Five-membered Hetero Ring Having Two Or More Ring Hetero Atoms Of Which At Least One Is Nitrogen Patents (Class 544/366)
  • Patent number: 4448963
    Abstract: 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: Grant
    Filed: February 22, 1982
    Date of Patent: May 15, 1984
    Assignee: 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
  • Patent number: 4438112
    Abstract: 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: Grant
    Filed: September 17, 1982
    Date of Patent: March 20, 1984
    Assignee: Glaxo Group Limited
    Inventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw
  • Patent number: 4436921
    Abstract: 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: Grant
    Filed: July 16, 1980
    Date of Patent: March 13, 1984
    Assignee: 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
  • Patent number: 4435397
    Abstract: 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: Grant
    Filed: March 26, 1981
    Date of Patent: March 6, 1984
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Shingo Matsumura, Hiroshi Enomoto, Yoshiaki Aoyagi, Haruo Tanaka
  • Patent number: 4433085
    Abstract: 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: Grant
    Filed: June 29, 1981
    Date of Patent: February 21, 1984
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ludwig Rottmaier, Rudolf Merten
  • Patent number: 4431589
    Abstract: 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: Grant
    Filed: December 3, 1981
    Date of Patent: February 14, 1984
    Assignee: Lilly House
    Inventors: Jiban K. Chakrabarti, Terrence M. Hotten, David J. Steggles
  • Patent number: 4428950
    Abstract: 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: Grant
    Filed: January 15, 1982
    Date of Patent: January 31, 1984
    Assignee: BASF Aktiengesellschaft
    Inventors: Albrecht Franke, Gerd Steiner, Peter C. Thieme, Dieter Lenke, Josef Gries, Hans-Juergen Teschendorf
  • Patent number: 4428953
    Abstract: 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: Grant
    Filed: March 8, 1982
    Date of Patent: January 31, 1984
    Assignee: Sandoz, Ltd.
    Inventors: Heinz Berner, Friederike Turnowsky, Georg Laber, Johannes Hildebrandt
  • Patent number: 4421758
    Abstract: 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: Grant
    Filed: December 11, 1981
    Date of Patent: December 20, 1983
    Assignee: Sankyo Company Limited
    Inventors: Isao Kawamoto, Masaki Nakahara
  • Patent number: 4421753
    Abstract: 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: Grant
    Filed: March 22, 1982
    Date of Patent: December 20, 1983
    Assignee: American Cyanamid Company
    Inventors: Andrew S. Tomcufcik, Walter E. Meyer, John P. Dusza
  • Patent number: 4416817
    Abstract: 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: Grant
    Filed: November 18, 1981
    Date of Patent: November 22, 1983
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Taisuke Matsuo, Michihiko Ochiai
  • Patent number: 4408049
    Abstract: 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: Grant
    Filed: March 26, 1982
    Date of Patent: October 4, 1983
    Assignee: The Upjohn Company
    Inventor: Martin Gall
  • Patent number: 4405620
    Abstract: 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: Grant
    Filed: January 19, 1981
    Date of Patent: September 20, 1983
    Assignee: Beecham Group Limited
    Inventors: Derek R. Buckle, Harry Smith
  • Patent number: 4404387
    Abstract: 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: Grant
    Filed: March 26, 1982
    Date of Patent: September 13, 1983
    Assignee: The Upjohn Company
    Inventor: Martin Gall
  • Patent number: 4404382
    Abstract: The present invention provides certain piperazinyl-substituted imidazoles which are useful for the treatment of sensitized humans for allergies and anaphylactic reactions.
