Bicyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 544/376)
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Patent number: 4859700Abstract: The invention relates to new 2-(2,3-dihydro-2-oxo-3-benzofuranyl)acetic acid compounds of general formula I: ##STR1## in which: R.sub.1 denotes a hydrogen atom, a linear or branched alkyl radical having 1 to 4 carbon atoms or a phenyl radical optionally substituted with a halogen atom or with an alkoxy radical containing 1 to 4 carbon atoms or an alkyl radical having 1 to 4 carbon atoms,R.sub.2 denotes a hydrogen or halogen atom, a hydroxyl radical, an alkyl radical having 1 to 4 carbon atoms or an alkoxy radical containing 1 to 4 carbon atoms,R denotes a hydroxyl radical, a linear or branched alkoxy radical having 1 to 4 carbon atoms, a benzyloxy radical or a radical of general formula A: ##STR2## in which: X and Y, which may be identical or different, each denote a linear or branched alkyl radical containing 1 to 5 carbon atoms, a radical of general formula A.sub.Type: GrantFiled: February 12, 1988Date of Patent: August 22, 1989Assignee: ADIR Et CieInventors: Gilbert Lavielle, Jean Lepagnol
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Patent number: 4855456Abstract: This invention discloses intermediates and a process for the preparation of 6-desmethyl-6-.alpha.-hydroxymethyl derivatives of lovastatin and analogs thereof at the 8-acyl side chain.Type: GrantFiled: February 29, 1988Date of Patent: August 8, 1989Assignee: Merck & Co., Inc.Inventors: Ta Jyh Lee, William F. Hoffman
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Patent number: 4851554Abstract: The disclosure relates to compounds of the formula ##STR1## and pharmaceutically acceptable addition salts thereof wherein X represents a single, direct bond or a substituted or unsubstituted alkylene chain containing 1 to 4 carbon atoms, wherein R.sub.5 is a lower alkyl group, wherein R.sub.6 is either hydrogen or methyl, wherein Am is selected from the class consisting of amino, lower mono and dialkylamino, piperidino, piperazino, N-lower alkyl piperazino, pyrrolidino, and morpholino groups, wherein Y.sub.1 and Y.sub.2 are identical and are hydrogen, a halogen, methyl or ethyl048505325 and n is an integer in the range of 1-5.Type: GrantFiled: September 30, 1987Date of Patent: July 25, 1989Assignee: University of Tennessee Research CorporationInventors: Thomas P. Kennedy, George W. Kabalka
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Patent number: 4845094Abstract: 2-phenylbenzoxepin derivatives having a hypoglycemic activity, hypotensive activity, and platelet coagulation inhibiting activity, a process for production of the derivatives, and pharmaceutical compositions containing the derivatives.Type: GrantFiled: June 19, 1987Date of Patent: July 4, 1989Assignee: Suntory LimitedInventors: Toshio Tatsuoka, Kayoko Nomura, Fumio Satoh, Takafumi Ishihara, Seiji Miyano, Kunihiro Sumoto
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Patent number: 4833142Abstract: Blood-pressure lowering compounds having a structure as shown in the accompanying formula sheets.Type: GrantFiled: November 9, 1987Date of Patent: May 23, 1989Assignee: Duphar International Research B.V.Inventors: Jan Hartog, Wouter Wouters, Lneke van Wijngaarden
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Patent number: 4812469Abstract: The invention relates to new acetamides derived from 2,3-dihydro-3-phenyl-2-benzofuranone, of general formula I ##STR1## in which: R.sub.1 denotes a hydrogen or halogen atom,R.sub.2 and R.sub.3, which may be identical or different, each denote a hydrogen atom or a linear or branched alkyl radical containing 1 to 4 carbon atoms, a benzyl radical optionally substituted with a halogen atom, with an alkoxy radical containing 1 to 4 carbon atoms or with an alkyl radical having 1 to 4 carbon atoms, or a 3,4-methylenedioxybenzyl radical, or form, together with the nitrogen to which they are attached, a 4-morpholinyl radical or a 1-piperazinyl radical.Type: GrantFiled: February 12, 1988Date of Patent: March 14, 1989Assignee: Adir Et CieInventors: Gilbert Lavielle, Jean Lepagnol
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Patent number: 4803203Abstract: Novel phenyl and heterocyclic tetrahydropyridyl and piperazinyl alkoxy benzheterocyclic compounds are described which have valuable neuroleptic properties by virture of their dopamine autoreceptor agonist activity. Methods of preparation, pharmeceutical compositions, and methods for treating psychoses, such a schizophrenia, are also described.Type: GrantFiled: June 16, 1987Date of Patent: February 7, 1989Assignee: Warner-Lambert CompanyInventors: Bradley W. Caprathe, Horace A. DeWald, Juan C. Jaen, Lawrence D. Wise
