Nitrogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/74)
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Patent number: 6403633Abstract: The present invention is directed to compounds of Formula I: wherein X is O, S or NR7 and R1-R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.Type: GrantFiled: April 10, 2001Date of Patent: June 11, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Carl R. Illig, Nalin L. Subasinghe, James B. Hoffman, Kenneth J. Wilson, M. Jonathan Rudolph, Juan José Marugán
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Publication number: 20020057050Abstract: The present invention relates to a novel class of thermostable hole-injection and hole-transport compounds having tunable glass transition temperatures and ionization potentials for use in organic light emitting diode (“OLED”) devices. In particular, the compounds of the present invention comprise a trityl aniline core structure with various substituents attached to the nitrogen group, the structures of which allow for the adjustment of the glass transition temperatures and ionization potentials of the compounds. The present invention also relates to microdisplay devices comprising the compounds of the present invention in the hole-injection/hole-transport layers.Type: ApplicationFiled: June 28, 2001Publication date: May 16, 2002Inventor: Xiaobo Shi
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Publication number: 20020052509Abstract: Calcilytic compounds and compositions and their use in treating abnormal bone or mineral homeostasis.Type: ApplicationFiled: December 4, 2001Publication date: May 2, 2002Applicant: SmithKline Beecham CorporationInventors: Pradip Kumar Bhatnagar, James Francis Callahan, Eric G. Del Mar, Maria Amparo Lago
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Publication number: 20020052401Abstract: This invention relates to a series of substituted benzophenone and sulfone compounds of the formula I 1Type: ApplicationFiled: July 2, 2001Publication date: May 2, 2002Applicant: Pfizer Inc.Inventor: John A. Lowe
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Publication number: 20020019437Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I): 1Type: ApplicationFiled: July 31, 2001Publication date: February 14, 2002Inventors: David W. Boykin, M. Syed Rahmathullah, Richard R. Tidwell, James E. Hall
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Patent number: 6339161Abstract: Olefin co- or homopolymers having a good molecular weight and short chain branching may be prepared in the presence of a tridentate complex of a Group 8, 9 or 10 metal.Type: GrantFiled: February 19, 2001Date of Patent: January 15, 2002Assignee: Nova Chemicals (International) S.A.Inventors: Wei Xu, Qinyan Wang, Ryan Paul Wurz
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Publication number: 20010056107Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor &agr;, nuclear factor &kgr;B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.Type: ApplicationFiled: July 16, 2001Publication date: December 27, 2001Inventors: George W. Muller, Mary Shire
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Patent number: 6329523Abstract: Novel compounds having the formula: wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.Type: GrantFiled: March 10, 1999Date of Patent: December 11, 2001Assignee: ISIS Pharmaceuticals, Inc.Inventors: Phillip Dan Cook, Haoyun An
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Patent number: 6313132Abstract: The invention relates to novel compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Ar are as defined in claim 1, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers. The compounds have anticholinergic activity, and the invention also relates to the compounds of Formula (I), the use of the compounds of Formula (I) for preparing anticholinergic drugs, the use of the compounds of Formula (I) for treating urinary tract incontinence, and methods for preparing the compounds of Formula (I).Type: GrantFiled: September 27, 1999Date of Patent: November 6, 2001Assignee: Pharmacia ABInventors: Rolf Johansson, Martin Haraldsson, Erik Ringberg, Ian Vagberg, Katarina Beierlein, Rikard Emond, Birger Sjoberg