    Type: Grant
    Filed: March 26, 1982
    Date of Patent: September 13, 1983
    Assignee: The Upjohn Company
    Inventor: Martin Gall
  • Patent number: 4402957
    Abstract: 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: Grant
    Filed: May 7, 1981
    Date of Patent: September 6, 1983
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Robert Hendrickx
  • Patent number: 4402956
    Abstract: 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: Grant
    Filed: February 12, 1981
    Date of Patent: September 6, 1983
    Assignee: Aziende Chimiche Riunite Angelini Francesco ACRAF SpA
    Inventors: Bruno Silvestrini, Leandro Baiocchi
  • Patent number: 4399285
    Abstract: 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: Grant
    Filed: October 24, 1980
    Date of Patent: August 16, 1983
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz Forster, Wolfgang Hofer, Fritz Maurer, Volker Mues, Ludwig Eue, Robert R. Schmidt
  • Patent number: 4391805
    Abstract: 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: Grant
    Filed: October 14, 1981
    Date of Patent: July 5, 1983
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ernst Blume, Wolfgang Schaper, Wolfgang Raether, Walter Dittmar
  • Patent number: 4386091
    Abstract: 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: Grant
    Filed: February 24, 1982
    Date of Patent: May 31, 1983
    Assignee: Mead Johnson & Company
    Inventors: Davis L. Temple, Jr., Walter G. Lobeck, Jr.
  • Patent number: 4378360
    Abstract: 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: Grant
    Filed: April 15, 1981
    Date of Patent: March 29, 1983
    Assignee: Beecham Group Limited
    Inventors: Derek R. Buckle, Harry Smith, John M. Tedder
  • Patent number: 4372953
    Abstract: 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: Grant
    Filed: February 27, 1981
    Date of Patent: February 8, 1983
    Assignee: Otsuka Pharmaceutical Company, Limited
    Inventors: Minoru Uchida, Takao Nishi, Kazuyuki Nakagawa
  • Patent number: 4368200
    Abstract: 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: Grant
    Filed: January 14, 1981
    Date of Patent: January 11, 1983
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Leo J. J. Backx
  • Patent number: 4358449
    Abstract: 1-(1,3,-Dioxolan-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles useful as antifungal and antibacterial agents.
    Type: Grant
    Filed: February 15, 1980
    Date of Patent: November 9, 1982
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jan Heeres, Leo J. J. Backx, Joseph H. Mostmans
  • Patent number: 4338317
    Abstract: 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: Grant
    Filed: March 16, 1981
    Date of Patent: July 6, 1982
    Assignee: Mead Johnson & Company
    Inventors: Davis L. Temple, Jr., Walter G. Lobeck, Jr.
  • Patent number: 4338453
    Abstract: 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: Grant
    Filed: September 17, 1980
    Date of Patent: July 6, 1982
    Assignee: The Upjohn Company
    Inventor: Martin Gall
  • Patent number: 4331674
    Abstract: 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: Grant
    Filed: July 27, 1977
    Date of Patent: May 25, 1982
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Kramer, Jorg Stetter, Karl H. Buchel, Paul-Ernst Frohberger, Wilhelm Brandes
  • Patent number: 4326066
    Abstract: 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: Grant
    Filed: January 7, 1980
    Date of Patent: April 20, 1982
    Assignee: Bayer Aktiengesellschaft
    Inventors: Udo Eckstein, Roderich Raue, Carl-Wolfgang Schellhammer
  • Patent number: 4316024
    Abstract: 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: Grant
    Filed: September 15, 1980
    Date of Patent: February 16, 1982
    Assignee: Bristol-Myers Company
    Inventors: Seiji Iimura, Jun Okumura, Takayuki Naito
  • Patent number: 4299959
    Abstract: 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: Grant
    Filed: January 31, 1979
    Date of Patent: November 10, 1981
    Assignee: Ciba-Geigy Corporation
    Inventor: Nalin B. Desai
  • Patent number: 4293462
    Abstract: 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: Grant
    Filed: December 10, 1979
    Date of Patent: October 6, 1981
    Assignee: Ciba-Geigy Corporation
    Inventors: Robert B. Woodward, Hans Bickel
  • Patent number: 4287195
    Abstract: 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: Grant
    Filed: April 4, 1979
    Date of Patent: September 1, 1981
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jan Heeres, Robert Hendrickx
  • Patent number: 4268512
    Abstract: 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: Grant
