Hetero Ring In Ionically Bonded Moiety Patents (Class 544/109)
  • Patent number: 4631283
    Abstract: The synthesis of substituted quinazolinones is described. The novel quinazolinones are renal vasodilators and thereby increase renal blood flow, and are useful as cardiovascular agents.
    Type: Grant
    Filed: August 27, 1984
    Date of Patent: December 23, 1986
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Victor T. Bandurco, Seymour D. Levine, Dennis M. Mulvey, Alfonso J. Tobia
  • Patent number: 4587296
    Abstract: Additives for rubber compositions, giving vulcanisates having improved retention of optimum physical properties, are compounds containing two or more groups of the formula --S--SO.sub.2 R linked by an organic bridging group, or polymers containing two or more groups of the formula --S--SO.sub.2 R attached to an organic polymer chain, where R represents (a) a radical OM where M is a monovalent metal, the equivalent of a multivalent metal, a monovalent in derived by the addition of a proton to a nitrogenous base, or the equivalent of a multivalent ion derived by the addition of two or more protons to a nitrogenous base, or (b) an organic radical selected from aliphatic, cycloaliphatic, aromatic and heterocyclic radicals, and radicals which are combinations of any two or more such radicals.
    Type: Grant
    Filed: April 11, 1985
    Date of Patent: May 6, 1986
    Assignee: Monsanto Europe, S.A.
    Inventor: Philippe G. Moniotte
  • Patent number: 4578383
    Abstract: Novel phosphorus containing antibiotic compounds that are antitumor agents designated CL 1565-A, CL 1565-B, CL 1565-T and their salts, a process for the production and the method of using said compounds, and pharmaceutical compositions containing various salts of the compounds of the invention alone or in combination with other antitumor agents in the treatment of microbial infections and neoplastic diseases, are provided.
    Type: Grant
    Filed: July 2, 1984
    Date of Patent: March 25, 1986
    Assignee: Warner-Lambert Company
    Inventors: Suresh S. Stampwala, James C. French, Josefino B. Tunac, Timothy R. Hurley, Richard H. Bunge
  • Patent number: 4486429
    Abstract: Compounds of the formula I: ##STR1## in which R represents a hydrogen atom or an alkyl radical containing from 1 to 8 carbon atoms and R.sub.1 and R.sub.2, which may be identical or different independently represent a hydrogen atom, an alkyl radical containing from 1 to 4 carbon atoms, a --CONH.sub.2 radical, a --CO.sub.2 alk.sub.1 radical in which alk.sub.1 represents an alkyl radical containing from 2 to 8 carbon atoms, or an--SO.sub.2 alk.sub.2 radical in which alk.sub.2 represents an alkyl radical containing from 1 to 8 carbon atoms, or R.sub.1 and R.sub.2 together with the nitrogen atom form a heterocycle provided that R.sub.1 and R.sub.2 are not both hydrogen, as well as the alkali metal, alkaline earth metal, ammonium or amine salts of compounds of formula I in which R represents a hydrogen atom. These compounds are useful in treating hyperchlorhydria, gastric or gastroduodenal ulcers, gastritis, hiatal hernias and gastric or gastroduodenal ailments accompanied by gastric hyperacidity.
    Type: Grant
    Filed: October 20, 1982
    Date of Patent: December 4, 1984
    Assignee: Roussel Uclaf
    Inventors: Mario Bianchi, Fernando Barzaghi
  • Patent number: 4438111
    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 saturtaed heterocyclic amino group; andR.sup.4 is thienylalkyl or furanylalkyl in which the ring may be substituted.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
  • 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: 4438092
    Abstract: New 5-amino-N-(substitutedphenyl)-1,3-disubstituted-1H-pyrazole-4-carboxamides useful as anticonvulsant agents for treating warm-blooded animals are disclosed. Also disclosed are intermediates and methods for preparing the new compounds and methods for using the new compounds.
    Type: Grant
    Filed: June 14, 1982
    Date of Patent: March 20, 1984
    Assignee: Warner-Lambert Company
    Inventors: Dietrich Schweiss, Ivan C. Nordin
  • Patent number: 4346097
    Abstract: New 5-amino-N-(substituted phenyl)-1,3-disubstituted-1H-pyrazole-4-carboxamides useful as anticonvulsant agents for treating warm-blooded animals are disclosed. Also disclosed are intermediates and methods for preparing the new compounds and methods for using the new compounds.