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Patent number: 6303782Abstract: A process is described for preparing an aromatic compound substituted by a tertiary nitrile of Formula (1.0.0): comprising treating a substituted aromatic compound of Formula (2.0.0): with a secondary nitrile of Formula (3.0.0): in the presence of a base having a pKa numerical value in the range of from about 17 to about 30, provided that the difference in pKa numerical values between said base and the corresponding tertiary nitrile of Formula (3.0.0) is no more than about 6; in an aprotic solvent having a dielectric constant (∈) of less than about 20; and at a reaction temperature in the range of from about 0° C. to about 120° C.; whereby there is formed said tertiary-nitrile-substituted aromatic compound final product of Formula (1.0.0); wherein the constituent parts W1, W2, W3, W4, and W5; and the substituent moieties R1, R2, R3, R4, R5, R6, and R7 in the compounds of Formulas (1.0.0), (2.0.0) and (3.0.Type: GrantFiled: March 1, 2000Date of Patent: October 16, 2001Assignee: Pfizer IncInventor: Stéphane Caron
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Patent number: 6281365Abstract: Organic platinum complexes active as anti-tumor agents in warm-blooded animals, and methods for synthesis of same, are described.Type: GrantFiled: May 26, 1989Date of Patent: August 28, 2001Assignee: American Cyanamid CompanyInventors: Ralph Grassing Child, Panayota Bitha, Joseph John Hlavka, Yang-I Lin
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Patent number: 6262101Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor &agr;, nuclear factor &kgr;B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovis replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.Type: GrantFiled: August 16, 2000Date of Patent: July 17, 2001Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 6262106Abstract: The compound of the above formula wherein R1-R5 are independently selected from hydrogen, alkyl and aryl and prodrugs thereof; and pharmaceutically acceptable salts thereof; and use of the compounds in therapy, particularly for treatment of a condition generally associated with abnormalities in glutamtergic transmission.Type: GrantFiled: September 13, 2000Date of Patent: July 17, 2001Assignee: Vernalis Research LimitedInventors: Nathaniel Julius Thomas Monck, Roger John Gillespie, Andrew James Bird
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Patent number: 6242607Abstract: The invention relates to glutarimides of formula (I): in which Ar represents a phenyl non substituted or substituted one or more times with one of the substituents selected from a halogen atom, a hydroxyl, a (C1-C4)alkoxy, a trifluoromethyl, a (C1-C4)alkyl, said substituents 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: November 10, 1999Date of Patent: June 5, 2001Assignee: Sanofi-SynthelaboInventors: Philippe Camus, Marcel Descamps, Joël Radisson
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Patent number: 6242637Abstract: The invention relates to compounds of the formula in which: A is a divalent radical selected from: A1) —O—CO— A2) —CH2—O—CO— A3) —O—CH2—CO— A4) —O—CH2—CH2— A5) —N(R1)—CO— A6) —N(R1)—CO—CO— A7) —N(R1)—CH2—CH2— A8) —O—CH2— in which: R1 is a hydrogen or a (C1-C4)-alkyl; and Am is a nitrogen-containing heterocycle.Type: GrantFiled: October 20, 1998Date of Patent: June 5, 2001Assignee: Sanofi-SynthelaboInventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
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Patent number: 6235768Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.Type: GrantFiled: May 10, 1999Date of Patent: May 22, 2001Assignee: Shionogi & Co., Ltd.Inventors: Fumihiko Wantanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani
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Patent number: 6225334Abstract: The invention concerns novel glyoxylic acid derivatives, a process for their preparation and their use as pesticides.Type: GrantFiled: January 11, 1999Date of Patent: May 1, 2001Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Klaus Stenzel, Ulrike Wachendorff-Neumann
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Patent number: 6215005Abstract: A process for the preparation of [2-(2-thienyl)-ethylamino]-(2-halogenophenyl)-acetonitriles of general formula (I) starting from 2-(2-thienyl)-ethyl-amine, alkalicyanide and o-halogeno-benzaldehyde. Compounds of general formula (I) are valuable intermediates.Type: GrantFiled: May 3, 2000Date of Patent: April 10, 2001Assignee: Sanofi-SynthelaboInventors: Alain Heymes, Bertrand Castro, Mária Bakonyi, Marianna Csatáriné Nagy, Leventéné Molnár
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Patent number: 6200353Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula at least one coupler comprising a compound of the formula: wherein R is selected from the group consisting of C1 to C2 alkyl and hydroxyethyl, R1 is selected from the group consisting of hydrogen, chlorine, bromine, C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 hydroxyalkyl and C1 to C3 hydroxyalkoxy, and X is O, S or NH.Type: GrantFiled: February 1, 2000Date of Patent: March 13, 2001Assignee: Bristol Myers Squibb CompanyInventors: Mu-Ill Lim, Linas R. Stasaitis, Yuh-Guo Pan
