Diazine Ring Patents (Class 544/114)
  • Patent number: 5395934
    Abstract: Racemic or optically active new 3(2H)-pyridazinone derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said 3(2H)-pyridazinone derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.
    Type: Grant
    Filed: December 21, 1992
    Date of Patent: March 7, 1995
    Assignee: EGIS Gyogyszergyar
    Inventors: Peter Matyus, Klara Czako, Ildiko Varga, Andrea Jednakovics, Agnes Papp, Ilona Bodi, Gyorgy Rabloczky, Andras Varro, Laszlo Jaszlits, Aniko Miklos, Luca Levay, Gvorgy Schmidt, Marton Fekete, Maria Kurthy, Katalin Szemeredi, Erzsebet Zara
  • Patent number: 5332816
    Abstract: The present invention relates to novel piperazine-piperidine compounds of the general formula (I) ##STR1## in which R.sub.1 is e.g. hydrogen or methyl, R.sub.2 is e.g. ethylene, m is zero or 1 and n is e.g. 1, and when n is 1, A is e.g. 2,2-dimethyl-1-propanoyl, n-butoxycarbonyl, n-tetradecyloxycarbonyl or 2,4-bis[N-butyl-(2',2',6',6'-pentamethyl-4'-piperidyl)amino]triazin-6-yl.The said compounds are effective as light stabilizers, heat stabilizers and oxidation stabilizers for organic materials.
    Type: Grant
    Filed: July 19, 1990
    Date of Patent: July 26, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Graziano Vignali, Valerio Borzatta
  • Patent number: 5278163
    Abstract: A novel 3(2H)-pyradazinone derivative of the formula (I) ##STR1## wherein, R represents an alkyl group having 1 to 4 carbon atoms substituted by a cycloalkyl group having 3 to 8 carbon atoms, an alkyl group having 1 to 4 carbon atoms substituted by a phenyl group which may be substituted or an alkyl group having 1 to 4 carbon atoms substituted by a heterocyclic group, R' represents a hydrogen atom, a halogen atom, an alkoxy group having 1 to 4 carbon atoms or a hydroxyl group having 1 to 4 carbon atoms, J represents any of various organic radicals. There is also provided a process for preparing said derivatives. These derivatives are useful as active ingredients of insecticidal, acaricidal and/or nematicidal compositions for agricultural and horticultural uses as well as of expellent compositions for pests parasitic on animals.
    Type: Grant
    Filed: October 5, 1992
    Date of Patent: January 11, 1994
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Tomoyuki Ogura, Yasuo Kawamura, Tatsuo Numata, Toshiyuki Umehara, Toshiro Miyake, Hiroshi Haruyama
  • Patent number: 5276036
    Abstract: The invention relates to 3-aminopyridazine derivatives.These compounds have the formula ##STR1## in which: R.sub.V is a linear or branched C.sub.1 -C.sub.4 alkyl group;R.sub.6 is hydrogen, a C.sub.1 -C.sub.3 alkoxy or a hydroxyl group; andZ is a group ##STR2## in which: n.sub.1 and n.sub.2 independently are zero or one,Y.sub.1 and Y.sub.2 independently are hydrogen or a C.sub.1 -C.sub.3 alkyl group, andT is a dialkylamino group in which the alkyls are C.sub.1 -C.sub.3, if Y.sub.1 or Y.sub.2 is other than hydrogen, or T is a heterocycle selected from: ##STR3## Application: drugs active on the central nervous system.
    Type: Grant
    Filed: May 15, 1992
    Date of Patent: January 4, 1994
    Assignee: Elf Sanofi
    Inventors: Jean-Jacques Bourguignon, Jean-Paul Kan, Camille G. Wermuth
  • Patent number: 5256667
    Abstract: Substituted quinazolinones and pyridopyrimidines of structural formula I ##STR1## are angiotensin II antagonists useful in the treatment of disorders related to the renin-angiotensin system (RAS) such as hypertension, congestive heart failure, ocular hypertension and certain CNS disorders.
    Type: Grant
    Filed: July 31, 1992
    Date of Patent: October 26, 1993
    Assignees: Merck & Co., Inc., E. I. Du Pont De Nemours & Co.
    Inventors: Eric E. Allen, Richard E. Olson
  • Patent number: 5229514
    Abstract: Compounds of formula III ##STR1## wherein R.sub.1 is hydrogen; X is oxygen or sulfur; A is C.sub.1 -C.sub.2 alkylene and Q is --COOR.sub.16, where R.sub.16 is C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkylthio-C.sub.1 -C.sub.4 alkyl are intermediates to compounds which have good pre- and post-emergence selective herbicidal and growth-regulating properties.
