Chalcogen Attached Indirectly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/186)
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Patent number: 6174908Abstract: Certain thiazolidinone and metathiazanone compounds, as described, are useful as potassium channel inhibitors and are especially useful for the treatment of cardiac arrhythmias and other diseases, conditions and disorders.Type: GrantFiled: May 1, 1999Date of Patent: January 16, 2001Assignees: ICAGen, Inc., Eli Lilly & Company Lilly Corporate CenterInventors: Michael F. Gross, Neil A. Castle, Jose S. Mendoza
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Patent number: 6159995Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
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Patent number: 6124467Abstract: The invention relates to a new process for the preparation of dithiazolyl-(2,2')-disulfides by oxidation of 2-mercaptothiazoles, to the dithiazolyl-(2,2')-disulfides that can be obtained in this way, and to the use thereof.Type: GrantFiled: December 3, 1999Date of Patent: September 26, 2000Assignee: Bayer AktiengesellschaftInventors: Wilfried Nolte, Heinrich Konigshofen, Adolf Sicheneder
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Patent number: 6121201Abstract: A compound represented by the formula (I) or its salt and herbicidal and desiccant use thereof: ##STR1## wherein X, Y are independently hydrogen, halogen, cyano, nitro, or (C.sub.Type: GrantFiled: September 23, 1998Date of Patent: September 19, 2000Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: David A. Pulman, Bai-Ping Ying, Shao-Yong Wu, Sandeep Gupta, Masamitsu Tsukamoto, Takahiro Haga
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Patent number: 6110946Abstract: There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl,R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl,R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl,R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, andR.sub.6, independently of R.sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.Type: GrantFiled: July 1, 1998Date of Patent: August 29, 2000Assignee: Novartis Finance CorporationInventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
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Patent number: 6107491Abstract: Diketopyrrolopyrroles of formula I ##STR1## wherein R.sub.1 is a radical of formula II--Y--X--Z--Q (II),whereinY is --CR.sub.3 R.sub.4, --SO.sub.2 --, --CO--, --Si(Hal).sub.2 --, --POHal--, wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen or C.sub.1 -C.sub.4 alkyl, and Hal is halogen,X is an unsubstituted or substituted carbocylic or heterocyclic arylene group,Z is a single bond, uninterrupted linear or branched C.sub.1 -C.sub.30 alkylene, or linear or branched C.sub.2 -C.sub.30 alkylene which is interrupted once or more than once by a hetero atom, --CH.dbd.CH--,--C.tbd.C--, --N.dbd.CH--, --CH.dbd.N-- or --NH--, or is C.sub.5 -C.sub.12 cycloalkylene,Q is a polyreactive functional group, andR.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR2## or R.sub.1, and R.sub.7 is hydrogen or C.sub.1 -C.sub.Type: GrantFiled: January 26, 1999Date of Patent: August 22, 2000Assignee: Ciba Specialty Chemicals CorporationInventor: Sameer Eldin
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Patent number: 6096898Abstract: One pot synthesis of 1,2,4-triazoles uses thioimidate intermediate and 1,2-dichloroethane solvent.Type: GrantFiled: October 22, 1999Date of Patent: August 1, 2000Assignee: Dow AgroSciences LLCInventors: David E. Podhorez, John W. Hull, Jr., Christine H. Brady
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Patent number: 6080772Abstract: The present invention relates to thiazole containing compounds capable of inhibiting protein tyrosine phosphatase activity. The invention further relates to the use of such compounds to modulate or regulate signal transduction by inhibiting protein tyrosine phosphatase activity. Finally, the invention relates to the use of such compounds to treat various disease states including diabetes mellitus.Type: GrantFiled: December 11, 1997Date of Patent: June 27, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, John Yudhistir Ramphal, G. Davis Harris, Jr., Asaad S. Nematalla
