Additional Nitrogen Containing Hetero Ring (e.g., Thiazole, Etc.) Patents (Class 544/82)
  • Patent number: 4966855
    Abstract: The invention provides new redox indicators and uses for these redox compounds (I): ##STR1## Wherein X is oxygen or sulphur, R.sub.1 is julolidine or tetrahydroquinoline, which can carry an alkyl radical on the nitrogen atom which, in turn, can be substituted by a sulphuric, phosphonic or carboxylic acid residues, or is (II); wherein R.sub.4 is hydroxyl or a mono- or dialkylated amino group, R.sub.5 and R.sub.6, which can be the same or different, are hydrogen, alkyl or alkoxy, R.sub.2 is hydrogen or alkyl, julolidine or tetrahydroquinoline, which can carry an alkyl on the nitrogen atom which alkyl can be substituted by sulphuric, phosphonic or carboxylic acids, or is III; wherein R.sub.5 and R.sub.6 are the same as in R.sub.1 and R'.sub.4 is hydroxyl, an amino or a mono-or dialkylated amino group, whereby the alkyl radicals can be substituted one or more times by hydroxyl, alkoxy, halogen, morpholine or a sulphuric, carboxylic or phosphonic acid residue, which acids can also be esterified, and R.sub.
    Type: Grant
    Filed: July 2, 1985
    Date of Patent: October 30, 1990
    Assignee: Boehringer Mannheim GmbH
    Inventors: Ulfert Deneke, Werner Guthlein, Wolfgang Weckerle, Hans Wielinger
  • Patent number: 4956467
    Abstract: Novel nucleophilic tertiary organophosphines and the specific cleavage of peptide bonds by nucleophilic tertiary organophosphines. This invention is of particular utility in providing chemical agents for use in the cleavage of proteins and the determination of the amino acid sequence of proteins.
    Type: Grant
    Filed: April 5, 1989
    Date of Patent: September 11, 1990
    Assignee: American Cyanamid Company
    Inventors: Lois M. Hinman, Libby S. Miller
  • Patent number: 4950755
    Abstract: Bis(morpholinomethyl) derivative of 1,2-bis(dioxopiperizinyl)propane of the formula: ##STR1## wherein R is CH.sub.3, R' is ##STR2## and the process for the synthesis thereof is provided. The compound of the present invention is water soluble, may be administered by intravenous injection and lessens the severity of doxorubicin-induced cardiotoxicity.
    Type: Grant
    Filed: September 28, 1988
    Date of Patent: August 21, 1990
    Assignee: Ohio State University
    Inventors: Donald T. Witiak, Hattiangadi B. Bhat
  • Patent number: 4948416
    Abstract: This invention relates to novel condensed ring sulfonylureas and their use as herbicides and growth regulants.
    Type: Grant
    Filed: March 27, 1989
    Date of Patent: August 14, 1990
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Robert J. Pasteris
  • Patent number: 4944790
    Abstract: 1,5-diphenylpyrazole-3-carboxylic acid derivatives of the formula ##STR1## in which each of R.sub.a and R.sub.b, independently of the other represents halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -haloalkyl, C.sub.2 -C.sub.5 -alkenyl, C.sub.2 -C.sub.5 -alkynyl or cyano, n represents zero or an integer from 1 to 3, and OR.sub.1 represents hydroxy, a plant-physiologically tolerable salt radical or any desired ester radical, are capable of antagonizing specifically the phytotoxic action of phenoxypropionic acid ester herbicides of the formula II ##STR2## in which G represents ##STR3## in which Hal.sub.1 represents fluorine, chlorine, bromine, iodine or trifluoromethyl, Hal.sub.2 represents hydrogen, fluorine, chlorine, bromine or trifluoromethyl, Z represents nitrogen or methine (--CH.dbd.), X represents an oxygen or sulphur atom, R.sub.1 ' represents halogen, trifluoromethyl, nitro, cyano, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.
    Type: Grant
    Filed: March 20, 1989
    Date of Patent: July 31, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Moser, Beat Bohner, Werner Fory
  • Patent number: 4906624
    Abstract: Certain trans-6-[[(substituted)pyridin-3-yl]-alkyl- and alkenyl]tetrahydro-4-hydroxypyran-2-ones and the corresponding ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.
