Chalcogen Or Nitrogen Attached Directly To The Tetrazole Ring By Nonionic Bonding Patents (Class 548/251)
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Patent number: 5389634Abstract: Imidazoles of the formula ##STR1## and their non-toxic, pharmaceutically acceptable salts with acids and bases having an antagonistic activity against angiotensin II receptors.Type: GrantFiled: June 9, 1993Date of Patent: February 14, 1995Assignee: Roussel-UclafInventors: Michel Fortin, Daniel Frechet, Gilles Hamon, Simone Jouquey, Jean-Paul Vevert
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Patent number: 5389663Abstract: An azole compound represented by the formula (I): ##STR1## wherein X is a nitrogen atom; Ar is a phenyl group substituted by halogen or a halogenated C.sub.1-4 alkyl 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; n denotes an integer of 0 to 2; and R.sup.7 is a hydrogen atom, a hydroxyl group which may be optionally acylated by an acyl group selected from acetyl, propionyl, butyryl, isobutyryl, phenylacetyl and benzoyl, or may form a bond together with R.sup.1 ; or a salt thereof.Type: GrantFiled: November 24, 1993Date of Patent: February 14, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Katsumi Itoh, Kenji Okonogi, Akihiro Tasaka
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Patent number: 5384407Abstract: A compound of the formula ##STR1## V, W, Y, and Z are each independently C--H, oxygen, nitrogen, or sulfur; T is C--H or nitrogen;n is 0 or 1;R.sup.4 is hydrogen or one, two or three substituents independently selected from C.sub.1 -C.sub.4 -alkyl, halo-substituted C.sub.1 -C.sub.4 -alkyl, hydroxy-substituted C.sub.1 -C.sub.4 -alkyl, halogen, hydroxy, C.sub.1 -C.sub.4 -alkoxy, mercapto, amino, mono-(C.sub.1 -C.sub.4 -alkyl)amino, di-(C.sub.1 -C.sub.4 -alkyl)amino, formamido, mono-(C.sub.1 -C.sub.4 -alkyl)amido, di-(C.sub.1 -C.sub.4 -alkyl)amido, cyano, nitro, C.sub.1 -C.sub.4 -alkoxycarbonyl, carboxyl, aminomethyl, mono-(C.sub.1 -C.sub.4 -alkyl)aminomethyl, di-(C.sub.1 -C.sub.4 -alkyl)aminomethyl, wherein free hydroxy and amino groups may be protected.Type: GrantFiled: March 30, 1994Date of Patent: January 24, 1995Assignee: Warner-Lambert CompanyInventors: Edgardo Laborde, Mel Schroeder
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Patent number: 5362880Abstract: Disclosed is a method of preparing a photographic coupler comprised of 1-aryl-3-substituted-4-heterocyclic-5-pyrazolone development inhibitor releasing coupler for use in a photographic element, said coupler capable of reacting with oxidized color developer to release a heterocyclic coupling-off group containing an inhibitor.Type: GrantFiled: June 30, 1992Date of Patent: November 8, 1994Assignee: Eastman Kodak CompanyInventor: William J. Begley
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Patent number: 5362744Abstract: Novel ACAT inhibitors useful in the treatment of atherosclerosis which are tetrazole-substituted ureas,Type: GrantFiled: November 22, 1993Date of Patent: November 8, 1994Assignee: Warner-Lambert CompanyInventors: Claude Forsey Purchase, Jr., Andrew D. White
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Patent number: 5359080Abstract: There is disclosed an acylacetamide-type yellow coupler having an acyl group represented by formula (I) and a silver halide color photographic material containing same. ##STR1## wherein R.sub.1 represents a monovalent group, Q represents a group of non-metallic atoms required to form together with the C a substituted or unsubstituted 3- to 5-membered cyclic hydrocarbon group or a substituted or unsubstituted 3- to 5-membered heterocyclic group having in the group at least one hetero atom selected from a group consisting of N, 0, S, and P, provided that R.sub.1 is not a hydrogen atom and does not bond to Q to form a ring.Type: GrantFiled: February 12, 1993Date of Patent: October 25, 1994Assignee: Fuji Photo Film Co., Ltd.Inventors: Yoshio Shimura, Hidetoshi Kobayashi, Yasuhiro Yoshioka
