Nitrogen Attached Directly To The Hetero Ring By Nonionic Bonding Patents (Class 549/68)
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Patent number: 6313302Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, or hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine. These compounds are useful as kappa agonists.Type: GrantFiled: January 26, 2001Date of Patent: November 6, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Patent number: 6310067Abstract: Urocanic acid derivatives useful as antiallergic agents represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R2 denotes hydrogen or lower alkyl, R3 denotes nitro, amino, cyano or COOR2, wherein R2 in said COOR2 is as defined above, and Q denotes carbon or nitrogen.Type: GrantFiled: August 3, 2000Date of Patent: October 30, 2001Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Kazumi Ogata, Kazuhiko Ito, Takahiro Sakaue, Sachiko Inoue, Shinya Ogino
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Publication number: 20010031781Abstract: 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: ApplicationFiled: April 10, 2001Publication date: October 18, 2001Inventors: Carl R. Illig, Nalin L. Subasinghe, James B. Hoffman, Kenneth J. Wilson, M. Jonathan Rudolph, Juan J. Marugan
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Patent number: 6297381Abstract: Disclosed are novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions. Also disclosed are processes of making such compounds.Type: GrantFiled: February 14, 2000Date of Patent: October 2, 2001Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Eugene R. Hickey, John R. Regan
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Patent number: 6291514Abstract: 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: August 11, 1999Date of Patent: September 18, 2001Assignee: 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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Patent number: 6248773Abstract: The invention relates to the use of cyclopentane heptan(ene)oic acid, 2-heteroarylalk(en)yl derivatives as ocular hypotensives.Type: GrantFiled: August 22, 2000Date of Patent: June 19, 2001Assignee: Allergan Sales, Inc.Inventor: Robert M. Burk
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Patent number: 6194449Abstract: The present invention relates to compounds of formulas (IA), (IB), and (IC): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.Type: GrantFiled: May 7, 1999Date of Patent: February 27, 2001Assignee: Medco Corp.Inventor: Pier Giovanni Baraldi
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Patent number: 6166074Abstract: Pharmaceutical compositions which are useful for the treatment of cancer or illnesses which arise due to an abnormally elevated cell proliferation comprise acyl derivatives of aromatic aldehydes, especially arylidene diesters and .alpha.-alkoxyarylidene esters of general formula (I).Type: GrantFiled: October 4, 1996Date of Patent: December 26, 2000Assignee: Norsk Hydro A.S.Inventors: Erik Olai Pettersen, Rolf Olaf Larsen, John Michael Dornish, Bernt B.o slashed.rretzen, Reidar Oftebro, Thomas Ramdahl, Vidar Moen
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Patent number: 6162814Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-.alpha. converting enzyme (TACE, tumor necrosis factor-.alpha.Type: GrantFiled: June 11, 1999Date of Patent: December 19, 2000Assignee: American Cyanamid CompanyInventors: Jeremy Ian Levin, Frances Christy Nelson
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Patent number: 6162823Abstract: The present invention provides compounds having the of the formula I: ##STR1## and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.Type: GrantFiled: March 12, 1997Date of Patent: December 19, 2000Assignee: G.D. Searle & Co.Inventors: Thomas Dale Penning, Stella Siu-tzyy Yu, James Malecha, Chi-Dean Liang, Mark Andrew Russell
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Patent number: 6156788Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: August 9, 1999Date of Patent: December 5, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6156741Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: December 5, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
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Patent number: 6153604Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: November 28, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
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Patent number: 6150397Abstract: The present invention relates to certain 5-aroylnaphthalene derivatives of formula (I): ##STR1## that are inhibitors of prostaglandin G/H synthase, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: June 21, 1999Date of Patent: November 21, 2000Assignee: Syntex (U.S.A.) Inc.Inventors: David Mark Rotstein, Eric Brian Sjogren
