23, 1988Date of Patent: September 11, 1990Assignee: Industria Chimica Profarmaco S.p.A.Inventors: Raffaello Fusco, Fulvio L. Piselli, Pier M. Boschi
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Patent number: 4948808Abstract: A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m--, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.Type: GrantFiled: July 28, 1988Date of Patent: August 14, 1990Assignee: Eisai Co., Ltd.Inventors: Shigeru Souda, Naoyuki Shimomura, Norihiro Ueda, Shuhei Miyazawa, Takashi Yamanaka, Kaname Miyamoto, Ieharu Hishinuma, Junichi Nagakawa, Naoko Nagaoka, Hidetoshi Kawashima, Tsutomu Kawata, Junsaku Nagaoka, Tsuneo Wakabayashi
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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: 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: 4940811Abstract: N,O-acylates, derived from N-acylated carbamic acids, of desferrioxamine B of the formula ##STR1## in which B represents a carbamoyl radical of the partial formula --CO--NH--Alk--CO--O--R.sub.a.sup.1 (II) in which R.sub.a.sup.1 represents C.sub.1 -C.sub.4 -alkyl or C.sub.2 -C.sub.4 -alkyenyl and Alk represents C.sub.1 -C.sub.7 -alkylene that is optionally substituted by hydroxy, C.sub.1 -C.sub.4 -alkanoyloxy, amino, C.sub.1 -C.sub.4 -alkoxycarbonyl, carbamoyl, phenyl, hydroxyphenyl, methoxyphenyl or by indolyl, and each of the symbols A.sup.1, A.sup.2 and A.sup.3, independently of the others, represents hydrogen, an acyl radical Ac derived from a carboxylic acid, or an above-defined carbamoyl radical of the partial formula II, form strong iron(III) and aluminium complexes in living cells.Type: GrantFiled: November 30, 1987Date of Patent: July 10, 1990Assignee: Ciba-Geigy CorporationInventor: Heinrich Peter
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Patent number: 4938794Abstract: A cinnoline derivative having the formula (I): ##STR1## in which X is --OH, --O.sup.- M.sup.+, --OR.sup.1 or ##STR2## wherein M.sup.+ is an alkali metal cation, an alkaline earth metal cation or ##STR3## in which R.sup.4, R.sup.5 and R.sup.6 are the same or different and each is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a C.sub.3 -C.sub.4 alkenyl group, a C.sub.3 -C.sub.4 alkynyl group, a C.sub.3 -C.sub.8 cycloalkyl group, a benzyl group or a phenyl group; R.sup.1 is a C.sub.1 -C.sub.9 alkyl group, a C.sub.3 -C.sub.6 alkenyl group, a C.sub.3 -C.sub.4 alkynyl group, a C.sub.1 -C.sub.3 alkoxy(C.sub.1 -C.sub.4) alkyl group, a C.sub.1 -C.sub.3 haloalkyl group, a C.sub.3 -C.sub.8 cycloalkyl group, a benzyl group or a phenyl group; and R.sup.2 and R.sup.3 are the same or different and each is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a C.sub.3 -C.sub.4 alkenyl group, a C.sub.3 -C.sub.4 alkynyl group, a C.sub.3 -C.sub.8 cycloalkyl group, a benzyl group in which at most two of hydrogen atoms at the .Type: GrantFiled: December 9, 1988Date of Patent: July 3, 1990Assignee: Sumitomo Chemical Company, LimitedInventors: Masato Mizutani, Masao Shiroshita, Masaharu Sakaki, Nobuaki Mito, Hiroki Okuda
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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: 4915727Abstract: A plant male sterilant, which comprises as an active ingredient a compound having the formula (I): ##STR1## in which X is --OH, --O.sup.- M.sup.+, --OR.sup.1 or ##STR2## wherein M.sup.+ is an alkali metal cation, an alkaline earth metal cation or ##STR3## in which R.sup.4, R.sup.5 and R.sup.6 are the same or different and each is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.4 alkenyl group, C.sub.3 -C.sub.4 alkynyl, C.sub.3 -C.sub.8 cycloslkyl, benzyl or phenyl group;R.sup.1 is a C.sub.1 -C.sub.9 alkyl, a C.sub.3 -C.sub.6 alkenyl, a C.sub.3 -C.sub.4 alkynyl, C.sub.1 -C.sub.3 alkoxy (C.sub.1 -C.sub.4)-alkyl, C.sub.3 -C.sub.8 cycloalkyl, benzyl or phenyl; andR.sup.2 and R.sup.3 are the same or different and each is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.4 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, a benzyl group in which at most two hydrogen atoms at the .alpha.-position thereof may be substituted by methyl, C.sub.2 -C.sub.Type: GrantFiled: December 24, 1987Date of Patent: April 10, 1990Assignee: Sumitomo Chemical Company, LimitedInventors: Masato Mizutani, Masao Shiroshita, Nobuaki Mito, Hiroki Okuda, Masaharu Sakaki