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Patent number: 5347010Abstract: Novel tetrazolinones of the formula (I) ##STR1## wherein X is chlorine or bromine,Y is hydrogen, chlorine, bromine, methyl or ethyl, andR.sup.1 and R.sup.2 are the same or different C.sub.2-4 alkyl, a process for their preparation, and the use of the new compounds as herbicides, especially against paddy-weeds.Type: GrantFiled: July 1, 1993Date of Patent: September 13, 1994Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Hidenori Hayakawa, Yukiyoshi Watanabe, Shin-ichi Narabu, Akihiko Yanagi
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Patent number: 5346927Abstract: Blowing agents of tetrazoles and their derivatives which have a melting point over 200.degree. C. and are used to manufacture the high quality foaming thermoplastic synthetic resin moldings, especially engineering or superengineering plastic moldings and said blowing agents generate no harmful gases and do not cause the deterioration of the thermoplastic synthetic resin moldings.Type: GrantFiled: September 8, 1992Date of Patent: September 13, 1994Assignee: Toyo Kasei Kogyo Company, Ltd.Inventors: Atsuhiro Onishi, Koichi Matsunami, Masanao Ebara, Hiroaki Tanaka
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Patent number: 5347009Abstract: Herbicidal 1-(3-halo-4-trifluoromethylphenyl) tetrazolinones of the formula ##STR1## wherein X represents halogen,R.sup.1 represents C.sub.1-3 alkyl, andR.sup.2 represents C.sub.1-3 alkyl.Type: GrantFiled: May 26, 1993Date of Patent: September 13, 1994Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Hidenori Hayakawa, Yukiyoshi Watanabe, Akihiko Yanagi
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Patent number: 5344814Abstract: Herbicidal 1-(3,4-disubstituted phenyl)tetrazolinones of the formula ##STR1## wherein X represents halogen,Y represents trifluoromethoxy or trifluoromethylthio,R.sup.1 represents propyl, isopropyl or allyl, andR.sup.2 represents propyl, isopropyl or allyl.Type: GrantFiled: May 26, 1993Date of Patent: September 6, 1994Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Hidenori Hayakawa, Yukiyoshi Watanabe, Akihiko Yanagi
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Patent number: 5342942Abstract: Pyrazolo[5,1-b]quinazoline compounds, salts thereof, methods of production, intermediates in their production, pharmaceutical compositions containing said compounds, and methods for treating neurodegenerative disorders, tumors of neuronal origin, inflammation, allergy, and pain, and methods for screening compounds that interact with the neurotrophic receptors using said compositions are disclosed.Type: GrantFiled: March 29, 1993Date of Patent: August 30, 1994Assignee: Warner-Lambert CompanyInventors: Juan C. Jaen, Bradley W. Caprathe
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Patent number: 5342954Abstract: Herbicidal 1-(3-halo-4-substituted phenyl)tetrazolinones of the formula ##STR1## wherein X represents halogen,Y represents isopropyl or isopropoxy,R.sup.1 represents ethyl, propyl, isopropyl or allyl, andR.sup.2 represents ethyl, propyl, isopropyl or allyl.Type: GrantFiled: May 26, 1993Date of Patent: August 30, 1994Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Hidenori Hayakawa, Yukiyoshi Watanabe, Akihiko Yanagi
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Patent number: 5338844Abstract: A 2-substituted-2-cyclopentenone compound represented by the following formula (I) and an anticancer agent and a bone formation accelerator comprising the same as an effective active ingredient: ##STR1##Type: GrantFiled: July 16, 1993Date of Patent: August 16, 1994Assignee: Teijin LimitedInventors: Satoshi Sugiura, Toru Minoshima, Atsuo Hazato, Yoshinori Kato