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Patent number: 6147063Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: November 14, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
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Patent number: 6136984Abstract: A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds.Type: GrantFiled: April 16, 1997Date of Patent: October 24, 2000Assignee: Novo Nordisk A/SInventor: Florencio Zaragoza D.o slashed.rwald
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Patent number: 6124324Abstract: Novel thiophene-ethyl-thiourea (TET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.Type: GrantFiled: June 23, 1999Date of Patent: September 26, 2000Assignee: Hughes InstituteInventors: Fatih M. Uckun, Taracad K. Ventatachalam
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Patent number: 6037455Abstract: The present invention is directed to novel propoxyphene derivatives which are synthesized for the covalent attachment to antigens (proteins or polypeptides) for the preparation of antibodies or receptors to propoxyphene and propoxyphene metabolites. The resulting novel antigens may be used for the production of antibodies or receptors using standard methods. Once generated, the antibodies or receptors and the novel derivatives which are covalently attached to proteins, polypeptides or labels may be used in the immunoassay process.Type: GrantFiled: November 9, 1992Date of Patent: March 14, 2000Assignee: Biosite Diagnostics IncorporatedInventor: Kenneth F. Buechler
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Patent number: 6037340Abstract: Methods for preparing thiophene and pyrrole-based heterocyclic compounds are disclosed. Also disclosed are libraries of thiophene and pyrrole-based heterocyclic compounds, methods for preparing the libraries of thiophene and pyrrole-based heterocyclic compounds, and methods for using the thiophene and pyrrole-based heterocyclic compounds and compound libraries of the invention. The compounds of the invention have biological activity including anti-cancer activity.Type: GrantFiled: May 28, 1997Date of Patent: March 14, 2000Assignee: Cadus Pharmaceutical CorporationInventors: Arlindo L. Castelhano, Bryan McKibben
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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: 6004724Abstract: New oximsulfonate compounds of the formulae I or II, ##STR1## wherein m is 0 or 1; x is 1 or 2; R.sub.1 is, for example phenyl, which is unsubstituted or substituted or R.sub.1 is a heteroaryl radical that is unsubstituted or substituted, or, if m is 0, R.sub.1 additionally is C.sub.2 -C.sub.6 alkoxycarbonyl, phenoxycarbonyl or CN; R'.sub.1 is for example C.sub.2 -C.sub.12 alkylene, phenylene; R.sub.2 has for example one of the meanings of R.sub.1 ; n is 1 or 2; R.sub.3 is for example C.sub.1 -C.sub.18 alkyl, R'.sub.3 when x is 1, has one of the meanings given for R.sub.3, or R'.sub.3 in the formula IV and when x is 2 in the formula 1, is for example C.sub.2 -C.sub.12 alkylene, phenylene; R.sub.4 and R.sub.5 are independently of each other for example hydrogen, halogen, C.sub.1 -C.sub.6 alkyl; R.sub.6 is for example hydrogen, phenyl; R.sub.7 and R.sub.8 are independently of each other for example hydrogen or C.sub.1 -C.sub.12 -alkyl; R.sub.9 is for example C.sub.1 -C.sub.12 alkyl; A is S, O, NR.sub.Type: GrantFiled: June 25, 1998Date of Patent: December 21, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Hitoshi Yamato, Hartmut Bleier, Jean-Luc Birbaum, Martin Kunz, Kurt Dietliker, Christoph De Leo, Toshikage Asakura
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Patent number: 5994563Abstract: Benzyl-phosphonate compounds represented by the formula I: ##STR1## are disclosed as useful in treating bone wasting diseases and as an immunosuppresant.Type: GrantFiled: January 19, 1999Date of Patent: November 30, 1999Assignee: Ortho Pharmaceutical CorporationInventors: Scott Beers, Roger F. Frechette, Elizabeth A. Malloy, Charles Schwender, Wei Wu
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Patent number: 5942387Abstract: This invention relates to a novel solid phase process for the preparation of thiophene combinatorial libraries. These libraries have use for drug discovery and are used to form wellplate components of novel assay kits.Type: GrantFiled: August 25, 1997Date of Patent: August 24, 1999Assignee: Eli Lilly and CompanyInventor: Sean Patrick Hollinshead
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Patent number: 5888421Type: GrantFiled: September 19, 1994Date of Patent: March 30, 1999Assignee: The Secretary of State for Defence in her Britannic Majesty's Government of the United Kingdom of Great Britain and Northern IrelandInventors: Kenneth Johnson Toyne, John William Goodby, Alexander Seed, George William Gray, Damien Gerad McDonnel, Edward Peter Raynes, Sally Elizabeth Day, Kenneth John Harrison, Michael Hird