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Patent number: 4914128Abstract: Acrylates of the general formula ##STR1## where R.sup.1 and R.sup.2 independently of one another are each C.sub.1 -C.sub.8 -alkyl, X is hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen, C.sub.1 -C.sub.4 -alkoxy, haloalkyl, cyano or nitro, W is unsubstituted or alkyl-substituted, saturated or unsaturated C.sub.1 -C.sub.10 -alkylene, Y is hydrogen, alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, aralkyl, aryl, aryloxy, halogen, an unsubstituted or substituted C.sub.4 H.sub.4 chain which is fused to the benzene radical, alkoxy, haloalkoxy, alkylthio, thiocyanato, cyano, NO.sub.2, ##STR2## where R' and R" independently of one another are each hydrogen, alkyl, alkoxy, alkylthio or cycloalkyl, or are phenyl which is unsubstituted or substituted by alkyl, halogen or alkoxy, m is 0 or 1, n is from 1 to 4 and Z is oxygen, sulfur, SO or SO.sub.2, and fungicides containing them.Type: GrantFiled: October 11, 1988Date of Patent: April 3, 1990Assignee: BASF AktiengesellschaftInventors: Ulrich Schirmer, Stefan Karbach, Ernst-Heinrich Pommer, Eberhard Ammermann, Wolfgang Steglich, Barbara A. M. Schwalge, Timm Anke
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Patent number: 4908451Abstract: A process is disclosed for the preparation of .alpha.-substituted carbonyl compounds, wherein .alpha.-substituted ketone is prepared by the following reaction: ##STR1## .alpha.-azo ester is prepared by the following reaction: ##STR2## and .alpha.-hydrozono ester is prepared by the following reaction: ##STR3## wherein the .alpha.-azo ester and .alpha.-hydrazono ester obtained by the above reactions include novel compounds, which are also disclosed.Type: GrantFiled: March 23, 1988Date of Patent: March 13, 1990Assignee: Agency of Industrial Science and TechnologyInventors: Masato Tanaka, Toshiyasu Sakakura
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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: 4906767Abstract: There is disclosed a family of new vinyl monomers capable of forming polymers by free radical polymerization. The vinyl monomer is of the formula ##STR1## wherein R.sub.1 and R.sub.2 are substituted or unsubstituted hydrocarbons, X is O, NH or NR.sub.3, and R.sub.3 is substituted or unsubstituted hydrocarbon.The intermediates in the synthesis of these monomers are new beta-chloroalanine ureas. The polymers are useful in film and fiber formation and display good toughness. These new vinyl monomers also form a cyclic monomer.Type: GrantFiled: June 30, 1987Date of Patent: March 6, 1990Assignee: The University of Southern MississippiInventors: Lon J. Mathias, David W. Kurz