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Patent number: 4798892Abstract: The present invention relates to compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1, wherein R.sub.1, R.sub.2 and R.sub.3 may be alike or different and may be hydrogen, alkyl, alkoxyalkyl cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 membered heterocyclic group and the pharmaceutically acceptable salts thereof. The compounds exhibit beta-adrenergic blocking activity and are also useful in the treatment of glaucoma.Type: GrantFiled: April 14, 1986Date of Patent: January 17, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Sheung T. Kam, William L. Matier, Ghanshyam Patil, Khuong H. X. Mai
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Patent number: 4791104Abstract: The invention is concerned with dihydrobenzothiophene and thiochromane derivatives of the generic formula ##STR1## The compounds show anti-hypertensive, platelet aggregation inhibiting, hypolipemic, antianoxic spasmolytic, anthithrombotic, calcium antagonizing and neuroleptic activity.Type: GrantFiled: December 10, 1986Date of Patent: December 13, 1988Assignee: Maggioni-Winthrop S.p.A.Inventors: Giampaolo Picciola, Mario Riva, PierGiuseppe De Meglio, Piergiorgio Gentili
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Patent number: 4788192Abstract: Novel 2-sulfamoylbenzo[b]thiopenes and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.Type: GrantFiled: March 12, 1987Date of Patent: November 29, 1988Assignee: Merck & Co., Inc.Inventors: Kenneth L. Shepard, Samuel L. Graham
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Patent number: 4782061Abstract: The invention relates to a group of new bicyclic heteroarylpiperazine derivatives of formula 1. It was found that these compounds have interesting psychotropic in particular anti-psychotic properties.The compounds can be prepared according to methods known for the synthesis of analogous compounds.Type: GrantFiled: December 18, 1985Date of Patent: November 1, 1988Assignee: Duphar International Research B.V.Inventors: Cornelis G. Kruse, Johannes A. M. van der Heyden, Ineke van Wijngaarden, Jan Hartog, Berend Olivier
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Patent number: 4780466Abstract: There are disclosed compounds of the formula ##STR1## wherein the group A is ##STR2## where R.sub.1 and R.sub.2 are each independently hydrogen or loweralkyl, or R.sub.1 +R.sub.2 =(CH.sub.2).sub.m, m being 2 to 6, p is 1 or 2, and each X is independently hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, amino, loweralkylamino, diloweralkylamino, trifluoromethyl or loweralkylthio; W is O, H.sub.2 or [H, OH]; n is 2, 3 or 4; and R.sub.3 is ##STR3## where q is 1 or 2 and each Y is independently hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, amino, loweralkylamino, diloweralkylamino, trifluoromethyl or loweralkylthio, which are useful as antipsychotic, anxiolytic and analgesic agents.Type: GrantFiled: March 17, 1988Date of Patent: October 25, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Nicholas J. Hrib, John G. Jurcak
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Patent number: 4777252Abstract: Antibacterial activity is exhibited by 3-acylamino-2-oxoazetidines having in the 1-position an activating group of the formula ##STR1## wherein R is ##STR2## and R.sub.Type: GrantFiled: August 13, 1987Date of Patent: October 11, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: William A. Slusarchyk, Peter H. Ermann
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Patent number: 4772622Abstract: Novel diamino oxadiazoles, wherein one of the amine functions is connected to a basicly-substituted heterocyclic group through a linear or cyclic connecting group, which are useful for the suppression of gastric acid secretions in mammals. Compositions employing these compounds and processes for the preparation of such compounds from known N-cyano-S-methylisothiourea precursors by treatment with hydroxylamine and for alkylation of amine groups are also disclosed.Type: GrantFiled: June 16, 1986Date of Patent: September 20, 1988Assignee: Merck & Co., Inc.Inventors: Susan F. Britcher, William C. Lumma, Jr.