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Patent number: 5883106Abstract: 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, and C.sub.1-4 alkyl; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, and amino 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 and C.sub.1-4 alkyl; R.sup.1 and R.sup.2 are each C.sub.Type: GrantFiled: February 6, 1998Date of Patent: March 16, 1999Assignee: Pfizer Inc.Inventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
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Patent number: 5874472Abstract: Compounds of formula (I) and salts, esters and amides thereof, wherein R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.3-6 cycloalkyl group, a thiol group optionally substituted by a C.sub.1-6 alkyl group, or an amino group optionally substituted by one or two alkyl or alkenyl groups; R.sup.2 is H, C.sub.1-7 straight or branched chain alkyl, C.sub.3-6 cycloalkyl, C.sub.2-7 alkenyl or benzyl; A is a 5 or 6 membered aromatic carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or di C.sub.1-6 alkylamino; r is 0, 1 or 2; their use in medicine and in particular for conditions requiring inhibition of the NO Synthase enzyme, pharmaceutical formulations and processes for the preparation thereof are disclosed.Type: GrantFiled: March 18, 1996Date of Patent: February 23, 1999Assignee: Glaxo Wellcome Inc.Inventors: Barry George Shearer, Karl Witold Franzmann, Harold Francis Hodson
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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: 5859300Abstract: A process for the hydrogenation of imines with hydrogen under elevated pressure in the presence of iridium catalysts containing diphosphine ligands, with or without an inert solvent, the reaction mixture containing a soluble ammonium chloride, bromide or iodide or a soluble metal chloride, bromide, or iodide, wherein the reaction mixture additionally contains at least one solid acid with the exception of ion exchangers. Improved optical yields and high chemical conversion rates are achieved while the catalyst is easily separable.Type: GrantFiled: January 26, 1998Date of Patent: January 12, 1999Assignee: Novartis CorporationInventors: Hans-Peter Jalett, Bernd Siebenhaar
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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: 5786379Abstract: Novel pharmaceutically/cosmetically-active adamantyl-substituted biaromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a')-(f'): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: December 2, 1996Date of Patent: July 28, 1998Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 5783597Abstract: 2,5-Disubstituted thiophene derivatives, and more particularly, to 2-aryloxy-5-alkansulfonamido-thiophenes of the general formula: ##STR1## Wherein, R.sub.2 is CF.sub.3, C.sub.1 -C.sub.10 alkyl, or phenyl;X is O, S, or CH.sub.2 ; andR is aryl, C.sub.1 -C.sub.10 alkyl, or C.sub.3 -C.sub.8 cycloalkyl; which compounds are pharmacologically active in alleviating inflammation, asthma, arthritis, hypersensitivity, myocardial ischemia and dermatological conditions, such as, psoriasis and dermatitis, and gastrointestinal inflammatory conditions, such as, inflammatory bowel syndrome.Type: GrantFiled: March 4, 1997Date of Patent: July 21, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Scott Alan Beers, Michael Paul Wachter
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Patent number: 5777089Abstract: Phenol derivatives of the general formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3, X, Y and Z have the meanings stated in the description, are used in particular in nonlinear optics.Type: GrantFiled: October 15, 1996Date of Patent: July 7, 1998Assignee: BASF AktiengesellschaftInventors: Stefan Beckmann, Karl-Heinz Etzbach, Rudiger Sens
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Patent number: 5776859Abstract: The present invention discloses novel sodium channel active compounds, processes for making such compounds, and the use of such compounds as local anesthetics and pesticides.Type: GrantFiled: November 15, 1995Date of Patent: July 7, 1998Inventor: Alfred A. Nickel
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Patent number: 5773463Abstract: This invention describes the use of aminoindane and amino-tetrahydronaphthalene derivatives of general formula (I) ##STR1## in which Ar, X, R.sub.1, R.sub.2 and n are defined in claim 1, for the manufacture of a medicament for the treatment of disorders in which a calcium channel antagonist is indicated. Novel compounds falling within formula (I) are also claimed.Type: GrantFiled: January 22, 1996Date of Patent: June 30, 1998Assignee: SmithKline Beecham p.l.c.Inventors: John David Harling, Barry Sidney Orlek