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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: 4888043Abstract: The invention concerns compounds of the formula I ##STR1## wherein: Z is selected from hydrogen, alkyl, alkanoyl, sulfamoyl, carboxy and trifluoroacetamido;Y is selected from various carboxy or thiocarboxy groups, haloalkanoyl, alkylsulfonyl and haloalkylsulfonyl;R.sup.1 is selected from hydrogen, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl and alkynyl;R.sup.3 is selected from alkyl; andR.sup.4 is selected from hydrogen, alkyl, and alkoxycarbonyl.The compounds of the invention show herbicidal properties and plant growth regulating properties and in further embodiments and the invention provides processes for the preparation of compounds of formula I, intermediates useful in the preparation of the compounds of formula I, compositions containing as active ingredient a compound of formula I, and herbicidal and plant growth regulating processes utilizing compounds of formula I.Type: GrantFiled: June 20, 1986Date of Patent: December 19, 1989Assignee: ICI Australia LimitedInventors: Keith G. Watson, Craig G. Lovel
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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: 4877540Abstract: Methylolated and optionally etherified urethanes containing fluoroalkyl ligans with formaldehyde, with or witout subsequent etherification, and are in the form of their solutions or aqueous dispersions suitable for the treatment of textiles and leather.Type: GrantFiled: August 8, 1988Date of Patent: October 31, 1989Assignee: Cassella AktiengesellschaftInventors: Fritz Engelhardt, Karl Hintermeier, Manfred Muller, Norbert Munch, Hans Wagener
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Patent number: 4874803Abstract: The present invention comprises reaction products resulting from the reaction of hydrazido-substituted or certain amino-substituted polymer stabilizers and cyclic dianhydrides, as well as the use of such products. The polymer stabilizers of the invention are useful for protecting a large variety of synthetic polymeric organic materials from the degradative effects of heat, light and oxygen. Some of the modifiers are flame retardants and many are metal deactivators in addition to their primary activity.Type: GrantFiled: September 21, 1987Date of Patent: October 17, 1989Assignee: Pennwalt CorporationInventors: Arthur L. Baron, Terry N. Myers, Jerome Wicher
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Patent number: 4873264Abstract: Novel 1-(alkylphenoxyphenyl)-3-benzoyl ureas and a process for their preparation are provided. The novel ureas are useful as the active toxicant in pesticidal composition.Type: GrantFiled: March 7, 1988Date of Patent: October 10, 1989Assignee: Rhone-Poulenc Nederlands B.V.Inventors: David T. Chou, Paul A. Cain
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Patent number: 4873253Abstract: A phenylalanine derivative having the formula (I): ##STR1## wherein A represents ##STR2## B represents ##STR3## wherein m is 0, 1, or 2 and n is 3, 4, or 5; X represents (a) hydroxy, (b) nitro, (c) amino, (d) phenoxy which may be substituted with (i) halogen or (ii) nitro, (e) c.sub.1 -C.sub.4 alkyloxy which may be substituted wit (i) phenyl or (ii) benzoyl, (f) benzoyl, (g) pyridyloxy which may be substituted with (i) halogen or (ii) nitro, or (h) c.sub.1 -C.sub.4 alkyl which may by substituted with halogen;Y represents ##STR4## or --OR.sup.3 wherein R.sup.1 R.sup.2 are independently (a) hydrogen, (b) phenyl which may be substituted with (i) benzoyl, (ii) C.sub.1 -C.sub.4 alkylcarbonyl, (iii) C.sub.1 -C.sub.4 alkyl which may be further substituted with C.sub.1 -C.sub.4 alkoxycarbonyl or hydroxycarbonyl, (iv) C.sub.2 -C.sub.5 alkenyl which may be further substituted with hydroxycarbonyl or C.sub.1 -C.sub.4 alkoxycarbonyl, (v) C.sub.1 -C.sub.Type: GrantFiled: March 30, 1987Date of Patent: October 10, 1989Assignees: Shosuke Okamoto, Showa Denko Kabushiki KaishaInventors: Shosuke Okamoto, Yoshio Okada, Akiko Okunomiya, Taketoshi Naito, Yoshio Kimura, Morihiko Yamada, Norio Ohno, Yasuhiro Katsuura, Hiroshi Nojima, Takashi Shishikura