    Type: Grant
    Filed: September 30, 1980
    Date of Patent: August 24, 1982
    Assignee: Warner-Lambert Company
    Inventors: Dietrich Schweiss, Ivan C. Nordin
  • Patent number: 4342756
    Abstract: Compounds are described of the formula ##STR1## (and their salts and solvates) in which: X is cis or trans --CH.dbd.CH--;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.3 where R.sup.3 is H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl;Y is a saturated heterocyclic amino group having 5-8 ring members; andR.sup.2 is C.sub.2-4 alkanoyl, C.sub.3-6 alkenyl (optionally substituted), C.sub.1-12 alkyl, or substituted or unsubstituted phenylalkyl, biphenylalkyl or naphthylalkyl.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and anti-asthmatic agents.
    Type: Grant
    Filed: April 29, 1981
    Date of Patent: August 3, 1982
    Assignee: Glaxo Group Limited
    Inventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw, Norman F. Hayes
  • Patent number: 4329357
    Abstract: 2,3-Dihydro-1-benzothiepin-4-carboxamides, e.g. those of the formula ##STR1## Am=arylamino or N-alkyl-N-arylamino substituted by R X=HO, alkoxy, alkanoyloxy or alkyleneiminoR=alkyl, alkoxy, alkylmercapto, halo, CF.sub.3, CN, or NO.sub.2n=0-2or their salts with therapeutically useful bases, exhibit anti-inflammatory effects.
    Type: Grant
    Filed: February 9, 1981
    Date of Patent: May 11, 1982
    Assignee: Ciba-Geigy Corporation
    Inventor: Melvin H. Rosen
  • Patent number: 4320125
    Abstract: Thiazolylidene-oxo-propionitrile salt of the formula ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 have the meaning defined in the specification and B.sup.1 is an ammonium group or an alkali cation. The compounds are valuable as insecticides of a superior activity against specific groups of insects.
    Type: Grant
    Filed: May 13, 1980
    Date of Patent: March 16, 1982
    Assignee: Schering Aktiengesellschaft
    Inventors: Reinhold Puttner, Ulrich Buhmann, Hartmut Joppien
  • Patent number: 4299838
    Abstract: Tryptophan derivatives represented by the general formula: ##STR1## in which R denotes an acetyl group, M denotes an alkali metal or alkaline-earth metal (more particularly lithium or magnesium) having the value n or the quaternary ammonium cation of one of the following nitrogenous organic bases: morpholine and monoethanolamine; n is an integer equal to 1 or 2, and the formula (I) derivatives can be in the racemic DL form or the optically active L(+) form, the drugs being useful inter alia as agents having an increased effect on the central nervous system.
    Type: Grant
    Filed: February 17, 1978
    Date of Patent: November 10, 1981
    Assignee: La Cooperation Pharmaceutique Francaise
    Inventor: Jean P. Durlach
  • Patent number: 4299769
    Abstract: This disclosure describes novel substituted .omega.-heteroaroyl(propionyl or butyryl)-L-prolines and the esters and cationic salts thereof which are useful as hypotensive agents in mammals.
    Type: Grant
    Filed: April 28, 1980
    Date of Patent: November 10, 1981
    Assignee: American Cyanamid Company
    Inventors: Francis J. McEvoy, William B. Wright, Jr., Gary H. Birnberg, Jay D. Albright
  • Patent number: 4277484
    Abstract: 2,3-Dihydro-1-benzothiepin-4-carboxamides, e.g. those of the formula ##STR1## or their salts with therapeutically useful bases, exhibit anti-inflammatory effects.
    Type: Grant
    Filed: February 8, 1980
    Date of Patent: July 7, 1981
    Assignee: Ciba-Geigy Corporation
    Inventor: Melvin H. Rosen
  • Patent number: 4267122
    Abstract: Aminosulfonylcarboxylic acids and their manufacture from diamines and chlorosulfonylcarboxylic acids.
    Type: Grant
    Filed: September 27, 1978
    Date of Patent: May 12, 1981
    Assignee: BASF Aktiengesellschaft
    Inventors: Lucien Thil, Martin Fischer, Wolfgang Kindscher
  • Patent number: 4226998
    Abstract: 2,3-Dihydro-1-benzothiepin-4-carboxamides, e.g. those of the formula ##STR1## Am=arylamino or N-alkyl-N-arylamino substituted by R X=HO, alkoxy, alkanoyloxy or alkyleneiminoR=alkyl, alkoxy, alkylmercapto, halo, CF.sub.3, CN, or NO.sub.2n=0-2or their salts with therapeutically useful bases, exhibit anti-inflammatory effects.
    Type: Grant
    Filed: September 20, 1978
    Date of Patent: October 7, 1980
    Assignee: Ciba-Geigy Corporation
    Inventor: Melvin H. Rosen
  • Patent number: 4209446
    Abstract: Process for the preparation of piperonylidenecrotonic acid amides of the formula ##STR1## in which R.sub.1 and R.sub.2 have the meaning given in the disclosure wherein piperonal is reacted with crotonic acid amides of the formula ##STR2## in the presence of alkali metal hydroxides and dipolar aprotic diluents which are inert under the reaction conditions.
    Type: Grant
    Filed: December 13, 1978
    Date of Patent: June 24, 1980
    Assignee: Haarman & Reimer GmbH
    Inventors: Andreas Schulze, Hermann Oediger
  • Patent number: 4209445
    Abstract: Process for the preparation of piperonylidenecrotonic acids amides of the formula ##STR1## in which R.sub.1 and R.sub.2 have the meaning given in the disclosure wherein piperonal is reacted with crotonic acid amides of the formula ##STR2## in the presence of hydroxides of the formulaA.sup.+ OH.sup.-in whichA.sup.+ represents a quaternary ammonium or phosphonium group or an alkali metal complex with neutral organic complex ligands,and polar aprotic or polar, sterically hindered protic organic solvents which are inert under the reaction conditions.
    Type: Grant
    Filed: December 13, 1978
    Date of Patent: June 24, 1980
    Assignee: Haarman & Reimer GmbH
    Inventors: Hermann Oediger, Andreas Schulze
  • Patent number: 4185109
    Abstract: 2,3-Dihydro-1-benzothiepin-4-carboxamides, e.g. those of the formula ##STR1## or their salts with therapeutically useful bases, exhibit anti-inflammatory effects.
    Type: Grant
    Filed: November 23, 1977
    Date of Patent: January 22, 1980
    Assignee: Ciba-Geigy Corporation
    Inventor: Melvin H. Rosen
  • Patent number: 4181740
    Abstract: The present invention provides 1-(p-azidobenzoyl)-5-methoxy-2-methyl-3-indolylacetic acid and its pharmaceutically acceptable salts and esters and processes of preparation.
    Type: Grant
    Filed: May 13, 1977
    Date of Patent: January 1, 1980
    Assignee: Pierrel S.p.A.
    Inventors: Silvia Tricerri Zumin, Alberto Bianchetti
  • Patent number: 4166126
    Abstract: 2,3-Dihydro-1-benzothiepin-4-carboxamides, e.g. those of the formula ##STR1## Am=NH.sub.2, mono- or di-(alkyl or HO-alkyl)-amino, alkyleneimino, cycloalkylamino, iso- or heterocyclic arylamino or N-alkyl-N-arylaminoX=ho, alkoxy, alkanoyloxy or tert. AmR=h, alkyl, alkoxy, alkylmercapto, halo, CF.sub.3, CN or NO.sub.2n=0-2Or their salts with therapeutically useful bases, exhibit anti-inflammatory effects.
    Type: Grant
    Filed: January 27, 1977
    Date of Patent: August 28, 1979
    Assignee: Ciba-Geigy Corporation
    Inventor: Melvin H. Rosen
  • Patent number: 4137409
    Abstract: Carboxymethyloxysuccinic anhydrides and/or halides, their reaction products with active hydrogen compounds and methods for preparing the anhydrides, the halides and the reaction products are disclosed. The reaction products are variously useful in the fields of food flavorings, detergent builders, surfactants, lubricants, coatings, sizing agents and gasoline additives.
    Type: Grant
    Filed: April 4, 1978
    Date of Patent: January 30, 1979
    Assignee: Lever Brothers Company
    Inventor: Vincent Lamberti
  • Patent number: 4126634
    Abstract: Aminosulfonylcarboxylic acids and their manufacture from diamines and chlorosulfonylcarboxylic acids.
    Type: Grant
    Filed: August 1, 1977
    Date of Patent: November 21, 1978
    Assignee: BASF Aktiengesellschaft
    Inventors: Lucien Thil, Martin Fischer, Wolfgang Kindscher
  • Patent number: 4119783
    Abstract: Pharmaceutical compositions having as the active agent a compound of the formula ##STR1## useful for preventing allergic manifestations in sensitized mammals and novel compounds.
    Type: Grant
    Filed: February 18, 1977
    Date of Patent: October 10, 1978
    Assignee: The Upjohn Company
    Inventors: Charles M. Hall, John B. Wright
  • Patent number: 4087435
    Abstract: Novel 8-aza-9-dioxothiaprostanoic acid compounds, their salts, and derivatives, are prepared from ethyl 7-(3-hydroxymethyl-2-isothiazolidinyl)-5-heptynoate S,S-dioxide by first hydrogenating the triple bond over a Lindlar catalyst, followed by mild oxidation, to produce the corresponding 3-formyl compound, which is condensed with the ylide prepared from dimethyl-(2-oxoheptyl)phosphonate to produce the .alpha.,.beta.-unsaturated ketone, followed by reduction to the corresponding carbinol, and ester hydrolysis. The compounds are useful especially for the treatment of patients with poorly functioning kidneys, as hypotensives, or as platelet aggregation inhibitors.