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Patent number: 5756753Abstract: Naphthalene derivatives of the formula ##STR1## where the rings A and B may be benzofused,X is nitrogen or a radical of the formula CH or CH.dbd.CH--CH,Z is a heterocyclic radical or additionally, when x is CH.dbd.CH--CH, a 5- or 6-membered aromatic carbocyclic radical, andR.sup.1, R.sup.2 and R.sup.3 are hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.5 -C.sub.7 -cycloalkyl, are useful in nonlinear optics.Type: GrantFiled: December 24, 1996Date of Patent: May 26, 1998Assignee: BASF AktiengesellschaftInventors: Stefan Beckmann, Karl-Heinz Etzbach, Rudiger Sens
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Patent number: 5753239Abstract: Bi-aromatic compounds are provided along with methods for their preparation and use.Type: GrantFiled: June 6, 1995Date of Patent: May 19, 1998Assignee: Centre International de Recherches Dematologiques Galderma (Cird Galderma)Inventors: Jean-Philippe Rocher, Jean-Michel Bernardon
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Patent number: 5739140Abstract: Novel compounds of Formula I and methods of making and using the compounds which are useful as fungicides, particularly in the agricultural field: ##STR1## wherein C.sub.1 and C.sub.2 are carbon atoms which are part of an aromatic ring; W is alkoxyimino, alkoxymethylene or alkylthiomethylene; R.sub.1 is independently selected from the group consisting of halogen, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, wherein the alkyl or alkoxy are optionally substituted by halogen, and p is 0, 1, or 2; Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, NR.sub.2 wherein R.sub.2 is hydrogen or a lower aliphatic group, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 S(O)--, --OCH.sub.2 --, --SCH.sub.2 --, --S(O)CH.sub.2 --, --CH.sub.2 ON.dbd.C(R.sub.3)-- or --CH.dbd.NB wherein B is --O--CO--, --N.dbd.CR.sub.3, or --CR.sub.3 R.sub.4 -- wherein R.sub.3 and R.sub.4 are independently hydrogen or C.sub.1 -C.sub.Type: GrantFiled: October 23, 1996Date of Patent: April 14, 1998Assignee: Monsanto CompanyInventors: William P. Clinton, Jim I. McLoughlin, Anita E. Otal, John J. Parlow, Dennis P. Phillion, Ajit S. Shah
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Patent number: 5723648Abstract: Novel 4-oxoquinoline-3-carboxylic acid compounds of the formula: ##STR1## wherein R.sup.1 is cyclopropyl which may have 1 to 3 substituents of alkyl and halogen; phenyl which may be substituted by 1 to 3 substituents of alkoxy, halogen and OH; alkyl which may be substituted by halogen, alkanoyloxy or OH; alkenyl; or thienyl, R.sup.2 is 5- to 9-membered saturated or unsaturated heterocyclic ring which may be sustituted, R.sup.3 is alkyl, R is H or alkyl, and X is halogen, and pharmaceutically acceptable salts thereof, said compounds having excellent antimicrobial activity and hence being useful as an antimicrobial agent, and a pharmaceutical composition containing said compound as an active ingredient.Type: GrantFiled: July 5, 1996Date of Patent: March 3, 1998Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Hiraki Ueda, Hisashi Miyamoto, Hiroshi Yamashita, Hitoshi Tone
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Patent number: 5714605Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: October 10, 1995Date of Patent: February 3, 1998Assignees: Monsanto Company, G. D. SearleInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5712393Abstract: The present invention provides a compound of formula (1) ##STR1## in which: R.sub.4 represents a hydrogen atom, a halogen atom or a nitro group;R.sub.6 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.6) alkyl group;R.sub.7 represents a chlorine atom or a hydroxyl group; andZ represents: a phenyl group optionally substituted with one or more halogen atoms, straight or branched (C.sub.1 -C.sub.4)alkyl groups, straight or branched (C.sub.1 -C.sub.4)alkoxy groups, or trifluoromethyl, formyl, --CH.sub.2 OR, --CH.sub.2 OCOR, --CH.sub.2 CONRR', --CH.sub.2 ONCOR, --COOR, nitro, --NHR, --NRR' or --NHCOR groups, wherein R and R' are each, independently, a hydrogen atom or a (C.sub.1 -C.sub.7) alkyl group; a heterocyclic group optionally substituted as defined above for phenyl; or a cyclo(C.sub.5 -C.sub.8)alkyl group; additionally, when R.sub.Type: GrantFiled: November 24, 1995Date of Patent: January 27, 1998Assignee: SynthelaboInventors: Jean Michel Altenburger, Gilbert Lassalle
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Patent number: 5710173Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.Type: GrantFiled: June 7, 1995Date of Patent: January 20, 1998Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Asaad S. Nematalla, Gerald McMahon