    Filed: February 23, 1979
    Date of Patent: May 19, 1981
    Assignee: Societe d'Etudes Scientifiques et Industrielles de l'Ile-de-France
    Inventors: Michel Thominet, Gerard Bulteau, Jacques Acher, Claude Collignon
  • Patent number: 4267179
    Abstract: 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: Grant
    Filed: March 14, 1979
    Date of Patent: May 12, 1981
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jan Heeres, Leo J. J. Backx
  • Patent number: 4256881
    Abstract: 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: Grant
    Filed: October 18, 1979
    Date of Patent: March 17, 1981
    Assignee: Eastman Kodak Company
    Inventors: Michael J. Simons, David T. Southby, Hans G. Ling
  • Patent number: 4252721
    Abstract: 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: Grant
    Filed: March 29, 1979
    Date of Patent: February 24, 1981
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Bruno Silvestrini, Leandro Baiocchi
  • Patent number: 4242507
    Abstract: 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: Grant
    Filed: February 23, 1978
    Date of Patent: December 30, 1980
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masumi Itoh, Jiyoji Notani
  • Patent number: 4209516
    Abstract: 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: Grant
    Filed: August 31, 1978
    Date of Patent: June 24, 1980
    Assignee: Ciba-Geigy Corporation
    Inventors: Roland Heckendorn, Rene Meier
  • Patent number: 4209515
    Abstract: 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: Grant
    Filed: September 13, 1978
    Date of Patent: June 24, 1980
    Assignee: Ciba-Geigy Corporation
    Inventors: Roland Heckendorn, Rene Meier
  • Patent number: 4189434
    Abstract: 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: Grant
    Filed: March 28, 1977
    Date of Patent: February 19, 1980
    Assignee: BASF Aktiengesellschaft
    Inventors: Rolf Platz, Werner Fuchs, Norbert Rieber, Ulf-Rainer Samel, Johann Jung, Bruno Wuerzer
  • Patent number: 4177272
    Abstract: 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: Grant
    Filed: December 27, 1977
    Date of Patent: December 4, 1979
    Assignee: Science Union et Cie
    Inventors: Gilbert Regnier, Roger Canevari, Michel Laubie, Jean-Claude Poignant
  • Patent number: 4177155
    Abstract: 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: Grant
    Filed: May 19, 1977
    Date of Patent: December 4, 1979
    Assignee: Ciba-Geigy Corporation
    Inventors: Alan F. Popplewell, deceased, David R. Clark
  • Patent number: 4155913
    Abstract: Novel thienotriazolodiazepine derivatives and processes for their preparation are described. These compounds are useful as anticonvulsants, muscle-relaxants and sedatives.
    Type: Grant
    Filed: October 14, 1977
    Date of Patent: May 22, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Joseph Hellerbach, Paul Zeller, Dieter Binder, Otto Hromatka
  • Patent number: 4153618
    Abstract: 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: Grant
    Filed: April 4, 1977
    Date of Patent: May 8, 1979
    Assignee: Ciba-Geigy Corporation
    Inventor: Nalin B. Desai
  • Patent number: 4129735
    Abstract: 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: Grant
    Filed: September 24, 1976
    Date of Patent: December 12, 1978
    Assignee: American Home Products Corporation
    Inventors: John H. Sellstedt, Dieter H. Klaubert
  • Patent number: 4123432
    Abstract: 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: Grant
    Filed: December 23, 1977
    Date of Patent: October 31, 1978
    Assignee: American Home Products Corporation
    Inventors: John H. Sellstedt, Dieter H. Klaubert
  • Patent number: 4116960
    Abstract: 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: Grant
    Filed: September 24, 1976
    Date of Patent: September 26, 1978
    Assignee: American Home Products Corporation
    Inventors: John M. Sellstedt, Dieter H. Klaubert
  • Patent number: 4111950
    Abstract: 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: Grant
    Filed: February 4, 1977
    Date of Patent: September 5, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Andre Gagneux, Roland Heckendorn, Rene Meier
  • Patent number: 4097479
    Abstract: 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: Grant
    Filed: March 11, 1977
    Date of Patent: June 27, 1978
    Assignee: Miles Laboratories, Inc.
    Inventor: Theodore J. Leipzig
  • Patent number: T100505
    Abstract: 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: Grant
    Filed: March 17, 1980
    Date of Patent: April 7, 1981
    Inventors: Duane F. Morrow, Yao H. Wu