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Patent number: 6194443Abstract: The present invention pertains to new aminophenol derivatives of the following general formula (1), their preparation and their use as fungicides. wherein Y1, Y2, Y3, Y4, R1, and Z are as defined in the description.Type: GrantFiled: April 9, 1999Date of Patent: February 27, 2001Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Krüger, Heinz-Wilhelm Dehne, Klaus Stenzel
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Patent number: 6187808Abstract: This invention provides 6-amino-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one oximes and hydrazones which are useful in treating Parkinson's disease.Type: GrantFiled: September 27, 1999Date of Patent: February 13, 2001Assignee: Warner-Lambert CompanyInventors: Stephen Joseph Johnson, Leonard Theodore Meltzer, Lawrence David Wise
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Patent number: 6172091Abstract: Compounds of Formula I wherein the substituents are as described in the specification or pharmaceutically acceptable salts or stereochemically isomeric forms thereof, useful for treating diseases related to calcium imbalance and metabolism.Type: GrantFiled: October 13, 1999Date of Patent: January 9, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Judith Hope Cohen, Donald Ward Combs, Philip James Rybczynski
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Patent number: 6172103Abstract: 2-Cyano-3,5-dihydroxyhex-2-enecarboxamide derivatives are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases or disorders whose course involves increased connective tissue or cartilage degradation.Type: GrantFiled: November 24, 1999Date of Patent: January 9, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Wilfried Schwab, Ruth Raiss
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Patent number: 6132475Abstract: New p-diaminobenzene derivative compounds of the formula (I): ##STR1## and physiologically compatible water soluble salts thereof are described, wherein X represents oxygen, sulfur, selenium or N-R9. Compositions for dyeing keratin fibers including a combination of coupler and developer substance are described, in which the developer substance includes at least one of the new p-diaminobenzene derivative compounds.Type: GrantFiled: February 15, 1999Date of Patent: October 17, 2000Assignee: Wella AktiengesellschaftInventors: Laurent Chassot, Hans-Juergen Braun
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Patent number: 6127550Abstract: This invention is directed to methods for stereospecifically preparing [(1-optionally substituted aryl)- or (1-optionally substituted heteroaryl)]-2-substituted ethyl-2-amines, having chirality at the 2-position, and to intermediates to the substituted ethyl-2-amines.Type: GrantFiled: March 11, 1999Date of Patent: October 3, 2000Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Luc Grondard, Jean-Paul Casimir, Patrick Leon, Michael K. O'Brien, Matthew R. Powers, Daniel Robin
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Patent number: 6118007Abstract: A process, as a substitute for hydrolysis, for preparing a nitroguanidine derivative represented by the following formula (2): ##STR1## wherein A represents a substituted or unsubstituted aromatic or non-aromatic hydrocarbon ring, a substituted or unsubstituted aromatic or non-aromatic heterocycle, a hydrogen atom or a substituted or unsubstituted alkyl, alkenyl or alkynyl group; and R.sub.2 represents a hydrogen atom, a substituted or unsubstituted C.sub.1-6 alkyl, alkenyl or alkynyl group, which comprises reacting a compound represented by the following formula (1): ##STR2## wherein R.sub.1 represents a substituted or unsubstituted, linear or cyclic C.sub.1-10 alkyl group and A and R.sub.2 have the same meanings as defined above, with ammonia, a primary amine or a secondary amine, or a salt thereof.Type: GrantFiled: March 24, 1998Date of Patent: September 12, 2000Assignee: Mitsui Chemicals, Inc.Inventors: Koichi Ebihara, Tatsuo Kaiho, Michihiko Miyamoto, Daisuke Ura
