Five-membered Hetero Ring Having Two Or More Ring Hetero Atoms Of Which At Least One Is Nitrogen Patents (Class 544/366)
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Patent number: 4448963Abstract: 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 22, 1982Date of Patent: May 15, 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: 4438112Abstract: Prostanoids are described of the formulae ##STR1## (and the salts thereof) in which: X is cis or trans --CH.dbd.CH-- or CH.sub.2 CH.sub.2 --;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.10 where R.sup.10 is H, C.sub.1-6 alkyl or aralkyl;Y is a saturated heterocyclic amino group; andR.sup.4 is aralkyl (in which the aryl portion is substituted by alkylthio, alkylsulphinyl, alkylsulphonyl, alkanoylamino, aroylamino, phenalkyl, aminosulphonyl, alkanoylaminosulphonyl, phenylsulphonyl, nitro, tetrazolyl, substituted phenyl or thienyl).These compounds inhibit blood platelet aggregation and have bronchodilatory action, and may be formulated for use as anti-asthmatics and antithrombotic agents.Type: GrantFiled: September 17, 1982Date of Patent: March 20, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw
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Patent number: 4436921Abstract: 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: July 16, 1980Date of Patent: March 13, 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: 4435397Abstract: 4-(3-Aryloxy-2-hydroxypropyl)piperazines bearing a carbamyl group in the 1-position are .beta.-adrenergic blockers. A typical example is 1-carbamyl-4-{3-[2-allyl-3-(2-carbethoxyaminoethyl)phenoxy]-2-hydroxypropy l}piperazine.Type: GrantFiled: March 26, 1981Date of Patent: March 6, 1984Assignee: Nippon Shinyaku Co., Ltd.Inventors: Shingo Matsumura, Hiroshi Enomoto, Yoshiaki Aoyagi, Haruo Tanaka
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Patent number: 4433085Abstract: A triazolidine-3,5-dione/formaldehyde/amine condensate is disclosed of the formula ##STR1## in which wherein the terms R.sup.1, R.sup.2 and R.sup.5 are defined hereinafter in the specificationa process for the preparation of such condensate by reaction of a triazolidine-3,5-dione with formaldehyde and a suitable nitrogen compound and the use of the condensate as a flame-proofing agent for thermoplastics, especially polyamide and as an auxiliary for modifying polymeric substances.Type: GrantFiled: June 29, 1981Date of Patent: February 21, 1984Assignee: Bayer AktiengesellschaftInventors: Ludwig Rottmaier, Rudolf Merten
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Patent number: 4431589Abstract: These are described compounds of formula (I) ##STR1## or an acid addition salt thereof; in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, halogen, C.sub.1-4 haloalkyl, nitro, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio or phenylsulphonyl; in which R.sup.5 is a group of the formula ##STR2## where R.sup.7 is hydrogen or C.sub.1-6 alkyl, R.sup.8 is hydrogen or C.sub.1-4 alkyl and n is 0 or 1, provided that when R.sup.7 is hydrogen n is 0; and in which R.sup.6 is attached to the 1, 2 or 3 position of the triazole ring and is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, phenyl, benzyl or acyl. These compounds are pharmaceutically active and are especially useful in the treatment of disorders of the central nervous system. They are prepared by reacting an amine of formula R.sup.Type: GrantFiled: December 3, 1981Date of Patent: February 14, 1984Assignee: Lilly HouseInventors: Jiban K. Chakrabarti, Terrence M. Hotten, David J. Steggles
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Patent number: 4428950Abstract: Novel (hetarylphenoxy)-(phenylpiperazinyl)-propanols of the formula ##STR1## where R.sup.1 is hydrogen, amino or alkyl of 1 to 4 carbon atoms, R.sup.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy where alkyl is of 1 to 3 carbon atoms, the phenyl ring can be monosubstituted or disubstituted by R.sup.2, and the heterocyclic structure Het. is pyrimidinyl, triazol-1-yl, imidazol-1-yl, pyrazol-3-yl or isoxazol-3-yl, and their physiologically tolerated addition salts with acids, processes for their preparation, and pharmaceutical formulations which contain these compounds and exhibit predominantly hypotensive, sedative, neuroleptic and broncholytic properties.Type: GrantFiled: January 15, 1982Date of Patent: January 31, 1984Assignee: BASF AktiengesellschaftInventors: Albrecht Franke, Gerd Steiner, Peter C. Thieme, Dieter Lenke, Josef Gries, Hans-Juergen Teschendorf