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Patent number: 6063799Abstract: The instant invention provides novel crystalline Form II of (.+-.)-5-{[3,5-bis(1,1dimethylethyl)-4-hydroxyphenyl]methyl}-4-thiazolidin one having an x-ray powder diffraction patter with specific d spacings useful for treating inflammation, inflammatory bowel disease, allergies, arthritis and hypoglycemia utilizing the novel physical form as well as pharmaceutical compositions containing the same. A process for preparing Form II Tazofelone is described.Type: GrantFiled: February 25, 1998Date of Patent: May 16, 2000Assignee: Eli Lilly and CompanyInventors: Marvin M Hansen, Allen R Harkness, Susan M Reutzel
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Patent number: 6063800Abstract: The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 --A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.Type: GrantFiled: February 19, 1999Date of Patent: May 16, 2000Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
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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: 6057349Abstract: The present invention concerns novel compounds represented by the Formula: ##STR1## wherein: A is R.sup.1.sub.q (R.sup.3 R.sup.60 N).sub.m (Z)(NR.sup.2).sub.n ; m and q are each 0 or 1, with the proviso that when q is 1, m is 0 and when q is 0, m is 1; Z is C.dbd.O or SO.sub.2 ; n is 1 with the proviso that, when Z is C.dbd.O, m is 1; X is --NH--, --CH.sub.2 --, or --OCH.sub.2 --; Y is [2-imidazoline, 2-oxazolin] 2-thiazoline, [or 4-imidazole] R.sup.1 is H, lower alkyl, or phenyl, with the proviso that, when R.sup.1 is H, m is 1; R.sup.2, R.sup.3, R.sup.60 are each independently H, lower alkyl, or phenyl; R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are each independently hydrogen, lower alkyl, --CF.sub.3, lower alkoxy, halogen, phenyl, lower alkeny, hydroxyl, lower alkylsulfonamido, or lower cycloalkyl, wherein R.sup.2 and R.sup.Type: GrantFiled: March 8, 1999Date of Patent: May 2, 2000Assignee: F. Hoffman La Roche AGInventors: Richard Leo Cournoyer, Paul Francis Keitz, Counde O'Yang, Dennis Mitsugu Yasuda
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Patent number: 6054623Abstract: A method for the preparation of hydroxythiol compounds by reacting a hydroxyl-protected halide compound having the structure:X--R--OPgwith magnesium in a Grignard-suitable solvent to form a hydroxyl-protected magnesium halide compound, wherein R is selected from substituted or unsubstituted aliphatic radicals, substituted or unsubstituted cyclic aliphatic radicals, substituted or unsubstituted aromatic radicals, substituted or unsubstituted araliphatic radicals and substituted or unsubstituted heterocyclic radicals; Pg is a protecting group; and X is selected from the group consisting of F, Cl, Br and I; then reacting said hydroxyl-protected magnesium halide compound with sulfur in the Grignard-suitable solvent to form a hydroxyl-protected thiomagnesium halide compound; and hydrolyzing the protected hydroxyl group to form a hydroxythiomagnesium halide compound and converting the thiomagnesium halide to a thiol; wherein the protecting group is selected so that species formed by the de-protection of the protectType: GrantFiled: December 18, 1998Date of Patent: April 25, 2000Assignee: AlliedSignal Inc.Inventors: David Ryckman, Mingbao Zhang, Guohua Chen
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Patent number: 6025497Abstract: 5-Chloro-2-(4,4-difluorobutenylthio)thiazole is prepared from 2-mercaptothiazole by a multistep process involving S-alkylation, chlorination and dehydrochlorination and is converted by oxidation to the corresponding sulfone which is useful as an agricultural nematicide.Type: GrantFiled: April 23, 1998Date of Patent: February 15, 2000Assignee: Zeneca LimitedInventors: Martin Charles Bowden, Stephen Martin Brown
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Patent number: 6013649Abstract: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfone inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.Type: GrantFiled: July 22, 1997Date of Patent: January 11, 2000Assignee: Monsanto CompanyInventors: John N. Freskos, S. Zaheer Abbas, Gary A. DeCrescenzo, Daniel P. Getman, Robert M. Heintz, Brent V. Mischke, Joseph J. McDonald
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Patent number: 6005142Abstract: The instant invention provides a novel process for preparing benzyl-substituted rhodanine derivatives. Also provided are novel benzyl-substituted thiolamides and benzyl-substituted hemithioacetals. Such compounds are useful as intermediates in preparing the compounds by the process of the instant invention.Type: GrantFiled: February 25, 1998Date of Patent: December 21, 1999Assignee: Eli Lilly and CompanyInventors: James D Copp, Francis O Ginah, Marvin M. Hansen
