Additional Nitrogen Containing Hetero Ring (e.g., Thiazole, Etc.) Patents (Class 544/82)
-
Patent number: 4966855Abstract: 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: GrantFiled: July 2, 1985Date of Patent: October 30, 1990Assignee: Boehringer Mannheim GmbHInventors: Ulfert Deneke, Werner Guthlein, Wolfgang Weckerle, Hans Wielinger
-
Patent number: 4956467Abstract: 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: GrantFiled: April 5, 1989Date of Patent: September 11, 1990Assignee: American Cyanamid CompanyInventors: Lois M. Hinman, Libby S. Miller
-
Patent number: 4950755Abstract: 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: GrantFiled: September 28, 1988Date of Patent: August 21, 1990Assignee: Ohio State UniversityInventors: Donald T. Witiak, Hattiangadi B. Bhat
-
Patent number: 4948416Abstract: This invention relates to novel condensed ring sulfonylureas and their use as herbicides and growth regulants.Type: GrantFiled: March 27, 1989Date of Patent: August 14, 1990Assignee: E. I. du Pont de Nemours and CompanyInventor: Robert J. Pasteris
-
Patent number: 4944790Abstract: 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: GrantFiled: March 20, 1989Date of Patent: July 31, 1990Assignee: Ciba-Geigy CorporationInventors: Hans Moser, Beat Bohner, Werner Fory
-
Patent number: 4906624Abstract: 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: GrantFiled: August 2, 1988Date of Patent: March 6, 1990Assignee: Warner-Lambert CompanyInventors: Alexander W. Chucholowski, Mark W. Creswell, Bruce D. Roth, Drago R. Sliskovic
-
Patent number: 4904783Abstract: 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: GrantFiled: September 19, 1988Date of Patent: February 27, 1990Assignee: Ciba-Geigy CorporationInventor: Werner Topfl
-
Patent number: 4902336Abstract: 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: GrantFiled: September 19, 1988Date of Patent: February 20, 1990Assignee: Ciba-Geigy CorporationInventor: Werner Topfl
-
Patent number: 4897105Abstract: 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: GrantFiled: March 20, 1987Date of Patent: January 30, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Yoshiyuki Okada, Isao Aoki, Nobuyuki Okajima, Takashi Kuragano
-
Patent number: 4889857Abstract: 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: GrantFiled: September 29, 1988Date of Patent: December 26, 1989Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Kazuhiko Araki, Tsuyoshi Kuroda, Satoru Uemori, Akihiko Moriguchi, Yoshifumi Ikeda
-
Patent number: 4873253Abstract: 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: GrantFiled: March 30, 1987Date of Patent: October 10, 1989Assignees: Shosuke Okamoto, Showa Denko Kabushiki KaishaInventors: Shosuke Okamoto, Yoshio Okada, Akiko Okunomiya, Taketoshi Naito, Yoshio Kimura, Morihiko Yamada, Norio Ohno, Yasuhiro Katsuura, Hiroshi Nojima, Takashi Shishikura
-
Patent number: 4853383Abstract: 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: GrantFiled: September 8, 1986Date of Patent: August 1, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello
-
Patent number: 4851410Abstract: 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: GrantFiled: November 15, 1988Date of Patent: July 25, 1989Assignee: BASF AktiengesellschaftInventors: Bernd Ostersehlt, Norbert Rieber, Josef Gries
-
Patent number: 4847379Abstract: 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: GrantFiled: November 30, 1987Date of Patent: July 11, 1989Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
-
Patent number: 4845081Abstract: N-methylamino derivatives of biologically active substances which have enhanced delivery across topical membranes and pharmaceutical compositions adapted for topical administration containing same.Type: GrantFiled: September 12, 1986Date of Patent: July 4, 1989Assignee: University of FloridaInventor: Kenneth B. Sloan
-
Patent number: 4843068Abstract: 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: GrantFiled: December 29, 1986Date of Patent: June 27, 1989Assignee: Nihon Nohyaku Co., Ltd.Inventors: Hiroshi Hamaguchi, Hideo Takaishi, Tetsuji Ohshima, Takamichi Konno, Yukio Miyagi, Shiraiwa Yutaka, Takayuki Akita
