Having -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/220)
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Patent number: 6331507Abstract: There is disclosed substituted thiocarboxamides of the general formula (I) useful as herbicides.Type: GrantFiled: December 22, 1999Date of Patent: December 18, 2001Assignee: 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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Publication number: 20010051729Abstract: Novel reduction compositions are prepared from an active hydride, an additive, and a Lewis base in a hydrocarbon solvent. Such compositions can provide a superior reducing system for organic substrates.Type: ApplicationFiled: March 4, 1999Publication date: December 13, 2001Inventors: ANNE PAUTARD-COOPER, JOHN F. ENGEL, ERIC J. GRANGER, PHILIP F. SIMS, JAMES A. SCHWINDEMAN, TERRY L. RATHMAN
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Patent number: 6251829Abstract: This invention relates to herbicidal alpha-(2,4,5-trisubstituted)- and alpha-(2,5-disubstituted)-benzoyloxy-alpha-beta-, and/or beta-gamma-unsaturated-carboxylates and their derivatives, to compositions which contain these compounds, and to methods of use of these compounds.Type: GrantFiled: April 18, 2000Date of Patent: June 26, 2001Assignee: Rohm and Haas CompanyInventors: Bin Li, Ying Man, Zongjian Zhang, Longhe Xu, Adam Chi-Tung Hsu
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Patent number: 6242466Abstract: Phenylamidines of the formula (I) wherein: R6 is a C5-12-alkyloxycarbonyl group, and R7 is a hydrogen atom, or a C1-8-alkyl, C4-7-cycloalkyl, phenyl-C1-4-alkyl, or R8—CO—OCHR9— group, wherein R8 is a C1-4-alkyl, C1-4-alkoxy, C3-7-cycloalkyl, or C4-7-cycloalkoxy group, and R9 is a hydrogen atom or a C1-4-alkyl group, or a tautomer or pharmaceutically acceptable salt thereof. These compounds inhibit cell aggregation and are useful for the treatment or prevention of thrombosis, inflammation, bone degradation, tumors and tumor metastasis.Type: GrantFiled: July 14, 1999Date of Patent: June 5, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Frank Himmelsbach, Brian Guth, Hans-Dieter Schubert
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Patent number: 6197960Abstract: A process for producing a piperidinecarbinol represented by the general formula (2), which comprises reducing the trans isomer of a compound represented by the general formula (1): wherein R1 is a hydrogen atom, a lower alkyl group or an aralkyl group, R2 is a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, and X is a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, a dialkylamino group, an alkylthio group, an arylthio group or CmF2m+1— wherein m is an integer of from 1 to 20.Type: GrantFiled: April 11, 1997Date of Patent: March 6, 2001Assignee: Asahi Glass Company Ltd.Inventors: Shu-zhong Wang, Takashi Okazoe, Yasushi Matsumura, Nobuaki Mori, Jiro Nishino, Kazuhiro Ookura
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Patent number: 6143744Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: August 5, 1999Date of Patent: November 7, 2000Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.Inventors: Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Jian Jeffrey Chen, Robert Than Hendricks, Michael Joseph Melnick, Keith Adrian Murray Walker
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Patent number: 6080864Abstract: Selected derivatives of 1-oxyl-2,2,6,6-tetramethyl-4-hydroxypiperidine are surprisingly effective as inhibitors to prevent the premature polymerization of acrylic and methacrylic acids, their esters, their amides, vinyl acetate and acrylonitrile in the presence of water. Some of these derivatives are new compounds.Type: GrantFiled: February 1, 1999Date of Patent: June 27, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Glen T. Cunkle, Matthew E. Gande, Raymond Seltzer, Thomas F. Thompson
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Patent number: 6080742Abstract: Substituted benzamides corresponding to the formula I ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 have the meanings given herein, and their use in pharmaceutical compositions. The compounds are particularly useful as immunomodulators.Type: GrantFiled: September 24, 1999Date of Patent: June 27, 2000Assignee: Gruenenthal GmbHInventors: Tieno Germann, Stefanie Frosch, Oswald Zimmer
