Sulfur Containing Patents (Class 564/154)
  • Patent number: 6124502
    Abstract: This invention relates to matrix metalloproteinase (MMP) inhibiting compounds of the formula: ##STR1## where R.sup.1 is C.sub.1 -C.sub.12 alkyl, straight or branched and optionally substituted by halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, carboxamido, nitrile, mono- or di-(C.sub.1 -C.sub.6)alkylamino, thio, C.sub.1 -C.sub.6 alkylthio, aryl, --Oaryl or --OCH.sub.2 aryl where aryl is optionally substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, carboxy, halogen, cyano, nitro, carboxamido, or hydroxy; and C.sub.1 -C.sub.6 alkanesulfonyloxy. R.sup.2 is .alpha.-OH or .beta.-OH and R.sup.6 is H or R.sup.2 and R.sup.6 together are carbonyl; the chemical intermediates; and processes for the preparation of these compounds and the intermediates thereto.Matrix metalloproteinases (MMP) are a family of zinc-containing calcium dependent proteinases, including stromelysins, collagenases, and gelatinases.
    Type: Grant
    Filed: October 9, 1998
    Date of Patent: September 26, 2000
    Assignee: American Cyanamid Company
    Inventor: Jeremy Ian Levin
  • Patent number: 6084065
    Abstract: The present invention relates to oligopeptidic compounds having the general formula (I):K--[--A--].sub.z --[--B--].sub.w --L (I)The compounds having general formula (I) are antifungals for agricultural purposes.
    Type: Grant
    Filed: October 4, 1994
    Date of Patent: July 4, 2000
    Assignee: Isagro Spa
    Inventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Ernesto Signorini
  • Patent number: 6057322
    Abstract: Compounds of the formula I ##STR1## and the pharmaceutically tolerated salts thereof, are described. A process for their preparation and their use as medicaments in cardiovascular diseases are also described.
    Type: Grant
    Filed: July 30, 1997
    Date of Patent: May 2, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 6040339
    Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl or various other organic groups; R.sup.3 is alkyl; R.sup.4 is a group of formula (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX): ##STR2## wherein: A.sup.1 is a single bond, alkylene or alkenylene; A.sup.2 is or alkenylene; A.sup.3 is a single bond, alkyleneor alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or various other groups; R.sup.6 is alkyl or phenyl; R.sup.7 is hydrogen or alkyl; R.sup.8 is alkyl or various other groups; and n is 0 and pharmaceutically acceptable salts thereof have valuable inhibitory activity against acyl-CoA: cholesterol acyl transferase.
    Type: Grant
    Filed: May 28, 1998
    Date of Patent: March 21, 2000
    Assignee: Sankyo Company, Limited
    Inventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
  • Patent number: 6034136
    Abstract: Disclosed are compound of formula I whereinR represents hydrogen, lower alkyl, cycloalkyl, bicycloalkyl, adamantyl, aryl, biaryl, or mono- or di-(cycloalkyl, aryl or biaryl)-lower alkyl, di-(lower alkyl or aryl-lower alkyl)amino-lower alkyl, or (piperidino, morpholino, pyrrolidino)-lower alkyl;R.sub.1 represents hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, or (cycloalkyl, aryl or biaryl)-lower alkyl;R.sub.2 represents hydrogen, lower alkyl, lower alkoxy, aryl-lower alkyl, aryl-lower alkoxy, amino, mono- or di-(lower alkyl or aryl-lower alkyl)-amino, acylamino, or (lower alkyl or aryl-lower alkyl)-(thio, sulfinyl or sulfonyl);R.sub.3 represents hydrogen, lower alkyl, cycloalkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or C.sub.2 -C.sub.7 -alkyl interrupted by S, SO, SO.sub.2, O or N--R.sub.5 ;R.sub.4 represents hydrogen or acyl;R.sub.
    Type: Grant
    Filed: March 17, 1998
    Date of Patent: March 7, 2000
    Assignee: Novartis AG
    Inventor: Cynthia A. Fink
  • Patent number: 6034135
    Abstract: The present invention provides novel dimeric cationic lipids. The present invention further provides compositions of these lipids with anionic or polyanionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions and a kit for preparing the same.
