Double Bonded Divalent Chalcogen Containing Patents (Class 544/52)
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Patent number: 4666909Abstract: Compounds of the formula: ##STR1## wherein, R is H, alkyl, cycloalkyl, aryl or heteroaryl;R.sub.1 is H, alkyl, cycloalkyl, aryl, heteroaryl, substituted heteroaryl, aralkyl, substituted aryl, halo, OR.sup.2, SR.sup.2, NR.sub.2, CF.sub.3, NO.sub.2, CN, COOR.sup.2, CHO, SO.sub.3 H or SO.sub.2 NH.sub.2,whereinR.sup.2 is H, methyl, ethyl or propyl;Y is ##STR2## Z is O, S, NH or CH.sub.2 ; X is ##STR3## wherein R.sup.2 is H, methyl, ethyl or propyl;n is 1-10, and pharmaceutically acceptable salts thereof have antiallergy and antiinflammatory activity.Type: GrantFiled: September 16, 1985Date of Patent: May 19, 1987Assignee: USV Pharmaceutical Corp.Inventors: Howard Jones, Ernest Magnien, John H. Musser, Mujahid L. Shaikh
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Patent number: 4640916Abstract: 1,4-Benzothiazine derivatives of the formula; ##STR1## wherein R.sup.1 and R.sup.2 independently stand for hydrogen, halogen, a lower alkyl group, a lower alkoxy group or trifluoromethyl group, or R.sup.1 and R.sup.2, taken together, form a 5-7 membered ring represented by ##STR2## wherein n is an integer of 3 to 5 or a 5-6 membered ring represented by ##STR3## wherein m is 1 or 2, R.sup.3 and R.sup.4 independently stand for hydrogen, halogen, a lower alkyl group, a lower alkoxy group or trifluoromethyl group, R.sup.5 stands for hydrogen or a lower alkyl group, and A stands for an alkylene group or pharmaceutically acceptable salts thereof, are useful as prophylactic or therapeutic drugs for, among others, hypertension and ischemic cardiovascular diseases.Type: GrantFiled: November 27, 1985Date of Patent: February 3, 1987Assignee: Takeda Chemical Industries, Ltd.Inventors: Kanji Meguro, Kohei Nishikawa
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Patent number: 4621084Abstract: New imidazo-heterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or halogen,R.sup.2 is hydrogen, lower alkyl, halogen, aminomethyl optionally substituted with lower alkyl, or piperazin-1-yl-methyl optionally substituted with lower alkyl,R.sup.3 is a partially suturated heterocyclic group selected from benzothiazolinyl, benzoxazolinyl, benzimidazolinyl, 3,4-dihydro-2H-1,4-benzothiazinyl, 3,4-dihydro-2H-1,4-benzoxazinyl and 1,2,3,4-tetrahydroquinoxalinyl, which is substituted with oxo, thioxo, imino or lower alkylimino, and which may be substituted with lower alkyl optionally substituted with lower alkanoyloxy, lower alkoxycarbonyl, pyridyl or lower alkylamino; or an unsaturated heterocyclic group selected from benzoxazolyl and benzimidazolyl, which may be substituted with lower alkyl or pyridyl(lower)alkylthio, andY is .dbd.N-- or a group of the formula: ##STR2## in which R.sup.Type: GrantFiled: February 27, 1984Date of Patent: November 4, 1986Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Hisashi Takasugi
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Patent number: 4618361Abstract: The acylamide derivatives of the formula I below are suitable for use as a counter-agent, "antidote" or "safener" for protecting cultivated plants against the phytotoxic action of herbicides. Crops suitable in this respect are preferably millet, cereals, rice, maize and soya, and suitable herbicides are chloroacetanilides and thiolcarbamates.The acylamide derivatives have the formula I ##STR1## in which X is oxygen, sulfur, --SO-- or --SO.sub.2 --; R.sup.1 is C.sub.1 -C.sub.6 - halogenoalkyl, C.sub.1 -C.sub.6 -cyanoalkyl or C.sub.2 -C.sub.6 -halogenoalkenyl; R.sup.2 and R.sup.5 independently of one another are hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -halogenoalkyl, C.sub.2 -C.sub.4 -alkenyl, C.sub.2 -C.sub.4 -alkynyl or C.sub.2 -C.sub.4 -alkoxyalkyl; R.sup.3 and R.sup.4 independently of one another are hydrogen, C.sub.2 -C.sub.4 -alkenyl, C.sub.2 -C.sub.4 -alkynyl, cyano, C.sub.2 -C.sub.4 -alkoxyalkyl, --COOR.sup.8, --CO--NR.sup.9 R.sup.10 or C.sub.1 -C.sub.Type: GrantFiled: December 12, 1983Date of Patent: October 21, 1986Assignee: CIBA-GEIGY CorporationInventor: Hans Moser
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Patent number: 4612312Abstract: Glutarimide derivatives of the formula which are useful antihypertensive and antianxiety agents ##STR1## wherein R.sub.1 and R.sub.2 each independently represent hydrogen, a 1 to 4 carbon alkyl, a 1 to 4 carbon alkoxy, halogen, nitro, hydroxy, SO.sub.3 H, SO.sub.2 NH.sub.2, and when R.sub.1 and R.sub.2 are taken together, form a fused phenyl group at the 1,2- or 3,4- positions, with the proviso that when R.sub.1 and R.sub.2 are identical they each represent a hydrogen, a 1 to 4 carbon alkyl, a 1 to 4 carbon alkoxy, hydroxy or a halogen group; A and B independently represent an oxo, a thio or an imino group having the formula --N(R.sub.6)-- wherein the R.sub.6 group is hydrogen or a 1 to 4 carbon alkyl group; R.sub.3 is a hydrogen, a 1 to 4 carbon alkyl or hydroxyethyl group; n is an integer of from 2 to 5; and R.sub.4 and R.sub.5 represent methyl groups or when taken together form a cyclopentane or cyclohexane ring; its enantiomers; and the pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: June 13, 1985Date of Patent: September 16, 1986Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Marcel Hibert, Maurice W. Gittos
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Patent number: 4595685Abstract: Benzothiazine derivatives of the formula I ##STR1## with (R(1), R(1)', R(1)", R(4) and R(4)' equal to hydrogen, alkyl, alkoxy, halogen, nitro, hydroxyl, acetamido or amino; R(2) equal to hydrogen, alkyl, alkenyl, phenyl; R(3) equal to hydrogen, alkyl, alkenyl, phenyl; R(5) equal to hydrogen or (C.sub.1 -C.sub.Type: GrantFiled: December 21, 1984Date of Patent: June 17, 1986Assignee: Hoechst AktiengesellschaftInventors: Rainer Henning, Ulrich Lerch, Joachim Kaiser
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Patent number: 4584300Abstract: This invention relates to benzothiazine derivatives represented by the formula [I] and salts thereof, which are useful for treatment of cardiovascular diseases.Type: GrantFiled: January 17, 1984Date of Patent: April 22, 1986Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Jun-ichi Iwao, Tadashi Iso, Masayuki Oya
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Patent number: 4576942Abstract: Compounds of the formulae ##STR1## wherein, A is benzo, pyrido, thieno, pyrazolo, imidazo, pyrimido, isoxazolo, thiazolo, furo or pyrrolo;X is O, S, SO or SO.sub.2 ;R.sub.1 is H, alkyl, aryl, OH, OR, aryloxy, halogen, amino, nitro, cyano, COOR, trihalomethyl, ##STR2## R.sub.2. R.sub.3, R.sub.4 and R.sub.5 are identical or different and each represent H, alkyl, aryl, OH, OR, amino, alkylamino, dialkylamino, COOR, thio, alkylthio, cyano, or halogen; and n is 1-2; and pharmaceutically acceptable salts thereof having anti-allergy and anti-inflammatory activity.Type: GrantFiled: July 12, 1984Date of Patent: March 18, 1986Assignee: USV Pharmaceutical Corp.Inventor: Raymond D. Youssefyeh
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Patent number: 4552876Abstract: Compounds of the formula: ##STR1## wherein, R is H, alkyl, cycloalkyl, aryl, or heteroaryl;R.sub.1 is H, alkyl, cycloalkyl, aryl, heteroaryl, substituted heteroaryl, aralkyl, substituted aryl, halo, OR.sup.2, SR.sup.2, NR.sub.2, CF.sub.3, NO.sub.2, CN, COOR.sup.2, CHO, SO.sub.3 H or SO.sub.2 NH.sub.2,whereinR.sup.2 is H, methyl, ethyl or propyl;Y is ##STR2## Z is O, S, NH or CH.sub.2 ; X is --CH.sub.2 --, ##STR3## or --(CH.sub.2).sub.n CHOH(CH.sub.2).sub.n --; whereinR.sup.2 is H, methyl, ethyl or propyl;n is 1-10, and pharmaceutically acceptable salts thereof have antiallergy and antiinflammatory activity.Type: GrantFiled: July 9, 1984Date of Patent: November 12, 1985Assignee: USV Pharmaceutical Corp.Inventors: Howard Jones, Ernest Magnien, John H. Musser, Mujahid L. Shaikh