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Patent number: 4870210Abstract: There are disclosed compounds of the formula ##STR1## wherein ##STR2## R is hydrogen, lower alkyl, phenyl or benzyl; R.sup.1 is hydrogen, lower alkyl, trifluoromethyl, amino, mono- or di- lower alkylamino, nitro, hydroxy, carboxy, lower alkoxycarbonyl, lower alkoxy or halo;R.sup.2 is hydrogen or lower alkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other inflammatory conditions.Type: GrantFiled: December 18, 1987Date of Patent: September 26, 1989Assignee: American Home Products CorporationInventor: John H. Musser
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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: 4868215Abstract: N-aroyl N'-phenyl ureas having the formula ##STR1## wherein: Ar is a substituted phenyl, pyridyl or pyrimidinyl radical wherein the substituents are chloro, bromo, fluoro C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy, with the proviso that at least one substituent is positioned ortho to the carbonyl group; R.sub.3 and R.sub.4 are individually H or C.sub.1 -C.sub.4 alkyl or together they form the group ##STR2## Y is O or S; X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are individually H, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, alkylcarbonyl, alkoxycarbonyl, C.sub.1 -C.sub.3 alkylthio, NO.sub.2, CN or NR.sub.5 R.sub.6 wherein R.sub.5 and R.sub.6 are H or C.sub.1 -C.sub.3 alkyl with the provisos that at least one of X.sub.1, X.sub.2, X.sub.3 or X.sub.4 is other than H and (a) when three of X.sub.1, X.sub.2, X.sub.3 or X.sub.4 are H, the fourth substitution cannot be halogen or alkyl, (b) when X.sub.1 and X.sub.3 are H, X.sub.2 and X.sub.4 cannot both be halogen, (c) when X.sub.2 and X.sub.Type: GrantFiled: September 24, 1984Date of Patent: September 19, 1989Assignee: The Dow Chemical CompanyInventors: Barat Bisabri-Ershadi, Raymond H. Rigterink
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Patent number: 4866173Abstract: There are disclosed semicarbazides having antihypertensive and angiotensin converting enzyme inhibitory activity.Type: GrantFiled: November 23, 1987Date of Patent: September 12, 1989Assignee: Rorer Pharmaceutical CorporationInventor: Fu-chih Huang
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Patent number: 4861799Abstract: A benzoylurea compound having the formula: ##STR1## wherein each of X.sub.1 and X.sub.2 is a hydrogen atom, a halogen atom or a methyl group, provided that X.sub.1 and X.sub.2 are not simultaneously hydrogen atoms, Y is independently a hydrogen atom, a halogen atom, an alkyl group which may be substituted by halogen, a --CO.sub.2 R.sub.1 group wherein R.sub.1 is a hydrogen atom, a cation or an alkyl group, or a --OR.sub.1 group wherein R.sub.1 is as defined above, A.sub.1 is .dbd.N--or ##STR2## wherein Y is as defined above, W is an oxygen atom, a sulfur atom or ##STR3## wherein R.sub.1 is as defined above, k is an integer of from 1 to 3, l is 0 or 1, and Ar is ##STR4## wherein Z is independently a hydrogen atom, a halogen atom, an alkyl group which may be substituted by halogen, an alkoxy group which may be substituted by halogen, a nitro group, a cyano group or a --S(O).sub.n R.sub.2 group wherein R.sub.2 is an alkyl group which may be substituted by halogen and n is 0, 1 or 2, A.sub.Type: GrantFiled: September 30, 1987Date of Patent: August 29, 1989Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Takahiro Haga, Tadaaki Toki, Toru Koyanagi, Yasuhiro Fujii, Kiyomitsu Yoshida, Osamu Imai
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Patent number: 4859233Abstract: Disclosed are herbicidal compounds of the general formula I; ##STR1## wherein A is O-alkylene of 1 to 5 carbon atoms, O-alkenylene of 3 to 6 carbon atoms in which the unsaturation is non-adjacent the oxygen atom thereof or NH-alkylene in which the alkylene is of 1 to 5 carbon atoms, and --COZR is an acid function or forms certain ester or thioester functions, and the mono- and di-salt forms thereof.Type: GrantFiled: January 25, 1988Date of Patent: August 22, 1989Assignee: Sandoz Ltd.Inventor: John W. Williams
