Chalcogen Or Nitrogen Attached Directly To The Tetrazole Ring By Nonionic Bonding Patents (Class 548/251)
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Patent number: 5646292Abstract: Disclosed is a novel blowing agent of tetrazoles and their derivatives. The blowing agent comprising tetrazole derivatives is harmless, odorless and inexpensive. Moreover, the agent is low in physical sensitivities and safe in use, and generates clean gas by being sharply decomposed only due to temperature. The blowing agent of tetrazoles and their derivatives employs aminotetrazole derivatives represented by the general formula (1). The blowing agent offers foaming agents for resin molded bodies having good thermal properties, inflators for air bags serving as automobile safety protection, or smoking agents for diffusing chemicals by a low-cost inexpensive synthetic process.Type: GrantFiled: May 6, 1996Date of Patent: July 8, 1997Assignee: Toyo Kasei Kogyo Company LimitedInventors: Satoshi Nakagawa, Hideki Ogawa, Hiroaki Tanaka, Atsuhiro Onishi
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Patent number: 5641798Abstract: This invention provides novel bicyclic compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides intermediates useful in the synthesis of excitatory amino acid antagonists.Type: GrantFiled: June 1, 1995Date of Patent: June 24, 1997Assignee: Eli Lilly and CompanyInventor: James A. Monn
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Patent number: 5633387Type: GrantFiled: April 10, 1996Date of Patent: May 27, 1997Assignee: Nihon Bayer Agrochem K.K.Inventor: Fritz Maurer
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Patent number: 5612360Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: April 20, 1993Date of Patent: March 18, 1997Assignee: Eli Lilly and CompanyInventors: Donald B. Boyd, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, K. Jeff Thrasher, Venkatraghavan Vasudevan, Celia A. Whitesitt
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Patent number: 5612480Abstract: Novel 2-chloro and 2-bromo derivatives of 1,5-iminosugars are disclosed, especially such derivatives of 1,5-dideoxy-1,5-imino-D-glucitol. These compounds are useful inhibitors of glucosidase enzymes and also are useful as antiviral agents and as intermediates for the synthesis of other enzyme inhibitors and antiviral compounds.Type: GrantFiled: March 6, 1995Date of Patent: March 18, 1997Assignee: G. D. Searle & Co.Inventors: Thomas E. Barta, Richard A. Mueller
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Patent number: 5608074Abstract: An improved process for the preparation of 3-chlorobenzo[b]thiophene-2-carbonyl chlorides is described where a cinnamic acid is converted in the presence of thionyl chloride and a 4-N,N'-disubstituted aminopyridine in one step to the desired product.Type: GrantFiled: December 19, 1994Date of Patent: March 4, 1997Assignee: Warner-Lambert CompanyInventor: Jonathan Walker
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Patent number: 5607957Abstract: A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: September 29, 1994Date of Patent: March 4, 1997Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose L. Castro Pineiro, Victor G. Matassa
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Patent number: 5605920Abstract: Disclosed are herbicidal tetrazolinone derivatives, selective in paddy fields of the formula ##STR1## wherein X represents C.sub.1-4 alkyl,n represents 1, 2, 3 or 4,R.sup.1 and R.sup.2 each independently represents C.sub.1-6 alkyl, C.sub.2-4 alkenyl, C.sub.2-6 alkynyl, C.sub.3-8 cycloalkyl, aryl which may optionally be substituted (wherein the substituent is at least one radical selected from the group consisting of halogen, C.sub.1-4 alkyl, C.sub.1-2 haloalkyl, C.sub.1-2 haloalkoxy, C.sub.1-2 haloalkylthio, acyl, nitro and cyano) or aralkyl optionally substituted by halogen orR.sup.1 and R.sup.2 form, together with the N-atom to which they are bonded, a cyclic ring which may be substituted. Also, disclosed are novel intermediates useful in the preparation of the compounds of formula (I).Type: GrantFiled: March 20, 1996Date of Patent: February 25, 1997Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Yoshinori Kitagawa, Seishi Ito, Katsuhiko Shibuya, Tatsuya Yamaoka, Chieko Ueno, Yoshiko Kyo
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Patent number: 5594146Abstract: A process for producing 5-aminotetrazole comprising the steps of: reacting cyanamide with hydrazine in a solvent to form a salt of aminoguanidine; adding thereto an acid and then a nitrite to form a salt of diazoguanidine; and cyclizing the salt of diazoguanidine, upon heating, to thereby produce the 5-aminotetrazole, without isolating the intermediate product and also a process for producing 5-aminotetrazole or a metal salt thereof in the form of powder by spray drying.Type: GrantFiled: February 22, 1995Date of Patent: January 14, 1997Assignee: Nippon Carbide Kogyo Kabushiki KaishaInventors: Masahiro Murotani, Hajime Mura, Makoto Takeda, Hiroshi Shibafuchi
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Patent number: 5591862Abstract: Novel tetrazole derivatives represented by the formula ##STR1## wherein n denotes an integer of 1 to 3; A is an optionally substituted heterocyclic residue; Y is a divalent hydrocarbon residue; and X is CH or N, or pharmaceutically acceptable salts thereof have excellent hypoglycemic and hypolipidemic activities.Type: GrantFiled: June 8, 1994Date of Patent: January 7, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Hitoshi Ikeda, Yu Momose
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Patent number: 5589439Abstract: Herbicidal novel tetrazolinone derivatives of the formula: ##STR1## wherein R.sup.1 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl, alkoxy or phenyl which is optionally substituted, andR.sup.2 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl, alkoxy or phenyl which is optionally substituted, orR.sup.1 and R.sup.2 form, together with the nitrogen atom to which R.sup.1 and R.sup.2 are bonded, a 5- or 6-membered heterocyclic ring, optionally fused to a carbocyclic ring optionally and independently substituted by C.sub.1-4 alkyl, andR.sup.3 is a 5-membered heterocyclic radical containing at least one hereto atom selected from the group consisting of nitrogen, oxygen, and sulfur, optionally substituted by at least one substitutent selected from the group consisting of halogen, benzyl, phenyl, halogen-substituted phenyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkyl-sulfonyl and C.sub.Type: GrantFiled: July 28, 1995Date of Patent: December 31, 1996Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Koichi Moriya, Fritz Maurer, Seishi Ito, Katsuaki Wada, Kazuhiro Ukawa, Ryo Watanabe, Asami Ito, Natsuko Minegishi
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Patent number: 5576443Abstract: Disclosed is a novel near-infrared absorbing dye of formula: ##STR1## wherein X.sup.1, X.sup.2 independently represents --CR.sup.8 R.sup.9 --, --S--, --Se--, --NR.sup.10 --, --CH.dbd.CH-- or --O--;n is an integer of 2 or 3;R.sup.1 and R.sup.2 independently represent alkyl of 1 to 10 carbons or substituted alkyl of 1 to 10 carbons;R.sup.3 represents a ring chosen from a set consisting of aryl, substituted aryl, and a heterocyclic ring of a type present in photographic emulsions;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently represent hydrogen, alkyl of 1-10 carbons, substituted alkyl of 1-10 carbons, R.sup.4 and R.sup.5 taken together or R.sup.6 and R.sup.7 taken together can represent atoms necessary to form a 5 or 6-membered aliphatic ring, an aromatic six-membered ring, an aromatic 10-membered ring, a substituted aromatic six-member ring or a substituted aromatic 10-member ring;R.sup.8, R.sup.Type: GrantFiled: March 30, 1995Date of Patent: November 19, 1996Assignee: Sterling Diagnostic Imaging, Inc.Inventors: Dietrich M. Fabricius, Gregory C. Weed