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Patent number: 6066642Abstract: The present invention provides certain novel compounds, compositions, and a method of treating a mammal by blocking its adenosine receptors comprising administering at least one compound of the present invention. Examples of the present inventive compounds include certain flavonoids of formulae (I) and (II), wherein R.sub.1 to R.sub.4 are as defined in the description, and M is --CH(OH)--CH(R.sub.2)-- or --C(OH).dbd.C(R.sub.2)-- and R.sub.1, R.sub.2 are as defined in the description; or dihydropyridines of formula (III), wherein R.sub.2 to R.sub.6 are as defined in the description; or pyridines of formula (IV), wherein R.sub.2 to R.sub.6 are as defined in the description, or triazoloquinazolines of formula (V), wherein R.sub.1 and R.sub.2 are as defined in the description; and their derivatives, or pharmaceutically acceptable salts thereof.Type: GrantFiled: December 7, 1998Date of Patent: May 23, 2000Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Ji-Long Jiang, Yong-Chul Kim, Yishai Karton, Albert M. Van Rhee
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Patent number: 6066737Abstract: The subject invention pertains to optically-enriched compounds of formula (1), wherein Ar is a C.sub.6-20 aryl group; and R.sup.1 and R.sup.2 are independently H, alkyl or aryl. The subject invention also pertains to method of preparing these compounds. The subject compounds can be prepared by reduction of the corresponding 1,4-dihydropyridine-3-aldehyde, e.g., using hydrogen an a catalyst. The aldehyde can be prepared by hydrolytic cleavage of an aminal obtainable by the reaction of 3-pyridinecarboxaldehyde and a chiral C-2 symmetric diamine, an then stereoselective introduction of the Ar and COOCHR.sup.1 R.sup.2 groups.Type: GrantFiled: June 29, 1998Date of Patent: May 23, 2000Assignee: Chirotech Technology, Ltd.Inventors: Brian Michael Adger, Gerard Andrew Potter, Martin Edward Fox
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Patent number: 6022971Abstract: The present invention provides compounds of the formula (I): ##STR1## and the pharmaceutically acceptable salts thereof, wherein R is C.sub.3 -C.sub.7 cycloalkyl, aryl or C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl being optionally substituted by fluoro, --COOH, --COO(C.sub.1 -C.sub.4) alkyl, C.sub.3 -C.sub.7 cycloalkyl, adamantyl, aryl or het.sup.1, and said C.sub.3 -C.sub.7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, fluoro, fluoro(C.sub.1 -C.sub.4) alkyl and fluoro(C.sub.1 -C.sub.4)alkoxy;R.sup.1 is phenyl, benzyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo and trifluoromethyl;R.sup.2 represents various groups;X is C.sub.1 -C.sub.4 alkylene; andX.sup.1 is a direct link or C.sub.1 -C.sub.6 alkylene.Type: GrantFiled: January 26, 1998Date of Patent: February 8, 2000Assignee: Pfizer IncInventors: Alexander Roderick MacKenzie, Allan Patrick Marchington, Donald Stuart Middleton, Sandra Dora Meadows
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Patent number: 6008360Abstract: The invention relates to glutarimides of formula (I): ##STR1## in which Ar represents a phenyl non substituted or substituted one or more times with one of the substitutents selected from a halogen atom, a hydroxyl, a (C.sub.1 -C.sub.4)alkoxy, a trifluoromethyl, a (C.sub.1 -C.sub.4)alkyl, said substitutents being identical or different ; a pyridyl group; a thienyl group and X is methylene or ethylene, their salts and their enantiomers, as well as their method of preparation and their use for the preparation of the corresponding 3,3-disubstituted piperidines.Type: GrantFiled: September 3, 1998Date of Patent: December 28, 1999Assignee: Sanofi-SynthelaboInventors: Philippe Camus, Marcel Descamps, Joel Radisson
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Patent number: 5981539Abstract: The present invention discloses compounds of the formula ##STR1## any of its enantiomers or any mixture thereof, or a pharmaceutically-acceptable addition salt thereof, wherein X, Ar, R, R.sup.1, R.sup.2, n are as defined herein.Type: GrantFiled: May 29, 1998Date of Patent: November 9, 1999Assignee: Neurosearch A/SInventors: Oskar Axelsson, Dan Peters, Nielsen Elsebet stergaard, Palle Christophersen
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Patent number: 5958952Abstract: The present invention relates to phenyl amidines of general formula (I), ##STR1## in which R.sup.1 to R.sup.5 are as defined in claim 1, their tautomers, their stereoisomers and their mixtures and their salts, especially their physiologically acceptable salts with inorganic or organic acids or bases also having valuable pharmacological properties, preferably aggregation-limiting effects, producing them.Type: GrantFiled: December 17, 1997Date of Patent: September 28, 1999Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Volkhard Austel, Gunther Linz, Helmut Pieper, Brian Guth, Johannes Weisenberger