    Type: Grant
    Filed: March 6, 1997
    Date of Patent: March 7, 2000
    Assignee: Promega Biosciences, Inc.
    Inventors: David Aaron Schwartz, Brian Patrick Dwyer, William J. Daily, Kumar Srinivasan, Bob Dale Brown
  • Patent number: 6005010
    Abstract: Compounds of the formula ##STR1## where T is ##STR2## and R(A), R(B), R(C), R(D), R(E), R(F), x and y have the meanings indicated in the claims, and their pharmaceutically acceptable salts are effective inhibitors of the cellular sodium-proton antiporter (Na.sup.+ /H.sup.+ exchanger). These compounds are therefore outstandingly suitable for treatment of all illnesses which are to be attributed to increased Na.sup.+ /H.sup.+ exchange.
    Type: Grant
    Filed: August 20, 1997
    Date of Patent: December 21, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Andreas Weichert, Hans-Willi Jansen, Wolfgang Scholz
  • Patent number: 5994312
    Abstract: Compounds of general formula (I): ##STR1## have utility as inhibitors of matrix metalloproteinases and TNF.
    Type: Grant
    Filed: July 30, 1998
    Date of Patent: November 30, 1999
    Assignee: Darwin Discovery, Ltd.
    Inventors: John Montana, Andrew Douglas Baxter, David Alan Owen, Robert John Watson, Neil Phillipson
  • Patent number: 5981581
    Abstract: Phenylacetic acid derivatives of the formula I ##STR1##
    Type: Grant
    Filed: January 29, 1998
    Date of Patent: November 9, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Herbert Bayer, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5981490
    Abstract: Dipeptide compounds have therapeutic utility, inter alia, as metalloproteinase and TNF inhibitors.
    Type: Grant
    Filed: October 4, 1996
    Date of Patent: November 9, 1999
    Assignee: Darwin Discovery, Ltd.
    Inventors: Andrew Douglas Baxter, John Gary Montana, David Alan Owen
  • Patent number: 5972939
    Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor disorders. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.
    Type: Grant
    Filed: October 26, 1998
    Date of Patent: October 26, 1999
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Robert H. Chen, Min Xiang, John B. Moore, Jr., Mary Pat Beavers
  • Patent number: 5968984
    Abstract: Compounds characterized generally as alkylaminoalkyl-terminated .beta.-alanineamide amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein n is two or three; wherein x is a number selected from zero, one and two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, napthylmethyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is methyl; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: July 14, 1997
    Date of Patent: October 19, 1999
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran, Barbara B. Chen
  • Patent number: 5969184
    Abstract: The present invention is directed to the novel intermediate compounds of the formula: ##STR1## wherein, interalia, R.sub.4 is a substituted phenyl or an optionally substituted napthyl derivative.
    Type: Grant
    Filed: May 9, 1997
    Date of Patent: October 19, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Jerry Leroy Adams, Peter William Sheldrake, Timothy Francis Gallagher, Ravi Shanker Garigipati, Paul Elliot Bender, Jeffrey Charles Boehm, Joseph Sisko, Zhi-Qiang Peng, John C. Lee
  • Patent number: 5929278
    Abstract: Disclosed are novel inhibitors of metalloproteases, in particular matrix metalloproteases. The disclosed inhibitors are mercaptoketone and mercaptoalcohol compounds which are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, for example, arthropathy, dermatological conditions, bone resorption, inflammatory diseases, and tumor invasion and in the promotion of wound healing.
    Type: Grant
    Filed: May 19, 1998
    Date of Patent: July 27, 1999
    Assignee: Affymax Technologies N.V.
    Inventors: David A. Campbell, Dinesh V. Patel, Xiao-Yi Xiao
  • Patent number: 5880147
    Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl, --(C.dbd.O)--B.sup.1 (wherein B.sup.1 is hydrogen or alkyl), nitro, --NR.sup.c R.sup.d (wherein R.sup.c is hydrogen or alkyl and Rd is alkyl), hydroxy, protected hydroxy group, alkoxy, cyano, alkylthio, alkylsulfinyl, alkylsulfonyl or halogen;R.sup.3 is alkyl; R.sup.4 is a group of the formula (II) ##STR2## wherein A.sup.1 is a single bond, alkylene or alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or --A.sup.4 R.sup.5.sub.c wherein A is a single bond, alkylene or alkenylene and R.sup.5.sub.c is alkoxy; and n is 0, and pharmaceutically acceptable salts thereof. Such compounds have valuable inhibitory activity against acyl-CoA (cholesterol acyl transferase).