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Patent number: 5573999Abstract: .beta.-Substituted cinnamic acid derivatives of the formula 1, ##STR1## where R.sup.1 is alkyl, chlorine or bromine, --X-- is --O--, --S--, ##STR2## m is 0 or 1, --Y is --OR.sup.4, --O--N.dbd.CR.sup.5 R.sup.6, --NR.sup.7 R.sup.8, --N(OR.sup.9)R.sup.10 or --SR.sup.11, where the above-mentioned substituents R.sup.2 to R.sup.11 are alkyl, and R.sup.2, and R.sup.3 and R.sup.5 to R.sup.11 can also be hydrogen,Z is halogen, nitro, cyano, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, arylthioalkyl, hetarylalkyl, hetaryloxyalkyl, hetarylthioalkyl, alkenyl, aralkenyl, aryloxyalkenyl, arylthioalkenyl, hetarylalkenyl, hetaryloxyalkenyl, hetarylthioalkenyl, alkynyl, arylalkynyl, hetarylalkynyl, aryl, hetaryl, arylazo, acylamino, --OR.sup.12, --SR.sup.13, --SOR.sup.14, --SO.sub.2 R.sup.15, --COOR.sup.16, --CONR.sup.17 R.sup.18, --COR.sup.19, --CR.sup.20 .dbd.NR.sup.21, --N.dbd.CR.sup.22, R.sup.23, --CR.sup.24 .dbd.N--OR.sup.25, --CR.sup.25 R.sup.26 --O--, N.dbd.CR.sup.27 R.sup.28, --CH.sub.2 --OCOR.sup.39 or --NR.sup.37 R.Type: GrantFiled: May 15, 1995Date of Patent: November 12, 1996Assignee: BASF AktiengesellschaftInventors: Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Horst Wingert, Wolfgang von Deyn, Wassilios Grammenos, Hartmann Koenig, Harald Rang, Franz Roehl, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5565480Abstract: Angiotensin II receptor antagonists having the formula: ##STR1## which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma, pharmaceutical compositions including these antagonists, and methods of using these compounds to produce angiotensin II receptor antagonism in mammals.Type: GrantFiled: May 2, 1995Date of Patent: October 15, 1996Assignee: SmithKline Beecham CorporationInventors: John G. Gleason, Judith Hempel, David T. Hill, James Samanen, Joseph Weinstock
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Patent number: 5554633Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.Type: GrantFiled: January 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme, Ltd.Inventor: Martin R. Teall
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Patent number: 5541336Abstract: Novel herbicidal tetrazolinones of the formula ##STR1## wherein Y is hydrogen, bromine or methyl,R.sup.1 is ethyl or n-propyl, andR.sup.2 is cyclopentyl or cyclohexyl, with the proviso that the total number of carbon atoms in R.sup.1 and R.sup.2 is 7 or 8.The new tetrazolinones may be mixed with other herbicides.Type: GrantFiled: March 10, 1995Date of Patent: July 30, 1996Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Seishi Ito, Yukiyoshi Watanabe, Shin-ichi Narabu, Akihiko Yanagi
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Patent number: 5539123Abstract: A compound of the formula ##STR1## wherein R and R' together represent a primary or a secondary aliphatic amine. Also described are elastase enzyme inhibitory compositions including a carrier and an elastase enzyme inhibiting amount of the compounds of the invention. A method of selectively inhibiting the enzyme elastase in an animal or a human in need of such treatment includes administering to the animal or human an enzyme elastase inhibiting amount of one of the compounds of the invention or a composition thereof.Type: GrantFiled: August 26, 1994Date of Patent: July 23, 1996Assignee: University of Kentucky Research FoundationInventors: George A. Digenis, Nikolaos P. Rodis
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Patent number: 5530135Abstract: 1-Substituted-5(4H)-tetrazolinones of the formula (I) ##STR1## wherein R is alkyl, haloalkyl, cycloalkyl, phenyl, substituted phenyl or aralkyl, are obtained in very good yields by reacting, in a polar solvent, an isocyanate of the formula R-NCO (II) with sodium azide (NaN.sub.3) in a molar ratio of 1:1 and in the presence of aluminum chloride (AlCl.sub.3), followed by the addition of water and a mineral acid in excess.Type: GrantFiled: July 29, 1994Date of Patent: June 25, 1996Assignee: Nihon Bayer Agrochem K.K.Inventors: Akihiko Yanagi, Yukiyoshi Watanabe, Shin-ichi Narabu
