Nitrogen In Acid Moiety Patents (Class 560/12)
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Patent number: 4980349Abstract: The invention relates to new compounds corresponding to formula I: ##STR1## in which: W represents C=O, CH.sub.2 or CHOH,Z represents ##STR2## R.sub.1 and R.sub.2 represent especially Cl or F, R, R' and R" represent especially H,X represents especially CH.sub.2,Y represents especially COOH,u and v are two integers ranging from 0 to 10,p and q take the value 0 or 1,n and m are two integers ranging 0 to 10 andt is 0 or 1the total number of carbon atoms in the chain ##STR3## ranging from 2 to 20, and to their physiologically acceptable salts obtained with organic or inorganic acids.These compounds are useful for preparing medicinal products which have, especially, anti-inflammatory properties.Type: GrantFiled: November 12, 1987Date of Patent: December 25, 1990Assignee: SANOFIInventors: Pierre Roger, Jean-Paul Fournier, Alain Martin, Jean Choay
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Patent number: 4980372Abstract: A benzoylaminophenoxybutanoic acid derivative of general formula: ##STR1## [wherein R.sup.1 represents hydrogen atom or alkyl group of from 1 to 4 carbon atoms(s),A represents oxygen atom, sulfur atom or sulfinyl (SO) group, two R.sup.1 s represents methyl groups or chlorine atoms at the same time or cyclopentane, cyclohexane or benzene ring together with the carbon atoms of benzene ring each attaching,R.sup.2 represents a group of general formula: ##STR2## {wherein B represents oxygen atom, sulfur atom or a group of general formula:NR.sup.11 (wherein R.sup.11 represents hydrogen atom or alkyl group of from 1 to 4 carbon atom(s)),R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 represent, independently, hydrogen atom, alkyl group of from 1 to 4 carbon atom(s) halogen atom, trifluoromethyl group or cyclobutylmethyl group,m represents 0 or 1,n represents an integer of from 1 to 5, andR.sup.9 and R.sup.Type: GrantFiled: May 6, 1988Date of Patent: December 25, 1990Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Hiroshi Terashima, Yoshinobu Arai
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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: 4975460Abstract: Novel indanoxyacetic acid derivatives of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group, a substituted or unsubstituted phenyl group, naphtyl group or a sulfur-containing heterocyclic group, R.sup.2 is hydroxy group or a protected hydroxy group, p is an integer of 2 or 3, and q is an integer of 0 or 1, and a salt thereof are disclosed.Said derivative (I) and a salt thereof are useful as a platelet aggregation-inhibiting agent and an agent for the treatment, amelioration and/or prophylaxis of a variety of thrombosis, embolism, coronary and cerebral vascular smooth muscl vellication, asthma, and the like.Type: GrantFiled: February 17, 1989Date of Patent: December 4, 1990Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takeo Iwakuma, Harumichi Kohno, Yasuhiko Sasaki, Katsuo Ikezawa, Akio Odawara
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Patent number: 4975444Abstract: Compounds of the formula ##STR1## wherein A is a carbocyclic, saturated or unsaturated ring; R.sup.1 is hydrogen or alkyl; R and R.sup.4 are each alkyl, cycloalkyl, benzyl or a readily hydrolyzable ester group; Y is a bond or a straight or branch alkylene; R.sup.2 is hydrogen, aryl, heterocyclic, R.sup.6 CONR.sup.5, R.sup.7 NR.sup.5 CO, R.sup.7 NR.sup.5 SO.sub.2 --or R.sup.8 SO.sub.2 NR.sup.5 --where R.sup.5 is hydrogen, alkyl or aralkyl; R.sup.6 is alkyl, aryl, aralkyl, heterocyclic, heterocyclyalkyl or a group of the formula ##STR2## where R.sup.9 is hydrogen, hydroxy, alkoxy, alkyl, hydroxyalkyl, aralkyl, alkylene, heterocyclic, heterocyclylalkyl, R.sup.12 CONH--, R.sup.12 SO.sub.2 NH-- or (R.sup.13).sub.2 N--; R.sup.10 and R.sup.11 are each hydrogen or alkyl; or R.sup.10 is hydrogen and R.sup.11 is aminoalkyl, imidazolylmethyl, aryl, aralkyl, aralkoxyalkoxy, hydroxyalkyl or methylthioalkyl; or R.sup.10 and R.sup.Type: GrantFiled: August 25, 1989Date of Patent: December 4, 1990Assignee: Pfizer Inc.Inventors: John C. Danilewicz, Keith James, Ryszard J. Kobylecki