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Patent number: 4843094Abstract: Compounds presented by the general formula: ##STR1## [wherein when Y is oxygen, R.sup.2 is H, alkyl, alkoxy, alkoxymethyl, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --CH.dbd.CH--COOR.sup.3, halogen, --CF.sub.3, --COR.sup.4, --OCOR.sup.4, --CH.sub.2 OCOR.sup.4, --SO.sub.2 R.sup.4, --OSO.sub.2 R.sup.4, --CONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6, --CONH--SO.sub.2 NR.sup.5 R.sup.6, --NHSO.sub.2 R.sup.7, --NO.sub.2, --OH, --CH.sub.2 OH, guanidino, benzyloxy, guanidinophenylthiomethyl, morpholinosulfonylphenoxymethyl, pyridyloxymethyl, or (1,1-dioxothiazol-3-yl)carbonyl, or when Y is sulfur, R.sup.2 is H, alkyl, alkoxy, halogen, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --NO.sub.2, or --SO.sub.2 NR.sup.5 R.sup.6, and n represents an integer of one to five, and when n represents more than two, each of R.sup.2 may be the same group or the different group.Type: GrantFiled: November 12, 1986Date of Patent: June 27, 1989Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Katsuhiro Imaki, Yoshinobu Arai, Hiroyuki Ohno
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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: 4822729Abstract: Cyan-forming color couplers according to the formula: ##STR1## wherein Z is hydrogen or a coupling off group, R.sup.1 is hydrogen, a halogen atom, alkyl, or alkoxy, R.sup.2 is hydrogen or alkyl, R.sub.3 is hydrogen, a halogen atom, alkyl, alkoxy, alkylsulphonyl, alkanamidosulphonyl, alkoxycarbonyl, alkanamidocarbonyl, alkanamido, alkylsulphonamido, or cyano, R.sup.4 is a substituent standing at the 3- or 6-position of the phenol and selected from hydrogen, a halogen atom, and alkyl, and n is 0 or 1. These couplers can be incorporated into (a) red-sensitized silver halide emulsion layer(s) of a photographic multilayer color element or in a non-light-sensitive colloid layer in water-permeable relationship with the red-sensitized emulsion layer(s).Type: GrantFiled: November 24, 1987Date of Patent: April 18, 1989Assignee: AGFA-Gevaert, N.V.Inventors: Marcel J. Monbaliu, Paul L. Van Meerbeeck
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Patent number: 4820730Abstract: Amidine compounds of formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof are novel and are of use as anti-trypsin, anti-plasmin, anti-kallikrein, anti-thrombin and anti-complement agents which may be administered orally. These amidine compounds can be produced by the reaction between a carboxylic acid compound of formula (II) ##STR2## or a reactive intermediate thereof and 6-amidino-2-naphthol of formula (III) ##STR3## or preferably an acid addition salt thereof.Type: GrantFiled: July 11, 1988Date of Patent: April 11, 1989Assignee: Torii & Co., Ltd.Inventors: Setsurou Fujii, Toshiyuki Okutome, Toyoo Nakayama, Shigeki Nunomura, Kimio Sudo, Shinichi Watanabe, Masateru Kurumi, Takuo Aoyama
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Patent number: 4814349Abstract: The present invention relates to methods for controlling insect populations and for protecting living plants from insect attack by applying to said plants or to the soil in which they are growin an insecticidally-effective amount of a substituted benzoic acid 1 or 2-alkyl or 2-cycloalkylhydrazide.Novel substituted benzoic acid 1 and 2-alkyl and 2-cycloalkylhydrazides effective as insecticides or intermediates for the preparation of insecticidal diacylhydrazides also are presented.Type: GrantFiled: November 12, 1986Date of Patent: March 21, 1989Assignee: American Cyanamid CompanyInventors: Roger W. Addor, David G. Kuhn, Donald P. Wright, Jr.
