1,2-diazole (including Hydrogenated) Patents (Class 546/211)
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Patent number: 4917992Abstract: Salts of 1-phenyl-3-pyrazolidinones which are useful photographic silver halide developing agents.Type: GrantFiled: October 23, 1987Date of Patent: April 17, 1990Assignee: Ciba-Geigy AGInventors: Malcolm D. Tirel, William E. Long
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Patent number: 4918083Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereof, or a pharmaceutically acceptable solvate thereof, wherein:Z represents a residue of a substituted or unsubstituted aryl group,A.sup.1 represents a substituted or unsubstituted methylene group or a substituted or unsubstituted ethylene group;A.sup.2 represents a substituted or unsubstituted methylene group or a substituted or unsubstituted ethylene group;providing that at least one of A.sup.1 or A.sup.2 represents a substituted methylene group or a substituted ethylene group,X represents O or NR.sup.o wherein R.sup.Type: GrantFiled: November 24, 1987Date of Patent: April 17, 1990Assignee: Beecham Group p.l.c.Inventors: John M. Berge, Lee J. Beeley
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Patent number: 4916234Abstract: Chromogenic dicyanomethylenepyrazolinone for thermographic recording processes and the corresponding cyanomethylene dyes of the formula ##STR1## in which R is hydrogen, hydroxyl, amino, alkyl, cycloalkyl, aryl, aralkyl or a heterocyclic radical, T.sub.1 and T.sub.2, independently of one another, are each hydrogen, unsubstituted or halogen-, hydroxyl-, cyano- or lower alkoxy-substituted alkyl having a maximum of 12 carbon atoms, cycloalkyl having 5 to 10 carbon atoms or unsubstituted or halogen-, cyano-, lower alkyl- or lower alkoxy-(ring)substituted phenalkyl or phenyl, or T.sub.1 and T.sub.2 together with the nitrogen linking them are a five- or six-membered heterocyclic radical, and rings A and B, independently of one another, are unsubstituted or substituted by halogen, cyano, nitro, lower alkyl, lower alkoxy, (lower alkyl)carbonyl or (lower alkoxy)carbonyl.Type: GrantFiled: June 8, 1989Date of Patent: April 10, 1990Assignee: Ciba-Geigy CorporationInventors: Hans Junek, Manfred Klade
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Patent number: 4916150Abstract: N-[alkylamino)alkyl]-3,4(or 4,5)-diaryl-1H-pyrazole-1-(branched)alkanamides and pyrazole-1-alkanamines useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic acid with an appropriate diamine followed by reduction or by reacting the anion of a lower-alkyl ester of a pyrazole-1-acetic acid with an alkylating agent followed by displacement of the ester by an appropriate amine.Type: GrantFiled: March 22, 1989Date of Patent: April 10, 1990Assignee: Sterling Drug Inc.Inventors: Denis M. Bailey, Ronald G. Powles
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Patent number: 4914227Abstract: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.Type: GrantFiled: May 16, 1986Date of Patent: April 3, 1990Assignee: Banyu Pharmaceutical Company, Ltd.Inventors: Tetsuji Miyano, Kunio Suzuki, Ryosuke Ushijima, Susumu Nakagawa
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Patent number: 4909830Abstract: Herbicidal 3-aminopyrazolin-5-ones of the formula ##STR1## in which R.sup.1 stands for alkyl, alkenyl, halogenoalkyl, halogenoalkenyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, for optionally substituted aralkyl or for optionally substituted aryl,R.sup.2 stands for hydrogen or alkyl,R.sup.3 stands for hydrogen or alkyl,R.sup.4 stands for hydrogen, alkyl, alkenyl, alkinyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonylalkyl or alkanoyl, orR.sup.3 and R.sup.4 together stand for an alkylene or alkenylene radical, each of which is divalent,X stands for halogen, alkyl, alkoxy, alkylthio, halogenoalkyl. halogenoalkoxy or halogenoalkylthio, andZ stands for hydrogen, halogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy or halogenoalkylthio,and acid addition salts thereof. Intermediates of the formula ##STR2## are also disclosed.Type: GrantFiled: November 10, 1988Date of Patent: March 20, 1990Assignee: Bayer AktiengesellschaftInventors: Uta Jensen-Korte, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
