Benzene Ring Bonded Directly To Ring Nitrogen Of The Five -membered Hetero Ring Patents (Class 548/563)
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Patent number: 7176323Abstract: A process for the production of a ?-ketoacetal compound wherein the desired product is obtained by a simple procedure in a high yield as a high purity product. The reaction scheme for the process is as follows: wherein Ar is an aryl group; X is a halogen atom; Ra and Rb is an alkyl or alkoxy group; and W is an alkylene group.Type: GrantFiled: February 9, 2005Date of Patent: February 13, 2007Assignee: Sankyo Company, LimitedInventors: Rei Okazaki, Shunshi Kojima
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Patent number: 6967107Abstract: The present invention describes carbamic acid ester-derived and valeric acid ester-derived polyfunctional cross-linker molecules, and methods for their synthesis and use. The inclusion of polymeric moieties such as poly(alkylene oxide) in the cross-linkers of the present invention can provide advantageous solubility properties in aqueous environments. Such cross-linkers may be used to form conjugates for use in a variety of assay formats.Type: GrantFiled: March 14, 2005Date of Patent: November 22, 2005Assignee: Biosite, Inc.Inventors: Kenneth F. Buechler, Mariusz G. Banaszczyk, Joseph Barry Noar
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Patent number: 6911468Abstract: A compound of the formula (I): wherein X1 and X2 are the same or different and each is a bond or a spacer having 1 to 20 atom(s) in the main chain; one of R1 and R2 is a cycle group having substituent(s) selected from 1) an optionally substituted carboxy-C1-6 alkoxy group and 2) an optionally substituted carboxy-C1-6 aliphatic hydrocarbon group, wherein the cycle group optionally has additional substituent(s), and the other is an optionally substituted cycle group or a hydrogen atom; and R3, R4 and R5 are the same or different and each is a hydrogen atom or a substituent, or R4 may link together with R3 or R5 to form an optionally substituted ring; provided that when R3 is a hydrogen atom, R4 is a hydrogen atom and R5 is methyl, X2—R2 is not 4-cyclohexylphenyl; when R3 is 4-methoxyphenyl, R4 is a hydrogen atom and R5 is methyl, X2—R2 is not 4-methoxyphenyl; and when R1 or R2 is a hydrogen atom, the adjacent X1 or X2 is not a C1-7 alkylene; or a salt thereof exhibits a protein tyrosine phosphatase inhibiType: GrantFiled: May 21, 2001Date of Patent: June 28, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Takahiro Matsumoto, Nozomi Katayama, Hiroshi Mabuchi
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Patent number: 6887952Abstract: The present invention describes carbamic acid ester-derived and valeric acid ester-derived polyfunctional cross-linker molecules, and methods for their synthesis and use. The inclusion of polymeric moieties such as poly(alkylene oxide) in the cross-linkers of the present invention can provide advantageous solubility properties in aqueous environments. Such cross-linkers may be used to form conjugates for use in a variety of assay formats.Type: GrantFiled: February 12, 2004Date of Patent: May 3, 2005Assignee: Biosite, Inc.Inventors: Kenneth F. Buechler, Mariusz G. Banaszczyk, Joseph Barry Noar
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Patent number: 6887893Abstract: Certain cyclooxygenase-2 inhibitors are useful for the treatment and prevention of tumors and tumor-related disorders and cachexia.Type: GrantFiled: December 16, 1998Date of Patent: May 3, 2005Assignee: Sankyo Company, LimitedInventors: Shinichi Kurakata, Masaharu Hanai, Saori Kanai, Tomio Kimura
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Patent number: 6811573Abstract: Colorants for keratin fibers containing 1,3-diamino-4-heteroarylbenzene derivatives of general formula (I) or the physiologically tolerated salts thereof as well as novel 1,3-diamino-4-heteroarylbenzene derivatives.Type: GrantFiled: June 26, 2002Date of Patent: November 2, 2004Assignee: Wella AktiengesellschaftInventors: Laurent Chassot, Hans-Juergen Braun