    Type: Grant
    Filed: February 17, 1977
    Date of Patent: May 2, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., James H. Jones, John B. Bicking
  • Patent number: 4066769
    Abstract: Novel compounds of the formula ##STR1## wherein X is hydrogen, alkyl of one to six carbon atoms, inclusive, alkoxy of one to six atoms, inclusive, phenyl, cyano, nitro, trifluoromethyl, fluoro, chloro or bromo;R is hydrogen, alkyl of one to eight carbon atoms, inclusive, and a physiologically acceptable metal or amine cation and novel compositions wherein R is hydrogen or a physiologically acceptable metal or amine cation are used for prophylactically treating allergic disorders such as asthma.BRIEF SUMMARY OF THE INVENTIONIt has now been discovered that novel compounds of Formula I are useful in the prophylactic treatment of sensitized humans and animals for allergy and anaphylactic reactions of a reagin or non-reagin mediated nature. The compounds are formulated with pharmaceutical carriers for oral, parenteral, inhalation or rectal means of administration.
    Type: Grant
    Filed: December 23, 1976
    Date of Patent: January 3, 1978
    Assignee: The Upjohn Company
    Inventor: John B. Wright
  • Patent number: 4061649
    Abstract: Clavulanic acid sulphates of the formula ##STR1## wherein M.sup.1 is trimethylamine, dimethylalanine, pyridine, N-methylpyridine or N-methylmorpholino, are useful for their antibacterial activity and are also useful as intermediates for the production of antibacterially active compounds.
    Type: Grant
    Filed: April 9, 1976
    Date of Patent: December 6, 1977
    Assignee: Beecham Group Limited
    Inventor: Thomas Trefor Howarth
  • Patent number: 4060522
    Abstract: Amidosulfocarboxylic acids, their preparation from primary or secondary amines and chlorosulfocarboxylic acids, and their use as anticorrosive agents.
    Type: Grant
    Filed: March 15, 1976
    Date of Patent: November 29, 1977
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang Kindscher, Martin Fischer, Karl Eicken, Guenter Vitt
  • Patent number: 4058390
    Abstract: Amine salts of 3-phenyl-6-halo-4-hydroxypyridazines of the formula: ##STR1## in which X is a chlorine or bromine atom, R.sub.1 is an alkyl group containing up to 14 carbon atoms, which group may be substituted by a hydroxy group, an alkoxy group containing up to 10 carbon atoms, cyano group, amino group or lower mono- or lower dialkylamino group, an alkenyl group containing up to 6 carbon atoms or a cycloalkyl group containing 5, 6 or 7 carbon atoms, and R.sub.2 and R.sub.3 have the same meaning as R.sub.1 or each is a hydrogen atom, or R.sub.1 and R.sub.2 together with the nitrogen atom of the amine form a 5- or 6-membered heterocyclic group which may also contain oxygen and which may be mono- or di- substituted by alkyl, and herbicidal compositions containing them.
    Type: Grant
    Filed: December 16, 1975
    Date of Patent: November 15, 1977
    Assignee: Chemie Linz Aktiengesellschaft
    Inventors: Rupert Schonbeck, Engelbert Kloimstein, Erwin Wittmann
  • Patent number: 4055596
    Abstract: The invention is concerned with novel 16-aryloxy-, 16-alkoxy-, 16-arylthio- and 16-alkylthio-8-aza-9-dioxothia-11,12-seco-prostaglandins and processes for their preparation. These novel compounds are useful as pharmaceuticals since they can be used in animals for estrus synchronization and treatment of infertility due to persistence of luteal function.
    Type: Grant
    Filed: July 14, 1976
    Date of Patent: October 25, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., James H. Jones
  • Patent number: 4045567
    Abstract: Hypolipemiant compositions comprising an effective amount of at least one 2-alkyl-5-thiazole-carboxylic acid derivative of the formula ##STR1## wherein R is hydrogen, an alkali metal, ammonium, the monovalent residue of an organic base or a substituted or unsubstituted alkyl and where R'.sub.1 is a linear alkyl of 1 to 12 carbon atoms, and a major amount of a pharmaceutical carrier; as well as the method of reducing the amount of sanguine lipids in warm-blooded animals utilizing the above-hypolipemiant compositions.
    Type: Grant
    Filed: February 27, 1976
    Date of Patent: August 30, 1977
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Odile Le Martret