Additional Hetero Ring Containing Patents (Class 540/524)
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Patent number: 5482920Abstract: Pyrimidinyloxy- and triazinyloxy- and pyrimidinylthio- and triazinylthio-butyric acid derivatives of formula I ##STR1## wherein Q is ##STR2## A is hydroxy or a group ##STR3## and the other substituents are as described in patent claim 1, and salts of compounds of formula I, have herbicidal action and are suitable as active ingredients in weed control compositions.Type: GrantFiled: February 15, 1994Date of Patent: January 9, 1996Assignee: Ciba-Geigy CorporationInventor: Christoph Luthy
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Patent number: 5470849Abstract: This invention relates to a method of inhibiting platelet aggregation, and compounds which are mimics of the peptide sequence Arg-Gly-Asp.Type: GrantFiled: April 30, 1993Date of Patent: November 28, 1995Assignee: SmithKline Beecham Corp.Inventors: James F. Callahan, William F. Huffman
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Patent number: 5434148Abstract: Disclosed are .beta.-carboline derivatives represented by the formula: ##STR1## wherein R.sup.1 represents hydrogen atom, a lower alkyl group, a lower alkoxy group or hydroxy group; R.sup.5 represents hydrogen atom, or R.sup.1 and R.sup.5 are bonded to represent a lower alkylenedioxy group; R.sup.2 represents hydrogen atom, a halogen atom, a lower alkoxy group or hydroxy group; R.sup.3 represents hydrogen atom, a carbamoyl lower alkyl group, a lower alkyl group, a carboxy lower alkyl group or a lower alkoxycarbonyl lower alkyl group; R.sup.4 represents hydrogen atom, a lower alkyl group, a carboxy lower alkyl group, a lower alkoxycarbonyl lower alkyl group, a lower alkanoyl group, an arylcarbonyl group, a lower alkanesulfonyl group, a lower alkoxycarbonyl group, an aralkyl group, formyl group or a di(lower alkyl)sulfamoyl group; n represents 0, 1 or 2; and the symbol * represents an asymmetric carbon atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.Type: GrantFiled: May 27, 1993Date of Patent: July 18, 1995Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, Masataka Hikota, Takeshi Yura, Toshiro Shikano, Masaaki Nagasaki
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Patent number: 5426091Abstract: A compound of formula (I): ##STR1## or a salt, enamine or the like, acylate, sulphonate, carbamate or ether derivative thereof; wherein X, X.sup.1 and X.sup.2 are independently oxygen or sulphur, R.sup.1 is an optionally substituted heterocyclic or cycloalkyl group, and Y is an optionally substituted C.sub.2 -C.sub.4 alkylene group which is optionally interposed by an oxygen atom, a group ##STR2## or an optionally mono-substituted nitrogen atom, wherein p is 0, 1 or 2, s is 0 or 1 and R.sup.b is alkyl or alkoxy; provided that when X, X.sup.1 and X.sup.2 are oxygen, R.sup.1 is not pyridyl or pyrimidinyl. Processes for the preparation of these compounds and herbicidal compositions containing them are also described and claimed.Type: GrantFiled: August 4, 1993Date of Patent: June 20, 1995Assignee: Zeneca LimitedInventors: John E. D. Barton, David Cartwright, John M. Cox, Glynn Mitchell, Charles G. Carter, David L. Lee, Francis H. Walker, Frank X. Woolard
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Patent number: 5424455Abstract: A heterocyclic compound of the formula, ##STR1## wherein A and B are each hydrogen, halogen, alkyl or alkoxy, R.sup.1 is alkylene having upto 6 carbon atoms, X is direct linkage or divalent group such as --O--, --S--and the like, T and U are each hydrogen or alkyl, l is 0 or 1 to 3, Q is 5-, 6- or 7- membered saturated or unsaturated heterocyclic residue, and Y is hydrogen, halogen, alkyl, alkoxy or ##STR2## and B are taken together with each other to form methylene-dioxy, which is useful for dyeing or printing hydrophobic fiber materials with superior dyeability to give a dyed or printed product of a red color excellent in fastness properties, particularly those such as washing fastness.Type: GrantFiled: July 28, 1993Date of Patent: June 13, 1995Assignee: Sumitomo Chemical Co., Ltd.Inventors: Jun Yamamoto, Yasuyoshi Ueda, Junichi Sekihachi, Yosuke Yamamoto, Takashi Omura
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Patent number: 5378713Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.Type: GrantFiled: November 4, 1991Date of Patent: January 3, 1995Assignee: Ortho Pharmaceutical CorporationInventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