    Type: Grant
    Filed: May 12, 1992
    Date of Patent: July 20, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Georg Pissiotas, Hans Moser, Hans-Georg Brunner
  • Patent number: 5204344
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
    Type: Grant
    Filed: February 5, 1991
    Date of Patent: April 20, 1993
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Petpiboon Prasit, Rejean Fortin, John H. Hutchinson, Michel L. Belley, Serge Leger, John Gillard, Richard Frenette
  • Patent number: 5204346
    Abstract: There are disclosed 3 [2(substituted alkyl)-3-oxo-2,3-dihydropyridazin-6-yl]-2-aryl pyrazolo [1,5-a]-pyridines useful for treating maladies requiring an adenosine antagonist, and preparative processes.
    Type: Grant
    Filed: July 15, 1991
    Date of Patent: April 20, 1993
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Youichi Shiokawa, Atsushi Akahane, Hirohito Katayama, Takafumi Mitsunaga
  • Patent number: 5204463
    Abstract: Pyridazinones of the following formula (I): ##STR1## where R.sup.1 -R.sup.4 are a variety of substituents and L is a linking group, a pharmaceutical composition for treating congestive heart failure, novel intermediates, methods for such treatment and processes for preparing compounds of formula (I).
    Type: Grant
    Filed: September 4, 1991
    Date of Patent: April 20, 1993
    Assignee: Glaxo Inc.
    Inventors: Thomas N. Wheeler, Terrence P. Kenakin, Joel E. Shaffer
  • Patent number: 5202323
    Abstract: A compound of the formula, ##STR1## or its pharmaceutically acceptable salt, and its preparation process and pharmaceutical compositions characterized by containing these compounds as effective ingredients.These compounds have strong antithrombotic activity, cardiotonic activity, vasodilator activity and anti-SRS-A activity, and are useful as prophylactic or therapeutic agents for various thrombotic affections, congestive heart failure, hypertension, asthma, immediate type allergy diseases and the like.
    Type: Grant
    Filed: October 16, 1991
    Date of Patent: April 13, 1993
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Keizo Tanikawa, Akira Saito, Takashi Matsumoto, Ryozo Sakoda, Nobutomo Tsuruzoe, Ken-ichi Shikada
  • Patent number: 5196532
    Abstract: Compounds of formula I ##STR1## where R.sup.1 and R.sup.2 are each hydrogen or methyl, A is an ethylene or methylene radical which is unsubstituted or substituted by methyl, hydroxyl or oxo,L is a saturated or unsaturated five-membered or six-membered heterocyclic structure which is unsubstituted or substituted by hydroxyl, mercapto, C.sub.1 -C.sub.6 -alkyl, or C.sub.1 -C.sub.4 -alkanoyl and has from 1 to 3 heteroatoms from the group consisting of N, O and S, the second and third heteroatoms being a nitrogen atom,R.sup.3 is hydrogen, a hydroxy or C.sub.1 -C.sub.6 -alkoxy group,R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen or methoxy,R.sup.5 is hydrogen or methoxy or tert-butyl,R.sup.6 is hydrogen methyl, nitrile or a C.sub.2 -C.sub.10 -ketal group or the radical --CHR.sup.7 OR.sup.8 --CHR.sup.7 --NR.sup.9 R.sup.10, --COR.sup.11, --SR.sup.12, ##STR2## in which R.sup.7 is hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.8 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.
    Type: Grant
    Filed: June 18, 1991
    Date of Patent: March 23, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans-Heiner Wuest, Bernd Janssen, William V. Murray, Michael P. Wachter, Stanley Bell
  • Patent number: 5194608
    Abstract: A dipeptide derivative of formula (I) is provided, which is capable of inhibiting the enzymatic activity of renin and thereby depressing the renin-angiotensin system and lowering the blood pressure. ##STR1## wherein: R.sup.1 is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, aryl, or heterocyclic radical;R.sup.2 is carbamoyl, aryl, 5- or 6-membered heterocyclic radical, C.sub.1 -C.sub.12 alkyl-S--, C.sub.1 -C.sub.12 alkyl-S--CH.sub.2 --, or C.sub.3 -C.sub.10 cycloalkyl-S--;R.sup.3 is aryl or 5- or 6-membered heterocyclic radical;R.sup.4 is R.sup.4' --SO.sub.2 or R.sup.4' --CO;R.sup.4' is aryl, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl; C.sub.3 -C.sub.10 cycloalkyl, or heterocyclic radical;X is CH.sub.2, NH, O, or S; andY is CO or NHSO.sub.2, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4' each may be substituted with one to three substituents.