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Patent number: 6107495Abstract: Novel thienylcyclohexane derivatives of general formula (I), wherein R' is the 2-thienyl or 3-thienyl radical, R is the cyano radical or a radical of formula --C(O)A, and R2" is a saturated or unsaturated optionally cyclic hydrocarbon radical, or an aryl radical, are disclosed. Methods for preparing said compounds, and the use thereof as novel industrial products for the synthesis of thienylcyclohexyl derivatives, are also disclosed.Type: GrantFiled: January 19, 1999Date of Patent: August 22, 2000Assignee: Societe d'Expansion Scientifique ExpansiaInventors: Jean-Bernard Cazaux, Michel Dafniet, Jean-Marc Kamenka, Eric Manginot
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Patent number: 6103907Abstract: Phenylalkylcarboxylic acid compounds of the formula: ##STR1## wherein R.sup.1 represents an alkyl group and the like, R.sup.2 represents an alkylene group, R.sup.3 represents a hydrogen atom and the like, X represents a substituted or unsubstituted aryl group and the like, Y represents an oxygen atom and the like, Z represents an alkylene group and the like, and W represents an alkyl group and the like),the pharmacologically acceptable salts thereof or the pharmacologically acceptable esters thereof are useful as therapeutic or preventive agents for hyperglycemia and the like.Type: GrantFiled: October 5, 1998Date of Patent: August 15, 2000Assignee: Sankyo Company, LimitedInventors: Hiroaki Yanagisawa, Makoto Takamura, Takashi Fujita, Toshihiko Fujiwara
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Patent number: 6096773Abstract: A method for the inhibition of the binding of .alpha..sub.4 .beta..sub.1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which .alpha..sub.4 .beta..sub.1 is involved.Type: GrantFiled: April 15, 1999Date of Patent: August 1, 2000Assignee: Texas Biotechnology Corporation, Inc.Inventors: Ian L. Scott, Bore G. Raju, Ronald J. Biediger, Vanessa O. Grabbe, Jamal Kassir, Karin M. Keller, Timothy P. Kogan, deceased, Shuqun Lin, Robert V. Market
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Patent number: 6080768Abstract: Compounds of the formula: ##STR1## wherein the variables are as defined in the specification. These compounds are useful in the treatment of arterial hypertension and heart failure, of renal insufficiency, of peripheral arteriopathies and of cerebrovascular insufficiencies.Type: GrantFiled: October 17, 1997Date of Patent: June 27, 2000Assignee: Zambon Group S.p.A.Inventors: Stefania Montanari, Paolo Cavalleri, Francesco Santangelo
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Patent number: 6077954Abstract: Novel compounds having the formula: ##STR1## wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.Type: GrantFiled: August 1, 1996Date of Patent: June 20, 2000Assignee: ISIS Pharmaceuticals, Inc.Inventors: P. Dan Cook, Haoyun An
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Patent number: 6063928Abstract: Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, amino and the like; X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; R.sup.1 and R.Type: GrantFiled: December 8, 1998Date of Patent: May 16, 2000Assignee: Pfizer IncInventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
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Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 6048882Abstract: Hepatic diseases can be prevented or treated by administering an isoprenylamine derivative represented by the general formula (II) ##STR1## [wherein n represents an integer of 4-12, m represents an integer of 0-3, Ar represents a phenyl group, a furyl group, a thienyl group or a pyridyl group, said group being optionally substituted with one or more of an alkyl group of 1-4 carbon atoms, and alkoxy group of 1-4 carbon atoms, a methylenedioxy group, a hydroxy group or a halogen atom, and R represents a hydrogen atom or an alkyl group of 1-4 carbon atoms] or a pharmacologically acceptable salt thereof at a daily dose of 0.01-500 .mu.g/kg.A lipid emulsion of the compound (II) is particularly useful and can be administered at a remarkably lowered dose as compared with other pharmaceutical preparations.Type: GrantFiled: August 8, 1997Date of Patent: April 11, 2000Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Tatsuya Ohwaki, Masako Yamada, Hiroyuki Yamazaki, Hitoshi Inoue, Yoshiyuki Tahara, Shigeo Kawase
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Patent number: 6048890Abstract: A thiophene derivative containing a phenylamidino group represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different from each other and are hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms or an alkoxyl group having 1 to 4 carbon atoms; or a pharmacologically acceptable salt thereof. The compound is useful for the treatment of inflammatory diseases.Type: GrantFiled: August 22, 1997Date of Patent: April 11, 2000Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Kiyomi Tanaka, Tokiko Nishida, Jun Nakano, Mamoru Inoue, Tsutomu Nakamura, Hayami Debuchi