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Patent number: 4973732Abstract: Polymers, such as polysiobutylene or ethylene-propylene copolymers, are functionalized by reaction with an activated imine to yield novel polymers.Type: GrantFiled: February 9, 1987Date of Patent: November 27, 1990Assignee: Texaco Inc.Inventors: Phillip B. Valkovich, Kechia J. Chou
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Patent number: 4973733Abstract: Polymers, such as polyisobutylene or ethylene-propylene copolymers, are functionalized by reaction with an activated imine to yield novel polymers.Type: GrantFiled: February 9, 1987Date of Patent: November 27, 1990Assignee: Texaco Inc.Inventors: Phillip B. Valkovich, Kechia J. Chou
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Patent number: 4968829Abstract: Substituted phenoxy, phenylthio and anilino compounds, intermediates therefor, synthesis thereof, and their use for the control of pests.Type: GrantFiled: June 19, 1989Date of Patent: November 6, 1990Assignee: Sandoz Ltd.Inventor: Clive A. Henrick
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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: 4958043Abstract: A composition useful for incorporation into polymer compositions employed for food packaging or the like comprising a bis- or tris-methine compound having the structural formula ##STR1## wherein A is selected from the radicals ##STR2## wherein R' and R" are each selected from chlorine, bromine, fluorine, alkyl, alkoxy, aryl, aryloxy and arylthio;each n is independently 0, 1, 2;R.sub.1 is selected from a large variety of radicals such as cycloalkyl, phenyl, and straight or branched alkyl which may be substituted;R.sub.2 is alkylene or the like;R.sub.3, R.sub.4, and R.sub.5 are each selected from hydrogen and alkyl; andP and Q and P.sup.1 and Q.sup.1 are selected from cyano, carbalkoxy, carbaryloxy, carbaralkyloxy, or the like.The invention compositions are especially useful in combination with molding or fiber-grade condensation polymer; most preferably such polymer having copolymerized therein a total of from 1.Type: GrantFiled: April 18, 1988Date of Patent: September 18, 1990Assignee: Eastman Kodak CompanyInventors: Max A. Weaver, Wayne P. Pruett, Samuel D. Hilbert
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Patent number: 4954513Abstract: This invention relates to alkanoic acid compounds having phenyl and heteroarylthio substituents which are useful as leukotriene antagonists, pharmaceutical compositions containing such compounds, and methods of treating diseases in which leukotrienes are a factor by administration of an effective amount of the above compounds or compositions.Type: GrantFiled: December 23, 1988Date of Patent: September 4, 1990Assignee: SmithKline Beecham CorporationInventors: John G. Gleason, Ralph F. Hall, Joanne Smallheer
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Patent number: 4952726Abstract: N-Phenylsulfonyl-N'-pyrimidinyl- and -triazinylureas of the formula I ##STR1## wherein A is 3,3,3-trifluoropropyl or 3,3-difluorobutyl,R.sup.1 is hydrogen, halogen, nitro, cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkylsulfonyl, C.sub.1 -C.sub.4 -alkylsulfonyl, --CO--R.sup.6, --NR.sup.7 R.sup.8, --CO--NR.sup.9 R.sup.10 or --SO.sub.2 --NR.sup.11 R.sup.12,R.sup.2 is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkysulfonyl or C.sub.1 -C.sub.4 -alkylsulfonyl,R.sup.3 and R.sup.4 independently of one another are each hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.2 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, C.sub.2 -C.sub.4 -alkoxyalkyl, C.sub.1 -C.sub.4 -alkoxy or --NR.sup.13 R.sup.13,R.sup.5 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy,R.sup.6 is C.sub.1 -C.Type: GrantFiled: November 21, 1989Date of Patent: August 28, 1990Assignee: Ciba-Geigy CorporationInventors: Willy Meyer, Konrad Oertle