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Patent number: 4428953Abstract: Novel pleuromutilin derivatives of formula I, ##STR1## in which R.sub.1 is ethyl or vinyl,m is 0 or 1, andR.sub.2 is a heterocyclic radical, in which a 5- or 6-membered, unsaturated or saturated heterocyclic ring containing one or more hetero atoms selected from oxygen, sulphur and nitrogen, is attached to the --S(CH.sub.2).sub.m --group,provided that when m is 0, R.sub.2 is other than pyridyl,their production and use as antimicrobial agents are described.Type: GrantFiled: March 8, 1982Date of Patent: January 31, 1984Assignee: Sandoz, Ltd.Inventors: Heinz Berner, Friederike Turnowsky, Georg Laber, Johannes Hildebrandt
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Patent number: 4421758Abstract: Compounds of formula (I): ##STR1## [wherein: Q represents a .dbd.CH-- group or a nitrogen atom;R.sup.1 represents a methylene group, a group of formula--CH.sub.2 CH(R.sup.3)--OCH.sub.2 --(R.sup.3 being a substituted or unsubstituted phenyl group) or a group of formula--(CH.sub.2).sub.n --CH(R.sup.4)--O--(n being 1 or 2 and R.sup.4 being a substituted or unsubstituted phenyl or phenylalkyl group); andA represents a group of formula--OR.sup.2(R.sup.2 being an alkenyl group, an alkynyl group or a substituted or unsubstituted alkyl or phenyl group) or a group of formula--CH.sub.2 --XR.sup.11(X being an oxygen or sulphur atom and R.sup.11 being an aryl or aralkyl group or, when X represents an oxygen atom, R.sup.11 being a hydrogen atom or a carbonyloxy or sulphonyloxy group) andacid addition salts and metal complexes thereof are valuable antimicrobial agents having low toxicity to humans and other animals and are especially valuable for the eradication of fungi.Type: GrantFiled: December 11, 1981Date of Patent: December 20, 1983Assignee: Sankyo Company LimitedInventors: Isao Kawamoto, Masaki Nakahara
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Patent number: 4421753Abstract: This disclosure describes novel 1-(5-amino-4H-1,2,4-triazol-3-yl)-4-substituted-piperazines which are useful as hypotensive agents in mammals.Type: GrantFiled: March 22, 1982Date of Patent: December 20, 1983Assignee: American Cyanamid CompanyInventors: Andrew S. Tomcufcik, Walter E. Meyer, John P. Dusza
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Patent number: 4416817Abstract: Novel 3-methoxy-2-oxoazetidine derivatives, which are shown by the following formula ##STR1## wherein R.sub.1 is amino, acylated amino or protected amino, are of value as intermediates for the synthesis of useful compounds represented by the formula ##STR2## wherein R.sub.1 has the same meaning as defined above, as drugs in the treatment of bacterial infections.Type: GrantFiled: November 18, 1981Date of Patent: November 22, 1983Assignee: Takeda Chemical Industries, Ltd.Inventors: Taisuke Matsuo, Michihiko Ochiai
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Patent number: 4408049Abstract: The present invention provides certain substituted-piperazinyl-1,2,4-triazoles which are useful for the treatment of sensitized humans for allergies and anaphylactic reactions.Type: GrantFiled: March 26, 1982Date of Patent: October 4, 1983Assignee: The Upjohn CompanyInventor: Martin Gall