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Patent number: 4904686Abstract: Compounds of the following formula have pharmacutical properties: ##STR1## in which R.sup.1 and R.sup.2 independently are hydrogen, halo, nitro, amino, C.sub.2-5 acylamino, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene bridge, R.sup.3 is C.sub.1-4 alkyl or C.sub.2-4 alkenyl, and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.2 --, and n is 1, 2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a C.sub.1-3 alkylene chain; and salts thereof.Type: GrantFiled: April 11, 1988Date of Patent: February 27, 1990Assignee: Lilly Industries LimitedInventors: Maria I. F. Fernandez, Terrence M. Hotten, David E. Tupper
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Patent number: 4898880Abstract: N-[(heterocycle)alkyl]-3,4 (or 4,5)-diaryl-1H-pyrazole-1-acetamides and pyrazole-1-propanamides, useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic or propanoic acid with an appropriate (heterocycle-alkyl) amine or by reacting a pyrazole-1-acetic or propanoic acid with an appropriate (heterocycle-alkyl)amine.Type: GrantFiled: March 22, 1989Date of Patent: February 6, 1990Assignee: Sterling Drug Inc.Inventors: Denis M. Bailey, George Y. Lesher, Thomas E. D'Ambra
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Patent number: 4888352Abstract: N-[(disubstituted amino)alkyl]-3,4 or 5-aryl-1H-pyrazole-1-acetamides, useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic acid with an appropriate diamine.Type: GrantFiled: March 22, 1989Date of Patent: December 19, 1989Assignee: Sterling Drug Inc.Inventors: Denis M. Bailey, Virendra Kumar
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Patent number: 4870095Abstract: N-[(disubstituted amino)alkyl]-3,4 (or 4,5)-diaryl-1H-pyrazole-1-acetamides and pyrazole-1-propanamides, useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic or propanoic acid with an appropriate diamine or by reacting a lower-alkyl ester of a pyrazole-1-acetic or propanoic acid with an .omega.-aminoalkanol, followed by activation of the alcohol and displacement by an appropriate amine.Type: GrantFiled: March 22, 1989Date of Patent: September 26, 1989Assignee: Sterling Drug, Inc.Inventor: Denis M. Bailey
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Patent number: 4857643Abstract: 2-Substituted thiazolidines compounds having formula I ##STR1## wherein X is a CH.sub.2, O or S, R is hydroxy or an acyloxy, alkyloxy, alkenyloxy or alkinyloxy group, R.sub.1 is hydrogen or a group of formula ##STR2## R.sub.2 is hydrogen or a free or esterified carboxy group, R.sub.a and R.sub.b are hydrogen or methyl, p is zero or 1, R.sub.3 is hydrogen, a C.sub.1 -C.sub.2 alkylsulphonyl group, a phenyl or p-Cl phenyl, p-methylsulphonyl group or an acyl group; are useful as mucus regulating, antitussive and antibronchospastic agents.Type: GrantFiled: November 3, 1988Date of Patent: August 15, 1989Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Carmelo A. Gandolfi, Silvano Spinelli, Odoardo Tofanetti, Raimondo Russo, Sergio Tognella
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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
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Patent number: 4849521Abstract: The present invention is directed to an improved stereoselective tandem substitution and reduction of an imine precursor to the cis form of 3-substituted-4-(phenylanilo)piperidine compounds or their substituted derivatives.Type: GrantFiled: November 2, 1987Date of Patent: July 18, 1989Assignee: BOC, Inc.Inventors: Linas V. Kudzma, H. Kenneth Spencer, Sherry A. Severnak
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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
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Patent number: 4837333Abstract: This disclosure relates to a class of novel substituted alkylidene imidazole derivatives and pharmaceutically acceptable salts thereof. The disclosure further describes pharmaceutical compositions containing such compounds and to the use of such compounds and compositions as agents for selectively inhibiting the action of the enzyme thromboxane synthetase.Type: GrantFiled: May 14, 1987Date of Patent: June 6, 1989Assignee: G. D. Searle & Co.Inventors: Paul W. Manley, Roderick A. Porter, Mun F. Lai