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Patent number: 4948809Abstract: The present invention provides sulphonylphenylalkylamines of the general formula: ##STR1## wherein R.sub.1 is an alkyl radical containing up to 6 carbon atoms, a cycloalkyl radical containing 3-7 carbon atoms or an aralkyl, aralkenyl or aryl radical, the aryl moiety, in each case, being optionally substituted one or more times by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino, C.sub.1 -C.sub.6 acylamino, C.sub.1 -C.sub.16 acyl or azide, R.sub.2 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical or an aralkyl or aralkenyl radical, the aryl moiety, in each case, optionally being substituted one or more times by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.1 -C.sub.12 dialkylamino, C.sub.1 -C.sub.6 acylamino, C.sub.1 -C.sub.Type: GrantFiled: December 5, 1988Date of Patent: August 14, 1990Assignee: Boehringer Mannheim GmbHInventors: Ernst-Christian Witte, Hans-Peter Wolff, Karlheinz Stegmeier, Johannes Pill
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Patent number: 4948810Abstract: Novel phenoxyacetic acid derivative of the formula: ##STR1## wherein R is a substituted or unsubstituted phenyl group, naphthyl group or a sulfur-containing 5-membered hetero-monocyclic group, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group or phenyl group, R.sup.5 is hydrogen atom or a lower alkyl group, R.sup.6 is carboxyl group, a protected carboxyl group, hydroxy group or a di(lower alkyl)-amino group, Ring A is a substituted or unsubstituted phenylene group, m is 0 or 1 and n is an integer 0 to 5, provided that, when m is 0,(1) at least either one of R.sup.1 to R.sup.4 is or/are a phenyl-lower alkyl group or phenyl group,(2) at least either one of R.sup.1 to R.sup.4 is or/are a lower alkyl group, and R.sup.6 is hydroxy group, or(3) all of R.sup.1 to R.sup.4 are hydrogen atom, and Ring A is a substituted phenylene group,or a pharmaceutically acceptable salt thereof are disclosed.Type: GrantFiled: February 6, 1989Date of Patent: August 14, 1990Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takeo Iwakuma, Takayuki Kawaguchi, Toyoharu Yamashita, Yasuhiko Sasaki, Tamotu Shimazaki
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Patent number: 4946981Abstract: Compounds of the formula ##STR1## wherein R is halogen, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, cyano, nitro, S(O).sub.n R wherein R is C.sub.1 -C.sub.4 alkyl and n is the integer 0, 1 or 2; and R.sup.2 through R.sup.8 are hydrogen or certain substituents, their salts, herbicidal compositions containing the compound or salts and the herbicidal use thereof.Type: GrantFiled: June 27, 1988Date of Patent: August 7, 1990Assignee: ICI Americas Inc.Inventors: Charles G. Carter, David L. Lee, William J. Michaely, Gary W. Kraatz
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Patent number: 4940812Abstract: Process for the introduction of functional or functionalizable substituents para to the amino group in 2-aminophenols and 3-aminophenols. The process proceeds in one step, with substitution occurring selectively at the position para to the amino group. Consequently, the reaction is surprisingly straightforward, with very little or no contamination by isomeric by-products. The process comprises reaction of (a) an aminophenol having an open para position to the amino function, with (b) an unhindered non-enolizble aldehyde, and (c) a thiol or sulfinic acid which acts as a nucleophile. In preferred embodiments, the process is conducted at a temperature of from about 50.degree. C. to about 100.degree. C., and in the presence of a polar solvent. The reaction is promoted by an acid having sufficient acidity to protonate the amino group of the aminophenol. Preferably, the acid promoter is a mineral acid, and it is present in an amount at least substantially equivalent to the amount of aminophenol reactant.Type: GrantFiled: July 17, 1989Date of Patent: July 10, 1990Assignee: Eastman Kodak CompanyInventors: Philip T. S. Lau, Danny R. Thompson
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Patent number: 4939133Abstract: The present invention relates to novel N-substituted 2-hydroxybenzamide and N-substituted 2-hydroxy-.alpha.-oxo-benezene acetamide compounds pharmaceutical compositions, and methods of use for therefore for the treatment of diseases in which products having lipoxygenase enzyme activity contribute to the pathological condition. Selected novel intermediates are also the present invention.Type: GrantFiled: October 1, 1985Date of Patent: July 3, 1990Assignee: Warner-Lambert CompanyInventors: David T. Connor, Daniel L. Flynn, Wiaczeslaw A. Cetenko, Jagadish C. Sircar, Charles F. Schwender, Elizabeth A. Johnson, Roderick J. Sorenson, Paul C. Unangst