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Patent number: 4405620Abstract: Compounds of the formula (I), or pharmaceutically acceptable salts thereof ##STR1## wherein X is phenyl, optionally substituted by one halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy; or pyridyl; R.sub.1 is hydrogen or C.sub.1-6 alkyl; and n is 1 to 6, pharmaceutical compositions containing them and a process for their preparation. These compounds are useful in the prophylaxis or treatment of diseases due to a histamine-mediated allergic response.Type: GrantFiled: January 19, 1981Date of Patent: September 20, 1983Assignee: Beecham Group LimitedInventors: Derek R. Buckle, Harry Smith
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Patent number: 4404387Abstract: The present invention provides certain substituted-piperazinyl-1,2,4-triazoles which are useful for the treatment of sensitized humans for allergies and anaphylactic reactions.Type: GrantFiled: March 26, 1982Date of Patent: September 13, 1983Assignee: The Upjohn CompanyInventor: Martin Gall
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Patent number: 4404382Abstract: The present invention provides certain piperazinyl-substituted imidazoles which are useful for the treatment of sensitized humans for allergies and anaphylactic reactions.Type: GrantFiled: March 26, 1982Date of Patent: September 13, 1983Assignee: The Upjohn CompanyInventor: Martin Gall
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Patent number: 4402957Abstract: Novel heterocyclic derivatives of [4-(piperazin-1-yl-phenoxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazoles and 1H-1,2,4-triazoles, useful as antifungal and antibacterial agents.Type: GrantFiled: May 7, 1981Date of Patent: September 6, 1983Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Heeres, Robert Hendrickx
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Patent number: 4402956Abstract: Novel compounds selected from the group consisting of 2-[3-[4-(3-chloro-4-fluorophenyl)-1-piperazinyl]propyl]-1,2,4-triazolo[4,3 -a]pyridine-3(2H)-one (I) and from its non-toxic pharmaceutically acceptable salts possess analgesic, anti-convulsant and anti-depressant activities.Type: GrantFiled: February 12, 1981Date of Patent: September 6, 1983Assignee: Aziende Chimiche Riunite Angelini Francesco ACRAF SpAInventors: Bruno Silvestrini, Leandro Baiocchi
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Patent number: 4399285Abstract: Tetrazolyloxycarboxylic acid amide compound of the formula ##STR1## wherein R is an optionally substituted radical selected from the group consisting of alkyl or aryl,R.sup.1 is hydrogen or alkyl,n is 0 or 1, andR.sup.2 and R.sup.3 are individually selected from hydrogen or optionally substituted radicals selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aralkyl and aryl, with the proviso that when n is 0,R.sup.2 and R.sup.3, together with the nitrogen atom to which they are bonded, form an optionally substituted, optionally partially unsaturated and optionally benzo-fused monocyclic or bicyclic radical which optionally contains one or more further hetero-atomsare effective herbicides.Type: GrantFiled: October 24, 1980Date of Patent: August 16, 1983Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Wolfgang Hofer, Fritz Maurer, Volker Mues, Ludwig Eue, Robert R. Schmidt
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Patent number: 4391805Abstract: 1-(1,3-Dioxolan-2-ylmethyl)-azoles of the general formula ##STR1## and their stereoisomers and their salts with physiologically acceptable acids, the preparation of these compounds, pharmaceutical formulations containing the latter and their use against mycoses, protozoa and Gram-positive and Gram-negative bacteria are described.Type: GrantFiled: October 14, 1981Date of Patent: July 5, 1983Assignee: Hoechst AktiengesellschaftInventors: Ernst Blume, Wolfgang Schaper, Wolfgang Raether, Walter Dittmar
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Patent number: 4386091Abstract: Phenoxyalkyl substituted-1,2,4-triazolones having antidepressant properties typified by 4-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-2,4-dihydro-2-(2-ph enoxyethyl)-3H-1,2,4-triazol-3-one are disclosed.Type: GrantFiled: February 24, 1982Date of Patent: May 31, 1983Assignee: Mead Johnson & CompanyInventors: Davis L. Temple, Jr., Walter G. Lobeck, Jr.
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Patent number: 4378360Abstract: Compounds of formula (I): ##STR1## wherein R is hydrogen, halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sub.1 is hydrogen or C.sub.1-6 alkyl; and n is 1 to 6 and pharmaceutically acceptable salts thereof; pharmaceutical compositions containing them; a process for their preparation; and their use in treating allergy.Type: GrantFiled: April 15, 1981Date of Patent: March 29, 1983Assignee: Beecham Group LimitedInventors: Derek R. Buckle, Harry Smith, John M. Tedder
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Patent number: 4372953Abstract: Tetrazole derivatives of the formula: ##STR1## wherein R.sup.1 is a lower alkykl, phenyl or a group of the formula: --S(O).sub.l --A--(X).sub.m --R.sup.3, and R.sup.2 is hydrogen, a lower alkyl, phenyl or a cycloalkyl when R.sup.1 is the group --S(O).sub.l --A--(X).sub.m --R.sup.3, or R.sup.2 is a group of the formula: --B--CO--R.sup.4 when R.sup.1 is a lower alkyl or phenyl and a pharmaceutically acceptable salt thereof, which have prophylactic or therapeutic activities against peptic and/or duodenal ulcers and are useful as an anti-ulcer drug; processes for the preparation of the tetrazole derivatives; and pharmaceutical composition containing said tetrazole derivatives.Type: GrantFiled: February 27, 1981Date of Patent: February 8, 1983Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Minoru Uchida, Takao Nishi, Kazuyuki Nakagawa
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Patent number: 4368200Abstract: Novel heterocyclic derivatives of (4-phenylpiperazin-1-yl-aryloxymethyl-1,3-dioxolan-2-yl)methyl-1H-imidazol es and 1H-1,2,4-triazoles, useful as antifungal and antibacterial agents.Type: GrantFiled: January 14, 1981Date of Patent: January 11, 1983Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Heeres, Leo J. J. Backx
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Patent number: 4358449Abstract: 1-(1,3,-Dioxolan-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles useful as antifungal and antibacterial agents.Type: GrantFiled: February 15, 1980Date of Patent: November 9, 1982Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Heeres, Leo J. J. Backx, Joseph H. Mostmans
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Patent number: 4338317Abstract: Phenoxyethyl substituted-1,2,4,-triazolones having antidepressant properties typified by 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-4-(2-phenoxyethyl)- 2H-1,2,4-triazol-3(4H)-one are disclosed.Type: GrantFiled: March 16, 1981Date of Patent: July 6, 1982Assignee: Mead Johnson & CompanyInventors: Davis L. Temple, Jr., Walter G. Lobeck, Jr.
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Patent number: 4338453Abstract: Novel aminoalkyl triazoles are provided which are useful for the treatment of sensitized humans and animals for allergies and anaphylactic reactions. Additionally, a number of the compounds are useful in the treatment of hypertension. These compounds are of the formula ##STR1## wherein R.sub.4 is hydrogen, alkyl, alkoxy, aryl, sulfonyl, or sulfinyl, R.sub.5 is aryl, R.sub.6 is hydrogen, hydroxy, alkyl, alkoxy, or alkanoyloxy, and R.sub.1 is piperidinyl or amino.Type: GrantFiled: September 17, 1980Date of Patent: July 6, 1982Assignee: The Upjohn CompanyInventor: Martin Gall
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Patent number: 4331674Abstract: 4-Phenoxy-4-(azolyl-1-yl)-butanoic acid derivatives of the formula ##STR1## in which A is --CO-- or CH(OH)--,Y is --CH.dbd. or --N.dbd.,Z is halogen, alkyl, alkenyl, halogenoalkyl, cycloalkyl, alkoxy, alkylthio, alkoxycarbonyl, phenyl, phenoxy, phenylalkyl, substituted phenyl, phenoxy or phenylalkyl, amino, cyano or nitro,R is cyano, --CO--OR.sup.3 or --CO--NR.sup.4 R.sup.5,R.sup.1 and R.sup.2 each independently is alkyl, phenyl or substituted phenyl, or conjointly form a carbocyclic ring,R.sup.3 is alkyl,R.sup.4 is hydrogen, alkyl, phenyl or substituted phenyl andR.sup.5 is hydrogen or alkyl, orR.sup.4 and R.sup.5 conjointly form a methylene bridge --(CH.sub.2).sub.m -- which can contain a further hetero-atom,m is 2, 3, 4, 5, 6 or 7,n is 0, 1, 2, 3, 4 or 5,and salts thereof, which possess fungicidal properties.Type: GrantFiled: July 27, 1977Date of Patent: May 25, 1982Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Jorg Stetter, Karl H. Buchel, Paul-Ernst Frohberger, Wilhelm Brandes
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Patent number: 4326066Abstract: Coumarin compounds of the formula ##STR1## in which the substituents have the meanings given inthe description,are valuable whiteners for natural fibre materials, such as wool, or synthetic polycondensates. They can also be used as scintillators and laser dyestuffs.Type: GrantFiled: January 7, 1980Date of Patent: April 20, 1982Assignee: Bayer AktiengesellschaftInventors: Udo Eckstein, Roderich Raue, Carl-Wolfgang Schellhammer
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Patent number: 4316024Abstract: Certain cephalosporins having a heterocyclicthiomethyl group at the 3-position such as cefoperazone are prepared by reacting a solution of a 7-acylamidocephalosporanic acid having a free amino group as part of said acyl substituent with about an equi-molar amount of the thiolester ##STR1## wherein --S-Het is the desired conventional heterocyclicthio group which displaces the 3-acetoxy group of the starting acid and ##STR2## is the conventional acyl group which displaces a hydrogen on the free amino group which is part of the acyl substituent of the starting 7-acylamidocephalosporanic acid.Type: GrantFiled: September 15, 1980Date of Patent: February 16, 1982Assignee: Bristol-Myers CompanyInventors: Seiji Iimura, Jun Okumura, Takayuki Naito
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Patent number: 4299959Abstract: A fluorescent pigment consisting of N-substituted iminocoumarins of the general formula I, ##STR1## wherein X.sub.1 is a cyano group, a carboxamido group or an aryl or a heteroaryl radical linked directly or through a --CO or --SO.sub.2 group,X.sub.2 is an amino group, hydroxy group or an alkoxy group and when it is an amino group, may carry an optionally substituted alkylene or alkylidene group bound in ortho position to the nitrogen atom and in para position with respect to the coumarin oxygen atom,X.sub.3 is a hydrogen atom, a halogen atom or a cyano group andX.sub.4 is a functionally converted carboxyl groups. The new dyestuffs dye polyester fiber in orange or red shades with good fastness.Type: GrantFiled: January 31, 1979Date of Patent: November 10, 1981Assignee: Ciba-Geigy CorporationInventor: Nalin B. Desai
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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: 4287195Abstract: Novel heterocyclic derivatives of [4-(piperazin-1-yl-phenloxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazoles and 1H-1,2,4-triazoles, useful as antifungal and antibacterial agents.Type: GrantFiled: April 4, 1979Date of Patent: September 1, 1981Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Heeres, Robert Hendrickx
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Patent number: 4268512Abstract: Novel substituted 2,3-alkylene bis (oxy) benzamides and derivatives thereof are disclosed. Also disclosed is a method for producing said compounds. The compounds have anxiolytic, psychostimulant, disinhibiting and thymoanaleptic properties useful therapeutically in the psychofunctional field, particularly in gastro-enterology, cardiology, urology, rheumatology and gynaecology.Type: GrantFiled: February 23, 1979Date of Patent: May 19, 1981Assignee: Societe d'Etudes Scientifiques et Industrielles de l'Ile-de-FranceInventors: Michel Thominet, Gerard Bulteau, Jacques Acher, Claude Collignon
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Patent number: 4267179Abstract: Novel heterocyclic derivatives of (4-phenylpiperazin-1-yl-aryloxymethyl-1,3-dioxolan-2-yl)methyl-1H-imidazol es and 1H-1,2,4-triazoles, useful as antifungal and antibacterial agents.Type: GrantFiled: March 14, 1979Date of Patent: May 12, 1981Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Heeres, Leo J. J. Backx
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Patent number: 4256881Abstract: Benzotriazole compounds employed as development restrainer precursors are described having on one nitrogen atom an alkali-hydrolyzable, N,N-disubstituted carbamoyl group. The compounds may have the following formula: ##STR1## wherein: R.sup.1 and R.sup.2 each represent a substituted or unsubstituted alicyclic, aliphatic, aromatic or heterocyclic moiety, or may be taken together with the nitrogen to which they are attached to form a heterocyclic ring; andR.sup.3, R.sup.4, R.sup.5 and R.sup.6 each represent hydrogen, nitro, lower alkyl, halogen, carbamoyl, sulfamoyl, RCONH-- or RSO.sub.2 NH--, wherein R is lower alkyl or aryl.Type: GrantFiled: October 18, 1979Date of Patent: March 17, 1981Assignee: Eastman Kodak CompanyInventors: Michael J. Simons, David T. Southby, Hans G. Ling
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Patent number: 4252721Abstract: Compounds of the general formula: ##STR1## in which alk and alk' represent the bivalent radicals; aliphatic alkyl chains; and R and R' represent the alkyl, halogen, hydrogen, alkyloxy, --OH, --CF.sub.3 or --SCH.sub.3 radicals. Said compounds of the formula I are effective and useful as antiglaucomic and antipsychotic agents and also as additive agents in the withdrawal treatment of various addictive conditions. Methods for their preparation are also disclosed.Type: GrantFiled: March 29, 1979Date of Patent: February 24, 1981Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Bruno Silvestrini, Leandro Baiocchi
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Patent number: 4242507Abstract: A novel process for the amidation or esterification which comprises reacting a compound having a carboxy group with a compound having an amino or imino group which can be acylated or with a compound having a hydroxy group in the presence of a sulfonic acid ester of the formula:R.sub.1 --SO.sub.2 --OR.sub.2wherein R.sub.1 is an organic group and R.sub.2 O-- is a residue of a strongly acidic N-hydroxy compound as a condensation agent, and a novel sulfonic acid ester useful as such a condensation agent and a process for the preparation thereof.Type: GrantFiled: February 23, 1978Date of Patent: December 30, 1980Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masumi Itoh, Jiyoji Notani
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Patent number: 4209516Abstract: The present invention relates to new triazole derivatives of the formula ##STR1## wherein R.sub.1 represents hydrogen, lower alkyl, optionally esterified or etherified hydroxymethyl, formyl, optionally functionally modified carboxy, or optionally mono- or disubstituted aminomethyl,R.sub.2 represents lower alkyl, and R.sub.3 represents hydrogen or lower alkyl, whereby R.sub.2 and R.sub.3 as lower alkyl can be bound directly, or in .beta.- or .gamma.-position also by way of oxygen, sulphur or the imino radical or a lower alkylimino radical, and the rings A and B independently of each other can be unsubstituted or substituted, and to their addition salts with inorganic and organic acids, in particular the pharmaceutically acceptable acid addition salts. These new compounds possess valuable pharmacological properties. In particular they have an anti-convulsive activity and are useful for the treatment of epilepsy and of conditions of tension and of agitation.Type: GrantFiled: August 31, 1978Date of Patent: June 24, 1980Assignee: Ciba-Geigy CorporationInventors: Roland Heckendorn, Rene Meier
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Patent number: 4209515Abstract: The present invention relates to new triazole derivatives of the formula ##STR1## wherein R.sub.1 represents hydrogen, lower alkyl, optionally esterified or etherified hydroxymethyl, formyl, optionally functionally modified carboxy, or optionally mono- or disubstituted aminomethyl, R.sub.2 represents lower alkyl, and R.sub.3 represents hydrogen or lower alkyl, whereby R.sub.2 and R.sub.3 as lower alkyl can be bound directly, or in .beta.- or .gamma.-position also by way of oxygen, sulphur or the imino radical or a lower alkylimino radical, and the rings A and B independently of each other can be unsubstituted or substituted, and to their addition salts with inorganic and organic acids, in particular the pharmaceutically acceptable acid addition salts. These new compounds possess valuable pharmacological properties. In particular they have an anticonvulsive activity and are useful for the treatment of epilepsy and of conditions of tension and of agitation.Type: GrantFiled: September 13, 1978Date of Patent: June 24, 1980Assignee: Ciba-Geigy CorporationInventors: Roland Heckendorn, Rene Meier
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Patent number: 4189434Abstract: New and valuable polycyclic compounds which contain nitrogen-containing rings and have a strong action on plants, agents for influencing plant growth containing these compounds, and a method of influencing plant growth with these compounds.Type: GrantFiled: March 28, 1977Date of Patent: February 19, 1980Assignee: BASF AktiengesellschaftInventors: Rolf Platz, Werner Fuchs, Norbert Rieber, Ulf-Rainer Samel, Johann Jung, Bruno Wuerzer
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Patent number: 4177272Abstract: Disubstituted piperazines of the formula: ##STR1## wherein: ##STR2## is naphthyl, benzo [b] furanyl, benzo [b] thienyl, benzodioxolyl, benzodioxanyl, benzodioxacycloheptanyl, coumaranyl, chromanyl, .DELTA..sup.3 -chromenyl, thiochromanyl or .DELTA..sup.3 -thiochromenyl,X is nitrogen and simultaneously Y is oxygen or sulfur, orX is sulfur, imino (NH) or methylimino (N CH.sub.3) and simultaneously Y is nitrogen, andR is hydrogen, lower alkyl, phenyl, halophenyl, lower-alkylphenyl or lower alkoxyphenyl.These compounds possess interesting pharmacological and therapeutic properties, and may be used as medicines, especially in the treatment of hypertension, peripheral vascular disorders and Parkinson's disease.Type: GrantFiled: December 27, 1977Date of Patent: December 4, 1979Assignee: Science Union et CieInventors: Gilbert Regnier, Roger Canevari, Michel Laubie, Jean-Claude Poignant
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Patent number: 4177155Abstract: Selected N-aminomethyl-triazoles and imidazoles are prepared by the Mannich reaction on benzotriazoles or benzimidazoles with formaldehyde and primary or secondary amines. The products consist mainly of the 1-isomers. The compounds are metal passivators and are used as additives for water-based functional fluids being in contact with metals. These compounds with polar substituents on the amino-group are especially useful in water-based fluids such as anti-freeze or metal-working fluids.Type: GrantFiled: May 19, 1977Date of Patent: December 4, 1979Assignee: Ciba-Geigy CorporationInventors: Alan F. Popplewell, deceased, David R. Clark
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Patent number: 4155913Abstract: Novel thienotriazolodiazepine derivatives and processes for their preparation are described. These compounds are useful as anticonvulsants, muscle-relaxants and sedatives.Type: GrantFiled: October 14, 1977Date of Patent: May 22, 1979Assignee: Hoffmann-La Roche Inc.Inventors: Joseph Hellerbach, Paul Zeller, Dieter Binder, Otto Hromatka
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Patent number: 4153618Abstract: A fluorescent pigment consisting of N-substituted iminocoumarins of the general formula I, ##STR1## wherein X.sub.1 is a cyano group, a carboxamido group or an aryl or a heteroaryl radical linked directly or through a --CO or --SO.sub.2 group,X.sub.2 is an amino group, hydroxy group or an alkoxy group and when it is an amino group, may carry an optionally substituted alkylene or alkylidene group bound in ortho position to the nitrogen atom and in para position with respect to the coumarin oxygen atom,X.sub.3 is a hydrogen atom, a halogen atom or a cyano group andX.sub.4 is a functionally converted carboxyl groups. The new dyestuffs dye polyester fiber in orange or red shades with good fastness.Type: GrantFiled: April 4, 1977Date of Patent: May 8, 1979Assignee: Ciba-Geigy CorporationInventor: Nalin B. Desai
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Patent number: 4129735Abstract: Anti-allergic agents of N-aromatic 1H-(or 2H) tetrazole-5-carboxamide derivation present the following formulae: ##STR1## in which R.sup.1 is --CN or --CONH.sub.2 ;R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halo, polyhalo(lower)alkyl, lower alkyl carbonyl or carb(lower)alkoxy;X is ##STR2## where R.sup.3 is lower alkyl and R.sup.4 is hydrogen or lower alkyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 24, 1976Date of Patent: December 12, 1978Assignee: American Home Products CorporationInventors: John H. Sellstedt, Dieter H. Klaubert
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Patent number: 4123432Abstract: Anti-allergic agents of N-aromatic 1H-(or 2H) tetrazole-5-carboxamide derivation present the following formulae: ##STR1## in which R.sup.1 is --CN or --CONH.sub.2 ;R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halo, polyhalo(lower)alkyl, lower alkyl carbonyl or carb(lower)alkoxy;X is --CH.sub.2 --, --O--, or ##STR2## where R.sup.3 is lower alkyl; and R.sup.4 is hydrogen or lower alkyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 23, 1977Date of Patent: October 31, 1978Assignee: American Home Products CorporationInventors: John H. Sellstedt, Dieter H. Klaubert
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Patent number: 4116960Abstract: Anti-allergic agents of N-aromatic 1H-(or 2H) tetrazole-5-carboxamide derivation present the following formulae: ##STR1## in which R.sup.1 is --CN or --CONH.sub.2 ;R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halo, polyhalo(lower)alkyl, lower alkyl carbonyl or carb(lower)alkoxy;X is --CH.sub.2 --, --O-- ##STR2## where R.sup.3 is lower alkyl and R.sup.4 is hydrogen or lower alkyl;Or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 24, 1976Date of Patent: September 26, 1978Assignee: American Home Products CorporationInventors: John M. Sellstedt, Dieter H. Klaubert
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Patent number: 4111950Abstract: Compounds of the class of 6-phenyl-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-carboxamides, their 5-oxides and their pharmaceutically acceptable acid addition salts have valuable pharmacological properties and are active ingredients for therapeutic compositions. In particular, these new compounds have an anti-convulsive and anti-aggressive action and inhibit somatic reflexes. Specific embodiments are N,N-dimethyl-6-phenyl-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-c arboxamide, 6-(o-fluorophenyl)-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-carb oxamide, N,N-dimethyl-6-(o-fluorophenyl)-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodia zepine-2-carboxamide and N,N-dimethyl-6-(o-chlorophenyl)-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodia zepine-2-carboxamide.Type: GrantFiled: February 4, 1977Date of Patent: September 5, 1978Assignee: Ciba-Geigy CorporationInventors: Andre Gagneux, Roland Heckendorn, Rene Meier
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Patent number: 4097479Abstract: Synthesis of 5-substituted tetrazoles via reaction of an organic nitrile with azide anion is improved by performing the reaction in an amine as solvent and in the presence of an acid-addition salt of the amine as catalyst.Type: GrantFiled: March 11, 1977Date of Patent: June 27, 1978Assignee: Miles Laboratories, Inc.Inventor: Theodore J. Leipzig
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Patent number: T100505Abstract: Triazolo[4,3-a]pyridin-3-(2H)-one derivatives containing a 4-(optionally substituted phenyl)piperazinyl component attached to the two position of the triazolo-[4,3-a]pyridine component via a divalent radical such as --(CH.sub.2).sub.5 --, --(CH.sub.2).sub.6 --, --CH.sub.3 CH(CH.sub.3)CH.sub.2 --, --CH.sub.2 C(CH.sub.3).sub.2 CH.sub.2 --, --CH.sub.2 CH.dbd.CHCH.sub.2 --, --CH.sub.2 C.tbd.CCH.sub.2 --, --CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 -- or a divalent cycloalkylene radical of 3 to 6 carbon atoms are disclosed. The compounds are useful in that they exhibit central nervous system pharmacological properties in standard laboratory tests considered predictive of analgetics, anti-psychotic (neuroleptics), antidepressant and antianxiety utility. Examples of specific embodiments of the invention are compounds having the formula______________________________________ ##STR1## Y R ______________________________________ ##STR2## 3-Cl ##STR3## H ##STR4## 3-Cl ##STR5## 3-CF.sub.3 ##STR6## 4-F CH.sub.2 CHCHCH.sub.Type: GrantFiled: March 17, 1980Date of Patent: April 7, 1981Inventors: Duane F. Morrow, Yao H. Wu