    Type: Grant
    Filed: August 2, 1988
    Date of Patent: March 6, 1990
    Assignee: Warner-Lambert Company
    Inventors: Alexander W. Chucholowski, Mark W. Creswell, Bruce D. Roth, Drago R. Sliskovic
  • Patent number: 4904783
    Abstract: N-Arylsulfonyl-N'-(4-mercaptomethyl-pyrimidinyl)-ureas of the formula ##STR1## (symbols in this formula defined herein) and the salts of these compounds with amines, alkali metal bases or alkaline-earth metal bases or with ammonium bases, have good pre- and post-emergence-selective, herbicidal and growth-regulating properties.
    Type: Grant
    Filed: September 19, 1988
    Date of Patent: February 27, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Werner Topfl
  • Patent number: 4902336
    Abstract: N-Arylsulfonyl-N'-(4-mercaptomethyl-pyrimidinyl-ureas of the formula ##STR1## (symbols in this formula defined herein) and the salts of these compounds with amines, alkali metal bases or alkaline-earth metal bases or with ammonium bases, have good pre- and post-emergence-selective, herbicidal and growth-regulating properties.
    Type: Grant
    Filed: September 19, 1988
    Date of Patent: February 20, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Werner Topfl
  • Patent number: 4897105
    Abstract: A compound of the general formula ##STR1## wherein R.sub.1 is a phenyl group which may be substituted, R.sub.2 and R.sub.3 respectively are a lower alkyl or lower alkoxy group, Z is CH or N and n is 0 or 1, or a salt thereof which is useful as a herbicide.
    Type: Grant
    Filed: March 20, 1987
    Date of Patent: January 30, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yoshiyuki Okada, Isao Aoki, Nobuyuki Okajima, Takashi Kuragano
  • Patent number: 4889857
    Abstract: A quinolonecarboxylic acid compound of the formula: ##STR1## wherein R.sup.1 is an alkyl group, a cycloalkyl group, a haloalkyl group, an alkenyl group, mono- or di-alkylamino groups, a phenyl group or a phenyl group substituted by one to three substituents selected from the group consisting of a halogen atom, an alkyl group, an alkoxy group, a hydroxy group, a nitro group or an amino group, R.sup.2 is a hydrogen atom, an alkyl group, a cycloalkyl group, an acyl group or an alkoxycarbonyl group, R.sup.3 is a hydrogen atom, an alkyl group or an aralkyl group, or R.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a heterocyclic ring, R.sup.4 is a hydrogen atom or an alkyl group, R.sup.5 is a hydrogen atom, an alkyl group, an aralkyl group or an ester residue which is readily hydrolyzable in vivo, X is a hydrogen atom, a halogen atom or an alkyl group, n is interger of 1 to 3, and a salt thereof, and pharmaceutical use thereof.
    Type: Grant
    Filed: September 29, 1988
    Date of Patent: December 26, 1989
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Kazuhiko Araki, Tsuyoshi Kuroda, Satoru Uemori, Akihiko Moriguchi, Yoshifumi Ikeda
  • Patent number: 4873253
    Abstract: A phenylalanine derivative having the formula (I): ##STR1## wherein A represents ##STR2## B represents ##STR3## wherein m is 0, 1, or 2 and n is 3, 4, or 5; X represents (a) hydroxy, (b) nitro, (c) amino, (d) phenoxy which may be substituted with (i) halogen or (ii) nitro, (e) c.sub.1 -C.sub.4 alkyloxy which may be substituted wit (i) phenyl or (ii) benzoyl, (f) benzoyl, (g) pyridyloxy which may be substituted with (i) halogen or (ii) nitro, or (h) c.sub.1 -C.sub.4 alkyl which may by substituted with halogen;Y represents ##STR4## or --OR.sup.3 wherein R.sup.1 R.sup.2 are independently (a) hydrogen, (b) phenyl which may be substituted with (i) benzoyl, (ii) C.sub.1 -C.sub.4 alkylcarbonyl, (iii) C.sub.1 -C.sub.4 alkyl which may be further substituted with C.sub.1 -C.sub.4 alkoxycarbonyl or hydroxycarbonyl, (iv) C.sub.2 -C.sub.5 alkenyl which may be further substituted with hydroxycarbonyl or C.sub.1 -C.sub.4 alkoxycarbonyl, (v) C.sub.1 -C.sub.
    Type: Grant
    Filed: March 30, 1987
    Date of Patent: October 10, 1989
    Assignees: Shosuke Okamoto, Showa Denko Kabushiki Kaisha
    Inventors: Shosuke Okamoto, Yoshio Okada, Akiko Okunomiya, Taketoshi Naito, Yoshio Kimura, Morihiko Yamada, Norio Ohno, Yasuhiro Katsuura, Hiroshi Nojima, Takashi Shishikura
  • Patent number: 4853383
    Abstract: Novel substituted imidazoles and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit pharmacological activity which includes antihypertensive activity and .beta.-adrenergic blocking activity.