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Patent number: 4548934Abstract: The present invention relates to novel 4H-1,4-benzothiazine derivatives and a method for their synthesis. The invention also relates to the pharmaceutical use of said derivatives, in particular their use as anti-infective agents, as agents for promoting growth and for improving feed stuff utilization in animals, and as preservations.Type: GrantFiled: August 1, 1983Date of Patent: October 22, 1985Assignee: Bayer AktiengesellschaftInventors: Gerd Fengler, Dieter Arlt, Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
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Patent number: 4540523Abstract: Cationic styryl dyestuffs of the formula ##STR1## in which A.sup.1 is an alkyleneoxy or alkyleneamino radical,D.sup.1 is a direct bond or divalent radical,An is an anion, andthe terminal phenyl ring is unsubstituted or substituted by CN, alkyl or alkoxy. The compounds are suitable for dyeing, enscribing and printing paper for dyeing and printing synthetic fibres, especially made of polyacrylonitrile, acid-modified polyesters or polyamides.Type: GrantFiled: October 17, 1980Date of Patent: September 10, 1985Assignee: Bayer AktiengesellschaftInventor: Hermann Beecken
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Patent number: 4535079Abstract: Object of the invention is a class of new organic compounds derived from 1,4-benzothiazine through substitution of an hydrogen atom in position 6, 7 or 8 by an oxypropanolammine radical monosubstituted in N and furthermore a series of new phenyl derivatives of 1,4-benzothiazine, obtained as intermediate in the synthesis of oxypropanolammine derivatives, and process for obtained the new compounds in form suitable for the preparation of pharmaceutical compositions having antihypertensive, vasodilating and antiarrhythmic activity.Type: GrantFiled: October 18, 1983Date of Patent: August 13, 1985Assignee: Mediolanum Farmaceutici S.R.L.Inventor: Arnaldo Fravolini
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Patent number: 4512990Abstract: Compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: Z is S;Y is halo, alkoxy, alkyl, or dialkylamino;a is 0, 1 or 2;b is an integer from 2-12 with the proviso that if b is 2 or 3, a cannot be 0, and with the further proviso that if X is OH, b cannot be 2-5 and with the further proviso that if X is --NH.sub.2, b cannot be 2-5; andX is selected from the group consisting of: --OH, OR.sup.1, --NH.sub.2, --NHR.sup.1, NR1/2, ##STR2## and --NHCONHR.sup.2 in which each R.sup.1 is independently alkyl or cycloalkyl or, in --NR1/2, both R.sup.1 s together are alkylene or form a piperazine ring optionally substituted at the ring N by alkyl or --CH.sub.2 CH.sub.2 OH; andR.sup.2 is alkyl, cycloalkyl, or optionally substituted phenyl;have antiinflammatory properties and are useful in the treatment of conditions characterized by inflammation and swelling.Type: GrantFiled: February 18, 1982Date of Patent: April 23, 1985Assignee: Syntex (U.S.A.), Inc.Inventors: Peter H. Nelson, Howard J. Ringold, Stefan H. Unger, Thomas R. Thieme
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Patent number: 4500709Abstract: This invention relates to novel compounds useful as intermediates in the preparation of cephalosporin compounds of antibacterial activity, having the formula ##STR1## wherein R.sup.1 is a group of the formula ##STR2## in which X is sulfur, oxygen or substituted or unsubstituted imino, andR.sup.2 is hydrogen or a saturated or unsaturated aliphatic hydrocarbon residue,a derivative at the carboxy group thereof and salt thereof.Type: GrantFiled: September 30, 1982Date of Patent: February 19, 1985Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Takashi Masugi, Takashi Ogino, Kiyoshi Tsuji
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Patent number: 4499272Abstract: 2-Hydroxy-3-halo-1-propanesulfonates are reacted with certain arylamines, preferably in the presence of a base such as KOH or NaOH in one or more of ethylene glycol, propylene glycol, 2-ethoxyethanol and the like to give 2-hydroxy-3-(arylamino)-1-propanesulfonates useful as couplers for acid dyes for polyamide fibers. The present coupler products which are derivatives of aniline, tetrahydroquinoline, and benzomorpholine, have the general formulae ##STR1## wherein the rings may be substituted with a wide variety of substituents known to the dye art;M is NH.sub.4.sup.+ or a group IA metal, preferably Na.sup.+, or K.sup.+ ; andR.sup.3 is hydrogen or a group such as alkyl, cycloalkyl and aryl, each of which may be substituted.Type: GrantFiled: August 20, 1982Date of Patent: February 12, 1985Assignee: Eastman Kodak CompanyInventors: John A. Hyatt, Clarence A. Coates, Jr.
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Patent number: 4466964Abstract: The invention relates to alkylurea derivatives of Formula (I), as defined in the specification, which alkylurea derivatives are useful as hypolipaemic agents. Also included in the invention are methods for the manufacture of said alkylurea derivatives compositions and medicaments containing said alkylurea derivatives and methods for the use of said alkylurea derivatives.Type: GrantFiled: September 27, 1982Date of Patent: August 21, 1984Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Kabbe, Hans-Peter Krause, Rudiger Sitt
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Patent number: 4420613Abstract: The present invention relates to new dihydrobenzothiazine compounds, to the production thereof and to the use thereof as stabilizers and co-stabilizers against the oxidative and/or thermal degradation of organic polymers.Type: GrantFiled: March 17, 1982Date of Patent: December 13, 1983Assignee: Bayer AktiengesellschaftInventors: Paul Uhrhan, Edmund Krauthausen, Kurt-Rainer Stahlke, Gerwolf Quaas, Lothar Ruetz
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Patent number: 4399279Abstract: 4H-1,4 benzothiazine derivatives having anorectic activity and their preparation including intermediate compounds are disclosed.Type: GrantFiled: April 30, 1982Date of Patent: August 16, 1983Assignee: G.D. Searle & Co.Inventors: Robert J. Chorvat, Bipinchandra N. Desai, Suzanne E. Radak
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Patent number: 4397849Abstract: This invention relates to novel benzothiazine derivatives having therapeutic effect on autoimmune diseases, to processes for preparation of such derivatives, and to pharmaceutical compositions containing such derivatives, the derivatives having the formula: ##STR1## wherein R.sup.1 is lower alkyl which may have one or more substituents selected from carboxy, aryl and carboxy(lower)cycloalkyl; aryl which may have one or more substituents selected from halogen, lower alkyl, halo(lower)alkyl and lower alkoxy; haloarylamino; or heterocyclic group;R.sup.2 is hydrogen, lower alkyl, lower alkylamino(lower)alkyl, aryl or ar(lower)alkyl;R.sup.3 is hydrogen, halogen, lower alkyl or lower alkoxy; andn is an integer 0 to 2.Type: GrantFiled: December 11, 1981Date of Patent: August 9, 1983Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Tsutomu Teraji, Teruo Oku, Youichi Shiokawa
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Patent number: 4346089Abstract: Compounds of the formula (I): ##STR1## and pharmaceutically acceptable salts and N-oxides thereof, wherein: R.sub.1 is a C.sub.1-6 alkoxy group;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, CF.sub.3, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkyl-S(O).sub.n wherein n is 0, 1 or 2, nitro, C.sub.1-6 alkoxy, hydroxy, or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two C.sub.1-6 alkyl groups;or R.sub.1 and R.sub.2 taken together are methylenedioxy or ethylenedioxy in which case R.sub.3 is any one of the groups given for R.sub.1 and R.sub.2 above;R.sub.4 is hydrogen, C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl;R.sub.5 is hydrogen or C.sub.1-4 alkyl;X is an oxygen or sulphur atom; or a sulphoxide group >S.about.O;p is 1 or 2; andr is 1 or 2; are useful in the treatment of disorders related to imparied gastrointestinal motility.Type: GrantFiled: January 28, 1981Date of Patent: August 24, 1982Assignee: Beecham Group LimitedInventors: Michael S. Hadley, Francis D. King, Roger T. Martin
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Patent number: 4268301Abstract: A process for producing novel 1,4-benzothiazine derivatives (I), ##STR1## (in which X is a halogen atom) and their derivatives, ##STR2## wherein R is a (C.sub.1 -C.sub.5) alkyl, (C.sub.3 -C.sub.6) cycloalkyl, phenyl, substituted phenyl, phenyl (C.sub.1 -C.sub.5) alkyl or phenoxy (C.sub.1 -C.sub.5) alkyl group, and herbicides containing these compounds as an active ingredient.Type: GrantFiled: April 10, 1979Date of Patent: May 19, 1981Assignee: Sumitomo Chemical Company, LimitedInventors: Tamon Uematsu, Shunichi Hashimoto, Hiromichi Oshio
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Patent number: 4254118Abstract: This invention discloses novel 1-oxo-5H-pyrimido[2,1-c][1,4]benzoxa(or thia)zine-2-carboxylic acid lower alkyl esters, derivatives thereof, process for their preparation, pharmaceutical compositions thereof and methods for using the compounds. The compounds of this invention are useful in the treatment of anaphylactic reactions and allergic conditions in a mammal.Type: GrantFiled: August 13, 1979Date of Patent: March 3, 1981Assignee: Ayerst, McKenna & Harrison Inc.Inventors: Jean A. Gauthier, Ivo L. Jirkovsky
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Patent number: 4134974Abstract: Cyclic derivatives of 1,4-benzoxazine and 1,4-benzothiazine are disclosd, such as, for instance, 1H,2,3,3a,4-tetrahydro-2-carbamoylmethyl-imidazo[5,1-c][1,4]benzoxazin-1-o ne and 1H,2,3,3a,4-tetrahydro-2-carbamoylmethyl-8-chloro-imidazo[5,1-c][1,4]benzo xazin-1-one. These compounds are active on the central nervous system, and function as antidepressant agents.Type: GrantFiled: December 8, 1976Date of Patent: January 16, 1979Assignee: Carlo Erba S. p. A.Inventors: Piero Melloni, Nicola Mongelli, Francesco Lauria, Alessandro Rossi, Raffaele Tommasini
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Patent number: 4120960Abstract: Therapeutic activity, and in particular the ability to induce diuresis or saluresis, has been discovered in 4-hydroxy- or 4-mercapto-2-aryl-1,2-dihydrophthalazine-1-acetic acids, the tautomers of these namely 4-oxo or thio-2-aryl-1,2-tetrahydrophthalazine-1-acetic acids, and in the ester and alcohol derivatives of the acids, and in the acyl derivatives of the 4-hydroxy or mercapto compounds and in the 3-alkyl derivatives of the 4-oxo or thio compounds. Therapeutic compositions and methods using the compounds are described, as also are novel compounds.Type: GrantFiled: August 1, 1977Date of Patent: October 17, 1978Assignee: The Boots Company LimitedInventors: Norman W. Bristow, Peter E. Macey, Kenneth J. Nichol, Malcolm F. Sim