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Patent number: 4831192Abstract: Compounds are disclosed of the formula ##STR1## Where R.sup.1 is an unsubstituted or substituted heterocyclic ring system; R.sup.2 is an unsubstituted or substituted phenyl; R.sup.3 is a lower alkyl or lower alkoxy, and L is selected from a wide variety of groups.Type: GrantFiled: December 31, 1987Date of Patent: May 16, 1989Assignee: BOC, Inc.Inventors: Bor-Sheng Lin, Joseph W. Scheblein
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Patent number: 4826993Abstract: 4-Substituted 1-(optionally substituted)diazolidinones are intermediates to 7-substituted bicyclic pyrazolidinone antimicrobials.Type: GrantFiled: May 14, 1986Date of Patent: May 2, 1989Assignee: Eli Lilly and CompanyInventors: Richard E. Holmes, Louis N. Jungheim
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Patent number: 4814001Abstract: Herbicidal and plant growth-regulating novel 5-acylamino-pyrazoles of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl or optionally substituted cycloalkyl,Ar represents in each case optionally substituted phenyl or pyridyl,X represents oxygen or sulphur,A represents a straight-chain or branched optionally substituted alkylene bridge,n represents the numbers 0 or 1 andY represents cyano or the grouping ##STR2## wherein X.sup.1 represents oxygen or sulphur andR.sup.3 represents hydroxyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, amino, alkylamino, dialkylamino, alkenylamino, dialkenylamino, alkyl-alkenylamino or a --OM radical,whereinM represents one equivalent of the cation of an inorganic or organic base.Intermediates therefor of the formula ##STR3## are also new.Type: GrantFiled: May 5, 1988Date of Patent: March 21, 1989Assignee: Bayer AktiengesellschaftInventors: Jorg Stetter, Otto Schallner, Reinhold Gehring, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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Patent number: 4810283Abstract: Novel 1-aryl-4-nitro-pyrazoles which exhibit herbicidal and plant growth-regulating activity of the formula ##STR1## in which R.sup.1 represents in each case optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl andR.sup.2 represents hydrogen, or represents in each case optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl, or represents a radical ##STR2## or R.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, represent a saturated heterocyclic radical, which can optionally contain further hetero atoms, andAr represents in each case optionally substituted phenyl or pyridyl,whereinX represents oxygen or sulphur andR.sup.Type: GrantFiled: October 30, 1986Date of Patent: March 7, 1989Assignee: Bayer AktiengesellschaftInventors: Reinhold Gehring, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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Patent number: 4791121Abstract: Compounds are disclosed of the formula ##STR1## where R.sup.2 is unsubstituted or substituted phenyl, R.sup.3 is lower alkyl, lower cycloalkyl or lower alkoxy lower alkyl, and L is selected from a wide variety of groups. This new class of compounds exhibit improved analgesic and anesthetic properties.Type: GrantFiled: November 2, 1987Date of Patent: December 13, 1988Assignee: The BOC Group, Inc.Inventors: Linas V. Kudzma, H. Kenneth Spencer, Sherry A. Severnak
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Patent number: 4791120Abstract: Compounds are disclosed of the formula ##STR1## where R.sup.1 is an unsubstituted or substituted heterocyclic ring system; R.sup.2 is an unsubstituted or substituted phenyl; R.sup.3 is a lower alkyl or lower alkoxy, and L is selected from a wide variety of groups.Type: GrantFiled: December 31, 1987Date of Patent: December 13, 1988Assignee: The BOC Group, Inc.Inventors: Bor-Sheng Lin, Linas V. Kudzma, H. Kenneth Spencer
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Patent number: 4783535Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed. The oxazepinones and oxazepinethiones prepared by the process have utility as antihistaminics with low sedative potential. Novel intermediate compounds are also disclosed.Type: GrantFiled: March 18, 1986Date of Patent: November 8, 1988Assignee: A. H. Robins Company, IncorporatedInventors: Young S. Lo, Albert D. Cale, Jr.
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Patent number: 4782086Abstract: Fungicidally active novel E-isomers of N.sup..alpha. -(2-cyano-2-alkoximino-acetyl)-amino acid derivatives and peptides of the general formula (I) ##STR1## in which R represents alkyl, alkenyl, alkinyl, cyanoalkyl, azolylalkyl or optionally substituted phenylalkyl, or represents optionally substituted cycloalkyl;R.sup.1 represents hydrogen, alkyl, optionally substituted phenyl or optionally substituted benzyl, or represents alkoxycarbonylamino;R.sup.2 represents hydrogen or alkyl;R.sup.3 represents hydrogen, alkyl, alkoxycarbonylalkyl, hydroxycarbonylalkyl, aminocarbonylalkyl, azolylalkyl, cyanoalkyl, hydroxyalkyl, alkenyl, alkinyl or optionally substituted cycloalkyl, or represents optionally substituted phenyl or phenylalkyl, or represents the groupingR.sup.4 --SO.sub.n --Z--R.sup.4 n and Z having various meanings, andX is --OH--OR.sup.1 or --NR.sup.2 R.sup.3.Type: GrantFiled: February 20, 1987Date of Patent: November 1, 1988Assignee: Bayer AktiengesellschaftInventors: Winfried Lunkenheimer, Hans Scheinpflug, Wilhelm Brandes
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Patent number: 4772309Abstract: A 5-Acylamino-pyrazole derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl or optionally substituted cycloalkyl,R.sup.3 represents hydrogen or alkyl,R.sup.4 represents hydrogen or alkyl,X represents oxygen or sulphur,n represents the integer 0, 1 or 2,Ar represents in each case optionally substituted phenyl or pyridyl andHet represents an optionally substituted 5- or 6- membered heterocyclic radical linked via a carbon atom,which exhibit herbicidal and plant growth regulating activity.Type: GrantFiled: March 19, 1987Date of Patent: September 20, 1988Assignee: Bayer AktiengesellschaftInventors: Jorg Stetter, Reinhold Gehring, Otto Schallner, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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Patent number: 4771066Abstract: Insecticidally and acarididally active 1-arylpyrazoles of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl or halogen alkyl,R.sup.2 represents alkyl, alkenyl, alkinyl, cycloalkyl, halogenoalkyl, halogenoalkenyl, alkoxyalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, optionally substituted aralkyl or optionally substituted aryl,R.sup.3 represents alkyl, alkenyl, alkinyl, halogenoalkyl, halogenoalkenyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl or optionally substituted aralkyl,R.sup.4 represents alkyl, alkenyl, alkinyl, halogenoalkyl, halogenoalkenyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl or optionally substituted aralkyl, and, in addition, also represents hydrogen in the case where R.sup.3 does not simultaneously represent unsubstituted alkyl, orR.sup.3 and R.sup.Type: GrantFiled: February 12, 1987Date of Patent: September 13, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhold Gehring, Uta Jensen-Korte, Otto Schallner, Jorg Stetter, Heinz-Jurgen Wroblowsky, Benedikt Becker, Wolfgang Behrenz, Bernhard Homeyer, Wilhelm Stendel
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Patent number: 4742060Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.Type: GrantFiled: January 21, 1986Date of Patent: May 3, 1988Assignee: Nihon Tokushu Noyaku Seizo K. K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
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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
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Patent number: 4740231Abstract: 1-Aryl-5-alkoximinoalkylamino-pyrazoles of the formula ##STR1## in which R represents cyano or nitro, or represents an optionally substituted heterocyclic radical,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl, or represents optionally substituted aryl,R.sup.3 represents hydrogen, alkyl or alkenyl, or represents in each case optionally substituted aralkyl or aryl andAr represents optionally substituted phenyl or pyridyl,are active as herbicides and plant growth regulants. Compounds of the formula ##STR2## in which R" has the same definition as R other than cyano, are also active and useful as intermediates as well.Type: GrantFiled: May 22, 1986Date of Patent: April 26, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhold Gehring, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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Patent number: 4732981Abstract: Salts of 1-phenyl-3-pyrazolidinones which are useful photographic silver halide developing agents.Type: GrantFiled: April 1, 1987Date of Patent: March 22, 1988Assignee: Ciba-Geigy AGInventors: Malcolm D. Tirel, William E. Long