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Patent number: 4801603Abstract: A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m --, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.Type: GrantFiled: December 24, 1986Date of Patent: January 31, 1989Assignee: Eisai Co., Ltd.Inventors: Shigeru Souda, Naoyuki Shimomura, Norihiro Ueda, Shuhei Miyazawa, Takashi Yamanaka, Kaname Miyamoto, Ieharu Hishinuma, Junichi Nagakawa, Naoko Nagaoka, Hidetoshi Kawashima, Tsutomu Kawata, Junsaku Nagaoka, Tsuneo Wakabayashi
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Patent number: 4783485Abstract: The invention relates to new benzoylurea compounds having insecticidal and acaricidal activity, of the general formula ##STR1## wherein R.sub.1 is a hydrogen atom or represents 1 or 2 halogen atoms;Ar is a para-phenylene group or a para-pyridylene group, which groups may be substituted with 1 or 2 substituents selected from the group consisting of chlorine, methyl and trifluoromethyl;B is an oxygen atom or represents a group having the formula ##STR2## wherein R.sub.Type: GrantFiled: September 26, 1986Date of Patent: November 8, 1988Assignee: Duphar International Research B.V.Inventors: Marius S. Brouwer, Arnoldus C. Grosscurt, Roelof Van Hes
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Patent number: 4782177Abstract: Acrylic acid derivatives of the general formula ##STR1## where R.sup.1 and R.sup.2 independently of one another are each alkyl, X is hydrogen, halogen, alkoxy, trifluoromethyl, cyano or nitro, Y is hydrogen, alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, aralkyl, aryl, aryloxy, halogen, an unsubstituted or substituted C.sub.4 H.sub.4 chain which is fused to the benzene radical, alkoxy, haloalkoxy, NO.sub.2, alkylthio, thiocyanato, cyano, ##STR2## R' and R" independently of one another are each hydrogen, alkyl, alkoxy, alkylthio or cycloalkyl or are each unsubstituted or substituted phenyl, and n is from 1 to 4, and fungicides containing these compounds.Type: GrantFiled: December 15, 1986Date of Patent: November 1, 1988Assignee: BASF AktiengesellschaftInventors: Ulrich Schirmer, Stefan Karbach, Ernst-Heinrich Pommer, Eberhard Ammermann, Wolfgang Steglich, Barbara A. M. Schwalge, Timm Anke
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Patent number: 4777182Abstract: Amidine compounds of formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof are novel and are of use as anti-trypsin, anti-plasmin, anti-kallikrein, anti-thrombin and anti-complement agents which may be administered orally. These amidine compounds can be produced by the reaction between a carboxylic acid compound of formula (II) ##STR2## or a reactive intermediate thereof and 6-amidino-2-naphthol of formula (III) ##STR3## or preferably an acid addition salt thereof.Type: GrantFiled: February 24, 1986Date of Patent: October 11, 1988Assignee: Torii & Co., Ltd.Inventors: Setsurou Fujii, Toshiyuki Okutome, Toyoo Nakayama, Shigeki Nunomura, Kimio Sudo, Shinichi Watanabe, Masateru Kurumi, Takuo Aoyama
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Patent number: 4760163Abstract: The disclosure is concerned with novel 3-aryluracils of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and X have the significances given in the description, as well as salts thereof and their manufacture, weed control compositions which contain such compounds as active ingredients and the use of the active ingredients or compositions for the control of weeds. The disclosure also concerns certain herbicidally active starting materials and weed control compositions containing these as active ingredients.Type: GrantFiled: January 25, 1988Date of Patent: July 26, 1988Assignee: Hoffmann-LaRoche Inc.Inventors: Jean Wenger, Paul Winternitz