    Type: Grant
    Filed: June 24, 1991
    Date of Patent: March 16, 1993
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tatsuo Toyoda, Toshihiro Fujioka, Kunio Hayashi, Masuhisa Nakamura, Naofumi Hashimoto
  • Patent number: 5187179
    Abstract: There are disclosed substituted imidazo[1,2-b][1,2,4]triazole derivatives of Formula I which are useful as angiotensin II antagonists.
    Type: Grant
    Filed: March 22, 1991
    Date of Patent: February 16, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Steven M. Hutchins, Malcolm MacCoss
  • Patent number: 5157035
    Abstract: Anti-virally active pyridazinamines, compositions containing the same and methods of treating viral diseases in warm-blooded animals.
    Type: Grant
    Filed: January 3, 1991
    Date of Patent: October 20, 1992
    Assignee: Janssen Pharmaceutica N. V.
    Inventors: Raymond A. Stokbroekx, Marcel J. M. Van der Aa, Joannes J. M. Willems, Marcel G. M. Luyckx
  • Patent number: 5138069
    Abstract: Substituted imidazoles such as ##STR1## are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure.
    Type: Grant
    Filed: December 6, 1988
    Date of Patent: August 11, 1992
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: David J. Carini, John J. V. Duncia, Pancras C. B. Wong
  • Patent number: 5130317
    Abstract: Pyrimidine-4,6-dicarboxylic acid diamides, processes for the use thereof, and pharmaceuticals based on these compoundsThe invention relates to pyrimidine-4,6-dicarboxylic acid diamides of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The compounds according to the invention inhibit proline hydroxylase and lysine hydroxylase and can be employed as fibrosuppressants and immunosuppressants.
    Type: Grant
    Filed: September 19, 1990
    Date of Patent: July 14, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ekkehard Baader, Martin Bickel, Volkmar Gunzler-Pukall, Stephan Henke
  • Patent number: 5098900
    Abstract: A 3(2H)pyridazinone of the formula: ##STR1## wherein R.sub.1 is C.sub.2 -C.sub.5 alkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.3 alkyl, chlorine or bromine; R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; and each of Y.sub.1, Y.sub.2 and Y.sub.3 which may be the same or different, is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, halogen, --(CH.sub.2).sub.l A [wherein A is substituted amino of the formula --N(R.sub.4) (R.sub.5) (wherein each of R.sub.4 and R.sub.5 which may be the same or different, is C.sub.1 -C.sub.4 alkyl, or R.sub.4 and R.sub.5 together form C.sub.4 -C.sub.6 alkylene), morpholino, 4-R.sub.6 -piperazin-1-yl (wherein R.sub.6 is C.sub.1 -C.sub.3 alkyl) or --OR.sub.7 (wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.3 alkyl), and l is an integer of 0 to 3], --OR.sub.8 [wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.5 alkenyl, benzyl or --(CH.sub.2).sub.q --R.sub.9 [wherein R.sub.9 is CO.sub.2 R.sub.3 (wherein R.sub.3 is as defined above), --CONHR.sub.3 (wherein R.
    Type: Grant
    Filed: April 11, 1988
    Date of Patent: March 24, 1992
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Motoo Mutsukado, Keizo Tanikawa, Ken-ichi Shikada, Ryozo Sakoda
  • Patent number: 5096904
    Abstract: Pyridazinones of the following formula (I): ##STR1## where R.sup.1 -R.sup.4 are a variety of substituents and L is a linking group, a pharmaceutical composition for treating congestive heart failure, novel intermediates, methods for such treatment and processes for preparing compounds of formula (I).
    Type: Grant
    Filed: July 20, 1990
    Date of Patent: March 17, 1992
    Assignee: Glaxo Inc.
    Inventors: Thomas N. Wheeler, Terrence P. Kenakin, Joel E. Shaffer
  • Patent number: 5093336
    Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: March 3, 1992
    Assignee: Hoechat-Roussel Pharmaceuticals, Inc.
    Inventors: Raymond W. Kosley, Jr., Bettina Spahl
  • Patent number: 5070090
    Abstract: Novel (thio)morpholinyl and piperazinyl alkylphenol ethers having antirhinoviral activity, compositions containing these compounds as active ingredient, and a method of inhibiting, combating or preventing the growth of viruses in warm-blooded animals suffering from diseases caused by these viruses.
