Ring Chalcogen In The Additional Hetero Ring Patents (Class 544/374)
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Patent number: 4547574Abstract: Quaternary ammonium compounds suitable for use in finishing cellulose fiber containing textile material are described. The compounds are of the general formula ##STR1## wherein:k is an integer of 1-2,n is an integer of 1-3,X is an anion of a strong acid, andY is selected from among ##STR2## which are bound to the nitrogen atoms of a heterocyclic compound, M, which is a 5 or 6 membered ring.Type: GrantFiled: November 6, 1984Date of Patent: October 15, 1985Assignee: Vyzkumny ustav zuslechtovaciInventors: Drahomir Dvorsky, Karel Cerovsky
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Patent number: 4542217Abstract: Quaternary ammonium compounds suitable for use in finishing cellulose fiber containing textile material are described. The compounds are of the general formula ##STR1## wherein k is an integer of 1-2,n is an integer of 1-3,X is an anion of a strong acid, andY is selected from among ##STR2## and ##STR3## groups which are bound to the nitrogen atoms of a heterocyclic compound, M, which is a 5 or 6 membered ring.Type: GrantFiled: November 6, 1984Date of Patent: September 17, 1985Assignee: Vyzkumny ustav zuslechtovaciInventors: Drahomir Dvorsky, Karel Cerovsky
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Patent number: 4542130Abstract: MIcrobicidally active 5-aminomethyl-1,3-oxathiolanes of the formula ##STR1## in which R.sup.1 is tetrahydronaphthyl, decahydronaphthyl or optionally substituted naphthyl, optionally substituted cycloalkyl or cycloalkenyl, optionally substituted phenyl, or alkyl which is substituted by phenyl, phenoxy, phenylthio, cyclohexyl, cyclohexyloxy or cyclohexylthio, each of which is optionally substituted,R.sup.2 is hydrogen or methyl,R.sup.3 is alkyl, andR.sup.4 is alkyl, alkenyl or optionally substituted aralkyl, orR.sup.3 and R.sup.4, together with the nitrogen atom to which they are bonded, form an optionally substituted saturated heterocyclic structure which can contain further heteroatoms,or a plant-tolerated addition product thereof with an acid or metal salt.Type: GrantFiled: June 27, 1984Date of Patent: September 17, 1985Assignee: Bayer AktiengesellschaftInventors: Joachim Weissmuller, Wolfgang Kramer, Dieter Berg, Paul Reinecke, Wilhelm Brandes, Gerd Hanssler
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Patent number: 4537989Abstract: A compound of the formula ##STR1## wherein X.sup.1 is a free or an esterified carboxyl group, or a group of the formula: ##STR2## (R.sup.a and R.sup.b are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7 membered saturated heterocyclic group), Y is a group of the formula: ##STR3## (R.sup.6 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) or ##STR4## (R.sup.6 is as defined above), R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sup.1 and R.sup.2, when taken together, mean a single linkage to form a double bond between the carbon atoms which they are linked, R.sup.3 is a hydroxyl group or a protected hydroxyl group, R.sup.4 is a hydrogen atom or a C.sub.1 -C.sub.Type: GrantFiled: April 15, 1983Date of Patent: August 27, 1985Assignee: Sumitomo Chemical Company, LimitedInventors: Keiichi Ono, Akihiko Sugie, Masami Muraoka, Michihiro Yamamoto
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Patent number: 4530925Abstract: Compounds are described of the formulae (1a) and (1b) ##STR1## in which: --COR.sup.1 is an ester group,n is 1 or 2,W is C.sub.1-7 alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,Y is a saturated heterocyclic amino group,R.sup.2 is substituted or unsubstituted phenylalkyl, thienylalkyl or naphthylalkyl or cinnamyl, andR.sup.3 is --H or C.sub.1-5 alkanoyl, including their salts.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic or antiasthmatic agents.Type: GrantFiled: March 14, 1984Date of Patent: July 23, 1985Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw
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Patent number: 4507297Abstract: A compound is disclosed which has the formula, ##STR1## where R.sup.1 is a hydrogen atom, or a straight or branched chain alkyl group having 1 to 4 carbon atoms, and R.sup.2 is a straight or branched chain alkyl group having 1 to 4 carbon atoms, ##STR2## in which n is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof. A process for producing the compound and a medicine containing the compound are also disclosed. Such medicine is effectively useful for inhibiting myocardial infarction.Type: GrantFiled: March 25, 1982Date of Patent: March 26, 1985Assignee: Nippon Chemiphar Co., Ltd.Inventors: Tomoh Masaki, Toshiro Kamishiro, Takashi Okazoe, Koichi Kumakura, Mitsuo Masaki
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Patent number: 4507292Abstract: Aryl N-oxalyl-N-methyl-carbamates of the general formula ##STR1## in which X represents an alkoxy, alkenoxy, alkinoxy, aryloxy, alkylthio, alkenylthio, alkinylthio or arylthio radical, each of which may be optionally substituted, or represents a radical of the general formula --N R.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are identical or different and represent a hydrogen atom or an alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl or aryl radical, each of which may be optionally substituted,or the radicals R.sup.3 and R.sup.4, together with the N atom to which they are bonded, form an optionally substituted heterocyclic ring, andR.sup.1 represents an aryl radical which is optionally substituted,are novel and find use as pesticides, especially for combating insects, acarids and nematodes.Type: GrantFiled: January 27, 1983Date of Patent: March 26, 1985Assignee: Bayer AktiengesellschaftInventors: Gerhard Heywang, Engelbert Kuhle, Wolfgang Behrenz, Ingeborg Hammann, Bernhard Homeyer
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Patent number: 4501874Abstract: This invention is novel compounds containing one or more 2,3-epoxyalkyl carbamate moieties wherein the carbamate nitrogen is tertiary; prepared by a process which comprises(A) contacting an epihalohydrin carbonate with a secondary amine-containing compound wherein the secondary amine has a pKa of between 6 and 12, in a polar organic solvent under conditions such that a 3-halo-2-hydroxyalkyl carbamate wherein the carbamate nitrogen is tertiary is prepared; and(B) contacting the 3-halo-2-hydroxyalkyl carbamate with an alkali metal hydroxide, alkaline earth metal hydroxide, a secondary amine with a pH of 8 or grater, or an ion-exchange resin with pendant moieties containing hydroxide moieties or a secondary amine moiety with a pH of 8 or greater, in a lower alkanol solvent under conditions such that the 3-halo-2-hydroxy moieties are converted to 2,3-epoxyalkyl moieties so as to prepare a 2,3-epoxyalkyl carbamate.Type: GrantFiled: May 2, 1984Date of Patent: February 26, 1985Assignee: The Dow Chemical CompanyInventor: Joseph W. Hanafin
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Patent number: 4499282Abstract: Quaternary ammonium compounds suitable for use in finishing cellulose fiber containing textile material are described. The compounds are of the general formula ##STR1## wherein k is an integer of 1-2,n is an integer of 1-3,X is an anion of a strong acid, andY is selected from among ##STR2## which are bound to the nitrogen atoms of a heterocyclic compound, n, which is a 5 or 6 membered ring.Type: GrantFiled: July 21, 1983Date of Patent: February 12, 1985Assignee: Vyzkumny ustav zuslechtovaciInventors: Drahomir Dvorsky, Karel Cerovsky
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Patent number: 4496723Abstract: Compounds which themselves are antibacterially active and/or which are useful as intermediates for producing antibacterially active materials such as penicillins and cephalosporins are obtained by the following syntheses:Benzyl-2-(2,2-dimethyl-1,3-dioxan-5-ylidene)-2(N-formyl-1)-aminoacetate to benzyl-2,2-dimethylspiro-[1,3-dioxane-5,5'-1',3-thiazoline]-4'-carboxylate to benzyl 2-(2,2-dimethyl-1,3-dioxan-5-ylidene)-2[N-(methylthiomethylene)-amino] acetate to benzyl 2-(trans-3-azido-4-methylthio-2-oxo-1-azetidinyl)-2-(2,2-dimethyl-1,3-diox an-5-ylidene) acetate to benzyl 2(trans-3-benzoylamino-4-methylthio-1-azetidinyl)-2-(2,2-dimethyl-1,3-diox an-5-ylidene) acetate to either (1) benzyl 2-(7-oxo-3-phenyl-4-oxa-2,6-diazabicyclo[3.2.0]hept-2-en-6-yl)-2-(2,2-dime thyl-1.3-dioxan-5-ylidene)acetate or (2) benzyl 2-(trans-3-benzoylamino-4-chloro-1-azetidinyl)-2-(2,2-dimethyl-1,3-dioxan- 5-ylidene) acetate and then to the product benzyl-7-benzoylamino-1-dethia-1-oxa-3-hydroxymethyl-cephem-4-carboxylate.Type: GrantFiled: June 20, 1983Date of Patent: January 29, 1985Assignee: Bayer AktiengesellschaftInventors: Dieter Hoppe, Heinz-Werner Kleemann
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Patent number: 4483988Abstract: Novel analgesic and antipsychotic agents having the formula ##STR1## in which R.sub.1 is hydrogen, hydroxy or halogen and R.sub.4 is hydrogen or, R.sub.1 and R.sub.4 are both hydroxy; Z is hydrogen or straight chain lower alkyl having from 1 to 4 carbon atoms and X is methylene, carbonyl, hydroxymethylene, thio, sulfinyl or sulfonyl, or Z and X, taken together, are methylidenyl, with the proviso that when X is sulfonyl or sulfinyl, Z is other than hydrogen; R.sub.5 is hydrogen or halogen, and R.sub.2 is H, a straight or branched lower alkyl group having from 1 to 4 carbon atoms, the group ##STR2## or the group ##STR3## wherein R.sub.3 is hydroxy, amino, alkylamino or dialkylamino wherein the alkyl moiety is straight or branched and has from 1 to 4 carbon atoms, diastereomers, enantiomers and pharmaceutically acceptable salts thereof.Type: GrantFiled: July 19, 1982Date of Patent: November 20, 1984Assignee: Richardson Merrell Inc.Inventors: Albert A. Carr, Robert A. Farr, John M. Kane
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Patent number: 4482549Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienzlalkyl, naphthylalkyl or cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: February 8, 1984Date of Patent: November 13, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter, Alan Wadsworth
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Patent number: 4468228Abstract: Quaternary ammonium compounds suitable for use in finishing cellulose fiber containing textile material are described. The compounds are of the general formula ##EQU1## wherein k is an integer of 1-2,n is an integer of 1-3,X is an anion of a strong acid, andY is selected from among ##STR1## which are bound to the nitrogen atoms of a heterocyclic compound, n, which is a 5 or 6 membered ring.Type: GrantFiled: July 21, 1983Date of Patent: August 28, 1984Assignee: Vykumny ustav zuslechtovaciInventors: Drahomir Dvorsky, Karel Cerovsky
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Patent number: 4460774Abstract: A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and an acid addition salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.Type: GrantFiled: February 12, 1982Date of Patent: July 17, 1984Assignee: Toyama Chemical Company, LimitedInventors: Takako Hori, Chosaku Yoshida, Yasuo Kiba, Ryuko Takeno, Joji Nakano, Jun Nitta, Sumiko Kishimoto, Shohachi Murakami, Hisatsugu Tsuda, Isamu Saikawa
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Patent number: 4459407Abstract: A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and a salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.Type: GrantFiled: February 2, 1982Date of Patent: July 10, 1984Assignee: Toyama Chemical Co., Ltd.Inventors: Takako Hori, Chosaku Yoshida, Yasuo Kiba, Ryuko Takeno, Joji Nakano, Jun Nitta, Sumiko Kishimoto, Shohachi Murakami, Hisatsugu Tsuda, Isamu Saikawa
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Patent number: 4459410Abstract: Diphenylalkanoether and diphenylalkanone oximeether derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an aryl group optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, di(C.sub.1 -C.sub.4)alkylamino, amino, benzyloxy, hydroxyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkysulfonyl, C.sub.1 -C.sub.4 alkanoylamino, C.sub.1 -C.sub.4 alkylmino and N-(C.sub.1 -C.sub.4)alkyl-N-(C.sub.1 -C.sub.4)alkanoylamino, Z.sup.1 is a group of the formula: ##STR2## (wherein R.sup.3 and R.sup.4 are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or an ar(C.sub.1 -C.sub.Type: GrantFiled: October 5, 1981Date of Patent: July 10, 1984Assignee: Sumitomo Chemical Company, LimitedInventors: Keiichi Ono, Hajime Kawakami, Junki Katsube
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Patent number: 4435571Abstract: The present invention relates to compounds of the formula ##STR1## wherein R' is hydrogen, straight or branched chain lower alkyl having from 1 to 4 carbon atoms or benzyl, Z is hydrogen or straight chain lower alkyl having from 1 to 4 carbon atoms, Y is hydrogen or a nitrogen blocking group selected from the group consisting of tertiary alkoxycarbonyl, benzyloxycarbonyl, cycloalkoxycarbonyl and vinyloxycarbonyl, R.sub.c is hydrogen, halogen or benzyloxy and R.sub.d is hydrogen, or R.sub.c and R.sub.d are benzyloxy; or an individual diastereomer thereof. Said compounds having use as intermediates in the production of enkephalin derivatives which in turn are used as analgesic and antipsychotic agents.Type: GrantFiled: July 19, 1982Date of Patent: March 6, 1984Assignee: Richardson Merrell Inc.Inventors: Albert A. Carr, Robert A. Farr, John M. Kane
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Patent number: 4426521Abstract: Novel cyanoguanidine derivatives, and acid addition salts thereof useful as medicines which have pharmacological actions such as anti-secretory effect, local anesthesia action and the like; and process for the preparation thereof.Type: GrantFiled: January 28, 1982Date of Patent: January 17, 1984Assignee: Eisai Co., Ltd.Inventors: Satoru Tanaka, Katsutoshi Shimada, Kazunori Hashimoto, Kiichi Ema, Koichiro Ueda
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Patent number: 4410521Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienylalkyl, naphthylalkyl or cinnamyl,and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstruction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: September 16, 1982Date of Patent: October 18, 1983Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter
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Patent number: 4387238Abstract: The epoxysuccinamic acid compounds of the present invention are prepared by reaction of monoesters of epoxysuccinic acid or monoesters of epoxysuccinic acid chloride with amino compounds. These epoxysuccinamic acid compounds have excellent anti-inflammatory activity, thiol protease inhibitory activity, muscular dystrophy inhibitory activity and anti-hypertensive activity without acceleration of vascular permeability.Type: GrantFiled: May 14, 1981Date of Patent: June 7, 1983Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masami Goi, Kazuya Kameo, Jiro Sawada, Kazunori Hanada, Masaharu Tamai, Kiyoshi Oguma
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Patent number: 4374990Abstract: A compound having the general formula or an acid addition salt thereof ##STR1## in which formula R.sub.1 is selected from the group consisting of(A) an at least mononuclear heterocyclic group having 4 to 10 carbon atoms in the ring system bound to the group ##STR2## through a carbon atom and containing at least one oxygen, nitrogen or sulphur atom,(B) substitution products of (A) containing at least one substituent selected from the group consisting of halogen, trifluoromethyl, hydroxy, alkoxy of 1 to 3 carbon atoms, unsubstituted amino, amino substituted by up to two alkyl groups each having 1 to 3 carbon atoms and alkyl groups having 1 to 6 carbon atoms,X is oxygen, sulphur or an NH-group,Y is an alkylene group having 1 to 3 carbon atoms in the chain, or an alkylene group having 1 to 3 carbon atoms in the chain substituted by (a) up to 3 alkyl groups each having up to 3 carbon atoms and a total of not more than 8 carbon atoms, or (b) substituted by one or two phenyl groups,R.sub.Type: GrantFiled: October 26, 1979Date of Patent: February 22, 1983Assignee: Hoechst AktiengesellschaftInventors: Rolf-Ortwin Weber, Alfons Soder, Istvan Boksay
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Patent number: 4354028Abstract: Novel amide acetals of the formula ##STR1## wherein R.sub.1 is hydrogen, methyl or Y and Y is the remnant of a hydroxyl-containing compound are claimed. The compounds are useful as water scavengers in fluid compositions.Type: GrantFiled: April 9, 1981Date of Patent: October 12, 1982Assignee: The Dow Chemical CompanyInventors: John Martin, George A. Doorakian, Lawrence G. Duquette
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Patent number: 4349679Abstract: Phthalide compounds of the formula ##STR1## wherein A and B, independently of the other, represent a monovalent radical of the formula ##STR2## wherein X.sub.1 represents an amino group of the formula ##STR3## X.sub.2 represents halogen or an amino group of the formula ##STR4## W is hydrogen or halogen, R.sub.1 and T.sub.1 each represents alkyl of at most 12 carbon atoms which is unsubstituted or substituted by halogen, hydroxyl, cyano, lower alkoxy or lower alkylcarbonyloxy, cycloalkyl, phenyl, benzyl or phenyl or benzyl which are substituted by halogen, nitro, lower alkyl or lower alkoxy, R.sub.2 and T.sub.2 each represents hydrogen, alkyl of at most 12 carbon atoms, which is unsubstituted or substituted by halogen, hydroxyl cyano, lower alkoxy or lower alkyl-carbonyloxy; cycloalkyl, benzyl or benzyl which is substituted by halogen, nitro, lower alkyl or lower alkoxy, and T.sub.2 may also represent acyl having 1 to 8 carbon atoms or each pair of substituents R.sub.1 and R.sub.2 or T.sub.1 and T.sub.Type: GrantFiled: May 10, 1979Date of Patent: September 14, 1982Assignee: Giba-Geigy CorporationInventors: Robert Garner, Michael J. Whitehead
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Patent number: 4336382Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of lower alkyl; R.sub.8 is selected from the group consisting of --O--(CH.sub.2).sub.n --wherein n is 2 to 20, ##STR2## and R.sub.6 is selected from the group consisting of hydrogen or lower alkoxy, and ##STR3## wherein R.sub.1 is selected from the group consisting of lower alkyl; R.sub.8 is selected from the group consisting of --O--(CH.sub.2).sub.n --wherein n is 2 to 20, ##STR4## and R.sub.6 is selected from the group consisting of hydrogen or lower alkoxy and racemates thereof.There are also disclosed processes and intermediates utilized to produce the end products.The end products have utility as agents exhibiting both .alpha. and selective .beta. adrenergic blocking action.Type: GrantFiled: August 25, 1980Date of Patent: June 22, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Kenneth E. Fahrenholtz, Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
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Patent number: 4334066Abstract: A pyran derivative represented by the formula ##STR1## wherein R.sub.1 and R.sub.4 are each the same or different alkyl having 1 to 6 carbon atoms, R.sub.2 and R.sub.3, when attached to a nitrogen atom, forms a saturated hetrocyclic ring which has as a hetero atom a nitrogen atom is addition to the nitrogen atom attached to R.sub.2 and R.sub.3, or oxygen atom, and an acid addition salt thereof. The compounds have antibacterial and insecticidal action.Type: GrantFiled: April 20, 1981Date of Patent: June 8, 1982Assignee: Otsuka Kagaku Yakuhin Kabushiki KaishaInventors: Yasuo Shimizu, Hisashi Takao, Shoji Asano, Shuya Shimada, Kazutoshi Kikkawa
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Patent number: 4323550Abstract: Halogenohydrates of N,N'-disubstituted derivatives of piperazine of the general formula: ##STR1## wherein YR is a hydroxylalkyl, polyhydroxyalkyl or epoxyalkyl wherein Y is a hydroxy, polyhydroxy or epoxy group, R is lower alkyl C.sub.2 -C.sub.4, and X is a member selected from the group consisting of fluorine, bromine, chlorine and iodine. The compounds have useful anticariogenic properties.Type: GrantFiled: February 17, 1977Date of Patent: April 6, 1982Inventor: Jean-Jacques Goupil
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Patent number: 4297354Abstract: Compounds of the steroisomeric formulas ##STR1## wherein R.sub.1 and R.sub.2, which may be identical to or different from each other, are each phenyl, substituted phenyl, thienyl or furyl;R.sub.3 is hydrogen or straight or branched alkyl of 1 to 3 carbon atoms; andR.sub.4 is straight or branched alkyl of 1 to 3 carbon atoms; orR.sub.3 and R.sub.4, together with each other and the nitrogen atom to which they are attached, form a piperidino, 4-amino-piperidino, 4-(lower alkylamino)-piperidino, piperazino, 4-(alkyl of 1 to 2 carbon atoms)-piperazino or morpholino radical; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antidepressants.Type: GrantFiled: December 15, 1980Date of Patent: October 27, 1981Assignee: Boehringer Ingelheim GmbHInventors: Karl-Heinz Weber, Claus Schneider, Gerhard Walther, Karl-Heinz Pook, Karin Boke, Wolf D. Bechtel
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Patent number: 4293462Abstract: The invention concerns a process for the manufacture of 7.beta.-amino-3-cephem-3-ol-4-carboxylic acid compounds by ring closure of esters of 2-[4-(substituted-thio)-3-acylamino-2-oxoazetidin-1-yl]-3-substituted-amin o-crotonic acids and solvolyzing the enamino group in the resulting 7.beta.-acylamino-3-substituted-amino-cephem-4-carboxylic acid esters.Type: GrantFiled: December 10, 1979Date of Patent: October 6, 1981Assignee: Ciba-Geigy CorporationInventors: Robert B. Woodward, Hans Bickel
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Patent number: 4291159Abstract: The present invention provides novel analogs of the thromboxanes. These thromboxane analogs are useful for a variety of pharmacologically useful purposes, most particularly as antithrombotic agents.Type: GrantFiled: January 28, 1980Date of Patent: September 22, 1981Assignee: The Upjohn CompanyInventor: Douglas R. Morton, Jr.
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Patent number: 4279902Abstract: Acetamide derivatives are provided having the structure ##STR1## wherein X is a single bond, --CH.sub.2 -- or --O--, R.sup.1 and R.sup.2 may be the same or different and are lower alkyl, phenyl-lower alkoxy-lower alkyl, lower alkenyl, phenyl-lower alkyl or lower alkoxy, or ##STR2## may be taken together to form a 5- to 7-membered heterocyclic ring optionally containing one other hetero atom, such as nitrogen, sulfur or oxygen; Y is hydroxyl, OR wherein R is lower alkyl, lower alkenyl or lower alkanoyl, or ##STR3## wherein R.sup.1 and R.sup.2, and R.sup.1 and R.sup.2 taken together with the nitrogen to which they are attached are as defined above, and n is 1 to 6.These compounds are useful as anti-arrhythmia agents and have been found to be effective in the treatment of acute myocardial infarction.Type: GrantFiled: August 6, 1980Date of Patent: July 21, 1981Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic P. Hauck, Glenn A. Jacobs
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Patent number: 4267175Abstract: A compound of the formula (I), and pharmaceutically acceptable salts thereof: ##STR1## 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, hydroxy, C.sub.1-6 alkoxy, C.sub.2-7 acyl, amino, amino substituted by one or two C.sub.1-6 alkyl groups, C.sub.2-10 acyl amino, aminosulphone, aminosulphone substituted by one or two C.sub.1-6 alkyl groups, C.sub.1-6 alkyl sulphone or nitro groups; andA is a C.sub.2-4 alkylene group;R.sub.5 and R.sub.6 are joined so that they form with the --N--A--N-- group to which they are attached, a 6, 7 or 8 membered heterocyclic ring;R.sub.7 is a C.sub.1-6 alkyl group, or an aryl --C.sub.1-6 akyl group in which the alkyl moiety is optionally substituted by a C.sub.1-6 alkyl or aryl group; have useful pharmacological activity, such as the ability to regulate the gastrointestinal function and to treat emesis.Type: GrantFiled: March 8, 1979Date of Patent: May 12, 1981Assignee: Beecham Group LimitedInventor: Eric A. Watts
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Patent number: 4247690Abstract: There is presented compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of aryl, substituted aryl, aralkyl, heteroaryl, cycloalkyl, lower alkyl, lower alkenyl, carboxy lower alkyl, carboalkoxy lower alkyl, aminoalkyl, substituted aminoalkyl, hydroxyalkyl, alkoxy alkyl, thioalkoxy alkyl and hydrogen.These compounds exhibit pharmacological activity as antihypertensive agents.Also presented are novel intermediates leading to the end products and a process to produce the end products.Type: GrantFiled: October 1, 1979Date of Patent: January 27, 1981Assignee: Hoffmann-La Roche Inc.Inventor: David Coffen
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Patent number: 4242343Abstract: Phenylpiperazine derivatives corresponding to the formula (I) ##STR1## in which n is 1, 2 or 3 and R represents the tetrahydrofuryl-2 radical, or the radical CH.sub.2 -SH, or a radical CH.sub.2 -S-alkyl, or a radical CH.sub.2 -O-alkyl or a radical CH.sub.2 -S-CO-alkyl, the alkyls having from 1 to 8 carbon atoms,and also their addition salts with pharmaceutically acceptable acids.These compounds are tranquilizers with psychotropic properties which permit their use in anxiety and depression.Type: GrantFiled: June 15, 1979Date of Patent: December 30, 1980Assignee: SynthelaboInventors: Henry Najer, Philippe Manoury
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Patent number: 4202978Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of lower alkyl; R.sub.8 is selected from the group consisting of --O--(CH.sub.2).sub.n --wherein n is 2 to 20, ##STR2## and R.sub.6 is selected from the group consisting of hydrogen or lower alkoxy, and ##STR3## wherein R.sub.1 is selected from the group consisting of lower alkyl; R.sub.8 is selected from the group consisting of --O--(CH.sub.2).sub.n --wherein n is 2 to 20, ##STR4## and R.sub.6 is selected from the group consisting of hydrogen or lower alkoxy and racemates thereof.There are also disclosed processes and intermediates utilized to produce the end products.The end products have utility as agents exhibiting both .alpha. and selective .beta. adrenergic blocking action.Type: GrantFiled: February 8, 1978Date of Patent: May 13, 1980Assignee: Hoffmann-La Roche Inc.Inventors: Kenneth E. Fahrenholtz, Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
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Patent number: 4189468Abstract: A cosmetic composition for the hair comprises at least one water-soluble crosslinked polymer obtained by crosslinking a polyamino-polyamide with a crosslinking agent, said polyamino-polyamide being prepared by the polycondensation of (a) an acidic compound selected from the group consisting of (i) organic dicarboxylic acid, (ii) ethylenically unsaturated aliphatic mono- or di-carboxylic acid, (iii) ester of said acids of (i) and (ii), and (iv) mixtures of (i), (ii) and (iii) on (b) a polyamine selected from the group consisting of bis-primary and mono- or bis-secondary polyalkylene polyamines, said polyamine (b) being replaceable by a member selected from the group consisting of (1) 0-20 mole percent hexamethylene diamine, (2) 0-40 mole percent bis-primary amine and (3) 0-40 mole percent bis-secondary amine, said crosslinking agent being selected from the group consisting of (a') simple bi-functional compounds selected from bis-halohydrins, bis-azetidinium, bis-haloacyl diamine and alkyl bis-halides, (b') oliType: GrantFiled: February 27, 1978Date of Patent: February 19, 1980Assignee: L'OrealInventors: Guy Vanlerberghe, Henri Sebag, Jean-Francois Grollier, Alexandre Zysman
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Patent number: 4179505Abstract: Novel 5-[4-(diarylmethyl)-1-piperazinylalkyl]benzimidazole derivatives having antiallergic and antihistaminic properties.Type: GrantFiled: January 4, 1978Date of Patent: December 18, 1979Assignee: Janssen Pharmaceutica N.V.Inventors: Alfons H. M. Raeymaekers, Josephus L. H. Van Gelder, Gustaaf M. Boeckx, Lodewijk L. Van Hemeldonck
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Patent number: 4147792Abstract: N-Acylated N-phenyl-aminotetrahydro-2-furanones of the formula I are valuable fungicidal active substances. They can be used as fungicidal compositions, particularly for combatting phytopathogenic fungi, e.g. against downy mildew on potatoes, tomatoes, grape vines and sugar beet and other plants. The novel compounds have a systemic action.Type: GrantFiled: January 30, 1978Date of Patent: April 3, 1979Assignee: Ciba-Geigy CorporationInventors: Walter Kunz, Wolfgang Eckhardt, Adolf Hubele
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Patent number: 4122035Abstract: A process for recovering a catalyst adsorbent from a polyol-adsorbent residue by treatment of the polyol-adsorbent residue with organic solvents. This adsorbent can then be recycled for use in the further removal of alkaline catalysts from polyether polyols.Type: GrantFiled: December 17, 1976Date of Patent: October 24, 1978Assignee: BASF Wyandotte CorporationInventor: Carl Casimer Cislo
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Patent number: 4115569Abstract: A compound having the general formula or an acid addition salt thereof ##STR1## in which formula R.sub.1 is selected from the group consisting ofA. an at least mononuclear heterocyclic group having 4 to 10 carbon atoms in the ring system bound to the group ##STR2## through a carbon atom and containing at least one oxygen, nitrogen or sulphur atom,B. substitution products of (A) containing at least one substituent selected from the group consisting of halogen, trifluoromethyl, hydroxy, alkoxy of 1 to 3 carbon atoms, unsubstituted amino, amino substituted by up to two alkyl groups each having 1 to 3 carbon atoms and alkyl groups having 1 to 6 carbon atoms,X is oxygen, sulphur or an NH-group,Y is an alkylene group having 1 to 3 carbon atoms in the chain, or an alkylene group having 1 to 3 carbon atoms in the chain substituted by (a) up to 3 alkyl groups each having up to 3 carbon atoms and a total of not more than 8 carbon atoms, or (b) substituted by one or two phenyl groups,R.sub.Type: GrantFiled: August 21, 1975Date of Patent: September 19, 1978Assignee: Hoechst AktiengesellschaftInventors: Rolf-Ortwin Weber, Alfons Soder, Istvan Boksay
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Patent number: 4112231Abstract: A process is provided for the condensation of epoxides with organic compounds having an active hydrogen atom, such as alcohols, polyols, and amines, in the presence of a neutral inorganic salt selected from the group consisting of sodium fluoborate, magnesium perchlorate, calcium perchlorate, manganese perchlorate, nickel perchlorate and zinc perchlorate.Type: GrantFiled: September 1, 1976Date of Patent: September 5, 1978Assignee: Berol Kemi ABInventors: Bengt John Gustaf Weibull, Leif Urban Folke Thorsell
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Patent number: 4092416Abstract: Benzopyrones of the formula ##STR1## wherein R.sub.1 is a hydrogen or halogen atom or a hydroxyl, lower alkyl, alkoxy, alkylthio or trifluoromethyl radical,R.sub.2, r.sub.3, r.sub.4 and R.sub.5 each independently is hydrogen, a halogen atom, a hydroxyl radical, a lower alkyl or lower alkoxy radical, or a lower alkyl or lower alkoxy radical substituted by at least one of hydroxyl, halogen, mesyloxy or tosyloxy or by an oxirane, dioxane or dioxolane ring,A is a lower alkylene radical, andn is 0, 1 or 2,And salts thereof exhibit anti-allergic activity.Type: GrantFiled: December 1, 1976Date of Patent: May 30, 1978Assignee: Boehringer Mannheim GmbHInventors: Werner Winter, Max Thiel, Kurt Stach, deceased, Androniki Roesch, by Werner Plattner, administrator, Wolfgang Schaumann