Chalcogen Attached Indirectly To The Tetrazole Ring By Nonionic Bonding Patents (Class 548/252)
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Patent number: 6284756Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.Type: GrantFiled: January 21, 2000Date of Patent: September 4, 2001Assignee: Eli Lilly and CompanyInventors: Nickolay Y Chirgadze, Richard W Harper, Todd J Kohn, Ho-Shen Lin, Jefferson R McCowan, Alan D Palkowitz, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Michael R Wiley, Minsheng Zhang
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Patent number: 6271241Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein X, R1, R2, R3, R4, R5, R6, R7, A, B, C, and D are variables defined herein. Such compounds useful in treatment of obesity and diabetes. The invention also provides labeled probes for the localization of cellular receptors that are involved in the modulation of blood glucose levels.Type: GrantFiled: March 31, 2000Date of Patent: August 7, 2001Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Alan Hutchison
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Patent number: 6271375Abstract: A process of direct metalation of phenyltetrazoles useful for preparing compounds of formula (II) intermediates for the synthesis of angiotensin II antagonists is described.Type: GrantFiled: April 27, 2000Date of Patent: August 7, 2001Assignee: Zambon Group S.p.A.Inventors: Marco Villa, Pietro Allegrini, Katiuscia Arrighi, Maurizio Paiocchi
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Patent number: 6252084Abstract: A class of novel 1H-indole-3-acetamides is disclosed together with the use of such indole compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.Type: GrantFiled: October 31, 1997Date of Patent: June 26, 2001Assignee: Eli Lilly and CompanyInventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim, Robert B. Hermann, Richard W. Schevitz
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Patent number: 6251925Abstract: The present invention relates to therapeutic biaryl derivatives of formula (I), and pharmaceutically acceptable derivatives thereof wherein R1 is a phenyl, naphthyl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, —NR6R6, and —NHSO2R6, where each R6 is independently hydrogen or C1-4alkyl; R2 is hydrogen or C1-6alkyl; X is oxygen, sulfur, —NH, or —NC1-4alkyl; R3 is cyano, tetrazol-5-yl, or —CO2R7 where R7 is hydrogen or C1-6alkyl; R4 and R5 are independently hydrogen, C1-6alkyl, —CO2H, —CO2C1-6alkyl, cyano, tetrazol-5-yl, halogen, trifluoromethyl, or C1-6alkoxy, or, when R4 and R5 are bonded to adjacent carbon atoms, R4 and R5 may, together with the carbon atoms to which they are bonded, form a fused 5 or 6 membered ring optionally containing one or two nitrogen, oxygen,Type: GrantFiled: December 13, 2000Date of Patent: June 26, 2001Assignee: Glaxo Wellcome Inc.Inventors: Kelly Horne Donaldson, Barry George Shearer, David Edward Uehling
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Patent number: 6245804Abstract: This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.Type: GrantFiled: May 29, 1998Date of Patent: June 12, 2001Assignee: Schering AktiengesellschaftInventors: Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
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Patent number: 6232334Abstract: Benzimidazole derivatives of the formula (I): wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R′ group; R1 is hydrogen or an optionally substituted hydrocarbon residue; R2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R′ is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is —O—, —S(O)m— or —N(R4)— wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases, strokes,Type: GrantFiled: August 18, 1999Date of Patent: May 15, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
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Patent number: 6211197Abstract: Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed. The compounds are represented by formula II: Ar1—W—Ar2—X—Q II The compounds of the invention are structurally different from NSAIDs and opiates, and are antagonists of the pain and inflammatory effects of E-type prostaglandins.Type: GrantFiled: October 4, 1999Date of Patent: April 3, 2001Assignee: Merck Frosst Canada & Co.Inventors: Michel Belley, Marc Labelle, Nicholas Lachance, Michel Gallant, Nathalie Chauret, Laird A. Trimble, Chun Li
