Sulfur Containing Patents (Class 564/154)
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Patent number: 6124502Abstract: 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: GrantFiled: October 9, 1998Date of Patent: September 26, 2000Assignee: American Cyanamid CompanyInventor: Jeremy Ian Levin
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Patent number: 6084065Abstract: 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: GrantFiled: October 4, 1994Date of Patent: July 4, 2000Assignee: Isagro SpaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Ernesto Signorini
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Patent number: 6057322Abstract: 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: GrantFiled: July 30, 1997Date of Patent: May 2, 2000Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 6040339Abstract: 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: GrantFiled: May 28, 1998Date of Patent: March 21, 2000Assignee: Sankyo Company, LimitedInventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
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Patent number: 6034136Abstract: 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: GrantFiled: March 17, 1998Date of Patent: March 7, 2000Assignee: Novartis AGInventor: Cynthia A. Fink
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Patent number: 6034135Abstract: 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: GrantFiled: March 6, 1997Date of Patent: March 7, 2000Assignee: Promega Biosciences, Inc.Inventors: David Aaron Schwartz, Brian Patrick Dwyer, William J. Daily, Kumar Srinivasan, Bob Dale Brown
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Patent number: 6005010Abstract: 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: GrantFiled: August 20, 1997Date of Patent: December 21, 1999Assignee: Hoechst AktiengesellschaftInventors: Jan-Robert Schwark, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Andreas Weichert, Hans-Willi Jansen, Wolfgang Scholz
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Patent number: 5994312Abstract: Compounds of general formula (I): ##STR1## have utility as inhibitors of matrix metalloproteinases and TNF.Type: GrantFiled: July 30, 1998Date of Patent: November 30, 1999Assignee: Darwin Discovery, Ltd.Inventors: John Montana, Andrew Douglas Baxter, David Alan Owen, Robert John Watson, Neil Phillipson
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Patent number: 5981581Abstract: Phenylacetic acid derivatives of the formula I ##STR1##Type: GrantFiled: January 29, 1998Date of Patent: November 9, 1999Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5981490Abstract: Dipeptide compounds have therapeutic utility, inter alia, as metalloproteinase and TNF inhibitors.Type: GrantFiled: October 4, 1996Date of Patent: November 9, 1999Assignee: Darwin Discovery, Ltd.Inventors: Andrew Douglas Baxter, John Gary Montana, David Alan Owen
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Patent number: 5972939Abstract: 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: GrantFiled: October 26, 1998Date of Patent: October 26, 1999Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Robert H. Chen, Min Xiang, John B. Moore, Jr., Mary Pat Beavers
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Patent number: 5968984Abstract: 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: GrantFiled: July 14, 1997Date of Patent: October 19, 1999Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran, Barbara B. Chen
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Patent number: 5969184Abstract: 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: GrantFiled: May 9, 1997Date of Patent: October 19, 1999Assignee: SmithKline Beecham CorporationInventors: 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
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Inhibitors of metalloproteases, pharmaceutical compositions comprising same and methods of their use
Patent number: 5929278Abstract: 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: GrantFiled: May 19, 1998Date of Patent: July 27, 1999Assignee: Affymax Technologies N.V.Inventors: David A. Campbell, Dinesh V. Patel, Xiao-Yi Xiao -
Patent number: 5880147Abstract: 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: GrantFiled: September 18, 1996Date of Patent: March 9, 1999Assignee: Sankyo Company, LimitedInventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
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Patent number: 5856572Abstract: 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: GrantFiled: August 14, 1996Date of Patent: January 5, 1999Assignee: Industrial Technology Research InstituteInventors: Guey-Sheng Liou, Sheng-Huei Hsiao, Jen-Chang Yang