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Patent number: 5336778Abstract: Novel substituted triazoles of the formula (I), which are useful as angiotensin II antagonists, are disclosed.Type: GrantFiled: June 22, 1992Date of Patent: August 9, 1994Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Christine L. Cantone, Linda L. Chang, Malcolm Maccoss, Prasun K. Chakravarty, William J. Greenlee, Arthur A. Patchett, Thomas F. Walsh
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Patent number: 5332757Abstract: The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula -A.sup.2 -X.sup.2 -A.sup.3 - which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.Type: GrantFiled: February 8, 1993Date of Patent: July 26, 1994Assignees: Zeneca Limited, Zeneca PHARMA S AInventors: Thomas G. C. Bird, Patrick Ple
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Patent number: 5332820Abstract: Novel substituted dibenzobicyclo[2.2.Type: GrantFiled: May 20, 1991Date of Patent: July 26, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventor: John J. V. Duncia
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Patent number: 5328916Abstract: New heterocyclic compounds of the formulaX--W--CR.sup.1 R.sup.2 --CO--Y--NR.sup.3 --CHR.sup.4 --CR.sup.5 --CH.sub.2 --(CR.sup.6 R.sup.7).sub.r --Z--Het Iin which R.sup.1 to R.sup.7, W, X, Y, Z, r and Het have the meanings defined herein, and the salts thereof, inhibit the activity of human plasma renin.Type: GrantFiled: May 2, 1991Date of Patent: July 12, 1994Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Peter Raddatz, Claus J. Schmitges, Klaus-Otto Minck
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Patent number: 5326776Abstract: Compounds are disclosed having the formula: ##STR1## wherein the substituents are defined herein. The compounds of the invention are angiotensin II receptor antagonists.Type: GrantFiled: February 24, 1993Date of Patent: July 5, 1994Assignee: Abbott LaboratoriesInventors: Martin Winn, Biswanath De, Thomas M. Zydowsky, Daniel J. Kerkman, John F. DeBernardis, Saul H. Rosenberg, Kazumi Shiosaki, Fatima Z. Basha, Kenneth P. Spina, Thomas W. von Geldern, Steven Boyd, Diane M. Yamamoto, Anthony K. L. Fung
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Patent number: 5312958Abstract: A process for the production of a compound of general formula ##STR1## wherein R represents cyano, carboxy which may be esterified or amidated or tetrazolyl which may be substituted, comprising brominating the corresponding methyl compound with a brominating agent such as N -bromoacetamide, N-bromophtalimide, N-bromosuccinimide and so on in a halogenated hydrocarbon solvent in the presence of an azobis compound.Type: GrantFiled: January 26, 1993Date of Patent: May 17, 1994Assignee: Takeda Chemical Industries, Ltd.Inventors: Syuji Suenaga, Hitoshi Kawaguchi, Takeshi Kato
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Patent number: 5312820Abstract: Carbamoyl and oxycarbonyl derivatives of biphenylmethylamines of structure I are angiotensin-II antagonists with balanced AT.sub.1 and AT.sub.2 activity useful in the treatment of hypertension and related disorders and ocular hypertension. ##STR1## where X is --O-- or --N(R.sup.7)--.Type: GrantFiled: July 17, 1992Date of Patent: May 17, 1994Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Linda L. Chang, William J. Greenlee, Steven M. Hutchins, Ralph A. Rivero