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Patent number: 4935240Abstract: A benzoylaminophenoxybutanoic acid derivative of general formula: ##STR1## [wherein A represents oxygen atom, sulfur atom or sulfinyl (SO) group,R.sup.1 represents hydrogen atom or methyl group,R.sup.2 represents a group of the general formula: ##STR2## {wherein B represents oxygen atom, sulfur atom or a group of general formula: NR" (wherein R" represents hydrogen atom or alkyl group of from 1 to 4 carbon atoms(s)), R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 represent, independently, hydrogen atom, alkyl group of from 1 to 4 carbon atom(s), halogen atom or trifluoromethyl group,m represents 0 or 1,n represents an integer of from 1 to 4, andR.sup.9 and R.sup.10 represent, independently, hydrogen atom, alkyl group of from 1 to 5 carbon atom(s) or a group of general formula: ##STR3## (wherein R.sup.12, R.sup.13, R.sup.14 and R.sup.15 represent, independently, hydrogen atom, alkyl group of from 1 to 4 carbon atom(s), halogen atom or trifluoromethyl group, and 1 represents an integer of from 1 to 4.Type: GrantFiled: May 6, 1988Date of Patent: June 19, 1990Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Hiroshi Terashima, Yoshinobu Arai
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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: 4931465Abstract: Fungicidally active novel benzaldoxime carbamate derivatives of the formula ##STR1## in which X represents hydrogen or halogen,Y represents halogen or alkyl,Z represents hydrogen, halogen, alkyl, alkoxy or halogenoalkyl, andR represents alkyl, halogenoalkyl, cyanoalkyl, and also phenyl or phenylalkyl, both of which are optionally monosubstituted to polysubstituted by identical or different substituents, or represents tosyl, or cycloalkyl which is optionally monosubstituted to polysubstituted by identical or different substituents,with the exception of those compounds in which X represents 2-chloro, Y represents 6-chloro and Z represents 4-methyl. Many of the benzaldoxime intermediates therefor are also new.Type: GrantFiled: March 8, 1988Date of Patent: June 5, 1990Assignee: Bayer AktiengesellschaftInventors: Christa Fest, Wilhelm Brandes, Stefan Dutzmann, Gerd Hanssler, Karl-Heinz Kuck
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Patent number: 4929736Abstract: Certain amino-acid derivatives are disclosed as effective inhibitors of human leukocyte elastase and therefore useful in preventing the imbalance of this proteolytic enzyme in vivo. The compounds specifically are derivatives L-valine, L-norvaline, L-norleucine, and L-methionine methyl ester azolides succinimides or pyridones and sulfonate salts, and related compounds such as L-leucine and L-phenylalanine methyl ester derivatives. The compounds were found to be excellent inhibitors in that they embody both inhibitory and anti-oxidant or anti-inflammatory activity.Type: GrantFiled: November 6, 1987Date of Patent: May 29, 1990Assignee: Board of Trustees of the Wichita State UniversityInventor: William C. Groutas
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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: 4912221Abstract: The instant invention relates to optically pure, L-(S)forms of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid compounds and their method of preparation from optionally pure L-phenylalanine precursor compounds and their preparation utilizing novel in situ cationic catalyst systems.Type: GrantFiled: October 27, 1988Date of Patent: March 27, 1990Assignee: Occidental Chemical CorporationInventors: Neil J. O'Reilly, Henry C. Lin
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Patent number: 4910327Abstract: There are provided novel alkyl esters of substituted 2-methyl-3-quinolinecarboxylic acid and quinoline-2,3-dicarboxylic acid; novel dialkyl 3-(substituted)phenylaminobut-2-ene-dioates, useful as intermediates for the preparation of highly effective 2-(2-imidazolin-2-yl)quinoline herbicidal agents and methods for the preparation thereof.Type: GrantFiled: March 27, 1989Date of Patent: March 20, 1990Assignee: American Cyanamid CompanyInventor: Robert F. Doehner, Jr.
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Patent number: 4908475Abstract: New compounds which have potent V.sub.2 -vasopressin antagonistic activity are prepared by a 1,6-cyclization using peptide bond formation. The structures of the compounds are characterized by a Pas.sup.1,6 or Tas.sup.1,6 cyclized unit. Also a chiral synthesis of the optically pure Pas intermediates is described.Type: GrantFiled: May 9, 1988Date of Patent: March 13, 1990Assignee: SmithKline Beckman CorporationInventors: James F. Callahan, William F. Huffman, Kenneth A. Newlander, Nelson C. F. Yim
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Patent number: 4908467Abstract: N-Phenylsulfonyl-B'-pyrimidinyl- and -triazinylureas of the formula I ##STR1## wherein A is 3,3,3-trifluoropropyl or 3,3-difluorobutyl,R.sup.1 is hydrogen, halogen, nitro, cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkylsulfinyl, C.sub.1 -C.sub.4 -alkylsulfonyl, --CO--R.sup.6, --NR.sup.7 R.sup.8, --CO--NR.sup.9 R.sup.10 or --SO.sub.2 --NR.sup.11 R.sup.12,R.sup.2 is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkylsulfinyl or C.sub.1 -C.sub.4 -alkylsulfonyl,R.sup.3 and R.sup.4 independently of one another are each hydrogen, halogen C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.2 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, C.sub.2 -C.sub.4 -alkoxyalkyl, C.sub.1 -C.sub.4 -alkoxy or --NR.sup.12 R.sup.13,R.sup.5 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy,R.sup.6 is C.sub.1 -C.Type: GrantFiled: April 8, 1988Date of Patent: March 13, 1990Assignee: Ciba-Geigy CorporationInventors: Willy Meyer, Konrad Oertle
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Patent number: 4906666Abstract: The present invention provides compounds of the general formula: ##STR1## wherein Ar is a phenyl radical optionally substituted by alkyl, alkenyl, alkoxy, alkylthio, alkanoyl, hydroxyl, hydroxyalkyl, carboxyl, alkoxycarbonyl, carbamoyl, nitro, amino or halogen, A is a straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.8 aliphatic hydrocarbon radical which is optionally substituted by a hydroxyl group, n is 0, 1 or 2, B is a straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.8 -aliphatic hydrocarbon radical and R is 5-(1H)-tetrazolyl, --CO--NH-tetrazolyl, ##STR2## CN, SCN, OH, halogen, 5-(1H)-tetrazolylthio, ##STR3## or CO--O--NH--R.sub.1, wherein R.sub.Type: GrantFiled: February 5, 1987Date of Patent: March 6, 1990Assignee: Boehringer Mannheim GmbHInventors: Erhard Reinholz, Walter-Gunar Friebe, Wolfgang Kampe, Jurgen Mertin, Otto-Henning Wilhelms
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Patent number: 4904819Abstract: Bicyclic sulfonamide derivatives represented by the formula: ##STR1## (wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 is lower alkyl, aralkyl, or aryl which may be substituted by lower alkyl, alkoxy, acetoxy, hydroxy, halogen, nitro or phenyl; and the wavy line indicates R or S configuration or their mixture) or their salt being used as antithrombotic, antivasoconstricting, and antibronchoconstricting drugs and the process therefor.Type: GrantFiled: April 28, 1988Date of Patent: February 27, 1990Assignee: Shionogi & Co., Ltd.Inventors: Sanji Hagishita, Kaoru Seno
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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: 4898877Abstract: Novel circulation-active cyclohexenecarboxylates of the formula ##STR1## in which R.sup.1 is an organic radical,R.sup.2 is an optionally substituted aryl radical,R.sup.3 is an optionally substituted alkyl or aryl radical,X and Y are --CN, --COR.sup.4, --SO.sub.2 R.sup.4, --COOR.sup.5, --CONR.sup.6 R.sup.7 or --SO.sub.2 NR.sup.6 R.sup.7, andR.sup.4, R.sup.5, R.sup.6 and R.sup.7 are various organic radicals.Type: GrantFiled: February 18, 1988Date of Patent: February 6, 1990Assignee: Bayer AktiengesellschaftInventors: Horst Meyer, Eckhard Schwenner, Martin Bechem, Rainer Gross, Matthias Schramm, Michael Kayser, Siegbert Hebisch
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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: 4885027Abstract: Arylmethylenesulfonamidoacetamide and thioacetamide derivatives and arylmethylenesulfonamidoester intermediates therefor. The compounds are useful as selective herbicides especially with respect to the prevention and elimination of barnyardgrass in grass crops, especially in rice crops.Type: GrantFiled: November 14, 1986Date of Patent: December 5, 1989Assignee: Chevron Research CompanyInventor: Patricia B. Pomidor
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Patent number: 4874846Abstract: Process for the preparation of aryloxy-benzoic acids containing a sulphonamide group by the direct reaction of a phenoxy-benzoic acid with a sulphonamide, in the presence of a halogenating agent such as P(O)Cl.sub.3.Type: GrantFiled: May 26, 1987Date of Patent: October 17, 1989Assignee: Rhone-Poulenc Agrochimie S.A.Inventor: Alain Chene
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Patent number: 4872902Abstract: The invention relates to the novel cyclohexanediones of formula I ##STR1## in which R is hydrogen or C.sub.1 -C.sub.6 -alkyl,A is R.sub.2, OR.sub.3 or NR.sub.3 R.sub.4,R.sub.2 is C.sub.1 -C.sub.6 -alkyl that is unsubstituted or is mono-substituted by C.sub.1 -C.sub.4 -alkoxy or mono- or poly-substituted by halogen, or is C.sub.3 -C.sub.6 -cycloalkyl,R.sub.3 is C.sub.1 -C.sub.6 -alkyl or C.sub.3 -C.sub.6 -cycloalkyl, or is phenyl or benzyl each of which is unsubstituted or is mono-, di- or tri-substituted by R.sub.5,R.sub.4 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.3 -C.sub.6 -cycloalkyl,R.sub.3 and R.sub.4 are, in addition, together with the nitrogen atom to which they are bonded, a pyrrolidine, morpholine or piperidine radical,B is one of the radicals ##STR2## m is 0, 1, 2 or 3, R.sub.5 is halogen, nitro, cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkylsulphinyl or C.sub.1 -C.sub.Type: GrantFiled: February 8, 1988Date of Patent: October 10, 1989Assignee: Ciba-Geigy CorporationInventor: Hans-Georg Brunner
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Patent number: 4871756Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4, E.sub.4 and the slow reacting substance of anaphylaxis.As such, these compounds will be useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: February 17, 1987Date of Patent: October 3, 1989Assignee: Merck Frosst Canada, Inc.Inventors: John Gillard, Joshua Rokach, Patrice C. Belanger
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Patent number: 4869748Abstract: Herbicidal compounds of the formula ##STR1## wherein R is halogen; C.sub.1 -C.sub.2 alkyl; C.sub.1 -C.sub.2 alkoxy; trifluoromethoxy; difluoromethoxy; nitro; cyano; C.sub.1 -C.sub.2 haloalkyl; R.sup.a SO.sub.n - wherein n is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl, trifluoromethyl or difluoromethyl;R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; andR.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.Type: GrantFiled: December 2, 1988Date of Patent: September 26, 1989Assignee: ICI Americas Inc.Inventor: Christopher G. Knudsen
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Patent number: 4866196Abstract: Novel phenoxyacetic acid of the formula: ##STR1## wherein Ring A is phenylene group or a phenylene group having 1 to 2 substituent(s) selected from a lower alkyl group, a lower alkoxy group and a halogen atom; either one or two group(s) of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are a lower alkyl group, and the other groups are hydrogen atom; R.sup.5 is phenyl group or a phenyl group having 1 to 3 substituent(s) selected from a lower alkyl group, a halogen atom a lower alkoxy group and nitro group; and --COOR.sup.6 is carboxyl group or a protected carboxyl group, or a salt thereof are disclosed. Said derivative (I) and a salt thereof have a potent platelet aggregration-inhibiting activity.Type: GrantFiled: January 4, 1988Date of Patent: September 12, 1989Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takeo Iwakuma, Takayuki Kawaguchi, Toyoharu Yamashita, Yasuhiko Sasaki, Tamotu Shimazaki
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Patent number: 4861913Abstract: Bicyclic sulfonamido derivatives represented by the formula: ##STR1## wherein R.sub.1 is a hydrogen or lower alkyl; R.sub.2 is an alkyl, substituted or unsubstituted aryl, aralkyl or heterocycle; R.sub.3 is a hydrogen or methyl; X is an alkylene or alkenylene which may be substituted by a fluorine atom or atoms an may contain an oxygen, sulfur and/or phenylene in the chain; Y is straight or branched alkylene or alkenylene, oxygen, or sulfur; m is 0 or 1; and n is 0, 1 or 2, or their salt, said derivatives being useful as antithrombotic, anti-vasoconstricting, and anti-bronchoconstricting drugs.Type: GrantFiled: November 5, 1986Date of Patent: August 29, 1989Assignee: Shionogi & Co., Ltd.Inventors: Masayuki Narisada, Mitsuaki Ohtani, Fumihiko Watanabe, Sanji Hagishita, Kaoru Seno, Susumu Kamata, Nobuhiro Haga, Tatsuo Tsuri, Tadahiko Tsushima, Kenji Kawada