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Patent number: 6541639Abstract: The present invention provides of method of preparing phenyl-substituted azoles. This method uses an efficient ligand-accelerated Ullmann coupling reaction of anilines with azoles. The coupling products are useful for preparing factor Xa inhibitors.Type: GrantFiled: July 25, 2001Date of Patent: April 1, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jiacheng Zhou, Pasquale N. Confalone, Hui-Yin Li, Philip Ma, Lynette M. Oh, Lucius T. Rossano, Charles G. Clark, Chris Teleha
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Patent number: 6515143Abstract: The invention relates to a process for the preparation of ortho-alkylated benzoic acid derivatives of the formula I characterized in that an aryl bromide of the formula II is reacted with a secondary or tertiary organolithium compound and CO2.Type: GrantFiled: January 8, 2002Date of Patent: February 4, 2003Assignee: Merck KGaAInventors: Ekkehard Bartmann, Ingeborg Stein
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Patent number: 6489480Abstract: This description addresses fluorinated amine compounds meeting the general formula R′iArF—ER2, where ArF is a fluoroaryl group, E is nitrogen or phosphorous, each R is independently a C1-C20 hydrocarbyl group; or the two Rs may connect to form an unsubstituted or substituted C2-C20 cycloaliphatic group, R′ is a C1-C20 hydrocarbyl or halogenated hydrocarbyl, and i is 0, 1 or 2. These compounds may be protonated with strong Bronsted acids to form protonated amine compounds that are useful for the preparation of organometallic catalyst-cocatalyst compounds comprising noncoordinating or weakly coordinating anions. The resulting organometallic catalyst-cocatalyst complexes can be effectively used as olefin polymerization catalysts.Type: GrantFiled: December 11, 2000Date of Patent: December 3, 2002Assignee: ExxonMobil Chemical Patents Inc.Inventor: George Rodriguez
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Patent number: 6451824Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: September 17, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
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Patent number: 6451736Abstract: There is disclosed substituted thiocarboxamides compounds of the formula (I): wherein R1, R2, R3 and Z are as defined in the specification. The compounds are useful as herbicides.Type: GrantFiled: September 25, 2001Date of Patent: September 17, 2002Assignee: Bayer AktiengesellschaftInventors: Karl-Heinz Linker, Kurt Findeisen, Roland Andree, Mark-Wilhelm Drewes, Andreas Lender, Otto Schallner, Wilhelm Haas, Hans-Joachim Santel, Markus Dollinger
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Patent number: 6433002Abstract: A compound of formula (I): compositions containing them and methods of use to control pests.Type: GrantFiled: April 12, 2001Date of Patent: August 13, 2002Assignee: Rhone-Poulenc Inc.Inventors: Jamin Huang, Scot Kevin Huber
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Patent number: 6417372Abstract: The present invention relates to arylpyrrole particles which are prepared by a process in which the particles are aged and milled, and pesticidal suspension concentrate compositions comprising them. The size of the particles of this invention remains surprisingly stable during storage.Type: GrantFiled: April 2, 2001Date of Patent: July 9, 2002Assignee: BASF AktiengesellschaftInventors: Mimi Yih-Pei Chou Schaaf, Steven Brunt, Jian James Xu, Andrew Evelyn Goldsmith, Anthony Francis Walker, Patrick C. Mowery, Edward S. Donoghue, Srinivasan Rajan
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Patent number: 6414005Abstract: Compounds represented by the general formula (1): [wherein R1 is typically an aminoalkyl group; R2 is typically a hydrogen atom, a lower alkyl group, R3 or SR4 (where R4 is typically a lower alkyl group); Ar is typically a 5-membered aromatic heterocyclic group] have an NOS inhibiting activity and are useful as therapeutics of cerebrovascular diseases and other pharmaceuticals.Type: GrantFiled: May 4, 2000Date of Patent: July 2, 2002Assignee: Chugai Seiyaku Kabushiki KaishaInventor: Toshihiko Makino
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Patent number: 6316486Abstract: The present invention relates to new compounds of the formula (I) in which X represents halogen, Y represents halogen or alkyl and Z represents halogen or alkyl, with the proviso that always one of the radicals Y and Z represents halogen while the other represents alkyl, and Het represents one of the groups in which A, B, D and G have the meanings given in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: October 31, 1997Date of Patent: November 13, 2001Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Peter Dahmen, Markus Dollinger, Hans-Joachim Santel, Alan Graff, Wolfram Andersch, Norbert Mencke, Andreas Turberg
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Patent number: 6248765Abstract: Novel imidazole derivatives as histamine receptor H3 antagonists and/or agonists, preparation thereof and therapeutical uses thereof. Chemical compounds for use as histamine receptor H3 agonists, partial agonists or antagonists, having general formula (Ia) or (Ib), the use thereof for making drugs, and methods for revealing the agonist, partial agonist or antagonist activity of such compounds in vivo, are disclosed.Type: GrantFiled: January 9, 1997Date of Patent: June 19, 2001Assignees: Institut National de la Sante et de la Recherche Medical, Societe Civile BioprojetInventors: Jean-Charles Schwartz, Jean-Michel Arrang, Monique Garbarg, Agnes Quemener, Jeanne-Marie Lecomte, Xavier Ligneau, Walter G. Schunack, Holger Stark, Katja Purand, Annette Huls, Reidemeister Sybille, Athmani Salah, Charon Robbin Ganellin, Nadia Pelloux-Leon, Wasyl Tertiux, Michael C. O. Krause, Sadek Bassem
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Patent number: 6242613Abstract: The present invention relates to arylpyrrole particles which are prepared by a process in which the particles are aged and milled, and pesticidal suspension concentrate compositions comprising them. The size of the particles of this invention remains surprisingly stable during storage.Type: GrantFiled: April 6, 1999Date of Patent: June 5, 2001Assignee: American Cyanamid Co.Inventors: Mimi Yih-Pei Chou Schaaf, Steven Brunt, Jian James Xu, Andrew Evelyn Goldsmith, Anthony Francis Walker, Patrick C. Mowery, Edward S. Donoghue, Srinivasan Rajan
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Patent number: 6110958Abstract: Compounds of formula (I) ##STR1## wherein the substituents are as defined herein, are antiparasitic agents.Type: GrantFiled: December 1, 1999Date of Patent: August 29, 2000Assignee: Pfizer Inc.Inventors: Bernard Joseph Banks, Nathan Anthony Logan Chubb
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Patent number: 6022379Abstract: Pyrrole derivatives of 1,4-naphthoquinone and of 1,4-dihydroxynaphthalene, dye compositions containing them and the corresponding dyeing process.Type: GrantFiled: February 27, 1998Date of Patent: February 8, 2000Assignee: L'OrealInventors: Sylvie Genard, Herve Andrean, Michel Hocquaux
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Patent number: 6013836Abstract: This invention relates to N'-substituted-N,N'-disubstitutedhydrazines of formula I ##STR1## wherein X and X' are independently O, S, or NR; A' and B' are independently substituted or unsubstituted aryl or aromatic heterocycle; wherein F is alkyl, alkenyl, or aralkyl; and wherein E is a tertiary carbon containing organic radical having a total of at least four carbon and halogen atoms but not more than six halogen atoms, or a non-tertiary carbon containing non-haloalkyl organic or organometallic radical having at least five atoms other than hydrogen, oxygen and halogen which are useful as insecticides, compositions containing those compounds, methods of producing the compounds, and methods of their use. More particularly, the invention relates to insect growth regulating compounds and compositions, and methods of using such compounds and compositions. Compounds of the present invention are particularly suitable for controlling plant-destructive insects in crops of cultivated plants, ornamentals and forestry.Type: GrantFiled: May 22, 1995Date of Patent: January 11, 2000Assignee: Rohm and Haas CompanyInventors: Adam Chi-Tung Hsu, Harold Ernest Aller, Dat Phat Le, Donald Wesley Hamp, Barry Weinstein, Raymond August Murphy
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Patent number: 6004903Abstract: Benzoyl derivatives of the formula I ##STR1## where Z is a 5-membered or 6-membered heterocyclic, saturated or unsaturated radical containing one to three hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen,Q is a cyclohexane-1, 3-dione ring bonded in the 2-position and of the formula II, ##STR2## or conventional agricultural salts of the compounds I.Type: GrantFiled: August 14, 1997Date of Patent: December 21, 1999Assignee: Basf AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Franz Rohl, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
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Patent number: 5935990Abstract: A class of pyrrolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as described in the specification.Type: GrantFiled: December 9, 1997Date of Patent: August 10, 1999Assignee: G.D. Searle & Co.Inventors: Ish K. Khanna, Richard M. Weier, Yi Yu
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Patent number: 5908858Abstract: Compounds of formula (I) and (II): ##STR1## ?wherein R is hydrogen, halogen or alkyl; R.sup.1 is alkyl, amino or substituted amino; R.sup.2 is optionally substituted phenyl; R.sup.3 is hydrogen, halogen or optionally substituted alkyl; R.sup.4 is hydrogen, optionally substituted alkyl, cycloalkyl, aryl, or aralkyl! have valuable analgesic, anti-inflammatory, anti-pyretic and anti-allergic activities and have the ability to inhibit the production of leukotrienes and to inhibit bone resorption. They are relatively free from the side effects which generally result from the administration of compounds having these kinds of activities.Type: GrantFiled: March 26, 1997Date of Patent: June 1, 1999Assignee: Sankyo Company, LimitedInventors: Tomio Kimura, Yasuo Noguchi, Akira Nakao, Keisuke Suzuki, Shigeru Ushiyama, Akihiro Kawara, Masaaki Miyamoto
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Patent number: 5849775Abstract: Benzoylguaridines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4), R(5) are as defined in the specification, and pharmaceutically tolerated salts thereof.Type: GrantFiled: June 30, 1997Date of Patent: December 15, 1998Assignee: Hoechst AktiengesellschaftInventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5824691Abstract: Guanidine derivatives of the formula: ##STR1## wherein Y is C--R.sup.1(in which R.sup.1 is hydrogen, lower alkyl, hydroxy, protected hydroxy, etc.,)R.sup.2 is pyrrolyl, tetrazolyl, pyrazolyl, etc.,R.sup.3 is hydrogen, lower alkoxy, hydroxy, protected hydroxy, etc.,Z is C--R.sup.4(in which R.sup.4 is hydrogen, carboxy, protected carboxy, nitro, halogen, hydroxy(lower)alkyl, etc.,), andW is R.sup.12(in which R.sup.12 is hydrogen, lower alkoxy, nitro, hydroxy or protected hydroxy)and pharmaceutically acceptable salts thereof which are useful as a medicament which are useful in inhibiting Na.sup.+ /H.sup.+ exchange in cells and in the prevention of cardiovascular diseases, cerebrovascular diseases, renal diseases, arteriosclerosis and shock.Type: GrantFiled: November 9, 1995Date of Patent: October 20, 1998Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Atsushi Kuno, Yoshikazu Inoue, Hisashi Takasugi, Hiroaki Mizuno, Kumi Yamasaki
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Patent number: 5763610Abstract: A composition comprising a nitrogen-containing olefinic compound and a process for using the nitrogen-containing olefinic compound to produce a water-soluble polymer which has applications in a subterranean formation are provided. The nitrogen-containing olefinic compound can be made from an amine and an alkylating agent. The polymer produced can be used in drilling fluids, workover fluids, completion fluids, permeability corrections, water or gas coning prevention, fluid loss prevention, matrix acidizing, fracture acidizing, and combinations of any two or more thereof.Type: GrantFiled: February 21, 1997Date of Patent: June 9, 1998Assignee: Phillips Petroleum CompanyInventors: Iqbal Ahmed, Ahmad Moradi-Araghi, Odd Ivar Eriksen
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Patent number: 5726324Abstract: Process for preparing complex pesticidal 1-(haloaryl)heterocyclic compounds by reacting 1-(nitroaryl)heterocycles with metallic halide salts. 1-(Nitroaryl)pyrrole intermediates useful in said process.Type: GrantFiled: February 13, 1997Date of Patent: March 10, 1998Assignee: Rhone-Poulenc Inc.Inventors: Jamin Huang, Scot Kevin Huber, Alain Chene
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Patent number: 5665739Abstract: Benzoylguanidines of the formula I are described ##STR1## in which R(1)=hydrogen, Hal, --NO.sub.2, --C.tbd.N, --CF.sub.3, R(4)--SO.sub.m or R(5)R(6)N--SO.sub.2 --, R(4) and R(5) are alk(en)yl or CF.sub.3, R(5) also having the meaning of H,R(2)=is heteroaryl or --SR(10), --OR(10), --NR(10)R(11), --CR(10)R(11)R(12); where R(10) is --C.sub.a H.sub.2a -heteroaryl, and R(11) and R(12) are as defined for R(10) and also hydrogen or alkyl,R(3) is as defined for R(1) or is alkyl, --X--R(13) where X is oxygen, S, NR(14), where R(13) is H or (cyclo)alkyl.They are obtained from a compound of the formula II ##STR2## by reacting it with guanidine.Type: GrantFiled: May 15, 1995Date of Patent: September 9, 1997Assignee: Hoechst AktiengesellschaftInventors: Hans-Jochen Lang, Heinz-Werner Kleeman, Wolfgang Scholz, Udo Albus
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Patent number: 5573999Abstract: .beta.-Substituted cinnamic acid derivatives of the formula 1, ##STR1## where R.sup.1 is alkyl, chlorine or bromine, --X-- is --O--, --S--, ##STR2## m is 0 or 1, --Y is --OR.sup.4, --O--N.dbd.CR.sup.5 R.sup.6, --NR.sup.7 R.sup.8, --N(OR.sup.9)R.sup.10 or --SR.sup.11, where the above-mentioned substituents R.sup.2 to R.sup.11 are alkyl, and R.sup.2, and R.sup.3 and R.sup.5 to R.sup.11 can also be hydrogen,Z is halogen, nitro, cyano, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, arylthioalkyl, hetarylalkyl, hetaryloxyalkyl, hetarylthioalkyl, alkenyl, aralkenyl, aryloxyalkenyl, arylthioalkenyl, hetarylalkenyl, hetaryloxyalkenyl, hetarylthioalkenyl, alkynyl, arylalkynyl, hetarylalkynyl, aryl, hetaryl, arylazo, acylamino, --OR.sup.12, --SR.sup.13, --SOR.sup.14, --SO.sub.2 R.sup.15, --COOR.sup.16, --CONR.sup.17 R.sup.18, --COR.sup.19, --CR.sup.20 .dbd.NR.sup.21, --N.dbd.CR.sup.22, R.sup.23, --CR.sup.24 .dbd.N--OR.sup.25, --CR.sup.25 R.sup.26 --O--, N.dbd.CR.sup.27 R.sup.28, --CH.sub.2 --OCOR.sup.39 or --NR.sup.37 R.Type: GrantFiled: May 15, 1995Date of Patent: November 12, 1996Assignee: BASF AktiengesellschaftInventors: Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Horst Wingert, Wolfgang von Deyn, Wassilios Grammenos, Hartmann Koenig, Harald Rang, Franz Roehl, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5482942Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.Type: GrantFiled: June 28, 1994Date of Patent: January 9, 1996Assignee: American Home Products CorporationInventors: Richard M. Soll, Paul J. Dollings
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Patent number: 5371239Abstract: This invention relates to methods and compositions for treating, controlling, preventing and protecting warm-blooded animals from infestation and infection by helminths, acarids and arthropod endo- and ectoparasites by administering or applying to the animals a nitropyrrole or pyrrole carbonitrile compound.Type: GrantFiled: February 26, 1992Date of Patent: December 6, 1994Assignee: American Cyanamid CompanyInventor: Mary E. Doscher
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Patent number: 5292755Abstract: Benzoylguanidines of the formula I ##STR1## where R(1) or R(2) is equal to R(6)--S(O).sub.n -- or R(7)R(8)N--O.sub.2 S--and the other substituent R(1) or R(2) is in each case equal to H, F, Cl, Br, I, alkyl, alkoxy or phenoxy, R(6)--S(O).sub.n or R(7)R(8)N--and R(6) is equal to alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl,R(7) and R(8) are equal to alkyl or phenylalkyl or phenyl,and in which R(7) and R(8) may also together be a C.sub.4 --C.sub.7 chain, and in which R(7) and R(8), together with the nitrogen atom to which they are bonded, may be a dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system,and where R(3), R(4) and R(5) are equal to hydrogen or alkyl, or R(3) and R(4) are together an alkylene chain or R(4) and R(4) are together an alkylene chain,and where n is equal to zero, 1 or 2and their pharmaceutically tolerable salts are outstanding antiarrhythmics.Type: GrantFiled: January 31, 1992Date of Patent: March 8, 1994Assignee: Hoechst AktiengesellschaftInventors: Heinrich C. Englert, Hans-Jochen Lang, Wolfgang Linz, Bernward Scholkens, Wolfgang Scholz
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Patent number: 5210218Abstract: Novel 2- or 3-chloropyrroles represented by the general formula: ##STR1## wherein R.sup.1 represents hydrogen atom, chlorine atom, alkyl group, or aryl group which may optionally be substituted, with the proviso that any one of the two groups represented by R.sup.1 is chlorine atom,R.sup.2 represents alkyl group or aryl group which may optionally be substituted, andR.sup.3 represents tertiary alkyl group which may be substituted by phenyl, or phenyl which may optionally be substituted, andprocesses for preparing the same.Type: GrantFiled: October 15, 1991Date of Patent: May 11, 1993Assignee: Nihon Bayer Agrochem K.K.Inventors: Shinzo Kagabu, Itsumi Kawai, Katsuaki Wada
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Patent number: 5128485Abstract: There is provided a synthesis of 2-aryl-5-(trifluoromethyl)pyrrole compounds via the condensation of a suitable enamine with an .alpha.-haloketone.Type: GrantFiled: December 17, 1990Date of Patent: July 7, 1992Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 5017213Abstract: Herbicidal 1-phenylpyrroles of the formula ##STR1## wherein each R.sup.1 represents methyl or together form a tetramethylene group,R.sup.2 represents hydrogen, C.sub.1-6 alkyl, cyclopropylmethyl, C.sub.1-4 alkoxy-C.sub.1-2 alkyl, C.sub.1-4 alkylthio-C.sub.1-2 alkyl, C.sub.1-4 alkylsulfinyl-C.sub.1-2 alkyl, C.sub.1-4 alkylsulfonyl-C.sub.1-2 alkyl, benzyl or phenylethyl which are optionally substituted by halogen, C.sub.3-4 alkenyl, C.sub.3-4 alkynyl, C.sub.3-4 haloalkenyl, C.sub.2-3 cyanoalkyl or carbmoylmethyl, thiocarbamoylmethyl, trimethylsilylmethyl, CH.sub.2 COOR.sup.3, ##STR2## or a C.sub.1-2 alkyl group which is connected with an optionally substituted 5-6 membered heterocyclic group, whereinR.sup.3 represents C.sub.1-6 alkyl or C.sub.5-6 cycloalkyl,R.sup.4 represents hydrogen, methyl, ethyl or cyclopropyl,R.sup.5 represents OR.sup.6 or N(CH.sub.3).sub.2, in whichR.sup.6 represents hydrogen, C.sub.1-5 alkyl, allyl, propargyl or benzyl, andn represents 0 to 1.Type: GrantFiled: July 7, 1989Date of Patent: May 21, 1991Assignee: Nihon Tokushu Noyaku Seizo K. K.Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Hiroshi Miyauchi, Tadao Asami
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Patent number: 4950678Abstract: Novel substituted N-(heterocyclic-substituted phenyl)-N'-benzoyl-ureas, processed for producing these compounds, intermediates therefor, compositions thereof and the use of the compounds for the control of pests.Type: GrantFiled: July 27, 1989Date of Patent: August 21, 1990Assignee: Sandoz Ltd.Inventors: Robert L. Carney, John M. Gruber, Alfred S. T. Lui
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Patent number: 4906758Abstract: Pyrroles of the formula I ##STR1## are prepared by a process in which a dialkoxytetrahydrofuran of the formula II ##STR2## where R.sup.2 to R.sup.5 in the formulae (I) and (II) are identical or different and are each hydrogen, a straight-chain or branched alkyl or alkenyl radical of not more than 12 carbon atoms, a cycloalkyl or cycloalkenyl radical of 5 to 8 carbon atoms, an aryl, alkylaryl or aralkyl radical of 6 to 16 carbon atoms, and two non-adjacent radicals R.sup.6 to R.sup.9 are alkoxy and the other two radicals R.sup.6 to R.sup.9 are hydrogen, is reacted with ammonia or a primary amine H.sub.2 NR.sup.1, where R.sup.1 in formula (I) is hydrogen, alkyl, aryl, alkylaryl, aralkyl or cycloalkyl, in the presence of an acidic, solid, heterogeneous catalyst. Zeolites, for example those of the pentasil type or faujasite type, or phosphates, acidic oxides, phosphoric acid or boric acid on a carrier can be used as the solid heterogeneous catalysts.Type: GrantFiled: August 12, 1988Date of Patent: March 6, 1990Assignee: BASF AktiengesellschaftInventors: Wolfgang Hoelderich, Michael Hesse, Hardo Siegel
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Patent number: 4904679Abstract: Pyrrolophenylalkanolamines of the formula ##STR1## R.sup.1 and R.sup.2 represent hydrogen or various radicals, R.sup.3 represents hydrogen, acyl or trialkylsilyl,R.sup.4 represents hydrogen or alkyl,R.sup.5 represents hydrogen, or, together with R.sup.3, represents ##STR2## wherein R.sup.7 represents hydrogen or alkyl, andR.sup.6 represents branched or cyfclic alkyl, which is optionally substituted,and salts thereof promote the yield of animals. Many new intermediates are also shown.Type: GrantFiled: April 22, 1988Date of Patent: February 27, 1990Assignee: Bayer AktiengesellschaftInventors: Hartmund Wollweber, Jurgen Stoltefuss, Friedrich Berschauer, Ann de Jong, Martin Scheer