    Type: Grant
    Filed: September 18, 1996
    Date of Patent: March 9, 1999
    Assignee: Sankyo Company, Limited
    Inventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
  • Patent number: 5856572
    Abstract: Disclosed is a wholly aromatic polyamide prepared by reacting 1,4-naphthyl or 2,6-naphthyl containing diacids with aromatic diamines. The polymers of the invention are readily soluble in a variety of organic solvents including DMAc, NMP and pyridine, and have good thermal stability. Transparent, tough and flexible films of these polymers can be cast from the solutions thereof and these polyamides are easily processable high-performance polymer materials.
    Type: Grant
    Filed: August 14, 1996
    Date of Patent: January 5, 1999
    Assignee: Industrial Technology Research Institute
    Inventors: Guey-Sheng Liou, Sheng-Huei Hsiao, Jen-Chang Yang
  • Patent number: 5852213
    Abstract: This invention relates to matrix metalloproteinase (MMP) inhibiting compounds of the formula: ##STR1## where R.sup.1 is C.sub.1 -C.sub.12 alkyl, straight or branched and optionally substituted by halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, carboxamido, nitrile, mono- or di-(C.sub.1 -C.sub.6)alkylamino, thio, C.sub.1 -C.sub.6 alkylthio, aryl, --Oaryl or --OCH.sub.2 aryl where aryl is optionally substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, carboxy, halogen, cyano, nitro, carboxamido, or hydroxy; and C.sub.1 -C.sub.6 alkanesulfonyloxy. R.sup.2 is .alpha.-OH or .beta.-OH and R.sup.6 is H or R.sup.2 and R.sup.6 together are carbonyl; the chemical intermediates; and processes for the preparation of these compounds and the intermediates thereto.Matrix metalloproteinases (MMP) are a family of zinc-containing calcium dependent proteinases, including stromelysins, collagenases, and gelatinases.
    Type: Grant
    Filed: July 2, 1997
    Date of Patent: December 22, 1998
    Assignee: American Cyanamid Company
    Inventor: Jeremy Ian Levin
  • Patent number: 5847005
    Abstract: The present invention relates to benzamidoxime derivatives represented by the formula ?I!; ##STR1## wherein R.sup.1 is unsubstituted or substituted C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted C.sub.2 -C.sub.4 alkenyl or unsubstituted or substituted C.sub.2 -C.sub.4 alkynyl, R.sup.2 is phenyl optionally having substituents or heterocycle optionally having substituents, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are each independently hydrogen, halogen, 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 haloalkoxy, C.sub.1 -C.sub.4 alkylthio or the like, and r.sub.1 and r.sub.2 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl or the like, having excellent fungicidal activity and being useful as a fungicide for agricultural and horticultural use, and methods for preparation thereof.
    Type: Grant
    Filed: August 14, 1997
    Date of Patent: December 8, 1998
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Isamu Kasahara, Hirohito Ooka, Shinsuke Sano, Hiroyasu Hosokawa, Homare Yamanaka
  • Patent number: 5847206
    Abstract: New fluorinated derivatives useful as surfactants or in the transport of drug or markers, or in drug targeting, and preparations containing the derivatives, for medical, cosmetic and veterinary uses, having the formula: ##STR1## wherein R.sub.F is a fluorinated radical, X is a linear or branched alkylene, R.sup.1 is H or CH.sub.3, R.sup.2 is a radical having at least one OH group, R.sup.3 is a radical derived from an amino acid or a peptide, 1.ltoreq.n.ltoreq.50 and 0.ltoreq.m.ltoreq.200 with 0.2.ltoreq.n/n+m.ltoreq.1.These derivatives can be used as prodrugs or in formulating pharmaceutical, cosmetic and veterinary preparations, in biology and medicine, notably in compositions acting as carriers of oxygen and other gases, of contrast agents, or as carriers of substances used in therapy, or as carriers of markers.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 8, 1998
    Assignee: Alliance Pharmaceutical Corp.