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Patent number: 5852213Abstract: 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: GrantFiled: July 2, 1997Date of Patent: December 22, 1998Assignee: American Cyanamid CompanyInventor: Jeremy Ian Levin
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Patent number: 5847005Abstract: 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: GrantFiled: August 14, 1997Date of Patent: December 8, 1998Assignee: Nippon Soda Co., Ltd.Inventors: Isamu Kasahara, Hirohito Ooka, Shinsuke Sano, Hiroyasu Hosokawa, Homare Yamanaka
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Patent number: 5847206Abstract: 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: GrantFiled: June 7, 1995Date of Patent: December 8, 1998Assignee: Alliance Pharmaceutical Corp.Inventors: Andre Pavia, Bernard Pucci, Jean G. Riess, Leila Zarif
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Patent number: 5840698Abstract: 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: GrantFiled: October 27, 1995Date of Patent: November 24, 1998Assignee: Affymax Technologies N.V.Inventors: David A. Campbell, Dinesh V. Patel, Xiao-Yi Xiao
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Inhibitors of metalloproteases, pharmaceutical compositions comprising same and methods of their use
Patent number: 5831004Abstract: 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: GrantFiled: October 27, 1995Date of Patent: November 3, 1998Assignee: Affymax Technologies N.V.Inventors: David A. Campbell, Dinesh V. Patel, Xiao-Yi Xiao -
Patent number: 5783735Abstract: 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: GrantFiled: May 25, 1995Date of Patent: July 21, 1998Assignee: 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
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Patent number: 5753652Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.Type: GrantFiled: April 4, 1995Date of Patent: May 19, 1998Assignee: Novartis CorporationInventors: Alexander Fassler, Guido Bold, Marc Lang, Shripad Bhagwat, Peter Schneider
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Patent number: 5712417Abstract: 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: GrantFiled: July 11, 1994Date of Patent: January 27, 1998Assignee: Abbott LaboratoriesInventors: Karl-Heinz Budt, Bernd Stowasser, Dieter Ruppert, Christoph Meichsner, Arnold Paessens, Jutta Hansen, Jochen Knolle
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Patent number: 5710311Abstract: 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: GrantFiled: September 29, 1995Date of Patent: January 20, 1998Assignee: L'OrealInventors: Alex Junino, Alain Genet, Alain Lagrange
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Patent number: 5708004Abstract: Hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: January 13, 1998Assignee: Monsanto CompanyInventors: John J. Talley, Kathryn L. Reed
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Patent number: 5708034Abstract: 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: GrantFiled: October 31, 1996Date of Patent: January 13, 1998Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans Jochen Lang, Udo Albus, Wolfgang Scholz
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Patent number: 5696071Abstract: 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: GrantFiled: January 7, 1997Date of Patent: December 9, 1997Assignee: Kao CorporationInventors: Akiko Okutsu, Tomohito Kitsuki, Katsumi Kita
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Patent number: 5696282Abstract: 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: GrantFiled: March 26, 1996Date of Patent: December 9, 1997Assignee: Phillips Petroleum CompanyInventors: James E. Shaw, Harry Porter
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Patent number: 5686633Abstract: 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: GrantFiled: December 31, 1991Date of Patent: November 11, 1997Assignee: Ciba Specialty Chemicals CorporationInventors: Eric Vieira, Hugh Stephen Laver
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Patent number: 5672759Abstract: 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: GrantFiled: January 19, 1996Date of Patent: September 30, 1997Assignee: L'OrealInventors: Alex Junino, Alain Genet, Alain Lagrange
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Patent number: 5672765Abstract: 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: GrantFiled: July 14, 1995Date of Patent: September 30, 1997Assignee: Bayer AktiengesellschaftInventors: Albrecht Marhold, Marianne Lohr, Heinrich Wamhoff
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Patent number: 5663436Abstract: 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: GrantFiled: May 1, 1996Date of Patent: September 2, 1997Assignee: Sumitomo Chemical Company, LimitedInventors: Akiko Kakimizu, Kenji Arai, Norio Kimura, Tomohiro Teramae
