Nitrogen In Substituent Q Patents (Class 564/86)
  • Patent number: 5663414
    Abstract: A novel benzenesulfonamide derivative represented by the formula: ##STR1## has an inhibitory activity against phospholipase A.sub.2, so that it is effective in the treatment of diseases for which such an activity is efficacious.
    Type: Grant
    Filed: December 29, 1995
    Date of Patent: September 2, 1997
    Assignee: Eisai Co., Ltd.
    Inventors: Hitoshi Oinuma, Takashi Hasegawa, Tadanobu Takamura, Kenichi Nomoto, Yoshiharu Daiku, Toshihiko Naito, Sachiyuki Hamano
  • Patent number: 5650533
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: July 22, 1997
    Assignee: Rhone-Poulenc Agriculture Ltd.
    Inventors: David Alan Roberts, Susan Mary Cramp, Derek Ian Wallis, Jean-Paul Bulot
  • Patent number: 5639769
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: January 17, 1996
    Date of Patent: June 17, 1997
    Assignee: G.D. Searle and Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5627283
    Abstract: Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 6, 1997
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Werner St uber, Gerhard Dickneite, Rainer Koschinsky, Cenek Kolar
  • Patent number: 5625089
    Abstract: Anilines of the formula ##STR1## where rings A and B may each be benzofused,X is a bridge member,R.sup.1 and R.sup.2 are each hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, halogen, hydroxysulfonyl, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl or C.sub.1 -C.sub.4 -alkylsulfonyl,R.sup.3 is hydrogen, amino, C.sub.1 -C.sub.4 -alkanoylamino or nitro, andY is vinyl or a radical of the formula C.sub.2 H.sub.4 --Q, where Q is a group detachable under alkaline reaction conditions.
    Type: Grant
    Filed: February 28, 1996
    Date of Patent: April 29, 1997
    Assignee: BASF Aktiengesellschaft
    Inventor: Manfred Patsch
  • Patent number: 5616799
    Abstract: A process for the preparation of glycoloylanilide of the formula (G) ##STR1## is recited that involves reacting a nitrobenzene with hydrogen and, if desired, with a carbonyl compound, in the presence of a noble metal catalyst and a solvent, reacting the compound produced with chloroacetyl chloride, reacting the resulting product with a benzyl alcohol and with a base, or reacting the resulting compound with an O-benzylglycoloyl chloride, and debenzylating the resulting benzylglycoloylanilide product by reacting with hydrogen in the presence of a noble metal catalyst. The invention also relates to a process for the preparation of O-benzylglycoloylanilide.
    Type: Grant
    Filed: April 17, 1995
    Date of Patent: April 1, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Siegfried Planker, Theodor Papenfuhs
  • Patent number: 5616797
    Abstract: 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: Grant
    Filed: December 9, 1994
    Date of Patent: April 1, 1997
    Assignee: Eastman Kodak Company
    Inventors: John C. Wilson, Peter S. Alexandrovich, Steven M. Bonser
  • Patent number: 5612339
    Abstract: 2-Hydroxy-3-aminopropylsulfonamides are provided along with methods for synthesizing and using such compounds, and chemical intermediates employed in the synthetic methods.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: March 18, 1997
    Assignee: Trustees Of The University Of Pennsylvania
    Inventors: Paul Sprengeler, Amos B. Smith, III, Ralph F. Hirschmann, Akihisa Yokoyama
  • Patent number: 5610320
    Abstract: 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: Grant
    Filed: May 26, 1995
    Date of Patent: March 11, 1997
    Assignee: 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
  • Patent number: 5602281
    Abstract: A process for preparing a physically stable crystalline .gamma.-modification of para-aminobenzenesulfonamide comprises cooling a para-aminobenzenesulfonamide solution in water or an organic solvent at rate of at least 2.degree. C./min to complete crystallization thereof and subsequently separating the resulting crystals and drying thereof.
    Type: Grant
    Filed: May 11, 1995
    Date of Patent: February 11, 1997
    Inventor: Nikolai B. Leonidov
  • Patent number: 5591754
    Abstract: Benzoylguanidines, process for their preparation, their use as a medicament and medicament containing them.The invention relates to benzoylguanidines of the formula I ##STR1## where R(1) or R(2) is R(3)-S(O).sub.n -- or R(4)R(5)N--O.sub.2 S-- and the other substituent R(1) or R(2) in each case is H, OH, F, Cl, Br, I, alkyl, alkoxy, benzyloxy or phenoxy, R(3)-S(O).sub.n or R(4)R(5)N-- or 3,4-dehydropiperidine and R(3) is alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl, R(4) and R(5) are alkyl or phenylalkyl or phenyl,and in which R (4) and R (5) can also together be a C.sub.4 -C.sub.7 -chain, and in which R(4) and R(5), together with the nitrogen atom to which they are bonded, can be a dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system,and where n is zero, 1 or 2 and their pharmaceutically tolerable salts are excellent antiarrhythmics.