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Patent number: 5310927Abstract: The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof whereinR.sup.1 represents a hydrogen atom or a halogen atom or a group selected from C.sub.1-6 alkyl, C.sub.2-6 alkenyl, fluoroC.sub.1-6 alkyl, C.sub.1-6 alkoxy, --CHO, --CO.sub.2 H or --COR.sup.2 ;Ar represents the group ##STR2## Het represents an N-linked imidazolyl group optionally substituted by one, two or three substituents.The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.Type: GrantFiled: May 15, 1992Date of Patent: May 10, 1994Assignee: Glaxo Group LimitedInventors: Barry C. Ross, David Middlemiss, David I. C. Scopes, Torquil I. M. Jack, Kevin S. Cardwell, Michael D. Dowle, Duncan B. Judd
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Patent number: 5302610Abstract: Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney.Type: GrantFiled: December 19, 1991Date of Patent: April 12, 1994Assignee: G. D. Searle & Co.Inventors: Robert E. Manning, David B. Reitz
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Patent number: 5294722Abstract: Imidazoles of the formula ##STR1## are prepared by treating a ketone ##STR2## with a nitrogenic acid, nitrite or nitrate in the presence of an acid to form a hydroxynitrile ##STR3## which is treated with R.sup.2 --CHO and an ammonium to form an N-hydroxyimidazole ##STR4## which is reduced in the presence of a buffer. In these compounds, R.sup.1 is hydrogen, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl;R.sup.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, or --(CH.sub.2).sub.m Z(CH.sub.2).sub.n R.sup.3, each of which is optionally substituted with F or --CO.sub.2 R.sup.1 ; or aryl or aralkyl, each of which is optionally substituted with 1 or 2 groups selected from halogen, lower alkoxy, lower alkyl, or nitro;R.sup.3 is hydrogen, alkyl, cycloalkyl, lower alkenyl, or lower alkynyl;and the remaining symbols are as defined in the specification.Type: GrantFiled: April 16, 1992Date of Patent: March 15, 1994Assignee: E. R. Squibb & Sons, Inc.Inventor: Kyoung S. Kim
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Patent number: 5283340Abstract: A photographic naphtholic coupler comprising a ballast free naphtholic coupler moiety containing a --CONH.sub.2 group in the 2- position and a ballasted coupling-off group in the 4- position enables good wash out of dye formed upon oxidative coupling from a photographic material during processing of such a photographic material. Such a naphtholic coupler is useful in photographic silver halide materials and processes.Type: GrantFiled: June 4, 1992Date of Patent: February 1, 1994Assignee: Eastman Kodak CompanyInventors: William J. Begley, Teh-hsuan Chen, Hans G. Ling, John W. Harder, Arlyce T. Bowne
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Patent number: 5264583Abstract: A method of forming a washout photographic coupler comprising a coupler moiety (COUP) containing a substituted or unsubstituted ballasted releasing group (A) selected from aryloxy, thioaryloxy, heterocyclicoxy, and thioheterocyclicoxy releasing groups having attached thereto a phenoxy timing group containing a photographically useful group (PUG), the releasing group capable of intramolecular displacement to release the timing group, the method comprising:(a) providing a coupler moiety (COUP) having the releasing group (A) in a coupling off position, the releasing group (A) having a 2 position containing a carbamyl chloride;(b) reacting the carbamyl chloride with a phenoxy timing group having an amine blocked with a carbamate group, the reacting being carried out in the presence of a base to form a first product;(c) removing the carbamate group using an acid to provide a coupler moiety (COUP) having a releasing group (A) and phenoxy timing group having an amine group; and(d) reacting the amine group to form aType: GrantFiled: June 24, 1992Date of Patent: November 23, 1993Assignee: Eastman Kodak CompanyInventors: William J. Begley, Donald Singleton, Jr.
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Patent number: 5254595Abstract: Aryloxypropanolaminotetralins with beta-antagonist activity of the formula ##STR1## wherein R is hydrogen, hydroxy or methoxy and Ar is an optionally substituted aromatic or heteroaromatic group, in optically active or inactive form as well as their acid addition salts are described.A process for their preparation and pharmaceutical compositions containing the compounds of formula (i) or their pharmaceutically acceptable acid addition salts, are also described.Type: GrantFiled: January 9, 1992Date of Patent: October 19, 1993Assignee: Elf SanofiInventors: Umberto Guzzi, Marco Baroni, Sergio Boveri, Luciano Manara, Alberto Bianchetti
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Patent number: 5240924Abstract: An N-acylamino acid derivative of the formula: ##STR1## wherein the substituents are herein defined, or a salt thereof, which is useful as hypotensive drugs.Type: GrantFiled: December 31, 1991Date of Patent: August 31, 1993Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
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Patent number: 5239081Abstract: A process for preparation of a 2,3 or 4-oxo-benzaldehyde or ketone compound by reaction of a 2,3 or 4-hydroxy benzaldehyde or ketone with an ortho, meta or parabromo or chloralkylphenoxy compound comprises reaction of the bromo or chloroalkylphenoxy compound with potassium iodide to form an iodo compound in situ; then, reaction of the resulting product with a 2, 3 or 4-hydroxybenzaldehyde or ketone in the presence of alkylpyridine and a dipolar aprotic solvent. The resulting compounds are useful for formation of photographic color couplers for use in photographic materials.Type: GrantFiled: July 1, 1991Date of Patent: August 24, 1993Assignee: Eastman Kodak CompanyInventors: William J. Begley, Robert C. Stewart
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Patent number: 5237070Abstract: Novel compounds which are 2,6-di-t-butylphenols substituted on the 4 position by an anilino group, which anilino group is substituted by a carboxyl substituent, a tetrazolyl substituent or an N-methyltetrazolyl substituent, are useful antiallergic agents. Pharmaceutical compositions containing and pharmacological methods of using such compounds are also disclosed, as are synthetic intermediates for preparing such compounds. Certain of the synthetic intermediates also exhibit useful antiallergic activity.Type: GrantFiled: May 16, 1991Date of Patent: August 17, 1993Assignee: Riker Laboratories, Inc.Inventor: Robert A. Scherrer
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Patent number: 5235058Abstract: There is disclosed a 3(5)-hydrazinopyrazole compound represented by the following formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an aryl group, a heterocyclic group, a hydroxyl group, an alkoxy group, or an aryloxy group, R.sub.2 represents a hydrogen atom or an acyl group, X represents an aryloxy group, an alkoxy group, a heterocyclic oxy group, or an azolyl group, M represents a hydrogen ion or a metal ion, Y represents an acid radical, and n is 0 or a positive number.Type: GrantFiled: September 17, 1991Date of Patent: August 10, 1993Assignee: Fuji Photo Film Co., Ltd.Inventors: Tadahisa Sato, Keizo Kumura
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Patent number: 5234917Abstract: 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 30, 1990Date of Patent: August 10, 1993Inventors: Joseph A. Finkelstein, Judith Hempel, Richard M. Keenan, James Samanen, Joseph Weinstock
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Patent number: 5233029Abstract: The invention relates to elaiophylin derivatives of the formula I, II and III ##STR1## in which the substituents R(1), R(2), R(3) and R(3)' have the specified meanings. The compounds have antibacterial and antiviral activity.Type: GrantFiled: October 31, 1990Date of Patent: August 3, 1993Assignee: Hoechst AktiengesellschaftInventors: Peter Hammann, Gerhard Kretzschmar