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Patent number: 5998452Abstract: The present invention is directed to a compound represented by formula (I): wherein, for example, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 each represents a hydrogen atom; R.sub.6 and R.sub.7 each represent a substituted or unsubstituted lower alkyl group; A represents a group represented by formula (II): ##STR1## wherein R.sub.5 represents, for example, a hydrogen atom; and n represents an integer of 2 to 6, or a stereoisomer or optical isomer thereof and a pharmaceutically acceptable salt thereof and compositions and methods for treating ischemic diseases. The compounds represented by formula (I) have an inhibitory action on calcium overload in addition to a vasorelaxing activity (calcium antagonism) and an inhibitory action on lipid peroxidation and are useful as a preventive or treating agent for ischemic diseases and hypertension.Type: GrantFiled: October 7, 1997Date of Patent: December 7, 1999Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Nobuhiro Ohi, Tatsuya Kato, Tomokazu Ozaki, Kazuhiko Tamura, Yoshiyuki Suzuki, Michitaka Akima
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Patent number: 5990135Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: May 31, 1995Date of Patent: November 23, 1999Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing Leung Sham, Dale J. Kempf, Chen Zhao
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Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
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Patent number: 5919944Abstract: Diketopyrrolopyrroles of formula I ##STR1## wherein R.sub.1 is a radical of formula II--Y--X--Z--Q (II),whereinY is --CR.sub.3 R.sub.4, --SO.sub.2 --, --CO--, --Si(Hal).sub.2 --, --POHal--, wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen or C.sub.1 -C.sub.4 alkyl, and Hal is halogen,X is an unsubstituted or substituted carbocylic or heterocyclic arylene group, Z is a single bond, uninterrupted linear or branched C.sub.1 -C.sub.30 alkylene, or linear or branched C.sub.2 -C.sub.30 alkylene which is interrupted once or more than once by a hetero atom, --CH.dbd.CH--, --C.tbd.C--, --N.dbd.CH--, --CH.dbd.N-- or --NH--, or is C.sub.5 -C.sub.12 cycloalkylene,Q is a polyreactive functional group, andR.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR2## or R.sub.1, and R.sub.7 is hydrogen or C.sub.1 -C.sub.Type: GrantFiled: July 20, 1998Date of Patent: July 6, 1999Assignee: Ciba Specialty Chemicals CorporationInventor: Sameer Eldin
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Patent number: 5914328Abstract: Novel heterocyclic ether compounds of the formula: ##STR1## wherein *, A,B, n, R.sup.1, R.sup.2 and X are specifically defined, or pharmaceutically-acceptable salts or prodrugs thereof, which are useful in selectively activating or inhibiting neurotransmitter release; to therapeutically-effective pharmaceutical compositions of these compounds; and to the use of said compositions to activate or inhibit neurotransmitter release in mammals.Type: GrantFiled: June 7, 1995Date of Patent: June 22, 1999Assignee: Abbott LaboratoriesInventors: Nan-Horng Lin, Mark W. Holladay, Melwyn A. Abreo, David E. Gunn, Suzanne A. Lebold, Richard L. Elliott, Yun He
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Patent number: 5905158Abstract: The invention relates to novel UVB/UVA-absorbing chromophores that are present in the natural products of a marine hydroid, and derivatives thereof, useful as sunscreening agents. Furthermore, the present invention relates to methods for protecting skin from the damaging effects of solar ultraviolet radiation. This method comprises topically applying to the skin an effective coating of a sunscreen composition of the present invention. Additional embodiments of the invention use these natural UV-absorbing compounds, or derivative thereof, as additives as a means of providing UV-protective plastics, paints, and waxes.Type: GrantFiled: September 12, 1997Date of Patent: May 18, 1999Inventor: Niels L. Lindquist