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Patent number: 4900839Abstract: A series of novel heterocyclic-substituted 2-(1H)-quinolone compounds have been prepared, including the 3,4-dihydro derivatives thereof, wherein the heterocyclic ring moiety is a pyrrolyl, imidazolyl, pyrazolyl, triazolyl or tetrazolyl group attached by a nitrogen atom of said group to the 5-, 6-, 7- or 8-positions of the quinolone ring. These particular compounds are useful in therapy as highly potent inotropic agents and therefore, are of value in the treatment of various cardiac conditions. Preferred member compounds include 6-(2,4-dimethylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, 6-(2,4-dimethyl-5-nitroimidazol-1-yl)-8-methyl-2-(1H)-quinolone, 8-methyl-6-(tetrazol-1-yl)-2-(1H)-quinolone, 8-methyl-6-(1,2,4-triazol-4-yl)-2-(1H)-quinolone, and 6-(4-cyano-2-methylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, respectively. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: January 27, 1989Date of Patent: February 13, 1990Assignee: Pfizer Inc.Inventors: Simon F. Campbell, David A. Roberts
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Patent number: 4897223Abstract: Color-forming agents of the general formula ##STR1## wherein X denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy, acyloxy, alkoxycarbonyloxy, alkylamino, dialkylamino, acylamino, aralkylamino or arylamino,Q denotes cyano, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, carbamoyl, N-alkylcarbamoyl, N,N-dialkylcarbamoyl, N-alkyl-N-aryl-carbamoyl, acyl, alkoxysulphonyl, aralkoxysulphonyl, sulphamoyl, N-alkylsulphamoyl, N,N-dialkylsulphamoyl, alkylsulphonyl, arylsulphonyl or aralkylsulphonyl andR denotes alkyl, alkenyl or aralkyl,further isocyclic or heterocyclic rings can be fused on to the rings A, B, C and D, and the cyclic and acyclic radicals and the rings A, B, C and D can carry further substituents, are used for the preparation of pressure-sensitive recording materials.Type: GrantFiled: March 1, 1988Date of Patent: January 30, 1990Assignee: Bayer AktiengesellschaftInventors: Udo Eckstein, Hubertus Psaar, Roderich Raue
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Patent number: 4816604Abstract: The compounds of formula I, ##STR1## where the substituents have various significances, and physiologically acceptable hydrolyzable derivatives thereof having the hydroxy group in the 2 position of the 3-aminopropoxy side chain in esterifield form, are useful as cardioselective .beta.-adrenoceptor blocking agents.Type: GrantFiled: March 9, 1987Date of Patent: March 28, 1989Assignee: William J. LouisInventors: William J. Louis, Richard Berthold, Andre Stoll
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Patent number: 4792568Abstract: This invention relates to new lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic properties. The present new compounds are of the formula: ##STR1## and salts thereof; wherein, R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aralkyl, phenyl, naphthyl, or a nitrogen oxygen or sulfur heterocyclic; andY.sub.1 and Y are independently hydrogen, lower alkyl, hydroxy, lower alkoxy, aryloxy, lower aralkoxy, aryl, lower aralkyl, carboxy, lower carbalkoxy, lower carbaralkoxy, carbaryloxy, formyl, or alkyl, alkenyl or alkynyl containing up to 6 carbon atoms in the principal chain and up to a total of 10 carbon atoms;provided that when Y and Y.sub.1 are both hydrogen or when Y.sub.1 is hydrogen and Y is CHO, the R is other than hydrogen, unsubstituted phenyl, or lower alkyl.Type: GrantFiled: April 14, 1986Date of Patent: December 20, 1988Assignee: Rorer Pharmaceutical CorporationInventor: Joseph Auerbach
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Patent number: 4666936Abstract: Amide derivatives of 2-(p-aminobenzyl)-butyric acid and esters thereof having a hypolipidemizing and hypocholesterolemizing pharmaceutical activity and their preparation are described.Included are compounds of the formula ##STR1## wherein R and R' together represent the group ##STR2## or the group ##STR3## and R" is hydrogen or a 1 to 6 carbon alkyl group.Type: GrantFiled: August 7, 1985Date of Patent: May 19, 1987Assignee: Medosan Industrie Biochimiche Riunite S.p.A.Inventor: Alessandro Baglioni