    Inventors: Andre Pavia, Bernard Pucci, Jean G. Riess, Leila Zarif
  • Patent number: 5840698
    Abstract: Disclosed are novel inhibitors of collagenase-1 and stromelysin-I metalloproteases. The disclosed inhibitors are mercaptoketone and mercaptoalcohol compounds which are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, for example, arthropathy, dermatological conditions, bone resorption, inflammatory diseases, and tumor invasion and in the promotion of wound healing.
    Type: Grant
    Filed: October 27, 1995
    Date of Patent: November 24, 1998
    Assignee: Affymax Technologies N.V.
    Inventors: David A. Campbell, Dinesh V. Patel, Xiao-Yi Xiao
  • Patent number: 5831004
    Abstract: Disclosed are novel inhibitors of metalloproteases, in particular matrix metalloproteases. The disclosed inhibitors are mercaptoketone and mercaptoalcohol compounds which are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, for example, arthropathy, dermatological conditions, bone resorption, inflammatory diseases, and tumor invasion and in the promotion of wound healing.
    Type: Grant
    Filed: October 27, 1995
    Date of Patent: November 3, 1998
    Assignee: Affymax Technologies N.V.
    Inventors: David A. Campbell, Dinesh V. Patel, Xiao-Yi Xiao
  • Patent number: 5783735
    Abstract: A process for preparing polymeric amides is disclosed. The process comprises sequentially reacting a hydrocarbon polymer functionalized (e.g., via the Koch reaction) to contain acid, ester, thioacid and/or thioester groups with a heavy polyamine to form a partially derivatized product in which at least about 85% of the functional groups are converted to heavy (thio)amide groups, and then reacting the partially derivatized product with an excess of light amine to complete the derivatization by converting substantially all of the remaining functional groups to light (thio)amide groups. Products of the foregoing process are also disclosed, which products are useful as additives in fuels and in lubricants.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: July 21, 1998
    Assignee: Exxon Chemical Patents Inc.
    Inventors: Jacob I. Emert, Joseph V. Cusumano, David C. Dankworth, William D. Diana, William B. Eckstrom, Keith R. Gorda, Antonio Gutierrez, Jon E. Stanat, Warren A. Thaler, Stephen Zushma
  • Patent number: 5753652
    Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.
    Type: Grant
    Filed: April 4, 1995
    Date of Patent: May 19, 1998
    Assignee: Novartis Corporation
    Inventors: Alexander Fassler, Guido Bold, Marc Lang, Shripad Bhagwat, Peter Schneider
  • Patent number: 5712417
    Abstract: The present invention relates to compounds of the formula I ##STR1## wherein A, Y, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, l, m and the corresponding radicals labeled with * are defined as stated in the description, a process for their preparation and their use for the inhibition of retroviral proteases.
    Type: Grant
    Filed: July 11, 1994
    Date of Patent: January 27, 1998
    Assignee: Abbott Laboratories
    Inventors: Karl-Heinz Budt, Bernd Stowasser, Dieter Ruppert, Christoph Meichsner, Arnold Paessens, Jutta Hansen, Jochen Knolle
  • Patent number: 5710311
    Abstract: At least one 2-sulphured metaphenylenediamine of formula (I) ##STR1## used for dyeing keratin fibres, wherein Z is alkyl, aralkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl or aminoalkyl; R.sub.1 and R.sub.2, which are the same or different, are hydrogen, alkyl, monohydroxyalkyl, polyhydroxyalkyl, monocarbamylalkyl, dialkylcarbamyl, aminoalkyl, acyl carbalkoxy, carbamyl, or monoalkylcarbamyl; R.sub.3 is hydrogen, alkyl, nitrile, amide, fluoroalkyl, or --COOR; and the corresponding acid salts. A method for dyeing keratin fibres, and novel 2-sulphured metaphenylenediamines, are also disclosed.
