The -c(=x)- Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 548/201)
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Patent number: 5312826Abstract: Disclosed are a dicarboxylic acid compound represented by the formula (I): ##STR1## wherein R represents hydrogen atom, a lower alkyl group, phenyl group or hydroxyl group; R.sup.1 represents a straight or branched alkyl group having 1 to 10 carbon atoms or a lower alkyl group substituted by a group selected from aryl group, a sulfur- or nitrogen-containing heterocyclic monocyclic group and a cycloalkyl group having 4 to 8 carbon atoms; R.sup.2 represents a substituted or unsubstituted aryl group, a cycloalkyl group having 4 to 8 carbon atoms or a sulfur-containing or nitrogen-containing heterocylcic group; X represents sulfur atom, oxygen atom or a substituted or unsubstituted imino group; Y.sup.1 represents imino group, oxygen atom or sulfur atom and Y.sup.2 represents nitrogen atom, or Y.sup.1 represents a vinylene group and Y.sup.2 represents a group: --CH.dbd.Type: GrantFiled: June 19, 1992Date of Patent: May 17, 1994Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Ken-ichi Nunami, Tameo Iwasaki, Kazuo Matsumoto, Koji Yano, Isao Yamaguchi
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Patent number: 5312825Type: GrantFiled: September 3, 1992Date of Patent: May 17, 1994Assignee: Yason S.r.l.Inventor: Giuseppe Quadro
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Patent number: 5300656Abstract: Coumarin deviatives of the formula ##STR1## in which R.sup.1 denotes cyano,R.sup.2 represents phenyl or thiazolyl bonded in the 2-, 4-, or 5-position,R.sup.3 denotes hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxycarbonyl-C.sub.1 -C.sub.4 -alkyl andR.sup.4 represents hydrogen, C.sub.1 -C.sub.4 -alkyl or phenylsulphonyl, where C.sub.1 -C.sub.4 -alkyl can be substituted by hydroxyl, amino, carboxyl or C.sub.1 -C.sub.4 -alkoxy-carbonyl and phenyl can be monosubstituted or disubstituted by chlorine, bromine or C.sub.1 -C.sub.4 -alkyl, where furthermore R.sup.3 and R.sup.4, together with the N atom which they substitute, can denote a morpholine ring, a piperazine ring or a triazole ring which can carry one or two substituents from the group comprising methyl, ethyl and phenyl, andwhere furthermore one of the radicals R.sup.2, R.sup.3 and R.sup.4 denotes or carries a primary or secondary amino group, the hydroxyl group, the carboxyl group or the C.sub.1 -C.sub.Type: GrantFiled: July 16, 1992Date of Patent: April 5, 1994Assignee: Bayer AktiengesellschaftInventors: Eberhard Kuckert, Gunther Beck, Florin Seng, Antonius Lobberding
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Patent number: 5296495Abstract: Compounds of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, A, X and Y are as defined and pharmaceutically acceptable salts thereof; which have activities as leukotriene and Slow Reacting Substance of Anaphalaxis (SRS-a) antagonists or inhibitors, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or treatment of allergy or inflamation in human beings or animals.Type: GrantFiled: August 12, 1992Date of Patent: March 22, 1994Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Kazuo Okumura, Shinji Shigenaga, Hiroshi Matsuda
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Patent number: 5290756Abstract: Compounds of the formula: ##STR1## wherein X is hydrogen, halo, trihalomethyl, alkyl, nitroor cyano; X.sup.1 is hydrogen, halo, or trihalomethyl; R.sup.1 and R.sup.2 are hydrogen, alkyl phenyl or benzyl; n is 1 to 5, and Z is halo, cyano, nitro, trihalomethyl, methylthio, methylsulfinyl, methylsulfonyl, acetyl, phenyl, or heterocycle, and compositions containing these compounds exhibit herbicidal activity.Type: GrantFiled: June 8, 1982Date of Patent: March 1, 1994Assignee: Rohm and Haas CompanyInventors: Colin Swithenbank, Ted Fujimoto
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Patent number: 5273986Abstract: Compounds of the formula: ##STR1## wherein the substituents are as described in the specification, antagonize LTD.sub.4 action and thus, are useful in treating bronchial asthma, pulmonary anaphylaxis, cystic fibrosis, chronic bronchitis, bronchiectasis, respiratory distress syndrome and pulmonary oedema.Type: GrantFiled: July 2, 1992Date of Patent: December 28, 1993Assignee: Hoffmann-La Roche Inc.Inventors: George W. Holland, John R. Vermeulen, William J. Zally