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Patent number: 5708178Abstract: Novel acceptor-donor-acceptor and donor-acceptor-donor compounds for use in forming a thermally-stable electro-optic waveguide are disclosed. Also disclosed is a thermally stable waveguide material containing thermally stable acceptor-donor-acceptor or donor-acceptor-donor guest dipole compounds in a temperature-resistant polymer matrix. The waveguide has selected regions in which the net dipoles of the guest molecules are oriented, for electro-optic switching when an electric field is placed across these regions.Type: GrantFiled: September 20, 1996Date of Patent: January 13, 1998Assignee: Lockheed Martin CorporationInventors: Susan P. Ermer, Doris S. Y. Leung, Steven M. Lovejoy
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Patent number: 5681966Abstract: Enantiomerically enriched disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes 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.It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.Type: GrantFiled: June 7, 1995Date of Patent: October 28, 1997Assignee: Cytomed, Inc.Inventors: Xiong Cai, Gurmit Grewal, Sajjat Hussoin, Aberra Fura, Ralph Scannell, Tesfaye Biftu
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Patent number: 5679800Abstract: Compounds of the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are as defined in the specification and R.sub.3 is amino or --N.dbd.N--K, wherein K is a coupling component radical. The compounds wherein R.sub.3 is --N.dbd.N--K are useful as disperse dyes, and those wherein it is amino are useful as intermediates in the synthesis of those wherein it is --N.dbd.N--K.Type: GrantFiled: July 15, 1992Date of Patent: October 21, 1997Assignee: Clariant Finance (BVI) LimitedInventors: Robert Egli, Beat Henzi
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Patent number: 5648486Abstract: 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: May 12, 1993Date of Patent: July 15, 1997Assignee: CytoMed, Inc.Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
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Patent number: 5612483Abstract: Nitro-substituted aromatics can be directly aminated with amines in the presence of simple bases and oxygen.Type: GrantFiled: September 6, 1995Date of Patent: March 18, 1997Assignee: Bayer AktiengesellschaftInventor: Manfred Jautelat
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Patent number: 5602119Abstract: Succinoylamino hydroxyethylamino sulfamic acid derivative compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: January 31, 1995Date of Patent: February 11, 1997Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 5583132Abstract: Sulfonylalkanoylamino hydroxyethylamino sulfamic acid compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: February 2, 1995Date of Patent: December 10, 1996Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 5571810Abstract: This invention relates to new thiophene derivatives having antiinflammatory and analgesic activities and represented by the general formula [I]: ##STR1## wherein R.sup.1 is hydrogen, halogen, cyano, substituted lower alkyl, substituted or unsubstituted lower alkenyl, acyl, nitro, substituted or unsubstituted amino, sulfo, substituted or unsubstituted sulfamoyl, N-containing heterocyclicsulfonyl, hydoxy, substituted or unsubstituted heterocyclic group,R.sup.2 is substituted or unsubstituted aryl, andR.sup.3 is substituted or unsubstituted aryl, provided that R.sup.3 is aryl substituted with substituent(s) selected from the group consisting of amino, mono(lower)-alkylamino, acylamino, lower alkyl(acyl)amino and sulfamoyl when R.sup.1 is hydrogen, halogen or cyano, and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: April 13, 1995Date of Patent: November 5, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Kiyoshi Tsuji, Nobukiyo Konishi, Katsuya Nakamura
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Patent number: 5567723Abstract: Compounds having the structural formula ##STR1## wherein R is C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkyl; R.sup.1 is fluorenyl, thienyl, pyridyl or thiazolyl, unsubstituted or substituted by one or more substituents selected from C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylthio, halogen, C.sub.1 -C.sub.4 haloalkyl and nitro; and R.sup.2 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.2 -C.sub.6 alkoxyalkyl. The compounds of this invention are effective for controlling mites and nematodes.Type: GrantFiled: July 5, 1995Date of Patent: October 22, 1996Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd./LteeInventors: Mark A. Dekeyser, Derek J. McPhee, Paul T. McDonald