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Patent number: 4703119Type: GrantFiled: June 4, 1985Date of Patent: October 27, 1987Assignee: Bayer AktiengesellschaftInventors: Egbert Wehinger, Horst Meyer
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Patent number: 4695566Abstract: 3-(aminoalkylaminocarbonylmethoxy)-5-phenylpyrazole compounds corresponding to the formula: ##STR1## in which R.sub.1, R.sub.2, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 and R.sub.9 may be hydrogen or lower alkyl groups, or R.sub.5 with R.sub.6 and/or R.sub.8 with R.sub.9 may also form specified cyclic groups, R.sub.3 and R.sub.4 may be hydrogen, halogen, lower alkyl, lower alkoxy, trifluoromethyl, nitro, hydroxy or alkylene dioxy, and Z represents an alkylene chain or the 2-hydroxypropylene chain. The compounds possess pharmacological, in particular antiarrhythmic, properties.Type: GrantFiled: July 2, 1985Date of Patent: September 22, 1987Assignee: Kali-Chemie Pharma GmbHInventors: Henning Heinemann, Wolfgang Kehrbach, Uwe Schoen, Gerd Buschmann, Ulrich Kuhl
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Patent number: 4687846Abstract: Salts of 1-phenyl-3-pyrazolidinones which are useful photographic silver halide developing agents.Type: GrantFiled: February 28, 1986Date of Patent: August 18, 1987Assignee: Ciba-Geigy AGInventors: Malcolm D. Tirel, William E. Long
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Patent number: 4687858Abstract: An ester of a compound having the formula ##STR1## wherein R.sub.1 represents hydrogen atom or a lower alkyl group,R.sub.2 represents a lower alkyl group or a lower alkenyl group,n is an integer of 1 to 4,Z represents a halogen atom, nitro group, a lower alkyl group, a halogenated lower alkyl group, a lower alkoxy group, a lower alkanesulfonyl group, cyano group, a lower alkylthio group, an alkanoyl group having 2 to 5 carbon atoms, or benzoyl group, and when n is 2, 3, or 4, Z's may be the same or different.The esters are suitable for use in herbicidal compositions.Type: GrantFiled: January 15, 1985Date of Patent: August 18, 1987Assignee: Sankyo Company LimitedInventors: Takuo Konotsune, Katsuhiko Kawakubo
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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
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Patent number: 4666921Abstract: Special pyrazole derivatives corresponding to the general formula I which have a highly selective action on histamine-H.sub.2 receptors are described. Compared with other drugs known to be effective in their action on histamine-H.sub.2 receptors, these compounds have improved pharmacological properties. A method of preparation of these compounds is also described.Type: GrantFiled: October 15, 1985Date of Patent: May 19, 1987Assignee: Ludwig Heumann & Co. GmbHInventors: Rolf Herter, Helmut Schickaneder, Peter Morsdorf, Stefan Postius, Istvan Szelenyi, Kurt H. Ahrens
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Patent number: 4661496Abstract: 2,4-Dihydro-5-[(substituted)phenyl]-4,4-disubstituted-3H-pyrazol-3-one compounds as cardiotonic and antihypertensive agents, pharmaceutical compositions and methods of treating diseases with such agents as well as a process for the preparation of said compounds are described.Type: GrantFiled: August 19, 1985Date of Patent: April 28, 1987Assignee: Warner-Lambert CompanyInventor: Glenn C. Morrison
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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
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Patent number: 4599427Abstract: The new azolylmethylamines can be prepared by reaction of amines and azoles with formaldehyde. They can be used in microbicidal agents.Type: GrantFiled: September 28, 1983Date of Patent: July 8, 1986Assignee: Bayer AktiengesellschaftInventors: Siegfried Oeckl, Hans-Georg Schmitt, Wilfried Paulus, Hermann Genth