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Patent number: 4751230Abstract: The invention relates to 2,3-dihydrobenzofuran derivatives of the general formula: ##STR1## in which: each of X.sub.1 and X.sub.2, which are identical or different, represents a hydrogen or halogen atom or an alkoxy radical containing from 1 to 4 carbon atoms,X.sub.3 represents a hydrogen atom or an alkyl radical having from 1 to 4 carbon atoms,Y represents a hydrogen atom or a hydroxy radical, each of R.sub.1 and R.sub.2, which are identical or different, represents an alkyl radical having from 1 to 4 carbon atoms,or R.sub.1 represents a methyl radical and R.sub.2 represents a phenylalkyl grouping or a 2-indanyl grouping, each of which may be substituted or unsubstituted,or R.sub.1 and R.sub.2 together form, with the nitrogen atom to which they are attached, a piperazinyl radical, a tetrahydroisoquinolyl radical, a morpholinyl radical or a tetrahydrothienopyridinyl radical.Type: GrantFiled: July 16, 1987Date of Patent: June 14, 1988Assignee: ADIR et CompagnieInventors: Gilbert Lavielle, Yves-Michel Gargouil, Jean-Paul Vilaine
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Patent number: 4748173Abstract: Heterocyclic aminoalkyl esters of mycophenolic acid, and the derivatives and pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.Type: GrantFiled: September 23, 1987Date of Patent: May 31, 1988Assignee: Syntex (U.S.A.) Inc.Inventors: Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
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Patent number: 4736031Abstract: Novel condensed seven-membered heterocyclic compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy,R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom,X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated,Y is >C.dbd.O or >CH--OR.sub.5 in which R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl,A is oxygen atom or sulfur atom, E is oxygen atom or methylene, andG is lower alkylene, provided that when A is sulfur atom, E is methylene,and salts thereof exhibit serotonin S.sub.Type: GrantFiled: April 15, 1986Date of Patent: April 5, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Minoru Hirata
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Patent number: 4728650Abstract: There are provided novel 3,4-dihydrobenzopyran derivatives having anti-peptic ulcer, antitussive and/or expectorant activity. Also provided are medicinal uses of said 3,4-dihydrobenzopyran derivatives.Type: GrantFiled: May 13, 1986Date of Patent: March 1, 1988Assignee: Kuraray Co., Ltd.Inventors: Katsushi Eziri, Koichi Kanehira, Manzo Shiono, Yoshiji Fujita, Johji Yamahara
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Patent number: 4727069Abstract: Heterocyclic aminoalkyl esters of mycophenolic acid, and the derivatives and pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.Type: GrantFiled: January 30, 1987Date of Patent: February 23, 1988Assignee: Syntex (U.S.A.) Inc.Inventors: Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
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Patent number: 4713393Abstract: Phenylalkyl-2,3-dihydrobenzofurans and analogs were prepared by (1) nucleophilic substitution involving an appropriately substituted 2,3-dihydrobenzofuranol (or 2,3-dihydrobenzopyranol) and a cinnamylhalide followed by reduction; or (2) by Wittig reaction involving a halomethyl derivative of 2,3-dihydrobenzofuran (or 2,3-dihydrobenzopyran and an aryl or a heteroaryl aldehyde followed by reduction. These compounds were found to be potent anti-inflammatory agents.Type: GrantFiled: April 25, 1985Date of Patent: December 15, 1987Assignee: Merck & Co., Inc.Inventors: Michael N. Chang, Kathryn L. Thompson, David A. Boulton
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Patent number: 4711960Abstract: Isochromans, isothiochromans, 2-benzoxepins and 2-benzothiepins are described. The compounds possess hypotensive and anti-psychotic properties; methods and compositions using them are described.Type: GrantFiled: January 28, 1986Date of Patent: December 8, 1987Assignee: The Upjohn CompanyInventor: John M. McCall
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Patent number: 4707550Abstract: The synthesis of thienopyrimidine-2,4-dione derivatives and their urea intermediates is described. The novel urea intermediates and thienopyrimidine-2,4-dione derivatives are general vasodilating agents and anti-hypertensive agents. The compounds are useful as cardiovascular agents.Type: GrantFiled: January 21, 1987Date of Patent: November 17, 1987Assignee: Ortho Pharmaceutical CorporationInventors: Jeffery B. Press, Ronald K. Russell
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Patent number: 4704462Abstract: Substituted 2,3,3a,6-tetrahydro-6-oxobenzofuran derivatives have been prepared. These neolignans are found to have potent and specific PAF (Platelet-Activating-Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by PAF, for example, pain, fever, inflammation, cardiovascular disorder, asthma, lung edema, allergic disorders, skin diseases, psoriasis, toxic shock syndrome and adult respiratory distress syndrome.Type: GrantFiled: August 22, 1985Date of Patent: November 3, 1987Assignee: Merck & Co., Inc.Inventors: Michael N. Chang, San-Bao Hwang, Mitree M. Ponpipom, Robert L. Bugianesi
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Patent number: 4704390Abstract: Novel phenyl and heterocyclic tetrahydropyridyl and piperazinyl alkoxy benzheterocyclic compounds are described which have valuable neuroleptic properties by virtue of their dopamine autoreceptor agonist activity. Methods of preparation, pharmaceutical compositions, and methods for treating psychoses, such as schizophrenia, are also described.Type: GrantFiled: November 5, 1986Date of Patent: November 3, 1987Assignee: Warner-Lambert CompanyInventors: Bradley W. Caprathe, Horace A. DeWald, Juan C. Jaen, Lawrence D. Wise
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Patent number: 4701456Abstract: Aminoalkyoxybenzopyranones of the formula ##STR1## wherein R.sub.1 is of the formula ##STR2## are described as well as methods of preparation, pharmaceutical compositions and methods for treating anxiety and psychoses such as schizophrenia therewith.Type: GrantFiled: June 18, 1985Date of Patent: October 20, 1987Assignee: Warner-Lambert CompanyInventors: Horace A. Dewald, Lawrence D. Wise, Thomas G. Heffner
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Patent number: 4678787Abstract: Novel 4H-1-benzopyran-4-ones and their sulfur containing analogs are disclosed which are efficacious for the treatment of psychosis including schizophrenia.Type: GrantFiled: November 22, 1985Date of Patent: July 7, 1987Assignee: Warner-Lambert CompanyInventors: Juan C. Jaen, Lawrence D. Wise
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Patent number: 4675320Abstract: Antimicrobial 2-nitro-3-phenylbenzofurans wherein the benzo or the 3-phenyl portion of the molecule is bonded to an alkylene or an oxyalkylene group which is in turn bonded to a basic nitrogen atom or to the nitrogen atom of an (N-lower alkanoyl)amino group.Type: GrantFiled: May 15, 1985Date of Patent: June 23, 1987Assignee: Riker Laboratories, Inc.Inventors: Robert A. Scherrer, Richard M. Stern, Walton J. Hammar
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Patent number: 4672062Abstract: 3-amino-2,3-dihydro-1-benzoxepine compounds corresponding to the general Formula I ##STR1## wherein R.sub.1 and R.sub.2 may each be hydrogen, halogen, lower alkyl or lower alkoxy, or if one of R.sub.1 and R.sub.2 is hydrogen, the other may also be nitro or trifluoromethyl, R.sub.3 represents hydrogen or a lower alkyl group which optionally may be substituted by hydroxy, lower alnoxy, an optionally substituted phenyl group or an optionally substituted amino group, and R.sub.4 represents hydrogen or lower alkyl, or R.sub.3 and R.sub.4 together with the nitrogen atom form a 5 or 6 member heterocycle. The compounds exhibit pharmacological, especially antidepressive, activity.Type: GrantFiled: November 4, 1985Date of Patent: June 9, 1987Assignee: Kali-Chemie Pharma GmbHInventors: Heinrich-Wilhelm Ohlendorf, Michael Ruhland, Klaus-Ullrich Wolf
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Patent number: 4670560Abstract: The synthesis of thienopyrimidine-2,4-dione derivatives and their urea intermediates is described. The novel urea intermediates and thienopyrimidine-2,4-dione derivatives are generally vasodilating agents and anti-hypertensive agents. The compounds are useful as cardiovascular agents.Type: GrantFiled: April 28, 1986Date of Patent: June 2, 1987Assignee: Ortho Pharmaceutical CorporationInventors: Jeffery B. Press, Ronald K. Russell
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Patent number: 4670439Abstract: The present invention provides 2H-1-benzopyran-2-one derivatives of the general formula: ##STR1## wherein either R.sub.1 is a lower alkyl radical, optionally substituted by phenyl, which can be substituted by lower alkyl, lower alkoxy, hydroxyl or halogen, and R.sub.2 is trifluoromethyl, cyano, hydroxymethyl, alkoxymethyl, acyloxymethyl, halogenomethyl, aminomethyl, mono- or dialkylaminomethyl, acyl, carboxyl, alkoxycarbonyl or carbamoyl, which can be mono- or disubstituted by lower alkyl; or R.sub.1 is trifluoromethyl, cyano, hydroxymethyl, alkoxymethyl, acyloxymethyl, halogenomethyl, aminomethyl, mono- or dialkylaminomethyl, acyl, carboxyl, alkoxycarbonyl or carbamoyl, which can be mono- or disubstituted by lower alkyl, and R.sub.2 is a lower alkyl radical, optionally substituted by phenyl, which can be substituted by lower alkyl, lower alkoxy, hydroxyl or halogen, and R.sub.Type: GrantFiled: July 16, 1985Date of Patent: June 2, 1987Assignee: Boehringer Mannheim GmbHInventors: Ernst-Christian Witte, Peter Neubert, Androniki Roesch
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Patent number: 4670569Abstract: The present invention relates to 5-fluoro-PGI.sub.2 derivatives of Formula I. These compounds are useful for the treatment of platelet dysfunction. Also disclosed is the process for preparing them and the appropriate intermediates.Type: GrantFiled: March 8, 1985Date of Patent: June 2, 1987Assignee: G. D. Searle & Co.Inventors: Leonard N. Nysted, Raphael Pappo
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Patent number: 4670041Abstract: Compounds of the formula ##STR1## wherein X is (--CR.sub.4 R.sub.4 --).sub.m in which m is 0 or 1;Y is (--CR.sub.5 R.sub.6 --).sub.n in which n is 0, 1 or 2;Z is (--CR.sub.7 R.sub.7 --).sub.p in which p is 1, 2, or 3; the sum of m+n+p is an integer of 2 to 5, inclusive;R.sub.2 and R.sub.3 each is H or alkyl, and the like;R.sub.1 is H or alkyl; andW is an unsaturated moiety, are useful as plant growth regulators and herbicides.Type: GrantFiled: September 13, 1982Date of Patent: June 2, 1987Assignee: E. I. du Pont de Nemours and CompanyInventors: George B. Payne, Samuel B. Soloway, James E. Powell, Steven A. Roman, Willy D. Kollmeyer
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Patent number: 4665097Abstract: Novel bicyclooxyaryl thioureas are provided together with methods for their preparation and use as the active toxicant in pesticidal compositions.Type: GrantFiled: March 31, 1983Date of Patent: May 12, 1987Assignee: Union Carbide CorporationInventor: Paul A. Cain
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Patent number: 4659737Abstract: Substituted benzopyrans of the formula ##STR1## in which --A-- is a single or double bond,X is a direct bond, optionally substituted methylene, oxygen or optionally substituted --NH--, and the various other radicals can have various meanings,or pharmaceutically acceptable addition salts thereof, which possess anti-hypertensive activity.Type: GrantFiled: March 25, 1985Date of Patent: April 21, 1987Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Kabbe, Ulrich Niewohner, Arno Widdig, Andreas Knorr, Bernward Garthoff, Stanislav Kazda
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Patent number: 4652566Abstract: A [2-hydroxy-3-(4-phenylpiperazinyl)propoxy]benzofuran derivative having the formula (I): ##STR1## wherein X is acetyl, carbamoyl, cyano, a lower alkoxycarbonyl, carboxyl or 1-hydroxyethyl group, R is hydrogen atom, a lower alkoxy group, a lower alkyl group or a halogen atom; R is attached to an arbitrary position of ortho-position, meta-position and para-position to N-phenyl group, and a group having the formula: ##STR2## is attached to an arbitrary position of 4, 5, 6 and 7 positions to benzofuran ring or the salt thereof, a process for preparing the same and an antihypertensive agent containing the same as an effective component. The benzofuran derivative has a strong .alpha.-adrenergic blockade effect and calcium antagonistic effect with a more decreased side-effect.Type: GrantFiled: March 19, 1985Date of Patent: March 24, 1987Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Jun Nakano, Michiko Nagahara, Mitsuo Hayashida, Yuji Suzuki, Yohichi Maruyama
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Patent number: 4652649Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## wherein the substituents are defined hereinbelow.Type: GrantFiled: February 20, 1985Date of Patent: March 24, 1987Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
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Patent number: 4634768Abstract: This invention relates to derivatives of 3-methylflavone-8-carboxylic acid represented by the formula (1) ##STR1## wherein R represents a hydrogen atom, a lower alkyl group or a group ##STR2## (wherein R.sup.1 and R.sup.2 represent a lower alkyl group or R.sup.1 and R.sup.2, when taken together with the nitrogen atom to which they are attached, may form a heterocyclic ring with or without an intervening hetero atom, and n is an integer of 1 to 4), and X represents a halogen atom, which are useful as intermediates.This invention also relates to processes for preparing the same.Type: GrantFiled: April 4, 1985Date of Patent: January 6, 1987Assignees: Yamamoto Chemical Industrial Co., Ltd., Osaka Municipal GovernmentInventors: Hiroshige Inoue, Kenichi Fukushima, Ikuzo Nishiguchi
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Patent number: 4631282Abstract: Antihypertensive compounds of formula (I): ##STR1## wherein the various substituents are defined hereinbelow.Type: GrantFiled: June 20, 1985Date of Patent: December 23, 1986Assignee: Beecham Group PlcInventor: Frederick Cassidy
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Patent number: 4623486Abstract: Certain novel p-aminomethylbenzoyl derivatives of 4-hydroxy-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide and several other closely-related known oxicams have been prepared. These particular compounds are useful in therapy as prodrug forms of the known anti-inflammatory and analgesic oxicams. Preferred member compounds include 2-methyl-4-[4-(morpholinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-benzoth iazine-3-carboxamide 1,1-dioxide, 2-methyl-4-[4-(piperidinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-benzoth iazine-3-carboxamide 1,1-dioxide, 2-methyl-N-(6-methyl-2-pyridinyl)-4-[4-(piperidinomethyl)benzoyloxy]-2H-1, 2-benzothiazine-3-carboxamide 1,1-dioxide, 2-methyl-4-[4-(4-methylpiperazinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2 -benzothiazine-3-carboxamide 1,1-dioxide and 2-methyl-4-[4-(pyridiniummethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-benzoth iazine-3-carboxamide 1,1-dioxide chloride. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: May 29, 1985Date of Patent: November 18, 1986Assignee: Pfizer Inc.Inventor: Joseph G. Lombardino
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Patent number: 4616035Abstract: Combating pests such as insects, arachnids and nematodes with novel N-oxalyl-N-methylcarbamic acid esters of the formula ##STR1## in which R represents alkyl, alkenyl, alkinyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenalkylthio, halogen, nitro, dialkylamino, alkylsulphinyl, alkylsulphonyl, cycloalkyl or a saturated, optionally substituted heterocyclic radical with one or more hetero-atoms from the group comprising O, S and N, or forms a ring which is fused onto the phenyl radical, optionally contains one or more hetero-atoms from the group comprising O, S and N and is optionally substituted.Type: GrantFiled: October 15, 1984Date of Patent: October 7, 1986Assignee: Bayer AktiengesellschaftInventors: Gerhard Heywang, Engelbert Kuhle, Bernhard Homeyer
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Patent number: 4605740Abstract: The present invention relates to a process for the production of N-substituted acrylic acid amides by conversion of 2-carboalkoxy-t-oxabicyclo(2,2,1)hept-5-enes with primary or secondary amines to 2-carboxamide-7-oxabicyclo(2,2,1)hept-5-enes and the thermal decomposition of the latter, preferably in the presence of Lewis acids and in a vacuum, to furane and N-substituted acrylic acid amides. The process according to the invention results in high purity N-substituted acrylic acid amides that are, in the main, free of bifunctional monomers which would disrupt the subsequent polymerization of the N-substituted acrylic acid amides by undesired cross-linking.Type: GrantFiled: September 22, 1983Date of Patent: August 12, 1986Assignee: Chemische Fabrik Stockhausen GmbHInventor: Alfons Landscheidt
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Patent number: 4604392Abstract: A 2-substituted benzofuran derivative of general formula I or II ##STR1## in which R.sub.1 and R.sub.2, can be the same or different, and are a hydrogen atom, a halogen atom, an alkyl group containing 1 to 4 carbon atoms, an arylalkyl group, an aryl group, a hydroxyl group, an alkoxy group, or an NH.sub.2, NH-alkyl, N(alkyl).sub.2, NH(CO-alkyl), NH(CO-aryl) or NO.sub.2 group, or R.sub.1 and R.sub.2 can together form a ring of 5-8 carbon atoms; R.sub.3 is a hydrogen atom, an alkyl group containing 1 to 4 carbon atoms or an aryl group; R.sub.4 is a hydrogen atom, an alkyl group, an aryl or an arylalkyl group, R.sub.5 is a hydroxyl group, an alkoxy group, an OCO-alkyl, an OCO-aryl, OCOHN-alkyl or OCONH-aryl group, ##STR2## where n is a number between 1 and 4, R.sub.7 is a hydrogen atom or an alkyl group containing 1 to 4 carbon atoms, and R.sub.8 and R.sub.Type: GrantFiled: August 17, 1984Date of Patent: August 5, 1986Assignee: A. Menarini S.A.S.Inventors: Vittorio Pestellini, Mario Ghelardoni, Carlo Alberto Maggi, Gabrio Roncucci, Alberto Meli
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Patent number: 4596876Abstract: Novel adducts of phthalaldehyde are disclosed, as well as imaging compositions and imaging elements incorporating them. A method is also disclosed for minimizing dimensional changes in the element during processing.Type: GrantFiled: September 14, 1983Date of Patent: June 24, 1986Assignee: Eastman Kodak CompanyInventors: Thap DoMinh, Max H. Stern
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Patent number: 4590193Abstract: This invention relates to 3-(2-(4-phenylpiperazinylethyl)anilino)-isobenzofuranones, their method of preparation and their use in the treatment of conditions such as hypertension, and allergies.These compounds are characterized by the formula: ##STR1## in which R.sub.1 may be one or more substituents located at the ortho, meta, or para positions selected from the group of H, CH.sub.3, CF.sub.3, F, Cl and OCH.sub.3 ; R.sub.2 and R.sub.3 are the same or different and are H or OCH.sub.3. These compounds are in the form of free bases or their pharmaceutically safe salts. They can be obtained by a reaction between a 2-(phenylpiperazinylethyl) aniline and an aromatic aldehyde having an acid function at the ortho position of the carboxaldehyde function.These derivatives are useful for the treatment of hypertension and allergic conditions.Type: GrantFiled: July 27, 1983Date of Patent: May 20, 1986Assignee: Societe Cortial, S.A.Inventors: Marie-Helene Creuzet, Claude Feniou, Francoise Guichard, Gisele Prat, Henri Pontagnier
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Patent number: 4577021Abstract: 1H-2-benzopyran-1-yl alkyl or 1-(isochroman-1-yl) alkyl 4-phenyl piperazines are prepared and exhibit antipsychotic and hypotensive activity.Type: GrantFiled: April 1, 1985Date of Patent: March 18, 1986Assignee: The Upjohn CompanyInventor: John M. McCall
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Patent number: 4563458Abstract: The invention relates to substituted 4-aminomethylene-chromans and chromens of Formula (I) infra, as well as methods for making of said chromans and chromens, compositions containing said chromans and chromens and methods for the use of said chromans, chromens and compositions containing said chromans and chromens. The compounds and compositions of the invention are useful for their circulation influencing activity.Type: GrantFiled: December 13, 1983Date of Patent: January 7, 1986Assignee: Bayer AktiengesellschaftInventors: Arno Widdig, Hans-Joachim Kabbe, Andreas Knorr, Ulrich Benz
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Patent number: 4563527Abstract: Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.Type: GrantFiled: July 19, 1984Date of Patent: January 7, 1986Assignee: Torii & Co., Ltd.Inventors: Setsuro Fujii, Toyoo Nakayama, Shigeki Nunomura, Kimio Sudo, Shin-ichi Watanabe, Toshiyuki Okutome, Yojiro Sakurai, Masateru Kurumi, Takuo Aoyama
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Patent number: 4558043Abstract: Benzofurans or 2,3-dihydrobenzofurans of the formula ##STR1## in which R.sub.1 represents hydrogen or an aliphatic radical,R.sub.2 represents an amino group disubstituted by a bivalent aliphatic radical which is optionally interrupted by at least one hetero atom,and the aromatic ring may be additionally substituted,and the salts thereof, have anti-inflammatory and/or analgesic activities.Type: GrantFiled: July 11, 1984Date of Patent: December 10, 1985Assignee: Ciba Geigy CorporationInventors: Paul Wenk, Werner Breitenstein, Marcus Baumann
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Patent number: 4556656Abstract: Isochromans, isothiochromans, 2-benzoxepins, and 2-benzothiepins are described. The compounds possess hypotensive and anti-psychotic properties; methods and compositions using them are described.Type: GrantFiled: April 4, 1979Date of Patent: December 3, 1985Assignee: The Upjohn CompanyInventor: John M. McCall
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Patent number: 4546177Abstract: The present invention provides novel 1-(6-hydroxy-4- or 7-methoxy or 4,7-dimethoxy-5-benzofuranyl)-4-substituted-1,3-butanediones which are useful as intermediates in the synthesis of khellin and related anti-atherosclerotic furochromones.Type: GrantFiled: April 24, 1984Date of Patent: October 8, 1985Assignee: The Upjohn CompanyInventor: Ronald B. Gammill