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Patent number: 4644009Abstract: Provided are new compounds having valuable therapeutic activity. These compounds are of the formula: ##STR1## and salts thereof, whereinX=O, S or NR.sub.2 ;Z=(CHR.sub.3).sub.n C(R.sub.3))OH)--, ##STR2## --CH.sub.3 .dbd.CH.sub.3 CR.sub.3 (OH)--, or --(CHR.sub.3).sub.n', M=--O--, --S--, or ##STR3## Z.sub.1 is an alkylene chain of 0-5 carbon atoms in the principal chain and a total of 7 carbon atoms;R.sub.1 is H, phenyl, naphthyl or a sulfur, nitrogen or oxygen-heterocyclic ring;R.sub.2 is H, alkyl, aryl or aralkyl;R.sub.3 is H or CH.sub.3 ;n=0-5; andn'=1-5.Type: GrantFiled: October 29, 1984Date of Patent: February 17, 1987Assignee: USV Pharmaceutical CorporationInventors: Fu-chih Huang, Joseph Auerbach
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Patent number: 4626592Abstract: Amines and amides are N,N-cyclodialkylated by reaction with an unstrained cyclic ether in the presence of a B-subgroup metal oxide alkylation catalyst, preferably a Group IV-B metal oxide such as titanium dioxide.Type: GrantFiled: December 24, 1984Date of Patent: December 2, 1986Assignee: Ethyl CorporationInventor: Duane C. Hargis
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Patent number: 4624958Abstract: Diamidines of the formula ##STR1## wherein X is a propylene, isobutylene, guanidine, pyrrole, tetrazole, imidazole or substituted imidazole group; and 2-[4-(2-imidazolinyl)phenyl]-6-(2-imidazolinyl)indole, are useful in the treatment of certain protozoal infections in mammals, particularly in cattle.Type: GrantFiled: August 28, 1985Date of Patent: November 25, 1986Assignee: Pfizer Inc.Inventor: Edward A. Glazer
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Patent number: 4617316Abstract: Insecticidal compounds of the formula: ##STR1## in which A is chloro and B is hydrogen or A and B are both fluoro, X is oxygen or sulfur and one of R.sup.1 and R.sup.2 is or includes an optionally substituted 5-membered heteroaryl ring, their method for preparation and formulation, insecticidal compositions thereof, and their use to control insects, are disclosed and exemplified.Type: GrantFiled: December 20, 1985Date of Patent: October 14, 1986Assignee: FMC CorporationInventor: Ernest L. Plummer
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Patent number: 4560769Abstract: Pyrroles are prepared by a process in which ammonia or an amine is reacted with a but-2-ene-1,4-diol in the presence of a supported catalyst containing copper, silver, zinc, palladium, nickel, cobalt and/or platinum and/or compounds of these metals as catalytic materials, and in the presence or absence of compounds of chromium and/or manganese as additional catalysts, in the gas phase.The pyrroles obtainable by the process of the invention are useful starting materials for the preparation of dyes, corrosion inhibitors, drugs and pesticides.Type: GrantFiled: March 9, 1984Date of Patent: December 24, 1985Assignee: BASF AktiengesellschaftInventors: Helmuth Menig, Martin Fischer, Karl Baer
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Patent number: RE39420Abstract: Compounds of formula (I) and (II): [wherein R is hydrogen, halogen or alkyl; R1 is alkyl, amino or substituted amino; R2 is optionally substituted phenyl; R3 is hydrogen, halogen or optionally substituted alkyl; R4 is hydrogen, optionally substituted alkyl, cycloalkyl, aryl, or aralkyl] have valuable analgesic, anti-inflammatory, anti-pyretic and anti-allergic activities and have the ability to inhibit the production of leukotrienes and to inhibit bone resorption. They are relatively free from the side effects which generally result from the administration of compounds having these kinds of activities.Type: GrantFiled: September 29, 2000Date of Patent: December 5, 2006Assignee: Sankyo Company, LimitedInventors: Tomio Kimura, Yasuo Noguchi, Akira Nakao, Keisuke Suzuki, Shigeru Ushiyama, Akihiro Kawara, Masaaki Miyamoto
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Patent number: RE32896Abstract: Amines and amides are N,N-cyclodialkylated by reaction with an unstrained cyclic ether in the presence of a B-subgroup metal oxide alkylation catalyst, preferably a Group IV-B metal oxide such as titanium dioxide.Type: GrantFiled: March 23, 1987Date of Patent: March 28, 1989Assignee: Ethyl CorporationInventor: Duane C. Hargis