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Patent number: 5232948Abstract: Monocyclic aryl compounds having selective LTB.sub.4 antagonists properties and comprising an amido substituent, a substituent group having a terminal carboxylic acid or derivative thereof and a lipophilic substituent, therapeutic compositions and methods of treatment of disorders which result from LTB.sub.4 activity using the monocyclic aryl compounds are disclosed.Type: GrantFiled: September 10, 1990Date of Patent: August 3, 1993Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Fu-Chih Huang, Wan K. Chan, Charles A. Sutherland, Robert A. Galemmo, Jr., Michael N. Chang
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Patent number: 5227393Abstract: Compounds of formula I ##STR1## wherein Z, R, R.sub.1, R.sub.2 and X are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.Type: GrantFiled: December 9, 1991Date of Patent: July 13, 1993Assignee: Ciba-Geigy CorporationInventors: Marc Lang, Edmond Differding, Jaroslav Stanek
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Patent number: 5223517Abstract: Heterocyclically substituted cycloalkano[b]-indolesulphonamides can be prepared by reaction of appropriate N-unsubstituted indoles with acrylonitrile, followed by hydrolysis, esterification or amidation, or by reaction of heterocyclically substituted hydrazines with cycloalkanones or by subsequent introduction of the heterocyclic group into appropriate indole derivatives. The heterocyclically substituted cycloalkano[b]-indolesulphonamides can be employed for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, asthma, allergies and for the prophylaxis of myocardial infarcts.Type: GrantFiled: August 23, 1991Date of Patent: June 29, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich E. Muller, Ulrich Niewohner, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
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Patent number: 5194623Abstract: Novel compounds derived from azlactones act as precursors for photographically active groups. The active groups are released at an appropriate time in the use of photographic and photothermographic systems.Type: GrantFiled: August 31, 1990Date of Patent: March 16, 1993Assignee: Minnesota Mining and Manufacturing CompanyInventors: Larry R. Krepski, Sharon M. Simpson
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Patent number: 5187271Abstract: A class of N-substituted (.alpha.-imidazolyl-toluyl)pyrrole compounds 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 each of R.sup.0 and R.sup.1 is independently selected from hydrido, alkyl, hydroxyalkyl, formyl, halo, haloalkyl, cycloalkylcarbonyl, alkoxy, aroyl, aryloxy, aralkoxy, alkylcarbonyl, alkoxycarbonyl, cyano, nitro, carboxyl, alkylcarbonyloxy, alkylcarbonyloxyalkyl, alkoxycarbonylalkyl, aralkoxycarbonylalkyl, alkylsulfonyl, aralkylsulfonyl, arylsulfonyl; 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, propylthio, butylthio, and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.Type: GrantFiled: February 28, 1991Date of Patent: February 16, 1993Assignee: G. D. Searle & Co.Inventors: Philippe R. Bovy, Joe T. Collins, Robert E. Manning
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Patent number: 5183810Abstract: Substituted imidazoles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I, are useful as angiotensin II antagonists.Type: GrantFiled: August 13, 1991Date of Patent: February 2, 1993Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, Arthur A. Patchett, David Hangauer, Thomas F. Walsh, Kenneth J. Fitch, Ralph A. Rivero, Daljit S. Dhanoa
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Patent number: 5182339Abstract: A pyrazoloazoleazomethine dye represented by formula (I) ##STR1## wherein, R.sub.1 represents a substituent having a Hammett's substituent constant value of at least 0.6; Za, Zb, and Zc each represents ##STR2## (wherein R.sub.2 represents a hydrogen atom or a substituent), or .dbd.N--; when Zc=Zb is a carbon-carbon double bond, it may form a part of an aromatic ring; R.sub.3, R.sub.4, and R.sub.5 each represents a hydrogen atom or a substituent; and n represents 1 or 2; said dye may form a dimer or higher polymer by combining with each other or to a polymer through a divalent or higher valent group at R.sub.1, Za, Zb, or Zc.Type: GrantFiled: December 5, 1990Date of Patent: January 26, 1993Assignee: Fuji Photo Film Co., Ltd.Inventors: Shigeki Yokoyama, Tadahisa Sato, Keizo Kimura, Nobuo Furutachi, Osamu Takahashi
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Patent number: 5179123Abstract: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxgen, sulfur, --CH.dbd.CH--or --CH.dbd.N--; wherein R.sub.1 is alkyl, alkenyl or alkynyl of about 1 to 20 carbon atoms; wherein R is --CO.sub.2 R.sup.2, tetrazole, methylsulfonamide or benzenesulfonamide, wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbon atoms or a pharmaceutically acceptable cation and R.sup.3 is hydroxyl or halogen, having utility as LTB.sub.4 synthesis inhibitors.Type: GrantFiled: November 4, 1991Date of Patent: January 12, 1993Assignee: G. D. Searle & Co.Inventors: Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro
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Patent number: 5177092Abstract: Azole compounds including azoles and azolium salts, and their use as transglutaminase inhibitors are disclosed.Type: GrantFiled: June 17, 1991Date of Patent: January 5, 1993Assignee: Merck & Co., Inc.Inventors: David C. Remy, John J. Baldwin, David A. Claremon, Stella W. King
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Patent number: 5143922Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic acitvity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: November 20, 1990Date of Patent: September 1, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
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Patent number: 5141843Abstract: A developer liquid suited for use in development of photographic silver halide emulsion layer materials which liquid contains:1) hydroquinone or a substituted hydroquinone as sole developing agent or said hydroquinone as main developing agent in combination with an auxiliary developing agent in an amount less than 10 mole % with respect to the main developing agent,2) an inorganic compound yielding free sulphite ions in an amount of at least 5 grams per liter,3) an organic anti-fogging agent corresponding to the following general formula (Z): ##STR1## wherein: X.sup.2 represents an alkyl group or an aryl group including said groups in substituted form or an amino group including said group in substituted form;the amount of anti-fogging agent being in the range of 50 mg to 1 g per liter,4) a polymer containing a plurality of alkylene oxide units, and5) the necessary alkaline material to have in said liquid a pH of at least 10.5. Optional additives can also be present in the developing liquid.Type: GrantFiled: March 27, 1991Date of Patent: August 25, 1992Assignee: AGFA-Gevaert N. V.Inventors: Richard A. Ooms, Piet Kok, Jean-Marie O. Dewanckele
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Patent number: 5140038Abstract: The present invention provides sulphonamides of the general formula: ##STR1## wherein R.sup.1 and R.sup.2, which can be the same or different, are hydrogen or halogen atoms or C.sub.1 -C.sub.6 -alkyl, trifluoro-methyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, N-alkylaminocarbonyl or N,N-dialkylaminocarbonyl radicals or, when R.sup.1 and R.sup.2 are alkyl radicals ortho to one another, R.sup.1 and R.sup.2, together with the carbon atoms to which they are attached, form a saturated or unsaturated C.sub.5 -C.sub.7 -alkylene ring, R.sup.3 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical, a phenylalkyl or phenylalkenyl radical, the phenyl moiety of which can be substituted by halogen, alkyl or trifluoromethyl, C is a --(CH.sub.2).sub.m -- radical, in which m is 0, 1, 2 or 3, or a branched C.sub.2 -C.sub.5 alkylene radical, whereby a methylene radical --CH.sub.Type: GrantFiled: August 31, 1989Date of Patent: August 18, 1992Assignee: Boehringer Mannheim GmbHInventors: Ernst-Christian Witte, Karlheinz Stegmeier, Liesel Doerge
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Patent number: 5136868Abstract: Herbicidal aryltetrazolinones and thiones of the formula ##STR1## in which W is oxygen or sulfur; R is alkyl, fluoroalkyl, alkenyl, haloalkenyl, cyanoalkyl, alkylthioalkyl, haloalkoxyalkyl, trifluoromethylthio or alkoxyalkyl; one of X.sup.1 and X.sup.2 is fluorine, chlorine, or bromine and the other is fluorine, chlorine, bromine, alkyl, nitro or haloalkyl; and Z is a group selected from a variety of substituents including 2-propynyloxy as disclosed and exemplified.Type: GrantFiled: December 28, 1989Date of Patent: August 11, 1992Assignee: FMC CorporationInventor: George Theodoridis
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Patent number: 5137884Abstract: N-tetrazolyl beta-lactams of the Formula: ##STR1## and the pharmaceutically acceptable salts thereof wherein R.sup.2 is hydrogen, alkyl having 1 to 6 carbon atoms or carboalkoxy having 2 to 7 carbon atoms; andZ is ##STR2## and W is ##STR3## thus forming a zwitterion, or Z is ##STR4## wherein R.sup.1 is benzyl, phenyloxymethyl or ##STR5## wherein Y is alkoxy or substituted alkoxy having 1 to 6 carbon atoms wherein the substituent on the alkoxy group is --COOH; andW is ##STR6## wherein R.sup.3 is H, M or --CH.sub.2 COOM, wherein M is a pharmaceutically acceptable cation are disclosed. The compounds are useful as antibiotics.Type: GrantFiled: November 16, 1983Date of Patent: August 11, 1992Assignee: Merck & Co., Inc.Inventors: W. Alexander Andrus, Burton G. Christensen, James V. Heck
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Patent number: 5138068Abstract: Novel 1-phenyl-5-oxo-2-tetrazolines of formula I ##STR1## in which R.sup.1 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.5 -C.sub.6 cycloalkenyl, C.sub.1 -C.sub.4 alkyl- or halo-substituted C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.4 alkyl- or halo-substituted C.sub.5 -C.sub.6 cycloalkenyl, halo-, C.sub.1 -C.sub.4 alkoxy- or phenyl-substituted C.sub.3 -C.sub.6 alkenyl, halo-, C.sub.1 -C.sub.4 alkoxy- or phenyl-substituted C.sub.3 -C.sub.8 alkynyl, or C.sub.1 -C.sub.8 alkyl that is substituted by halogen, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl, cyano, hydroxy, halophenyl, C.sub.1 -C.sub.4 alkylphenyl or by a heteroaromatic radical,R.sup.2 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, cyclopentenyl or cyclohexenyl, or is C.sub.1 -C.sub.6 alkyl that is substituted by halogen, by C.sub.1 -C.sub.Type: GrantFiled: May 22, 1991Date of Patent: August 11, 1992Assignee: Ciba-Geigy CorporationInventors: Josef Ehrenfreund, Erich Stamm
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Patent number: 5135938Abstract: Leukotriene antagonist thiadiazoles have been prepared.Type: GrantFiled: March 30, 1990Date of Patent: August 4, 1992Assignee: SmithKline Beecham CorporationInventors: John G. Gleason, Ralph F. Hall, Irene Uzinskas
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Patent number: 5128346Abstract: A compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are substituents; R.sub.6 is hydrogen, loweralkyl, cycloalkyl, loweralkenyl, arylalkyl, (substituted aryl)alkyl, or (heterocyclic)alkyl; B is a bond, an alkylene group, an alkenylene group, an alkadienylene group or a heteroatom containing linking group; D is a substituted acyl group or tetrazolyl; Z is CO, C(S) or S(O).sub.2 ; Ar is a heterocyclic group; and n is 1 to 3.Also disclosed are a composition and a method for antagonizing CCK, a composition and method for treating or preventing gastrointestinal, central nervous, appetite regulating and pain regulating systems, a composition and method for treating or preventing hyperinsulinemia, methods of making the compounds and intermediates useful in making the compounds.Type: GrantFiled: August 23, 1990Date of Patent: July 7, 1992Assignee: Abbott LaboratoriesInventors: Alex M. Nadzan, James F. Kerwin, Chun W. Lin
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Patent number: 5118812Abstract: A pyrazoloazole series coupler having the following formula (I) ##STR1## wherein R.sub.1 represents a substituent having a Hammett's substituent constant .sigma..sub.p of at least 0.6;X represents a hydrogen atom or a group capable of being released by the coupling reaction with the oxidation product of an aromatic primary amine developing agent;Za, Zb and Zc each represents .dbd.CH--, ##STR2## (wherein R.sub.2 represents a hydrogen atom or a substituent), .dbd.N-- or --NH--;one of Za--Zb bond and Zb--Zc bond is a double bond and the other is a single bond;when Zb--Zc is a carbon-carbon double bond, this Zb--Zc may form a part of another aromatic ring;R.sub.1, R.sub.2 or X may be a divalent linking group forming a dimer, or R.sub.1 or R.sub.Type: GrantFiled: July 6, 1990Date of Patent: June 2, 1992Assignee: Fuji Photo Film Co., Ltd.Inventors: Shigeki Yokoyama, Tadahisa Sato, Keizo Kimura, Nobuo Furutachi, Osamu Takahashi