    Type: Grant
    Filed: September 8, 1986
    Date of Patent: August 1, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Patent number: 4851410
    Abstract: 1,4-disubstituted pyrazole derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 independently of one another are each hydrogen, lower alkyl or benzyl, or R.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, may be a pyrrolidino, piperidino or morpholino radical, n is an integer from 2 to 5 and Z is a radical of the formula ##STR2## or QNR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 have the same meanings as above, Q is ##STR3## A is CHR.sup.3 or NR.sup.3 in which R.sup.3 is CN, NO.sub.2, SO.sub.2 -aryl or SO.sub.2 -lower alkyl and m may be 0 or 1, and their pharmaceutically tolerated salts, processes for their preparation, pharmaceutical compositions containing the compounds of formula I, the use of such compositions and an intermediate of the formula III ##STR4## where R.sup.1, R.sup.2 and n have the same meanings as above, in the preparation of the compounds of the formula I.The compounds are useful to block histamine H.sub.2.sup.- receptors.
    Type: Grant
    Filed: November 15, 1988
    Date of Patent: July 25, 1989
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Ostersehlt, Norbert Rieber, Josef Gries
  • Patent number: 4847379
    Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein X is oxygen or nitrogen and R.sub.4 is aryl, are disclosed. These novel compounds are useful, for example, as cardiovascular agents.
    Type: Grant
    Filed: November 30, 1987
    Date of Patent: July 11, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4845081
    Abstract: N-methylamino derivatives of biologically active substances which have enhanced delivery across topical membranes and pharmaceutical compositions adapted for topical administration containing same.
    Type: Grant
    Filed: September 12, 1986
    Date of Patent: July 4, 1989
    Assignee: University of Florida
    Inventor: Kenneth B. Sloan
  • Patent number: 4843068
    Abstract: A pyrazole oxime derivative represented by the general formula (I) which is useful as an insecticide and fungicide, ##STR1## wherein the structural elements are defined in the specification, and the method of controlling said pests. The compounds represented by the general formula (I) can be synthesized by the methods disclosed in the specification.
    Type: Grant
    Filed: December 29, 1986
    Date of Patent: June 27, 1989
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Hiroshi Hamaguchi, Hideo Takaishi, Tetsuji Ohshima, Takamichi Konno, Yukio Miyagi, Shiraiwa Yutaka, Takayuki Akita
  • Patent number: 4838926
    Abstract: This invention relates to certain novel pyridine sulfonamide compounds, to composition containing such compounds, and to a method of use of such compositions to control the growth of undesired vegetation.
    Type: Grant
    Filed: September 14, 1987
    Date of Patent: June 13, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Mary A. Hanagan, Barry A. Wexler
  • Patent number: 4833246
    Abstract: A novel pyrazolone dye represented by the following formula (I), which can be effectively used as a filter dye, an irradiation inhibiting dye, an antihalation dye or the like in a photographic light-sensitive material: ##STR1## wherein R.sub.1 and R.sub.2 each represents --COOR or ##STR2## R and R' each represents a hydrogen atom, an alkyl group, or an aryl group or may combine with each other to form a 5- or 6-membered ring; Q.sub.1 and Q.sub.2 each represents an aryl group; X.sub.1 and X.sub.2 each represents a linkage group; Y.sub.1 and Y.sub.2 each represents a sulfo group or a carboxyl group; L.sub.1, L.sub.2 and L.sub.3 each represents a methine group; L.sub.4 and L.sub.5 each represents an alkylene group; m.sub.1 and m.sub.2 each represents 1 or 2; n represents 0, 1 or 2; p.sub.1 and p.sub.2 each represents 0 or 1; q.sub.1 and q.sub.2 each represent 0, 1, 2, 3 or 4; and s.sub.1 and s.sub.2 each represents 1 or 2.
    Type: Grant
    Filed: December 2, 1987
    Date of Patent: May 23, 1989
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Keiichi Adachi, Shigeru Ohno, Yoshio Inagaki, Nobuo Seto, Yoshihiro Jinbo
  • Patent number: 4831151
    Abstract: Compounds of the formula ##STR1## wherein the various substituents are defined hereinbelow and the pharmaceutically acceptable acid addition salts thereof, possess pharmacological properties. In particular, they possess antibacterial, antimycotic, protozoacidal and/or anthelmintic properties.