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Patent number: 6191289Abstract: There are disclosed an industrially favorable process for producing a tetrazole compound of general formula (1): characterized in that a nitrile of general formula (2): R1CN (2) is reacted with hydrazine or a salt thereof in the presence of a catalyst, followed by reaction with a nitrous acid compound of general formula (3): ANO2 (3) or a nitrile of general formula (2) is reacted with hydrogen sulfide, followed by reaction with an alkyl halide of general formula (4): R4J (4) with hydrazine or a salt thereof, and then with a nitrous acid compound of general formula (3); and an intermediate of general formula (5): R1C(═R5)R6 (5) which is useful for the production of the tetrazole compound (in which R1 to R6, A and J in the above formulas are as defined in the specification).Type: GrantFiled: October 21, 1998Date of Patent: February 20, 2001Assignee: Sumitomo Chemical Company, LimitedInventors: Hideki Ushio, Takayuki Higashii, Masayoshi Minai, Akihiko Nakamura
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Patent number: 6168776Abstract: Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.Type: GrantFiled: April 18, 1997Date of Patent: January 2, 2001Assignee: University of PittsburghInventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
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Patent number: 6143774Abstract: The invention relates to the new products of formula (I): ##STR1## in which: R.sub.1 represents alkyl, optionally substituted or cycloalkyl optionally interrupted by heteroatoms,R.sub.2 ; R.sub.3 both represent or carry an acid function or an acid isosteric function,and Y represents phenyl substituted in particular by a dioxol radical,these products being in all the isomeric forms and the salts, as medicaments.Type: GrantFiled: June 9, 1998Date of Patent: November 7, 2000Assignee: Hoechst Marion RousselInventors: Bertrand Heckmann, Simone Jouquey, Jean-Paul Vevert, Jidong Zhang
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Patent number: 6143918Abstract: Methods for preparing novel dibenzoylresorcinol-based compounds are disclosed, wherein the dibenzoylresorcinol is bonded to the residue of either an alcohol or a carboxylic acid group, via a methylene carboxylate linking group; and wherein the dibenzoylresorcinol is bonded directly to a substituted or unsubstituted aryl group which does not include a pendent hydroxyl group. The groups attached to the dibenzoylresorcinol may contain a wide variety of functional sites which permit further reaction, e.g., copolymerization. The described compounds are very useful as UV light absorbers and may be used to form improved coating compositions which usually include a transparent, polymeric matrix material. The coating compositions may be applied to various substrates, e.g., thermoplastics, to afford a selection of enhanced properties, such as UV light resistance and abrasion resistance.Type: GrantFiled: July 2, 1999Date of Patent: November 7, 2000Assignee: General Electric CompanyInventors: James Edward Pickett, Wen P Liao, Amy Kathleen Simonian, Gregory Ronald Gillette
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Patent number: 6140352Abstract: Disclosed herein are selective beta 3 adrenergic agonists represented by the following structural formula: ##STR1## The variables in the structural formula shown above are defined in the specification. Also disclosed are methods of using these compounds for agonizing the beta 3 adrenergic receptor in patients in need of such treatment, for example, patients in need of treatment for obesity or Type II diabetes.Type: GrantFiled: May 4, 1998Date of Patent: October 31, 2000Assignee: Eli Lilly and CompanyInventors: Thomas A. Crowell, Deborah A. Evrard, Charles D. Jones, Brian S. Muehl, Christopher J. Rito, Anthony J. Shuker, Andrew J. Thorpe, Kenneth J. Thrasher
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Patent number: 6136834Abstract: A tetrazole derivative of formula (I) ##STR1## wherein R is H, alkyl, alkoxy, carbocyclic ring, alkyl or alkoxy substituted by carbocyclic ring;AA.sup.1 and AA.sup.2 is a bond or ##STR2## and ##STR3## respectively, or AA.sup.1 and AA.sup.2, together, may have the formula (a); ##STR4## and Y is formula (b) ##STR5## wherein the Tet ring is tetrazole; Z is alkylene, alkenylene, O, S, SO, SO.sub.2, NR.sup.26, methylene in alkylene replaced by O, S, --SO--, --SO.sub.2 -- or --NR.sup.26 --; and E is H, alkyl, or COOR.sup.27.Type: GrantFiled: June 29, 1998Date of Patent: October 24, 2000Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Makoto Tanaka, Tohru Miyazaki, Hiroyuki Ohno
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Aryl- and hetaryl-sulfonamide derivatives, their preparation and their use as endothelin antagonists
Patent number: 6133442Abstract: Compounds of formula I ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl;R.sup.2 signifies phenyl or substituted phenyl;R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ;R.sup.4 signifies hydrogen or lower-alkyl;R.sup.5 signifies hydrogen or a residue R.sup.7, andR.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; orR.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue;R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl;R.sup.a signifies hydrogen, lower-alkyl or hydroxy;R.sup.b signifies hydrogen or lower-alkyl;Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.8, --OC(O)OR.sup.Type: GrantFiled: March 5, 1999Date of Patent: October 17, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz -
Patent number: 6110963Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein A is C or N;B is O, S, N, or CH.dbd.CH;E is ##STR2## or --X--D; D is ##STR3## or alkyl of 1-12 carbon atoms; X is CO, CH(OH), CH.sub.2, or --CH--S-2-benzothiazole;Y is hydrogen, alkyl of 1-6 carbon atoms, or halogen;Z is O, S, or N;R is hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, or trifluoromethyl;R.sup.1 is alkyl of 1-12 carbon atoms, aryl of 6-10 carbon atoms, aralkyl of 7-15 carbon atoms, halogen, Het-alkyl wherein the alkyl moiety contains 1-6 carbon atoms, or aryl mono-, di- or tri-substituted with a substituent selected from the group consisting of halogen, alkyl of 1-6 carbon atoms, trifluoromethyl, and alkoxy of 1-6 carbon atoms;Het is ##STR4## G is O, S, or N; and the remaining variables are as defined in claim 1, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin or hyperglycemia.Type: GrantFiled: May 10, 1999Date of Patent: August 29, 2000Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 6110962Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein A is hydrogen, halogen, or OH;B and D are each, independently, hydrogen, halogen, CN, alkyl of 1-6 carbon atoms, aryl, aralkyl of 6-12 carbon atoms, nitro, amino or OR;R is hydrogen, alkyl of 1-6 carbon atoms, --COR.sup.1, --CH.sub.2 CO.sub.2 R.sup.1, --CH(R.sup.1a)CO.sub.2 R.sup.1, or --SO.sub.2 R.sup.1 ;R.sup.1 and R.sup.1a are each, independently, hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms or aryl;E is S, SO, SO.sub.2, O;X is hydrogen, halogen, alkyl of 1-6 carbon atoms, CN, perfluoroalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, aryloxy, arylalkoxy of 6-12 carbon atoms, nitro, amino, alkylsulfanyl of 1-6 carbon atoms, arylsulfanyl, pyridylsulfanyl, 2-N,N-dimethylaminoethylsulfanyl, or --OCH.sub.2 CO.sub.2 R.sup.1b ;R.sup.1b is hydrogen or alkyl of 1-6 carbon atoms;Y and Z are each, independently, hydrogen or OR.sup.2 ;R.sup.Type: GrantFiled: May 10, 1999Date of Patent: August 29, 2000Assignee: American Home Products CorporationInventors: Jay E. Wrobel, Arlene J. Dietrich, Zenan Li
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Patent number: 6107311Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is O or S; and(f) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: April 9, 1998Date of Patent: August 22, 2000Assignee: The Procter & Gamble CompanyInventors: Laurence Ichih Wu, John Michael Janusz
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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: 6096740Abstract: The present invention relates to pharmaceutical compositions for preventing or alleviating neurotoxicity. Said pharmaceutical compositions comprise as their active ingredient the stereospecific (+) enantiomers, having (3S,4S) configuration, of .DELTA..sup.6 -tetrahydrocannabinol (THC) type compounds of general formula (I), as defined hereinbelow.Type: GrantFiled: September 28, 1998Date of Patent: August 1, 2000Assignees: Ramot University Authority for Applied Research and Industrial Development Ltd., Yissum Research Develpoment Company of the Hebrew University in JersusalemInventors: Raphael Mechoulam, Emil Pop, Mordechai Sokolovsky, Yoel Kloog, Anat Biegon
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Patent number: 6090839Abstract: The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compounds which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.Type: GrantFiled: December 19, 1997Date of Patent: July 18, 2000Assignee: Merck & Co., Inc.Inventors: Alan D. Adams, Derek Von Langen, Richard L. Tolman, Hiroo Koyama
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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: 6063587Abstract: Tetrazolium salt compounds represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen atom, nitro group, cyano group, carboxyl group or a halogen atom, preferably nitro group; R.sup.3 represents an alkyl group or an alkoxyl group, preferably methyl group or methoxy group; and M represents an alkali metal or an ammonium. The compounds are useful for quantitative measurement of a dehydrogenase, and characterized to have high water-solubility and excellent storage stability in the state of an aqueous solution.Type: GrantFiled: December 8, 1998Date of Patent: May 16, 2000Assignee: Dojindo Laboratories Co., Ltd.Inventors: Munetaka Ishiyama, Yoko Miyazono, Masanobu Shiga, Kazumi Sasamoto
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Patent number: 6060603Abstract: Disclosed are methods for modelling the three-dimensional structure (tertiary structure) of a ligand having one or more active sites employing a charge-transfer interaction. Also disclosed is a model for Angiotensin II derived from such method.Type: GrantFiled: May 6, 1997Date of Patent: May 9, 2000Assignee: PepMetics, Inc.Inventor: Graham J. Moore
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Patent number: 6054588Abstract: The compounds of the formula ##STR1## wherein R signifies halogen or lower alkyl;n signifies 0-3;R.sup.1 signifies lower alkyl; cycloalkyl; benzyl optionally substituted by hydroxy, halogen, lower alkoxy or lower alkyl; benzoyl optionally substituted by amino, lower alkyl-amino or di-lower alkylamino; acetyl or cycloalkyl-carbonyl; and ##STR2## signifies an aromatic 5-membered residue which is bonded via a N-atom and which contains further 1-3 N atoms in addition to the linking N atom,as well as their pharmaceutically acceptable salts as therapeutically active substances, especially for the control or prevention of acute and/or chronic neurological disorders.Type: GrantFiled: May 4, 1999Date of Patent: April 25, 2000Assignee: Hoffman-La Roche Inc.Inventors: Geo Adam, Sabine Kolczewski, Vincent Mutel, Heinz Stadler, Jurgen Wichmann, Thomas Johannes Woltering
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Patent number: 6048983Abstract: A process for preparing certain substituted benzopyran compounds is disclosed.Type: GrantFiled: February 8, 1999Date of Patent: April 11, 2000Assignee: SmithKline Beecham pl.cInventors: Robert Gordon Giles, Paul Oxley
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Patent number: 6048895Abstract: The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to the following formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, and Z are as defined. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof.The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using theses compounds or the compositions containing them.Type: GrantFiled: September 4, 1998Date of Patent: April 11, 2000Assignee: The Procter & Gamble CompanyInventors: John August Wos, Mitchell Anthony deLong, Jack S. Amburgey, Jr., Haiyan George Dai, Biswanath De, David Lindsey Soper
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Patent number: 6046227Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta..sub.3 receptor agonists useful in the treatment of Type II diabetes and obesity.Type: GrantFiled: December 4, 1998Date of Patent: April 4, 2000Assignee: Eli Lilly and CompanyInventors: Thomas Alan Crowell, Charles David Jones, Anthony John Shuker
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Patent number: 6046205Abstract: Compound of formula (I): ##STR1## wherein: n is 0 or 1,A represents a .sigma. bond or alkylene or alkenylene,X represents nitrogen or C--R.sub.2,R.sub.1 represents hydrogen or alkyl,G.sub.1 represents any one of the groups defined in the description.These compounds are useful for treating a living body afflicted with venous insufficiency, and/or migraine, and/or migraine associated with vascular diseases.Type: GrantFiled: April 26, 1999Date of Patent: April 4, 2000Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Olivier Muller, Christine Vayssettes-Courchay, Jean-Jacques Descombes, Tony Verbeuren
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Patent number: 6034248Abstract: The present invention provides an azole compound represented by the formula (I): ##STR1## wherein Ar is an optionally substituted phenyl group; R.sup.1 and R.sup.2, the same or different, are a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 may combine together to form a lower alkylene group; R.sup.3 is a hydrogen atom or an acyl group; X is a nitrogen atom or a methine group; A is Y.dbd.Z (Y and Z, the same or different, are a nitrogen atom or a methine group optionally substituted with a lower alkyl group) or an ethylene group optionally substituted with a lower alkyl group; n is an integer from 0 to 2; and Az is an optionally substituted azolyl group, or its salt, which is useful for a prevention and therapy of a fungal infection of a mammal as a antifungal agent.Type: GrantFiled: October 17, 1996Date of Patent: March 7, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Katsumi Itoh, Kenji Okonogi, Akihiro Tasaka
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Patent number: 6028092Abstract: This invention relates to novel formulations of salts of certain benzopyran compounds, to compositions containing them and their use in the treatment of certain disorders.Type: GrantFiled: June 17, 1998Date of Patent: February 22, 2000Assignee: SmithKline Beecham p.l.cInventors: Christopher John Banton, Phillip Christopher Buxton
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Patent number: 6022868Abstract: Disclosed are compounds of formula (I) selected from the following ##STR1## wherein Y is ##STR2## and wherein A, B, C, D, R, k, m, n, o, p, s, t and u are as defined in the specification. These compounds are useful in treating diseases in the central nervous system related to malfunctioning of the nicotinic cholinergic system.Type: GrantFiled: December 19, 1997Date of Patent: February 8, 2000Assignee: Novo Nordisk AlsInventors: Preben Houlberg Olesen, John Bondo Hansen
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Patent number: 6020355Abstract: Tetrazole derivatives of the formula wherein R is a substituted or unsubstituted phenyl group, heterocyclic group, or benzo-fused heterocyclic group,which exhibit activity as insecticides and acaricides.Type: GrantFiled: April 7, 1999Date of Patent: February 1, 2000Inventors: Mark Achiel Dekeyser, Paul Thomas McDonald
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Patent number: 6013673Abstract: A naphthyloxyacetic acid derivative of the formula (I) ##STR1## wherein R.sup.1 is H, alkyl, alkylene-(--COOR.sup.10, --OH, --CONR.sup.4 R.sup.5, --CONR.sup.6 -alkylene-OH, --NR.sup.4 R.sup.5, -cyano or -tetrazolyl); A is single bond, alkylene, alkenylene, --S-alkylene, --O-alkylene; B is NR.sup.3 CO, CONR.sup.3 ; R.sup.2 is (1) alkyl (2) alkenyl, (3) alkyl or alkenyl substituted by 1-3 of phenyl, cycloalkyl, naphthyl and heterocyclic ring containing nitrogen atom (the said ring may be substituted by 1-3 of alkyl, alkoxy and halogen etc.), (4) NR.sup.7 R.sup.8 or (5) alkylene-NR.sup.7 R.sup.8 ; non-toxic salt thereof, non-toxic acid addition salt thereof and hydrate thereof can bind the PGE.sub.2 receptor and exhibits the activity to antagonize or agonize for PGE.sub.2., therefore, they are useful as PGE.sub.2 antagonist or PGE.sub.2 agonist.Type: GrantFiled: January 23, 1998Date of Patent: January 11, 2000Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Yuuki Nagao, Kazuhiko Torisu, Takayuki Maruyama
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Patent number: 6008368Abstract: Pharmaceutical compositions comprising a compound selected from a class of N-substituted (.alpha.-imidazolyl-toluyl)pyrrole compounds are described for use in treatment of circulatory disorders. Compositions of particular interest comprise angiotensin II antagonist compounds of the formula ##STR1## wherein m is one; wherein R.sup.0 is selected from CH.sub.2 OH, CO.sub.2 H, CHO, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, CH.sub.2 OCH.sub.3, CH.sub.2 OCHOCH.sub.3 and CH.sub.2 --CO.sub.2 C.sub.2 H.sub.5 ; wherein R.sup.1 is selected from Cl, CF.sub.3, CHO, n-butyl, cyano, CO.sub.2 CH.sub.3 and CO.sub.2 CH.sub.2 CH.sub.3 ; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, propylthio, butylthio and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.9 and R.sup.10 is hydrido; wherein each of R.sup.5 and R.sup.Type: GrantFiled: November 24, 1997Date of Patent: December 28, 1999Assignee: G. D. Searle & Co.Inventors: Philippe R. Bovy, Joe T. Collins, Robert E. Manning
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Patent number: 6004989Abstract: Benzimidazole derivatives of the formula (I): ##STR1## wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R' group; R.sup.1 is hydrogen or an optionally substituted hydrocarbon residue; R.sup.2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R' is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is --O--, --S(O).sub.m -- or --N(R.sup.4)-- wherein m is an integer of 0, 1 or 2 and R.sup.4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g.Type: GrantFiled: March 29, 1999Date of Patent: December 21, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
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Patent number: 6001823Abstract: Novel methods for the treatment and/or prophylaxis of diseases caused by tissue-adhering bacteria are disclosed. By interacting with periplasmic molecular chaperones it is achieved that the assembly of pili is prevented or inhibited and thereby the infectivity of the bacteria is diminished. Also disclosed are methods for screening for drugs as well as methods for the de novo design of such drugs, methods which rely on novel computer drug modelling methods involving an approximative calculation of binding free energy between macromolecules. Finally, novel pyranosides which are believed to be capable of interacting with periplasmic molecular chaperones are also disclosed.Type: GrantFiled: June 5, 1995Date of Patent: December 14, 1999Inventors: Scott Hultgren, Meta Kuehn, Zheng Xu, Derek Ogg, Mark Harris, Matti Lepisto, Jan Kihlberg, Charles Hal Jones
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Patent number: 5994391Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.Type: GrantFiled: July 2, 1998Date of Patent: November 30, 1999Assignee: G.D. Searle and CompanyInventors: Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
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Patent number: 5985901Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: May 22, 1998Date of Patent: November 16, 1999Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Feroze Ujjainwalla, Thomas F. Walsh, Matthew J. Wyvratt, Jr., Jonathan R. Young, Lin Chu
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Patent number: 5981438Abstract: The present invention relates to novel 1-Phenyl-5-anilinotetrazoles of the formula (I): ##STR1## wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4, m and n have the meaning provided in the specification, precesses for their preparation and their use as microbiocides, insecticides and/or herbicides.Type: GrantFiled: January 22, 1998Date of Patent: November 9, 1999Assignee: Nihon Bayer Agrochem K.K.Inventors: Fritz Maurer, Kaori Kido, Yoshio Kurahashi, Haruko Sawada, Keiko Tanaka, Yuichi Otsu, Yumi Hattori, Katsuhiko Shibuya, Takahisa Abe, Toshio Goto, Seishi Ito
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Patent number: 5977124Abstract: .beta.-adrenergic agonists for the treatment of diseases/conditions such as obesity and diabetes. The compounds have formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, W, X, Y and Z are as defined in the specification.Type: GrantFiled: November 4, 1997Date of Patent: November 2, 1999Assignee: Pfizer Inc.Inventor: Robert L. Dow
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Patent number: 5972930Abstract: This invention provides a compound of the formula: ##STR1## and its pharmaceutically acceptable salts, wherein Ar.sup.1 is selected from groups of the following formulae: ##STR2## wherein, R.sup.1 and R.sup.2 are independently hydrogen or C.sub.1 -C.sub.6 alkyl;W is (CH.sub.2).sub.n wherein n is from 1 to 3, or --CH.dbd.CH--;X is C.sub.1 -C.sub.6 alkoxy or halo C.sub.1 -C.sub.6 alkoxy; andAr.sup.2 is phenyl optionally substituted by halogen atom.These compounds are useful in the treatment of a gastrointestinal disorder, a central nervous system (CNS) disorder, an inflammatory disease, emesis, urinary incontinence, pain, migraine, sunburn, angiogenesis, diseases, disorders and adverse conditions caused by Helicobacter pylori, or the like in a mammalian subject, especially humans.Type: GrantFiled: August 7, 1997Date of Patent: October 26, 1999Assignee: Pfizer, Inc.Inventors: Hiroki Koike, Hiroaki Wakabayashi
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Patent number: 5965741Abstract: The invention provides compounds of formula I: ##STR1## wherein A, B, D, X, R.sup.1, and R.sup.3 have any of the values defined in the specification, as well as N-oxides thereof, S-oxides thereof, pharmaceutically acceptable salts thereof, and in vivo hydrolizable esters and amides thereof, that are useful to relieve pain. The invention also provides pharmaceutical compositions as well as synthetic and therapeutic methods relating to such compounds.Type: GrantFiled: February 21, 1997Date of Patent: October 12, 1999Assignee: Zeneca LimitedInventors: Gloria Anne Breault, Howard Tucker, John Oldfield, Peter Warner
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Aryl- and hetaryl-sulfonamide derivatives, their preparation and their use as endothelin antagonists
Patent number: 5962682Abstract: Compounds of formula (I) ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl; R.sup.2 signifies phenyl or substituted phenyl; R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ; R.sup.4 signifies hydrogen or lower-alkyl; R.sup.5 signifies hydrogen or a residue R.sup.7, and R.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; or R.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue; R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl; R.sup.a signifies hydrogen, lower-alkyl or hydroxy; R.sup.b signifies hydrogen or lower-alkyl; Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.Type: GrantFiled: August 18, 1997Date of Patent: October 5, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz -
Patent number: 5955492Abstract: This invention relates to novel carboxylic acid indole compounds and compositions for use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: September 24, 1998Date of Patent: September 21, 1999Assignee: SmithKline Beecham CorporationInventors: Scott K. Thompson, Stacie M. Halbert, Katherine L. Widdowson
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Patent number: 5948779Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasias, including precancerous and cancerous lesions.Type: GrantFiled: December 12, 1997Date of Patent: September 7, 1999Assignee: Cell Pathways, Inc.Inventors: Gerhard J. Sperl, Paul Gross, Klaus Brendel, Gary A. Piazza, Rifat Pamukcu
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Patent number: 5922763Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.Type: GrantFiled: November 26, 1997Date of Patent: July 13, 1999Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
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Patent number: 5869504Abstract: Tetrazole derivatives of the formula ##STR1## wherein R is a substituted or unsubstituted phenyl group, heterocyclic group, or benzo-fused heterocyclic group,which exhibit activity as insecticides and acaricides.Type: GrantFiled: November 4, 1997Date of Patent: February 9, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Mark Achiel Dekeyser, Paul Thomas McDonald
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Patent number: 5859258Abstract: Losartan potassium is an angiotensin II antagonist useful in the treatment of hypertension and congestive heart failure. ##STR1## This invention relates to the process for the controlled crystallization of losartan potassium utilizing anti-solvent addition combined with massive seeding in order to obtain the desired crystal morphology and bulk physical properties necessary for successful formulation.Type: GrantFiled: October 28, 1997Date of Patent: January 12, 1999Assignee: Merck & Company, Inc.Inventors: Patrick Breen, Erik A. Dienemann, Albert D. Epstein, Karen A. Larson, Michael T. Kennedy, Hari Mahadevan
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Patent number: 5856490Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: September 4, 1997Date of Patent: January 5, 1999Assignee: AllerganInventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna