Chalcogen Or Nitrogen Attached Directly To The Tetrazole Ring By Nonionic Bonding Patents (Class 548/251)
  • Patent number: 5389634
    Abstract: 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: Grant
    Filed: June 9, 1993
    Date of Patent: February 14, 1995
    Assignee: Roussel-Uclaf
    Inventors: Michel Fortin, Daniel Frechet, Gilles Hamon, Simone Jouquey, Jean-Paul Vevert
  • Patent number: 5389663
    Abstract: 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: Grant
    Filed: November 24, 1993
    Date of Patent: February 14, 1995
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Katsumi Itoh, Kenji Okonogi, Akihiro Tasaka
  • Patent number: 5384407
    Abstract: 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: Grant
    Filed: March 30, 1994
    Date of Patent: January 24, 1995
    Assignee: Warner-Lambert Company
    Inventors: Edgardo Laborde, Mel Schroeder
  • Patent number: 5362880
    Abstract: 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: Grant
    Filed: June 30, 1992
    Date of Patent: November 8, 1994
    Assignee: Eastman Kodak Company
    Inventor: William J. Begley
  • Patent number: 5362744
    Abstract: Novel ACAT inhibitors useful in the treatment of atherosclerosis which are tetrazole-substituted ureas,
    Type: Grant
    Filed: November 22, 1993
    Date of Patent: November 8, 1994
    Assignee: Warner-Lambert Company
    Inventors: Claude Forsey Purchase, Jr., Andrew D. White
  • Patent number: 5359080
    Abstract: 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: Grant
    Filed: February 12, 1993
    Date of Patent: October 25, 1994
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Yoshio Shimura, Hidetoshi Kobayashi, Yasuhiro Yoshioka
  • Patent number: 5347010
    Abstract: 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: Grant
    Filed: July 1, 1993
    Date of Patent: September 13, 1994
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Toshio Goto, Hidenori Hayakawa, Yukiyoshi Watanabe, Shin-ichi Narabu, Akihiko Yanagi
  • Patent number: 5346927
    Abstract: 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: Grant
    Filed: September 8, 1992
    Date of Patent: September 13, 1994
    Assignee: Toyo Kasei Kogyo Company, Ltd.
    Inventors: Atsuhiro Onishi, Koichi Matsunami, Masanao Ebara, Hiroaki Tanaka
  • Patent number: 5347009
    Abstract: 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: Grant
    Filed: May 26, 1993
    Date of Patent: September 13, 1994
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Toshio Goto, Hidenori Hayakawa, Yukiyoshi Watanabe, Akihiko Yanagi
  • Patent number: 5344814
    Abstract: 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: Grant
    Filed: May 26, 1993
    Date of Patent: September 6, 1994
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Toshio Goto, Hidenori Hayakawa, Yukiyoshi Watanabe, Akihiko Yanagi
  • Patent number: 5342942
    Abstract: 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: Grant
    Filed: March 29, 1993
    Date of Patent: August 30, 1994
    Assignee: Warner-Lambert Company
    Inventors: Juan C. Jaen, Bradley W. Caprathe
  • Patent number: 5342954
    Abstract: 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: Grant
    Filed: May 26, 1993
    Date of Patent: August 30, 1994
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Toshio Goto, Hidenori Hayakawa, Yukiyoshi Watanabe, Akihiko Yanagi
  • Patent number: 5338844
    Abstract: 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: Grant
    Filed: July 16, 1993
    Date of Patent: August 16, 1994
    Assignee: Teijin Limited
    Inventors: Satoshi Sugiura, Toru Minoshima, Atsuo Hazato, Yoshinori Kato
  • Patent number: 5336778
    Abstract: Novel substituted triazoles of the formula (I), which are useful as angiotensin II antagonists, are disclosed.
    Type: Grant
    Filed: June 22, 1992
    Date of Patent: August 9, 1994
    Assignee: 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
  • Patent number: 5332757
    Abstract: 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: Grant
    Filed: February 8, 1993
    Date of Patent: July 26, 1994
    Assignees: Zeneca Limited, Zeneca PHARMA S A
    Inventors: Thomas G. C. Bird, Patrick Ple
  • Patent number: 5332820
    Abstract: Novel substituted dibenzobicyclo[2.2.