    Type: Grant
    Filed: April 21, 1986
    Date of Patent: May 16, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Helmut Link, Marc Montavon, Eva M. Karpitschka, Wilhelm Klotzer, Renate Mussner
  • Patent number: 4808727
    Abstract: The pharmaceutically acceptable salts corresponding to the imidazolium hydrogen carbonates of the formula ##STR1## wherein the symbol Q is arylene or heteroarylene, the group --NR.sup.1 R.sup.2 is a basic amino group, R.sup.3 is hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkyl, lower alkylthio, lower alkoxy or the group --(A).sub.n --Ra, R.sup.4 is a saturated or partially unsaturated lower hydrocarbon group, a basic amino group or the group --N.dbd.CRc--Rb, --CHRcRd, --NH--CHRcRd, --NH--CO--Re or --CHRc--CO--Re, R.sup.5 is hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkyl, aryl or a fused benzene ring, R.sup.
    Type: Grant
    Filed: September 29, 1987
    Date of Patent: February 28, 1989
    Assignee: Hoffmann-LaRoche Inc.
    Inventor: Helmut Link
  • Patent number: 4788283
    Abstract: Compounds containing a group of the formula I ##STR1## in which R is H or C.sub.1 -C.sub.4 -alkyl, R.sup.1 is H, CN, an acyloxy group or a free valency and R.sup.2 and R.sup.3 are organic radicals can be prepared in a simple manner from the corresponding compounds containing a group of the formula Ia ##STR2## by stepwise reaction with phosgene and a secondary amine R.sup.2 --NH--R.sup.3 in the presence of a molar amount of a base. The N-diorganocarbamoyl compounds containing the group I are outstanding light stabilizers, in particular for organic polymers. They can be converted by secondary reactions into other compounds which contain the group I and which are not accessible by direct phosgenation. Many of the products thus obtainable by phosgenation or conversion are novel compounds.
    Type: Grant
    Filed: March 21, 1986
    Date of Patent: November 29, 1988
    Assignee: Ciba-Geigy Corporation
    Inventor: Friedrich Karrer
  • Patent number: 4783537
    Abstract: Novel .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.-[hydroxy(aralkyl and cycloalkyl)]acetic acid derivatives and .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.[alkanoyloxy(aralkyl and cycloalkyl)]acetic acid derivatives, such as N,N-dimethyl-2-(hydroxyphenylmethyl)-4-dimethylamino-2-phenylbutanamide, 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanenitrile, ethyl 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanoate, and N,N-dimethyl-2[(acetyloxy)phenylmethyl]-4-dimethylamino-2-phenylbutanamide , useful in the treatment of cardiovascular disease.
    Type: Grant
    Filed: November 13, 1985
    Date of Patent: November 8, 1988
    Assignee: Pennwalt Corporation
    Inventor: Robert J. Murray
  • Patent number: 4769371
    Abstract: Pyridine compounds of the formula ##STR1## wherein R.sub.4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents due to their calcium entry blocking vasodilator activity.
    Type: Grant
    Filed: May 1, 1987
    Date of Patent: September 6, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4753934
    Abstract: Compounds of the formula ##STR1## wherein A, B, R.sub.1, X and Q are substituents of various types, and acid addition salts thereof. The compounds are useful as fungicides.
    Type: Grant
    Filed: September 29, 1986
    Date of Patent: June 28, 1988
    Assignee: Celamerck GmbH & Co. KG
    Inventors: Josef Nickl, Helmut Pieper, Jurgen Curtze, Christo Drandarevski, Sigmund Lust
  • Patent number: 4743290
    Abstract: Thiophenesulfonamides of the formula ##STR1## are useful as herbicides.
    Type: Grant
    Filed: November 26, 1986
    Date of Patent: May 10, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Joel R. Christensen, John Cuomo, George Levitt
  • Patent number: 4740232
    Abstract: Herbicidally active 5-amino-1-phenylpyrazoles of the formula ##STR1## in which R is CN, or an ester or amido group,R.sup.1 is an organic radical,R.sup.2 is an organic radical, hydrogen or an acyl or thioacyl radical,R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 can be hydrogen or various organic radicals but at least one is a haloalkyl, haloalkoxy, haloalkylthio, haloalkylsulphinyl or haloalkylsulphonyl radical, but R is not CN at the same time as R.sup.5 is CF.sub.3. The compounds ##STR2## are intermediates therefor and are also herbicidal.
    Type: Grant
    Filed: July 11, 1985
    Date of Patent: April 26, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhold Gehring, Jorg Stetter, Otto Schallner, Ludwig Eue, Hans-Joachim Santel, Robert R. Schmidt
  • Patent number: 4735959
    Abstract: There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.
    Type: Grant
    Filed: May 14, 1985
    Date of Patent: April 5, 1988
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Grell, Gerhart Griss, Robert Sauter, Rudolf Hurnaus, Eckhard Rupprecht, Nikolaus Kaubisch, Joachim Kahling, Bernhard Eisele
  • Patent number: 4728652
    Abstract: 1,4-Dihydropyrimidines of the formula ##STR1## wherein X is sulfur or oxygen and R.sub.4 is aryl or heterocyclo and disclosed. These compounds are useful as cardiovacular agents, particularly anti-hypertensive agents, due to their vasodilator activity.
    Type: Grant
    Filed: April 21, 1986
    Date of Patent: March 1, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4711958
    Abstract: Amino acid derivatives represented by formula ##STR1## wherein His represents an L-histidyl group, X represents a straight or branched alkoxy group having 1 to 7 carbon atoms, a straight or branched alkylamino group having 1 to 7 carbon atoms, a cycloalkyloxy group having 3 to 7 carbon atoms, a morpholino group, said alkoxy group having one or more halogen atoms as substituents; or a pharmaceutically acceptable salt, are useful in the treatment of hypertension.
    Type: Grant
    Filed: April 1, 1987
    Date of Patent: December 8, 1987
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kinji Iizuka, Tetsuhide Kamijo, Tetsuhiro Kubota, Kenji Akahane, Hideaki Umeyama, Yoshiaki Kiso
  • Patent number: 4689414
    Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3 or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;R.sub.5 is hydrogen, alkyl, aryl, arylalkyl, cyano, nitro, ##STR2## Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl-(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl-(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## amino, or substituted amino; m is 0 or an integer of 1 to 6;n is an integer of 1 to 6; andp is an integer of 2 to 6.
    Type: Grant
    Filed: February 24, 1986
    Date of Patent: August 25, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4687507
    Abstract: N-(heterocyclicaminocarbonyl)arylsulfonamides in which the aryl radical is substituted in the 2-position by a carboxy radical, ester, thioester, or amide thereof; e.g. N-[(4,6-dimethylpyrimidin-2-yl)-aminocarbonyl]-2-methoxycarbonylbenzenesul fonamide or N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-2-methoxycarbonylbenze nesulfonamide; are useful for the regulation of plant growth and as pre-emergence and post-emergence herbicides.
    Type: Grant
    Filed: August 9, 1985
    Date of Patent: August 18, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: George Levitt
  • Patent number: 4685956
    Abstract: Herbicidally active 1-aryl-5-hydrazinopyrazoles of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents cyano or nitro,R.sup.3 represents hydrogen, or represents in each case optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl, or represents a radical ##STR2## or represents a radical --SO.sub.2 --R.sup.7, R.sup.4 represents hydrogen, or represents in each case optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl, or represents a radical ##STR3## or represents a radical --SO.sub.2 --R.sup.7, R.sup.5 represents hydrogen: or, in the case where R.sup.4 represents hydrogen, also represents a radical ##STR4## or represents a radical --SO.sub.2 --R.sup.7, or represents in each case optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl, wherein, in each case,X represents oxygen or sulphur,R.sup.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: August 11, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhold Gehring, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt
  • Patent number: 4684656
    Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR2## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR3## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.
    Type: Grant
    Filed: March 14, 1986
    Date of Patent: August 4, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4683228
    Abstract: A guanidine derivative of the formula I: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is substituted by a hydroxy radical and into which is optionally inserted, as part of the backbone of the chain, one or two groups selected from oxygen and sulphur atoms and NH and 1-6C N-alkyl radicals; and the pharmaceutically-acceptable acid additions salts thereof. Pharmaceutical compositions and methods of manufacture are also described. The compound of the formula I is a histamine H-2 antagonist and is therefore useful in ulcer therapy.
    Type: Grant
    Filed: January 22, 1985
    Date of Patent: July 28, 1987
    Assignees: ICI Americas Inc., Imperial Chemical Industries PLC
    Inventors: Karin M. Kirkland, Derrick M. Mant
  • Patent number: 4675045
    Abstract: Thiocarbonylsulfonylureas, useful as herbicides and plant growth regulants, herbicidal compositions employing these compounds and methods of applying them to soil or directly to plants have been discovered.
    Type: Grant
    Filed: May 2, 1986
    Date of Patent: June 23, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Wallace C. Petersen
  • Patent number: 4675319
    Abstract: Novel piperazine derivatives having the general formula: ##STR1## wherein R is hydrogen or lower alkyl, A is straight or branched chain lower alkyl, and R.sub.1 and R.sub.2 are each hydrogen, amino, alkylamino, dialkylamino, mono- or di(hydroxyalkyl)amino, morpholino, pyrrolidino, piperidino, N-alkylpiperazino, 1,3-dithiolan-2-ylidenamino, or N-alkylureido, with the proviso that at least one of R.sub.1 and R.sub.2 is other than hydrogen, or the isomeric mixtures, individual enantiomers or pharmaceutically acceptable acid addition salts thereof, are therapeutically useful antianaphylactic and antibronchospastic agents.
    Type: Grant
    Filed: June 9, 1986
    Date of Patent: June 23, 1987
    Assignee: Recordati S. A. Chemical and Pharmaceutical Company
    Inventors: Dante Nardi, Amedeo Leonardi, Gianni Motta, Pietro Cazzulani
  • Patent number: 4666902
    Abstract: Tetrahydropyridazinones of the formula I ##STR1## wherein R denotes an optionally substituted carbocyclic or heterocyclic radical, R.sup.1 denotes hydrogen; alkyl; aralkyl, which is optionally substituted in the aryl part; or acyl, and R.sup.2 denotes hydrogen; alkyl, which can optionally be substituted; or optionally substituted phenyl; and their acid addition compounds, if these can be prepared.The tetrahydropyridazinone derivatives of the formula I according to the invention and their physiologically acceptable salts exhibit useful pharmacological actions.
    Type: Grant
    Filed: June 8, 1984
    Date of Patent: May 19, 1987
    Assignee: Cassella Aktiengesellschaft
    Inventors: Gerhard Zoller, Rudi Beyerle, Melitta Just, Piero Martorana, Helmut Bohn, Rolf-Eberhard Nitz
  • Patent number: 4666967
    Abstract: The invention provides polyurethanes and polyisocyanurate having incorporated therein a flame retardant amount of a salt formed by reaction between dimethyl methyl phosphonate, monomethyl methyl phosphonate or methyl phosphonic acid, and a compound of the general formula (I). ##STR1## in which X is O, S or NH, R.sup.1 is H, alkyl with 1 to 4 carbon atoms, alkenyl of up to 4 carbon atoms, CN, CONH.sub.2 or NH.sub.2, R.sup.2 is H, alkyl with 1 to 4 carbon atoms or alkenyl of up to 4 carbon atoms or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocyclic ring of up to 6 carbon atoms which may optionally contain another hetero atom and R is H, an alkyl group with 1 to 8 carbon atoms, an aryl group with 6 to 10 carbon atoms, a cycloalkyl group with 5 to 12 carbon atoms or a heterocyclic group with up to 9 ring carbon atoms, or, together with R.sup.1 forms an alkylene chain of 3 to 10 carbon atoms, or R is a group NHR.sup.3 wherein R.sup.
    Type: Grant
    Filed: January 22, 1986
    Date of Patent: May 19, 1987
    Assignee: Ciba-Geigy Corporation
    Inventors: Norman Richardson, deceased, Brian G. Clubley, Richard J. Dellar
  • Patent number: 4666924
    Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S--where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A) is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted heteroaryl. These compounds are useful in the treatment of various cardiac arrhythmias.
    Type: Grant
    Filed: June 4, 1984
    Date of Patent: May 19, 1987
    Assignee: E. I. Du Pont de Nemours & Co.
    Inventors: David M. Stout, William L. Matier
  • Patent number: 4656180
    Abstract: Diamine derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--A--NH--R--NH--B--Q'--(CH.sub.2).sub.n NR.sup.3 R.sup.4 (I)which have a highly selective action on histamine-H.sub.2 receptors and are therefore suitable for use as anti-ulcerative agents are described. Processes for the preparation of these compounds and pharmaceutical preparations containing these compounds are also described.