    Type: Grant
    Filed: September 29, 1995
    Date of Patent: January 20, 1998
    Assignee: L'Oreal
    Inventors: Alex Junino, Alain Genet, Alain Lagrange
  • Patent number: 5708004
    Abstract: Hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: January 13, 1998
    Assignee: Monsanto Company
    Inventors: John J. Talley, Kathryn L. Reed
  • Patent number: 5708034
    Abstract: Substituted sulfonimidamides, processes for their preparation, their use as a medicament or diagnostic, and medicament comprising themSulfonimidamides of the formula I ##STR1## in which at least one of the three substituents R(1), R(2) and R(3) is a benzoylguanidine, and in which the other substituents have the meanings indicated in the claims, are outstandingly suitable as medicaments having action on the cardiovascular system; that is as antiarrhythmic pharmaceuticals having a cardioprotective component as well as for treating ischemically induced damage; also in operative interventions, such as organ transplantation.
    Type: Grant
    Filed: October 31, 1996
    Date of Patent: January 13, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans Jochen Lang, Udo Albus, Wolfgang Scholz
  • Patent number: 5696071
    Abstract: Described are a tris(3-aminopropyl)amine derivative represented by the following formula (1): ##STR1## wherein R represents a C.sub.1-24 alkyl or alkenyl group which may have --OH, A represents a C.sub.1-6 alkylene or alkenylene group which may have --OH, --COOH or --SO.sub.3 H, Y.sup.1 represents --COOH, --SO.sub.3 H or --OSO.sub.3 H , Y.sup.2 represents --OH, --OSO.sub.3 H or --OCO--A--COOH and n stands for 0 or 1, or a salt or quaternized product thereof; and a detergent composition containing the same. The compound according to the present invention has low skin or hair irritation, has excellent foaming power and imparts favorable touch feeling to the skin or the like.
    Type: Grant
    Filed: January 7, 1997
    Date of Patent: December 9, 1997
    Assignee: Kao Corporation
    Inventors: Akiko Okutsu, Tomohito Kitsuki, Katsumi Kita
  • Patent number: 5696282
    Abstract: A process comprises contacting, in the presence of a catalyst, hydrogen sulfide or a mercaptan such as, for example, n-dodecyl mercaptan with an .alpha.,.beta.-unsaturated carbonyl or .alpha.,.beta.-unsaturated cyano compound such as, for example, methyl acrylate wherein the catalyst comprises a pyridine derivative such as, for example, 4-(dimethylamino)pyridine or an ion exchange resin such as, for example, "AMBERLYST A-21" to produce a 3-hydrocarbylthio derivative of the .alpha.,.beta.-unsaturated carbonyl or .alpha.,.beta.-unsaturated cyano compound such as, for example, methyl 3-(dodecylthio)propionate.
    Type: Grant
    Filed: March 26, 1996
    Date of Patent: December 9, 1997
    Assignee: Phillips Petroleum Company
    Inventors: James E. Shaw, Harry Porter
  • Patent number: 5686633
    Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.
    Type: Grant
    Filed: December 31, 1991
    Date of Patent: November 11, 1997
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Eric Vieira, Hugh Stephen Laver
  • Patent number: 5672759
    Abstract: The invention relates to a dye composition for keratinic fibers comprising an oxidation colorant precursor of the type ortho and/or para and a sulfured metaphenylenediamine having formula (I) ##STR1## wherein Z is alkyl, aralkyl, monohydroxyalkyl or polyhydroxyalkyl, aryl or aminoalkyl, as well as the acid salts thereof, with the condition that R.sub.1 and R.sub.2 do not represent simultaneously hydrogen when Z is alkyl or hydroxyalkyl, as well as the acid salts corresponding to the compounds of formula (I).
    Type: Grant
    Filed: January 19, 1996
    Date of Patent: September 30, 1997
    Assignee: L'Oreal
    Inventors: Alex Junino, Alain Genet, Alain Lagrange
  • Patent number: 5672765
    Abstract: Aromatic, ring-fluorinated compounds are prepared by reaction of corresponding chlorine compounds or bromine compounds with alkali metal fluorides using a diamide as solvent. Most of the diamides which can be used are novel compounds.
