Abstract: There are provided novel nitrogen-containing bicyclic compounds which are useful in the treatment of physiological or drug induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.
Abstract: Unsaturated cyclohexenone oxime ethers I ##STR1## (Q=H, alkylcarbonyl, benzoyl, alkali metal or alkaline earth metal ion, substituted or unsubstituted ammonium ion, phosphonium ion, sulfonium ion, sulfoxonium ion, an equivalent of a transition metal cation;W=--C.tbd.C-- or --CH.dbd.CH--;R.sup.1 =substituted or unsubstituted cycloalkyl, cycloalkenyl or 6-membered heterocyclic group which has 1-2 oxygen and/or sulfur atoms and can be saturated or partially unsaturated; substituted or unsubstituted 5-membered saturated heterocycle with 1-2 oxygen and/or sulfur atoms; substituted or unsubstituted 5-membered heteroaromatic group with 1-2 nitrogen atoms and/or 1 oxygen or sulfur atom; substituted or unsubstituted phenyl, pyridyl or R.sup.9 --X-substituted alkyl with X=O, S, --SO--, --SO.sub.2 -- andR.sup.9 =alkyl, phenyl, 5/6-membered hetaryl with 1-3 hetero atoms;R.sup.2 =alkyl;R.sup.3 =H, alkyl;R.sup.4 =H, halogen, alkyl;R.sup.5 =H, alkyl;or R.sup.3 +R.sup.4, R.sup.3 +R.sup.5 or R.sup.4 +R.sup.5 together form C.
Type:
Grant
Filed:
January 28, 1993
Date of Patent:
April 18, 1995
Assignee:
BASF Aktiengesellschaft
Inventors:
Juergen Kast, Norbert Meyer, Ulf Misslitz, Albrecht Harreus, Harald Rang, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen
Abstract: Substituted derivatives of deoxymyoinositol of general formula (I): ##STR1## in which R.sup.1, R.sup.2 and R.sup.5 are identical or different and represent a linear or branched alkyl group of 3 to 14 carbon atoms.R.sup.3 and R.sup.4 are identical or different and represent a hydrogen atom, a protecting group of the hydroxyl groups or the residue of formula --CO--(CH.sub.2).sub.n --CH.sub.3in whichn represents the number 12, 13, 14, 15, 16 or 17, and their salts, process for preparing them and their use in medicaments.
Type:
Grant
Filed:
August 12, 1993
Date of Patent:
April 18, 1995
Assignee:
Bayer Pharma
Inventors:
Erwin Bischoff, Zhan Gao, Stefan Wohlfeil, Gabriele Hecker, Jeannine Cleophax, Didier Dubreuil, Stephane Gero, Alice Olesker, Catherine Verre-Sebrie, Mauro V. de Almeida, Georges Vass
Abstract: Compositions of dimethyloldimethylhydantoin, monomethyloldimethylhydantoin, and dimethylhydantoin having less than 0.1% by weight of free formaldehyde based upon 100% by weight of total composition; and wherein the weight ratio of dimethyloldimethylhydantoin to monomethyloldimethylhydantoin ranges from about 1:1.25 to about 3.5:1, are provided. These compositions may be prepared (1) by reacting dimethylhydantoin and a formaldehyde-containing source wherein the molar ratio of formaldehyde to dimethylhydantoin ranges from about 1.2:1 to about 1.55:1 or (2) by admixing (a) from about 80 to about 90% by weight of an aqueous solution of methyloldimethylhydantoin having greater than about 0.1% by weight of free formaldehyde with (b) about 20 to about 10% by weight of dimethylhydantoin based upon 100% weight of aqueous dimethyloldimethylhydantoin solution and dimethylhydantoin combined.
Abstract: The novel 2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-propanol derivertives of the formula (I): ##STR1## wherein, R.sup.0, R.sup.1 and R.sup.2 are the same or different and represent a hydrogen atom or a lower alkyl group; A represents a formula: ##STR2## wherein, X stands for a chemical bond or a formula: ##STR3## (wherein, X' stands for a chemical bond or an alkylene group having 1 to 5 carbon atoms which may contain sulfur or oxygen atom as the constituent atoms, R.sup.5 and R.sup.6 are the same or different and stand for a hydrogen atom or a lower alkyl group), R.sup.3 stands for an aromatic heterocyclic group which may be substituted, n denotes 0, 1 or 2), and R.sup.4 stands for a hydrogen atom or an alkanoyl group, or a physiologically acceptable salt thereof have antifungal activities, and they are used for preventing or treating infectious diseases caused by fungi.
Abstract: There are described formazan dyes of the formula ##STR1## where n is 1 or 2,Kat.cndot. is the equivalent of a cation,Me is copper or nickel,X is a radical of the formula CO-O or SO.sub.2 -O,Y is vinyl or a radical of the formula C.sub.2 H.sub.4 -Q, where Q is a group which is detachable under alkaline reaction conditions,the ring A may be substituted and benzofused,the ring B is substituted and may be benzofused, andthe ring C may be substituted,the use thereof for dyeing or printing hydroxyl- or nitrogen-containing organic substrates, and novel hydrazones.
Abstract: Maleimide derivatives, i.e., the compounds of Formula I: ##STR1## wherein: R.sup.1 is H, halo, alkyl, OH, alkoxy, haloalkyl, NO.sub.2, or NR.sup.5 R.sup.6 ;R.sup.2 is H or CN;R.sup.3 is aryl or heteroaryl, provided that R.sup.3 is heteroaryl when R.sup.2 is H and R.sup.4 is NR.sup.5 R.sup.6 ; andR.sup.4 is NR.sup.5 R.sup.6 or isothiourea,where R.sup.5 and R.sup.6 are independently H or lower alkyl;and the pharmaceutically acceptable salts thereof, and their use as chemotherapeutic agents.
Abstract: Reactive dyestuffs which, in the form of the free acid, have the following formula ##STR1## in which X denotes fluorine, chlorine or bromine andSO.sub.2 -Z denotes a specific reactive radical,the remaining substituents having the meaning given in the description, and show improved fixation yield in dyeing.
Type:
Grant
Filed:
April 27, 1993
Date of Patent:
April 11, 1995
Assignee:
Bayer Aktiengesellschaft
Inventors:
Manfred Hoppe, Eckhard Bock, Wolfram Reddig, Thomas Eizenhofer, Wolfgang Harms, Karl-Josef Herd
Abstract: Triarylborane derivatives corresponding to the formula (1) ##STR1## in which R either represents a group --CR.sub.1 R.sub.2 R.sub.3 where R.sub.1, R.sub.2 and R.sub.3 are each, independently of one another, a (C.sub.1 -C.sub.2)alkyl or aryl group, or represents a group --CH.sub.2 OR.sub.4 where R.sub.4 is a (C.sub.1 -C.sub.2)alkyl or benzyl group, or represents a group --Si(R.sub.5).sub.3 where R.sub.5 is a (C.sub.1 -C.sub.2)alkyl or aryl group, R being in the 1 or 2 position of the tetrazole ring, their preparation and their use as synthesis intermediates.
Type:
Grant
Filed:
August 9, 1994
Date of Patent:
April 11, 1995
Assignee:
Synthelabo
Inventors:
Isaac Chekroun, Guy Rossey, Michel Magnat
Abstract: Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.
Type:
Grant
Filed:
February 24, 1993
Date of Patent:
April 11, 1995
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jean Ackermann, David Banner, Klaus Gubernator, Kurt Hilpert, Gerard Schmid
Abstract: Disclosed is a process for preparing chiral compounds of the formula (I) ##STR1## wherein: X.sup.1 and X.sup.2 are independently F or Cl; and E is --SO.sub.2 R.sup.2, wherein R.sup.2 is C.sub.1 -C.sub.6 alkyl, --C.sub.6 H.sub.4 CH.sub.3 or --CF.sub.3 ; its enantiomer and racemates thereof, useful in the synthesis of tetrahydrofuran azole antifungals. Novel compounds of the formula ##STR2## wherein: X.sup.1 and X.sup.2 are independently F or Cl; B represents --C(O)Q* or --CH.sub.2 OR"; Q* represents a chiral auxiliary group; R" represents a hydroxy protecting group selected from --CH.sub.2 C.sub.6 H.sub.5, or --C(O)R.sup.1, wherein R.sup.1 is C.sub.1 -C.sub.6 alkyl; and A represents Cl, Br, I or triazolyl; are also disclosed.
Type:
Grant
Filed:
April 30, 1993
Date of Patent:
April 4, 1995
Assignee:
Schering Corporation
Inventors:
Anil K. Saksena, Viyyoor M. Girijavallabhan, Russell E. Pike, Haiyan Wang, Raymond G. Lovey, Yi-Tsung Liu, Ashit K. Ganguly, William B. Morgan, Aleksey Zaks
Abstract: This invention relates to novel substituted tryptamine and phenalkylamine and related compounds, pharmaceutical compositions thereof and methods of using said compounds and compositions for a number of pharmaceutical indications including (but not limited to): 1. central nervous system and psychiatric disorders (e.g., sleep disorders, epilepsy and other convulsive disorders, anxiety, psychiatric diseases, neurodegenerative diseases, fever); 2. chronobiological-based disorders (e.g., jet lag, delayed sleep syndrome, shift-work, seasonal affective disorder); 3. endocrine indications (e.g., contraception and infertility, precocious puberty, premenstrual syndrome, hyperprolactinemia, growth hormone deficiency); 4. cancer and other proliferative diseases; 5. immune system disorders and conditions associated with senescence; 6. ophthalmological diseases; 7. animal breeding (e.g., regulation of fertility, puberty, pelage color).
Type:
Grant
Filed:
April 5, 1994
Date of Patent:
April 4, 1995
Assignee:
Interneuron Pharmaceuticals, Inc.
Inventors:
Kay J. D'Orlando, Kenneth W. Locke, Emile M. Bellott, Richard L. Gabriel, Michael D. Nohrden, Yesh P. Sachdeva, Salah A. Zahr, Emile Al-Farhan, Subramaniam Krishnananthan
Abstract: Disclosed is a novel UV light absorbing compound which can preferably be employed in the art of colored molding plastics, resin films, heat-sensitive transfer materials, liquid crystal display materials, color photographs and the like, and method for producing thereof. The UV light absorbing compound is characterized by the general formula: ##STR1## wherein R.sup.1 represents linear or branched alkyl or aralkyl group, and R.sup.2 represents --CN or --COOR.sup.3, wherein R.sup.3 represents substituted or unsubstituted alkyl or aralkyl group.
Abstract: This invention relates to an improvement in a process for making 2,6-di-tertiarybutyl-4-mercaptophenol and 4,4-isopropylidenedithio-bis-(2,6-di-tertiarybutylphenol) which comprises reduction of bis (3,5-di-tertiarybutyl-4-hydroxyphenyl)polysulfide with hydrogen gas at a temperature range of from about 20.degree. C. to about 90.degree. C. in the presence of a catalytic amount of cobalt-molybdenum catalyst.
Abstract: A process for the production of indole derivatives, which is characterized in that in the presence of phosphoric acid a substitution with an imine is performed, and intermediate products of this process and the production of these intermediate products are described.
Type:
Grant
Filed:
March 8, 1993
Date of Patent:
March 28, 1995
Assignee:
Schering Aktiengesellschaft
Inventors:
Gregor Haffer, Helmut Borner, Wolfgang Kubler, Klaus Nickisch
Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their methods of use for antagonizing angiotensin II receptors in mammals.
Type:
Grant
Filed:
April 20, 1993
Date of Patent:
March 28, 1995
Assignee:
Eli Lilly and Company
Inventors:
Donald B. Boyd, Kenneth L. Hauser, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Kumiko Takeuchi, K. Jeff Thrasher, Celia A. Whitesitt
Abstract: The polyamino oligomers of this invention are obtained by reacting diisopropenylbenzenes or bis(.alpha.-hydroxyisopropyl)benzenes and anilines in the presence of an acid catalyst and characterized by the recurring unit having an indane skeleton. These polyamino oligomers can be used as curing agent for laminate resins. Also, they can be reacted with maleic anhydride to prepare polymaleimide compounds of this invention.The polymaleimide compounds of this invention are low in melting point (or softening point) and, in combination with a substance producing three-dimensional crosslinkage such as triallyl isocyanurate, aromatic diamine, etc., can provide thermosetting resin compositions suited for producing copper-clad laminates. The copper-clad laminates obtained from the thermosetting resin compositions of this invention are low in dielectric constant, heat-resistant and also low in water absorptivity, so that they are useful for multi-layer printed boards.
Abstract: A method is provided for preparing carboxylic acid intermediates of the structure ##STR1## wherein an aldehyde of the structure ##STR2## is prepared and subjected to a Horner-Emmons reaction to form the ester of the structure ##STR3## and the ester is hydrogenated to the carboxylic acid which may be used in making the final anti-thrombotic--anti-vasospastic compounds.
Type:
Grant
Filed:
April 20, 1994
Date of Patent:
March 21, 1995
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Michael A. Poss, Paul D. Pansegrau, Shaopeng Wang, John K. Thottathil, Janak Singh, Richard H. Mueller