-
Patent number: 4838926Abstract: 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: GrantFiled: September 14, 1987Date of Patent: June 13, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Mary A. Hanagan, Barry A. Wexler
-
Patent number: 4833246Abstract: 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: GrantFiled: December 2, 1987Date of Patent: May 23, 1989Assignee: Fuji Photo Film Co., Ltd.Inventors: Keiichi Adachi, Shigeru Ohno, Yoshio Inagaki, Nobuo Seto, Yoshihiro Jinbo
-
Patent number: 4831151Abstract: 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: GrantFiled: April 21, 1986Date of Patent: May 16, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Helmut Link, Marc Montavon, Eva M. Karpitschka, Wilhelm Klotzer, Renate Mussner
-
Patent number: 4808727Abstract: 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: GrantFiled: September 29, 1987Date of Patent: February 28, 1989Assignee: Hoffmann-LaRoche Inc.Inventor: Helmut Link
-
Patent number: 4788283Abstract: 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: GrantFiled: March 21, 1986Date of Patent: November 29, 1988Assignee: Ciba-Geigy CorporationInventor: Friedrich Karrer
-
Patent number: 4783537Abstract: 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: GrantFiled: November 13, 1985Date of Patent: November 8, 1988Assignee: Pennwalt CorporationInventor: Robert J. Murray
-
Patent number: 4769371Abstract: 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: GrantFiled: May 1, 1987Date of Patent: September 6, 1988Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
-
Patent number: 4753934Abstract: 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: GrantFiled: September 29, 1986Date of Patent: June 28, 1988Assignee: Celamerck GmbH & Co. KGInventors: Josef Nickl, Helmut Pieper, Jurgen Curtze, Christo Drandarevski, Sigmund Lust
-
Patent number: 4743290Abstract: Thiophenesulfonamides of the formula ##STR1## are useful as herbicides.Type: GrantFiled: November 26, 1986Date of Patent: May 10, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: Joel R. Christensen, John Cuomo, George Levitt
-
Patent number: 4740232Abstract: 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: GrantFiled: July 11, 1985Date of Patent: April 26, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhold Gehring, Jorg Stetter, Otto Schallner, Ludwig Eue, Hans-Joachim Santel, Robert R. Schmidt
-
Patent number: 4735959Abstract: 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: GrantFiled: May 14, 1985Date of Patent: April 5, 1988Assignee: Dr. Karl Thomae GmbHInventors: Wolfgang Grell, Gerhart Griss, Robert Sauter, Rudolf Hurnaus, Eckhard Rupprecht, Nikolaus Kaubisch, Joachim Kahling, Bernhard Eisele
-
Patent number: 4728652Abstract: 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: GrantFiled: April 21, 1986Date of Patent: March 1, 1988Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
-
Patent number: 4711958Abstract: 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: GrantFiled: April 1, 1987Date of Patent: December 8, 1987Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kinji Iizuka, Tetsuhide Kamijo, Tetsuhiro Kubota, Kenji Akahane, Hideaki Umeyama, Yoshiaki Kiso
-
Patent number: 4689414Abstract: 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: GrantFiled: February 24, 1986Date of Patent: August 25, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
-
Patent number: 4687507Abstract: 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: GrantFiled: August 9, 1985Date of Patent: August 18, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: George Levitt
-
Patent number: 4685956Abstract: 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: GrantFiled: July 14, 1986Date of Patent: August 11, 1987Assignee: Bayer AktiengesellschaftInventors: Reinhold Gehring, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt
-
Patent number: 4684656Abstract: 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: GrantFiled: March 14, 1986Date of Patent: August 4, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
-
Patent number: 4683228Abstract: 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: GrantFiled: January 22, 1985Date of Patent: July 28, 1987Assignees: ICI Americas Inc., Imperial Chemical Industries PLCInventors: Karin M. Kirkland, Derrick M. Mant
-
Patent number: 4675045Abstract: 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: GrantFiled: May 2, 1986Date of Patent: June 23, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Wallace C. Petersen
-
Patent number: 4675319Abstract: 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: GrantFiled: June 9, 1986Date of Patent: June 23, 1987Assignee: Recordati S. A. Chemical and Pharmaceutical CompanyInventors: Dante Nardi, Amedeo Leonardi, Gianni Motta, Pietro Cazzulani
-
Patent number: 4666902Abstract: 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: GrantFiled: June 8, 1984Date of Patent: May 19, 1987Assignee: Cassella AktiengesellschaftInventors: Gerhard Zoller, Rudi Beyerle, Melitta Just, Piero Martorana, Helmut Bohn, Rolf-Eberhard Nitz
-
Patent number: 4666967Abstract: 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: GrantFiled: January 22, 1986Date of Patent: May 19, 1987Assignee: Ciba-Geigy CorporationInventors: Norman Richardson, deceased, Brian G. Clubley, Richard J. Dellar
-
Patent number: 4666924Abstract: 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: GrantFiled: June 4, 1984Date of Patent: May 19, 1987Assignee: E. I. Du Pont de Nemours & Co.Inventors: David M. Stout, William L. Matier
-
Patent number: 4656180Abstract: 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: GrantFiled: March 5, 1985Date of Patent: April 7, 1987Assignee: Ludwig Heumann & Co., GmbHInventors: Stefan Postius, Rolf Herter, Peter Morsdorf, Helmut Schickaneder, Istvan Szelenyi, Kurt H. Ahrens
-
Patent number: 4639479Abstract: 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: GrantFiled: September 20, 1985Date of Patent: January 27, 1987Assignee: The BFGoodrich CompanyInventors: John T. Lai, Pyong N. Son
-
Patent number: 4629495Abstract: 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: GrantFiled: July 13, 1983Date of Patent: December 16, 1986Assignee: May & Baker LimitedInventors: Leslie R. Hatton, Edgar W. Parnell, David A. Roberts
-
Patent number: 4618607Abstract: 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: GrantFiled: December 10, 1982Date of Patent: October 21, 1986Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Kazuhiko Araki, Hideki Ao, Jun Inui, Kenichi Aihara
-
Patent number: 4615726Abstract: 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: GrantFiled: December 18, 1984Date of Patent: October 7, 1986Assignee: Hoechst AktiengesellschaftInventors: Roland Schmierer, Reinhard Handte, Hilmar Mildenberger, Klaus Bauer, Hermann Bieringer, Helmut Burstell
-
Patent number: 4616002Abstract: 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: GrantFiled: January 6, 1986Date of Patent: October 7, 1986Assignee: Ciba-Geigy CorporationInventors: Bruno Kamber, Thomas Leutert, Hans Kuhnis, Kurt Eichenberger
-
Patent number: 4572910Abstract: 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: GrantFiled: March 3, 1983Date of Patent: February 25, 1986Assignee: Riker Laboratories, Inc.Inventor: James J. Wade
-
Patent number: 4562184Abstract: Novel substituted-aminohydroxypropoxy-thiadiazoles and pharmaceutically acceptable salts thereof exhibit .beta.-adrenergic blocking activity.Type: GrantFiled: April 2, 1984Date of Patent: December 31, 1985Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello
-
Patent number: 4550118Abstract: 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: GrantFiled: October 24, 1983Date of Patent: October 29, 1985Assignees: Ikeda Mohando Co., Ltd., Otsuka Pharmaceutical Co., Ltd.Inventors: Toshiya Sugino, Fujio Nohara, Tomoaki Fujinawa, Kazuo Ogawa, Teruo Mizukami, Shunichi Shirai
-
Patent number: 4523018Abstract: 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: GrantFiled: October 21, 1982Date of Patent: June 11, 1985Assignee: Yamamoto Kagaku Gosei Co., Ltd.Inventors: Yojiro Kumagae, Yasuhisa Iwasaki
-
Patent number: RE33125Type: GrantFiled: July 11, 1986Date of Patent: December 5, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Henry F. Campbell, Thomas H. Scholtz, George H. Douglas