    Type: Grant
    Filed: July 14, 1995
    Date of Patent: September 30, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Albrecht Marhold, Marianne Lohr, Heinrich Wamhoff
  • Patent number: 5663436
    Abstract: There is disclosed a novel isothiazolone derivative of the formula: ##STR1## wherein X.sup.1 and X.sup.2 are the same or different and are independently hydrogen, chlorine or bromine; and R is haloalkoxy. The isothiazolone derivative is effective as a microbicide. Also disclosed are a microbicidal composition containing the isothiazolone derivative as an active ingredient, and an intermediate compound for use in the production of the isothiazolone derivative.
    Type: Grant
    Filed: May 1, 1996
    Date of Patent: September 2, 1997
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Akiko Kakimizu, Kenji Arai, Norio Kimura, Tomohiro Teramae
  • Patent number: 5654301
    Abstract: The present invention relates to compounds of the formula ##STR1##
    Type: Grant
    Filed: January 12, 1993
    Date of Patent: August 5, 1997
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Harold L. Kohn, Darrell Watson
  • Patent number: 5641820
    Abstract: The present invention relates to silica-filled rubber compositions containing dialkyleneamide polysulfides of the formula ##STR1## where R.sup.1 is independently selected from alkylene groups having 1 to 18 carbon atoms and x is an integer of from 2 to 7.
    Type: Grant
    Filed: December 26, 1995
    Date of Patent: June 24, 1997
    Assignee: The Goodyear Tire & Rubber Company
    Inventors: Lawson Gibson Wideman, Paul Harry Sandstrom
  • Patent number: 5633403
    Abstract: Substantive UV-absorbing cinnamido amine cationic quaternary salts are disclosed. Detergent and household cleaning product compositions and hair and skin personal care product compositions, as well as sunscreen and tanning lotion compositions, containing the compounds of the present invention are also described.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 27, 1997
    Assignee: Croda, Inc.
    Inventors: Kevin F. Gallagher, Abel G. Pereira
  • Patent number: 5629347
    Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is R.sup.9 CR.sup.10 R.sup.11 or CH.sub.2 R.sup.9 CR.sup.10 R.sup.11 where R.sup.9 is H or OH and R.sup.10 and R.sup.11 are optionally substituted phenyl, optionally substituted benzyl, C.sub.5-7 cycoalkyl or (C.sub.5-7 cycloalkyl)methyl; R.sup.1 and R.sup.2 are H, optionally substituted C.sub.1-6 alkyl, optionally substituted phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, COR.sup.a, COOR.sup.a, COC.sub.1-6 alkylhalo, COC.sub.1-6 alkylNR.sup.a R.sup.b, CONR.sup.12 C.sub.1-6 alkylCONR.sup.a R.sup.b, CONR.sup.a R.sup.b, or SO.sub.2 R.sup.a, or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.q optionally substituted by oxo where one methylene group may optionally be replaced by O or NR.sup.x ; R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 is optionally substituted phenyl(C.sub.1-3 alkyl); X and Y are H, or X and Y together are .dbd.O; and Z is O, S, or NR.sup.7 ; are tachykinin antagonists.
    Type: Grant
    Filed: December 22, 1993
    Date of Patent: May 13, 1997
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Christopher J. Swain, Martin R. Teall, Brian J. Williams
  • Patent number: 5629343
    Abstract: Novel N-(mercaptoacyl)peptidyl compounds are useful as inhibitors of matrix metalloendoproteinases which degrade major components of articular cartilage and basement membranes causing degenerative diseases such as arthritis, periodontal disease, corneal ulceration, are described. For example, N-(2-thiomethyl-4-phenyl-butanoyl)-L-leucinamide was prepared and its inhibitory activity against stromelysin was tested in vitro.
    Type: Grant
    Filed: February 23, 1995
    Date of Patent: May 13, 1997
    Assignee: Merck & Co., Inc.
