Chalcogen Or Nitrogen Attached Directly To The Tetrazole Ring By Nonionic Bonding Patents (Class 548/251)
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Patent number: 6159973Abstract: The subject of the invention is the compounds of formula (I):Q(CH.sub.2).sub.a --(X.sub.1).sub.b --Q.sub.1 --Q.sub.2 --C(X.sub.2)--N(R.sub.1)(R.sub.2) (I)in which:Q represents an aryl radical,X.sub.1 represents oxy, thio, sulphinyl or sulphonyl,X.sub.2 represents oxygen or sulphur,Q.sub.1 represents a cyclopropanediyl radical,Q.sub.2 represents an arylene radical,R.sub.1 and R.sub.2 represent:either a hydrogen atom or a hydrocarbon radicalor one of the groupsR.sub.3 --C.dbd.X.sub.3, (R.sub.3).sub.2 --P.dbd.X.sub.3, T.sub.2 --R.sub.5 or S(O).sub.j --N(R.sub.6)(R.sub.7)in which X.sub.3 represents an oxygen atom or a sulphur atom, T.sub.2 represents a bivalent oxy, carbonyl or oxycarbonyl group and j is equal to 0, 1 or 2,their preparation process and their use as pesticides.Type: GrantFiled: July 21, 1999Date of Patent: December 12, 2000Assignee: Hoechst Schering Agrevo S.A.Inventors: Jacques Demassey, Michel Gohar, Christian Wehrey
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Patent number: 6156907Abstract: The invention relates on the one hand to a novel preparation of compounds of the formula (I) ##STR1## in which R.sub.1 is an aromatic or heteroaromatic radical, aromatic-aliphatic or heteroaromatic-aliphatic radical, a heterocyclic radical, a cycloaliphatic radical, a cycloaliphatic-aliphatic radical or an aliphatic radical,and on the other hand to novel compounds of the formula (I).Type: GrantFiled: January 8, 1999Date of Patent: December 5, 2000Assignee: Novartis AGInventor: Robert Portmann
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Patent number: 6143732Abstract: The Sesquiterpene derivatives are useful as antivirus agents, which are shown by the formula: ##STR1## wherein R.sup.1 is hydrogen or halogen; and R.sup.2 is hydrogen, halogen, --OR.sup.7 (wherein R.sup.7 is hydrogen etc.) or --NHR.sup.8 (wherein R.sup.8 is hydrogen etc.) etc., or R.sup.1 and R.sup.2 taken together may form oxo or .dbd.NR.sup.9 (wherein R.sup.9 is hydroxy etc.);R.sup.3 is hydrogen or halogen; R.sup.4 is hydrogen, halogen, --OR.sup.10 (wherein R.sup.10 is hydrogen etc.), or --NHR.sup.11 (wherein R.sup.11 is hydrogen etc.), or R.sup.3 and R.sup.4 taken together may form oxo or .dbd.NR.sup.12 (wherein R.sup.12 is hydroxy etc.) or R.sup.2 and R.sup.4 taken together may form an unsaturated bond or --O--;A is .dbd.NR.sup.5 (wherein R.sup.5 is hydrogen, lower alkyl etc.)R.sup.6 is hydrogen, cyano etc.,X is hydrogen, cyano etc.,Y.sup.1 and Y.sup.2 are both hydrogens, or taken together may form oxo;Z.sup.1 and Z.sup.2 are both hydrogens, or taken together may form oxo, or Z.sup.1 is hydrogen and Z.Type: GrantFiled: September 20, 1999Date of Patent: November 7, 2000Assignee: Shionogi & Co., Ltd.Inventors: Kenichi Sugita, Naohiko Hattori
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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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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: 6069257Abstract: A process for preparing certain substituted benzopyran compounds of formula (I) ##STR1## is disclosed.Type: GrantFiled: July 6, 1999Date of Patent: May 30, 2000Assignee: SmithKline Beecham p.l.c.Inventors: Robert Gordon Giles, Norman John Lewis, Paul Oxley, John Kirby Quick
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Patent number: 6057319Abstract: The invention encompasses the novel compound of formula (I) useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of formula (I).Type: GrantFiled: October 2, 1998Date of Patent: May 2, 2000Assignee: Merck Frosst Canada & Co.Inventors: Cameron Black, Serge Leger, Petpiboon Prasit, Zhaoyin Wang, Pierre Hamel, Yongxin Han, Gregory Hughes
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Patent number: 6051586Abstract: This invention related to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.Type: GrantFiled: November 23, 1998Date of Patent: April 18, 2000Assignee: Bayer CorporationInventors: Gaetan H. Ladouceur, Richard D. Connell, Jeremy Baryza, Ann-Marie Campbell, Timothy G. Lease, James H. Cook
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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: 6011045Abstract: The present invention relates to compounds of the formula IA--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: January 4, 2000Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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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: 5998456Abstract: Benzimidazole compounds represented by the formula set out below and analogs thereof, wherein Y represents a single bond or sulfur atom; Z represents oxygen atom, sulfur atom, or N--R.sup.4 ; R.sup.1 and R.sup.2 independently represent hydrogen, a halogen atom, alkyl group or other; R.sup.1 and R.sup.4 independently represent hydrogen, alkyl group, acyl group or other; n and m independently represent an integer of 1, 2, or 3; and L represents a linking group such as C.sub.2-12 alkylene group or an alkylene group containing one or more phenylene groups or ether groups. The compounds are useful as an active ingredient of a medicament such as a preventive and therapeutic medicament for hyperlipemia or arterial sclerosis.Type: GrantFiled: January 16, 1998Date of Patent: December 7, 1999Assignee: Fuji Photo Film Co., Ltd.Inventors: Kozo Aoki, Kazuhiro Aikawa
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Patent number: 5990145Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: November 23, 1999Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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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: 5981550Abstract: 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 9, 1999Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Thomas F. Walsh, Feroze Ujjainwalla, Matthew J. Wyvratt, Jr., Jonathan R. Young, Lin Chu
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Patent number: 5977169Abstract: This invention comprises novel substituted tetronic acid type compounds, 2, 4(3H, 5H)-furandiones, that are useful for the inhibition of the HIV protease enzyme. The compounds may be useful for the treatment of a person with AIDS or AIDS related diseases. The compounds may be used in the attempt to retard the further replication of any retrovirus containing the aspartyl protease enzyme. Compounds are represented by the formula below.Type: GrantFiled: July 28, 1997Date of Patent: November 2, 1999Inventors: Robert A. Chrusciel, Linda L. Maggiora, Suvit Thaisrivongs, James M. Tustin, Clark W. Smith, Ruben A. Tommasi, Paul A. Aristoff, Harvey I. Skulnick, W. Jeffrey Howe, Gordon L. Bundy
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Patent number: 5968963Abstract: Certain compounds have been synthesized and found to be effective inhibitors of phospholipase A.sub.2 (PLA.sub.2), and thereby useful in the treatment of intestinal cholesterol absorption and the disease states arising therefrom, such as hypercholesterolemia and coronary artery disease.Type: GrantFiled: March 4, 1996Date of Patent: October 19, 1999Assignee: Warner-Lambert CompanyInventor: Reynold Homan
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Patent number: 5962656Abstract: A photographic element comprising a support having situated thereon at least one silver halide emulsion layer, the layer containing a photographic coupler represented by the formulaCOUP--T.sup.1 --T.sup.2 --(T.sup.3).sub.b --PUGwhereinCOUP is a coupler moiety having a coupling site to which T.sup.1 is attached;T.sup.1 and T3 are timing or linking groups;T.sup.2 is an indazole timing or linking group which, after release from T.sup.1, functions by electron transfer down a conjugated chain to release T.sup.3 or PUG, and which is represented by the formula: ##STR1## wherein ** denotes the point of attachment to T.sup.1 and *** denotes the point of attachment to T.sup.3 or PUG;R.sup.1 and R.sup.2 are independently selected from hydrogen, or an aliphatic, carbocyclic, or heterocyclic group, or may be bonded together to form a 5, 6, or 7 membered ring;V is independently a substituent group as further defined;q is 0, 1, 2, 3 or 4;b is 0 or 1; andPUG is a photographically useful group.Type: GrantFiled: June 10, 1997Date of Patent: October 5, 1999Assignee: Eastman Kodak CompanyInventors: William James Begley, Teh Hsuan Chen, Donald Singleton, Jr., Frank Dino Coms
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Patent number: 5942622Abstract: The subject of the invention is the products of formula (I): in which one of A and B represents a nitrogen atom and the other one of A and B represents a methine radical, such that:A represents either nitrogen substituted in particular by alkyl,or methine substituted in particular by phenyl, thienyl or pyridyl,B represents either nitrogen substituted in particular by cyclohexylalkyl,or methine substituted in particular by alkylthio,R.sub.1 represents in particular carboxy,R represents in particular halogen,as well as the isomers and salts of said products of formula(I).Type: GrantFiled: April 22, 1998Date of Patent: August 24, 1999Assignee: Hoechst Marion RousselInventors: Stanislas Didierlaurent, Michel Fortin, Jidong Zhang
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Patent number: 5932740Abstract: 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: January 23, 1998Date of Patent: August 3, 1999Assignee: Sterling Diagnostic Imaging, Inc.Inventors: Dietrich Max Fabricius, Gregory Charles Weed
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Patent number: 5929075Abstract: The present invention provides novel compounds of formula ##STR1## the N-oxides, the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof, wherein A and B taken together form a bivalent radical of formula:--N.dbd.CH-- (a), --CH.dbd.N-- (b), --CH.sub.2 --CH.sub.2 -- (c), --CH.dbd.CH-- (d), --C(.dbd.O)--CH.sub.2 -- (e), --CH.sub.2 --C(.dbd.O)-- (f); R.sup.1 is hydrogen, C.sub.1-6 alkyl, or halo; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-6 cycloalkyl or C.sub.1-8 alkyl substituted with hydroxy, oxo, C.sub.3-6 cycloalkyl or aryl. Het is five- or six-membered optionally substituted heterocyclic ring. The use as a medicine, especially as a lipid lowering agent is disclosed as well as pharmaceutical compositions and processes for preparing compounds and compositions.Type: GrantFiled: April 9, 1997Date of Patent: July 27, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Heeres, Leo Jacobus Jozef Backx, Robert Jozef Maria Hendrickx, Luc Alfons Leo Van der Eycken, Didier Robert Guy Gabriel de Chaffoy de Courcelles
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Patent number: 5929106Abstract: Dihydroisoindole compounds of formula (I), wherein the substituents are as defined herein, are disclosed as being useful as endothelin receptor antagonists. The compounds are applied in the treatment of cardiovascular and renal diseases.Type: GrantFiled: October 27, 1997Date of Patent: July 27, 1999Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Robert Gene Franz, M. Amparo Lago, Aiming Gao
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Patent number: 5922744Abstract: The present invention provides a compound of formula: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6a and R.sup.6b are defined herein or a pharmaceutically acceptable salt thereof, a process for its preparation, intermediates and its use as a tachykinin antagonist.Type: GrantFiled: January 12, 1998Date of Patent: July 13, 1999Assignee: Merck Sharp & Dohme LimitedInventors: Timothy Harrison, Andrew Pate Owens
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Patent number: 5877323Abstract: Herbicidally active 1-aryl-4-carbamoyl-tetrazolinones of the formula (I) ##STR1## in which Ar represents optionally substituted aryl,R.sup.1 represents in each case optionally substituted alkyl, alkenyl, alkinyl or alkoxy, andR.sup.2 represents in each case optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, or, together with R.sup.1, represents alkanediyl,are obtained in good yields and at high purity by reacting 1-aryl-tetrazolinones of the formula (II) with phosgene in the presence of a diluent at temperatures of between 0.degree. C. and 150.degree. C. ("first process step"), and reacting the resulting (novel) 1-aryl-4-chlorocarbonyl-tetrazolinones of the formula (III) with amines of the formula (IV) in the presence of a diluent, and, where appropriate, in the presence of a further basic compound, at temperatures of between -20.degree. C. and +100.degree. C.Type: GrantFiled: February 12, 1998Date of Patent: March 2, 1999Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Uwe Stelzer, Carl Casser
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Patent number: 5874586Abstract: Herbicidally active 1-aryl-4-carbamoyl-tetrazolinones of the formula (I) ##STR1## in which Ar represents optionally substituted aryl,R.sup.1 represents in each case optionally substituted alkyl, alkenyl, alkinyl or alkoxy, andR.sup.2 represents in each case optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, or, together with R.sup.1, represents alkanediyl,are obtained in good yields and at high purity by reacting 1-aryl-tetrazolinones of the formula (II) with phosgene in the presence of a diluent at temperatures of between 0.degree. C. and 150.degree. C. ("first process step"), and reacting the resulting (novel) 1-aryl-4-chlorocarbonyl-tetrazolinones of the formula (III) with amines of the formula (IV) in the presence of a diluent, and, where appropriate, in the presence of a further basic compound, at temperatures of between -20.degree. C. and +100.degree. C.Type: GrantFiled: February 4, 1998Date of Patent: February 23, 1999Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Uwe Stelzer, Carl Casser
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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
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Patent number: 5840895Abstract: Compounds of formulae (II), (III), (IV) and (V) or salts thereof are intermediates for pharmacologically active tricyclic benzazepine and benzothiazepine derivatives, ##STR1## wherein R represents hydrogen, alkyl, phenylalkyl, or a protective group of a triazole ring, R.sup.1 -R.sup.5 represent hydrogen, alkyl, alkenyl, alkoxy, amino, oxim or hydroxyl, and R.sup.41 represents hydrogen, C.sub.1-6 alkyl which may be optionally substituted, or a protective group for a carboxyl group.Type: GrantFiled: June 26, 1997Date of Patent: November 24, 1998Assignee: Meiji Seika Kabushiki KaishaInventors: Yasuo Ohtsuka, Takashi Shishikura, Hiroko Ogino, Kenichi Fushihara, Mami Kawaguchi, Seiji Tsutsumi, Megumi Imai, Keiko Shito, Koji Tsuchiya, Junko Tanaka, Takako Iwasaki, Shigeru Hoshiko, Takashi Tsuruoka
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Patent number: 5834604Abstract: A photographic element comprising a support having situated thereon at least one silver halide emulsion layer, the element further comprising a photographic coupler represented by the formulaCOUP--(T.sup.1).sub.b --T.sup.2 --(T.sup.3).sub.c --PUGwherein the substituents are as defined in the specification.Type: GrantFiled: September 4, 1997Date of Patent: November 10, 1998Assignee: Eastman Kodak CompanyInventors: William James Begley, Frank Dino Coms, Teh-Hsuan Chen, Donald Singleton, Jr.
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Patent number: 5834521Abstract: Tetracyclic compounds having the following structure are described: ##STR1## wherein R.sub.1 -R.sub.10 are as defined. The tetracyclic compounds are capable of potent effects on steroid sensitive tissues and have demonstrated increased uterine weight, antiovulatory effects and potent steroid receptor binding. The compounds have therapeutic utility in reproductive applications such as fertility control, labor induction, ovulation induction and spermatogenesis. Methods for preparing the tetracyclic compounds from substituted indanones are also described.Type: GrantFiled: August 5, 1996Date of Patent: November 10, 1998Assignee: Ortho Pharmaceutical CorporationInventors: John H. Dodd, Lisa A. Dixon, James L. Bullington, Charles F. Schwender
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Patent number: 5817809Abstract: A photographic element comprising a support having situated thereon at least one silver halide emulsion layer, the element further comprising a photographic coupler represented by the formulaCOUP--(T.sup.1).sub.b --T.sup.2 --(T.sup.3).sub.c --PUGwhereinCOUP is a coupler moiety having a coupling site to which T.sup.1 is attached;T.sup.1 is a timing or linking group which releases from COUP during processing and which functions by electron transfer down a conjugated or unconjugated chain, or by a nucleophilic displacement reaction, to release T.sup.2 ;T.sup.2 is a triazole timing or linking group which, after release from T.sup.1, functions by a nucleophilic displacement reaction to release T.sup.3 or PUG and is represented by the formula: ##STR1## wherein ** denotes the point of attachment to T.sup.1 and *** denotes the point of attachment to T.sup.3 or PUG;R.sup.Type: GrantFiled: September 4, 1997Date of Patent: October 6, 1998Assignee: Eastman Kodak CompanyInventors: William James Begley, Frank D. Coms, Teh-Hsuan Chen
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Patent number: 5783593Abstract: The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.Type: GrantFiled: April 29, 1996Date of Patent: July 21, 1998Assignee: Abbott LaboratoriesInventors: William R. Baker, Saul H. Rosenberg, Anthony K. L. Fung, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, Stephen J. O'Connor, Rajnandan N. Prasad, Wang Shen, David M. Stout, Gerard M. Sullivan
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Patent number: 5767286Abstract: 1,4-Disubstituted-5(4H)-tetrazolinones of the formula (I) ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 have the meanings given in the specification), which are known to be useful as herbicides, can be obtained in very good yields by reacting the corresponding 1-substituted-5(4H)-tetrazolinones with the corresponding carbamoyl chlorides in the presence of 4-dimethylaminopyridine.Type: GrantFiled: September 23, 1994Date of Patent: June 16, 1998Assignee: Nihon Bayer Agrochem K. K.Inventors: Akihiko Yanagi, Yukiyoshi Watanabe, Shin-ichi Narabu
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Patent number: 5763619Abstract: Disclosed is a method for removing a protective group of an N-protected tetrazolyl compound which comprises reacting said N-protected tetrazolyl compound with a mineral acid under substantially anhydrous conditions in the presence of an alcohol, insuring a high reaction yield of the object tetrazolyl compound.Type: GrantFiled: August 16, 1996Date of Patent: June 9, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Yasushi Shida, Kokichi Yoshida
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Patent number: 5760037Abstract: These compounds correspond to the following general formula: ##STR1## where: n is 0, 1, or 2,m is are 1, 2, or 3,R, R.sub.1, R.sub.2, and R.sub.3, whether identical or different, represent an atom of hydrogen or a linear or branched alkyl radical at C.sub.1 -C.sub.4,R.sub.1 and R.sub.2, or R.sub.2 and R.sub.3 taken together can form a 5- or 6-group cycle,X and Y, whether identical or different, represent a nitrogenous aromatic heterocycle in position 2,Z.sub.1, Z.sub.2, and Z.sub.3, whether identical or different, represent an atom of hydrogen, a linear or branched alkyl radical at C.sub.1 -C.sub.4, the radical --OR.sub.4 or --NR.sub.4 R'.sub.4,R.sub.4 and R'.sub.4 represent an atom of hydrogen or a linear or branched alkyl radical at C.sub.1 -C.sub.4,and the metallic salts and complexes thereof.Use in pharmaceutical and cosmetic compositions to protect the organism from oxidizing stress situations linked to certain pathological states.Type: GrantFiled: July 23, 1996Date of Patent: June 2, 1998Assignee: L'OrealInventors: Jean-Baptiste Galey, Jacqueline Dumats
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Patent number: 5750532Abstract: The disclosed invention is compounds represented by the formula ##STR1## and pharmacetically acceptable acid salts thereof, wherein each Z is independently tetiary butyl, phenyl, naphthyl or adamantyl; substituted phenyl, wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile, nitro, phenylsulfonyl, loweralkyl-sulfonyl, oxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, lower alkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl, hydroxyiminoloweralkyl hydroxyloweralkyl or carbonyl; or 4 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen with the remaining member of the ring being at least one carbon, and optionally sulfur or oxygen,X and Y are each independently a bond, ##STR2## each Q is independently a divalent substituted or unsubstituted, straight or branched chain lower alkanediyl, lower alkanediyl-cycloalkanediyl-lower alkanediyl, lower alkenediyl, lower alkynediyl, phenylene, dihydrofuraType: GrantFiled: May 30, 1995Date of Patent: May 12, 1998Assignee: Schering CorporationInventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace
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Patent number: 5750549Abstract: The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, A, Q, W, X, Y, Z and n are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.Type: GrantFiled: October 15, 1996Date of Patent: May 12, 1998Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Ping Chen, Philippe L. Durette, Paul Finke, Jeffrey Hale, Edward Holson, Ihor Kopka, Malcolm MacCoss, Laura Meurer, Sander G. Mills, Albert Robichaud
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Patent number: 5747420Abstract: Novel herbicidal tetrazolinone derivatives of the formula ##STR1## and intermediates therefor of the formula ##STR2## wherein R.sup.1 is alkyl substituted by halogen, andR.sup.2 and R.sup.3 each independently is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or substituted phenyl, orR.sup.2 and R.sup.3 together with the N-atom to which they are attached, which may form a 5- or 6-membered heterocyclic ring.Type: GrantFiled: November 3, 1995Date of Patent: May 5, 1998Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Seishi Ito, Kazuhiro Ukawa, Yukiyoshi Watanabe, Shin-ichi Narabu, Akihiko Yanagi
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Patent number: 5705653Abstract: 3-Cyclopentylpropylazide and p-chlorosulfonylphenylisocyanate undergo cycloaddition to form 1-cyclopropyl-4-(p-chlorosulfonylphenyl) tetrazone-5-one, a key intermediate in the synthesis of an important .beta.3-agonist.Type: GrantFiled: February 4, 1997Date of Patent: January 6, 1998Assignee: Merck & Co., Inc.Inventor: Guo J. Ho
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Patent number: 5703107Abstract: The present invention is directed to a new class of 3-amido and 3-sulfamido-indolyl NMDA antagonists and their use in the treatment of a number of disease states.Type: GrantFiled: November 6, 1995Date of Patent: December 30, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Francesco G. Salituro, Bruce M. Baron
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Patent number: 5691366Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)-alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4 wherein Y is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.Type: GrantFiled: October 31, 1995Date of Patent: November 25, 1997Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
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Patent number: 5686392Abstract: The herbicidally active substituted N-carbamoyl-tetrazolinones of the formula (I) ##STR1## in which R.sup.1 represents, inter alia, an (optionally substituted) phenyl radical,R.sup.2 represents, inter alia, an alkyl radical, andR.sup.3 represents, inter alia, a cycloalkyl radical,are obtained in very good yields and at high purity--i.e. free from the isomeric O-carbamoyloxytetrazoles (Ia)--by reacting tetrazolinones of the formula (II) with carbamoyl halides of the formula (III) (X=halogen) ##STR2## in the presence of an acid acceptor and in the presence of a diluent, at temperatures of between 0.degree. C. and 200.degree. C., and either isomerizing the O-carbamoylation product of the formula (Ia), which is formed under these circumstances as a byproduct, into the desired product of the formula (I) by heating, or else converting it by hydrolysis or alcoholysis into water-soluble, and thus readily separable, components (variable (a)).Type: GrantFiled: February 1, 1996Date of Patent: November 11, 1997Assignee: Bayer AktiengesellschaftInventors: Uwe Stelzer, Wolfgang Gau, Karl-Julius Reubke
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Patent number: 5677464Abstract: A compound of the formula (V): ##STR1## wherein Ar' is a halogenated phenyl group, R is a hydrocarbon residue having a functional group at the .alpha.-carbon, R.sup.3' is an optionally substituted aliphatic or aromatic hydrocarbon residue or an optionally substituted aromatic heterocyclic group, Y and Z are, the same or different, a nitrogen atom or a methine group optionally substituted with a lower alkyl group, and (R) and (S) represent configurations, which is an optically active intermediate for production of optically active triazole compounds (I): ##STR2## wherein the symbols have the same meanings as defined above, and methods of preparing the compounds (V) and (I).Type: GrantFiled: May 30, 1995Date of Patent: October 14, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Katsumi Itoh, Akihiro Tasaka, Hiroshi Hosono
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Patent number: 5674894Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.Type: GrantFiled: May 15, 1995Date of Patent: October 7, 1997Assignee: G.D. Searle & Co.Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
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Patent number: 5668087Abstract: Herbicidal 1-alkenyltetrazolinones of the formula: ##STR1## wherein R.sup.1 represents the group: ##STR2## or the group: ##STR3## R.sup.2 and R.sup.3, independently of one another, represent C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl which may optionally be substited by methyl, C.sub.2-4 alkenyl, C.sub.2-5 alkynyl, phenyl which may optionally be substituted or aralkyl which may optionally be substituted, orR.sup.2 and R.sup.3 may optionally form, together with the N-atom to which they are bonded, a heterocyclic ring which may optionally be substituted, and novel intermediates therefor.Type: GrantFiled: March 15, 1996Date of Patent: September 16, 1997Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Yoshinori Kitagawa, Seishi Ito, Katsuhiko Shibuya, Kazuhiro Ukawa, Yoshiko Kyo, Natsuko Minegishi
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Patent number: 5654257Abstract: 1-cycloalkenyltetrazolinone derivatives of the following herbicidal formula ##STR1## R.sup.1 is cycloalkenyl which may optionally be substituted by halogen C.sub.1-4 alkyl, or bicycloalkenyl which may optionally be substituted by halogen or C.sub.1-4 alkyl, andR.sup.2 and R.sup.3 each independently is alkyl, cycloalkyl, phenyl (optionally substituted by a member selected from the group consisting of nitro, cyano, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy and alkylthio), alkenyl and alkynyl,orR.sup.2 and R.sup.3 together with the N-atom to which they are bonded form, a 5- or 6-membered heterocyclic ring which may optionally contain a further hetero atom, said heterocyclic ring optionally being benzo-condensed, or a C-.sub.Type: GrantFiled: February 15, 1996Date of Patent: August 5, 1997Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Yoshinori Kitagawa, Seishi Ito, Katsuhiko Shibuya, Tatsuya Yamaoka, Chieko Ueno, Yoshiko Kyo
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Patent number: 5654310Abstract: Triazolopyrimidines of the formula ##STR1## where A, D and X have the meanings stated in the description, and their preparation are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: June 1, 1995Date of Patent: August 5, 1997Assignee: BASF AktiengesellschaftInventors: Rainer Schlecker, Hans-Joerg Treiber, Berthold Behl, Hans Peter Hofmann
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Patent number: 5652198Abstract: Selective herbicidal tetrazolinones of the formula ##STR1## wherein X is hydrogen or halogen,Y is hydrogen or C.sub.1-4 alkyl,R.sup.1 is C.sub.1-4 alkyl, andR.sup.2 is cycloheptyl or cyclooctyl.and synergistic mixtures thereof.Type: GrantFiled: March 6, 1996Date of Patent: July 29, 1997Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Seishi Ito, Yukiyoshi Watanabe, Shin-ichi Narabu, Akihiko Yanagi
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Patent number: 5650511Abstract: Derivatives of 9-deazaguanine are prepared by reacting an aldehyde or ketone with a dialkylaminomalonate to form the corresponding enamine. The enamine is then reacted with a base to form a cyclic pyrrole. The cyclic pyrrole is reacted with an urea compound to provide a protected guanidino compound. The guanidino is converted to the desired 9-deazaguanine derivative by reacting with trifluoracetic acid or with an alkoxide or hydroxide followed by neutralization with an acid.Type: GrantFiled: December 12, 1995Date of Patent: July 22, 1997Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Arthur J. Elliott, David A. Walsh
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Patent number: 5650374Abstract: Herbicidal 1-cyclopropyl tetrazolinones of the formula ##STR1## wherein X represents C.sub.1-3 alkyl, C.sub.2-4 alkenyl or halogen,n represents 0 to 5,R.sup.1 and R.sup.2 each independently represents C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl which may optionally be substituted by C.sub.1-3 alkyl, epoxy-C.sub.3-5 alkan-1-yl, phenyl which may optionally be substituted, or aralkyl which may optionally be substituted, orR.sup.1 and R.sup.2 together with the N-atom to which they are attached, represent a cyclic ring which may be substituted, and some novel intermediates therefor.Type: GrantFiled: November 7, 1995Date of Patent: July 22, 1997Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Yoshinori Kitagawa, Seishi Ito, Katsuhiko Shibuya, Kazuhiro Ukawa, Yoshiko Kyo