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Patent number: 5936090Abstract: The present invention provides improved processes for the chemical reduction of imide esters to the corresponding amino alcohols with yields greater than 76%. A specific range of ethereal to hydrocarbon solvent ratio is used. The improved yield can be achieved using as a reducing agent lithium aluminum hydride or the less costly sodium aluminum hydride in combination with an additive such as lithium chloride.Type: GrantFiled: May 22, 1997Date of Patent: August 10, 1999Assignee: FMC CorporationInventors: Anne Pautard-Cooper, Philip Franklin Sims, James Anthony Schwindeman
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Patent number: 5935951Abstract: The invention relates to novel 1-acyl-4-aliphatylaminopiperidine compounds of ##STR1## formula (I), in which R.sub.1 is a benzoyl, naphthoyl or cycloalkanoyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen and/or trifluoromethyl; R.sub.2 is cycloalkyl or a phenyl or naphthyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen, nitro, cyano and/or trifluoromethyl; R.sub.3 and R.sub.4 together are lower alkylene or aza-, oxa- or thia-lower alkylene; or R.sub.3 is lower alkyl, lower alkoxy-lower alky, di-lower alkylamino-lower alkyl or a radical of the formula --(CH.sub.2).sub.n --C(.dbd.O)--R.sub.5 (Ia); and R.sub.4 is hydrogen, lower alkyl or a radical of the formula --(CH.sub.2).sub.n --C(.dbd.O)--R.sub.5 (Ia); R.sub.Type: GrantFiled: March 5, 1997Date of Patent: August 10, 1999Assignee: Novartis Finance CorporationInventors: Silvio Ofner, Siem Jacob Veenstra
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Patent number: 5908934Abstract: A process for the preparation of compounds of formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3, m, n and q are as defined herein; which comprises the steps of (a)reacting a compound of formula III ##STR2## with a chiral acid in an organic solvent to form a salt of a compound of formula I and (b) treating the salt of a compound of formula I with an aqueous base to obtain the compounds of formula I. Compounds of formula I are intermediates useful in the preparation of protein kinase inhibitors.Type: GrantFiled: September 12, 1997Date of Patent: June 1, 1999Assignee: Bristol-Myers Squibb CompanyInventor: Kyoung Soon Kim
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Patent number: 5874589Abstract: Disclosed are methods for synthesizing very large collections of diverse diverse tetramic acids, tetronic acids, pentamic acids, pentonic acids, and derivatives thereof and synthetic compound libraries comprising compounds prepared by such methods.Type: GrantFiled: July 18, 1997Date of Patent: February 23, 1999Assignee: Glaxo Wellcome, Inc.Inventors: David A. Campbell, Todd T. Romoff
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Patent number: 5844102Abstract: A compound of the formula ##STR1## wherein n, m, and p, which may be the same or different, are a number between 0 and 5; q is a number between 0 and 10; R.sub.1, R.sub.2 R.sub.3 R.sub.4 and R.sub.5, which may be the same or different, are a hydrogen, a hydroxyl, a halogen, a hydrocarbon or an O-hydrocarbon group having between 1 and 6 carbons which is aliphatic, alicyclic or aromatic, or a glycosyl group; and R.sub.4 is a glycosyl group, is disclosed. Nitrogen oxides of such compounds are also included. These novel compounds have been found to be potent glycohydrolase inhibitors. Processes for preparing these novel compounds and methods for their use in the treatment of diabetes mellitus are also provided.Type: GrantFiled: September 7, 1994Date of Patent: December 1, 1998Assignee: University of Maryland Baltimore CountyInventors: Michael R. Sierks, Mikael Bols, Troels Skrydstrup
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Patent number: 5789405Abstract: An oxaspiro ?2,5!octane derivative of the formula: ##STR1## useful in inhibiting angiogenesis in solid tumors.Type: GrantFiled: June 5, 1991Date of Patent: August 4, 1998Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Chiyoshi Kasahara, Takehiko Ohkawa, Masashi Hashimoto