    Type: Grant
    Filed: May 20, 1991
    Date of Patent: July 26, 1994
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: John J. V. Duncia
  • Patent number: 5328916
    Abstract: 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: Grant
    Filed: May 2, 1991
    Date of Patent: July 12, 1994
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Peter Raddatz, Claus J. Schmitges, Klaus-Otto Minck
  • Patent number: 5326776
    Abstract: Compounds are disclosed having the formula: ##STR1## wherein the substituents are defined herein. The compounds of the invention are angiotensin II receptor antagonists.
    Type: Grant
    Filed: February 24, 1993
    Date of Patent: July 5, 1994
    Assignee: Abbott Laboratories
    Inventors: 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
  • Patent number: 5312958
    Abstract: 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: Grant
    Filed: January 26, 1993
    Date of Patent: May 17, 1994
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Syuji Suenaga, Hitoshi Kawaguchi, Takeshi Kato
  • Patent number: 5312820
    Abstract: 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: Grant
    Filed: July 17, 1992
    Date of Patent: May 17, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Linda L. Chang, William J. Greenlee, Steven M. Hutchins, Ralph A. Rivero
  • Patent number: 5310927
    Abstract: 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: Grant
    Filed: May 15, 1992
    Date of Patent: May 10, 1994
    Assignee: Glaxo Group Limited
    Inventors: Barry C. Ross, David Middlemiss, David I. C. Scopes, Torquil I. M. Jack, Kevin S. Cardwell, Michael D. Dowle, Duncan B. Judd
  • Patent number: 5302610
    Abstract: 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: Grant
    Filed: December 19, 1991
    Date of Patent: April 12, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Robert E. Manning, David B. Reitz
  • Patent number: 5294722
    Abstract: 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: Grant
    Filed: April 16, 1992
    Date of Patent: March 15, 1994
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Kyoung S. Kim
  • Patent number: 5283340
    Abstract: 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: Grant
    Filed: June 4, 1992
    Date of Patent: February 1, 1994
    Assignee: Eastman Kodak Company
    Inventors: William J. Begley, Teh-hsuan Chen, Hans G. Ling, John W. Harder, Arlyce T. Bowne
  • Patent number: 5264583
    Abstract: 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 a
    Type: Grant
    Filed: June 24, 1992
    Date of Patent: November 23, 1993
    Assignee: Eastman Kodak Company
    Inventors: William J. Begley, Donald Singleton, Jr.
  • Patent number: 5254595
    Abstract: 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: Grant
    Filed: January 9, 1992
    Date of Patent: October 19, 1993
    Assignee: Elf Sanofi
    Inventors: Umberto Guzzi, Marco Baroni, Sergio Boveri, Luciano Manara, Alberto Bianchetti
  • Patent number: 5240924
    Abstract: 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: Grant
    Filed: December 31, 1991
    Date of Patent: August 31, 1993
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
  • Patent number: 5239081
    Abstract: 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: Grant
    Filed: July 1, 1991
    Date of Patent: August 24, 1993
    Assignee: Eastman Kodak Company
    Inventors: William J. Begley, Robert C. Stewart
  • Patent number: 5237070
    Abstract: 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: Grant
    Filed: May 16, 1991
    Date of Patent: August 17, 1993
    Assignee: Riker Laboratories, Inc.
    Inventor: Robert A. Scherrer
  • Patent number: 5235058
    Abstract: 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: Grant
    Filed: September 17, 1991
    Date of Patent: August 10, 1993
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Tadahisa Sato, Keizo Kumura
  • Patent number: 5234917
    Abstract: 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: Grant
    Filed: November 30, 1990
    Date of Patent: August 10, 1993
    Inventors: Joseph A. Finkelstein, Judith Hempel, Richard M. Keenan, James Samanen, Joseph Weinstock
  • Patent number: 5233029
    Abstract: 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: Grant
    Filed: October 31, 1990
    Date of Patent: August 3, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Peter Hammann, Gerhard Kretzschmar
  • Patent number: 5232948
    Abstract: 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: Grant
    Filed: September 10, 1990
    Date of Patent: August 3, 1993
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Fu-Chih Huang, Wan K. Chan, Charles A. Sutherland, Robert A. Galemmo, Jr., Michael N. Chang
  • Patent number: 5227393
    Abstract: 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: Grant
    Filed: December 9, 1991
    Date of Patent: July 13, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Marc Lang, Edmond Differding, Jaroslav Stanek
  • Patent number: 5223517
    Abstract: 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: Grant
    Filed: August 23, 1991
    Date of Patent: June 29, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich E. Muller, Ulrich Niewohner, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
  • Patent number: 5194623
    Abstract: 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: Grant
    Filed: August 31, 1990
    Date of Patent: March 16, 1993
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Larry R. Krepski, Sharon M. Simpson
  • Patent number: 5187271
    Abstract: 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: Grant
    Filed: February 28, 1991
    Date of Patent: February 16, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Philippe R. Bovy, Joe T. Collins, Robert E. Manning
  • Patent number: 5183810
    Abstract: Substituted imidazoles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I, are useful as angiotensin II antagonists.
    Type: Grant
    Filed: August 13, 1991
    Date of Patent: February 2, 1993
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, Arthur A. Patchett, David Hangauer, Thomas F. Walsh, Kenneth J. Fitch, Ralph A. Rivero, Daljit S. Dhanoa
  • Patent number: 5182339
    Abstract: 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: Grant
    Filed: December 5, 1990
    Date of Patent: January 26, 1993
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Shigeki Yokoyama, Tadahisa Sato, Keizo Kimura, Nobuo Furutachi, Osamu Takahashi
  • Patent number: 5179123
    Abstract: 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: Grant
    Filed: November 4, 1991
    Date of Patent: January 12, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro
  • Patent number: 5177092
    Abstract: Azole compounds including azoles and azolium salts, and their use as transglutaminase inhibitors are disclosed.
    Type: Grant
    Filed: June 17, 1991
    Date of Patent: January 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: David C. Remy, John J. Baldwin, David A. Claremon, Stella W. King
  • Patent number: 5143922
    Abstract: 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: Grant
    Filed: November 20, 1990
    Date of Patent: September 1, 1992
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
  • Patent number: 5141843
    Abstract: 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: Grant
    Filed: March 27, 1991
    Date of Patent: August 25, 1992
    Assignee: AGFA-Gevaert N. V.
    Inventors: Richard A. Ooms, Piet Kok, Jean-Marie O. Dewanckele
  • Patent number: 5140038
    Abstract: The present invention provides sulphonamides of the general formula: ##STR1## wherein R.sup.1 and R.sup.2, which can be the same or different, are hydrogen or halogen atoms or C.sub.1 -C.sub.6 -alkyl, trifluoro-methyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, N-alkylaminocarbonyl or N,N-dialkylaminocarbonyl radicals or, when R.sup.1 and R.sup.2 are alkyl radicals ortho to one another, R.sup.1 and R.sup.2, together with the carbon atoms to which they are attached, form a saturated or unsaturated C.sub.5 -C.sub.7 -alkylene ring, R.sup.3 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical, a phenylalkyl or phenylalkenyl radical, the phenyl moiety of which can be substituted by halogen, alkyl or trifluoromethyl, C is a --(CH.sub.2).sub.m -- radical, in which m is 0, 1, 2 or 3, or a branched C.sub.2 -C.sub.5 alkylene radical, whereby a methylene radical --CH.sub.
    Type: Grant
    Filed: August 31, 1989
    Date of Patent: August 18, 1992
    Assignee: Boehringer Mannheim GmbH
    Inventors: Ernst-Christian Witte, Karlheinz Stegmeier, Liesel Doerge
  • Patent number: 5136868
    Abstract: 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: Grant
    Filed: December 28, 1989
    Date of Patent: August 11, 1992
    Assignee: FMC Corporation
    Inventor: George Theodoridis
  • Patent number: 5137884
    Abstract: 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: Grant
    Filed: November 16, 1983
    Date of Patent: August 11, 1992
    Assignee: Merck & Co., Inc.
    Inventors: W. Alexander Andrus, Burton G. Christensen, James V. Heck
  • Patent number: 5138068
    Abstract: 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: Grant
    Filed: May 22, 1991
    Date of Patent: August 11, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Josef Ehrenfreund, Erich Stamm
  • Patent number: 5135938
    Abstract: Leukotriene antagonist thiadiazoles have been prepared.
    Type: Grant
    Filed: March 30, 1990
    Date of Patent: August 4, 1992
    Assignee: SmithKline Beecham Corporation
    Inventors: John G. Gleason, Ralph F. Hall, Irene Uzinskas
  • Patent number: 5128346
    Abstract: 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: Grant
    Filed: August 23, 1990
    Date of Patent: July 7, 1992
    Assignee: Abbott Laboratories
    Inventors: Alex M. Nadzan, James F. Kerwin, Chun W. Lin
  • Patent number: 5118812
    Abstract: 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: Grant
    Filed: July 6, 1990
    Date of Patent: June 2, 1992
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Shigeki Yokoyama, Tadahisa Sato, Keizo Kimura, Nobuo Furutachi, Osamu Takahashi