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Patent number: 4752615Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, particularly their strains resistant to benzimidazole, thiophanate and/or cyclic imide fungicides.Type: GrantFiled: November 13, 1986Date of Patent: June 21, 1988Assignee: Sumitomo Chemical Company, LimitedInventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
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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: 4734520Abstract: Crosslinking components for hydroxy and/or primary and/or secondary amino group containing paint binders for the crosslinking of synthetic resins carrying at least two groups capable of ester or amide formation with carboxylic acids. In particular there is disclosed the use of the crosslinking components in compositions for electrodeposition (ED) whereby at 120.degree. C. and above coatings with extraordinary paint performance are obtained. The use of methyl or ethyl esters gives extremely low condensation losses. The crosslinking components are obtained through reaction of one mole of a diisocyanate, preferably at room temperature, in the presence of sodium, or preferably sodium phenolate, as catalyst, with at least one mole of a CH-active alkyl ester of the general formula X--CH.sub.2 --COOR, wherein X is --COOR, --CN or CH.sub.3 --CO-- and R is an alkyl radical with 1 to 8 C-atoms and subsequent reaction of the free isocyanate groups with polyamines of the general formula H.sub.2 N--(R--NH).sub.n --R--NH.Type: GrantFiled: May 29, 1986Date of Patent: March 29, 1988Assignee: Vianova Kunstharz, A.G.Inventors: Helmut Plum, Willibald Paar
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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: 4717736Abstract: Compounds having the formula: ##STR1##are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory agents and cytoprotective agents.Type: GrantFiled: November 21, 1984Date of Patent: January 5, 1988Assignee: Merck Frosst Canada, Inc.Inventors: Joshua Rokach, Robert N. Young
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Patent number: 4711905Abstract: A 2,4-dihalogenobenzoyl-(thio)urea of the formula ##STR1## in which X represents sulphur or oxygen,X.sup.1 and X.sup.2 are identical or different and represent fluorine, chlorine, bromine or iodine,R.sup.1 represents hydrogen, halogen or optionally substituted radicals from the series comprising alkyl, alkoxy and alkylthio,R.sup.2 represents hydrogen, halogen, cyano, nitro, or optionally substituted radicals from the series comprising alkyl, alkylthio, alkylsulphonyl, alkoxy, aryloxy, alkylcarbonyl, alkoxycarbonyl, alkoxycarbonylalkyl and alkoxycarbonylalkylthio, orR.sup.1 and R.sup.2 together represent an optionally substituted alkylenedioxy radical or --CF.sub.2 --O--CF.sub.2 --O--,R.sup.3 represents hydrogen, halogen or an optionally substituted alkyl, alkoxy or aryloxy radical, andR.sup.4 represents hydrogen, halogen, or optionally substituted radicals from the series comprising alkyl, alkylthio and alkoxy, with the exception of those cases in which X represents oxygen, X.sup.1 andX.sup.Type: GrantFiled: June 19, 1985Date of Patent: December 8, 1987Assignee: Bayer AktiengesellschaftInventors: Wilhelm Sirrenberg, Erich Klauke, Ingeborg Hammann, Wilhelm Stendel
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Patent number: 4710574Abstract: Disclosed is the hydrocarboxylation of defined enamides with CO and a compound ROH to make amino acids or amido esters, either of which can be hydrolyzed to .alpha.-amino acids.Type: GrantFiled: November 16, 1983Date of Patent: December 1, 1987Assignee: The Standard Oil CompanyInventors: Mark C. Cesa, James D. Burrington