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Patent number: 6042620Abstract: New p-diaminobenzene derivative compounds of the formula (I): ##STR1## and physiologically compatible water soluble salts thereof are described, wherein X represents oxygen, sulfur, selenium or N-R9, wherein R9 represents hydrogen, an alkyl group, a hydroxyalkyl group, a phenyl group or an acetyl group; and the remaining R groups each represent variously hydrogen, hydroxy, amino, nitro, nitrile, alkyl, alkoxy, hydroxyalkyl, cyclic or aromatic groups, among others. Compositions for dyeing keratin fibers including a combination of coupler and developer substance are disclosed, in which the developer substance includes at least one of the new p-diaminobenzene derivative compounds.Type: GrantFiled: February 25, 1999Date of Patent: March 28, 2000Assignee: Wella AGInventors: Hans-Juergen Braun, Laurent Chassot
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Patent number: 6043368Abstract: The present invention provides a method of preparing thieno[3,2-c]pyridine derivatives of formula I: ##STR1## wherein R.sub.1 is selected from the group consisting of lower alkyl; lower alkylene phenyl; substituted lower alkylene phenyl wherein the phenyl is substituted from 1 to 3 times with lower alkyl, lower alkoxy, lower acyloxy, hydroxy, nitro and halo; lower alkylene naphthyl, lower alkylene thienyl; lower alkylene diphenyl; lower alkylene-hydroxy-phenyl; substituted lower alkylene-hydroxy-phenyl wherein the phenyl is substituted from 1 to 3 times with lower alkyl, lower alkoxy, lower acyloxy, hydroxy, nitro, and halo; lower alkylene-hydroxy-naphthyl; lower alkylene-hydroxy-thienyl; lower alkylene-hydroxy-diphenyl, and R.sub.2 is H or lower alkylene. The method comprises reacting a compound of a formula II: ##STR2## with a cyclic dioxy or cyclic dithio in the presence of catalyst.Type: GrantFiled: September 4, 1996Date of Patent: March 28, 2000Assignee: Poli Industria Chimica, S.P.A.Inventors: Ambrogio Magni, Giovanni Signorelli
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Patent number: 6034273Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-(arylmethylene)-1-chloro-1-(perfluoroalkyl)methylamine compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds.The present invention provides N-(arylmethylene)-1-chloro-1-(perfluoroalkyl)methylamine compounds which are useful as intermediates in the preparation of arylpyrrole compounds.Type: GrantFiled: June 29, 1999Date of Patent: March 7, 2000Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 6022895Abstract: Substituted amino compounds of general formula (I) ##STR1## are described, as are a method of preparing them and their use as drugs, especially as analgesics.Type: GrantFiled: March 11, 1998Date of Patent: February 8, 2000Assignee: Gruenenthal GmbHInventors: Oswald Zimmer, Wolfgang Werner Alfred Strassburger, Helmut Heinrich Buschmann, Werner Englberger, Elmar Josef Friderichs
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Patent number: 6011161Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-(perfluoroalkylmethyl)arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds. In addition, the present invention provides N-(perfluoroalkylmethyl)arylimidoyl chloride compounds which are useful as intermediates in the preparation of arylpyrrole compounds.Type: GrantFiled: February 9, 1999Date of Patent: January 4, 2000Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 5965773Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-(perfluoroalkylmethyl)arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds.In addition, the present invention provides N-(perfluoroalkylmethyl)arylimidoyl chloride compounds which are useful as intermediates in the preparation of arylpyrrole compounds.Type: GrantFiled: February 9, 1999Date of Patent: October 12, 1999Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 5942538Abstract: The present invention relates to benzamidoxime derivatives represented by the formula ?I!; ##STR1## wherein R.sup.1 is unsubstituted or substituted C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted C.sub.2 -C.sub.4 alkenyl or unsubstituted or substituted C.sub.2 -C.sub.4 alkynyl, R.sup.2 is phenyl optionally having substituents or heterocycle optionally having substituents X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are each independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkylthio or the like, and r.sub.1 and r.sub.2 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl or the like, having excellent fungicidal activity and being useful as a fungicide for agricultural and horticultural use, and methods for preparation thereof.Type: GrantFiled: June 26, 1998Date of Patent: August 24, 1999Assignee: Nippon Soda Co., Ltd.Inventors: Isamu Kasahara, Hirohito Ooka, Shinsuke Sano, Hiroyasu Hosokawa, Homare Yamanaka