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Patent number: 5783702Abstract: Cisapride, i.e. cis-4-amino-5-chloro-N-?1-?3-(4 fluoro-phenoxy)propyl!-3-methoxy-4-piperidinyl!-2-methoxy-benzamide, and similar benzamide derivatives, are prepared from novel 1-aryloxyalkyl- or 1-aralkyl-3-arylcarbonyloxy-4-oxo-piperidines, by nuclear substituent re arrangement involving acyl transfer under animal forming conditions, to give the corresponding 1-aryloxyalkyl- or 1-aralkyl-3-hydroxy-4-lower alkoxy-4-arylamido piperidine. This in turn is readily converted to the corresponding 3-oxo-4-arylamido-piperidine by reaction with strong organic acid, which can then be reduced, deprotected and 3-methylated to give the final compound, e.g. cisapride.Type: GrantFiled: August 21, 1996Date of Patent: July 21, 1998Assignee: Torcan Chemical Ltd.Inventors: Yee-Fung Lu, Clarke Slemon, Raymond So, Jan Oudenes, Teng-Ko Ngooi
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Patent number: 5776951Abstract: The present invention is concerned with diaryl compounds of formula (l) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.Type: GrantFiled: April 11, 1996Date of Patent: July 7, 1998Assignee: Glaxo Wellcome Inc.Inventors: Richard James Arrowsmith, John Gordon Dann, Karl Witold Franzmann, Simon Teanby Hodgson, Peter John Wates
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Patent number: 5767293Abstract: Oxaspiro?2,5! octanes of the formula ##STR1## inhibit angiogenesis and are particularly suitable for the treatment of solid tumors. In preferred embodiments, R.sup.1 is a carbamoyl derivative, R.sup.2 is an alkoxy substituent and R.sup.3 is ##STR2## Pharmaceutical salts of these compounds, such as methyl, amonium and organic amine salts also exhibit desirable properties.Type: GrantFiled: August 5, 1994Date of Patent: June 16, 1998Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Chiyoshi Kasahara, Takehiko Ohkawa, Masashi Hashimoto
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Patent number: 5726185Abstract: Acetic acid derivatives of the formula ##STR1## wherein L, M, T and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion, and are manufactured by cleaving protecting groups in the corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.Type: GrantFiled: December 1, 1994Date of Patent: March 10, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Paul Hadvary, Marianne Hurzeler Muller, Marcel Muller, Beat Steiner, Thomas Weller
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Patent number: 5665884Abstract: Cisapride, i.e. cis-4-amino-5-chloro-N-[1-[3-(4 fluoro-phenoxy)propyl]-3-methoxy-4-piperidinyl]-2-methoxy-benzamide, and similar benzamide derivatives, are prepared from novel 1-aryloxyalkyl- or 1-aralkyl-3-arylcarbonyloxy-4-oxo-piperidines, by nuclear substituent re arrangement involving acyl transfer under animal forming conditions, to give the corresponding 1-aryloxyalkyl- or 1-aralkyl-3-hydroxy-4-lower alkoxy-4-arylamido piperidine. This in turn is readily converted to the corresponding 3-oxo-4-arylamido-piperidine by reaction with strong organic acid, which can then be reduced, deprotected and 3-methylated to give the final compound, e.g. cisapride.Type: GrantFiled: August 21, 1996Date of Patent: September 9, 1997Assignee: Torcan Chemical Ltd.Inventors: Yee-Fung Lu, Raymond So, Clarke Slemon, Jan Oudenes, Teng-Ko Ngooi
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Patent number: 5631209Abstract: This invention relates to glutarimide compounds exhibiting herbicidal activity having the structure ##STR1## wherein A is carbonyl, thiocarbonyl or methylene, A.sup.1 is carbonyl or methylene, Q is O or (CH.sub.2).sub.n where n is 0 or 1, D is CH or N and R, R.sup.1, R.sup.2, T, X, Y and Z are as defined within, compositions containing these compounds and methods of using these compounds as herbicides and algicides.Type: GrantFiled: June 6, 1995Date of Patent: May 20, 1997Assignee: Rohm and Haas CompanyInventors: Barry C. Lange, John W. Ashmore, Jane Wissinger-Cornille, Colin M. Tice
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Patent number: 5616711Abstract: A method of producing an aminobutene derivative of formula (I) by allowing a butenol derivative of formula (II) to react with an amide derivative of formula (III) is disclosed. The aminobutene derivative of formula (I) can be deprotected to produce an aminobutene derivative of formula (I-1) or an aminobutene derivative of formula (I-2): ##STR1## The aminobutene derivative of formula (I-A) can also be deprotected to produce the aminobutene derivative of formula (I-B). Any or all of the above aminobutene derivatives are useful as intermediates for producing anti-ulcer drugs, and anti-ulcer drugs having an inhibitory effect on gastric acid secretion based on the antagonism against histamine H.sub.2 receptor.Type: GrantFiled: August 6, 1993Date of Patent: April 1, 1997Assignee: Fujirebio Inc.Inventors: Hiroshi Ikawa, Hajime Matsumoto, Masakatsu Matsumoto, Yasuo Sekine, Masato Nishimura, Akihiko Hosoda