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Patent number: 5523312Abstract: Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1## wherein Het.sub.1 is chosen from the group consisting of oxazolyl, isoxazolyl, oxadiazolyl;Y is an alkylene bridge of 3 to 9 carbon atoms;Het.sub.2 is benzofuranyl or indolyl;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, acetyl, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluromethyl, or cyano; andR.sub.3 is oxazolyl, oxadiazolyl, isoxazolyl or any of these substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: September 27, 1994Date of Patent: June 4, 1996Assignee: Sterling Winthrop Inc.Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Gee-Hong Kuo, Theodore J. Nitz, Michael Reuman
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Patent number: 5519142Abstract: Compound of the general formula ##STR1## wherein R is an ester-activating group, m and n are identical or different and 0-6, p=0, 2-4, and q and s=1, p=0 if s=0 and p=2-4 if s=1. The compound is novel and suitable for the reproducible coupling of immunological substances at a high yield.Type: GrantFiled: March 29, 1994Date of Patent: May 21, 1996Assignee: Boehringer Mannheim GmbHInventors: Eva Hoess, Erasmus Huber, Christine Markert-Hahn, Beatus Ofenloch-Haehnle
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Patent number: 5519043Abstract: The compound having the formula: ##STR1## and a method of treating an inflammatory condition comprising administering to an animal in need of such treatment an effective amount of at least one compound represented by the formula.Type: GrantFiled: May 5, 1993Date of Patent: May 21, 1996Assignee: Scios Nova Inc.Inventor: John J. Perumattam
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Patent number: 5512681Abstract: Novel imidazolinone derivatives of formula (I), which are useful as angiotensin II antagonists, are disclosed: ##STR1##Type: GrantFiled: September 30, 1993Date of Patent: April 30, 1996Assignee: E. I. Du Pont de Nemours and CompanyInventors: George A. Boswell, Indawati DeLucca, Mimi L. Quan
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Patent number: 5510379Abstract: .beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, 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: GrantFiled: December 19, 1994Date of Patent: April 23, 1996Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5508419Abstract: This invention relates to novel bis-biphenyl substituted 3-mercapto-1,2,4-tetrazoles and to pharmaceutically acceptable salts thereof.The compounds are angiotensin II receptor antagonists, and are useful in treating hypertension (lowering high blood pressure), congestive heart failure, elevated ocular pressure, cerebral stroke, angina, cardiac insufficiency, myocardial infarction or diabetic nephropathy.The invention also relates to a pharmaceutical composition comprising a compound of the invention, a method of treating a physiological condition in a mammal that is mediated by angiotensin II which comprises administering to the mammal an effective amount of a compound of the invention, and novel processes for preparing the compounds of the invention.Type: GrantFiled: September 9, 1994Date of Patent: April 16, 1996Assignee: Ortho Pharmaceutical CorporationInventors: Victor T. Bandurco, William V. Murray, Michael P. Wachter, Charles F. Schwender
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Patent number: 5506243Abstract: Since sulfonamide derivatives of the present invention show strong inhibitory activity against cysteine protease such as calpain papain, cathepsin B, cathepsin H, cathepsin L, they can be used as remedies for muscular dystrophy, cataract, myocardial infarction, stroke, Alzheimer's disease, amyotrophia, osteoporosis, hypercalcemia or the like.Type: GrantFiled: April 28, 1994Date of Patent: April 9, 1996Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Toshiro Sakaki, Chizuko Takahashi, Yoshiyuki Fujimura
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Patent number: 5502204Abstract: A process for the preparation of a 1-substituted-5(4H)-tetrazolinone of the formula ##STR1## wherein R.sub.1 is defined in the specificationn is 0, 1, 2, 3 or 4,which comprises reacting a 1-substituted-5(4H)-tetrazolinethione of the formula ##STR2## with an ethylene oxide of the formula ##STR3## wherein R.sup.2 represents hydrogen, methyl or ethyl,in the presence of a base and in the presence of water, an alcohol or a mixture thereof.Type: GrantFiled: September 7, 1994Date of Patent: March 26, 1996Assignee: Nihon Bayer Agrochem K.K.Inventors: Akihiko Yanagi, Yukiyoshi Watanabe, Shin-ichi Narabu
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Patent number: 5495023Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4whereinY is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.Type: GrantFiled: May 3, 1994Date of Patent: February 27, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
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Patent number: 5494925Abstract: 2-Heterocyclyloxymethyl and 2-heterocyclylthiomethyL-1,2,5-thiadiazolidin-3-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.Type: GrantFiled: December 2, 1994Date of Patent: February 27, 1996Assignee: Sterling Winthrop Inc.Inventors: John J. Court, Ranjit C. Desai, Dennis J. Hlasta
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Patent number: 5491241Abstract: This invention provides novel bicyclic compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides intermediates useful in the synthesis of excitatory amino acid antagonists.Type: GrantFiled: October 18, 1993Date of Patent: February 13, 1996Assignee: Eli Lilly and CompanyInventor: James A. Monn
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Patent number: 5489693Abstract: Cyclic imino derivatives of the formula ##STR1## wherein X and R.sub.a to R.sub.g are as defined herein, useful for their inhibitory effects on aggregation, pharmaceutical compositions containing the compounds and processes for preparing them.Type: GrantFiled: April 26, 1993Date of Patent: February 6, 1996Inventors: Guenter Linz, Volkhard Austel, Frank Himmelsbach, Johannes Weisenberger, Thomas Mueller, Helmut Pieper, Elke Seewaldt-Becker
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Patent number: 5484935Abstract: Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 and R.sup.3 are each C.sub.1-4 alkyl or C.sub.1-4 alkyl-carbonyl, and R.sup.2 is carboxy, tetrazolyl, C.sub.1-4 alkyl-sulphonamido or --CR.sup.4 R.sup.5 CO.sub.2 H where R.sup.4 and R.sup.5 are each hydrogen or C.sub.1-4 alkyl; provided that when R.sup.1 and R.sup.3 are both methyl and when R.sup.1 and R.sup.3 are both methylcarbonyl, R.sup.2 is not carboxy; and salts and esters thereof.Type: GrantFiled: August 11, 1994Date of Patent: January 16, 1996Assignee: Lilly Industries LimitedInventors: Peter T. Gallagher, Terence A. Hicks, William M. Owton
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Patent number: 5484780Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their methods of use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: December 14, 1994Date of Patent: January 16, 1996Assignee: Eli Lilly and CompanyInventors: Donald B. Boyd, Kenneth L. Hauser, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Kumiko Takeuchi, K. Jeff Thrasher, Celia A. Whitesitt
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Patent number: 5482960Abstract: Novel indole and indoline nonpeptide antagonists of endothelin I are described, as well as novel intermediates used in their preparation, methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure and subarachnoid hemorrhage.Type: GrantFiled: November 14, 1994Date of Patent: January 9, 1996Assignee: Warner-Lambert CompanyInventors: Kent A. Berryman, Amy M. Bunker, Annette M. Doherty, Jeremy J. Edmunds
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Patent number: 5482957Abstract: Azole derivatives, process for their preparation, and their useAzole derivatives of the formula (I) ##STR1## in which A, L, O, R.sup.1, X, Y, Z and q have the meanings given, process for their preparation, pharmaceutical preparations and the use of the compounds are described. Azole derivatives of the formula I where the symbols have for example the following meanings:R.sup.1 is (C.sub.2 -C.sub.10)-alkyl,Z is nitrogen,X and Y are independently of one another CR.sup.2,L is --CH.sub.2 --,q is zero or 1,A is a biphenyl radical which is substituted for example by R.sup.15,R.sup.2 is halogen or hydrogen,R.sup.15 is SO.sub.2 --NH--CO--OR.sup.6 andR.sup.6 is phenyl,are highly active antagonists of angiotensin II receptors.Type: GrantFiled: April 28, 1994Date of Patent: January 9, 1996Assignee: Hoechst AktiengesellschaftInventors: Adalbert Wagner, Heinrich Englert, Heinz-Werner Kleemann, Hermann Gerhards, Bernward Scholkens, Reinhard Becker, Wolfgang Linz, Jean-Paul Vevert, John-Claude Caille
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Patent number: 5472973Abstract: The compound having the formula: ##STR1## and a method of treating an inflammatory condition comprising administering to an animal in need of such treatment an effective amount of at least one compound represented by the formula.Type: GrantFiled: December 4, 1992Date of Patent: December 5, 1995Assignee: Scios Nova Inc.Inventor: John J. Perumattam
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Patent number: 5468866Abstract: Methods of preparing bis-(1(2)H-tetrazol-5-yl)-amine (BTA) having improved physical and chemical characteristics are disclosed. In the process, a dicyanamide salt and an azide salt are reacted at high temperature in the presence of an acid reagent. Best yields are obtained when the reaction is allowed to proceed for approximately 48 hours. The dicyanamide salt is preferably present in a stoichiometric excess. The acid reagent has a pK.sub.a in the range from about 3 to about 9. The reaction mixture is acidified to a pH less than 3. Several variations of the acidification step permit control of particle size and morphology. Small, rounded particles are prepared by rapidly cooling the hot crude reaction product coincidentally with acidification. This is preferably accomplished by adding the hot crude reaction product directly to cold concentrated acid. The precipitated particles are isolated to yield BTA.Type: GrantFiled: January 4, 1994Date of Patent: November 21, 1995Assignee: Thiokol CorporationInventors: Thomas K. Highsmith, Robert M. Hajik, Robert B. Wardle, Gary K. Lund, Reed J. Blau
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Patent number: 5466820Abstract: An azole compound represented by the formula (I): ##STR1## wherein Ar is a substituted phenyl group; R.sup.1 and R.sup.2 independently are a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 may combine together to form a lower alkylene group; R.sup.3 is a group bonded through a carbon atom; R.sup.4 is a hydrogen atom or an acyl group; X is a nitrogen atom or a methine group; and Y and Z independently are a nitrogen atom or a methine group which may optionally be substituted with a lower alkyl group, or a salt thereof, which is useful for prevention and therapy of fungal infections of mammals as antifungal agent.Type: GrantFiled: August 19, 1994Date of Patent: November 14, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Katsumi Itoh, Kenji Okonogi, Norikazu Tamura
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Patent number: 5463071Abstract: Compounds of the formula ##STR1## wherein X.sub.1 to X.sub.5 are as defined herein, the tautomers, the stereoisomers including the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases. The compounds are useful for inhibiting undesirable cell aggregation.Type: GrantFiled: November 8, 1993Date of Patent: October 31, 1995Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Guenter Linz, Volkhard Austel, Helmut Pieper, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
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Patent number: 5461049Abstract: Amide tetrazoles of the formula ##STR1## wherein aryl includes phenyl and naphthyl, unsubstituted or substituted, X is .dbd.O, .dbd.N--R.sub.5, or --NR.sub.3 R.sub.4, where R.sub.2, R.sub.4, and R.sub.5 include alkyl and alkoxy and R.sub.3 includes alkyl, are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia or atherosclerosis.Type: GrantFiled: May 27, 1994Date of Patent: October 24, 1995Assignee: Warner-Lambert CompanyInventors: Patrick M. O'Brien, Drago R. Sliskovic
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Patent number: 5459144Abstract: The invention relates to compounds of the formula ##STR1## wherein Z, X, Q, Y, W, and W' are as described herein. These compounds have antiviral activity, and certain of these compounds have antiinflammatory activity and are PAF inhibitors.Type: GrantFiled: December 17, 1993Date of Patent: October 17, 1995Assignee: Schering CorporationInventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace
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Patent number: 5455222Abstract: Disclosed are substituted-5-thiomethylthiocyanato-1H-tetrazole compounds corresponding to the formula ##STR1## wherein R represents a C.sub.1 -C.sub.6 straight or branched chain alkyl radical, a C.sub.3 -C.sub.6 cycloalkyl or a phenyl radical of the formula ##STR2## wherein each X independently represents hydrogen, halo, a C.sub.1 -C.sub.6 straight or branched chain alkyl radical, a C.sub.3 -C.sub.6 cycloalkyl radical, a C.sub.1 -C.sub.6 straight or branched chain alkoxy radical, a C.sub.3 -C.sub.6 cycloalkoxy radical, cyano or nitro and n is 0-5.These compounds have been found to exhibit antimicrobial and marine antifouling activity in industrial and commercial applications and compositions containing these compounds are so employed.Type: GrantFiled: December 21, 1994Date of Patent: October 3, 1995Assignee: The Dow Chemical CompanyInventors: Ravi B. Shankar, Duane R. Romer, R. Garth Pews
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Patent number: 5451682Abstract: A process of preparing 5-aminotetrazole ("5-AT") which proceeds at substantially neutral pH is disclosed. In the process, cyanamide or dicyandiamide and an azide salt are reacted at elevated temperature in the presence of an acid reagent. The acid reagent has a pK.sub.a in the range from about 3 to about 7. Large quantities of hydrazoic acid are not produced during the reaction. Upon completion of the reaction, the reaction mixture is acidified to a pH less than 3 to protonate the 5-AT. Several variations of the acidification step permit control of particle size and morphology. The precipitated particles are isolated to yield 5-AT.Type: GrantFiled: January 10, 1994Date of Patent: September 19, 1995Assignee: Thiokol CorporationInventors: Thomas K. Highsmith, Gary K. Lund
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Patent number: 5451597Abstract: A class of N-substituted (.alpha.-imidazolyltoluyl)pyrrole compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein R.sup.0 is selected from CH.sub.2 OH, CO.sub.2 H, CHO, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, CH.sub.2 OCH.sub.3, CH.sub.2 OCHOCH.sub.3 and CH.sub.2 --CO.sub.2 C.sub.2 H.sub.5 ; wherein R.sup.1 is selected from Cl, CF.sub.3, CHO, n-butyl, cyano, CO.sub.2 CH.sub.3 and CO.sub.2 CH.sub.2 CH.sub.3 ; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, propylthio, butylthio and hydroxyalkyl; wherein each of R.sub.3, R.sub.4, R.sup.6, R.sup.7, R.sup.9 and R.sup.10 is hydrido; wherein each of R.sup.5 and R.sup.Type: GrantFiled: May 27, 1993Date of Patent: September 19, 1995Assignee: G.D. Searle & Co.Inventors: Philippe R. Bovy, Joe T. Collins, Robert E. Manning
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Patent number: 5447949Abstract: Angiotensin II receptor antagonists having the formula: ##STR1## which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma, pharmaceutical compositions including these antagonists, and methods of using these compounds to produce angiotensin II receptor antagonism in mammals.Type: GrantFiled: November 15, 1993Date of Patent: September 5, 1995Assignee: SmithKline Beecham CorporationInventors: Gerald R. Girard, David T. Hill, Joseph Weinstock
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Patent number: 5440042Abstract: Disclosed is a novel near-infrared absorbing dye of formula: ##STR1## wherein X.sup.1, X.sup.2 independently represents --CR.sup.8 R.sup.9 --, --S--, --Se--, --NR.sup.10 --, --CH.dbd.CH-- or --O--;n is an integer of 2 or 3;R.sup.1 and R.sup.2 independently represent alkyl of 1 to 10 carbons or substituted alkyl of 1 to 10 carbons;R.sup.3 represents a ring chosen from the set consisting of aryl, substituted aryl, and heterocyclic containing 5 or 6 carbons in the ring;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently represent hydrogen, alkyl of 1-10 carbons, substituted alkyl of 1-10 carbons, R.sup.4 and R.sup.5 taken together or R.sup.6 and R.sup.7 taken together may represent the atoms necessary to form a 5 or 6-membered aliphatic ring, an aromatic six-membered ring, an aromatic 10-membered ring, a substituted aromatic six-member ring or a substituted aromatic 10-member ring;R.sup.8, R.sup.Type: GrantFiled: May 26, 1993Date of Patent: August 8, 1995Assignee: E. I. Du Pont de Nemours and CompanyInventors: Dietrich M. Fabricius, Gregory C. Weed
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Patent number: 5424449Abstract: The compound 5-aminotetrazole is prepared by a process which comprises (a) reacting a hydrazine salt of a mineral acid with cyanamide to form the corresponding aminoguanidine salt, (b) diazotizing the aminoguanidine salt to the corresponding guanylazide salt, and (c) cyclizing the guanylazide salt to 5-aminotetrazole.Type: GrantFiled: October 28, 1994Date of Patent: June 13, 1995Assignee: Olin CorporationInventors: Eugene F. Rothgery, Karl O. Knollmueller
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Patent number: 5412117Abstract: Benzopyran derivatives represented by formula (I): ##STR1## wherein X represents =O, =S, =N-Z (Z represents a lower alkyl group, etc.), or =CHNO.sub.2 ; Y represents a substituted amino group, an alkoxy group, an alkylthio group, etc., and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 each represent a hydrogen atom, a lower alkyl group, etc., are disclosed. The benzopyran derivatives exhibit K.sup.+ channel activating activities and are widely applicable as antiasthmatics, antiepileptics, and the like.Type: GrantFiled: January 26, 1993Date of Patent: May 2, 1995Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Koga, Hiroyuki Nabata
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Patent number: 5405969Abstract: The invention provides a process for making a thioether compound having the formula:A--S--Rcomprising reacting:(1) Compound I having the formula:A--H (I)where A comprises a carbon atom bonded to H where that carbon is either capable of ionizing to a nucleophilic state or is conjugated to such an atom, with(2) Compound II having the formula:H--SR or RSSR (II)wherein R is selected from the group consisting of:(a) a substituted or-unsubstituted aryl group or alicyclic group, said groups being carbocyclic or heterocyclic, and(b) a thiocarbonyl group,in the presence of a base and an oxidizing agent that is free of reactive halogen and that is capable of oxidizing H--SR to RSSR.Type: GrantFiled: December 10, 1993Date of Patent: April 11, 1995Assignee: Eastman Kodak CompanyInventors: Charles W. Wright, Joan C. Potenza, John E. Leary, Jr., Chang K. Kim
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Patent number: 5393768Abstract: This invention provides novel benzene derivatives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.Type: GrantFiled: July 16, 1993Date of Patent: February 28, 1995Assignee: Eli Lilly and CompanyInventor: Robert D. Dillard
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Patent number: 5389660Abstract: There are disclosed new substituted imidazo-fused 5-membered ring heterocyclic compounds and derivatives thereof which are useful as angiotensin II antagonists.Type: GrantFiled: October 7, 1992Date of Patent: February 14, 1995Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, David B. R. Johnston, Malcolm MacCoss, Nathan B. Mantlo, Arthur A. Patchett, Prasun K. Chakravarty, Thomas F. Walsh