    Type: Grant
    Filed: March 5, 1985
    Date of Patent: April 7, 1987
    Assignee: Ludwig Heumann & Co., GmbH
    Inventors: Stefan Postius, Rolf Herter, Peter Morsdorf, Helmut Schickaneder, Istvan Szelenyi, Kurt H. Ahrens
  • Patent number: 4639479
    Abstract: A polyalkylenepolyamine ("PAPA") main chain having pendant substituted 2-oxo-piperazinyl-triazines attached to the N atoms of the PAPA main chain are novel compounds which have highly desirable UV-light stabilizing (UV-S) activity coupled with unexpectedly good thermal stability. These compounds, referred to as "pendant piperazinyl triazines" or P[PIP-T] for brevity, are used in polymer recipes to formulate a stabilized polymeric composition comprising a light-degradable organic polymer containing an effective amount of a P[PIP-T] sufficient to stabilize the polymer. A P[PIP-T] is especially effective in a polyolefin in which there is from about 0.1 percent by weight (% by wt), to about 5% by wt, and is also effective in a wide variety of pastel colored and/or transparent commercially significant polymers.
    Type: Grant
    Filed: September 20, 1985
    Date of Patent: January 27, 1987
    Assignee: The BFGoodrich Company
    Inventors: John T. Lai, Pyong N. Son
  • Patent number: 4629495
    Abstract: Herbicidal compounds of the formula: ##STR1## wherein A represents R.sup.1 R.sup.2 N-- (wherein R.sup.1 represents C.sub.1-8 alkyl or C.sub.2-8 alkenyl or alkynyl unsubstituted or substituted by CN, OH, C.sub.1-6 alkoxy, carboxy, C.sub.2-9 alkoxycarbonyl, aminocarbonyl optionally substituted by C.sub.1-8 alkyl or C.sub.2-8 alkenyl, C.sub.1-8 alkoxyaminocarbonyl, C.sub.1-8 alkanesulphonamidocarbonyl, --C(.dbd.O)Het, where Het represents a nitrogen-containing heterocyclic group, or one or more halogen atoms or R.sup.1 represents C.sub.3-6 cycloalkyl optionally substituted by C.sub.1-4 alkyl and R.sup.2 represents H or R.sup.1, or R.sup.1 represents C.sub.1-4 alkylthio and R.sup.2 represents H, or A represents R.sup.p (R.sup.q)--C.dbd.N-- (wherein R.sup.p represents C.sub.1-4 alkoxy or amino substituted by one or two C.sub.1-4 alkyl groups and R.sup.q represents H or C.sub.1-4 alkyl) or A represents 2-oxo-azetidin-1-yl, 2-oxo-pyrrolidin-1-yl or 2-oxo-piperidin-1-yl optionally substituted by C.sub.
    Type: Grant
    Filed: July 13, 1983
    Date of Patent: December 16, 1986
    Assignee: May & Baker Limited
    Inventors: Leslie R. Hatton, Edgar W. Parnell, David A. Roberts
  • Patent number: 4618607
    Abstract: 1,4-Dihydropyridine-3,5-dicarboxylic acid ester derivatives of the general formula: ##STR1## or acid addition salts thereof, wherein W is --CH.dbd. or --N.dbd.; Y is --CH.dbd.CH--, --O--, --S--, --CH.dbd.N(O)p-- (p is zero or 1) or --N(R)-- (R is hydrogen or lower alkyl); X.sup.1, X.sup.2 and X.sup.3 are the same or different, and are each hydrogen, halogen, nitro, trifluoromethyl, cyano or lower alkylthio; Z is aryl or 5- or 6-membered aromatic heterocyclic ring (which may have a substituent or two or three substituents which may be the same or different, and the substituent may be halogen, lower alkyl, lower alkoxy, lower alkanoylamino, cyano, nitro, lower alkylthio, trifluoromethyl, sulfamoyl, di-lower alkylsulfamoyl, amino or di-lower alkylamino); ##STR2## is 5- to 7-membered heterocyclic ring which may have nitrogen atom, oxygen atom, sulfur atom or unsaturated bond on the ring, and may be substituted by lower alkyl, lower alkoxycarbonyl, lower alkanoylamino, ethylenedioxy or --(CH.sub.2).sub.m --OR.sup.
    Type: Grant
    Filed: December 10, 1982
    Date of Patent: October 21, 1986
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Kazuhiko Araki, Hideki Ao, Jun Inui, Kenichi Aihara
  • Patent number: 4615726
    Abstract: Compounds of the formula ##STR1## wherein A denotes N or CR.sup.4, B denotes a carboxyl, carbo-(thio) ester, (substituted) carboxamide or carboxanilide, carbohydroxy(alkoxy)-amide, (substituted) carbohydrazide or (substituted) oxazoline group, X and Y denote, inter alia, alkyl or, together, spiroalkyl, Z denotes a carbo-(di)(thio) ester, carboxyl, (substituted) (thio)-carboxamide or -carboxanilide group or the radical of a ketone-acid or of a ketone-ester and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 denote H or are identical or different and denote halogen, alkyl, alkoxy, alkoxycarbonyl, halogenoalkyl, NO.sub.2, CN, (substituted) phenyl or phenoxy, or two of these radicals can form a --CH.dbd.CH--CH.dbd.CH-- group, are useful total or selective herbicides for application by the pre-emergence and, in some cases, the post-emergence method.
    Type: Grant
    Filed: December 18, 1984
    Date of Patent: October 7, 1986
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Roland Schmierer, Reinhard Handte, Hilmar Mildenberger, Klaus Bauer, Hermann Bieringer, Helmut Burstell
  • Patent number: 4616002
    Abstract: Compounds of the formula I ##STR1## in which n represents 1, 2 or 3, Ar represents a carbocyclic or heterocyclic aryl radical, Ac represents the acyl radical of an acid, Z represents a radical --OR.sub.7 or --NR.sub.8 R.sub.9, R.sub.1 represents hydrogen, unsubstituted or substituted lower alkyl, a carbocyclic or heterocyclic aryl radical or free, etherified or esterified hydroxy, R.sub.2 and R.sub.3, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl, formyl or functionally modified formyl, carboxy or functionally modified carboxy, a carbocyclic or heterocyclic aryl radical or unsubstituted or mono- or di-substituted amino, R.sub.4 represents hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl or a carbocyclic or heterocyclic aryl radical, R.sub.7, R.sub.8 and R.sub.
    Type: Grant
    Filed: January 6, 1986
    Date of Patent: October 7, 1986
    Assignee: Ciba-Geigy Corporation
    Inventors: Bruno Kamber, Thomas Leutert, Hans Kuhnis, Kurt Eichenberger
  • Patent number: 4572910
    Abstract: 1,2,4-Triazolo[1,5-c]pyrimidines substituted at the 5 or 7 positions through a nitrogen atom which is part of a heterocyclic ring have been found to have potent bronchodilator activity. Methods for inducing bronchodilation, pharmaceutical compositions and synthetic processes are also disclosed.
    Type: Grant
    Filed: March 3, 1983
    Date of Patent: February 25, 1986
    Assignee: Riker Laboratories, Inc.
    Inventor: James J. Wade
  • Patent number: 4562184
    Abstract: Novel substituted-aminohydroxypropoxy-thiadiazoles and pharmaceutically acceptable salts thereof exhibit .beta.-adrenergic blocking activity.
    Type: Grant
    Filed: April 2, 1984
    Date of Patent: December 31, 1985
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Patent number: 4550118
    Abstract: Compounds of Formula I are described ##STR1## in which X and Y are independently --NH--, --O-- or --S--; Z may be a pyrimidine, triazine, triazole, thiazole, thiadiazole ring. The methods of preparation are described. The compounds are useful as antipeptic ulcer agents.
    Type: Grant
    Filed: October 24, 1983
    Date of Patent: October 29, 1985
    Assignees: Ikeda Mohando Co., Ltd., Otsuka Pharmaceutical Co., Ltd.
    Inventors: Toshiya Sugino, Fujio Nohara, Tomoaki Fujinawa, Kazuo Ogawa, Teruo Mizukami, Shunichi Shirai
  • Patent number: 4523018
    Abstract: Chromogenic compounds of colorless or lightly colored form are disclosed having the following structural formula: ##STR1## wherein X represents an optionally substituted aminophenyl, indolyl, julolidinyl, kairolyl, piperidinophenyl, pyrrolidinophenyl, morpholinyl, carbazolyl or indolizinyl radical. The compounds of this invention are eligible for use in pressure-sensitive and heat-sensitive record materials and manifold marking systems.
    Type: Grant
    Filed: October 21, 1982
    Date of Patent: June 11, 1985
    Assignee: Yamamoto Kagaku Gosei Co., Ltd.
    Inventors: Yojiro Kumagae, Yasuhisa Iwasaki
  • Patent number: RE33125
    Type: Grant
    Filed: July 11, 1986
    Date of Patent: December 5, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Henry F. Campbell, Thomas H. Scholtz, George H. Douglas