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Patent number: 5270317Abstract: The invention relates to N-substituted heterocyclic derivatives and its salts.These derivatives have the formula ##STR1## in which the substituents are as defined in the specification.Type: GrantFiled: November 20, 1991Date of Patent: December 14, 1993Assignee: Elf SanofiInventors: Claude Bernhart, Jean-Claude Breliere, Jacques Clement, Dino Nisato, Pierre Perreault, Claude Muneaux, Yvette Muneaux
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Patent number: 5252735Abstract: This invention relates to compounds of Formula I ##STR1## which are useful as antiatherosclerotic agents and inhibitors of cell proliferation for the treatment of proliferative diseases. In addition, various compounds of Formula I are useful inhibitors of platelet aggregation.Type: GrantFiled: February 25, 1992Date of Patent: October 12, 1993Assignee: The Upjohn CompanyInventor: Joel Morris
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Patent number: 5244867Abstract: Oxazole- and thiazolecarboxamides of the formulae Ia and Ib ##STR1## where the substituents have the following meanings: X oxygen or sulfur;R.sup.2 formyl, 4,5-dihydrooxazol-2-yl or --COYR.sup.5 ;Y oxygen or sulfur; andR.sup.4 is methyl and herbicidal agents containing compounds of the formulae Ia or Ib as active ingredients.Type: GrantFiled: December 26, 1991Date of Patent: September 14, 1993Assignee: BASF AktiengesellschaftInventors: Klaus Ditrich, Volker Maywald, Gerhard Hamprecht, Albrecht Harreus, Bruno Wuerzer, Karl-Otto Westphalen
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Patent number: 5223489Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl optionally substituted aryl; or amino optionally substituted; andR.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 are taken together with the attached nitrogen atom to form a heterocyclic group optionally substituted;R.sup.3 is hydrogen or lower alkyl; andR.sup.Type: GrantFiled: January 30, 1992Date of Patent: June 29, 1993Assignee: Ujisawa Pharmaceutical Co., Ltd.Inventors: Keiji Hemmi, Masahiro Neya, Hiroshi Marusawa, Keisuke Imai, Natsuko Kayakiri, Masashi Hashimoto
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Patent number: 5212160Abstract: 3-L-(5-thioxo-L-prolyl)thiazolidine-4-carboxylic acid and the derivatives thereof have valuable immunostimulating, antioxidant, antiradical and antiageing properties. They are prepared by thionating the corresponding 3-L-pyroglutamyl-L-thiazolidine-4-carboxylic acid derivatives or by condensing 5-thioxo-L-proline with the corresponding L-thiazolidine-4-carboxylic acid derivatives.Type: GrantFiled: January 16, 1991Date of Patent: May 18, 1993Assignee: Poli Industria Chimica S.p.A.Inventors: Stefano Poli, Lucio Del Corona, Germano Coppi
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Patent number: 5210205Abstract: Compounds of formula V ##STR1## and C.sub.1 -C.sub.6 carboxylic acid esters thereof, wherein R.sub.1 is selected from the group consisting of CH.sub.3, C.sub.2 H.sub.5, n-C.sub.3 H.sub.7, isoC.sub.3 H.sub.7, CH.sub.2 --O--CH.sub.3, CH.sub.2 --O--C.sub.2 H.sub.5, CH.sub.2 --O--CHF.sub.2 and cyclopropyl and R.sub.2 is cyclopropyl or C.sub.1 -C.sub.3 alkyl.Type: GrantFiled: March 18, 1992Date of Patent: May 11, 1993Assignee: Ciba-Geigy CorporationInventor: Adolf Hubele
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Patent number: 5208231Abstract: A triazole compound having the formula (I): ##STR1## wherein R.sub.1 and R.sub.2 represent a hydrogen atom, a lower alkyl group or a dialkylcarbamoyl group, or R.sub.1 and R.sub.2 may be bonded to form an alkylene group, an oxyalkylene group or a thioalkylene group which may be substituted with a lower alkyl group, R.sub.3 represents a hydrogen atom or CONRR' where R and R' represent an alkyl group, an alkenyl group, an alkynyl group, a cyanoalkyl group or a phenyl group or benzyl group which may be substituted, or R and R' may be bonded to form an alkylene group, an oxyalkylene group or a thioalkylene group which may be substituted with a lower alkyl group; R.sub.4 represents ##STR2## where R.sub.5 represents a hydrogen atom, a lower alkyl group or a phenyl group, R.sub.6 represents a lower alkyl group, or R.sub.5 and R.sub.6 may be bonded to form an alkylene group, with a proviso that R.sub.1 and R.sub.Type: GrantFiled: April 20, 1992Date of Patent: May 4, 1993Assignee: S.D.S. Biotech K.K.Inventors: Toshiya Kimata, Tetsuo Tsuruya, Shunji Hayashi, Kazuhiro Kojima, Satoshi Yamanaka, Kiyoshi Sakuma
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Patent number: 5191085Abstract: Optically active salts are disclosed of the formula (I): ##STR1## wherein Ac represents an acyl group, R.sup.1 hydrogen or methyl, R.sup.2 and R.sup.3 identical or different substitutes, preferably methyl. The salts can be obtained from the corresponding optically active carbonic acid and DL-3-cyano-2-hydroxypropyl trimethylammonium hydroxide. The diastereomeric salt pairs are easily split from one another and separated again, so that the process is suited for producing optically active 3-cyano-2-hydroxypropyl trimethylammonium salts.Type: GrantFiled: March 27, 1991Date of Patent: March 2, 1993Assignee: Degussa AktiengesellschaftInventors: Harald Jakob, Klaus Huthmacher, Herbert Klenk
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Patent number: 5187290Abstract: Compounds of the formula ##STR1## wherein Z is oxygen or sulfur are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inbitition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.Type: GrantFiled: September 29, 1986Date of Patent: February 16, 1993Assignee: E. R. Squibb & Sons, Inc.Inventor: Eric M. Gordon
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Patent number: 5183827Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O or NR'; where R' is hydrogen or lower alkyl; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 18, 1991Date of Patent: February 2, 1993Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 5169858Abstract: A composition for therapy of tumors having high tyrosinase activity contains the reaction product of penicillamine with a cytotoxic aldehyde, or pharmaceutically acceptable salts or esters thereof, and a pharmaceutically acceptable vehicle. The preferred compounds are 5,5-dimethyl-2-phenyl-4-thiazolidine carboxylic acid or 5,5-dimethyl-2-(2-hydroxyphenyl)-4-thiazolidine carboxylic acid, or pharmaceutically acceptable salts or esters thereof. Treatment preferably comprises an intra-arterial drip. Diagnosis of tumors suitable for treatment by means of these compositions may be accomplished by administering a radioactive copper salt and scanning for accumulations of radioactivity. This will indicate sites of high tyrosinase activity.Type: GrantFiled: February 26, 1986Date of Patent: December 8, 1992Inventor: David Rubin
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Patent number: 5149356Abstract: Herbicidal sulphonylaminocarbonyl-triazolinones having substituents which are bonded via sulphur, of the formula ##STR1## in which n represents the numbers 0, 1 or 2,R.sup.1 represents hydrogen, hydroxyl or amino, or represents an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, aralkyl, aryl, alkoxy, alkenyloxy, alkylamino, cycloalkylamino and dialkylamino,R.sup.2 represents an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aralkyl and aryl, andR.sup.3 represents an optionally substituted radical from the series comprising alkyl, aralkyl, aryl and heteroaryl,as well as salts of compounds of the formula (I),Also new are the compounds of the following formula: ##STR2## in which n, R.sup.1 and R.sup.2 have the abovementioned meanings andZ represents halogen, alkoxy, aralkoxy or aryloxy.Type: GrantFiled: October 15, 1991Date of Patent: September 22, 1992Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Muller, Peter Babczinski, Hans-Joachim Santel, Robert R. Schmidt
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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: 5120723Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.Type: GrantFiled: May 10, 1990Date of Patent: June 9, 1992Assignee: University of Southern CaliforniaInventors: Kelvin W. Gee, Michael B. Bolger
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Patent number: 5118683Abstract: Compounds of the formula I ##STR1## wherein R.sup.5 represents C.sub.1 to C.sub.6 -alkyl or the group --(CH.sub.2).sub.n --Z--(CH.sub.2).sub.m --Ar;Z represents O, S or --CH.sub.2 --;n represents an integer of 1 to 8;m represents zero or an integer of 1 to 8;one of R.sup.1 and R.sup.2 represents the group ##STR2## and the other represents hydrogen or R.sup.7 CO--; R.sup.7 is C.sub.1 to C.sub.10 alkyl, C.sub.3 to C.sub.8 cycloalkyl, aryl, heteroaryl, --N(R.sup.9 R.sup.10), or R.sup.11 O--; R.sup.3, R.sup.4, R.sup.9, and R.sup.10 are each independently selected from hydrogen, C.sub.1 to C.sub.6 alkyl and Ar.sup.1 ; R.sup.6 and R.sup.11 are each independently C.sub.1 -C.sub.8 alkyl; Ar and Ar.sup.1 are each independently selected from the group consisting of phenyl or phenyl substituted by one or two substituents selected from the group consisting of R.sup.12, R.sup.13 O--; R.sup.14 S(O).sub.x --, R.sup.15 CO--, (R.sup.16 R.sup.17)NCO--, F, Cl, Br, I, NO.sub.2, CF.sub.3, CN, or phenyl; R.sup.12, R.sup.13, R.sup.Type: GrantFiled: June 13, 1990Date of Patent: June 2, 1992Assignee: Schering CorporationInventors: David J. Blythin, Ho-Jane Shue
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Patent number: 5118811Abstract: Amino acid derivatives of the formula ##STR1## wherein: Q is W--(CH.sub.2).sub.m --(A).sub.n --CO--B-- whereinA is oxygen atom or --NH--;B is ##STR2## or --(CH.sub.2).sub.l -- wherein X is sulfur atom or --CH.sub.2 --, and l is an integer from 1 to 3;W is ##STR3## wherein Hal is halogen atom; n is an integer of 0 or 1; andm is an integer from 0 to 3;Y is sulfur atom or --CH.sub.2 --; andR is hydrogen atom, formyl group, C.sub.1-5 alkoxycarbonyl group, --C.tbd.N or ##STR4## wherein R.sup.1 is hydrogen atom, andR.sup.2 is hydroxyl group, C.sub.1-5 alkylcarboxy group, phenylcarboxy group, C.sub.1-5 alkoxy group or phenyl C.sub.1-5 alkoxy group;with the proviso that when R is hydrogen atom, formyl group or C.sub.1-5 alkoxycarbonyl group, W is ##STR5## The compounds mentioned above specifically inhibit prolyl endopeptidase activity and are useful as agents for the treatment and prevention of dementia and amnesia.Type: GrantFiled: December 12, 1990Date of Patent: June 2, 1992Assignees: Japan Tobacco Inc., Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Itsuo Uchida, Koji Kobayashi, Kazuhiko Nishii, Kunio Iwata, Shin Hara, Koretake Anami
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Patent number: 5116954Abstract: Substituted six-membered benzo-fused heterocycles of the formula (I) ##STR1## in which: X=0, NH, S.fwdarw.(O).sub.n (n=0 or 2);R.sub.1 is phenyl, phenyl substituted by methoxy, hydroxy, chlorine, fluorine, diethylaminoethoxy, phenoxy, 2-methyl-4-thiazolyl, 2-amino-4-thiazolyl, phenyl, amino, nitro, terbutyl, carboxymethyl, acetamido, dimethyltriazenyl, benzoyl, hexyl, undecyl, trifluoromethyl, carbamoyl; or R.sub.1 is trifluoromethyl, pyridyl-2,pyridyl-4;R.sub.2 is H, methoxy, hydroxy; orR.sub.1 and R.sub.2 are --CH.dbd.CH--CH.dbd.CH--;R.sub.3 and R.sub.4 are methoxy, hydroxy, fluorine or form a fused benzene ring;CR.sub.5 R.sub.6 R.sub.7 is carboxymethyl, --CH.sub.2 --PO.sub.3 H,--CH.sub.2 --PO(oET).sub.2, 4-methylpiperazinyl, aminomethyl,3-4-5-trimethoxyphenylaminomethyl, acetyl, bromoacetyl, hydroxyethyl, acetoxyethyl, mercaptomethyl, acetylthiomethyl, methoxy-carbopnylthiomethyl, --CH--CONH.sub.2, ##STR2## substituted thiazolyl, subsituted furanone, imidazo(1,2-a)pyridinyl, indolizinyl, or R.sub.4 and R.Type: GrantFiled: August 2, 1989Date of Patent: May 26, 1992Assignee: Lipha, Lyonnaise Industrielle PharmaceutiqueInventors: Philippe Briet, Jean-Jacques Berthelon, Francois Collonges
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Patent number: 5110936Abstract: 3-(L-pyroglutamyl)-L-thiazolidine-4-carboxylic acid and derivatives thereof are prepared by condensing L-pyroglutamic acid or its substitution products, either in the presence of dicyclohexylcarbodiimmide or the like, or by condensation of active derivatives of L-pyroglutamic acid with 4-thiazolidine-carboxylic acid derivatives.Type: GrantFiled: October 9, 1990Date of Patent: May 5, 1992Assignee: Roli Industria Chimica S.p.A.Inventors: Stefano Poli, Lucio Del Corona
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Patent number: 5106992Abstract: 3,5-Dihydroxypentanoic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy-2-methyl)-substituted-thiazolidine derivatives and have the structure ##STR1## wherein Z is ##STR2## R.sup.6 is an alkali metal, lower alkyl or H; R.sup.1 and R.sup.2 are the same or different and are H, lower alkyl or aryl; X is S, O, ##STR3## or a single bond; R.sup.7 is lower alkyl; R.sup.3 is lower alkyl or aryl; R.sup.4 and R.sup.5 are the same or different and are H or lower alkyl; and --- represents a single bond or a double bond, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents.In addition, novel intermediates for use in preparing the above mevinic acid derivatives are also provided.Type: GrantFiled: April 30, 1990Date of Patent: April 21, 1992Assignee: E. R. Squibb & Sons, Inc.Inventors: David R. Magnin, Eric M. Gordon
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Patent number: 5098466Abstract: Substituted semicarbazones, thiosemicarbazones and isothiosemicarbazones and salts thereof, intermediates therefor, synthesis thereof, and the use of said compounds for the control of weeds.Type: GrantFiled: August 21, 1990Date of Patent: March 24, 1992Assignee: Sandoz Ltd.Inventors: Richard J. Anderson, Michael M. Leippe, Joe T. Bamberg
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Patent number: 5096902Abstract: The invention relates to novel nitrogen- and sulfur-containing heterocyclic compounds of the formula (I), acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## Ar stands for an optionally mono- or polysubstituted aryl or heteroaryl group;R.sup.1 means a carbonyl or (C.sub.2-6 alkenyl)carbonyl group;R.sup.2 stands for hydrogen C.sub.1-6 alkyl, phenyl or phenyl (C.sub.1-4 alkyl) group;R.sup.3 means hydrogen or (C.sub.1-6 alkoxy)carbonyl group;R.sup.4 and R.sup.5 stand, independently from each other, for hydrogen or C.sub.1-6 alkyl group;R.sub.6 ogen, C.sub.1-6 alkyl group or halophenyl group;m is 0 or 1; andn is 1 or 2,with the proviso that R.sup.2 means hydrogen when m is 0.The compounds of formula (I) show a significant cerebral antihypoxic action and thus, they can be used for the treatment of diseases caused by hypoxic brain damages such as e.g.Type: GrantFiled: April 12, 1990Date of Patent: March 17, 1992Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Karoly Nador, Pal Scheiber, nee Szelecsenyi Andrasi, Bela Molnar, Laszlo Szporny, Bela Kiss, Egon Karpati, Eva Palosi, Dora Groo, Istvan Laszlovszky, Zsolt Szombathelyi, Adam Sarkadi, Aniko Gere, Mihaly Bodo, Katalin Csomor, Judit Laszy, Zsolt Szentirmay
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Patent number: 5094683Abstract: Herbicidal sulphonylaminocarbonyltriazolinones of the formula ##STR1## in which R.sup.1 represents hydrogen, hydroxyl or amino, or represents an optionally substituted radical from the series comprising alkyl, alkenyl, akinyl, cycloalkyl, aralkyl, aryl, alkoxy, alkenyloxy, alkylamino and dialkylamino,R.sup.2 represents hydrogen hydroxyl, mercapto or amino, or represents an optionally substituted radical from the series comprising alkyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, alkoxy, alkylamino and dialkylamino, andR.sup.3 represents an optionally substituted radical from the series comprising alkyl, aralkyl, aryl and heteroaryl, and salts thereof. Intermediates of the formula ##STR2## in which A.sup.1 represents in each case optionally substituted alkyl, alkenyl, cycloalkyl, alkoxy or dialkylamino andA.sup.2 represents hydrogen, or represents in each case optionally substituted alkyl, cycloalkyl, aralkyl, aryl or alkoxy,provided that both A.sup.1 and A.sup.Type: GrantFiled: April 29, 1991Date of Patent: March 10, 1992Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Klaus-Helmut Muller, Michael Schwamborn, Peter Babczinski, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
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Patent number: 5089513Abstract: The invention concerns a thiazole of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted aryl of up to 10 carbon atoms;A is a direct link to X, or is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar.sup.2 is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing 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, substituted (1-4C)alkyl or (2-6C)alkanoyl;Q 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, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said thiazole.Type: GrantFiled: July 11, 1989Date of Patent: February 18, 1992Assignees: ICI Pharma, Imperial Chemical Industries PLCInventors: Thomas G. C. Bird, Graham C. Crawley, Martin P. Edwards, Philip N. Edwards, Jean-Marc M. M. Girodeau, John F. Kingston
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Patent number: 5086054Abstract: Novel arylcycloalkanepolyalkylamines useful as anti-psychotic, anti-ischemia, anti-stroke, anti-dementia and anti-convulsant agents. These arylcycloalkanepolyalkylamines are selective high-affinity ligands to the sigma binding-sites containing three basic units: arylcycloalkyl group, an amine group and an intermediate chain. Their preparation and use for treatment of psychoses, ischemia, stroke, dementia and convulsions are also disclosed.Type: GrantFiled: July 31, 1990Date of Patent: February 4, 1992Assignee: SRI InternationalInventor: Daniel W. Parish
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Patent number: 5066644Abstract: Ester or amide derivatives of 3-pyroglutamylthiazolidine-4-carboxylic acid exhibit interesting immunostimulating, antitoxic, antiinflammatory, antioxidental, antiageing properties.Type: GrantFiled: February 9, 1990Date of Patent: November 19, 1991Assignee: Poli Industria Chimica S.p.A.Inventors: Stefano Poli, Germano Coppi, Lucio Del Corona
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Patent number: 5061720Abstract: Disclosed are novel substituted 4-thiazolidinone derivatives having cyclooxygenase and 5-lipoxygenase inhibiting properties and which are topical antiinflammatory agents for inflammed conditions of the skin having the formula: ##STR1## wherein R is hydrogen or loweralkyl; R.sup.1 is loweralkyl or aryl; X is --(CH.sub.2)-aryl, --O--(CH.sub.2).sub.0-3 -aryl, --C(O)(CH.sub.2).sub.0-3 -aryl, --CH(OH)--(CH.sub.2).sub.0-3 -aryl or 3,4 ##STR2## (to form naphthyl ring); aryl is phenyl, substituted phenyl, or 2,3 or 4 pyridyl; W is oxygen; Q is -(alk.sup.1).sub.0-1 --(O).sub.0-1 --(B).sub.0-1 --(alk.sup.2).sub.0-1 --[C(O)Z].sub.0-1 ; B is ##STR3## Z is OR.sup.3 or NR.sup.4 R.sup.5 where R.sup.3 is hydrogen, loweralkyl, or a pharmaceutically acceptable metal cation, R.sup.4 and R.sup.5 are hydrogen or loweralkyl; alk.sup.1 and alk.sup.Type: GrantFiled: September 13, 1989Date of Patent: October 29, 1991Assignee: A. H. Robins Company, Inc.Inventors: David A. Walsh, Ibrahim M. Uwaydah
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Patent number: 5053414Abstract: Heterocyclic compounds of the general formula: ##STR1## wherein Z represents methylene group or sulfur atom, R represents a general formula:G--E--D--B--A--G represents a carbocyclic or heterocyclic ring.Type: GrantFiled: April 5, 1989Date of Patent: October 1, 1991Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
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Patent number: 5041663Abstract: The invention relates to novel oxime ethers of the formula I ##STR1## wherein R.sub.1 is hydrogen, halogen, lower alkyl, lower haloalkyl, lower alkoxy, lower haloalkoxy, lower alkylthio, lower haloalkylthio, lower alkylsulfinyl, lower alkylsulfonyl, lower haloalkylsulfinyl, lower haloalkylsulfonyl or nitro, each of R.sub.2 and R.sub.3 is hydrogen, halogen, lower alkyl, lower alkoxy or lower haloalkoxy, and Q is an unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl or cycloalkyl group, a lower alkanoyl radical, an aliphatic, cycloaliphatic, aromatic or heterocyclic acyl radical which may be substituted or unsubstituted, a carbonyl or thiocarbonyl radical, an aryl or aralkyl radical, an acylimidomethyl radical, a phthalimidomethyl radical or a heterocyclic radical.These compounds are able to act as antidotes or safeners for protecting cultivated plants from the phytotoxic action of aggressive herbicides.Type: GrantFiled: December 11, 1990Date of Patent: August 20, 1991Assignee: Ciba-Geigy CorporationInventors: Henry Martin, Urs Fricker
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Patent number: 5032590Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical,are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: March 8, 1990Date of Patent: July 16, 1991Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 5028604Abstract: Novel condensed benzene derivatives having prolyl endopeptidase inhibitory, anti-hypoxic, and anti-amnesic activities are disclosed. The compounds are represented by the following (I), ##STR1## wherein A represents a methylene, ethylene, or propylene group, B represents a methylene or ethylene group, m denotes an integer of 0-5, X and Y, which may be same or different, individually represent a methylene group or sulfur atom, R.sup.1 represents a hydrogen atom, a carboxyl, lower alkyloxycarbonyl, hydroxymethyl, or formyl group, R.sup.2 represents a hydrogen atom, a halogen atom, a lower alkyl, lower alkoxy, nitro, or amino group, R.sup.3 represents a hydrogen atom or a lower alkyl group, and the dotted line may optionally be present. They are useful as a medicine for treating or preventing cerebral circulation disorder, cerebral metabolism disorder, or memory disturbance.Type: GrantFiled: December 1, 1989Date of Patent: July 2, 1991Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Motoki Torizuka, Tomoji Aotsuka, Mitsuo Soeda, Kuniyoshi Ogura, Yoshiaki Tanaka, Hisayoshi Kato, Naoki Nakata, Naoyoshi Miura, Hikari Morita
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Patent number: 5025001Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.Type: GrantFiled: March 24, 1989Date of Patent: June 18, 1991Assignee: Brigham and Women's HospitalInventors: Joseph Loscalzo, John Cooke
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Patent number: 5017618Abstract: Compounds having the formula ##STR1## and their pharmaceutically acceptable acid addition salts, wherein --X-- is --O--, --CH.sub.2 -- or --; .dbd.Y is .dbd.O or a derivatized keto group which is hydrolyzable or enzymatically convertible to a keto group; R is alkyl having from 1 to 12 carbon atoms or aralkyl having from 7 to 20 carbon atoms; and Ar is the 3-aromatic or heterocyclic residue of a 1-alkylamino-2-propanol having an aromatic or heterocyclic substituent at the 3-position and having .beta.-adrenergic blocking properties; are useful as .beta.-adrenergic blocking agents and are of particular interest in the treatment of glaucoma or for lowering intraocular pressure.Type: GrantFiled: September 18, 1989Date of Patent: May 21, 1991Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 5006548Abstract: Compounds of the general formula: ##STR1## wherein R.sup.1 is heterocyclic group other than pyridyl and which is unsubstituted or substituted with lower alkyl or lower alkoxycarbonyl, R.sup.2 is hydrogen, halogen, or nitro, and R.sup.3 is carboxy group or its functional derivative, with the proviso that when R.sup.1 is an unsubstituted furyl, or furyl mono- or polysubstituted with alkyl and R.sup.2 is hydrogen, then R.sup.3 is functional derivative of carboxy and, where applicable, pharmaceutically acceptable salts thereof are hyaluronidase inhibitors and useful as anti-allergic agent.Type: GrantFiled: August 7, 1989Date of Patent: April 9, 1991Assignee: Sawai Pharmaceutical Co., Ltd.Inventors: Toshio Satoh, Hitoshi Matsumoto, Hisao Kakegawa, Yoshiko Kato, Juichi Riku, Junji Yoshinaga, Yoshifumi Kanamoto
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Patent number: 4997848Abstract: Compounds of formula (I): ##STR1## in which: R represents hydrogen, methyl of hydroxy; X represents an alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or heterocyclic group; A represents a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y represents hydrogen, or an aryl, cycloalkyl or heterocyclic group] have valuable antihypercholesteremic activities and may be used in the treatment of disorders arising from a blood cholesterol imbalance in humans and other animals.Type: GrantFiled: October 21, 1988Date of Patent: March 5, 1991Assignee: Sankyo Company, LimitedInventors: Masaaki Kurabayashi, Hiroshi Kogen, Hiroshi Kadokawa, Hideshi Kurihara, Kazuo Hasegawa, Masao Kuroda
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Patent number: 4996218Abstract: Compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, which have .beta..sub.2 -adrenoreceptor stimulant activity. They may be used in the treatment of diseases associated with reversible airways obstruction, such as asthma and chronic bronchitis.In preferred embodiments, Q represents a chlorine atom or a trifluoromethyl group, X represents a C.sub.3-4 alkylene chain, Y a C.sub.1-5 alkylene chain, R, R.sup.1 and R.sup.2 are each preferably a hydrogen atom or a methyl group and Het represents a pyrimidinyl pyrazinyl, triazinyl, thiazolyl, quinolinyl, benzimidazolyl, benzothiazolyl, benzoxazolyl or pyridyl group.Type: GrantFiled: August 10, 1988Date of Patent: February 26, 1991Assignee: Glaxo Group LimitedInventor: Lawrence H. C. Lunts
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Patent number: 4992434Abstract: A microbicidal compostion contains as active ingredient 2-chloro-4-trifluoromethylthiazol-5-carbonic acid derivatives of the formula I ##STR1## R is organic radical with up to 40 carbon atoms, which optionally contains nitrogen, oxygen or sulfur atoms and which can be transformed by hydrolosis or oxydation into the directly to the thiazol ring bound carboxyl rest. These compounds have good microbicidal activity and are used for the control and prevention of infestation of plants by phytophathogenic microorganisms.Type: GrantFiled: April 11, 1989Date of Patent: February 12, 1991Assignee: Ciba-Geigy CorporationInventors: Werner Topfl, Robert Nyfeler, Werner Fory
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Patent number: 4988701Abstract: Cyclic amino-thioacetal amides of formula I ##STR1## wherein X is O, S, p is 1 or 2, R and R.sub.1 are optionally esterified hydrogen or carboxy, A is a single bond, methylene or ethylene, m is zero or 1, n is an integer 1 to 7 and y is a imidazole or .beta.-pyridylmethyl residue.Compounds I have valuable therapeutic properties.Type: GrantFiled: December 15, 1989Date of Patent: January 29, 1991Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Roberto Di Domenico, Carmelo A. Gandolfi, Silvano Spinelli, Bruno Lumachi, Odoardo Tofanetti, Sergio Tognella
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Patent number: 4977141Abstract: Non-peptidyl compounds characterized generally as aminoacyl aminodiol carbamates are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: October 1, 1987Date of Patent: December 11, 1990Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 4968681Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical, are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: November 15, 1988Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 4962117Abstract: Compounds having the formula: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, antiallergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: November 2, 1988Date of Patent: October 9, 1990Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Joseph G. Atkinson
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Patent number: 4952596Abstract: Compounds of the formula ##STR1## wherien R, R.sub.1, R.sub.2 and Y have the meanings mentioned in the description, processes for their preparation and their use in the pharmaceutical field are described.The compounds of formula I are endowed with antipyretic, anti-inflammatory, mucolitic and analgesic activity together with good gastric tolerability.In addition, the compounds of formula I are active in the treatment of ischemic or reperfusion syndromes.Type: GrantFiled: December 21, 1988Date of Patent: August 28, 1990Assignee: Zambon S.p.A.Inventors: Davide Della Bella, Angelo Carenzi, Dario Chiarino, Franco Pellacini
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Patent number: 4937255Abstract: For inhibiting 3-hydroxy-3-methylglutaryl coenzyme A and cholesterol biosynthesis, the novel disubstituted pyrroles of the formula ##STR1## in which R.sup.1 is aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen or cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, a cation or alkyl, aryl or aralkyl.Type: GrantFiled: March 16, 1989Date of Patent: June 26, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
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Patent number: 4916146Abstract: Novel N-substituted amino acid imide derivatives are disclosed. The compounds are represented by formula (I): ##STR1## wherein n represents an integer of 0 to 5, and X and Y, which may be the same or different, represent a methylene group or a sulfur atom, provided that not both X and Y are methylene groups at the same time. The compounds are useful as a medicine for treating or preventing cerebral circulation disorder, cerebral metabolism disorder, or memory disturbance.Type: GrantFiled: December 22, 1988Date of Patent: April 10, 1990Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Yoshiaki Tanaka, Tomoji Aotsuka, Naomi Kobayashi, Naoki Nakata, Kuniyoshi Ogura, Motoki Torizuka, Naoyoshi Miura, Heihachiro Arai
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Patent number: 4914208Abstract: The invention relates to the preparation of optically active salts of the general formula ##STR1## from which the corresponding optically active 3-chloro-2-hydroxypropyltrimethyl ammonium chloride can be obtained by treatment with mineral acid.The L(-) form of this compound is a valuable component for the synthesis of L(-) carnitine.Type: GrantFiled: October 17, 1988Date of Patent: April 3, 1990Assignee: Degussa AktiengesellschaftInventors: Harald Jakob, Klaus Huthmacher, Herbert Klenk, Axel Kleemann, Gunes Giray