Abstract: Compounds represented by the formula I (SEQ ID NO. 1) are disclosed: ##STR1## as well as pharmaceutically acceptable salts and hydrates thereof. R.sup.I represents C.sub.9 to C.sub.19 alkyl, C.sub.9 to C.sub.19 alkenyl, an aryl group which includes phenyl, biphenyl, naphthyl and terphenyl or a C.sub.1 to C.sub.12 alkyl, alkylamino, dialkylamino or alkoxyaryl group.R.sup.1, R.sup.2 and R.sup.4 independently represent H or --OH.R.sup.3 represents H, --OH, --O(CH.sub.2).sub.n NR.sup.V R.sup.VI, where R.sup.V and R.sup.VI independently represent H or C.sub.1-4 alkyl, or --O(CH.sub.2).sub.n NR.sup.V R.sup.VI R.sup.VII+ Y.sup.-, wherein R.sup.V and R.sup.VI are as defined above, R.sup.VII represents H or C.sub.1-4 alkyl, n is an integer of from 2-6 inclusive, and Y represents a counterion.R.sup.5 represents H, --CH.sub.3 or --OH;R.sup.6 represents H or --CH.sub.3 ;R.sup.7 represents H, --CH.sub.3, --CH.sub.2 C(.dbd.O)NH.sub.2, --(CH.sub.2).sub.2 NR.sup.V R.sup.VI or --(CH.sub.2).sub.2 NR.sup.V R.sup.VI R.sup.
Type:
Grant
Filed:
April 4, 1994
Date of Patent:
July 30, 1996
Assignee:
Merck & Co., Inc.
Inventors:
James M. Balkovec, Frances A. Bouffard, Regina M. Black
Abstract: This invention is directed to 2-aminoalkyl-5-aminoalkylamino substituted isoquino [8,7,6-cd]indazole-6-(2H)-ones and to 2-aminoalkyl-5-aminoalkylamino substituted-isoquino [5,6,7-cd] indazole-6(2H)-ones. These compounds have been shown to have antitumor activity.
Type:
Grant
Filed:
August 11, 1993
Date of Patent:
May 21, 1996
Assignees:
Boehringer Mannheim Italia, S.p.A., University of Vermont & State Agricultural College
Inventors:
A. Paul Krapcho, Ernesto Menta, Ambrogio Oliva, Silvano Spinelli
Abstract: A process for the production of bis(fluoromethyl)ether by contacting formaldehyde with hydrogen fluoride in a reaction/distillation vessel. The reaction/distillation vessel is preferably a reaction/distillation column through which formaldehyde and hydrogen fluoride preferably flow in counter current.The bis(fluoromethyl)ether may be converted to difluoromethane, preferably by heating the bis(fluoromethyl)ether to elevated temperature in the presence of a metal, metal oxide, metal fluoride or metal oxyfluoride catalyst.
Type:
Grant
Filed:
May 5, 1994
Date of Patent:
April 9, 1996
Assignee:
Imperial Chemical Industries PLC
Inventors:
John S. Martin, Thomas A. Ryan, Rachel A. Spooncer
Abstract: There is provided a process for the manufacture of 2-alkoxymethylacrolein compounds via the reaction of an appropriate alcohol and acrolein in the presence of an acid and a trisubstituted amine to form an intermediate and the subsequent reaction of the intermediate with formaldehyde in the presence of an acid and a disubstituted amine. There is also provided a process for the manufacture of 3-alkoxymethylquinolines from 2-alkoxymethylacrolein.
Type:
Grant
Filed:
November 5, 1993
Date of Patent:
April 9, 1996
Assignee:
American CYanamid Company
Inventors:
Henry L. Strong, David A. Cortes, Zareen Ahmed
Abstract: 14.alpha.,17.alpha.-(Propano-and 17.sup.2 -propeno)-estratrienes of general formula I ##STR1## in which R.sup.1 means a hydrogen atom, a methyl or an acyl group with 1-12 carbon atoms,R.sup.2 means a hydrogen atom or an acyl group with 1-12 carbon atoms and ##STR2## a C--C single or double bond. The new compounds of general formula I are estrogen effective just as ethinyl estradiol.
Type:
Grant
Filed:
October 29, 1993
Date of Patent:
February 13, 1996
Assignee:
Schering Aktiengesellschaft
Inventors:
James R. Bull, Walter Elger, Karl-Heinrich Fritzemeier, Rolf Krattenmacher
Abstract: Process for the preparation of 3.beta.-aminocholanic acid derivativesA process for the preparation of 3.beta.-aminocholanic acid derivatives of the formula II ##STR1## wherein R(1), R(2) and R(3) have the meanings given, starting from the corresponding 3.beta.-hydroxycholanic acid esters, is described.
Type:
Grant
Filed:
March 7, 1994
Date of Patent:
January 23, 1996
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Alfons Enhsen, Heiner Glombik, Werner Kramer, Gunther Wess
Abstract: The invention provides compounds of the general formula I ##STR1## wherein R.sub.1 is a hydrogen atom, a negative charge or an ester residue; R is:a) --(CH.sub.2).sub.n --A--CO.sub.2 H, --(CH.sub.2)n--A--SO.sub.3 H or --(CH.sub.2).sub.n --A--PO.sub.3 H.sub.2, wherein n is either zero, one or two and A is a group --CH.dbd.CH-- (either E or Z), --OCH.sub.2 --, --SCH.sub.2 -- or --CHOH--;b) --(CH.sub.2).sub.n --PO.sub.3 H.sub.2, --(CH.sub.2).sub.n SO.sub.2 NHCN, --(CH.sub.2).sub.n NHSO.sub.3 H, --(CH.sub.2).sub.n CONHSO.sub.2 CH.sub.3 or --(CH.sub.2).sub.n CONHSO.sub.2 CF.sub.3, wherein n is as defined above;c) --(CH.sub.2 S).sub.m --W--(CH.sub.2).sub.n Z, wherein W is an arylene group or a heterocyclediyl group, m is 0 or 1, n is as above defined, and Z represents CO.sub.2 H, PO.sub.3 H.sub.2, SO.sub.2 NHCN, NHSO.sub.3 H, CONHSO.sub.2 CH.sub.3 or CONHSO.sub.2 CF.sub.3 ;d) ##STR2## wherein Y is O or NH and X is NH, N--OH or N--O--(CH.sub.2).sub.n+1 COOH wherein n is as defined above; ore) --(CH.sub.2 S).sub.
Type:
Grant
Filed:
April 9, 1993
Date of Patent:
January 2, 1996
Assignee:
Farmitalia Carlo Erba S.r.l.
Inventors:
Giuseppina Visentin, Franco Zarini, Daniela Jabes, Ettore Perrone, Costantino della Bruna, Marco Alpegiani
Abstract: A method of treating psychosis including administering an antipsychotically effective amount of an ergolinyl derivative of 2-propinylamine of the formula I ##STR1## wherein, R.sub.1, R.sub.2, and R.sub.3 independently represent a hydrogen atom or a straight-chain or branched-chain C.sub.1 -C.sub.6 alkyl group, X represents a hydrogen or a halogen atom, Z represents a carbonyl or methylene group, and C.sub.9 - - - -C.sub.10 represents a single or a double, diastereomeric forms, racemates and acid addition salts thereof.
Type:
Grant
Filed:
December 2, 1993
Date of Patent:
January 2, 1996
Assignee:
Lek, Tovarna Farmacevtskih in Kemicnih
Inventors:
Rudolf Rucman, Breda Bole-Vunduk, Magdalena Ocvirk, Bogomila Lavric, Igor Krisch
Abstract: The present invention is directed to a class of 3-phosphono-pyrrolidine derivatives as described by Formula I and their use as NMDA antagonists.
Abstract: Certain 3-amino-cycloalkanyl and cycloalkenyl derivatives of 5-cyano-substituted indoles of Formula I are useful antidepressant agents. ##STR1## The substituent R.sup.1 is hydrogen or C.sub.1-4 alkyl and R.sup.2 is C.sub.1-4 alkyl or --(CH.sub.2).sub.p --Ar with Ar being a phenyl, pyridinyl, pyrimidinyl or 1,4-benzodioxan-2-yl moiety. The symbol m is zero or 1, n is 1 to 3 and p is zero or 1 to 4.
Type:
Grant
Filed:
January 6, 1994
Date of Patent:
November 21, 1995
Assignee:
Bristol-Myers Squibb Company
Inventors:
Joseph A. Cipollina, Ronald J. Mattson, Charles P. Sloan
Abstract: Oxime ether derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 are each hydrogen or alkyl, Het is quinolyl, unsubstituted or substituted, and X is oxygen or sulfur, their plant-tolerated acid addition salts, metal complexes and N-oxides, and fungicides containing these compounds.
Type:
Grant
Filed:
May 4, 1994
Date of Patent:
November 21, 1995
Assignee:
BASF Aktiengesellschaft
Inventors:
Bernd Wenderoth, Siegbert Brand, Franz Schuetz, Thomas Kuekenhoehner, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
Abstract: Novel perylene compounds based on perylene-3,4,9,10-tetracarboxylic acid monoanhydride monoimides which are substituted by alkylene- or arylenesulfonic acid groups on one or both imide nitrogen atoms, or on corresponding tetracarboxylic acid diimides, or on a halogenation product thereof, have properties which render them accessible, in addition to their use as dispersing agent for pigments of the same class of compound or other categories, also for direct use as pigments and fluorescent dyestuffs as well as polymer-soluble dyestuffs.
Abstract: Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds of the formulas I to XVI are disclosed (See specification for definitions of the substituents). Specifically, the compounds are 1-azabicyclo [3.2.1]oximes, 1-azabicyclo[3.3.1]oximes, 1-aza-4-oxobicyclo[3.3.1]oximes, 1-aza-4-oxobicyclo[3.2.
Abstract: A composition comprising bis(fluoromethyl)ether and less than an equimolar amount of water, a process for the production of the composition comprising contacting formaldehyde with hydrogen fluoride and separating at least some of the by-product water from bis(fluoromethyl)ether, and use of the composition for the production of difluoromethane.
Type:
Grant
Filed:
June 29, 1994
Date of Patent:
October 31, 1995
Assignee:
Imperial Chemical Industries PLC
Inventors:
Jane L. Butcher, Thomas A. Ryan, Leslie Burgess
Abstract: The invention concerns hydroxylamine derivatives of the formula I ##STR1## wherein R.sup.4 is hydrogen, carbamoyl, (1-4C)alkyl, (2-5C)alkanoyl, N-(1-4C)alkylcarbamoyl, N,N-di-(1-4C)alkylcarbamoyl, benzoyl or phenylsulphonyl;R.sup.5 includes hydrogen, (1-4C)alkyl and (2-5C)alkanoyl;R.sup.6 is hydrogen, (1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl;R.sup.7 is hydrogen or (1-4C)alkyl;Ar.sup.1 is phenylene;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl, thiazolediyl, oxazolediyl, thiadiazolediyl or oxadiazolediyl;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is independently (1-3C)alkylene and X.sup.
Abstract: Azabicyclo [2.2.2.]octan-3-imines of the general formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein are prepared by reacting a compound of the formula ##STR2## with a compound of the formula ##STR3## wherein A is MgCl, MgBr or Li.
Abstract: Fibrinogen receptor antagonists of the ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets, for example ##STR2##
Abstract: Derivatives of 4-anilinoquinoline having the formula: ##STR1## where X is O or H.sub.2 and Z is 1-substituted-4-piperidinylamino or diloweralkylaminoloweralkyl inhibit binding of tritiated bradykinin to guinea pig ileum and inhibit bradykinin-induced writhing in mice. Bradykinin is a nonapeptide formed in plasma as a result of inflammation or injury and produces pain when it binds with pain receptors. A drug which inhibits the binding of bradykinin therefore has analgetic properties.
Abstract: A method is provided for making a 4-hydroxy-tetraorganopiperidinyloxy, such as 4-OH TEMPO. These free radical spin-traps can be used as anaerobic inhibitors which have been found useful for polymerizing reactive acrylic monomers.