Abstract: The present invention relates to derivatives of pyridazine of formula: ##STR1## in which R.sub.1 is alkyl or a phenyl group and R.sub.2 is H or R.sub.1 and R.sub.2 form, with the carbon atoms to which they are attached, a benzene cycle, R.sub.3 is H or phenyl and R.sub.4 is ##STR2## in which R.sub.5 is H or CH.sub.3 and R.sub.6 is H, OH, OR or OCOR; it also relates to a process for preparing the products of formula (I) and to the drugs containing at least one of said products.
Type:
Grant
Filed:
August 7, 1984
Date of Patent:
December 1, 1987
Assignee:
Sanofi
Inventors:
Camille G. Wermuth, Jean-Pierre Chambon
Abstract: Chemical compounds are provided including pyrazine diazohydroxides (I), as well as methods for their production, pharmaceutical compositions comprising the compounds, and methods of treatment using the compounds in dosage form. Compounds of the invention have pharmacological properties and are useful cytostatic agents and cell growth inhibiting agents.
Type:
Grant
Filed:
November 13, 1984
Date of Patent:
November 24, 1987
Assignee:
Board of Trustees of the University of Alabama
Inventors:
David C. Baker, Elli S. Hand, Rudiger D. Haugwitz, Venkatachala L. Narayanan, Jang B. Rampal
Abstract: Esters of optically active 2-arylalkanoic acids I ##STR1## where Ar is an isocyclic or heterocyclic aryl radical and R.sup.1 and R.sup.2 are each C.sub.1 -C.sub.4 -alkyl, are prepared by subjecting an optically active ester II ##STR2## where X is Cl, Br or --O--SO.sub.2 --Y and Y is Cl or a hydrocarbon radical, to a Friedel-Crafts reaction with an aromatic compound ArH (III).
Type:
Grant
Filed:
February 4, 1985
Date of Patent:
November 17, 1987
Assignee:
BASF Aktiengesellschaft
Inventors:
Gerhard Fritz, Manfred Eggersdorfer, Hardo Siegel
Abstract: Nitriles and thioamides of fused ring pyridine compounds such as 5,6,7,8-tetrahydroquinolines are prepared from metal derivatives of the starting compounds such as 8-lithio-5,6,7,8-tetrahydroquinolines which have been prepared by treating a 5,6,7,8-tetrahydroquinoline with a metal amide prepared in situ from a metal alkyl and an N-benzylidine-N-alkylamine.
Abstract: Novel pyrazinyl sulfonamides of the formulaQ--SO.sub.2 --NH.sub.2wherein Q is a substituted pyrazine group are intermediates for the production of sulfonylureas and suflonylthioureas which are useful in controlling weeds or selectively influencing plant growth.
Type:
Grant
Filed:
March 21, 1986
Date of Patent:
November 17, 1987
Assignee:
CIBA-GEIGY Corporation
Inventors:
Beat Bohner, Werner Fory, Rolf Schurter, Georg Pissiotas
Abstract: This invention relates to novel herbicidally effective, dihydroimidazopyrrolopyridines and derivatives thereof which are useful for the control of undesirable monocotyledonous and dicotyledonous plant species. The invention also relates to a process for the preparation of said herbicidally effective compounds.
Abstract: Substituted 2,5-dihydro- and 2,4,4a,5-tetrahydro-3H-indeno[1,2-c]pyridazin-3-ones and pharmaceutically acceptable salts thereof are useful as cardiotonic and antihypertensive agents.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen; alkyl of 1 to 7 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; monosubstituted alkyl of 1 to 3 carbon atoms, where the substituent is pyridyl, methypyridyl, phenyl, mono-, di- or trisubstituted phenyl, where the substituents on the phenyl ring, which may be identical to or different from each other, are selected from the group consisting of one amino, one dimethylamino, one to two hydroxyls, one to three methoxys and one to three halogens; .omega.-monosubstituted alkyl of 2 to 4 carbon atoms, where the substituent is hydroxyl or di(alkyl of 1 to 3 carbon atoms)amino; phenyl; monohalo-phenyl; unsubstituted or monosubstituted straight or branched alkanoyl of 1 to 6 carbon atoms, where the substituent is phenyl, methoxyphenyl or cycloalkyl of 3 to 7 carbon atoms; or unsubstituted or monosubstituted phenylsulfonyl, where the substituent is methyl or methoxy; andR.sub.
Type:
Grant
Filed:
July 24, 1986
Date of Patent:
October 13, 1987
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Norbert Hauel, Volkhard Austel, Joachim Heider, Manfred Reiffen, Willi Diederen, Walter Haarman
Abstract: The invention relates to novel cephem compounds, of high antimicrobial activity, of the formula ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is lower alkyl substituted with 1 to 3 halogen atoms,R.sup.3 is thiadiazolylthiomethyl which may be substituted with lower alkyl, or tetrazolylthiomethyl which may be substituted with lower alkyl or lower alkenyl, andR.sup.4 is carboxy or protected carboxy, and a pharmaceutically acceptable salt thereof.