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Patent number: 5360800Abstract: The invention relates to tricyclic lactams of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenyl C.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl or phenoxymethyl,one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl C.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkhyl group;n represents 2 or 3; and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.Type: GrantFiled: August 7, 1991Date of Patent: November 1, 1994Assignee: Glaxo Group LimitedInventors: Ian H. Coates, Peter C. North, Alexander W. Oxford
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Patent number: 5356891Abstract: The present invention relates to compounds having anti-ischaemic activity of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and Z are as defined herein. The present invention further relates to a method of preparing such compounds, as well as compositions having anti-ischaemic activity which comprise such compounds and a method of treating ischaemia.Type: GrantFiled: November 16, 1992Date of Patent: October 18, 1994Inventors: Donald T. Witiak, Ineke van Wijngaarden, Raghunathan V. Nair, Josephus H. M. Lange, Jacobus A. J. den Hartog
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Patent number: 5340822Abstract: The invention relates to polycyclic amine compounds of formula (I) ##STR1## where Y. m. Ar', n, p, Q, T, q and Z are defined herein. The invention also relates to methods of making the compounds of formula (I) and pharmaceutical compositions which contain the compounds of formula (I). The inventive compounds are useful as neurokinin receptor antagonists, and are useful for the treatment of any substance P-dependent and neurokinin-dependent pathological condition.Type: GrantFiled: May 4, 1992Date of Patent: August 23, 1994Assignee: Elf SanofiInventors: Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Pierre Goulaouic, deceased, by Marie Bousquet, heir, by Catherine M. L. Goulaouic, heir
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Patent number: 5317017Abstract: There are disclosed certain compounds identified as N-biphenyl-3-amido substituted benzolactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzolactams as the active ingredient thereof are also disclosed.Type: GrantFiled: September 30, 1992Date of Patent: May 31, 1994Assignee: Merck & Co., Inc.Inventors: Hyun O. Ok, William R. Schoen, Matthew Wyvratt
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Patent number: 5300647Abstract: Hindered amines based on various 2,2,6,6-tetraalkylated nitrogen-containing heterocyclic moieties wherein the hindered nitrogen atom on the ring is substituted with O-acyl, O-carbamoyl or O-carbonate substituents and the 4-position of the ring is substituted with a variety of groups, are effective as light stabilizers in diverse substrate systems.Type: GrantFiled: May 28, 1993Date of Patent: April 5, 1994Assignee: Ciba-Geigy CorporationInventors: Roger F. Malherbe, Roland A. E. Winter, James P. Galbo
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Patent number: 5292734Abstract: This disclosure describes novel 2, 3, 6 substituted quinazolinones having the formula: ##STR1## wherein X, R, and R.sup.6 are described in the specification which have activity as angiotensin II (AII) antagonists.Type: GrantFiled: April 23, 1993Date of Patent: March 8, 1994Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Aranapakam M. Venkatesan
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Patent number: 5284857Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.Type: GrantFiled: December 21, 1990Date of Patent: February 8, 1994Assignee: Ortho Pharmaceutical CorporationInventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
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Patent number: 5281585Abstract: Fibrinogen receptor antagonists of the formula: ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.Type: GrantFiled: November 6, 1992Date of Patent: January 25, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Nathan Ihle, George D. Hartman, Laura M. Turchi, William F. Hoffman
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Patent number: 5248683Abstract: Compounds of the formula ##STR1## in which A.sub.1 and A.sub.2 independently of one another are CO--C.sub.1 -C.sub.4 alkyl, COO--C.sub.1 -C.sub.4 alkyl, CO--CF.sub.3, CO--N(R).sub.2 or cyano;A.sub.1 and A.sub.2 together are CO(X).sub.n --C.sub.1 -C.sub.3 alkylene-(X).sub.n CO, CO(X).sub.n --C.sub.1 -C.sub.3 alkylene-(X).sub.n CO which is substituted by C.sub.1 -C.sub.4 alkyl, COOR, CON(R).sub.2, cyano or phenyl, it being possible for the phenyl ring, in turn, to be substituted by halogen, methyl, trifluoromethyl, methoxy, nitro or cyano; CO--N(R)--CO--N(R)--CO;R is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl or C.sub.3 -C.sub.6 alkynyl;X is oxygen, sulfur or N(CH.sub.3);X.sub.1, X.sub.2 and X.sub.3 independently of one another are hydrogen, halogen, methyl, methylthio, methoxy or nitro;n is 0 or 1;including the salts of the compounds of the formula I with agriculturally acceptable organic or inorganic bases, and including the metal complexes; have valuable microbicidal properties.Type: GrantFiled: June 4, 1992Date of Patent: September 28, 1993Assignee: Ciba-Geigy CorporationInventors: Hans-Georg Brunner, Walter Kunz, Rolf Schurter
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Patent number: 5247081Abstract: Processes for the preparation of biotinylated polynucleotides and analogues thereof and protected intermediate products for use in such processes are described and claimed. The processes may be conveniently used in the automated synthesis of biotinylated polynucleotide on a DNA synthesizer. The polynucleotides so prepared may be used as labelled probes e.g. as diagnostic tools for clinical and research uses.Type: GrantFiled: August 23, 1988Date of Patent: September 21, 1993Assignee: Imperial Chemical Industries PLCInventor: Michael D. Edge
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Patent number: 5244888Abstract: Substituted 8-alkoxy-1,2,3,3a,8,8a-hexahydroindeno[1,2-c]pyrroles; 5-alkoxy-2,3,4,4a,9,9a-hexahydro-1-H-indeno[2,1-c]pyridines; and 9-alkoxy-2,3,3a,4,5,9a-hexahydro-1H-benz[e]isoindoles are selective 5-HT receptor agents and are thus useful in the treatment of anxiety, depression, and hypertension.Type: GrantFiled: July 9, 1991Date of Patent: September 14, 1993Assignee: Abbott LaboratoriesInventors: John F. DeBernardis, Michael D. Meyer, Kevin B. Sippy
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Patent number: 5240919Abstract: Compounds of general formula (I): ##STR1## where R, X, A, B and p are defined in the description. Medicinal products useful for treating sleep disorders comprising the same.Type: GrantFiled: March 9, 1992Date of Patent: August 31, 1993Assignee: Adir et CompagnieInventors: Said Yous, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
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Patent number: 5236935Abstract: The present invention relates to novel benzopyran derivatives of formula (I) which have superior selectivity in the treatment of hypertension by lowering blood pressure with a relaxation activity on vascular smooth muscle. The present invention also relates to processes for preparing such compounds; and to a pharmaceutical compositions containing such compounds as an active ingredient. ##STR1## wherein: R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, a fluorine, chlorine or hydrogen atom; R.sup.A and R.sup.B are, each independently, an amino, C.sub.1-6 alkoxy, C.sub.1-6 alkyl group or an optionally substituted phenyl group; and R.sup.C and R.sup.D are a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is ##STR3## wherein R.sup.Type: GrantFiled: May 21, 1992Date of Patent: August 17, 1993Assignee: Korea Research Institute of Chemical TechnologyInventors: Sung-Eun Yoo, Kyu Y. Yi, Nak C. Jeong, Jee H. Suh, Seon-Ju Kim, Hwa-Sup Shin, Byung H. Lee, Kyu S. Jung
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Patent number: 5223616Abstract: A heterocyclic compound which is useful for dyeing or printing hydrophobic fiber materials and which has the following formula (I), ##STR1##wherein A.sub.1, A.sub.2, A.sub.3 and A.sub.4 are each hydrogen, halogen, alkyl, alkoxy or alkenyl, X.sub.1 is --O-- or the like, R.sub.1 is a methylene or the like, X.sub.2 is a direct linkage or a divalent group of --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## in which R.sub.3 is a hydrogen atom or a C.sub.1-4 alkyl group, ##STR3## in which R.sub.3 is as defined above, T and u are each independently hydrogen or a C.sub.1-4 alkyl, l is O or an integer of 1 to 3, Q is an unsubstituted or substituted 5-, 6- or 7-membered saturated or unsaturated heterocyclic residue, Y is hydrogen, C.sub.1-4 alkyl, a C.sub.1-4 alkoxy group or the like.Type: GrantFiled: November 4, 1991Date of Patent: June 29, 1993Assignee: Sumitomo Chemical Company, Ltd.Inventors: Jun Yamamoto, Junichi Sekihachi, Yosuke Yamamoto, Kazuhiro Machiguchi, Yutaka Kayane