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Patent number: 5872129Type: GrantFiled: July 31, 1997Date of Patent: February 16, 1999Assignee: Auckland UniServices LimitedInventors: William Alexander Denny, William Robert Wilson, Moana Tercel
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Patent number: 5869067Abstract: The present invention relates to new aromatic compounds, to their preparation and to their use in human and veterinary medicine and in cosmetic compositions.Type: GrantFiled: September 26, 1994Date of Patent: February 9, 1999Assignee: Centre International De Recherches Dermatologiques Galderma (CIRD Galderma)Inventors: Jean-Phillippe Rocher, Jean-Michel Bernardon
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Patent number: 5856323Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: June 7, 1995Date of Patent: January 5, 1999Assignee: CytoMed, Inc.Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
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Patent number: 5856560Abstract: A process and intermediates for preparing .alpha.Type: GrantFiled: December 10, 1996Date of Patent: January 5, 1999Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Heinz Isak, Horst Wingert, Hubert Sauter, Michael Keil, Markus Nett, Remy Benoit, Ruth Muller
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Patent number: 5843980Abstract: A method of treating Pneumocystis carinii pneumonia in a subject in need of such treatment is disclosed. The method comprises orally administering to the subject a bis-benzamidoxime of Formula II ##STR1## wherein: R.sub.1 and R.sub.2 are each independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl or alkylaminoalkyl; R.sub.3 is H, loweralkyl, oxyalkyl, alkoxyalkyl, hydroxyalkyl, cycloalkyl, aryl, aminoalkyl, alkylaminoalkyl or halogen; R.sub.4 is --OY, or R.sub.1 and R.sub.4 together represent, ##STR2## wherein R.sub.5 is ##STR3## Y is H or loweralkyl; n is an integer from 0 to 2; and A is a heterocyclic aromatic group selected from the group consisting of: ##STR4## wherein R.sub.6 and R.sub.7 are each independently selected from the group consisting of H, loweralkyl, halogen, oxyalkyl, oxyaryl, or oxyarylalkyl, or a pharmaceutically acceptable salt thereof, that is reduced in the subject to produce a benzamidine having anti-P.Type: GrantFiled: November 15, 1996Date of Patent: December 1, 1998Assignees: Georgia State University Research Foundation, Inc., The University of North Carolina at Chapel HillInventors: James E. Hall, Richard R. Tidwell, David W. Boykin
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Patent number: 5834498Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate .alpha. configuration, solid triangles are used to indicate .beta. configuration, dashed bonds represent a double bond, or a single bond, R is a substituted heteroaryl radical, R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2, Y is .dbd.O or represents 2 hydrogen radicals. Certain of the compounds represented by Formula I comprise another aspect of the present invention.Type: GrantFiled: October 7, 1996Date of Patent: November 10, 1998Assignee: AllerganInventor: Robert M. Burk
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Patent number: 5817834Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-(perfluoroalkylmethyl)arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds. In addition, the present invention provides N-(perfluoroalkylmethyl)arylimidoyl chloride compounds which are useful as intermediates in the preparation of arylpyrrole compounds.Type: GrantFiled: February 9, 1998Date of Patent: October 6, 1998Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 5811582Abstract: Dimethyl-(3-aryl-but-3-enyl)-amine compounds, a method of preparing them, and the use of the compounds as pharmaceutical active ingredients are described.Type: GrantFiled: March 12, 1997Date of Patent: September 22, 1998Assignee: Gruenenthal GmbHInventors: Helmut Heinrich Buschmann, Wolfgang Werner Alfred Strassburger, Elmar Josef Friderichs, Babette-Yvonne Koegel