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Patent number: 5900427Abstract: This invention relates to the use of heteroarenesulfonyl groups as protecting groups for amino groups, particularly the amino groups of amino acids, and specifically to nitrogen-protected (N-protected) amino acid reagents, which are particularly well-suited for use in peptide syntheses. In particular, the N-protected amino acid reagent is an N-heteroarenesulfonyl-protected amino acid halide. The heteroarenesulfonyl protecting groups are readily removed under relatively mild conditions.Type: GrantFiled: May 3, 1996Date of Patent: May 4, 1999Assignee: Wisconsin Alumni Research FoundationInventors: Edwin Vedejs, Jiabing Wang, Shouzhong Lin, Artis Klapars
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Patent number: 5859036Abstract: The present invention relates to derivatives of formula ##STR1## and to their use in therapeutics especially as drugs with anti-inflammatory and analgesic properties.Type: GrantFiled: October 31, 1997Date of Patent: January 12, 1999Assignee: Laboratories UPSAInventors: Eric Sartori, Jean-Marie Teulon
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Patent number: 5849921Abstract: Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo?1,2-a!pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-?(2-ethyl-4-methyl-6-(5,6,7,8-tetrahydroimidazo?1,2-a!pyridin-2-yl)-ben zimidazol-1-yl)-methyl!-biphenyl-2-carboxylic acid.Type: GrantFiled: June 2, 1995Date of Patent: December 15, 1998Assignee: Astra AktiebolagInventors: Robin Bernad Boar, Alan John Cross, Duncan Alastair Gray, Richard Alfred Green
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Patent number: 5789408Abstract: Compounds of formula (I) are active antiviral compounds useful in the treatment of viral infections in mammals. The compounds of the invention are readily prepared by reaction of a suitable 2-thiothiazole derivative with an appropriate Het-(CH.sub.2).sub.n -halide.Type: GrantFiled: January 11, 1996Date of Patent: August 4, 1998Assignee: Pfizer Inc.Inventors: Edward Fox Kleinman, Hiroko Masamune, Vinod Dipak Parikh
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Patent number: 5777127Abstract: Disclosed is a novel near-infrared absorbing dye of formula: ##STR1## wherein X.sup.1, x.sup.2 independently represents --CR.sup.8 R.sup.9 --, --S--, --Se--, --NR.sup.10 --, --CH.dbd.CH-- or --O--;n is an integer of 2 or 3;R.sup.1 and R.sup.2 independently represent alkyl of 1 to 10 carbons or substituted alkyl of 1 to 10 carbons;R.sup.3 represents a ring chosen from a set consisting of aryl, substituted aryl, and a heterocyclic ring of a type present in photographic emulsions;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently represent hydrogen, alkyl of 1-10 carbons, substituted alkyl of 1-10 carbons, R.sup.4 and R.sup.5 taken together or R.sup.6 and R.sup.7 taken together can represent atoms necessary to form a 5 or 6-membered aliphatic ring, an aromatic six-membered ring, an aromatic 10-membered ring, a substituted aromatic six-member ring or a substituted aromatic 10-member ring;R.sup.8, R.sup.Type: GrantFiled: October 18, 1996Date of Patent: July 7, 1998Assignee: Sterling Diagnostic Imaging, Inc.Inventors: Dietrich Max Fabricius, Gregory Charles Weed
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Patent number: 5750712Abstract: A class of novenl compounds represented by the formula (I) ##STR1## wherein R.sub.1 s are the same or different groups and each represents hydrogen atom or alkyl group having 1 to 4 carbon atoms; R.sub.2 is phenyl group, naphthyl group, or either phenyl or naphthyl substituted with at least one hydroxyl, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms; R.sub.3 is hydrogen atom, alkyl group having 1 to 4 carbon atoms or CH.sub.2 COOR.sub.4 group, in which R.sub.4 is hydrogen atom or alkyl group having 1 to 12 carbon atoms; n is 0 or 1, the configuration of 5-methylene group includes both E-isomer and Z-isomer, providing excepting the case wherein R.sub.1 is hydrogen or methyl, R.sub.2 is 3,5-di-t-butyl-4-hydroxyphenyl, R.sub.3 is hydrogen and n is 0 or pharmacologically acceptable salts thereof when R.sub.3 or R.sub.4 is hydrogen atomThe invention also concerns preparation methods thereof.Type: GrantFiled: June 21, 1995Date of Patent: May 12, 1998Inventors: Fumio Yoneda, Mayumi Watanabe, Masatoshi Sakae, Masanori Katsurada, Takaaki Sabato
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Patent number: 5739346Abstract: This invention relates to reactive derivatives of 2-(2-aminothiazol-4-yl)-2-methoxyimino acetic acid and 1H-tetrazol-1-acetic acid of the following general formula I, ##STR1## wherein R.sub.3 = ##STR2## as well as to use thereof in the manufacture of cephalosporin antibiotics such as cefotaxime, ceftriaxone and cefazolin.Type: GrantFiled: March 26, 1996Date of Patent: April 14, 1998Assignee: Lupin Laboratories LimitedInventors: Debashish Datta, Vinod George, Bishwa Prakash Rai
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Patent number: 5728696Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.Type: GrantFiled: June 5, 1995Date of Patent: March 17, 1998Assignee: Hoechst AktiengesellschaftInventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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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: 5675023Abstract: The present invention relates to a chromone derivative and an aldose reductase inhibitor comprising said compound as efective component, which is represented by the following formula: ##STR1## wherein R.sub.1 and R.sub.2 each represent a lower alkyl group, etc., R.sub.3 represents an oxygen atom, a sulfur atom, etc., R.sub.7 represents a phenyl group substituted or not substituted, etc., and R represents a hydrogen atom or a lower alkoxy group. The present compounds exhibit superior inhititory action on aldose reductase and are useful for the treatment of various complications of diseases in diabetes, such as cataract, retinopathy, keratopathy, nephropathy, and neuropathy.Type: GrantFiled: June 6, 1995Date of Patent: October 7, 1997Assignee: Tsumura & Co.Inventors: Yasushi Igarashi, Takuji Yamaguchi, Yoshimitsu Ogawa, Mika Tomita, Hiroko Hayashi, Toshitsugu Sato, Kunio Hosaka
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Patent number: 5663185Abstract: Heteroaromatic compounds of the formulae IA and IB ##STR1## where the dashed line is a double bond between the carbon atom and a Z atom, and the index and the substituents have the following meanings:R.sup.1alkyl, alkoxy, alkylaminoR.sup.2alkyl;Aa direct bond; alkylene, alkenylene, alkynylene; O, S, S-oxides, N and alkylene derivatives or oxime radicals thereofBhydrogen, halogen,alkyl, alkenyl, alkynyl; cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, aryl, hetarylUCH.sub.2, CHCl, CHR.sup.2 or NOR.sup.2 ;Xhydrogen, cyano, nitro, halogen,alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, hetaryl; oxi- and thio derivatives thereof, carbonyl derivatives thereof, carbonyloxy derivatives thereof, amino derivatives thereof, oxime derivatives thereof,amino which may bear one or two of the abovementioned groups;m1 or 2,Yoxygen or sulfur;Z.sup.1 -Z.sup.2, Z.sub.3 -Z.sub.Type: GrantFiled: March 20, 1995Date of Patent: September 2, 1997Assignee: BASF AktiengesellschaftInventors: Bernd Mueller, Hubert Sauter, Horst Wingert, Hartmann Koenig, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5633272Abstract: A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydroxyl, lower alkyl, carboxyl, lower carboxyalkyl, lower aminocarbonylalkyl, lower alkoxycarbonylalkyl, lower aralkyl, lower alkoxyalkyl, lower aralkoxyalkyl, lower alkylthioalkyl, lower aralkylthioalkyl, lower alkylaminoalkyl, lower aryloxyalkyl, lower arylthioalkyl, lower haloalkyl, lower hydroxylalkyl, cycloalkyl, cycloalkylalkyl, and aralkyl; wherein R.sup.3 is selected from cycloalkyl, cycloalkenyl, aryl, and heteroaryl; wherein R.sup.Type: GrantFiled: June 7, 1995Date of Patent: May 27, 1997Inventors: John J. Talley, David L. Brown, Srinivasan Nagarajan, Jeffery S. Carter, Richard M. Weier, Michael A. Stealey, Paul W. Collins, Roland S. Rogers, deceased, Karen Seibert
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Patent number: 5631376Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: May 31, 1995Date of Patent: May 20, 1997Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
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Patent number: 5614544Abstract: [Object]To provide a new 2,4-oxazolidinedione derivative possessing excellent hypoglycemic and hypolipidemic activities.[Constituent]A 2,4-oxazolidinedione derivative represented by the general formula: ##STR1## wherein X represents --CH.sub.2 --, --C(.dbd.O)--, --CH(OH)--, --C(.dbd.NOH)-- or --CH.dbd.CH--; R represents a hydrocarbon residue or heterocyclic group which may be substituted; n represents an integer from 0 to 5, and m represents an integer from 1 to 3; ....... represents a single or double bond; provided that n is an integer from 1 to 5 when X is --C(.dbd.O)--, or a pharmacologically acceptable salt thereof.Type: GrantFiled: September 8, 1994Date of Patent: March 25, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Hitoshi Ikeda, Yu Momose
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Patent number: 5599825Abstract: There are provided methine compounds having the following structure and their analogs, with a high solubility and are usefull as an active ingredient for pharmaceutical composition for treatment of cancer: ##STR1##Type: GrantFiled: April 12, 1995Date of Patent: February 4, 1997Assignee: Fuji Photo Film Co., Ltd.Inventors: Noriaki Tatsuta, Akihiko Okegawa, Masayuki Kawakami, Keizo Koya
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Patent number: 5591862Abstract: Novel tetrazole derivatives represented by the formula ##STR1## wherein n denotes an integer of 1 to 3; A is an optionally substituted heterocyclic residue; Y is a divalent hydrocarbon residue; and X is CH or N, or pharmaceutically acceptable salts thereof have excellent hypoglycemic and hypolipidemic activities.Type: GrantFiled: June 8, 1994Date of Patent: January 7, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Hitoshi Ikeda, Yu Momose
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Patent number: 5563277Abstract: The instant invention provides a novel process for preparing benzyl-substituted rhodanine derivatives. The process is particularly useful for synthesizing the enantiomers of such derivatives. Also provided are novel benzyl-substituted mercaptopropanoic acids and benzyl-substituted thiazolidinones. Such compounds are useful for treating inflammatory bowel disease and, accordingly, the present invention provides a method of treating inflammatory bowel disease in mammals utilizing such novel compounds as well as pharmaceutical compositions containing same.Type: GrantFiled: December 21, 1994Date of Patent: October 8, 1996Assignee: Eli Lilly and CompanyInventors: Marvin M. Hansen, Allen R. Harkness, Michael J. Martinelli, Vien V. Khau
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Patent number: 5519040Abstract: The present invention provides novel carbonic anhydrase inhibitors represented by the structural formula: ##STR1## whereinType: GrantFiled: April 29, 1994Date of Patent: May 21, 1996Assignee: AllerganInventors: Ken Chow, Michael E. Garst, Judith M. Holmes
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Patent number: 5512679Abstract: 2-aryl-ethane-sulphonic acids of the formulaAr.sup.1 --CH.sub.2 --CH.sub.2 --SO.sub.3 H (I),in whichAr.sup.1 denotes a carbocyclic or heterocyclic aromatic radical which can be bound to an anellated benzene nucleus,can be obtained by reaction of the underlying vinyl aromatic compound with sulphurous acid, if the reaction is carried out in the presence of an amine of the formulaN(R.sup.1,R.sup.2,R.sup.3 (III),in whichR.sup.1, R.sup.2 and R.sup.3 have the meaning mentioned in the description.Type: GrantFiled: September 8, 1994Date of Patent: April 30, 1996Assignee: Bayer AktiengesellschaftInventors: Jurgen-Dietrich Meier, Christian Munster, Volker Kass, Horst Siffrin
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Patent number: 5498719Abstract: The present invention provides a novel synthetic route to a key precursor, i.e., an (S,S)-.alpha.-fluoro-2,2-dimethyl-1,3-dioxolane-4-propanoic acid ester useful in the preparation of FddA and FddC. The instant diastereoselective process utilizes a novel intermediate which contains a chiral auxiliary. The chiral auxiliary can be any chiral auxiliary moiety such as for example an auxiliary containing a substituted oxazolidinone group. The intermediate containing the chiral auxiliary is fluorinated utilizing a fluorination method applied for the first time in the synthesis of fluorinated sugars to give a fluorinated intermediate which after removal of the chiral group provides the desired key intermediate. In summary, in the instant process, a fluorine is introduced diastereoselectively into an intermediate via the reaction of a chiral enolate with an electrophilic fluorinating agent and the intermediate which is fluorinated is derived from mannitol.Type: GrantFiled: January 31, 1994Date of Patent: March 12, 1996Assignee: The United States of America as represented by the Secretary of the Department of Health & Human ServicesInventors: Victor E. Marquez, John S. Driscoll, Magbool A. Siddiqui
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Patent number: 5492925Abstract: There are provided thienyl- and furylpyrrole compounds of formula I ##STR1## and their use for the control of insects and acarina. Further provided are compositions and methods comprising those compounds for the protection of plants from attack by insects and acarina.Type: GrantFiled: August 31, 1993Date of Patent: February 20, 1996Assignee: American Cyanamid CompanyInventors: Roger W. Addor, Joseph A. Furch, III, Laurelee A. Duncan, Jack K. Siddens, deceased
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Patent number: 5472965Abstract: A novel imidazole derivatives of formula I: ##STR1## wherein R.sup.1 is hydrogen, alkyl, halogen, or optionally substituted aryl; R.sup.2 is alkyl, optionally substituted aryl optionally substituted aralkyl, or optionally substituted hetero ring group; R.sup.3 is hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl, or optionally substituted hydroxyalkyl; R.sup.4 is hydrogen, alkyl, halogen, acyl, optionally substituted hydroxyalkyl, optionally esterified or amidated carboxyl group, hydroxy group, aryl or arylthio; X is S, SO, SO.sub.2, CH.sub.2, or Se; n is an integer of 1 to 3, or a pharmaceutically acceptable salt thereof, said derivative having anti-HIV activity and being useful for the treatment of HIV infections.Type: GrantFiled: March 14, 1994Date of Patent: December 5, 1995Assignee: Shionogi & Co., Ltd.Inventors: Hirohiko Sugimoto, Masaru Ogata, Hiroshi Matsumoto, Ken-ichi Sugita, Akihiko Sato, Tamio Fujiwara
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Patent number: 5461067Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed wherein R.sub.1, R.sub.2, R.sub.5, R.sub.6, Y.sub.m and Y'.sub.n are herein defined.Type: GrantFiled: February 1, 1994Date of Patent: October 24, 1995Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
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Patent number: 5459144Abstract: The invention relates to compounds of the formula ##STR1## wherein Z, X, Q, Y, W, and W' are as described herein. These compounds have antiviral activity, and certain of these compounds have antiinflammatory activity and are PAF inhibitors.Type: GrantFiled: December 17, 1993Date of Patent: October 17, 1995Assignee: Schering CorporationInventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace
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Patent number: 5457125Abstract: The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 is hydrogen, (1-4C)alkyl, halogeno-(2-4C)alkyl, hydroxy-(2-4C)alkyl, cyano-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl;R.sup.5 is hydrogen, (1-4C)alkyl, halogeno-(2-4C)alkyl, hydroxy-(2-4C)alkyl, cyano-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl, or a heteroaryl moiety selected from pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, furyl, thienyl, oxazolyl and thiazolyl;A.sup.4 is (1-4C)alkylene;Ar.sup.1 is phenylene, pyridinediyl or pyrimidinediyl;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl or thiazolediyl;R.sup.1 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- wherein each of A.sup.2 and A.sup.3 is independently (1-3C)alkylene and X.sup.Type: GrantFiled: August 19, 1994Date of Patent: October 10, 1995Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Philip N. Edwards, Michael S. Large
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Patent number: 5420289Abstract: This invention relates to substituted indole derivatives possessing lipoxygenase inhibitory, phospholipase A.sub.2 inhibitory and leukotriene antagonist activity, which are useful as anti-inflammatory, antiallergic and cytoprotective agents.Type: GrantFiled: March 10, 1993Date of Patent: May 30, 1995Assignee: American Home Products CorporationInventors: John H. Musser, Anthony F. Kreft, III, Amedeo A. Failli, Christopher A. Demerson, Uresh S. Shah, James A. Nelson
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Patent number: 5395845Abstract: In all possible stereoisomer forms and mixtures thereof of the formula ##STR1## wherein one of R.sub.1, R.sub.2 or R.sub.Type: GrantFiled: February 8, 1993Date of Patent: March 7, 1995Assignee: Roussel-UclafInventors: Marc Benoit, Jean-Pierre Demoute, Christian Wehrey
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Patent number: 5387690Abstract: Provided is a method of treating inflammatory bowel disease in mammals utilizing certain benzyl-substituted rhodanine derivatives. Also provided are novel benzyl-substituted rhodanine derivatives and pharmaceutical compositions thereof, as well as a novel process for selectively isolating in substantially pure enantiomeric form the enantiomers of certain racemic benzyl-substituted rhodanine derivatives.Type: GrantFiled: May 28, 1993Date of Patent: February 7, 1995Assignee: Eli Lilly and CompanyInventors: Jaswant S. Gidda, Jill A. Panetta, Michael L. Phillips