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Patent number: 5654301Abstract: The present invention relates to compounds of the formula ##STR1##Type: GrantFiled: January 12, 1993Date of Patent: August 5, 1997Assignee: Research Corporation Technologies, Inc.Inventors: Harold L. Kohn, Darrell Watson
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Patent number: 5641820Abstract: 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: GrantFiled: December 26, 1995Date of Patent: June 24, 1997Assignee: The Goodyear Tire & Rubber CompanyInventors: Lawson Gibson Wideman, Paul Harry Sandstrom
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Patent number: 5633403Abstract: 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: GrantFiled: June 6, 1995Date of Patent: May 27, 1997Assignee: Croda, Inc.Inventors: Kevin F. Gallagher, Abel G. Pereira
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Patent number: 5629347Abstract: 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: GrantFiled: December 22, 1993Date of Patent: May 13, 1997Assignee: Merck Sharp & Dohme Ltd.Inventors: Christopher J. Swain, Martin R. Teall, Brian J. Williams
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Patent number: 5629343Abstract: 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: GrantFiled: February 23, 1995Date of Patent: May 13, 1997Assignee: Merck & Co., Inc.Inventors: William Hagmann, Ihor Kopka
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Patent number: 5625075Abstract: 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: GrantFiled: June 2, 1995Date of Patent: April 29, 1997Assignee: NeoRx CorporationInventors: Ananthachari Srinivasan, Alan R. Fritzberg, David S. Jones
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Patent number: 5587513Abstract: The present invention relates to novel polyether-substituted compounds of imides and their use as surface-active agents.Type: GrantFiled: January 20, 1995Date of Patent: December 24, 1996Inventors: Klaus Pohmer, Rainer Weber, Cornelia D orzbach-Lange, Reinhard Haida, Hans-Heinrich Moretto
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Patent number: 5583248Abstract: 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: GrantFiled: April 5, 1995Date of Patent: December 10, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Joseph A. Martin, Gareth J. Thomas
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Patent number: 5583257Abstract: 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: GrantFiled: May 18, 1995Date of Patent: December 10, 1996Assignee: L'OrealInventors: Alex Junino, G erard Malle, Bernadette Luppi
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Patent number: 5580904Abstract: 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: GrantFiled: June 24, 1994Date of Patent: December 3, 1996Assignee: Drug Delivery System Institute, Ltd.Inventors: Toyoaki Ishikura, Teruomi Ito, Takashi Kato, Kazutoshi Horie, Hiroshi Ishihara, Takashi Senou
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Patent number: 5536723Abstract: 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: GrantFiled: October 6, 1994Date of Patent: July 16, 1996Assignee: Brigham & Women's HospitalInventors: Joseph Loscalzo, John Cooke
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Patent number: 5532412Abstract: 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: GrantFiled: September 13, 1994Date of Patent: July 2, 1996Assignee: Teijin LimitedInventors: Toshitsugu Matsuki, Toshihiro Santa
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Patent number: 5527962Abstract: 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: GrantFiled: May 5, 1994Date of Patent: June 18, 1996Assignee: Alliance Pharmaceutical Corp.Inventors: Andre A. Pavia, Bernard Pucci, Jean G. Riess, Leila Zarif
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Patent number: 5521160Abstract: 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: GrantFiled: January 4, 1995Date of Patent: May 28, 1996Assignee: 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
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Patent number: 5510530Abstract: 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: GrantFiled: May 11, 1994Date of Patent: April 23, 1996Assignee: Bayer AktiengesellschaftInventors: Michael Grosse-Bley, Bruno Bomer, Rolf Grosser, Dieter Arlt, Walter Lange
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Patent number: 5510378Abstract: Hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: April 23, 1996Assignee: G.D. Searle & Co.Inventors: John J. Talley, Kathryn L. Reed
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Patent number: 5504115Abstract: 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: GrantFiled: June 28, 1994Date of Patent: April 2, 1996Assignee: Merck & Co., Inc.Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith