Nitro Or Nitroso In Substituent Q Patents (Class 564/87)
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Patent number: 5777168Abstract: This invention relates to a process for producing N-alkyl-dinitroalkylaniline and particularly N-sec-butyl-4-tert-butyl-2,6-dinitroaniline by methylation of an alkylphenol followed by a one or two stage dinitration of the resulting alkylanisole which is followed by reaction with an amine.Type: GrantFiled: June 3, 1997Date of Patent: July 7, 1998Assignee: SRM Chemical, Ltd. Co.Inventors: Stefan Kwiatkowski, Krzysztof Pupek, Brenda L. Lawrence, Lowell J. Lawrence
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Patent number: 5760064Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 6, 1997Date of Patent: June 2, 1998Assignee: G.D. SearleInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5734081Abstract: Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N,R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.Type: GrantFiled: June 1, 1995Date of Patent: March 31, 1998Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Edward Faith Elslager, Rocco Dean Gogliotti
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Patent number: 5705528Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein thyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: ##STR1## wherein R.sup.1 represents farnesyl, geranyl or geranyl-geranyl;Z represents C--R.sup.6 or N;R.sup.2 represents H, CN, the groups COOR.sup.7, SO.sub.3 R.sup.7, CONR.sup.7 R.sup.8 and SO.sub.2 NR.sup.7 R.sup.7, wherein R.sup.7 and R.sup.8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO.sub.3 M, wherein M is a cation;R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato;X represents O, S, SO, SO.sub.2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.Type: GrantFiled: November 10, 1994Date of Patent: January 6, 1998Assignee: Ramot University Authority for Applied Research & Industrial DevelopmentInventor: Yoel Kloog
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Patent number: 5689006Abstract: This invention relates to a process for producing N-alkyl-dinitroalkylaniline and particularly N-sec-butyl-4-tert-butyl-2,6-dinitroaniline by methylation of an alkylphenol followed by nitration of the resulting alkylanisole which is followed by reaction with an amine.Type: GrantFiled: June 29, 1995Date of Patent: November 18, 1997Assignee: SRM Chemical, Ltd. Co.Inventors: Stefan Kwiatkowski, Krzysztof Pupek, Brenda L. Lawrence, Lowell J. Lawrence
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Patent number: 5668291Abstract: Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N, R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.Type: GrantFiled: June 7, 1995Date of Patent: September 16, 1997Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Edward Faith Elslager, Rocco Dean Gogliotti
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Patent number: 5668178Abstract: Phenylthiols and dithiobisbenzamides are potent antibacterial and antiviral agents.Type: GrantFiled: May 19, 1995Date of Patent: September 16, 1997Assignee: Warner-Lambert CompanyInventors: Edward Faith Elslager, Rocco Dean Gogliotti
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Patent number: 5663441Abstract: This invention relates to a process for producing mono- and di- N-alkyl-dinitroalkylaniline or dinitroaniline derivative and particularly N-sec-butyl-4-tert-butyl-2,6-dinitroaniline by methylation of an alkylphenol or phenol derivative followed by nitration of the resulting acetic acid alkylanisole or anisole derivative which is followed by reaction with an amine. Acetic acid by-product produced during nitration is recycled by converting back to acetic anhydride.Type: GrantFiled: March 22, 1996Date of Patent: September 2, 1997Assignee: SRM Chemical, Ltd. Co.Inventors: Stefan Kwiatkowski, Krzysztof Pupek, Brenda L. Lawrence, Lowell J. Lawrence
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Patent number: 5650533Abstract: The invention relates to 4-substituted isoxazole derivatives of formula I: ##STR1## wherein R, R.sup.1, R.sup.2, Q and n have the meaning defined in the description which possess valuable herbicidal properties.Type: GrantFiled: June 2, 1995Date of Patent: July 22, 1997Assignee: Rhone-Poulenc Agriculture Ltd.Inventors: David Alan Roberts, Susan Mary Cramp, Derek Ian Wallis, Jean-Paul Bulot
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Patent number: 5639769Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: January 17, 1996Date of Patent: June 17, 1997Assignee: G.D. Searle and Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5616797Abstract: An electrophotographic toner having polymeric binder and a charge control agent selected from the group consisting of sulfonamides having the general structure: ##STR1## and metal salts thereof. T.sup.1 is independently selected from H, alkyl having from 1 to 20 carbons, cycloalkyl having from 3 to 18 carbons, and aromatic and heteroaromatic ring systems having a solitary ring or 2 to 3 linked or fused rings. R.sup.1 is O, S, N--H, N--R.sup.5, or N--L--R.sup.5 ; where L is a linking group selected from: ##STR2## and R.sup.5 is independently selected from alkyl having from 1 to 20 carbons, cycloalkyl having from 3 to 18 carbons, and aromatic and heteroaromatic ring systems having a solitary ring or 2 to 3 linked or fused rings. L.sup.1 and L.sup.2 are each independently a direct link or divalent alkyl or fluoroalkyl having from 1 to 20 carbons. R.sup.a and R.sup.Type: GrantFiled: December 9, 1994Date of Patent: April 1, 1997Assignee: Eastman Kodak CompanyInventors: John C. Wilson, Peter S. Alexandrovich, Steven M. Bonser
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Patent number: 5610320Abstract: Sulfonamide compounds of the formula or pharmacologically acceptable salts thereof: ##STR1## wherein: R.sup.1 is a hydrogen atom, halogen atom, lower alkyl group, lower alkoxy group, hydroxyl group, nitro group, phenoxy group, cyano group, acetyl group, amino group or a protected amino group; R.sup.2 and R.sup.3 may be the same or different from each other and each is a hydrogen atom, halogen atom, lower alkyl group or lower alkoxy group; R.sup.4 and R.sup.7 may be the same or different from each other and each is a hydrogen atom or a lower alkyl group; R.sup.5 and R.sup.6 may be the same or different from each other and each is a hydrogen atom, halogen atom, lower alkoxy group, amino group or amino group substituted with a lower alkyl or a phenyl group; A is .dbd.CH--; B is .dbd.CH--; and E is selected from the group consisting of ##STR2## in which Q is an oxygen atom or a sulfur atom; and R.sup.Type: GrantFiled: May 26, 1995Date of Patent: March 11, 1997Assignee: Eisai Co., Ltd.Inventors: Hiroshi Yoshino, Norihiro Ueda, Hirovuki Sugumi, Jun Niijima, Yoshihiko Kotake, Toshimi Okada, Nozomu Koyanagi, Tatsuo Watanabe, Makoto Asada, Kentaro Yoshimatsu, Atsumi Iijima, Takeshi Nagasu, Kappei Tsukahara, Kyosuke Kitoh
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Patent number: 5599982Abstract: Process for preparing enantiomerically pure imidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-thiones of formula ##STR1## starting from 2,6-dihalo-3-nitrobenzyl derivatives (II) and suitably N-protected 1,2-diaminopropanes (III) ##STR2## Novel enantiomerically pure intermediates of formula (III) and (IV) prepared in the course of the present process.Type: GrantFiled: March 30, 1995Date of Patent: February 4, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Alfons G. M. De Knaep, Luc J. R. Moens, Eduard J. C. Vreysen
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Patent number: 5543570Abstract: Process for preparing enantiomerically pure imidazo[4,5,1 -jk][1,4]benzodiazepin -2(1H)-thiones of formula ##STR1## starting from 2,6-dihalo-3-nitrobenzyl derivatives (II) and suitably N-protected 1,2-diaminopropanes (III) ##STR2## Novel enantiomerically pure intermediates of formula (III) and (IV) are prepared in the course of the present process.Type: GrantFiled: March 30, 1995Date of Patent: August 6, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Alfons G. M. De Knaep, Luc J. R. Moens, Eduard J. C. Vreysen
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Patent number: 5521219Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: August 24, 1993Date of Patent: May 28, 1996Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5510388Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 31, 1995Date of Patent: April 23, 1996Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5508294Abstract: Sulfonamide-containing hydroxethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 31, 1995Date of Patent: April 16, 1996Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5463122Abstract: Antibacterial and antiviral phenylthiols and dithiobisbenzamides have the formula ##STR1## where n is 1 or 2, Y is hydrogen when n is 1, and a single bond when n is 2; and R.sup.1 and R.sup.11 are substituent groups, R.sup.4 is hydrogen or alkyl, and Z is hydrogen, alkyl, cycloalkyl or sulfamoylphenyl.Type: GrantFiled: August 5, 1994Date of Patent: October 31, 1995Assignee: Warner-Lambert CompanyInventors: Edward F. Elslager, Rocco D. Gogliotti
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Patent number: 5457237Abstract: Certain dihydroxyindanone compounds, and their pharmaceutically-acceptable salts, are inhibitors of tyrosine kinase enzymes, and so are useful for the control of tyrosine kinase dependent diseases (e.g., cancer, atherosclerosis).Type: GrantFiled: November 23, 1993Date of Patent: October 10, 1995Assignee: Pfizer Inc.Inventor: Robert L. Dow
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Patent number: 5451677Abstract: Substituted phenylsulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted alkyl epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.Type: GrantFiled: December 15, 1993Date of Patent: September 19, 1995Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, Robert J. Mathvink, Hyun O. Ok, Emma R. Parmee, Ann E. Weber
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Patent number: 5405988Abstract: The invention relates to 9-substituted bicyclo[3.3.0]octane derivatives of formula I, ##STR1## and their salts with physiologically compatible bases, as well as the .alpha.-, .beta.- or .gamma.-cyclodextrin clathrates, as well as the compounds of formula I encapsulated with liposomes, process for their production and their pharmaceutical use.Type: GrantFiled: June 11, 1993Date of Patent: April 11, 1995Assignee: Schering AktiengesellschaftInventors: Ulrich Klar, Helmut Vorbruggen, Hartmut Rehwinkel, Karl Thierauch, Peter Verhallen
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Patent number: 5221750Abstract: 2-aryl-4-isoxazolin-3-1-derivatives of formula (I), useful as intermediates for positive working compounds in silver halide photographic materials ##STR1## wherein R.sup.1 represents a substituted or unsubstituted alkyl having from 1 to 6 carbon atoms or a substituted or unsubstituted aryl having from 6 to 24 carbon atoms; and R.sup.2, R.sup.3, and R.sup.4, are the same or different, each having up to 20 carbon atoms and each represents hydrogen, a substituted or unsubstituted alkoxy, a substituted or unsubstituted aryloxy, a substituted or unsubstituted acyl, a substituted or unsubstituted alkoxycarbonyl, a substituted or unsubstituted aryloxycarbonyl, halogen, nitro, a substituted or unsubstituted carbamoyl, a substituted or unsubstituted sulfamoyl, a substituted or unsubstituted sulfonyl, cyano, or trifluoromethyl, with the proviso that at least one of said R.sup.2 and R.sup.3 is cyano, a substituted or unsubstituted sulfonyl, trifluoromethyl, or nitro.Type: GrantFiled: January 13, 1992Date of Patent: June 22, 1993Assignee: Fuji Photo Film Co., Ltd.Inventors: Koki Nakamura, Shigeru Nakamura
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Patent number: 5189211Abstract: A sulfonamide derivative represented by the Formula: ##STR1## wherein A, B, X, Y, R, m and n are as defined in the specification, and a salt thereof have thromboxane A.sub.2 antagonism, therefore they are useful, for example, as blood platelet aggregation inhibiting agents.Type: GrantFiled: July 26, 1991Date of Patent: February 23, 1993Assignees: Taisho Pharmaceutical Co., Ltd., Nippon Suisan Kaisha, Ltd.Inventors: Masakazu Sato, Yutaka Kawashima, Jun Goto, Yoshiyuki Chiba, Mikio Satake, Chuzo Iwata, Takeshi Imanishi
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Patent number: 5152826Abstract: An herbicide compound of the 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; orR.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; orR.sup.3 and R.sup.4 together are 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; orR.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.4 alkyl; (b) C.sub.1 -C.sub.Type: GrantFiled: October 16, 1991Date of Patent: October 6, 1992Assignee: Imperial Chemical Industries PLCInventor: Christopher G. Knudsen
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Patent number: 5081284Abstract: A novel N-substituted peptidyl compound represented by the general formula (1): ##STR1## where R.sub.1 is a straight-chained or branched acyl group having 2-10 carbon atoms, a branched, cyclic or partly branched cyclic alkyloxycarbonyl group having 4-15 carbon atoms, a substituted or unsubstituted benzyloxycarbonyl group, a 2,2,2-trichloroethyloxycarbonyl group, a 2-(trimethylsilyl)ethyloxycarbonyl group, a p-toluensulfonyl group, an o-nitrophenylsulfenyl group, a diphenylphosphonothioyl group, a triphenylmethyl group, a 2-benzoyl-1-methylvinyl group or a 4-phenylbutyryl group; R.sub.2 is a hydrogen atom or when taken together with R.sub.1, may form a phthaloyl group; R.sub.3 is an isobutyl group, a n-butyl group or an isopropyl group; R.sub.4 is a butyl group, a benzyl group or a methylthioethyl group; and R.sub.5 is a hydrogen atom or a chloromethyl group, which inhibits the activity of cysteine proteinases.Type: GrantFiled: June 29, 1989Date of Patent: January 14, 1992Assignee: Suntory LimitedInventors: Naoki Higuchi, Masayuki Saitoh, Norio Iwasawa, Motoo Sumida, Hiroshi Shibata
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Patent number: 5061706Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is hydroxy, alkoxy, aryloxy, aralkyloxy, cycloalkylalkoxy, cycloalkoxy, or acyloxy; andR.sup.5, R.sup.6, R.sup.7 and R.sup.8 independently are hydrogen, NO.sub.2, halogen CN, SO.sub.2 NR'R', SO.sub.2 R', CF.sub.3, or OR', wherein R' is hydrogen or C.sub.1-4 -alkyl;The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.Type: GrantFiled: December 15, 1989Date of Patent: October 29, 1991Assignee: Novo Nordisk A/SInventors: Tage Honoree, Poul Jacobsen, Flemming E. Nielsen, Lars Nafrim
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Patent number: 5047420Abstract: Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.Type: GrantFiled: August 21, 1989Date of Patent: September 10, 1991Assignee: Merck & Co., Inc.Inventors: Donald W. Graham, Tesfaye Biftu, John C. Chabala, Michael N. Chang, Yuan-Ching P. Chiang, Kathryn L. Thompson, Shu S. Yang
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Patent number: 4971620Abstract: Disclosed herein is a sulfonamide compound represented by the formula (I): ##STR1## wherein A represents a phenyl group which may be substituted, B represents a phenyl group which may be substituted, R represents a lower alkyl group, a lower alkoxy group or a lower haloalkyl group, W represents a hydroxyl group or a halogen atom, and z represents a halogen atom, a lower alkysulfonyloxy group which may be substituted, or a phenylsulfonyloxy group which may be substituted, and a herbicidal composition containing the sulfonamide compound as an effective ingredient.Type: GrantFiled: January 27, 1989Date of Patent: November 20, 1990Assignee: Mitsubishi Kasei CorporationInventors: Tetsuo Jikihara, Manabu Katsurada, Toyohiko Shike, Osamu Ikeda, Hisao Watanabe, Tetsuo Takematsu, Koichi Yoneyama
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Patent number: 4954160Abstract: The invention provides compounds of the general formula ##STR1## wherein R represents a hydrogen atom, or an optionally substituted alkyl or acyl group, or an alkenyl or alkynyl group or an inorganic or organic cation;R.sup.1 represents an alkyl, haloalkyl, alkenyl, alkynyl or optionally substituted aralkyl or phenyl group;R.sup.2 represents an optionally substituted alkyl or phenalkyl group or a cycloalkyl, alkenyl, haloalkenyl or alkynyl group;each R.sup.3 represents an optionally substituted alkyl group;one of R.sup.4 or R.sup.5 represents a hydrogen atom or an alkyl group while the other of R.sup.4 and R.sup.5 represents an optionally substituted phenyl group; together with their use as herbicides and their preparation using novel intermediates.Type: GrantFiled: September 21, 1988Date of Patent: September 4, 1990Assignee: Shell Internationale Research Maatschappij, B.V.Inventors: Terence Gilkerson, Robert W. Shaw
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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: 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: 4939147Abstract: Compounds of the formula, ##STR1## in which one of R.sub.30 and R.sub.40 represents a substituted phenylalkyl group and the other of R.sub.30 and R.sub.40 represents hydrogen or halogen, and R.sub.50 and R.sub.60 each independently represent hydrogen or alkyl.The compounds of the invention are useful for the treatment or prophylaxis of renal failure or cardiovascular disease.Type: GrantFiled: August 2, 1989Date of Patent: July 3, 1990Assignee: Fisons plc.Inventors: John Dixon, Brian Springthorpe, Francis Ince
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Patent number: 4921524Abstract: The invention provides compounds of the general formula ##STR1## wherein R represents a hydrogen atom, or an optionally substituted alkyl or acyl group, or an alkenyl or alkynyl group or an inorganic or organic cation;R.sup.1 represents an alkyl, haloalkyl, alkenyl, alkynyl or phenyl group;R.sup.2 represents an optionally substituted alkyl or phenalkyl group or a cycloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl group;R.sup.3 represents a hydrogen atom or an alkyl group; andone of R.sub.4 and R.sup.5 represents a hydrogen atom or an alkyl group, while the other of R.sup.4 and R.sup.5 represents an optionally substituted phenyl group; together with their use as herbicides and their preparation using novel intermediates.Type: GrantFiled: April 14, 1988Date of Patent: May 1, 1990Assignee: Shell Internationale Research Maatschappij B.V.Inventors: Terence Gilkerson, Robert W. Shaw, David C. Jennens
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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: 4902787Abstract: A method of producing a UV lightfast disperse dyestuff comprising selecting a disperse dyestuff having predetermined chromophoric groups, selecting a photostabilizer compound, designing a hybrid disperse dye molecular structure which contains the chromophoric groups of the selected disperse dyestuff and also contains the molecular structural features of the selected photostabilizer compound, and synthesizing the thus designed hybrid disperse dyestuff molecule. Such a method produces a hybrid dye molecule which is a UV lightfast analog of a disperse dyestuff having predetermined chromophoric groups, said hybrid dye molecule containing in its molecular structure the chromophoric groups of the selected disperse dyestuff and also containing the molecular structural features of a photostabilizer compound.Type: GrantFiled: April 21, 1988Date of Patent: February 20, 1990Assignee: North Carolina State UniversityInventor: Harold S. Freeman
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Patent number: 4897423Abstract: A compound of the formula: ##STR1## wherein: n is an integer 2,3,4, or 5; R.sub.1 is hydrogen or an alkyl group; andR.sub.2 and R.sub.3 are defined as follows:R.sub.2 is hydrogen or an alkyl group;R.sub.3 is hydrogen or an alkyl group; orR.sub.2 and R.sub.3 together form a heterocyclic ring, e.g. piperidine, pyrrolidine.The compounds have high radiosensitizing activity, and act as agents toxic to hypoxic cells in the absence of radiation.Type: GrantFiled: August 2, 1988Date of Patent: January 30, 1990Assignee: Merck & Co. Inc.Inventors: Walfred S. Saari, Edward L. Engelhardt
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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: 4883914Abstract: There are provided novel benzenesulfonyl carboxamide compounds and novel intermediate benzenesulfonyl-2-imidazolin-5-one compounds, novel intermediates and methods for the preparation of said compounds, and a method for controlling a variety of annual and perennial plant species utilizing novel benzenesulfonyl carboxamide compounds and novel intermediate benzenesulfonyl 2-imidazolin-5-one compounds.Type: GrantFiled: July 7, 1988Date of Patent: November 28, 1989Assignee: American Cyanamid CompanyInventors: Sergio I. Alvarado, Alvin D. Crews, Jr., Peter J. Wepplo, Robert F. Doehner, Jr., Thomas E. Brady, David M. Gange, Desiree L. Little
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Patent number: 4880821Abstract: A compound of the formula ##STR1## wherein: R.sub.1 and R.sub.2 are defined as follows:R.sub.1 is hydrogen, an alkyl group, or an alkyl group having one or more hydroxy groups;R.sub.2 is an alkyl group having one or more hydroxy groups, or an alkyl group containing an amino group in which the amino function is substituted with hydrogen or one or two individual alkyl groups same or different, or two alkyl groups which together form a cyclic amine, e.g. piperidine;R.sub.3 is hydrogen or an alkyl group; andR.sub.4 is hydrogen or an alkyl group.The compounds have high radiosensitizing activity and selectivity for hypoxic cells.Type: GrantFiled: August 17, 1988Date of Patent: November 14, 1989Assignee: Merck & Co., Inc.Inventor: Walfred S. Saari
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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: 4853415Abstract: 2-(Substituted sulfamyl) derivatives of 4-nitrobenzamide are disclosed as agents that increase the sensitivity of hypoxic cancer cells to x-rays and .gamma.-radiation. Methods of preparing such compounds, protocols for administering them to human patients and animals, and pharmaceutical compositions containing them are also disclosed.Type: GrantFiled: December 5, 1988Date of Patent: August 1, 1989Assignee: Merck & Co., Inc.Inventors: Edward L. Engelhardt, Walfred S. Saari
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Patent number: 4851575Abstract: Process for the preparation of 2-nitro-4-sulfamyldiphenylamine dyestuffs of the formula (1) ##STR1## in which R.sub.1 and R.sub.2 each denote a hydrogen, chlorine or bromine atom or a C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy group or a phenoxy group which can be substituted on the benzene nucleus by chlorine or bromine atoms or C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or trifluoromethyl groups, or denote a naphthoxy group, and R.sub.2 can also be an -N-(C.sub.1 -C.sub.4 -alkyl).sub.2, -NH-(C.sub.1 -C.sub.4 -alkyl), -NH-(C.sub.1 -C.sub.4 -alkanoyl) or -NH-benzoyl group, and R.sub.3 and R.sub.4 each denote a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.2 -alkoxy-C.sub.1 -C.sub.4 -alkyl or C.sub.5 -C.sub.6 -cycloalkyl group, and R.sub.4 can also be a phenyl group which can be substituted by chlorine or bromine atoms or C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, -N-(C.sub.1 -C.sub.4 -alkyl).sub.2, -NH-(C.sub.1 -C.sub.4 -alkyl), -NH-(C.sub.1 -C.sub.Type: GrantFiled: May 28, 1987Date of Patent: July 25, 1989Assignee: Hoechst AktiengesellschaftInventors: Werner Brodt, Theodor Papenfuhs
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Patent number: 4845284Abstract: This application discloses new substituted 3-nitrobenzensulfonamides which are useful in enhancing the effect of therapeutic radiation. It also discloses pharmaceutical composition of such compounds, and a method of treatment of patients by administering an effective amount of a substituted 3-nitrobenzenesulfonamide to a patient in need of radiation therapy.Type: GrantFiled: December 3, 1986Date of Patent: July 4, 1989Assignee: Merck & Co., Inc.Inventors: Edward L. Engelhardt, Walfred S. Saari
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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: 4837307Abstract: A 2,2'-bridged[1,1'-biphenyl]-3-ylmethyl compound of the following formula is an intermediate to insecticidal esters. ##STR1## wherein n is 1-4 and Y is a leaving group readily displaced by carboxylate anions.Type: GrantFiled: January 16, 1984Date of Patent: June 6, 1989Assignee: FMC CorporationInventor: Ernest L. Plummer
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Patent number: 4783213Abstract: 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, phenyl or substituted phenyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.1 and R.sup.2 together are C.sub.2 -C.sub.5 alkylene;R.sup.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or substituted phenyl with the proviso that R.sup.1 and R.sup.3 are not both phenyl or substituted 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.Type: GrantFiled: August 20, 1987Date of Patent: November 8, 1988Assignee: Stauffer Chemical CompanyInventor: David L. Lee
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Patent number: 4781751Abstract: 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, C.sub.1 -C.sub.4 alkyl, halogen, phenyl or substituted phenyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.1 and R.sup.2 together are C.sub.2 -C.sub.5 alkylene;R.sup.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or substituted phenyl, with the proviso that R.sup.1 and R.sup.3 are not both phenyl or substituted phenyl;R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.5 is hydrogen, halogen or C.sub.1 -C.sub.4 alkyl;R.sup.6 is halogen, cyano, nitro, trifluoromethyl, --C(O)--OR.sup.f wherein R.sup.f is C.sub.1 -C.sub.4 alkyl, or --C(O)NR.sub.2.sup.b wherein R.sup.b is hydrogen or C.sub.1 -C.sub.2 alkyl;R.sup.7 and R.sup.8 independently are (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.Type: GrantFiled: October 2, 1987Date of Patent: November 1, 1988Assignee: Stauffer Chemical CompanyInventor: Hsiao-Ling M. Chin
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Patent number: 4780127Abstract: 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 30, 1986Date of Patent: October 25, 1988Assignee: Stauffer Chemical CompanyInventors: William J. Michaely, Gary W. Kraatz
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Patent number: 4780569Abstract: 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.n - wherein n is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl;R.sup.1 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy;R.sup.2, R.sup.3, R.sup.4, 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.Type: GrantFiled: June 9, 1986Date of Patent: October 25, 1988Assignee: Stauffer Chemical CompanyInventor: David L. Lee
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Patent number: 4764433Abstract: An agent for the protection of material containing an N-sulphenylated benzenesulphonamide of the formula ##STR1## wherein R.sup.1, and R.sup.2 and R.sup.3 independently of one another represent hydrogen, halogen, nitro, alkyl or halogenoalkyl andR.sup.4 denotes an unsubstituted or substituted, saturated or unsaturated, aliphatic or cycloaliphatic radical, the aliphatic radicals being uninterrupted or heteroatoms or being interrupted by one or more hetero-atoms. The N-sulphenylated benzenesulphonamide-containing agents are useful for protecting industrial materials, for example, paints and timber, against attack by microorganisms, such as bacteria, fungi, yeasts, algae, slimes and viruses.Type: GrantFiled: August 15, 1986Date of Patent: August 16, 1988Assignee: Bayer AktiengesellschaftInventors: Engelbert Kuhle, Wilfried Paulus, Michael Fischler, Hans-Georg Schmitt