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Patent number: 5596005Abstract: Omega-deoxy-azapyranose compounds, processes of making and using the same are disclosed, as are a process of making omega-deoxy-azafuranose compounds.Type: GrantFiled: December 23, 1993Date of Patent: January 21, 1997Assignee: The Scripps Research InstituteInventors: Chi-Huey Wong, Tetsuya Kajimoto, Kun-Chin Liu, Lihren Chen
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Patent number: 5594151Abstract: The present invention relates to a novel class of phenylboronic acid complexing reagents useful for the preparation of bioconjugates, and the method of making and using such reagents. In the present invention, in the place of prior art Avidin-Biotin and Digoxigenin-anti-Digoxigenin systems, phenylboronic acid complexing reagents are utilized in conjunction with phenylboronic acid reagents (many of which are known in the prior art) to facilitate chemical conjugation without the use of intermediary biological macromolecules. Reagents suitable for the modification of a bioactive species for the purpose of incorporating a phenylboronic acid complexing moiety for subsequent conjugation to a different bioactive species having pendant phenylboronic acid moleties are of General Formula I or General Formula II. ##STR1## wherein group X is selected from either H, OH, NH.sub.2, NHCH.sub.3, NHOH and NHOCH.sub.Type: GrantFiled: January 28, 1994Date of Patent: January 14, 1997Assignee: Prolinx, Inc.Inventor: Mark L. Stolowitz
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Patent number: 5591846Abstract: New nonionic radiographic contrast agents having the formula ##STR1## wherein Y is a single bond, ##STR2## R.sub.1, R.sub.1 ' and R.sub.2 are the same or different and are hydrogen, alkyl or hydroxyalkyl.Hydroxyalkyl refers to such alkyl groups having 1 or more hydroxy groups. Preferred hydroxyalkyl groups include: ##STR3## R.sub.3 and R.sub.4 are the same or different and are hydrogen, methyl or --CH.sub.2 CH.sub.2 OH; R.sub.5 is hydrogen, alkyl, --CH.sub.2 CH.sub.2 OH, CH.sub.2 OH or OH and R.sub.6 is alkyl, --CH.sub.2 CH.sub.2 OH, CH.sub.2 OH, OH or hydrogen and may be the same or different than R.sub.5 and m is zero or one, with the proviso that no methylene or methine carbon atom of the heterocyclic ring is attached to both a nitrogen and an oxygen atom with the additional proviso that when Y is a single bond, m is not zero. These new contrast agents are water soluble and have desirable low osmolality and anticoagulant properties.Type: GrantFiled: October 27, 1993Date of Patent: January 7, 1997Assignee: Bracco International B.V.Inventors: Ramachandran S. Ranganathan, Thangavel Arunchalam, Edmund R. Marinelli, Radhakrishna K. Pillai
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Patent number: 5585387Abstract: Cisapride, i.e. cis-4-amino-5-chloro-N-[1-[3-(4 fluoro-phenoxy)propyl]-3-methoxy-4-piperidinyl]-2-methoxy-benzamide, and similar benzamide derivatives, are prepared from novel 1-aryloxyalkyl- or 1-aralkyl-3-arylcarbonyloxy-4-oxo-piperidines, by nuclear substituent re arrangement involving acyl transfer under animal forming conditions, to give the corresponding 1-aryloxyalkyl- or 1-aralkyl-3-hydroxy-4-lower alkoxy-4-arylamido piperidine. This in turn is readily converted to the corresponding 3-oxo-4-arylamido-piperidine by reaction with strong organic acid, which can then be reduced, deprotected and 3-methylated to give the final compound, e.g. cisapride.Type: GrantFiled: October 7, 1994Date of Patent: December 17, 1996Assignee: Torcan Chemical Ltd.Inventors: Yee-Fung Lu, Raymond So, Clarke Slemon, Jan Oudenes, Teng-Ko Ngooi
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Patent number: 5559237Abstract: The present process involves ring opening and ring closure of compounds containing a tetrahydrofuroyl ##STR1## to provide facile synthesis of compounds containing a piperidin-2-one group of the formula ##STR2##Type: GrantFiled: July 15, 1994Date of Patent: September 24, 1996Assignee: Bracco International B.V.Inventors: Ramachandran S. Ranganathan, Thangavel Arunachalam, Kenneth J. Natalie, Jr.