    Inventors: William Hagmann, Ihor Kopka
  • Patent number: 5625075
    Abstract: The present invention provides metal chelating compounds, to chelates and chelate-targeting agent conjugates formed from the chelating compounds, and to methods for making and using these compositions. The chelating compounds incorporate two nitrogen atoms and three sulfur atoms ("N.sub.2 S.sub.3 "), two nitrogen atoms and four sulfur atoms ("N.sub.2 S.sub.4 "), or three nitrogen atoms and three sulfur atoms ("N.sub.3 S.sub.3 "). Metals, and metal oxides, capable of being chelated by the compounds include those that are radionuclides, such as .sup.99m Tc and .sup.186/188 Re.The targeting agent portion of the chelate-targeting agent conjugates provided includes antibodies, peptides, hormones, enzymes and biological response modifiers. Methods for making the conjugates are provided and encompass the addition of a metal, or metal oxide, to a chelating compound prior to attachment to a targeting agent as well as subsequent to the attachment.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: April 29, 1997
    Assignee: NeoRx Corporation
    Inventors: Ananthachari Srinivasan, Alan R. Fritzberg, David S. Jones
  • Patent number: 5587513
    Abstract: The present invention relates to novel polyether-substituted compounds of imides and their use as surface-active agents.
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: December 24, 1996
    Inventors: Klaus Pohmer, Rainer Weber, Cornelia D orzbach-Lange, Reinhard Haida, Hans-Heinrich Moretto
  • Patent number: 5583248
    Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aralkanoyl, heterocyclylcarbonyl or a group of the formula: ##STR2## R.sup.2 is alkyl, cycloalkylalkyl or aralkyl; R.sup.3 is hydrogen and R.sup.4 is hydroxy or R.sup.3 and R.sup.4 together are oxo; R.sup.5 is alkoxycarbonyl or alkylcarbamoyl; R.sup.6 and R.sup.7 together are trimethylene or tetramethylene optionally substituted by alkyl or on adjacent carbon atoms by tetramethylene; R.sup.8 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aroyl, aralkanoyl or heteroeyelylearbonyl; and R.sup.9 is alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, cyanoalkyl, carbamoyl-alkyl, alkylthioalkyl, alkoxyalkyl or alkoxycarbonylalkyl:and pharmaceutically acceptable acid addition salts of those compounds of formula I which are basic, inhibit aspartyl proteases of viral origin and can be used in the form of medicaments for the prophylaxis or treatment of viral infections.
    Type: Grant
    Filed: April 5, 1995
    Date of Patent: December 10, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Joseph A. Martin, Gareth J. Thomas
  • Patent number: 5583257
    Abstract: Alkylamino-mercaptoalkylamides have the formula ##STR1## wherein A represents the divalent radical --(CH.sub.2).sub.n --, wherein n is a whole number ranging from 2 to 5, or the divalent radical --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 --,m is 0, 1 or 2,R.sub.1 represents hydrogen or linear or branched lower alkyl having 1-5 carbon atoms,R.sub.2 and R.sub.3, each independently, represent hydrogen or a linear or branched lower alkyl having 1-4 carbon atoms with the proviso that R.sub.2 and R.sub.3 are not hydrogen simultaneously and the salts of the compound of formula I as well as the corresponding disulfides with the exclusion of the disulfide in which A=--(CH.sub.2).sub.2 --, m=0, R.sub.1 and R.sub.2 =H and R.sub.3 =--C.sub.2 H.sub.5. The compound of formula I is used as a reducing agent in a cosmetic composition for the permanent deformation of hair.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: December 10, 1996
    Assignee: L'Oreal
    Inventors: Alex Junino, G erard Malle, Bernadette Luppi
  • Patent number: 5580904
    Abstract: According to the present invention, a novel compound group which can pass through blood-brain barrier (BBB) with carrying a drug thereon and stay within brain to release the drug and a well-known compound group having the properties described above are provided.The compound represented by the general formula ##STR1## wherein, R.sup.1 represents C.sub.1-6 alkyl which may be substituted by a group selected from hydroxyl, carboxyl, amino group which may be substituted by C.sub.1-6 alkyl, and a five- to seven-membered saturated heterocyclic ring,R.sup.2 represents hydrogen or C.sub.1-6 alkyl,R.sup.3 represents hydrogen or C.sub.1-6 alkyl which may be substituted by hydroxyl,R.sup.4 represents hydrogen or C.sub.1-6 alkyl,R.sup.5 represents an amino acid residue, or --S--R.sup.6 or --CO--R.sup.6 wherein R.sup.6 represents C.sub.1-14 alkyl which may be substituted by a five- to seven-membered saturated ring; C.sub.