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Patent number: 5223523Abstract: Compounds for an methods of controlling plant diseases using thiooxazolidinones, oxazolidindiones and agriculturally suitable compositions containing them are disclosed.Type: GrantFiled: December 12, 1991Date of Patent: June 29, 1993Assignee: E. I. Du Pont de Nemours and CompanyInventors: John B. Adams, Jr., Detlef Geffken, Dennis R. Rayner
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Patent number: 5206149Abstract: This invention relates to a method of high sensitivity luminescence analysis using, as an enhancer, 2-hydroxy-9-fluorenone, the compound expressed by the following formula ##STR1## or an oxazole compound expressed by the formula ##STR2## in the formula R.sub.1 representing hydrogen, C.sub.n H.sub.2n+1 (here, n representing a positive integer of 1 to 4), XC.sub.n H.sub.2n (here, X representing F, Cl, Br or I, and n representing a positive integer of 1 to 4), C.sub.n H.sub.2n+1 CO.sub.2 (n being as defined above), a phenyl group, a naphthyl group, C.sub.n H.sub.2n+1 C.sub.6 H.sub.4 (n being as defined above), YC.sub.6 H.sub.4 (Y representing F, Cl, Br, I or a phenyl group) or XYC.sub.6 H.sub.3 (X and Y being as defined above).Type: GrantFiled: February 5, 1991Date of Patent: April 27, 1993Assignee: Toray Industries, Inc.Inventors: Yoshihiro Oyama, Shuntaro Hosaka, Tetsuya Makino
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Patent number: 5190937Abstract: Novel compounds of formula (I), and pharmaceutically acceptable salts thereof; their preparation; compositions containing them; and their use in the treatment of conditions in which degradation of connective tissue and other proteinaceous components of the body occurs: ##STR1## in which, R.sub.1 is --OH; alkoxy; aryloxy or aralkyloxy in each of which the aryl group is optionally substituted; --NR.sub.6 R.sub.7, where each of R.sub.6 and R.sub.7 is independently hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an optional oxygen or sulphur atom or an optionally substituted second nitrogen atom in the ring; or a group:--NH--CH(R.sub.8)--C(O)--R.sub.9where R.sub.8 is hydrogen; alkyl optionally substituted by --OH, alkoxy, --NR.sub.6 R.sub.7 as defined for R.sub.1, guanidine, --CO.sub.2 H, --CONH.sub.2, --SH, or --S--alkyl; or --CH.sub.2 --Ar where Ar is optionally substituted aryl or heteroaryl; and R.sub.Type: GrantFiled: January 11, 1991Date of Patent: March 2, 1993Assignee: Beecham Group p.l.c.Inventors: Roger E. Markwell, Ian Hughes
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Patent number: 5175157Abstract: Disclosed are new cyclic amine derivatives of the formula I ##STR1## wherein the substituents are defined in the specification. These compounds are useful as for treating sinus tachycardia.Type: GrantFiled: July 3, 1991Date of Patent: December 29, 1992Assignee: Boehringer Ingelheim GmbHInventors: Manfred Psiorz, Joachim Heider, Andreas Bomhard, Manfred Reiffen, Norbert Hauel, Klaus Noll, Berthold Narr, Christian Lillie, Walter Kobinger, Jurgen Dammgen
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Patent number: 5169844Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in inhibition of absorption of cholesterol and thus lowers serum cholesterol levels. Compounds of the formula below: ##STR1## where R.sup.1 is selected from alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or arylalkyl and R.sup.2 is hydrogen or alkyl or --NR.sup.1 R.sup.2 is morpholine, thiomorpholine or 4-substituted or unsubstituted piperidine and R.sup.3, R.sup.4, R.sup.5, R.sup.6 are hydrogen, alkyl, alkoxy, halogen, nitro, cyano, perhaloalkyl, alkanoyloxy, alkoxycarbonyl or hydroxycarbonyl have been shown to inhibit the enzymes CEH and/or ACAT in in vitro tests to inhibit absorption of radio-labeled cholesterol in rats.Type: GrantFiled: December 20, 1991Date of Patent: December 8, 1992Assignee: American Home Products CorporationInventors: Thomas J. Commons, Donald P. Strike
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Patent number: 5164386Abstract: Pharmacologically active R(-) 3-quinuclidinol derivatives are described which are muscarinic receptor blocking agents useful for the treatment of gastrointestinal and respiratory tract disorders of the following formula (I) ##STR1## wherein R represents a linear or branched lower alkyl group, a cycloalkyl-C.sub.1-2 alkyl or an aralkyl group, or it is absent;X represents the anion of an organic or inorganic acid, or it is absent, when R is absent;R.sub.1 represents H, a linear or branched lower alkyl group or an acyl group of the type R.sub.2 --CO, in which R.sub.Type: GrantFiled: June 20, 1990Date of Patent: November 17, 1992Assignee: Istituto de Angeli S.p.A.Inventors: Enzo Cereda, Giuseppe Bietti, Giovanni B. Schiavi, Arturo Donetti, Antonio Schiavone, Henri N. Doods
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Patent number: 5157034Abstract: Antipsychotic compounds having the formula ##STR1## wherein Z is H or Cl; Y is O or S; n is 1-4; separately, X is H or (C.sub.1 -C.sub.2)alkyl and L is R(CH.sub.2).sub.m CO, m is 0 or 1-3, R is (C.sub.1 -C.sub.6)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, phenyl, naphthyl, furyl, benzofuranyl, thienyl, benzothienyl, pyrrolyl, indolyl, isoindolyl or one of said groups substituted on aromatic or heteroaromatic ring with fluoro, chloro, (C.sub.1 -C.sub.2)alkyl or (C.sub.1 -C.sub.2)alkoxy; or together L and X, in combination with the nitrogen to which they are attached, form certain cyclic imides, 4-substituted piperidines or a cyclic sulfonamide.Type: GrantFiled: February 27, 1991Date of Patent: October 20, 1992Assignee: Pfizer Inc.Inventors: Gene M. Bright, Kishor A. Desai, Thomas F. Seeger
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Patent number: 5149823Abstract: A novel class of sulfonamoyl-substituted 1,6-diaza[4.4]spirodilactams, having a sulfonamoyl substituent on the hydrocarbyl group attached to each spiro ring nitrogen atom, is useful for the preparation of polymers, including polyamides and as latent curing agents for epoxy resins.Type: GrantFiled: August 9, 1990Date of Patent: September 22, 1992Assignee: Shell Oil CompanyInventor: Pen-Chung Wang
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Patent number: 5134140Abstract: The antipsychotic, antidepressant, anxiolytic compounds of the formula: ##STR1## wherein Z is phenyl or phenyl substituted with alkyl, alkoxy, hydroxy, halogen or methylenedioxy or Z is one of the structures ##STR2## in which m is one of the integers 0, 1 or 2; R.sup.6 is hydrogen or alkyl; Y is H.sub.2 or O; or Z, taken with R.sup.1, forms one of the structures ##STR3## R.sup.1 is hydrogen or alkyl; R.sup.2 is hydrogen alkyl or phenyl; R.sup.3 is hydrogen or alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido of 2 to 6 carbon atoms or sulfonamido, or R.sup.4 and R.sup.5 together form methylenedioxy, ethylenedioxy, or propylenedioxy; n is one of the integers 2, 3 or 4; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 21, 1991Date of Patent: July 28, 1992Assignee: American Home Products CorporationInventor: Gary P. Stack
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Patent number: 5116958Abstract: Disperse dyes, which produce dyeings of excellent thermomigration fastness, consisting of a chromophore and a lactam or oxime radical which detaches on heating to leave an isocyanate or isothiocyanate group, which reacts with a suitable group in the environment. The disclosed dyes are described by the formula ##STR1## where F is the radical of a dye which is free of water-solubilizing groups,B is a bridge member or a direct bond,Z is O or S andV is the radical of a group H--V, where H--V is an oxime of the formula ##STR2## or a lactam of the formula ##STR3## in which R.sup.1 and R.sup.2 are each independently of the other substituted or unsubstituted alkyl or aryl, orR.sup.1 and R.sup.2 together with the carbon atom linking them form a cycloaliphatic ring,R is hydrogen or alkyl andn is an integer from 4 to 11.Type: GrantFiled: January 5, 1990Date of Patent: May 26, 1992Assignee: Ciba-Geigy CorporationInventors: Peter Liechti, Martin Trottmann
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Patent number: 5110585Abstract: The invention relates primarily to quaternized polycyclic compounds having the formula ##STR1## wherein m is an integer having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; R.sub.2 together with the quaternary nitrogen, forms a 5 to 14 membered heterocyclic ring, said ring containing at least 2 hetero atoms selected from the group of nitrogen, sulfur and oxygen; R.sub.1 forms a double bond in the heterocyclic ring of the quaternized nitrogen or is alkyl, alkyleneoxyalkyl, alkylhydroxy, aryl, aralkyl, aralkenyl, alkaryl, alkylamidoalkyl and X.sup.- is an anion. The invention also relates to the preparation and use of said quaternized polycyclic compounds.Type: GrantFiled: March 1, 1989Date of Patent: May 5, 1992Assignee: ISP Investments Inc.Inventors: Ratan K. Chaudhuri, David J. Tracy, Robert B. Login, Michael W. Helioff
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Patent number: 5106971Abstract: The prior art solvent process for the manufacture of an oxo-piperazinyl triazine (PIP-T) compound required carrying out the reaction between an appropriately hindered cyclic amine and cyanuric chloride in the presence of caustic catalyst, in alkylbenzene solution, typically toluene. The chloride ions generated during the reaction, in presence of water present in the reaction zone, produced serious corrosion and resulted in off-color product which had a melt absorptivity greater than 3.5 mL/gm.cm. This "color" in the product made the product generally unmarketable. Another process to make a PIP-T termed "the solventless" process used no toluene solvent, and no caustic but required such a very large excess of amine that the catalytic function of the amine.HCl salt went unnoticed.Type: GrantFiled: April 12, 1991Date of Patent: April 21, 1992Assignee: The B. F. Goodrich CompanyInventors: George Kletecka, Victor L. Ledesma, Ronald M. Kovach
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Patent number: 5104869Abstract: Renin inhibiting compounds containing a single .alpha.-amino acid of the formula: ##STR1## and analogs thereof which inhibit the substrate-cleaving acting or renin, pharmaceutical compositions containing these compounds, processes for producing the compounds and methods of treating hypertension which employ the novel renin inhibitors.Type: GrantFiled: October 25, 1990Date of Patent: April 14, 1992Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Charles Frederick, Jeremy I. Levin, Fuk-Wah Sum, Marvin F. Reich
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Patent number: 5093336Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: July 6, 1989Date of Patent: March 3, 1992Assignee: Hoechat-Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Bettina Spahl
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Patent number: 5079356Abstract: Urea derivatives with .alpha.,.beta.-ethylenically unsaturated carboxyl or carboxamide radicals, produced by reaction of ethylenically unsaturated isocyanates with ammonia or amines or by reaction of ethylenically unsaturated amines with isocyanates in the absence of water, optionally in bulk, it being possible to carry out the reaction for improved reaction control advantageously in inert organic solvents or also in so-called reactive diluents, i.e. copolymerizable ethylenically unsaturated monomeric compounds which remain inert under the reaction conditions, such as for example vinyl esters, (meth)acrylates, vinyl aromatics.The urea derivatives produced according to the invention have in their monomeric form slight to moderate or in some cases good solubility in water and/or in organic solvents. They are polymerizable or copolymerizable via their .alpha., .beta.Type: GrantFiled: July 2, 1990Date of Patent: January 7, 1992Assignee: Hoechst AGInventor: Hans-Ullrich Huth
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Patent number: 5075302Abstract: Mercaptoacyl aminolactam inhibitors of endopeptidases of the formula ##STR1## wherein Y is -(CHR.sup.5).sub.n (CR.sup.3 R.sup.4)- or -(CR.sup.3 R.sup.4).sub.p X(CR.sup.3 R.sup.4).sub.q -,wherein two substituents selected from the group consisting of R.sup.3, R.sup.4 and R.sup.5, can form a benzene, cyclopentane or cyclohexane ring;X is -O-, -S-, -SO- or -SO.sub.2 -;Q is hydrogen or R.sup.6 CO-;m is 1 or 2;n is 1, 2, 3 or 4;p is 1 or 2;q is 2 or 3;R.sup.1 is lower alkyl, aryl or heteroaryl;R.sup.2 is hydrogen, lower alkyl, hydroxylower alkyl, lower alkoxylower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.3 and R.sup.4 are independently hydrogen, lower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.5 is hydrogen, lower alkyl, aryllower alkyl, heteroaryllower alkyl, hydroxy, lower alkoxy, mercapto, or lower alkylthio; and R.sup.Type: GrantFiled: March 9, 1990Date of Patent: December 24, 1991Assignee: Schering CorporationInventor: Bernard R. Neustadt
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Patent number: 5070088Abstract: Novel calcium channel blockers having the formula ##STR1## wherein X is oxygen or sulfur and wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 are as defined herein, are disclosed. These compounds are useful, for example, as anti-ischemic agents.Type: GrantFiled: December 19, 1989Date of Patent: December 3, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5051436Abstract: Novel N-acyl- and N-sulfonylbenzo-1,2,3-thiadiazole-7-carboxylic acid amides of formula ##STR1## in which X.sub.1 and X.sub.2 independently of one another are each hydrogen or together 1 to 3 halogen atoms; A is sulfonyl or carbonyl; Y is phenyl or phenyl substituted by C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 alkoxy, halogen, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 alkoxycarbonyl, C.sub.1 -C.sub.3 alkanoyloxymethyl, cyano and/or by nitro; R is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.3 -C.sub.5 alkenyl or C.sub.3 -C.sub.5 alkynyl; and in which, furthermore, the group ##STR2## wherein A.sub.1 is methylene, carbonyl or sulfonyl; X.sub.3 is hydrogen, methyl or halogen; m is 2, 3 or 4; and n is zero, 1 or 2.The novel active ingredients have plant-protecting properties and are suitable especially for the preventive protection of plants against attack by phytopathogenic microorganisms such as fungi, bacteria and viruses.Type: GrantFiled: February 16, 1990Date of Patent: September 24, 1991Assignee: Ciba-Geigy CorporationInventors: Walter Kunz, Rolf Schurter