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Patent number: 4589905Abstract: The present invention is directed to compounds of the formula ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl, ##STR2## each of R.sup.2 and R.sup.3 is taken separately and is independently hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.4 alkynyl, C.sub.3 -C.sub.4 cycloalkyl or C.sub.1 -C.sub.3 alkoxy, orR.sup.2 and R.sup.3 are taken together with the nitrogen atom to which they are attached and form piperidine, morpholine or pyrrolidine;each R.sup.4 independently is halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -Cphd 4 alkoxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy or cyano;X is 0 or S; andm is 0-3;with the provisos that when R.sup.4 is C.sub.1 -C.sub.4 alkyl, that substituent exists at other than the 2 or 6 position of the phenyl ring; and when R.sup.2 is C.sub.1 -C.sub.3 alkoxy, R.sup.3 is other than C.sub.1 -C.sub.3 alkoxy.These compounds exhibit activity as terrestrial herbicides, aquatic herbicides, and aquatic algicides.Type: GrantFiled: September 13, 1984Date of Patent: May 20, 1986Assignee: Eli Lilly and CompanyInventor: James R. Beck
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Patent number: 4587051Abstract: A compound having the formula ##STR1## can be prepared by heating an anion having the formula ##STR2## with a cation having the formula ##STR3## or a cation having the formula ##STR4##Type: GrantFiled: May 21, 1984Date of Patent: May 6, 1986Assignee: E. R. Squibb & Sons, Inc.Inventor: William H. Koster
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Patent number: 4587047Abstract: Antibacterial activity is exhibited by .beta.-lactams having a ##STR1## substituent in the 1-position and an acylamino substituent in the 3-position wherein Z is oxygen or sulfur, and R is alkyl, alkenyl, alkynyl, substituted alkyl, phenyl, substituted phenyl, a 5,6 or 7-membered heterocycle (R.sub.c), phenylalkyl, (substituted phenyl)alkyl, R.sub.c -alkyl or --NR.sub.a R.sub.b wherein R.sub.a and R.sub.b are the same or different and each is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, phenylalkyl, or (substituted phenyl)alkyl or one of R.sub.a and R.sub.b is hydrogen, alkyl, phenyl, substituted phenyl, phenylalkyl or (substituted phenyl)alkyl and the other is amino, alkanoylamino, arylcarbonylamino, alkoxycarbonylamino, alkylsulfonylamino, alkylamino, dialkylamino, phenylamino, (substituted phenyl)amino, hydroxy, cyano, alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, (substituted phenyl)alkoxy, R.sub.c, R.sub.c -alkyl, R.sub.Type: GrantFiled: April 1, 1982Date of Patent: May 6, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Hermann Breuer, William A. Slusarchyk, Theodor Denzel, Uwe D. Treuner
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Patent number: 4576943Abstract: This disclosure describes certain pyrazolo[1,5-a]pyrimidines useful as hypotensive and/or anxiolytic agents, or as agents for the treatment of cognitive and related neural behavioral problems in mammals.Type: GrantFiled: October 9, 1984Date of Patent: March 18, 1986Assignee: American Cyanamid CompanyInventors: Andrew S. Tomcufcik, Walter E. Meyer, John P. Dusza, Shin S. Tseng
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Patent number: 4560508Abstract: 4-Cyano-2-azetidinone derivatives represented by the formula ##STR1## wherein R.sup.1 is an amino group which may be acylated or protected, X is a hydrogen atom or a methoxy group and W is a hydrogen atom or a sulfo group, and methods of producing the same, for example, as represented by ##STR2## wherein R.sup.2 is an acylated or protected amino group, Y is a halogen atom or a group having the formula --OCOR.sup.3, --SCOR.sup.3 or --S(O).sub.n --R.sup.3 (R.sup.3 being a hydrocarbyl group and n an integer 1 or 2), R.sup.4 is an amino group which may be acylated or protected and X is as defined above. Compounds [I] are useful as advantageous intermediates for the synthesis of optically active 4-substituted-2-azetidinone derivatives, and, when W=SO.sub.3 H, [I] are also useful as antimicrobial agents and as beta-lactamase inhibitors.Type: GrantFiled: December 20, 1982Date of Patent: December 24, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Taisuke Matsuo, deceased, Michihiko Ochiai, Shoji Kishimoto
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Patent number: 4550119Abstract: 2,4-Dihydro-5-[(substiuted)phenyl]-4,4-disubstituted-3H-pyrazol-3-one compounds as cardiotonic and antihypertensive agents, pharmaceutical compositions and methods of treating diseases with such agents as well as a process for the preparation of said compounds are described.Type: GrantFiled: March 12, 1984Date of Patent: October 29, 1985Assignee: Warner-Lambert CompanyInventor: Glenn C. Morrison
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Patent number: 4550105Abstract: Disclosed are compounds of the general formula: ##STR1## wherein R.sub.1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R' is hydrogen, R or R.sup.4 wherein R is an organic residue attached to the azetidine ring through a carbon atom therein and R.sub.4 is azido, a halogen, an amino group which may optionally be acylated or a group of the formula --OR.sub.5, ##STR2## or --S--S--R.sub.5 wherein R.sub.5 is an organic residue and n is 0, 1 or 2, and pharmaceutically acceptable salts and esters thereof.The compounds have antimicrobial and/or .beta.-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals.Type: GrantFiled: December 3, 1981Date of Patent: October 29, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Taisuke Matsuo, Shoji Kishimoto, Michihiko Ochiai
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Patent number: 4526982Abstract: 2,4-Dihydro-5-[(substituted)phenyl]-4,4-disubstituted-3H-pyrazol-3-one compounds as cardiotonic and antihypertensive agents, pharmaceutical compositions and methods of treating diseases with such agents as well as a process for the preparation of said compounds are described.Type: GrantFiled: May 23, 1983Date of Patent: July 2, 1985Inventor: Glenn C. Morrison
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Patent number: 4515959Abstract: Herbicidal and fungicidal compounds of the formula ##STR1## wherein R.sup.1 is (a) a phenyl group optionally substituted by one or more halogen atoms, cyano groups, alkoxy groups, methylene- or ethylene-dioxy groups, alkyl groups, or haloalkyl groups (e.g. trifluoromethyl groups); or (b) a heteroaromatic group optionally substituted by one or more alkyl groups, haloalkyl groups or halogen atoms X is a 5-membered heteroaromatic radical linked by a ring nitrogen atom to the carbon atom bearing Y, and optionally substituted by one or more alkyl groups, and Y is a CN group; a --CSNH.sub.2 group; a --CO.sub.2 R.sup.4 group wherein R.sup.4 is an esterifying radical, for example an alkyl radical; or an amide group --CONR.sup.5 R.sup.6 wherein each of R.sup.5 and R.sup.6 may be a hydrogen atom or an alkyl radical (e.g. an alkyl radical of 1 to 6 carbon atoms).Type: GrantFiled: August 17, 1982Date of Patent: May 7, 1985Assignee: Imperial Chemical Industries PLCInventors: Ian T. Kay, Robert A. Noon
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Patent number: 4482716Abstract: The new compounds of the general formula ##STR1## where R.sub.1 is hydrogen, alkyl or cyclic alkyl, R.sub.2 and R.sub.3 are each hydrogen, alkyl, a carboxylic acid, ester or amide group or cyano, and R.sub.4, R.sub.5 and R.sub.6 are each alkyl or aryl, are useful as antihalation dyes and as image dyes in photographic materials for dye-bleaching processes.Type: GrantFiled: April 22, 1983Date of Patent: November 13, 1984Assignee: Ciba-Geigy AGInventor: William E. Long
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Patent number: 4470932Abstract: Carboxylic acid anhydrides of the general formulaR--CO--O--CO--R' (I)in whichR and R' are identical or different and represent an optionally substituted alkyl group having 1 to 18 carbon atoms, an optionally substituted cycloalkyl group having 3 to 12 carbon atoms or an optionally substituted aryl group, or represent an optionally substituted 5-membered or 6-membered heterocyclic radical which additionally can be fused to a benzene ring,are obtained in high yields by a process in which a trimethylsilyl carboxylate of the general formulaR--CO--OSi(CH.sub.3).sub.3 (II)in whichR has the meaning given above, is reacted with a carboxylic acid-halide of the general formulaR'CO--X (III)in whichR' has the meaning given above, andX represents a halogen atom, if appropriate in the presence of a catalyst and, if appropriate, in the presence of a diluent, at a temperature between 20.degree. and 250.degree. C.The carboxylic acid anhydrides are valuable intermediate products for organic syntheses.Type: GrantFiled: October 22, 1982Date of Patent: September 11, 1984Assignee: Bayer AktiengesellschaftInventor: Kurt Findeisen
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Patent number: RE33125Type: GrantFiled: July 11, 1986Date of Patent: December 5, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Henry F. Campbell, Thomas H. Scholtz, George H. Douglas