    Type: Grant
    Filed: June 24, 1994
    Date of Patent: December 3, 1996
    Assignee: Drug Delivery System Institute, Ltd.
    Inventors: Toyoaki Ishikura, Teruomi Ito, Takashi Kato, Kazutoshi Horie, Hiroshi Ishihara, Takashi Senou
  • Patent number: 5536723
    Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.
    Type: Grant
    Filed: October 6, 1994
    Date of Patent: July 16, 1996
    Assignee: Brigham & Women's Hospital
    Inventors: Joseph Loscalzo, John Cooke
  • Patent number: 5532412
    Abstract: An aromatic o-hydroxyamide compound of the formula (I) ##STR1## wherein the formula: ##STR2## is a divalent aromatic group the formula: ##STR3## R.sup.1 =H, halogen, C.sub.1-10 alkyl group, or C.sub.1 -alkoxyl group, Ar.sub.1, Ar.sub.2, Ar.sub.3 =a divalent aromatic groups, X, Y=O or S, and n=0 or 1, has an excellent ultraviolet ray-absorption and heat-resistance and is useful for enhancing an ultraviolet ray-resistance of polymeric materials, for example, wholly aromatic polyamide fibers.
    Type: Grant
    Filed: September 13, 1994
    Date of Patent: July 2, 1996
    Assignee: Teijin Limited
    Inventors: Toshitsugu Matsuki, Toshihiro Santa
  • Patent number: 5527962
    Abstract: New fluorinated derivatives useful as surfactants or in the transport of drug or markers, or in drug targeting, and preparations containing the derivatives, for medical, cosmetic and veterinary uses, having the formula: ##STR1## wherein R.sub.F is a fluorinated radical, X is a linear or branched alkylene, R.sup.1 is H or CH.sub.3, R.sup.2 is a radical having at least one OH group, R.sup.3 is a radical derived from an amino acid or a peptide, 1.ltoreq.n.ltoreq.50 and 0.ltoreq.m.ltoreq.200 with 0.2.ltoreq.n/n+m.ltoreq.1.These derivatives can be used as prodrugs or in formulating pharmaceutical, cosmetic and veterinary preparations, in biology and medicine, notably in compositions acting as carriers of oxygen and other gases, of contrast agents, or as carriers of substances used in therapy, or as carriers of markers.
    Type: Grant
    Filed: May 5, 1994
    Date of Patent: June 18, 1996
    Assignee: Alliance Pharmaceutical Corp.
    Inventors: Andre A. Pavia, Bernard Pucci, Jean G. Riess, Leila Zarif
  • Patent number: 5521160
    Abstract: The present invention is concerned with novel sulfuric acid esters of sugar alcohols and sugar alcohol-like compounds of the formula ##STR1## Also described are methods for the treatment and/or prophylaxis of arteriosclerotic changes in the vascular wall as well as a process for the manufacture of the compounds of formula I and their salts.
    Type: Grant
    Filed: January 4, 1995
    Date of Patent: May 28, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Chucholowski, Jurgen Fingerle, Niggi Iberg, Hans P. Marki, Rita Muller, Michael Pech, Marianne Rouge, Gerard Schmid, Thomas Tschopp, Hans P. Wessel
  • Patent number: 5510530
    Abstract: The invention relates to new optically active sulphur-containing amino acid derivatives, a process for their preparation, their polymerization to give optically active polymers and the use of these optically active polymers as adsorbents for chromatographic separation of racemates into enantiomers.
    Type: Grant
    Filed: May 11, 1994
    Date of Patent: April 23, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Grosse-Bley, Bruno Bomer, Rolf Grosser, Dieter Arlt, Walter Lange
  • Patent number: 5510378
    Abstract: Hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: April 23, 1996
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Kathryn L. Reed
  • Patent number: 5504115
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: April 2, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith