Chalcogen Attached Directly To The Carbocyclic Ring Of The Quinoline Ring System By Nonionic Bonding Patents (Class 546/177)
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Patent number: 6211196Abstract: Benzyloxy-substituted, fused N-heterocycles, because of their ability to act as bradykinin receptor antagonists, have been found to be useful as therapeutics for the treatment and prevention of liver cirrhosis or Alzheimer's disease. This application describes such compounds, as well as processes for their preparation and use. The compounds according to this invention include compounds of formula (I) in which B, D, R1, and R2 have the meanings indicated herein.Type: GrantFiled: March 26, 1998Date of Patent: April 3, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Holger Heitsch, Adalbert Wagner, Klaus Wirth, Bernward Schölkens
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Patent number: 6159985Abstract: The subject invention involves compounds having the structure: wherein the C.sub..alpha. --N.sub..beta. and C.sub.5 -C.sub.6 bonds are independently single or double bonds, R1 is selected from alkyl, aryl, and heterocycle; R2-R13 are independently selected from hydrogen and other substituents; and pharmaceutically-acceptable salts thereof. The subject invention also involves pharmaceutical compositions containing such compounds, and methods for treating or preventing diseases and disorders using such compounds.Type: GrantFiled: September 21, 1999Date of Patent: December 12, 2000Assignee: The Procter & Gamble CompanyInventors: Song Liu, David Edward Portlock, Schwe Fang Pong
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Patent number: 6140341Abstract: Aminoalkyl and acylaminoalkyl ethers which are distinguished by high affinity for the bradykinin B.sub.2 receptor and improved solubility in water are described. These aminoalkyl and acylaminoalkyl ethers can be represented by the formula (I) ##STR1## in which R.sup.1,R.sup.2,R.sup.3 are alkyl, aryl, alkylaryl, halogen, hydrogen, cycloalkyl, CHO, CO--O-alkyl, COOH; R.sup.4, R.sup.5 are hydrogen, halogen, alkoxy, nitro, cyano, S-alkyl; n is a number from 1 to 8; R.sup.6 is hydrogen, alkyl, alkylalkenyl, alkylaryl; R.sup.7 is hydrogen and a substituted or unsubstituted acyl radical. A process for preparing the compounds of the formula (I) is likewise described.Type: GrantFiled: March 12, 1997Date of Patent: October 31, 2000Assignee: Hoechst AktiengesellschaftInventors: Holger Heitsch, Adalbert Wagner, Klaus Wirth, Bernward Scholkens, Gerhard Nolken
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Patent number: 6124415Abstract: What is described herein is a crosslinked polyvinylpyrrolidone (PVPP) copolymer of vinyl pyrrolidone (VP) and monomer derived from 1-vinyl-3-(E)-ethylidene pyrrolidone (EVP).Type: GrantFiled: August 4, 1999Date of Patent: September 26, 2000Assignee: ISP Investment Inc.Inventors: Edward G. Malawer, Victor Kabanov, Kolazi S. Narayanan, Michael A. Tallon, Susan Y. Tseng, Philip F. Wolf
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Patent number: 6083959Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl,R.sup.2 is hydrogen, lower alkyl or a heterocyclic group,R.sup.3 is hydrogen, lower alkyl or halogen,R.sup.4 is lower alkyl or halogen,R.sup.5 is nitro or amino substituted with substituent(s) selected from the group consisting of lower alkyl and acyl, andA is lower alkylene.Type: GrantFiled: October 26, 1998Date of Patent: July 4, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Hiroshi Kayakiri, Shigeki Satoh, Yoshito Abe, Yuki Sawada, Takayuki Inoue, Hirokazu Tanaka
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Patent number: 6063791Abstract: The present invention relates to compounds selected from the group consisting of(i) the compounds of formula I: ##STR1## in which: X is a halogen atom or a methyl group,A is a group --N(R.sub.3)CO-- or --CO--N(R.sub.3)--,B is a single bond, --CH.sub.2 -- or --CH.sub.2 --O--,R.sub.1 is H, a C.sub.1 -C.sub.3 alkyl group or a CF.sub.3 group,R.sub.2 and R.sub.3 are each independently H or a C.sub.1 -C.sub.3 alkyl group,W is CH or N, andn is 2, 3, 4 or 5; and(ii) their addition salts.It further relates to the process for their preparation and to their use in therapeutics, especially for combating pathological conditions involving bradykinin.Type: GrantFiled: May 6, 1999Date of Patent: May 16, 2000Assignee: Fournier Industrie et SanteInventors: Pierre Dodey, Michel Bondoux, Patrick Houziaux, Martine Barth, Khan Ou
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Patent number: 6011160Abstract: What is described herein is a crosslinked polyvinylpyrrolidone (PVPP) copolymer of vinyl pyrrolidone (VP) and monomer derived from 1-vinyl-3-(E)-ethylidene pyrrolidone (EVP).Type: GrantFiled: September 18, 1997Date of Patent: January 4, 2000Assignee: ISP Investments Inc.Inventors: Edward G. Malawer, Victor Kabanov, Kolazi S. Narayanan, Michael A. Tallon, Susan Y. Tseng, Philip F. Wolf
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Patent number: 5905149Abstract: Quinolylmethylen-oxindole derivatives having general formula (I), wherein R is H or --(CH.sub.2).sub.n --COR.sub.7 group in which n is an integer of 1 to 4 and R.sub.7 is hydroxy, amino, C.sub.1 -C.sub.6 alkoxy or --NR.sub.5 R.sub.6 in which one of R.sub.5 and R.sub.6 is hydrogen or C.sub.1 -C.sub.6 alkyl and the other is C.sub.1 -C.sub.6 alkyl or R.sub.5 and R.sub.6 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle or R.sub.7 is a N-terminally linked peptidyl residue containing from 1 to 3 aminoacids in which the terminal carboxyl group may be present as such, as amide, as alkali metal salt or as a C.sub.1 -C.sub.4 alkyl ester, one or two of R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are selected from: a) --X--(CH.sub.2).sub.m --NH.sub.2, --X--(CH.sub.2).sub.m --NR.sub.5 R.sub.6 or --X--(CH.sub.2).sub.m --NHR.sub.8 group; b) --NH--C(.dbd.NH)--NR.sub.5 R.sub.6, --NH--C(.dbd.NH)--NHR.sub.8, --N.dbd.CH--NH.sub.2, --N.dbd.Type: GrantFiled: January 29, 1998Date of Patent: May 18, 1999Assignee: Pharmacia & Upjohn S.p.AInventors: Carlo Battistini, Antonella Ermoli, Sergio Vioglio, Franco Buzzetti, Dario Ballinari
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Patent number: 5866295Abstract: The present invention relates to novel photosensitive quinolone compounds, specifically novel 3-diazo 2,4-quinolinedione compounds, that may be used in a variety of applications, such as, photosensitive coating compositions, pharmaceuticals, agricultural, amongst others. The invention further relates to a process for making the novel photosensitive 3-diazo 2,4-quinolinedione compounds. These compounds are particularity useful as a photoactive component in a positive working photoresist composition, particularity for use as a deep ultraviolet (UV) photoresist.Type: GrantFiled: March 7, 1997Date of Patent: February 2, 1999Assignee: Clariant Finance (BVI) LimitedInventors: Joseph E. Oberlander, Dana L. Durham, Dinesh N. Khanna
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Patent number: 5807866Abstract: A process for producing a compound of the formu5la ##STR1## comprising the step of reacting a compound of the formula ##STR2## with a compound of the formula ##STR3## to form a compound of the formula ##STR4## wherein R.sup.2a is selected from the groups recited above for R.sup.2, or R.sup.2a --X-- is a protected hydroxyl group, and Z is a group of formula --Y--R.sub.5 recited above, or a group that can be converted into a group of said formula --Y--R.sup.5. Intermediates of formula IV and composition containing substantially optically pure enantiomers of Formula (I) are included within the scope of the invention.Type: GrantFiled: November 19, 1996Date of Patent: September 15, 1998Assignees: The University of East Anglia, Eli Lilly and CompanyInventors: Nicholas James Bach, Stephen Richard Baker, Jeremy Gilmore, Russell Andrew Lewthwaite, Alexander McKillop, Jason Scott Sawyer, George Richard Stephenson, Michael William John Urquhart
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Patent number: 5756422Abstract: Substituted quinoline compounds, processes for their preparation, composition containing them, and their use as safenersCompounds of the formula I and salts thereof ##STR1## in which R.sup.1 ?lacuna! CN, C(.dbd.Z)--Q(A.sub.i X.sub.i).sub.q --R, --C(.dbd.Z)--QR*, 1,2,3,4-tetrazol-5-yl, 1,3,4-triazol-2-yl, 1,3-oxazol-2-yl,and the remaining radicals are as defined in claim 1, are suitable for use as safeners for protecting crop plants such as, for example, cereals, rice and maize, against herbicide damage.Some of the compounds are known and some are novel and they can be prepared from quinolin-8-oxy derivatives by the processes of claim 7.Type: GrantFiled: October 18, 1995Date of Patent: May 26, 1998Assignee: Hoechst Schering AgrEvo GmbHInventors: Xenia Holdgrun, Lothar Willms, Klaus Bauer, Hermann Bieringer
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Patent number: 5741789Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.Type: GrantFiled: June 6, 1995Date of Patent: April 21, 1998Assignee: Eli Lilly and CompanyInventors: David J. Hibschman, Joseph H. Krushinski, Jr., Kurt Rasmussen, Vincent P. Rocco, John M. Schaus, Dennis C. Thompson
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Patent number: 5728715Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.Type: GrantFiled: October 30, 1996Date of Patent: March 17, 1998Assignee: Rohm and Haas CompanyInventors: Enrique Luis Michelotti, Anne Ritchie Egan, Ronald Ross, Jr., Willie Joe Wilson
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Patent number: 5721255Abstract: The present invention relates to novel substituted benzylamino nitrogen containing non-aromatic heterocycles and, specifically, to compounds of the formula ##STR1## wherein W, R.sup.1, R.sup.2, R.sup.3 and A are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.Type: GrantFiled: February 15, 1995Date of Patent: February 24, 1998Assignee: Pfizer Inc.Inventors: Harry R. Howard, Masami Nakane, Masaya Ikunaka, Kunio Satake, Terry J. Rosen, John A. Lowe, III, Brian T. O'Neill, Fumitaka Ito
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Patent number: 5695684Abstract: A mesomorphic compound represented by a formula (I) containing a quinoline-2,6-diyl skeleton is suitable as a component for a liquid crystal composition providing improved response characteristics and a high contrast. A liquid crystal device is constituted by disposing the liquid crystal composition between a pair of electrode plates. The liquid crystal device may preferably be used as a display panel constituting a liquid crystal apparatus providing good display characteristics.Type: GrantFiled: March 27, 1995Date of Patent: December 9, 1997Assignee: Canon Kabushiki KaishaInventors: Yoko Kosaka, Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Shinichi Nakamura
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Patent number: 5670511Abstract: Indolepiperidine derivatives of the formula I ##STR1## and their physiologically acceptable salts exhibit action on the central nervous system, in particular dopamine-agonistic or dopamine-antagonistic action.Type: GrantFiled: January 16, 1996Date of Patent: September 23, 1997Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Joachim Marz, Hartmut Greiner, Christoph Seyfried, Gerd Bartoszyk
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Patent number: 5576437Abstract: The subject invention involves methods of treating nasal congestion comprising administration, to a human or lower animal in need of such treatment of a safe and effective amount of a compound having the following structure: ##STR1## wherein: (a) R is unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl; and(b) R' is selected from hydrogen; unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl; unsubstituted C.sub.1 -C.sub.3 alkylthio or alkoxy; hydroxy; thiol; cyano; and halo.The subject invention also involves the use of such compounds for preventing or treating other respiratory, ocular and/or gastrointestinal disorders. The subject invention also involves novel compounds having the above structure wherein R' is hydrogen or fluoro or cyano.Type: GrantFiled: August 18, 1994Date of Patent: November 19, 1996Assignee: The Procter & Gamble CompanyInventors: Thomas L. Cupps, Sophie E. Bogdan
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Patent number: 5569669Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.2', R.sub.2", R.sub.2'", R.sub.3 and n are as defined in the description, an optical isomer, and an addition salt thereof with a pharmaceutically-acceptable acid or base,and medicinal product containing the same useful for treating a mammal afflicted with a disorder associated to 5-HT.sub.1A or 5-HT.sub.2C receptors.Type: GrantFiled: March 10, 1995Date of Patent: October 29, 1996Assignee: Adir et CompagnieInventors: G erald Guillaumet, Marie-Claude Viaud, Pierre Renard, G erard Adam, Daniel-Henri Caignard, B eatrice Guardiola-Lemaitre, Marie-Claire Rettori
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Patent number: 5541199Abstract: Compounds of the formula: ##STR1## in which n is one of the integers 1, 2, 3,or 4; m is one of the integers 0 or 1; R is ##STR2## or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.Type: GrantFiled: June 2, 1995Date of Patent: July 30, 1996Assignee: American Home Products CorporationInventor: Richard E. Mewshaw
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Patent number: 5519022Abstract: The invention concerns .alpha.,.alpha.-dialkylbenzyl derivatives of the formula I ##STR1## wherein Ar.sup.1 is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;the phenylene group may optionally bear one or two substituents R.sup.3 ;each of R.sup.1 and R.sup.2, which may be the same or different is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, fluoro-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl, provided that both of R.sup.1 and R.sup.2 are not methyl or fluoromethyl; andQ is cyano, amino, nitro, formyl, (1-4C)alkoxy, thiazolyl or (2-4C)alkanoyl;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.Type: GrantFiled: November 10, 1993Date of Patent: May 21, 1996Assignees: Imperial Chemical Industries Plc, ICI PharmaInventors: Philip N. Edwards, David Waterson
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Patent number: 5492915Abstract: This invention relates to compounds having selective LTB.sub.4 antagonist properties. Therapeutic compositions comprising said compounds and methods for the treatment of disorders involving LTB.sub.4 agonist-mediated activity utilizing said compositions wherein the compounds are described by the formula ##STR1## wherein R.sub.4, X, R, Y, R', Q, m and n are herein defined, and pharmaceutically acceptable salts thereof.Type: GrantFiled: October 6, 1994Date of Patent: February 20, 1996Assignee: Rhone-Poulenc Rorer S.A.Inventors: Norbert Dereu, Wolfram Hendel, Richard Labaudiniere
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Patent number: 5488056Abstract: The present invention provides a method for treating anxiety in humans using heterocyclic compounds.Type: GrantFiled: October 31, 1994Date of Patent: January 30, 1996Assignee: Eli Lilly and CompanyInventors: Neil C. Bodick, Franklin P. Bymaster, Walter W. Offen, Harlan E. Shannon
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Patent number: 5488057Abstract: The present invention provides novel aryl- and heteroarylethenylene derivatives which are useful as tyrosine kinase activity inhibitors.Type: GrantFiled: August 23, 1994Date of Patent: January 30, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Antonio Longo, Maristella Colombo
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Patent number: 5486612Abstract: This invention relates to pharmaceutical N-benzyl dihydroindole compounds having the general formula: ##STR1## and their use as LTD.sub.4 antagonists.Type: GrantFiled: December 14, 1993Date of Patent: January 23, 1996Assignee: Eli Lilly and CompanyInventor: J. Scott Sawyer
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1,2-ethanediol derivative and salt thereof and cerebral function-improving agent comprising the same
Patent number: 5472984Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: December 29, 1993Date of Patent: December 5, 1995Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita -
Patent number: 5438141Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: May 21, 1993Date of Patent: August 1, 1995Assignee: Merck Frosst Canada, Inc.Inventors: Marc LaBell, Yves LeBlanc, Michel Belley, Erich L. Grimm, Daniel Guay, Yi B. Xiang
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Patent number: 5436344Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl, C.sub.1 to C.sub.4 alkoxy, C.sub.1 to C.sub.4 alkylthio or C.sub.1 to C.sub.6 alkyl and R.sup.2 is a group of the formula ##STR2## wherein R.sup.3 is hydrogen or C.sub.1 to C.sub.6 alkyl, R.sup.4 is --CH.dbd.C.sub.2, --CH.sub.2 --YR.sup.5, or --COR.sup.6, R.sup.5 is hydrogen or an acid labile alcohol protecting group, Y is oxygen or sulfur, and R.sup.6 is --NR.sup.7 R.sup.8 or --OR.sup.9 wherein R.sup.7, R.sup.8 and R.sup.9 are independently selected from hydrogen or C.sub.1 to C.sub.6 alkyl, or an alkaline or alkaline earth metal salt thereof, which are intermediates in the preparation of hydantoin aldose reductase inhibitors and methods of preparing these intermediates.Type: GrantFiled: March 18, 1994Date of Patent: July 25, 1995Assignee: Pfizer Inc.Inventor: George J. Quallich
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Patent number: 5407945Abstract: The invention concerns a cyclic ether derivative of the formula I ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a 9- or 10-membered bicyclic heterocyclic moiety;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar.sup.2 is optionally substituted phenylene or pyridylene;R.sup.1 includes hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl and (1-4C)alkylthio; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: July 30, 1993Date of Patent: April 18, 1995Assignees: Imperial Chemical Industries, Inc., ICI-PharmaInventors: Pierre A. R. Bruneau, Robert I. Dowell, David Waterson
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Patent number: 5380850Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.Type: GrantFiled: December 16, 1993Date of Patent: January 10, 1995Assignee: Merck Frosst Canada, Inc.Inventors: Petpiboon Prasit, Rejean Fortin, John H. Hutchinson, Michel L. Belley, Serge Leger, Richard Frenette, John Gillard
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Patent number: 5380852Abstract: Disclosed are compounds of the formula (I): ##STR1## The substituents are disclosed in the specification. The compounds are herbicidal safenets. Accordingly, processes for the preparation and use of the compounds of formula (I) are also disclosed.Type: GrantFiled: December 19, 1991Date of Patent: January 10, 1995Assignee: Hoechst AktiengesellschaftInventors: Rainer Schutze, Heinz-Josef Loher, Frank Ziemer, Klaus Bauer, Hermann Bieringer
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Patent number: 5334719Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.Type: GrantFiled: June 17, 1992Date of Patent: August 2, 1994Assignee: Merck Frosst Canada, Inc.Inventor: Richard Frenette
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Patent number: 5326766Abstract: Compounds of the formula (I): ##STR1## wherein: Het is pyridyl, pyrazinyl, pyrimidinyl, or pyridizinyl, optionally substituted with one or more groups selected from halo, lower alkyl, lower alkoxy, haloalkyl, haloalkoxy, NO.sub.2, CN, and lower alkoxy-carbonyl;Z is a C--C single bond, CH.sub.2, NH, O, S, --CH.sub.2 O--, or --OCH.sub.2 --; andthe remaining groups are as defined in the specification are useful as pesticides.Type: GrantFiled: August 19, 1992Date of Patent: July 5, 1994Inventors: Barry A. Dreikorn, Sylvester V. Kaster, Neil V. Kirby, Robert G. Suhr, Brian R. Thoreen
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Patent number: 5310743Abstract: 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalised carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.Type: GrantFiled: August 11, 1992Date of Patent: May 10, 1994Assignee: Ciba-Geigy Corp.Inventors: Walter Schilling, Silvio Ofner, Siem J. Veenstra
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Patent number: 5306820Abstract: (Quinolin-2-yl-methoxy)phenylacetic acids are known as inhibitors of enzymatic reactions in the context of arachidonic acid metabolism.Enantiomerically pure (quinolin-2-yl-methoxy)phenylacetic acids can be prepared in a simple manner and in high purity and yield by diastereoselective alkylation of corresponding (quinolin-2-yl-methoxy)phenylacetic acid menthyl esters and subsequent specific removal of the ester radical with acids.Type: GrantFiled: April 10, 1992Date of Patent: April 26, 1994Assignee: Bayer AktiengesellschaftInventors: Matthias Decker, Klaus-Helmut Mohrs, Siegfried Raddatz
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Patent number: 5296484Abstract: The compounds of the formula: ##STR1## wherein the substituents are herein below defined; are plant fungicides, insecticides, and miticides.Type: GrantFiled: March 20, 1989Date of Patent: March 22, 1994Assignee: DowElancoInventors: Michael J. Coghlan, Barry A. Dreikorn, Glen P. Jourdan, Robert G. Suhr
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Patent number: 5294622Abstract: The compounds of the formula: ##STR1## where the substituents are herein below defined, are fungicides, insecticides, and miticides.Type: GrantFiled: March 24, 1992Date of Patent: March 15, 1994Assignee: DowElancoInventors: Barry A. Dreikorn, Glen P. Jourdan, Robert G. Suhr
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Patent number: 5288749Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.Type: GrantFiled: December 20, 1991Date of Patent: February 22, 1994Assignee: Abbott LaboratoriesInventors: Michael D. Meyer, John F. DeBernardis, Rajnandan Prasad, Kevin B. Sippy, Karin R. Tietje
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Patent number: 5283245Abstract: The invention concerns a thiazole of the formula I, ##STR1## wherein Q.sup.1 is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents, or Ar is an optionally substituted 6-membered heterocyclene moiety contining up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl;R.sup.2 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl or substituted (1-4C)alkyl or R.sup.2 is optionally substituted benzoyl; andQ.sup.2 is optionally substituted thiazolyl;or a pharmaceutically-acceptable salt thereof.The invention also concerns processes for the manufacture of a thiazole of the formula I and pharmaceutical compositions containing said thiazole.Type: GrantFiled: November 18, 1991Date of Patent: February 1, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Graham C. Crawley, Martin P. Edwards
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Patent number: 5281593Abstract: A compound of the formula ##STR1## in which R.sup.1 is hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitrile, optionally protected carboxy, optionally protected tetrazolyl, trihalomethyl, hydroxy-C.sub.1-4 alkyl, aldehydo, --CH.sub.2 Z, --CH.dbd.CH--Z or --CH.sub.2 CH.sub.2 Z where Z is optionally protected carboxy or optionally protected tetrazolyl; R.sup.2 is halo, nitrile, an optionally protected acid group or --CONR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are each hydrogen or C.sub.1-4 alkyl; R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl, or C.sub.1-4 alkyl substituted by --CONR.sup.7 R.sup.8 or an optionally protected acid group; R.sup.5 is ##STR2## where W is --CH.dbd.CH--, --CH.dbd.N--, --N.dbd.CH--, --O-- or --S--, R.sup.9 is hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trihalomethyl, and R.sup.10 is hydrogen, C.sub.1-4 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.1-4 alkyl-C.sub.3-6 cycloalkyl; R.sup.6 is hydrogen or C.sub.Type: GrantFiled: April 29, 1993Date of Patent: January 25, 1994Assignee: Lilly Industries LimitedInventors: Jeremy Gilmore, Alec Todd
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Patent number: 5236919Abstract: The invention concerns a heterocycle of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents orAr is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl;and R.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 4 to 7 ring atoms, wherein A.sup.2 and A.sup.3, which may be the same or different, each is (1-4C)alkylene and X.sup.Type: GrantFiled: May 11, 1992Date of Patent: August 17, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Graham C. Crawley, Philip N. Edwards, Jean-Marc M. M. Girodeau
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Patent number: 5235055Abstract: A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido or sulfonamido, or R.sup.1 and R.sup.2 together are methylenedioxy, ethylenedioxy or propylenedioxy; R.sup.3 is hydrogen or alkyl; n is one of the integers 2, 3 or 4; or a pharmaceutically acceptable salt thereof, are antipsychotic agents.Type: GrantFiled: September 2, 1992Date of Patent: August 10, 1993Assignee: American Home Products CorporationInventors: Gary P. Stack, Magid A. Abou-Gharbia
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Patent number: 5212182Abstract: This invention relates to novel quinolinyl- and naphthalenylbenzamides or benylamines and related disclosed compounds of the formula ##STR1## wherein X is nitrogen, NO or CR.sup.1 ; Y is C(R.sup.1)(R.sup.2)O, OC(R.sup.1)(R.sup.2), C(R.sup.1)(R.sup.2)N(R.sup.3), N(R.sup.3)C(R.sup.1)(R.sup.2) or C(R.sup.1).dbd.C(R.sup.2); wherein R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen or lower alkyl containing 1 to 10 carbon atoms; Z is oxygen or (R.sup.1)(R.sup.2); R.sup.4 is R.sup.1, benzyl, benzyl ring substituted with R.sup.5, benzyl alpha monosubstituted with R.sup.1, benzyl ring substituted with R.sup.5 and alpha monosubstituted with R.sup.1, phenyl, phenylalkyl containing 2 to 10 carbon atoms in the alkyl group or phenylalkyl ring substituted with R.sup.5 and containing 2 to 10 carbon atoms in the alkyl group; wherein R.sup.5 is R.sup.1, lower alkoxy containing 1 to 10 carbon atoms, halogen, trihalomethyl, NO.sub.2, N(R.sup.1)(R.sup.2) or C(O)N(R.sup.1)(R.sup.2); R.sup.6 is R.sup.1 or R.sup.6 is C(O)(R.Type: GrantFiled: October 3, 1990Date of Patent: May 18, 1993Assignee: American Home Products CorpoorationInventors: John H. Musser, Albert J. Molinari, Dominick Mobilio
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Patent number: 5204348Abstract: Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.Type: GrantFiled: December 3, 1991Date of Patent: April 20, 1993Assignee: Mitsui Toatsu Chemicals Inc.Inventors: Nobuyuki Fukazawa, Makoto Odate, Tsuneji Suzuki, Kengo Otsuka, Takashi Tsuruo, Wakao Sato
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Patent number: 5204344Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.Type: GrantFiled: February 5, 1991Date of Patent: April 20, 1993Assignee: Merck Frosst Canada, Inc.Inventors: Petpiboon Prasit, Rejean Fortin, John H. Hutchinson, Michel L. Belley, Serge Leger, John Gillard, Richard Frenette
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Patent number: 5202349Abstract: Substituted phenylacetylenes of the formula ##STR1## wherein one of the groups R.sub.1 is a hydrogen atom and the other represents the group of the formula ##STR2## in which R.sub.3 is hydrogen, methyl or ethyl and R.sub.4 is a methyl or an amino group and wherein R.sub.2 represents mono- or binuclear aromatic or heterocyclic residues containing sulfur, nitrogen or oxygen as hetero atoms and optionally being substituted by 1 to 3 substituents as defined, which specifically inhibit 5-lipoxygenase and are useful in pharmaceutical compositions for prophylaxis and treatment of diseases due to the action of leukotrienes.The compounds may be prepared by reacting a compound of the formula ##STR3## wherein R.sub.2 has the same meaning as above and one of the groups R.sub.7 is a hydrogen atom and the other represents the group of the formula --COR.sub.3, with hydroxylamine to form the oxime which then is reduced to the corresponding hydroxylamine compound into which the group of the formula --COR.sub.4 is introduced.Type: GrantFiled: July 18, 1991Date of Patent: April 13, 1993Assignee: Gruenenthal GmbHInventors: Oswald Zimmer, Werner Vollenberg, Ulrich Seipp, Werner Englberger, Michael Haurand, Brigitte J. Bosman, Johannes Schneider
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Patent number: 5187180Abstract: (Quinolin-2-ylmethoxy)Heterotetrahydrocarbazoles as inhibitors of the biosynthesis of leukotrienes useful in the treatment of asthma and eye inflamation.Type: GrantFiled: July 12, 1991Date of Patent: February 16, 1993Assignee: Merck Frosst Canada, Inc.Inventor: John W. Gillard
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Patent number: 5180836Abstract: Disclosed are novel imidazole derivatives having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are H, alkyl, cycloalkyl, aryl, aralkyl or halogen-substituted alkyl, or R.sup.1 and R.sup.2 are combined to form a heterocyclic ring; R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are H, halogen, alkoxy, aralkyloxy, alkyl, alkoxycarbonyl, nitro, amino, acyl, fluorine substituted-alkyl, or fluorine substituted-alkoxy, or R.sup.3 is combined with R.sup.2 to form a heterocyclic ring; R.sup.8 and R.sup.9 are H, halogen, alkoxy, alkyl, alkoxycarbonyl, nitro, amino, acyl, fluorine substituted-alkyl, fluorine substituted-alkoxy, or aryl group which may have a substituent, or R.sup.8 and R.sup.9 are combined to form an alicyclic ring; R.sup.7 is, where R.sup.8 and R.sup.9 are not combined, H, and, where R.sup.8 and R.sup.9 are combined, H, alkyl which may have a substituent, aryl which may have a substituent, arylcarbonyl which may have a substituent, or a sulfur-containing heterocyclic group; and n is 0 or 1.Type: GrantFiled: November 1, 1991Date of Patent: January 19, 1993Assignee: Nippon Chemiphar Co., Ltd.Inventors: Susumu Okabe, Mitsuo Masaki, Tomio Yamakawa, Hitoshi Matsukura, Yutaka Nomura
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Patent number: 5147878Abstract: Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: ##STR1## in which: B represents a --S, --SO--, or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen such as chlorine, bromine or iodine, A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical in which the hydroxy is optionally substituted by a lower alkyl radical, Ar represents a group ##STR2## R.sub.4 denotes hydrogen or an alkyl radical and Cy represents a cyclic group.Type: GrantFiled: April 19, 1990Date of Patent: September 15, 1992Assignee: SanofiInventors: Jean Gubin, Pierre Chatelain
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Patent number: 5142060Abstract: Herbicidal substituted sulphonylaminotriazolinones of the formula ##STR1## in which R.sup.1 represents an optionally substituted radical from the group consisting of alkyl, aralkyl, aryl and heteroaryl,R.sup.2 represents hydrogen or the group --SO.sub.2 --R.sup.1 where R.sup.1 has the abovementioned meaning,R.sup.3 represents hydrogen, halogen, hydroxyl, mercapto, amino or an optionally substituted radical from the group consisting of alkyl, cycloalkyl, aralkyl, aryl, alkoxy, alkenyloxy, alkinyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkenylthio, alkinylthio, aralkoxy, aralkylthio, alkylamino and dialkylamino,R.sup.4 represents hydrogen, halogen, hydroxyl, amino or an optionally substituted radical from the group consisting of alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino and dialkylamino,X represents nitrogen or a CH group,Y represents nitrogen or a CR.sup.5 group whereR.sup.Type: GrantFiled: October 17, 1991Date of Patent: August 25, 1992Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Muller, Rolf Kirsten, Joachim Kluth, Klaus Konig, Hans-Jochem Riebel, Peter Babczinski, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
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Patent number: 5134148Abstract: The invention concerns a heterocycle of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl;and R.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 4 to 7 ring atoms, wherein A.sup.2 and A.sup.3, which may be the same or different, each is (1-4C)alkylene and X.sup.Type: GrantFiled: September 5, 1991Date of Patent: July 28, 1992Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Graham C. Crawley, Philip N. Edwards, Jean-Marc M. M. Girodeau