    Type: Grant
    Filed: May 5, 1995
    Date of Patent: January 7, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans-Jochen Lang, Andreas Weichert, Heinz-Werner Kleemann, Heinrich Englert, Wolfgang Scholz, Udo Albus
  • Patent number: 5576436
    Abstract: Conjugates of fluorescent labels with specific, selective, and high affinity ligands for receptors have been synthesized and used to directly measure binding to receptors.
    Type: Grant
    Filed: March 2, 1994
    Date of Patent: November 19, 1996
    Assignee: Pharmaceutical Discovery Corporation
    Inventors: R. Tyler McCabe, Christopher A. Rhodes, Bruce F. DeCosta
  • Patent number: 5554653
    Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.
    Type: Grant
    Filed: December 22, 1992
    Date of Patent: September 10, 1996
    Assignee: Eli Lilly and Company
    Inventors: Kwan Hui, Charles D. Jones, Louis N. Jungheim, Timothy A. Shepherd
  • Patent number: 5545838
    Abstract: Compounds of the formula ##STR1## wherein Z is SO or SO.sub.2 possess renin inhibition activity and are useful in treating hypertension and other diseases where the reduction of the levels of circulating angiotensin II are beneficial.
    Type: Grant
    Filed: January 27, 1992
    Date of Patent: August 13, 1996
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Michael A. Poss
  • Patent number: 5527829
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
    Type: Grant
    Filed: May 23, 1994
    Date of Patent: June 18, 1996
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventor: Vincent J. Kalish
  • Patent number: 5521219
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: August 24, 1993
    Date of Patent: May 28, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5510386
    Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A-B have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: March 11, 1994
    Date of Patent: April 23, 1996
    Assignee: Zeneca Limited
    Inventors: James R. Empfield, Daniel R. Mayhugh, Keith Russell
  • Patent number: 5510388
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: April 23, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5508294
    Abstract: Sulfonamide-containing hydroxethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: April 16, 1996
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5508306
    Abstract: This invention relates to novel aromatic amine compounds having the structure: ##STR1## where each W, Z.sup.1 and Z.sup.2 is independently H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, OH, F, Cl, Br, I, NO.sub.2, CN, SO.sub.2 NHR.sup.3, NR.sup.4.sub.2, CONR.sup.3.sub.2, COR.sup.5 ; where each R.sup.1 and R.sup.2 is independently H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl; where each X and Y is independently CH.sub.2, NR.sup.4, S, S.dbd.O, SO.sub.2 ; where n is 0, 1 or 2; where each p and q is independently 1 or 2; where R.sup.3 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl; where R.sup.4 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or COR.sup.3 ; and where R.sup.5 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl, C.sub.1 -C.sub.6 straight or branched chain alkoxy or OH.
    Type: Grant
    Filed: September 9, 1993
    Date of Patent: April 16, 1996
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: George Chiu, Charles Gluchowski
  • Patent number: 5491170
    Abstract: .beta.-Carboxy sulfonyl compounds of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 is hydrogen or alkyl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is --O--, --S--, or --NR.sub.2 --, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.
    Type: Grant
    Filed: December 19, 1994
    Date of Patent: February 13, 1996
    Assignee: Warner-Lambert Company
    Inventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
  • Patent number: 5463081
    Abstract: The invention relates to novel intermediates for the preparation of a certain group of novel phenylsulfonylurea herbicides, which herbicides are particularly advantageous for use in crop protection. The novel intermediate compounds are of the formula II ##STR1## and of the formula VI, ##STR2## as defined in the specification and claims. The intermediate compounds may be used to prepare herbicidal and plant growth regulating compounds of the formula I or salts thereof: ##STR3## as defined in the specification. The herbicides so obtained are particularly suitable for selectively controlling weeds.
    Type: Grant
    Filed: September 21, 1993
    Date of Patent: October 31, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Oswald Ort, Klaus Bauer, Hermann Bieringer
  • Patent number: 5463122
    Abstract: 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: Grant
    Filed: August 5, 1994
    Date of Patent: October 31, 1995
    Assignee: Warner-Lambert Company
    Inventors: Edward F. Elslager, Rocco D. Gogliotti
  • Patent number: 5457114
    Abstract: Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.
    Type: Grant
    Filed: January 25, 1994
    Date of Patent: October 10, 1995
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Werner Stuber, Gerhard Dickneite, Rainer Koschinsky, Cenek Kolar
  • Patent number: 5457237
    Abstract: 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: Grant
    Filed: November 23, 1993
    Date of Patent: October 10, 1995
    Assignee: Pfizer Inc.
    Inventor: Robert L. Dow
  • Patent number: 5451677
    Abstract: 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: Grant
    Filed: December 15, 1993
    Date of Patent: September 19, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Michael H. Fisher, Robert J. Mathvink, Hyun O. Ok, Emma R. Parmee, Ann E. Weber
  • Patent number: 5449812
    Abstract: The compounds of the formula (I) ##STR1## in which R.sup.1 -R.sup.4, W, X, Y and Z are as defined in claim 1 are suitable for controlling harmful plants in crops.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: September 12, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 5447958
    Abstract: Pharmaceutical compositions are provided for the treatment of disorders in a subject, such as hypertension, congestive heart failure, angina pectoris, lower urinary tract dysfunction and prostatic hypertrophy. The compositions when administered to a subject produce an .alpha.-adrenergic blocking action and contain as an active ingredient sulfamoyl-substituted phenethylamine derivatives, such as optically active 5-2-[ 2-(2-ethoxyphenoxy)ethylamino] -2-methylethyl-2-methoxybenzenesulfonamide 2-methoxybenzenesulfonamide, and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: September 28, 1994
    Date of Patent: September 5, 1995
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kunihiro Niigata, Takashi Fujikura
  • Patent number: 5414121
    Abstract: Adducts containing mesogenic or rodlike moieties are prepared by reacting (1) at least one compound containing an average of more than one vicinal epoxide group per molecule with (2) at least one compound containing an average of more than one reactive hydrogen atom per molecule; with the proviso that at least one member of components (1) and (2) contains a mesogenic or rodlike moiety. These compounds are useful as curing agents for epoxy resins.
    Type: Grant
    Filed: September 8, 1993
    Date of Patent: May 9, 1995
    Assignee: The Dow Chemical Company
    Inventors: Robert E. Hefner, Jr., Jimmy D. Earls
  • Patent number: 5407951
    Abstract: The present invention provides sulphonamides of the general formula: ##STR1## wherein R.sup.1 and R.sup.2, which can be the same or different, are hydrogen or halogen atoms or C.sub.1 -C.sub.6 -alkyl, trifluoro-methyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, N-alkylaminocarbonyl or N,N-dialkylaminocarbonyl radicals or, when R.sup.1 and R.sup.2 are alkyl radicals ortho to one another, R.sup.1 and R.sup.2 together with the carbon atoms to which they are attached, form a saturated or unsaturated C.sub.5-C.sub.7 -alkylene ring, R.sup.3 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical, a phenylalkyl or phenylalkenyl radical, the phenyl moiety of which can be substituted by halogen, alkyl or trifluoromethyl, C is a --(CH.sub.2).sub.m --radical, in which m is 0, 1, 2 or 3, or a branched C.sub.2 -C.sub.5 -alkylene radical, whereby a methylene radical --CH.sub.
    Type: Grant
    Filed: June 30, 1992
    Date of Patent: April 18, 1995
    Assignee: Boehringer Mannheim GmbH
    Inventors: Ernst-Christian Witte, Karlheinz Stegmeier, Liesel Doerge
  • Patent number: 5405988
    Abstract: 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: Grant
    Filed: June 11, 1993
    Date of Patent: April 11, 1995
    Assignee: Schering Aktiengesellschaft
    Inventors: Ulrich Klar, Helmut Vorbruggen, Hartmut Rehwinkel, Karl Thierauch, Peter Verhallen
  • Patent number: 5401426
    Abstract: Lactobionic acid amide compositions synthesized from lactobionic acid and a mixture of primary fatty amines, which contains at least 30 percent by weight of fatty amines having a chain length of 14 to 18 carbon atoms, and their use as softening, detergent, emulsifying, foam stabilizing and/or thickening components of detergents, rinsing or cleaning agents, softeners or cosmetic formulations.
    Type: Grant
    Filed: October 15, 1993
    Date of Patent: March 28, 1995
    Assignee: Solvay Deutschland GmbH
    Inventors: Klaus-Guenter Gerling, Sabine Joisten, Kornelia Wendler, Claudia Schreer
  • Patent number: 5393790
    Abstract: A class of substituted spiro compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein n is a number selected from 0, 1 and 2; wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein R.sup.8 is selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, n-propyl, isopropyl, butyl, tert-butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, hydroxyl, mercapto, methylthio, ethylthio, cyano, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl, dichloropropyl, trifluoromethoxy, hydroxymethyl, methoxymethyl and ethoxymethyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: February 10, 1994
    Date of Patent: February 28, 1995
    Assignee: G.D. Searle & Co.
    Inventors: David B. Reitz, Robert E. Manning, Horng-Chi Huang, Jinglin Li
  • Patent number: 5391825
    Abstract: Pharmaceutical compositions are provided for the treatment of disorders in a subject, such as hypertension, congestive heart failure, angina pectoris, lower urinary tract dysfunction and prostatic hypertrophy. The compositions when administered to a subject produce an .alpha.-adrenergic blocking action and contain as an active ingredient sulfamoyl-substituted phenethylamine derivatives, such as optically active 5-2-[2-(2-ethoxyphenoxy)ethylamino]-2-methylethyl-2-methoxybenzenesulfonam ide, and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: December 28, 1993
    Date of Patent: February 21, 1995
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kunihiro Niigata, Takashi Fujikura
  • Patent number: 5382600
    Type: Grant
    Filed: December 19, 1991
    Date of Patent: January 17, 1995
    Assignee: Pharmacia Aktiebolag
    Inventors: Nils A. Jonsson, Bengt A. Sparf, Lembit Mikiver, Pinchas Moses, Lisbet Nilvebrant, Gunilla Glas
  • Patent number: 5373024
    Abstract: Benzoylguanidines of the formula I ##STR1## are described where R(1) is R(4)--SO.sub.m or R(5)R(6)N--SO.sub.z --, where R(4) and R(5) are alk(en)yl or --C.sub.n H.sub.2n --R(7), and where R(7) is a cycloalkyl or phenyl, where R(5) also has the meaning of H, and R(6) is H or C.sub.1 -C.sub.4 -alkyl, R(2) is hydrogen, halogen, alkyl, O--(CH.sub.2).sub.m C.sub.p F.sub.2p+1, --X--R(10), where X is O, S or NR(11), R(10) is H, (cyclo)alkyl(methyl) or --C.sub.n H.sub.2n --R(12) where R(12) is phenyl, and R(3) is defined, inter alia, as R(1), and their pharmaceutically tolerable salts.The compounds I are obtained by reaction of compounds of the formula II ##STR2## with guanidine, in which L is a leaving group which can be easily nucleophilically substituted.
    Type: Grant
    Filed: February 10, 1993
    Date of Patent: December 13, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Florian Lang, Hans-Jochen Lang, Dieter Mania, Andreas Weichert, Wolfgang Scholz, Udo Albus, Heinrich Englert
  • Patent number: 5354904
    Abstract: The sulfonamides have the formula ##STR1## where R.sup.1 is C.sub.1 -C.sub.13 -lkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.8 -alkanoyl or substituted or unsubstituted benzoyl, andR.sup.2 and R.sup.3 are each independently of one another substituted or unsubstituted C.sub.1 -C.sub.13 -alkyl, substituted or unsubstituted C.sub.5 -C.sub.7 -cycloalkyl or substituted or unsubstituted piperidinyt, or R.sup.2 may also be hydrogen.
    Type: Grant
    Filed: October 8, 1992
    Date of Patent: October 11, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Udo Mayer, Ulrike Schloesser
  • Patent number: 5332759
    Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein R.sub.3 represents a group ##STR2## R.sub.1, R.sub.2, R.sub.6, R.sub.7 being as defined in the description. Medicinal product useful in treating a disorder due to vasodilatation of the vascular system.
    Type: Grant
    Filed: January 21, 1993
    Date of Patent: July 26, 1994
    Assignee: Adir et Compagnie
    Inventors: Patrick Depreux, Daniel Lesieur, Habib Abdellaoui, Beatrice Guardiola, Gerard Adam, Pierre Renard, Bruno Pfeiffer
  • Patent number: 5331004
    Abstract: The invention relates to novel polybenzamide mustards having anticancer and hypoxia-selective properties, to methods of preparing the novel compounds, and to the use of these compounds as anticancer agents.The compounds have general formula (I) ##STR1## wherein M and M.sub.1 separately represent H, aziridinyl, N(Et)CH.sub.2 CH.sub.2 Y or N(CH.sub.2 CH.sub.2 Y).sub.2, where Y is Cl, Br, I or OSO.sub.2 Me; R and R.sub.1 separately represent up to three of H, NO.sub.2, aza (ring CH.dbd.replaced by N.dbd.), CH.sub.2 Q, SO.sub.2 NHQ or CONHQ, where Q is H, Me, (CH.sub.2).sub.n NMe.sub.2 (CH.sub.2).sub.n NHC(.dbd.NH)NH.sub.2 and n.dbd.2-4);X represents CONH, NHCO, O, CH.sub.2, NH or S; and A is (CH.sub.2).sub.n, where n.dbd.2 to 4, or a unit chosen from formulae (IIa to IIc) ##STR2## wherein Z.dbd.CH.sub.2 Q, SO.sub.2 NH.sub.Q or CONHQ, where Q is H, Me, (CH.sub.2).sub.n NMe.sub.2 (CH.sub.2).sub.n NHC(.dbd.NH)NH.sub.2 and n.dbd.2 to 4),or an acid addition salt or N-oxide thereof.
    Type: Grant
    Filed: July 16, 1992
    Date of Patent: July 19, 1994
    Assignee: Circadian Pharmaceuticals (Australia) Pty. Ltd.
    Inventors: William A. Denny, Graham J. Atwell
  • Patent number: 5292737
    Abstract: N,N'-Bis(sulfonamido)-2-amino-4-iminonaphthalen-1-ones and N,N'-Bis(amido)-2-amino-4-iminonaphthalen-1-ones are disclosed. Methods of inhibiting protein kinase C activity which comprises contacting protein kinase C with an effective amount of an N,N'-Bis(sulfonamido)-2-amino-4-iminonaphthalen-1-one or an N,N'-Bis(amido)-2-amino-4-iminonaphthalen-1-one are disclosed. Methods of treating an animal that is suspected of suffering from inflammatory, cardiovascular and/or neoplastic diseases which comprises administering an effective amount of an N,N'-Bis(sulfonamido)-2-amino-4-iminonaphthalen-1-one or an N,N'-Bis(amido)-2-amino-4-iminonaphthalen-1-one are disclosed.
    Type: Grant
    Filed: October 23, 1992
    Date of Patent: March 8, 1994
    Assignee: Sphinx Pharmaceuticals Corporation
    Inventor: Jean M. Defauw
  • Patent number: 5281626
    Abstract: A novel benzenesulfonamide derivative represented by the formula: ##STR1## has an inhibitory activity against phospholipase A.sub.2, so that it is effective in the treatment of diseases for which such an activity is efficacious.
    Type: Grant
    Filed: September 26, 1991
    Date of Patent: January 25, 1994
    Assignee: Eisai Co., Ltd.
    Inventors: Hitoshi Oinuma, Takashi Hasegawa, Tadanobu Takamura, Kenichi Nomoto, Yoshiharu Daiku, Toshihiko Naito, Sachiyuki Hamano
  • Patent number: 5262545
    Abstract: Fluorescent compounds useful in the determination of chloramphenicol acetyltransferase (CAT) enzyme activity are described. The compounds are fluorescent derivatives related in structure to chloramphenicol comprising a base, ##STR1## substituted at one to five aromatic ring positions by substituents, which may be the same or different, that are alkyl-, hydroxy-, alkoxy-, aryl-, halo-, nitro-, amino-, alkylamido-, or arylamido-; and a fluorescent moiety linked to the base at --NH-- by an aliphatic chain of 1-12 atoms other than hydrogen, where such atoms are carbon, nitrogen, oxygen, or sulfur, or combinations thereof. The substrate compounds are acylated in the presence of CAT to produce fluorescent mono- and diacylated products, which are then physically separated from the reaction mixture and quantitated by means of their fluorescence and/or absorbance.
    Type: Grant
    Filed: June 18, 1991
    Date of Patent: November 16, 1993
    Assignee: Molecular Probes, Inc.
    Inventors: Richard P. Haughland, Hee C. Kang, Steven L. Young, Michael H. Melner
  • Patent number: 5243074
    Abstract: An immunofluorescent assay method, characterized in using an immunodetective reagent, which is an antigen-like substance comprising a fluorescent substance and an antigen chemically bonded thereto with or without intervention of an additional chemical bond, said fluorescent substance being changed in the wavelength or intensity of the fluorescence when an antibody comes close thereto, and said antigen being specific to said antibody.
    Type: Grant
    Filed: November 21, 1990
    Date of Patent: September 7, 1993
    Assignee: Matsushita Electric Industrial Co., Ltd.
    Inventors: Tadayasu Mitsumata, Jinsei Miyazaki
  • Patent number: 5227401
    Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.
    Type: Grant
    Filed: October 29, 1991
    Date of Patent: July 13, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5223535
    Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R.sub.5 and R.sub.8 is independently propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.
    Type: Grant
    Filed: October 29, 1991
    Date of Patent: June 29, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5217855
    Abstract: A photographic processing composition containing at one compoud represented by formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, an aliphatic group, or an aromatic group, L.sub.1 and L.sub.2 each represents a divalent bonding group including an alkylene group and/or an arylene group; X represents a ##STR2## group (wherein R.sub.a, R.sub.b and R.sub.c each represents a hydrogen atom, an aliphatic group or an aromatic group, and R.sub.d represents an aliphatic group or an aromatic group); and Y represents a carboxy group, a hydroxy group, a phosphono group, a sulfo group or a salt thereof. The processing composition does not produce precipitate or sludge even when contaminated by metallic ions. A processing method using the processing composition is also disclosed.
    Type: Grant
    Filed: July 25, 1991
    Date of Patent: June 8, 1993
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Okada, Morio Yagihara, Shigeru Nakamura
  • Patent number: 5210203
    Abstract: Nucleic acid hybridization probes are provided which comprise an N.sup.4 -(substituted amino)cytosine moiety, wherein the substituted amino group comprises a tag moiety, whereby the probe is detected. Methods of preparing probes of the invention, intermediates used in such methods, and methods of using the probes of the invention in hybridization assays are also provided. Typical tag moieties employed with the probes of the invention are biotinyl, aminothiadiazole and fluorescein derivatives, connected to N.sup.4 -amino groups of modified cytosines of the probe through linker moieties. Probes tagged with biotin are typically detected by binding to the biotinyl moieties, through a streptavidin or avidin molecule, a reporter group which includes streptavidin or avidin and then detecting a signal due to the reporter group.
    Type: Grant
    Filed: May 7, 1992
    Date of Patent: May 11, 1993
    Assignee: Siska Diagnostics, Inc.
    Inventors: Gary F. Musso, Soumitra Ghosh, Emil T. Kaiser
  • Patent number: 5210257
    Abstract: Novel aryl ethers, containing both a carboxylic acid and a sulfonic acid functionality; and a process for making them are described. These difunctional aryl compounds comprise:i) a carboxylic acid group or its derivative,ii) a first aromatic group bonded to the carboxylic acid or its derivative,iii) a second aromatic group linked to the first aromatic group by a non-electron-withdrawing moiety,iv) a third aromatic group linked to the second aromatic group by a non-electron-withdrawing moiety, andv) a sulfonyl group or its derivative bonded to the third aromatic group.
    Type: Grant
    Filed: April 12, 1991
    Date of Patent: May 11, 1993
    Assignee: The Dow Chemical Company
    Inventor: William J. Harris
  • Patent number: 5198566
    Abstract: Disclosed herein are N-substituted-3-(substituted hydrazino)benzenesulfonamide derivatives of the formula (I): ##STR1## wherein R.sup.1 and CF.sub.3, COOH or CCl=CClCOOH, R.sup.2 is H, Cl, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.4 alkoxycarbonyl; Z is CH or N; X.sup.1 is C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxyl or Cl; and X.sup.2 is C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxyl, a process for the preparation thereof, and herbicidal compositions containing the N-substituted-3-(substituted hydrazino)benzenesulfonamide derivatives as active ingredients.
    Type: Grant
    Filed: June 3, 1992
    Date of Patent: March 30, 1993
    Assignee: Kureha Kagaku Kogyo K.K.
    Inventors: Hideo Arabori, Shiro Yamazaki, Masato Arahira, Aiko Murakami
  • Patent number: 5189211
    Abstract: 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: Grant
    Filed: July 26, 1991
    Date of Patent: February 23, 1993
    Assignees: Taisho Pharmaceutical Co., Ltd., Nippon Suisan Kaisha, Ltd.
    Inventors: Masakazu Sato, Yutaka Kawashima, Jun Goto, Yoshiyuki Chiba, Mikio Satake, Chuzo Iwata, Takeshi Imanishi