Abstract: A method for the production of an aqueous dispersion of a water insoluble N-substituted N',N'-alkylene urea having the general formula I: ##STR1## wherein R.sup.1 denotes alkyl having 6 to 20 carbon atoms, phenyl or ##STR2## in case of m=1, or R.sup.1 denotes alkylene having 6 to 20 carbon atoms, phenylene or ##STR3## in case of m=2, where X denotes H, CH.sub.3 or OCH.sub.3 and n is 0 or 1, R.sup.2 denotes H or CH.sub.3, R.sup.3 denotes H, CH.sub.3 or C.sub.2 H.sub.5 and R.sup.4 denotes H or CH.sub.3, by the reaction of an alkylene imine having 2 to 4 carbon atoms with an isocyanate represented by the general formula II:R-NCO (II)wherein R denotes an alkyl having 6 to 20 carbon atoms, ##STR4## wherein X and n are the same as above in the presence of at least one surface active agent selected from the group consisting of anionic surface active agents and nonionic surface active agents under vigorous stirring.
Abstract: There are disclosed novel imidazole derivatives of the formula. ##STR1## and derivatives of the formula ##STR2## the tautomers thereof, and non-toxic, pharmacologically acceptable addition salts thereof with inorganic or organic acids. The compounds described herein are useful in treating cardiac insufficiency.
Abstract: This application discloses antibacterial cephems of the formula: ##STR1## wherein R.sub.1 represents hydrogen, alkyl, alkenyl, heterocyclylalkyl, or aralkyl; R.sub.3 is a 5- or 6-membered heterocyclic ring selected from: ##STR2## and X is sulfur or oxygen. Included also are pharmaceutically acceptable salts and esters of such compounds; pharmaceutical compositions thereof, and methods of treatment comprising such compositions when an antibiotic effect is needed.
Abstract: Novel crystals of sodium 7.beta.-[2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido]-3-[(1,2,3-th iadiazol-5-yl)thiomethyl] ceph-3-em-4-carboxylate showing characteristic peaks at interplanar spacings (d) of 9.3, 8.9, 5.3, 5.1, 4.4, 4.3 and 3.8 .ANG. in the powder X-ray diffraction pattern which are very stable and do not easily cause discoloration and decomposition.
Type:
Grant
Filed:
November 26, 1984
Date of Patent:
September 8, 1987
Assignees:
Lederle (Japan), Ltd., Takeda Chemical Industries, Ltd.
Abstract: Disclosed are novel bis(arylpiperazinyl)sulfur compounds represented by formula I ##STR1## wherein: R.sub.1 and R.sub.2 are each independently hydrogen, lower alkyl, halogen, nitrile or methylthio; m and n are each independently 2 or 3; and X is a dithio, thio, sulfinyl or sulfonyl and nontoxic, pharmaceutically acceptable addition salts thereof. These compounds can be used for the prevention of allergic disorders, such as asthma, rhinitis, conjunctivitis, hay fever, urticaria, food allergies, and the like.
Type:
Grant
Filed:
November 20, 1984
Date of Patent:
September 8, 1987
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: 2-Amino-3,5-di-(halomethyl)-pyrazines of the general formula I ##STR1## where X is either chlorine or bromine, m and n may each be 0, 1, 2 or 3 and R.sup.1 and R.sup.2 are each hydrogen or a protective group or may furthermore be bonded to one another, in particular those compounds of the formula I in which m is 1 and n is 2 and/or R.sup.1 and R.sup.2 together form a phthaloyl radical, are useful intermediates for the pteridine building block of folic acid or folic acid analogs.They are obtained by a method in which a 2-amino-3,5-dimethylpyrazine of the general formula II ##STR2## is treated with a chlorinating or brominating agent and, where R.sup.1 and/or R.sup.2 are protective groups, these are, if desired, eliminated when the chlorination or bromination is complete.
Type:
Grant
Filed:
September 16, 1985
Date of Patent:
September 8, 1987
Assignee:
BASF Aktiengesellschaft
Inventors:
Hartmut Leininger, Wolfgang Littmann, Joachim Paust, Walter Trautmann
Abstract: The present invention refers to mitomycin analogs containing a disulfide group. These compounds are mitomycin C derivatives in which the 7-amino group bears an organic substituent incorporating a disulfide group. The compounds are inhibitors of experimental animal tumors.
Type:
Grant
Filed:
August 7, 1986
Date of Patent:
September 1, 1987
Assignee:
Bristol-Myers Company
Inventors:
Dolatrai M. Vyas, Yulin Chiang, Terrence W. Doyle
Abstract: This invention relates to N,N-diallyl-3-hydroxy azetidinium salts, homo- and co-polymers thereof; and the preparation thereof.This invention also relates to the use of the above polymers as demulsifiers.
Abstract: Novel 2-aminopyrazines and processes for the preparation of 2-aminopyrazines and pyrazines by reaction of an .alpha.-iminodiacetonitrile (a) with a hydrogen halide or (b) with an alcohol or a thioalcohol and a hydrogen halide or (c) with an alcohol or a thioalcohol in the presence of an alkali metal compound and/of an alkaline earth metal compound. The 2-aminopyrazines and pyrazines obtainable by the process of the invention are useful starting materials for the preparation of dyes, fungicides, bactericides, textile assistants, scents, folic acid derivatives, flavorings, and active ingredients in crop protection and drugs.
Abstract: Compounds of formula (I): ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl,C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, C.sub.1-6 alkyl-thiolmethyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.2 is nitro, cyano or C.
Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, antiobesity and platelet aggregation inhibitors and modifiers of gastrointestinal motility.
Type:
Grant
Filed:
September 3, 1985
Date of Patent:
August 11, 1987
Assignee:
Merck & Co., Inc.
Inventors:
Joel R. Huff, John J. Baldwin, Yojiro Sakurai, Joseph P. Vacca, James P. Guare, Jr.