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Patent number: 4709078Abstract: Acrylates of the general formula ##STR1## wherein R.sup.1 and R.sup.2 independently of one another are each C.sub.1 -C.sub.8 -alkyl, X is hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen, C.sub.1 -C.sub.4 -alkoxy, haloalkyl, cyano or nitro, W is unsubstituted or alkyl-substituted, saturated or unsaturated C.sub.1 -C.sub.10 -alkylene, Y is hydrogen, alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, aralkyl, aryl, aryloxy, halogen, an unsubstituted or substituted C.sub.4 H.sub.4 chain fused to the benzene radical, alkoxy, haloalkoxy, alkylthio, thiocyanato, cyano, NO.sub.2, aralkyloxy, ##STR2## and R' and R" independently of one another are each hydrogen, alkyl, alkoxy, alkylthio or cycloalkyl or are each phenyl which is unsubstituted or substituted by alkyl, halogen or alkoxy, and n is from 1 to 4, and fungicides containing them.Type: GrantFiled: May 21, 1986Date of Patent: November 24, 1987Assignee: BASF AktiengesellschaftInventors: Ulrich Schirmer, Stefan Karbach, Ernst-Heinrich Pommer, Eberhard Ammermann, Wolfgang Steglich, Barbara A. M. Schwalge, Timm Anke
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Patent number: 4701447Abstract: This invention relates to organic acid-substituted guanidine compounds. Also disclosed are methods for preparing the compounds, compositions containing them, and methods for their use as anthelmintics.Type: GrantFiled: September 23, 1983Date of Patent: October 20, 1987Assignee: Schering CorporationInventors: Dhiru B. Vashi, Jeffrey N. Clark, Neil A. Lindo
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Patent number: 4699923Abstract: N-Benzoyl-N'-phenylureas of the formula ##STR1## where X, Y, Z and R have the meanings given in the description, are used for insect control.Type: GrantFiled: March 27, 1986Date of Patent: October 13, 1987Assignee: BASF AktiengesellschaftInventors: Arno Lange, Karl Kiehs, Heinrich Adolphi
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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: 4684728Abstract: A biologically active compound can be solubilized by reaction in different sequences to form a derivative carrying the active moiety, a linking group such as an optionally substituted diisocyanate radical, a polyether moiety such as a polyoxyethylene radical, and a terminal group such as a butyl radical, e.g. ##STR1## n=1 to 400. The active materials can be agricultural chemicals, pharmaceuticals, and the like.Type: GrantFiled: December 28, 1979Date of Patent: August 4, 1987Assignee: Bayer AktiengesellschaftInventors: Edgar Mohring, Hanns P. Muller, Peter Roessler, Kuno Wagner, Helmut Tietz
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Patent number: 4683325Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: October 17, 1984Date of Patent: July 28, 1987Assignee: Merck Frosst Canada, Inc.Inventors: Richard Frenette, Joshua Rokach, Masatoshi Kakushima, Robert N. Young
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Patent number: 4681895Abstract: Novel N-phenyl-trans-4-guanidinomethylcyclohexanecarboxamide compounds of the formula: ##STR1## wherein R is hydrogen atom or a lower alkyl group, or a pharmaceutically acceptable salt thereof, which have excellent anti-ulcer activities and hence are useful as an anti-ulcer drug, and a pharmaceutical composition useful for the treatment and prophylaxis of peptic ulcers which comprises as an active ingredient the compound as set forth above in admixture with a conventional pharmaceutically acceptable carrier or diluent.Type: GrantFiled: March 6, 1986Date of Patent: July 21, 1987Assignee: Kanebo, Ltd.Inventors: Toshio Satoh, Goro Tsukamoto