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Patent number: 5496943Abstract: Disclosed is a novel heterocyclic compound selected from the group consisting of the compounds [IV] to [VII], [IX] and [X]. The heterocyclic compound is useful for reactive materials in chemical industry. A process for producing the heterocyclic compound is also disclosed.Type: GrantFiled: March 13, 1992Date of Patent: March 5, 1996Assignee: Nippon Paint Co., Ltd.Inventors: Otohiko Tsuge, Taizo Hatta, Satoshi Urano, Noriyuki Tsuboniwa, Ryuzo Mizuguchi
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Patent number: 5461071Abstract: A compound having the formula ##STR1## which is an anti-fungal agent is described. The producing organism Colletotricum accutatum is also described, along with a method of production.Type: GrantFiled: October 21, 1994Date of Patent: October 24, 1995Assignee: Merck & Co., Inc.Inventors: Evon A. Bolessa, Robert E. Schwartz, Gerald F. Bills, Robert A. Giacobbe, Fernando Pelaez Perez, Angeles Cabello Arroyo, Teresa Diez Matas, Isabel Martin Fernandez, Francisca Vincente Perez, Suzanne M. Mandala, Deborah L. Zink, Rosemary Thornton, John R. Thompson, James E. Curotto
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Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
Patent number: 5459270Type: GrantFiled: February 16, 1994Date of Patent: October 17, 1995Assignee: Merck Sharp & Dohme LimitedInventors: Brian Williams, Raymond Baker, Timothy Harrison, Christopher J. Swain -
Patent number: 5451679Abstract: Novel 2-chloro and 2-bromo derivatives of 1,5-iminosugars are disclosed, especially such derivatives of 1,5-dideoxy-1,5-imino-D-glucitol. These compounds are useful inhibitors of glucosidase enzymes and also are useful as antiviral agents and as intermediates for the synthesis of other enzyme inhibitors and antiviral compounds.Type: GrantFiled: March 8, 1994Date of Patent: September 19, 1995Assignee: G. D. Searle & Co.Inventors: Thomas E. Barta, Richard A. Mueller
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Patent number: 5439919Abstract: Arylglycinamide derivatives represented by a general formula (1) ##STR1## (wherein Ar denotes a phenyl group which may have 1 to 3 substituents or naphthyl group which may have 1 to 3 substituents, R.sub.1 and R.sub.4 denote identically or differently hydrogen atoms or lower alkyl groups with 1 to 3 carbon atoms, R.sub.2 denotes a lower alkyl group with 1 to 6 carbon atoms, cycloalkyl group with 3 to 6 carbon atoms, lower alkyl group with 1 to 4 carbon atoms which may have a phenyl group which may have 1 to 3 substituents, norbornyl group, adamantyl group or phenyl group which may have 1 to 3 substituents, R.sub.3 denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R.sub.2, R.sub.5 denotes a lower alkyl group with 1 to 6 carbon atoms or cycloalkyl group with 5 or 6 carbon atoms, R.sub.6 denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R.sub.Type: GrantFiled: July 20, 1993Date of Patent: August 8, 1995Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Hiroyuki Miyachi, Mitsuru Segawa, Emiko Tagami, Hideo Okubo
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Patent number: 5424319Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a piperidinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: December 16, 1993Date of Patent: June 13, 1995Assignee: G.D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5423998Abstract: Amino-derivative (poly)peroxycarboxylic acids which have the formula: ##STR1## wherein the symbols have the following meanings: R, R.sub.1, and R.sub.2, which may be equal to or different from one another, represent hydrogen atoms, alkyl groups or groups selected from R, R.sub.1 and R.sub.2, which taken together with the nitrogen atom to which they are linked, give rise to an aliphatic heterocyclic group, all of them being optionally substituted;A represents a (cyclo)alkylene group, an arylene group which may also be condensed with cycloaliphatic groups, a cycloalkylene-alkylene or an alkylene-cycloalkylene group, an arylene-alkylene or an alkylene-arylene group, which may be condensed with cyclo-aliphatic groups, wherein said alkylene group may also be interrupted by --CONR.sub.3 groups, wherein R.sub.3 represents a hydrogen atom or an alkyl or aryl group;X.sup.- represents HSO.sub.4.sup.- or CH.sub.3 SO.sub.3.sup.- ; a process for their preparation; and their use as bleaching agents.Type: GrantFiled: April 13, 1993Date of Patent: June 13, 1995Assignee: Ausimont S.r.l.Inventors: Carlo Venturello, Claudio Cavallotti