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Patent number: 4853398Abstract: This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.Type: GrantFiled: April 13, 1987Date of Patent: August 1, 1989Assignee: Eli Lilly and CompanyInventors: F. P. Carr, Robert D. Dillard, Doris E. McCullough
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Patent number: 4853028Abstract: Compounds of the formula ##STR1## wherein R is halogen, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, cyano, nitro, (S(O).sub.n R wherein R is C.sub.1 -C.sub.4 alkyl and n is the integer 0, 1 or 2; and R.sup.2 through R.sup.8 are hydrogen or certain substituents, their salts, herbicidal compositions containing the compound or salts and the herbicidal use thereof.Type: GrantFiled: December 4, 1987Date of Patent: August 1, 1989Assignee: Stauffer Chemical CompanyInventors: Charles G. Carter, David L. Lee, William J. Michaely
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Patent number: 4853403Abstract: A 3-phenylthiomethylstyrene derivative having the general formula (1): ##STR1## or salt thereof with a base, when X is hydroxyl group, R.sup.1 is hydrogen atom or R.sup.2 is hydrogen atom, a process for preparing the 3-phenylthiomethylstyrene derivative (1), and an antiallergic agent and a tyrosinekinase inhibiting agent containing the 3-phenylthiomethylstyrene derivative (1) as an effective component. The compound (1) of the present invention is a useful intermediate for preparing various organic compounds, and has excellent antiallergic and tyrosinekinase inhibiting activities.Type: GrantFiled: July 28, 1986Date of Patent: August 1, 1989Assignee: Kanegafuchi Kagaku Kogyo Kabushiki KaishaInventors: Tadayoshi Shiraishi, Naohiro Imai, Takeshi Domoto, Keiji Kameyama, Ikuo Katsumi, Takayoshi Hidaka, Kazunori Hosoe, Kiyoshi Watanabe
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Patent number: 4849563Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 s an alkyl of 1-6 carbon atoms, benzyl, phenyl, or phenyl substituted by halogen, alkoxy of 1 to 4 carbon atoms, alkyl of 1 to 4 carbon atoms, amino, or carbonyl substituents, or --RN(R').sub.2 wherein R and R' are each independently an alkyl of 1 to 4 carbon atoms; R.sub.2 is an aromatic substituent selected from the group consisting of phenyl, benzyl, and naphthyl, and A is an aromatic substitution selected from the group consisting of hydrogen, alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, halogen, --NO.sub.2, --NH.sub.2, --COOH, and --NHCOCH.sub.3. The compounds have been found to be alkylating agents having antineoplastic activity for use in inhibiting the growth of tumors.Type: GrantFiled: December 28, 1987Date of Patent: July 18, 1989Assignee: Yale UniversityInventors: Alan C. Sartorelli, Krishnamurthy Shyam, Robert T. Hrubiec
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Patent number: 4839357Abstract: Peptides of the formula: ##STR1## which comprise novel elements replacing the Phe(8)-His(9) sequence in renin-inhibitory peptides based on substrate analogy, which inhibit the substrate-cleaving action of renin and have improved bioavailability; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension or congestive heart failure or of establishing renin as a causative factor in these problems which employ the novel peptides.Type: GrantFiled: October 2, 1987Date of Patent: June 13, 1989Assignee: Merck & Co., Inc.Inventors: Arthur A. Patchett, William J. Greenlee, William H. Parsons, Prasun K. Chakravarty
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Patent number: 4837352Abstract: An intermediate compound having the structural formula ##STR1## wherein R is 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.n - wherein n is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl; R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; or R.sup.1 and R.sup.2 together are alkylene having 2 to 5 carbon atoms; R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; or R.sup.3 and R.sup.4 together can be oxo; R.sup.5 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.6 is hydrogen or C.sub.1 -C.sub.4 alkyl; or R.sup.5 and R.sup.6 together are alkylene having 2 to 5 carbon atoms; R.sup.7 and R.sup.8 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.Type: GrantFiled: March 21, 1988Date of Patent: June 6, 1989Assignee: Stauffer Chemical CompanyInventor: Christopher G. Knudsen
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Patent number: 4822906Abstract: Intermediate compounds of the structural formula ##STR1## wherein R.sup.60 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.n -- wherein n is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl, trifluoromethyl or difluoromethyl; or trifluoromethoxy or difluoromethoxy; R.sup.61 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.62 is hydrogen or C.sub.1 -C.sub.4 alkyl; or R.sup.61 and R.sup.62 together are C.sub.2 -C.sub.5 alkylene; R.sup.63 C.sub.1 -C.sub.4 alkyl; R.sup.64 is C.sub.1 -C.sub.4 alkyl; or R.sup.63 R.sup.64 together are C.sub.2 -C.sub.5 alkylene; R.sup.65 and R.sup.66 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.Type: GrantFiled: December 4, 1987Date of Patent: April 18, 1989Assignee: Stauffer Chemical CompanyInventor: Charles G. Carter
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Patent number: 4816066Abstract: Compounds of the formula ##STR1## wherein R is halogen, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl, cyano, nitro, S(O).sub.n R wherein R is C.sub.1 -C.sub.4 alkyl and n is the integer 0, 1 or 2; and R.sup.2 through R.sup.8 are hydrogen or certain substituents, their salts, herbicidal compositions containing the compound or salts and the herbicidal use thereof.Type: GrantFiled: December 4, 1987Date of Patent: March 28, 1989Assignee: Stauffer Chemical CompanyInventors: William J. Michaely, Gary W. Kraatz
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Patent number: 4816598Abstract: The invention relates to 4-amino-butanoic acid derivatives of general formula: ##STR1## in which: M represents an alkali metal atom,R represents a protected amino group,R.sub.1 represents a labile group,R.sub.2 represents hydrogen, a branched- or straight-chain alkyl radical having from 1 to 6 carbon atoms, a lower methyloxyalkyl, a lower methylthioalkyl, a lower (lower alkyl)-aminoalkyl, a lower di-(lower alkyl)-aminoalkyl or a lower hydroxyalkyl radical or R.sub.2 represents one of the radicals of general formulae:Cy--A--, Cy--O--A'--, R--A'-- or R.sub.Type: GrantFiled: June 16, 1987Date of Patent: March 28, 1989Assignee: SanofiInventors: Marcel Descamps, Walter Verstraeten
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Patent number: 4814485Abstract: The invention relates to new (4S)-4-aminobutanoic acid derivatives of general formula: ##STR1## in which: R represents an N-protective group,R.sub.1 represents hydrogen, an alkali metal atom such as lithium, sodium or potassium or a liabile group,R.sub.2 represents a group of formula: ##STR2## in which W represents hydrogen, a hydroxy group or an alkyl radical containing from 1 to 4 carbon atoms or an alkoxy radical containing from 1 to 4 carbon atoms, and to a process for the preparation of the said derivatives.The 4-aminobutanoic acid derivatives according to the invention are useful as synthesis intermediates for the preparation of peptides derived from statin analogues.Type: GrantFiled: December 2, 1986Date of Patent: March 21, 1989Assignee: SanofiInventors: Marcel Descamps, Dino Nisato, Walter Verstraeten
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Patent number: 4808338Abstract: Intermediate compounds of the formula ##STR1## wherein X is oxy, thio, sulfinyl or sulfonyl; R is halogen; C.sub.1 C.sub.2 alkyl; C.sub.1 -C.sub.2 alkoxy; trifluoromethoxy; difluoromethoxy; nitro; cyano; C.sub.1 -C.sub.2 haloalkyl; R.sup.a SO.sub.n -- wherein n is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl; trifluoromethyl or difluoromethyl; R.sup.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, or phenyl; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; or R.sup.1 and R.sup.2 together are C.sub.2 -C.sub.5 alkylene; R.sup.3 hydrogen, C.sub.1 C.sub.4 alkyl, or phenyl with the proviso that R.sup.1 and R.sup.3 are not both phenyl; R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.5 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.6 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, or phenyl; R.sup.7 and R.sup.8 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.Type: GrantFiled: February 1, 1988Date of Patent: February 28, 1989Assignee: Stauffer Chemical CompanyInventor: David L. Lee
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Patent number: 4804483Abstract: The present application relates to cationic block polyesters useful as soil release 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: January 13, 1988Date of Patent: February 14, 1989Assignee: GAF CorporationInventors: Anthony J. O'Lenick, Jr., Joseph J. Fanelli