    Type: Grant
    Filed: April 25, 1990
    Date of Patent: December 3, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Raymond A. Stokbroekx, Marcel J. M. Van der Aa
  • Patent number: 5059599
    Abstract: The present invention relates to derivatives of 1-phenyl 1,4-dihydro 3-amino 4-oxo pyridazines of the general formula I: ##STR1## and the production thereof. It also concerns pharmaceutical compositions comprising as active principle a compound of general formula I and use thereof for treatment of central nervous system disturbances, especially as an anxiolytic.
    Type: Grant
    Filed: June 6, 1990
    Date of Patent: October 22, 1991
    Assignee: Pierre Fabre Medicament
    Inventors: Gilbert Mouzin, Henri Cousse, Jean-Francois Patoiseau, Jean-Marie Autin, Dennis Bigg
  • Patent number: 5047406
    Abstract: Substituted cyclohexanols and cyclohexylamines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
    Type: Grant
    Filed: May 2, 1990
    Date of Patent: September 10, 1991
    Assignee: Warner-Lambert Co.
    Inventors: Bradley W. Caprathe, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
  • Patent number: 5026702
    Abstract: The invention relates to new morpholines and morpholine-N-oxides of formula ##STR1## wherein the substituents are defined hereunder, which compounds have valuable pharmacological properties, namely an effect on the metabolism, preferably the effect of lowering blood sugar and reducing body fat, and the effect of lowering the atherogenic .beta.-lipoproteins VLDL and LDL, and a performance enhancing effect in animals.
    Type: Grant
    Filed: March 23, 1989
    Date of Patent: June 25, 1991
    Assignee: Dr. Karl Thomae, GmbH
    Inventors: Manfred Reiffen, Michael Mark, Robert Sauter, Wolfgang Grell
  • Patent number: 5001137
    Abstract: A novel pyridine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a salt thereof which exhibit inhibitory activity or prolylendopeptidase and a pharmaceutical use thereof are disclosed.
    Type: Grant
    Filed: September 14, 1989
    Date of Patent: March 19, 1991
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Takanori Oe, Yuji Ono, Kazuyuki Kawasaki, Tohru Nakajima
  • Patent number: 4980355
    Abstract: Novel substituted isonicotinic acid amides of the general formula ##STR1## in which X in ortho/ortho'-position are equal and represent fluorine, chlorine, bromine or iodine;Q.sub.1 is unsubstituted pyridimin-4-yl, or pyrimidin-4-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.2 is unsubstituted pyrimidin-2-yl, or pyrimidin-2-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.3 is unsubstituted pyrimidin-5-yl, or pyrimidin-5-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.4 is pyridin-2-yl, pyridin-3-yl or pyridin-4-yl each of which is unsubstituted or substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.5 is pyridazin-3-yl or pyridazin-4-yl each of which is unsubstituted or substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.6 is unsubstituted pyrazin-2-yl, or pyrazin-2-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;R.sub.1, R.sub.2, R.sub.3 are hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl having from 1 to 3 halogen atoms, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.
    Type: Grant
    Filed: March 3, 1989
    Date of Patent: December 25, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Helmut Zondler, Alfred Meyer, Wolfgang Eckhardt, Walter Kunz
  • Patent number: 4968706
    Abstract: Compounds of formula I ##STR1## wherein Ar is an optionally substituted phenyl ring; B is a single bond, a group --(CH.sub.2 OCH.sub.2).sub.n being n=1 or 2, a 2,4-disubstituted-1,3-dioxolane ring or a 2,4-disubstituted-1,3-thioxolane ring, R is a single bond, an optionally substituted methylene or ethylene group and T is 2-, 3- or 4-pyridyl, an optionally salified or esterified carboxy group or a carboxyamide group. Said compounds are useful in treatment of respiratory diseases.
    Type: Grant
    Filed: August 11, 1988
    Date of Patent: November 6, 1990
    Assignee: Boehringer Mannhein Italia, S.p.A.
    Inventors: Silvano Spinelli, Roberto Di Domenico, Ernesto Menta, Bruno Lumachi, Licia Gallico, Sergio Tognella
  • Patent number: 4960777
    Abstract: Heteroaryloxy-.beta.-carboline derivatives of general Formula I ##STR1## wherein R.sup.1 is an optionally substituted heteroaryl residue,R.sup.2 is hydrogen, lower alkyl or lower alkoxyalkyl,X is a COOR.sup.3 -group wherein R.sup.3 means H or lower alkyl, or represents a CONR.sup.4 R.sup.5 -group wherein R.sup.4 and R.sup.5 mean respectively hydrogen or lower alkyl, R.sup.4 and R.sup.5 being capable of forming, together with the nitrogen atom, a 5- to 6-membered heterocycle, or means an oxadiazolyl residue of the formula ##STR2## wherein R.sup.6 means hydrogen, lower alkyl or cycloalkyl, are valuable pharmaceuticals.
