Nitrogen Bonded Directly To Chalcogen Patents (Class 548/197)
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Patent number: 4791200Abstract: The present invention relates to novel 2-substituted-4-aryloxyalkylamine thiazoles as described herein. The thiazoles are useful as antisecretory agents.Type: GrantFiled: June 22, 1987Date of Patent: December 13, 1988Assignee: Ortho Pharmaceutical CorporationInventors: Jeffery B. Press, Pauline Sanfilippo, Maud Urbanski
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Patent number: 4766138Abstract: Use of 4-(isoxazolyl)-thiazole-2-oxamic acid derivatives; method for preparing them and intermediate compounds useful for their preparation.Said compounds possess antiarthritic activity; compositions for pharmaceutical use containing said compounds as the active ingredients are also described.Type: GrantFiled: March 13, 1986Date of Patent: August 23, 1988Assignee: Zambon S.p.A.Inventors: Angelo Carenzi, Dario Chiarino, Davide Della Bella, Giancarlo Grancini
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Patent number: 4766137Abstract: 4-(isoxazolyl)-thiazole-2-oxamic acids, esters and salts thereof; method for preparing them and intermediate compounds useful for their preparation.Said compounds possess antiallergic and antianaphylactic activity and may be used in the pharmaceutical field.Compositions for pharmaceutical use containing said compounds as the active ingredients are also described.Type: GrantFiled: March 13, 1986Date of Patent: August 23, 1988Assignee: Zambon S.p.A.Inventors: Angelo Carenzi, Dario Chiarino, Davide Della Bella, Giancarlo Grancini
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Patent number: 4742060Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.Type: GrantFiled: January 21, 1986Date of Patent: May 3, 1988Assignee: Nihon Tokushu Noyaku Seizo K. K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
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Patent number: 4701447Abstract: This invention relates to organic acid-substituted guanidine compounds. Also disclosed are methods for preparing the compounds, compositions containing them, and methods for their use as anthelmintics.Type: GrantFiled: September 23, 1983Date of Patent: October 20, 1987Assignee: Schering CorporationInventors: Dhiru B. Vashi, Jeffrey N. Clark, Neil A. Lindo
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Patent number: 4663341Abstract: This invention relates to N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.Type: GrantFiled: January 11, 1985Date of Patent: May 5, 1987Assignee: Rohm and Haas CompanyInventor: Richard M. Jacobson
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Patent number: 4659727Abstract: Ethene derivatives of the formula:[R.sup.5 (R.sup.1 CR.sup.4 .dbd.CR.sup.2 R.sup.3).sub.m ].sub.n Iwherein R.sup.5 represents optionally substituted heterocyclyl or a group --CR.sup.4 .dbd.CR.sup.2 R.sup.3, or optionally substituted aryl, heterocyclylalkyl or arylalkyl and R.sup.1 represents --NR.sup.6 -- wherein R.sup.6 represents hydrogen or optionally substituted alkyl or aryl, or R.sup.5 represents a quinonoidal group, and R.sup.1 represents .dbd.N--, R.sup.4 represents hydrogen, alkoxy, alkylthio, trifluoromethyl or optionally substituted alkyl or aryl, R.sup.2 represents cyano, formyl, alkoxycarbonyl, alkylsulphonyl, dialkylcarbamoyl, dialkylthiocarbamoyl, aryloxycarbonyl, arylsulphinyl or arylsulphonyl, R.sup.3 represents a group R.sup.2 or hydrogen, nitro or optionally substituted aryl or aroyl or alkanoyl, and m and n are 1 or 2, and pharmaceutically acceptable salts thereof, with the exclusion of certain compounds in which R.sup.Type: GrantFiled: September 10, 1985Date of Patent: April 21, 1987Assignee: May & Baker LimitedInventors: Adnan H. Al-Shaar, Barbara J. Broughton, Robert K. Chambers, David W. Gilmour, Diane M. Kelsey, Peter Lowden, Edward Lunt, David J. Lythgoe, Ian McClenaghan, Duncan C. McDougall, Libert C. Saunders, Keith A. J. Stuttle, Peter J. Warne
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Patent number: 4647557Abstract: This invention relates to novel heterocyclic derivatives bearing an amino group and to processes for making said compounds.More particularly this invention provides novel heterocyclic compounds the hetero ring of which has two hetero atoms, the same or different, substituted with a free or substituted amino group.These compounds are useful as active ingredients of drugs.Type: GrantFiled: December 23, 1983Date of Patent: March 3, 1987Inventors: Gerard Moinet, Michel Schaeffer, Pierre Bessin, Jacqueline Bonnet
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Patent number: 4625025Abstract: Disclosed is a process for producing a heterocyclic compound having a nitromethylene group as the side chain, of the formula ##STR1## wherein Y represents a hydrogen atom, a halogen atom or a lower alkyl group, R represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aralkyl group, an alkenyl group, an alkynyl group or an acyl group, and n represents an integer of 2, 3 or 4,which comprises reacting a 2,2,2-trihalo-1-nitroethane compound with a 1-aminoalkanethiol compound or a 1-N-substituted derivative thereof.Type: GrantFiled: August 10, 1984Date of Patent: November 25, 1986Assignee: Ube Industries, Ltd.Inventors: Fumio Iwata, Katsumasa Harada, Ryoji Sugise
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Patent number: 4622330Abstract: Novel 3-amino or substituted amino pyrazoles are disclosed as having antiprotozoal and antiparasitic activity in particular anticoccidial activity and are useful for controlling cecal and or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry usually in admixture with animal sustenance.Type: GrantFiled: June 19, 1984Date of Patent: November 11, 1986Assignee: Merck & Co., Inc.Inventors: Richard J. Bochis, Richard A. Dybas, Edward F. Rogers
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Patent number: 4604243Abstract: An olefin, especially an activated olefin, is arylated by reaction with an arylamine, such as an aniline, in an inert polar organic solvent and in the presence of an alkyl nitrite, a hydrogen halide, and a catalytic amount of a copper catalyst having the copper in an oxidation state below +2.Type: GrantFiled: July 25, 1985Date of Patent: August 5, 1986Assignee: Ethyl CorporationInventor: Robert I. Davidson
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Patent number: 4596811Abstract: The invention relates to special heterocyclic compounds corresponding to general tautomeric formula I which are distinguished by improved antagonistic activity on histamine-H.sub.2 -receptors. The invention also relates to a process for producing these compounds and to medicaments containing them.Type: GrantFiled: October 18, 1983Date of Patent: June 24, 1986Assignee: Ludwig Heumann & Co., GmbHInventors: Istvan Szelenyi, Stefan Postius, Helmut Schickaneder, Herbert Hansen
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Patent number: 4514566Abstract: Carbamoyl-oxime compounds of the formula ##STR1## wherein A, R.sup.3, R.sup.4 and R.sup.5 are as hereinafter set forth, a process for their preparation, pesticidal compositions containing one or more of these compounds as the active ingredient, methods of use of such compositions for the control of pests, particularly insects, mites, nematodes and molluscs, and intermediates for the production of such compounds are described.Type: GrantFiled: October 27, 1983Date of Patent: April 30, 1985Assignee: Hoffmann-La Roche Inc.Inventors: Christoph Luthy, Paul Winternitz
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Patent number: 4458077Abstract: Compounds of the formulaAr--(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --ONHRwherein R is ##STR1## wherein R.sup.1 is hydrogen or lower alkyl;X is O or CH.sub.2 ;m=0 or 1;n=2 or 3; andAr is a moiety selected from the group ##STR2## wherein R.sub.2 is hydrogen or lower alkyl, ##STR3## with the proviso that when Ar is ##STR4## and X is CH.sub.2, then R is other than ##STR5## and the pharmacologically acceptable salts thereof have H.sub.2 -antagonist activity and activity in decreasing gastric acid secretions.Type: GrantFiled: November 22, 1982Date of Patent: July 3, 1984Assignee: American Home Products CorporationInventor: John R. Potoski
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Patent number: 4452985Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, cyano or cyano(lower)alkyl;R.sup.2 is hydrogen, cyano, carboxy, carbamoyl, guanyl, (lower)alkoxyimino, hydrazinocarbonyl, (lower)alkylaminoimino, ##STR2## with the proviso that one but never both of R.sup.1 and R.sup.2 is hydrogen; and the pharmacologically acceptable salts thereof exhibit H.sub.2 -receptor antagonist and gastric secretion inhibition activity.Type: GrantFiled: February 14, 1983Date of Patent: June 5, 1984Assignee: American Home Products CorporationInventors: Arthur A. Santilli, Anthony C. Scotese, Robert L. Morris, Stanley C. Bell
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Patent number: 4421757Abstract: Thiazoline derivatives of the formula I ##STR1## wherein R.sup.1 to R.sup.6 and Y have the meanings given, their physiologically tolerated salts, processes for their preparation, pharmaceutical preparations based on these compounds as well as their use as medicaments comprise the invention. In addition, intermediates are described.Type: GrantFiled: December 28, 1981Date of Patent: December 20, 1983Assignee: Hoechst AktiengesellschaftInventors: Hans-Jochen Lang, Bernhard Seuring, Ernold Granzer
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Patent number: 4409216Abstract: A compound, with hypoglycaemic activity, having formula (II) or a pharmaceutically acceptable acid addition salt thereof: ##STR1## wherein X represents oxygen or sulphur;R.sup.1 R.sup.2 are the same or different and represent hydrogen, halogen, C.sub.1-6 alkyl, phenyl, benzyl,C.sub.3-6 cycloalkyl, carbo-C.sub.1-6 alkoxy or C.sub.1-6 carboxy or R.sup.1 and R.sup.2 represent the remaining members of a benzene ring;R.sup.3 represents hydrogen, C.sub.1-6 alkyl, phenyl or benzyl;R.sup.4 represents hydrogen or C.sub.1-6 alkyl;R.sup.5 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.4 and R.sup.5 together represent the remaining members of a 5- or 6- membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl; andR.sup.Type: GrantFiled: April 11, 1980Date of Patent: October 11, 1983Assignee: Beecham Group LimitedInventor: Barrie C. C. Cantello
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Patent number: 4346088Abstract: Thiazoline derivatives of the general formula I ##STR1## wherein R.sup.1 to R.sup.7 have the specified meanings, physiologically acceptable acid addition salts thereof, processes for their preparation, pharmaceutical preparations based on these compounds and their use for acting on the serum lipoprotein spectrum. The invention moreover relates to compounds of the formulae ##STR2## wherein A, R, R.sup.1 to R.sup.7, Y and Z have the specified meanings.Type: GrantFiled: July 1, 1980Date of Patent: August 24, 1982Assignee: Hoechst AktiengesellschaftInventors: Hans-Jochen Lang, Bernhard Seuring, Ernold Granzer
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Patent number: 4331680Abstract: Novel compounds are described which are substituted benzophenone hydrazones. They have pesticidal activity, especially against insects and acarids, and pesticidal compositions and methods are described. Methods of making the compounds, and novel intermediates, are also described.Type: GrantFiled: August 25, 1980Date of Patent: May 25, 1982Assignee: The Boots CompanyInventors: David P. Giles, John C. Kerry, Antonin Kozlik, Bryan H. Palmer, Stephen W. Shutler, Robert J. Willis
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Patent number: 4331668Abstract: 3-Nitro-2-substituted aminopyrroles are histamine H.sub.2 -receptor antagonists. The 2- position substituent is a fully-unsaturated heterocyclyl alkyl group preferably with alkyl group interrupted by sulfur or oxygen. The 4- and 5- positions of the pyrrole ring can also be substituted.Type: GrantFiled: June 16, 1980Date of Patent: May 25, 1982Assignee: Smith Kline & French Laboratories LimitedInventors: Michael L. Roantree, Rodney C. Young
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Patent number: 4315931Abstract: Unsubstituted or substituted 5-phenyl- and 5-benzyl-4-amino-pyrimidine-2-imidoacid esters, their preparation, drugs containing these compounds, and their use in infectious diseases.Type: GrantFiled: July 3, 1978Date of Patent: February 16, 1982Assignee: BASF AktiengesellschaftInventors: Peter Scharwaechter, Klaus Gutsche, Wilhelm Kohlmann, Gerd Kroemer, deceased, by Norma Kroemer, legal representative, by Helmut Kroemer, legal representative, by Maria M. Kroemer, legal representative
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Patent number: 4307104Abstract: The compounds of this invention are 2,3-unsaturated nitrogen containing heterocyclic compounds with a 3-nitro group and a 2-(2-guanidino-4-thiazolyl alkylamino) group. These compounds have histamine H.sub.2 -antagonist activity. A particular compound of this invention is 2-[2-(2-guanidino-4-thiazolylmethylthio)ethylamino]-3-nitro-1,4,-5,6-tetra hydropyridine.Type: GrantFiled: October 14, 1980Date of Patent: December 22, 1981Assignee: Smith Kline & French Laboratories LimitedInventors: Michael L. Roantree, Rodney C. Young
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Patent number: 4283408Abstract: Novel guanidinothiazole compounds of the general formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, R.sub.1 represents an amino group, a lower alkyl group, a halogeno lower alkyl group, a substituted- or unsubstituted-aryl group, a mono- or di-lower alkylamino group, an arylamino group or an aralkylamino group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, Y represents a sulfur atom or a methylene group, m and n, each represents an integer of 1-3, and the pharmacologically acceptable acid addition salts thereof, they are useful as gastric acid secretion inhibitors.Type: GrantFiled: December 27, 1979Date of Patent: August 11, 1981Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Yasufumi Hirata, Isao Yanagisawa, Yoshio Ishii, Shinichi Tsukamoto, Noriki Ito, Yasuo Isomura, Masaaki Takeda
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Patent number: 4200578Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 and R.sup.3 each are independently hydrogen, (lower)alkyl, guanidino or --(CH.sub.2).sub.p NR.sup.4 R.sup.5 ; R.sup.4 and R.sup.5 each are independently hydrogen, (lower)alkyl or phenyl; n is 2 or 3; p is 1, 2 or 3; X is NR.sup.6 or CHR.sup.6 ; R.sup.6 is cyano, nitro, SO.sub.2 Ar or SO.sub.2 (lower)alkyl; and Ar is phenyl or phenyl containing 1 or 2 substituents selected from halogen and (lower)alkyl; and nontoxic, pharmaceutically acceptable salts thereof, are potent anti-ulcer agents.Type: GrantFiled: December 18, 1978Date of Patent: April 29, 1980Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4166856Abstract: The compounds are novel N-substituted-N'-heterocyclic alkylthioureas, guanidines and 1-nitro-2,2-diaminoethylene compounds which are histamine H.sub.2 -antagonists.Type: GrantFiled: March 31, 1978Date of Patent: September 4, 1979Assignee: Smith Kline & French Laboratories LimitedInventors: Graham J. Durant, Charon R. Ganellin, Geoffrey R. Owen, Rodney C. Young