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Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
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Patent number: 5041454Abstract: Substituted N-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides, their N-oxide forms, their pharmaceutically acceptable acid addition salts and stereochemically isomeric forms having gastrointestinal motility stimulating properties, compositions containing the same, and methods of treating warm-blooded animals suffering from motility disorders of the gastrointestinal system.Type: GrantFiled: April 19, 1990Date of Patent: August 20, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Michel A. J. De Cleyn
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Patent number: 5028711Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.Type: GrantFiled: July 6, 1989Date of Patent: July 2, 1991Assignee: Beiersdorf AktiengesellschaftInventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
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Patent number: 5001137Abstract: A novel pyridine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a salt thereof which exhibit inhibitory activity or prolylendopeptidase and a pharmaceutical use thereof are disclosed.Type: GrantFiled: September 14, 1989Date of Patent: March 19, 1991Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Takanori Oe, Yuji Ono, Kazuyuki Kawasaki, Tohru Nakajima
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Patent number: 4999371Abstract: 3,4-Dihydro-2H-benzo[b]pyrans of the formula I ##STR1## are described, in which R.sup.1 is H, OH, (C.sub.1 -C.sub.2)-alkoxy, (C.sub.1 -C.sub.2)-alkyl or NR.sup.4 R.sup.5,R.sup.4 and R.sup.5 being identical or different and representing H, (C.sub.1 -C.sub.2)-alkyl or (C.sub.1 -C.sub.3)-alkylcarbonyl,R.sup.2 and R.sup.3 are identical or different and are alkyl having 1-4 carbon atoms,Ar is an aromatic or heteroaromatic system which is unsubstituted or substituted,n is 1 or 2 andX is a (CH.sub.2).sub.r chain which can be interrupted by a heteroatom O, S or NR.sup.6, R.sup.6 being H or (C.sub.1 -C.sub.4)-alkyl andr being one of the numbers 2, 3, 4 or 5.Processes for the preparation of these compounds, their use and pharmaceutical products based on these compounds are also described.Type: GrantFiled: February 2, 1988Date of Patent: March 12, 1991Assignee: Hoechst AktiengesellschaftInventors: Heinrich C. Englert, Hans-Jochen Lang, Dieter Mania, Bernward Scholkens
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Patent number: 4992435Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.Type: GrantFiled: September 23, 1988Date of Patent: February 12, 1991Assignee: Ortho Pharmaceutical CorporationInventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
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Patent number: 4992434Abstract: A microbicidal compostion contains as active ingredient 2-chloro-4-trifluoromethylthiazol-5-carbonic acid derivatives of the formula I ##STR1## R is organic radical with up to 40 carbon atoms, which optionally contains nitrogen, oxygen or sulfur atoms and which can be transformed by hydrolosis or oxydation into the directly to the thiazol ring bound carboxyl rest. These compounds have good microbicidal activity and are used for the control and prevention of infestation of plants by phytophathogenic microorganisms.Type: GrantFiled: April 11, 1989Date of Patent: February 12, 1991Assignee: Ciba-Geigy CorporationInventors: Werner Topfl, Robert Nyfeler, Werner Fory
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Patent number: 4990506Abstract: A compound which is a 3-(acylaminomethyl)imidazo[1,2-a]pyridine derivative of formula (I) ##STR1## in which R.sub.1 denotes hydrogen; linear or branched C.sub.1 -C.sub.4 alkyl; or benzyl;R.sub.2 denotes linear or branched C.sub.1 -C.sub.6 alkyl; cyclohexyl; trichloromethyl; 1-propenyl; allyl; phenyl; 4-chlorophenyl; or benzyl:or R.sub.1 and R.sub.2 together denote a C.sub.3 -C.sub.5 aliphatic chain:X denotes halogen; C.sub.1 -C.sub.3 alkyl; methylthio; trifluoromethyl; optionally esterified carboxy of formula --COOR in which R denotes hydrogen or C.sub.1 -C.sub.6 alkyl; cyano; optionally mono- or dialkylated aminocarbonyl of formula --CONR.sub.3 R.sub.4 in which R.sub.3 and R.sub.4 independently denote hydrogen or C.sub.1 -C.sub.4 alkyl or together denote a chain of formula --(CH.sub.2).sub.2 --Z--(CH.sub.2).sub.2 -- in which Z denotes a direct bond, oxygen, sulphur, or a divalent group of formula --CH.sub.2 --, --NH-- or --N(C.sub.1 -C.sub.4 alkyl)--; alkylamino of formula NHR.sub.5 in which R.sub.Type: GrantFiled: October 24, 1989Date of Patent: February 5, 1991Assignee: SynthelaboInventors: Pascal George, Claudie Giron, Jacques Froissant
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Patent number: 4985444Abstract: The invention relates to pyrazolopyridine compounds for the treatment of melancholia, heart failure, hypertension, renal insufficiency, edema, obesity, bronchial asthma, gout, hyperuricemia, sudden infant death syndrome, immunosuppression, diabetes, myocardiac infection, thrombosis, obstruction, arteriosclerosis obliterans, thrombophlebitis, cerebral infarction, transient ischemic attack or angina pectoris, said compounds being of the formula ##STR1## wherein R.sup.1 is aryl, andR.sup.2 is unsaturated heterocyclic group which contains at least one heteroatom selected from the group consisting of N, O and S, which may have one or more suitable substituent(s),or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 18, 1990Date of Patent: January 15, 1991Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Youichi Shiokawa, Atsushi Akahane, Hirohito Katayama, Takafumi Mitsunaga
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Patent number: 4983623Abstract: The invention relates to derivatives of cyclic amino acids of the general formula ##STR1## in which R.sup.1 denotes hydrogen, alkyl, alkenyl or (subst.) aryl,R.sup.2 is hydrogen, alkyl, hydroxyl, alkoxy, (subst.) aryl, (subst.) aryloxy or (subst.) aroyl, or R.sup.1 and R.sup.2 together represent (subst.) benzylidene, or R.sup.1 and R.sup.2, together with the carbon atom carrying them, represent (subst.) cycloalkyl, R.sup.3 denotes hydrogen, hydroxymethyl, formyl, (subst.) alkenyl, (subst.) carboxycarbonyl, (subst.) carbamoylcarbonyl or (subst.) trifluoromethylcarbonyl, A represents a cyclic amino acid, X denotes oxygen, imino or N-alkylimino, m is 0-5 and n is 0 or 1, to a process for the preparation thereof, to agents containing them, and to the use thereof.Type: GrantFiled: December 13, 1988Date of Patent: January 8, 1991Assignee: Hoechst AktiengesellschaftInventors: Rainer Henning, Hansjorg Urbach, Franz Hock
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Patent number: 4980368Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;R.sub.2 and R.sub.3 are both hydrogen or together represent a bond;R.sub.4 is selected from C.sub.1-6 alkyl, phenyl, phenyl C.sub.1-4 alkyl, COR.sub.8 where R.sub.8 is hydroxy, C.sub.1-6 alkoxy or NR.sub.9 R.sub.10 where R.sub.9 and R.sub.10 are independently hydrogen or C.sub.1-4 alkyl and CH.sub.2 OR.sub.11 and R.sub.11 is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkanoyl;R.sub.5 is hydrogen, C.sub.1-6 alkyl or phenyl C.sub.1-4 alkyl;R.sub.6 is phenyl C.sub.1-7 alkyl in which the phenyl moiety is optionally substituted by one or two of halogen, ortho-nitro, meta- or para-methoxy, methyl or NR.sub.12 R.sub.13 wherein R.sub.12 and R.sub.13 are independently hydrogen or C.sub.1-6 alkyl or R.sub.12 and R.sub.13 together are C.sub.2-6 polymethylene or the phenyl moiety is 3,4-disubstituted by methylenedioxy or ethylenedioxy; andR.sub.7 is hydrogen or C.sub.Type: GrantFiled: December 23, 1986Date of Patent: December 25, 1990Assignee: Beecham-Wuelfing GmbH & Co. KGInventors: Dietrich Thielke, Dagmar Hoeltje
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Patent number: 4975439Abstract: Substituted N-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides, their N-oxide forms, their pharmaceutically acceptable acid addition salts and stereochemically isomeric forms having gastrointestinal motility stimulating properties, compositions containing the same, and methods of treating warm-blooded animals suffering from motility disorders of the gastrointestinal system.Type: GrantFiled: September 2, 1988Date of Patent: December 4, 1990Assignee: Janssen Pharmaceutical N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Michel A. J. De Cleyn