    Type: Grant
    Filed: September 20, 1989
    Date of Patent: October 2, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Biere, Andreas Huth, Dieter Rahtz, Ralph Schmiechen, Dieter Seidelmann, David Stephens, Mogens Engelstoft, John B. Hansen
  • Patent number: 4954501
    Abstract: New 6-phenyldihydro-3(2H)-pyridazinones corresponding to the following general formula ##STR1## are described. These compounds are readily prepared in a form suitable for oral administration and are distinguished by a high positive inotropic action and have only a slight effect on blood pressure and cardiac frequency. A process for their preparation and pharmaceutical preparations containing these compounds are also described.
    Type: Grant
    Filed: September 21, 1988
    Date of Patent: September 4, 1990
    Assignee: Heumann Pharma GmbH & Co.
    Inventors: Rolf Herter, Peter Morsdorf, Volker Pfahlert, Heidrun Engler, Helmut Schickaneder, Kurt-Henning Ahrens
  • Patent number: 4914093
    Abstract: Compounds of formula (I): ##STR1## (wherein Q is oxygen or sulfur, the dotted line is a single or double bond, A is alkylene, and R.sup.1 -R.sup.5 are a variety of atoms or organic groups)have excellent ability to potentiate myocardial contractivity and a variety of other properties, and can be used to treat cardiac disorders.
    Type: Grant
    Filed: March 16, 1989
    Date of Patent: April 3, 1990
    Assignee: Sankyo Company Limited
    Inventors: Yasuhiro Morisawa, Mitsuru Kataoka, Seiji Kumakura, Hiroyuki Koike, Shinsaku Kobayashi
  • Patent number: 4892946
    Abstract: N-(heterocyclicaminocarbonyl)arylsulfonamides in which the aryl radical is substituted in the 2-position by a carboxy radical, ester, thioester, or amide thereof; e.g. N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-2-methoxycarbonylbenzenesulf onamide or N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-2-methoxycarbonylbenze nesulfonamide; are useful for the regulation of plant growth and as pre-emergence and post-emergence herbicides.
    Type: Grant
    Filed: November 24, 1980
    Date of Patent: January 9, 1990
    Assignee: E. I. Du Pont De Nemours and Company
    Inventor: George Levitt
  • Patent number: 4871387
    Abstract: New pyri(mi)dyl-oxy- or -thio-benzoic acid derivatives of the formula ##STR1## are taught which have herbicidal and plant growth regulating activity. In the formula Z can be Ch or N, X is oxygen or sulphur, A is oxygen, sulphur, a radical R.sup.5 --N.dbd.or a radical R.sup.6 O--N.dbd.and B is oxygen, sulphur, a radical ##STR2## with the proviso that at least one of the radicals R.sup.1, R.sup.2 or R.sup.3 represents alkyl or a part of a 3- to 6-membered fused carbocyclic ring.
    Type: Grant
    Filed: December 4, 1986
    Date of Patent: October 3, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Sasse, Reiner Fischer, Hermann Hagemann, Hans-Joachim Santel, Robert R. Schmidt, Kalus Lurssen
  • Patent number: 4868300
    Abstract: Compounds of the formula ##STR1## wherein: z is O or I;X is ##STR2## a and b are 0, 1, or 2 and a+b=0, 1 or 2; R, R.sup.1, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, alkyl or aralkyl;R.sub.n is hydrogen, alkyl, aralkyl, acyl, carbalkoxy, carbamyl, carbalkoxyalkyl, hydroxyalkyl, alkoxyalkyl or amidino;R.sup.5 groups on vicinal carbon atoms may together form a carbon-carbon double bond when a or b=2;R groups on vicinal carbon atoms may together form a carbon-carbon double bond when R.sub.n is hydrogen and z=1;R.sup.4 and R.sup.5 geminal groups may together form a spiro substituent, --(CH.sub.2).sub.d --, where d is 2 to 5;R.sup.5 and R.sup.6 groups may together form a carbon-nitrogen double bond when R.sub.3 is hydrogen and a+b=1;R.sup.2 is hydrogen or --(CH.sub.2).sub.y --Y where y is 1-3;Y is hydrogen, --O--R.alpha., --S-R.alpha. or ##STR3## R.alpha. is hydrogen, alkyl, cycloalkyl or acyl; R.beta. is hydrogen or alkyl; andR.alpha. and R.beta.
    Type: Grant
    Filed: July 21, 1987
    Date of Patent: September 19, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, William C. Faith, Bruce F. Molino
  • Patent number: 4831030
    Abstract: The invention relates to compounds for treatment of hypertension, and cardiovascular and cerebrovascular diseases, which compounds are of the formula: ##STR1## wherein R.sup.1 is piperazinyl(lower)alkyl, carbamoyl substituted with piperazinyl(lower)alkyl, or piperazinylcarbonyl, in each of which a piperazinyl group may be substituted with lower alkyl, andR.sup.3 is hydrogen or halogen;R.sup.2 is phenyl substituted with nitro, andR.sup.4 is lower alkyl or halo(lower)alkyl; orR.sup.2 is lower alkyl, andR.sup.4 is phenyl substitured with nitro;and a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 12, 1986
    Date of Patent: May 16, 1989
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hisashi Takasugi, Atsushi Kuno, Hiroyoshi Sakai, Yoshie Sugiyama, Takao Takaya
  • Patent number: 4826835
    Abstract: This invention relates to compounds of the formula ##STR1## where Het is imidazol-1-y or 1,2,4-triozol-1-yl and py is 2-,3- or 4-pyridyl; and the uses of said compounds including methods for increasing cardio contractility and in the treatment of congestive heart failure, pharmaceutical compositions including the same and methods for the preparation thereof.
    Type: Grant
    Filed: February 5, 1987
    Date of Patent: May 2, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, William C. Faith
  • Patent number: 4826845
    Abstract: The invention relates to novel 3(2H)-pyridazinone-derivatives of the general formula (I), pharmaceutical compositions containing them and process for their preparation. In the general formula (I) ##STR1## stands for an ethyl or propyl group substituted by a terminal halogen atom or a hydroxyl or NR.sup.1 R.sup.2 group, whereinR.sup.1 represents hydrogen atom or an unsubstituted or optionally substituted benzyl group;R.sup.2 represents hydrogen atom or an unsubstituted or optionally substituted benzo[1,4]dioxan-2-yl-methyl or -ethyl group or a (CH.sub.2).sub.n --R.sup.3 group, whereinn is 2 or 3; andR.sup.3 stands for an unsubstituted or optionally substituted phenoxy or phenylthio group; andX stands for a hydrogen or halogen atom or an unsubstituted or optionally substituted, saturated or unsaturated 5- or 6-membered heterocyclic group containing a nitrogen atom and optionally an additional heteroatom, e.g.
    Type: Grant
    Filed: October 29, 1986
    Date of Patent: May 2, 1989
    Assignee: Richter Gedeon Vegyeszeti Gyar T.R.
    Inventors: Endre Kasztreiner, Gyorgy Rablocsky, Nandor Makk, Laszlo Jaszlits, Peter Matyus, Gyorgy Cseh, Ildiko Pribusz nee Rapp, Klara Czako, Eszter Diesler, Istvan Elekes, Laszlo Kaufer, Maria Kuhar nee Kurthy, Judit Kincsessy, Judit Kosary, Gyongyi Nagy nee Csokas
  • Patent number: 4818757
    Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
    Type: Grant
    Filed: December 28, 1987
    Date of Patent: April 4, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Harold N. Weller, III, Eric M. Gordon
  • Patent number: 4772622
    Abstract: Novel diamino oxadiazoles, wherein one of the amine functions is connected to a basicly-substituted heterocyclic group through a linear or cyclic connecting group, which are useful for the suppression of gastric acid secretions in mammals. Compositions employing these compounds and processes for the preparation of such compounds from known N-cyano-S-methylisothiourea precursors by treatment with hydroxylamine and for alkylation of amine groups are also disclosed.
    Type: Grant
    Filed: June 16, 1986
    Date of Patent: September 20, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Susan F. Britcher, William C. Lumma, Jr.
  • Patent number: 4707479
    Abstract: 1,4-Dihyropyridinecarboxamides of the formula ##STR1## and salts thereof, are effective for treating cardiac insufficiency, thromboses, thromboembolisms and ischaemias, for influencing the blood-sugar level and the circulation and as coronary therapeutic agents and anti-arrhythmic agents.
    Type: Grant
    Filed: December 5, 1985
    Date of Patent: November 17, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Horst Meyer, Gerhard Franckowiak, Ulrich Rosentreter, Rainer Gross, Gunter Thomas, Matthias Schramm, Michael Kayser, Friedel Seuter, Elisabeth Perzborn, Martin Bechem
  • Patent number: 4704391
    Abstract: The invention concerns compounds of formula I ##STR1## wherein R is a fluorine, bromine or iodine atom or the amino, acetylamino, methyl, cyano, hydroxyl, methoxy or trifluoromethyl group, the tautomeric forms thereof, and acid addition salts of the compounds in which R represents amino. The products have antithrombotic activity. They can be prepared according to methods known per se.
    Type: Grant
    Filed: November 28, 1986
    Date of Patent: November 3, 1987
    Assignee: Ciba-Geigy Corporation
    Inventor: Richard Goschke
  • Patent number: 4699908
    Abstract: The present invention relates to novel 6-phenyl-5-alkyl substituted-4,5-dihydro-3(2H)-pyridazinones of formula I: ##STR1## in which R.sub.1 is halogen, lower alkyl, lower alkoxy, NO.sub.2, NH.sub.2, NHCOR.sub.3 (R.sub.3 is H or C.sub.1 -C.sub.4 alkyl), CN, carboxy, lower alkoxycarbonyl, carbamoyl, CF.sub.3, or OH and R.sub.2 is C.sub.1 -C.sub.4 alkyl; the tautomeric forms and salts thereof; as their racemic mixtures or as the individual optically-active forms.Compounds (I) are useful in pharmaceutical preparations having improved antithrombotic activity.
    Type: Grant
    Filed: August 6, 1986
    Date of Patent: October 13, 1987
    Assignee: Ciba-Geigy Corporation
    Inventors: James Gainer, Richard Goschke
  • Patent number: 4698352
    Abstract: This invention relates to a novel 4-oxo-1,4-dihydronicotinic acid derivative ##STR1## or a salt thereof, wherein R.sup.1 is hydrogen or carboxyl-protecting group;R.sup.2 is substituted phenyl and naphthyl, or a substituted or unsubstituted heterocyclic group; andR.sup.3 is haloalkyl, aminoalkyl, or substituted or unsubstituted alkenyl, phenylalkenyl, naphthylalkenyl, phenylalkyl, naphthylalkyl, phenylalkynyl, naphthylalkynyl, heterocyclic alkyl, heterocyclic alkenyl, phenyl, naphthyl, cycloalkyl, cycloalkenyl, carboxylic acyl, iminoalkyl, heterocyclic or bridged hydrocarbon, which has a broad antibacterial spectrum and a low toxicity, and are useful for treatment of diseases of human beings and animals, to a process for producing the same and to an antibacterial agent containing the same.
    Type: Grant
    Filed: October 27, 1983
    Date of Patent: October 6, 1987
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Hirokazu Narita, Yoshinori Konishi, Jun Nitta, Shunjiro Misumi, Hideyoshi Nagaki, Isao Kitayama, Yoriko Nagai, Yasuo Watanabe, Nobuyuki Matsubara, Shinzaburo Minami, Isamu Saikawa
  • Patent number: 4689414
    Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3 or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;R.sub.5 is hydrogen, alkyl, aryl, arylalkyl, cyano, nitro, ##STR2## Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl-(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl-(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## amino, or substituted amino; m is 0 or an integer of 1 to 6;n is an integer of 1 to 6; andp is an integer of 2 to 6.
    Type: Grant
    Filed: February 24, 1986
    Date of Patent: August 25, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4684656
    Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR2## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR3## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.
    Type: Grant
    Filed: March 14, 1986
    Date of Patent: August 4, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4683228
    Abstract: A guanidine derivative of the formula I: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is substituted by a hydroxy radical and into which is optionally inserted, as part of the backbone of the chain, one or two groups selected from oxygen and sulphur atoms and NH and 1-6C N-alkyl radicals; and the pharmaceutically-acceptable acid additions salts thereof. Pharmaceutical compositions and methods of manufacture are also described. The compound of the formula I is a histamine H-2 antagonist and is therefore useful in ulcer therapy.
    Type: Grant
    Filed: January 22, 1985
    Date of Patent: July 28, 1987
    Assignees: ICI Americas Inc., Imperial Chemical Industries PLC
    Inventors: Karin M. Kirkland, Derrick M. Mant
  • Patent number: 4666902
    Abstract: Tetrahydropyridazinones of the formula I ##STR1## wherein R denotes an optionally substituted carbocyclic or heterocyclic radical, R.sup.1 denotes hydrogen; alkyl; aralkyl, which is optionally substituted in the aryl part; or acyl, and R.sup.2 denotes hydrogen; alkyl, which can optionally be substituted; or optionally substituted phenyl; and their acid addition compounds, if these can be prepared.The tetrahydropyridazinone derivatives of the formula I according to the invention and their physiologically acceptable salts exhibit useful pharmacological actions.
    Type: Grant
    Filed: June 8, 1984
    Date of Patent: May 19, 1987
    Assignee: Cassella Aktiengesellschaft
    Inventors: Gerhard Zoller, Rudi Beyerle, Melitta Just, Piero Martorana, Helmut Bohn, Rolf-Eberhard Nitz
  • Patent number: 4667033
    Abstract: The invention refers to substituted 6-(thien-2-yl)-3(2H)-pyridazinones of Formula I ##STR1##
    Type: Grant
    Filed: June 8, 1984
    Date of Patent: May 19, 1987
    Assignee: A. Nattermann & Cie GmbH
    Inventors: Gerd Hilboll, Sigurd Leyck, Gerrit Prop
  • Patent number: 4654340
    Abstract: The invention concerns compounds of formula I ##STR1## wherein R is a fluorine, bromine or iodine atom or the amino, acetylamino, methyl, cyano, hydroxyl, methoxy or trifluoromethyl group, the tautomeric forms thereof, and acid addition salts of the compounds in which R represents amino. The products have antithrombotic activity. They can be prepared according to methods known per se.
    Type: Grant
    Filed: May 5, 1986
    Date of Patent: March 31, 1987
    Assignee: Ciba-Geigy Corporation
    Inventor: Richard Goschke
  • Patent number: 4647564
    Abstract: This invention provides certain pyridazinone derivatives, their pharmaceutical formulations, and their use as positive inotropic agents.
    Type: Grant
    Filed: March 5, 1986
    Date of Patent: March 3, 1987
    Assignee: Eli Lilly and Company
    Inventor: David W. Robertson
  • Patent number: 4629495
    Abstract: Herbicidal compounds of the formula: ##STR1## wherein A represents R.sup.1 R.sup.2 N-- (wherein R.sup.1 represents C.sub.1-8 alkyl or C.sub.2-8 alkenyl or alkynyl unsubstituted or substituted by CN, OH, C.sub.1-6 alkoxy, carboxy, C.sub.2-9 alkoxycarbonyl, aminocarbonyl optionally substituted by C.sub.1-8 alkyl or C.sub.2-8 alkenyl, C.sub.1-8 alkoxyaminocarbonyl, C.sub.1-8 alkanesulphonamidocarbonyl, --C(.dbd.O)Het, where Het represents a nitrogen-containing heterocyclic group, or one or more halogen atoms or R.sup.1 represents C.sub.3-6 cycloalkyl optionally substituted by C.sub.1-4 alkyl and R.sup.2 represents H or R.sup.1, or R.sup.1 represents C.sub.1-4 alkylthio and R.sup.2 represents H, or A represents R.sup.p (R.sup.q)--C.dbd.N-- (wherein R.sup.p represents C.sub.1-4 alkoxy or amino substituted by one or two C.sub.1-4 alkyl groups and R.sup.q represents H or C.sub.1-4 alkyl) or A represents 2-oxo-azetidin-1-yl, 2-oxo-pyrrolidin-1-yl or 2-oxo-piperidin-1-yl optionally substituted by C.sub.
    Type: Grant
    Filed: July 13, 1983
    Date of Patent: December 16, 1986
    Assignee: May & Baker Limited
    Inventors: Leslie R. Hatton, Edgar W. Parnell, David A. Roberts
  • Patent number: 4629789
    Abstract: The present invention relates to novel 6-phenyl-5-alkyl substituted-4,5-dihydro-3(2H)-pyridazinones of formula I: ##STR1## in which R.sub.1 is halogen, lower alkyl, lower alkoxy, NO.sub.2, NH.sub.2, NHCOR.sub.3 (R.sub.3 is H or C.sub.1 -C.sub.4 alkyl), CN, carboxy, lower alkoxycarbonyl, carbamoyl, CF.sub.3, or OH and R.sub.2 is C.sub.1 -C.sub.4 alkyl; the tautomeric forms and salts thereof; as their racemic mixtures or as the individual optically-active forms.Compounds (I) are useful in pharmaceutical preparations having improved antithrombotic activity.
    Type: Grant
    Filed: October 22, 1985
    Date of Patent: December 16, 1986
    Assignee: Ciba-Geigy Corporation
    Inventors: James Gainer, Richard Goschke