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Patent number: 5378712Abstract: N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R"' and Q have the significance given in the description, can be used for the treatment or control of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion.Type: GrantFiled: March 19, 1992Date of Patent: January 3, 1995Assignee: Hoffmann-La Roche IncInventors: Leo Alig, Paul Hadvary, Marianne Hurzeler, Marcel Muller, Beat Steiner, Thomas Weller
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Patent number: 5342951Abstract: Novel derivatives of 1-deoxynojirimycin are disclosed which have thio or sulfinyl substituents at C-2 or C-3. These compounds are useful inhibitors of lentiviruses such as visna virus and human immunodeficiency virus. Methods of chemical synthesis of these derivatives and intermediates therefor are also disclosed.Type: GrantFiled: August 2, 1993Date of Patent: August 30, 1994Assignee: G.D. Searle & Co.Inventors: Francis J. Koszyk, Richard A. Mueller
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Patent number: 5321031Abstract: Amides of the formula ##STR1## wherein: R.sup.1 is A and R.sup.2 is B; R.sup.1 is B and R.sup.2 is A; or R.sup.1 and R.sup.2 are independently selected from the group B;A is phenyl, substituted phenyl, heteroaryl, or substituted heteroaryl;B is cycloalkyl, substituted cycloalkyl, heterocycloalkyl, or substituted heterocycloalkyl;R.sup.3 is an alkyl chain of 1 to 25 carbon atoms, branched or straight; an alkenyl chain of 2 to 25 carbon atoms, branched or straight; a substituted alkyl chain; a substituted alkenyl chain; an interrupted alkyl chain; an interrupted alkenyl chain; a substituted interrupted alkyl chain; or a substituted interrupted alkenyl chain;R.sup.4 is hydrogen, lower alkyl, phenyl, Q-substituted phenyl, heteroaryl or Q-substituted heteroaryl;R.sup.6 and R.sup.7 are both H, or R.sup.6 and R.sup.7 together represent =O;or a pharmaceutically acceptable salt thereof;useful as inhibitors of acyl-coenzyme A:cholesterol acyl transferase and therefore in the treatment of atherosclerosis are disclosed.Type: GrantFiled: September 23, 1992Date of Patent: June 14, 1994Assignee: Schering CorporationInventor: Sundeep Dugar
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Patent number: 5258518Abstract: 2-Substituted tertiary carbinol derivatives of deoxynojirimycin are disclosed having the formula ##STR1## wherein R.sub.4 =an alkyl, vinyl, alkenyl, alkynyl, aryl, aralkyl, alkenylalkyl, alkylnylalkyl or CH.sub.2 Y substituent having from about 1 to 10 carbon atoms;Y=OR', SR', NR'R', or N.sub.3 ;R=H or CH.sub.3 ; andR=H or an alkyl, aralkyl, alkenylalkyl, alkynylalkyl, aralkenyl, aralkynyl or hydroxyalkyl substituent, having from about 1 to 18 carbon atoms, provided that no carbon unsaturated bond is directly attached to nitrogen.These compounds have useful antiviral activity as demonstrated against lentivirus.Type: GrantFiled: April 1, 1992Date of Patent: November 2, 1993Assignee: G. D. Searle & Co.Inventors: Ish K. Khanna, Richard A. Mueller, Richard M. Weier
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Patent number: 5238947Abstract: The present invention are novel compounds of the formula: ##STR1## wherein R is OH, NH.sub.2, OW, or H; X is H, F, Cl, Br, I, OH, OW, NO.sub.2 or NH.sub.2 ; Y is H, F, Cl, I, or Br; W is C(O)Z or a C.sub.1 to C.sub.12 alkyl group; Z is an aliphatic or aromatic group of from C.sub.1 to C.sub.12 ; X and Y can both vary within the molecule; and if R is H, at least one of X or Y is not H. In a preferred embodiment, R is OH or NH.sub.2. The most preferred compound is (4-hydroxy-3-N-phenylacetylamino-2,6-piperidinedione), in which R is OH, X is H and Y is H. These compounds have cytostatic activity and insert stereochemically into DNA.Type: GrantFiled: May 21, 1991Date of Patent: August 24, 1993Assignees: University of Georgia Research Foundation, Inc., Stereochemical Genetics, Inc.Inventors: Lawrence B. Hendry, Chung K. Chu, Virendra B. Mahesh
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Patent number: 5231184Abstract: Novel pyridazinamine derivatives having antiviral activity, compositions containing these compounds as active ingredient, and a method of destructing viruses or preventing the growth thereof in warm-blooded animals suffering from diseases caused by these viruses. Processes for preparing said compounds and compositions.Type: GrantFiled: December 9, 1991Date of Patent: July 27, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond A. Stokbroekx, Marcel J. M. Van der Aa, Marcel G. M. Luyckx, Gilbert A. J. Grauwels
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Patent number: 5223018Abstract: The invention relates to new 1-phenyl-piperidine-2,6-diones of the formula I ##STR1## wherein R is C.sub.3 -C.sub.7 -cycloalkyl,R.sub.1 is hydrogen or halogen;R.sub.2 is hydrogen, cyano, nitro or halogen; andA is hydrogen, cyano, nitro or is an ether or carboxylic acid radical as defined in the description. The salts, complexes as well as the stereoisomeric forms of these compounds, their preparations, use and agrochemical compositions which contains them form also part of this invention.Type: GrantFiled: March 26, 1992Date of Patent: June 29, 1993Assignee: Ciba-Geigy CorporationInventors: Hans Moser, Georg Pissiotas, Hans-Georg Brunner
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Patent number: 5221746Abstract: O-acylated derivatives of 1,5-dideoxy-1,5-imino-D-glucitol are disclosed that contain an N-alkyl or N-aroyl radical in which from one to four of the free hydroxyl groups are O-acylated with carboxylic alkanoyl radicals selected from the group consisting of .omega.,.omega.,.omega.-trifluoro alkanoyl having from three to eight carbon atoms, carboxylic cycloalkanoyl groups having from four to eight carbon atoms and carboxylic acyclic alkanoyl groups having from two to ten carbon atoms, wherein the N-aroyl radical is selected from the group consisting of p-decylbenzoyl, 3-(p-chlorophenoxy)propanoyl, 2-(acetyloxy)benzoyl, [1,1'-biphenyl]-4-ylcarbonyl, 2-thiopheneacetyl, trans-3-furanacryloyl 3-methoxyphenylacetyl and 3-(trifluoromethyl)benzoyl, and wherein the N-alkyl contains from one to fourteen carbon atoms, provided that when N-alkyl contains from one to five carbon atoms the O-acylated groups are .omega.,.omega.,.omega.-trifluoro alkanoyl or carboxylic cycloalkanoyl.Type: GrantFiled: July 27, 1992Date of Patent: June 22, 1993Assignee: G. D. Searle & Co.Inventors: Richard A. Partis, Francis J. Koszyk, Richard A. Mueller
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Patent number: 5218121Abstract: Novel compounds represented by the formula: ##STR1## wherein R represents hydrogen, optionally substituted alkyl radicals having from 1 to about 10 carbon atoms, optionally substituted alkenyl radicals having from 1 to about 10 carbon atoms, optionally substituted aryl, alkaryl and aralkyl radicals having from about 6 to about 16 carbon atoms and optionally substituted acyl and acyloxy radicals having from about 1 to about 10 carbon atoms, manifest glycosidase inhibition activity.Type: GrantFiled: March 2, 1992Date of Patent: June 8, 1993Assignee: Monsanto CompanyInventors: Daniel P. Getman, Gary A. DeCrescenzo
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Patent number: 5206251Abstract: Novel derivatives of 1-deoxynojirimycin are disclosed which have amino or azido substituents at C-2 and/or C-3. These compounds are useful inhibitors of lentiviruses. Methods of chemical synthesis of these derivatives and intermediates therefor are also disclosed.Type: GrantFiled: April 1, 1992Date of Patent: April 27, 1993Assignee: G. D. Searle & Co.Inventors: Ish K. Khanna, Richard A. Mueller, Richard M. Weier
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Patent number: 5200523Abstract: Nojirimycin .delta.-lactam and deoxynojirimycin are each synthesized from 5,6-anhydro-3-O-benzyl-1,2-O-isopropylidene-L-idofuranose as a divergent intermediate by a method which comprises formation of the piperidine ring by connection of nitrogen between C-1 and C-5 with inversion of configuration at C-5 to form nojirimycin .delta.-lactam or between C-2 and C-6 with inversion of configuration at C-2.Type: GrantFiled: June 17, 1991Date of Patent: April 6, 1993Assignee: Monsanto CompanyInventor: George W. J. Fleet