Abstract: Compounds of formula (I) where R.sup.1 is thienyl, phenyl or furyl, X and Y are halogen or hydrogen and Q is alkoxy or amino are useful as analgesic and antiinflamatory agents.
Abstract: Dipeptide compounds and analogs thereof having a phosphonomethyl moiety are disclosed. These compounds inhibit Endothelin Converting Enzyme and are thus useful in treating conditions responsive to inhibition of production of Endothelin.
Abstract: Novel cyclohexene-ylidene derivatives of formula (I) are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production; they are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.
Type:
Grant
Filed:
September 29, 1994
Date of Patent:
February 25, 1997
Assignee:
SmithKline Beecham Corporation
Inventors:
Siegfried B. Christensen, IV, Cornelia J. Forster
Abstract: An improved method for the preparation of 2-chloro sulfinyl azetidin-4-one of the formula: ##STR1## wherein R is: hydrogen; C.sub.1 -C.sub.3 alkyl; halomethyl; cyanomethyl; phenyl; substituted phenyl; phenoxy, benzyloxy- or substituted benzyl; a group of the formula R.sub.2 --O--wherein R.sub.2 is t-butyl, 2,2,2-trichloroethyl, benzyl or substituted benzyl; a group of the formula R.sub.3 --(O).sub.n --CH.sub.2 wherein R.sub.3 is phenyl or substituted phenyl. The 2-chlorosulfinylazetidin-4-one is prepared by reacting a penicillin sulfoxide ester of the general formula ##STR2## wherein R and R.sub.1 have the meanings defined above with an N-chloro halogenating agent in an inert organic solvent. The reaction is carried out in the presence of an acid scavenging amount of a phosphate or hydrogen phosphate of an alkali metal, alkaline earth metal, ammonium, quaternary ammonium or mixtures thereof.
Type:
Grant
Filed:
December 27, 1993
Date of Patent:
February 18, 1997
Assignee:
Lupin Laboratories, Ltd.
Inventors:
Niranjan L. Gupta, Ramanathan Sankaran, Sakina Sitabkhan
Abstract: Substituted isoindolones I ##STR1## where R.sup.1 and R.sup.2 =H, unsubstituted or substituted alkyl, alkenyl, alkynyl, cyano, C.sub.1 -C.sub.6 -alkoxycarbonyl, formyl, C.sub.1 -C.sub.6 -alkylcarbonyl, unsubstituted or substituted phenylcarbonyl, C.sub.3 -C.sub.8 -cycloalkyl, or, if R.sup.1 =H, R.sup.2 additionally=unsubstituted or substituted phenyl, orR.sup.1 and R.sup.2, together with the carbon atom to which they are bonded, are an unsubstituted or substituted 3- to 8-membered carbo- or heterocycle;where R.sup.3 to R.sup.6 have the meanings given in the specification. The compounds are useful as herbicides and for the desiccation/defoliation of plants.
Type:
Grant
Filed:
November 22, 1994
Date of Patent:
February 11, 1997
Assignee:
BASF Aktiengesellschaft
Inventors:
Ralf Klintz, Elisabeth Heistracher, Peter Schaefer, Gerhard Hamprecht, Uwe Kardorff, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
Abstract: Novel compounds or formula (I) are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production. The compounds or the present invention are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition therefore.
Abstract: Novel cyclohexane-ylidene derivatives of formula (I) are described. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production. These compounds are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.
Abstract: The invention relates to phosphoric acid derivatives of the formula (I) ##STR1## in which R represents optionally substituted alkyl;R.sup.1 represents optionally substituted alkyl;R.sup.2 represents optionally substituted alkyl or optionally substituted alkenyl;R.sup.3 represents optionally substituted C.sub.4 -C.sub.6 -alkyl;X represents oxygen or sulphur, andY and Z represent identical or different radicals from the series comprising hydrogen, halogen, alkyl and alkoxy,which can be used as pesticides.
Type:
Grant
Filed:
December 7, 1994
Date of Patent:
January 28, 1997
Assignee:
Bayer Aktiengesellschaft
Inventors:
Fritz Maurer, Christoph Erdelen, Ulrike Wachendorff-Neumann, Jurgen Hartwig, Andreas Turberg, Norbert Mencke
Abstract: The invention relates to compounds of the formulas ##STR1## wherein R.sub.1, R.sub.2, X and Z are as described herein. These compounds are useful as antitumor agents.
Abstract: Disclosed herein are compounds referred to as "fused pyrrolocarbazoles" which possess a variety of functional activities. The disclosed compounds are represented by the following general formula: ##STR1## Methodologies for the synthetic production of fused pyrrolocarbazoles are also disclosed, as well as exemplary, uses of the compounds.
Abstract: Disclosed herein are compounds referred to as "fused pyrrolocarbazoles" which possess a variety of functional activities. The disclosed compounds are represented by the following general formula: ##STR1## Methodologies for the synthetic production of fused pyrrolocarbazoles are also disclosed, as well as exemplary uses of the compounds.
Abstract: A method of production of an ether compound from an acetal compound or a ketal compound which is excellent in conversion and selectivity and does not cause corrosion of apparatuses and a novel useful polyvinyl ether compound as lubricating oil for compression-type refrigerators, electric insulation oil and the like are disclosed. The method of production of the present invention comprises reaction of an acetal compound or a ketal compound with hydrogen in the presence of a solid catalyst having acidic property and hydrogenation ability to produce the corresponding ether compound. The polyvinyl ether compound of the present invention comprises the constituting unit expressed by the general formula: ##STR1## (characters in the general formula are the same as those described in the specification), contains none of unsaturated bond, acetal structure and aldehyde structure in the molecule and has weight average molecular weight in the range of 300 to 3000.
Abstract: 1-amino-2-cyclohexene compounds represented by the following formula (I): ##STR1## wherein the substituents are as defined in the specification, a process for preparing the compounds and their use as intermediates in the production of medicinal and agricultural agents is disclosed.
Abstract: Compounds of formula (I) ##STR1## wherein R.sub.1 represents either a hydrogen atom, or a (C.sub.1 -C.sub.4)alkyl group,X represents either a sulphur atom, an oxygen atom or a methylene group,Z.sub.1 represents either a hydrogen atom, or a 1,1-dimethylethyl group,Z.sub.2 represents either a hydrogen atom, a triphenylmethyl group, or a phenylmethoxycarbonyl group, andn=1 or 2,and addition salts to inorganic or organic acids thereof as synthetic intermediates.
Type:
Grant
Filed:
November 5, 1993
Date of Patent:
December 17, 1996
Assignee:
Synthelabo
Inventors:
Gilbert Lassalle, Thomas Purcell, Daniel Galtier, Paul H. Williams, Fr ed eric Galli
Abstract: The invention relates to new substituted benzimidazoles of the general formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 have the meanings given in the disclosure, which are useful as pest control agents, and to a process for their preparation.
Type:
Grant
Filed:
April 24, 1995
Date of Patent:
December 17, 1996
Assignee:
Bayer Aktiengesellschaft
Inventors:
Winfried Lunkenheimer, Bernd Baasner, Folker Lieb, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wilhelm Stendel, Ulrich G orgens
Abstract: Novel cytotoxic agents comprising a cell binding agent chemically linked to one or more analogue or derivative of CC-1065 are described. The therapeutic use of the cytotoxic agents is also described. These cytotoxic agents have therapeutic use because they deliver the cytotoxic drugs to a specific cell population in a targeted fashion.
Type:
Grant
Filed:
July 6, 1995
Date of Patent:
December 17, 1996
Assignee:
Immunogen Inc.
Inventors:
Ravi V. J. Chari, Viktor S. Goldmakher, Walter A. Blattler
Abstract: A process for the catalytical preparation of condensation products of formaldehyde, in which formaldehyde or a formaldehyde-forming compound is caused to undergo reaction using a catalyst which has been produced, in the presence of an auxiliary base, from a triazolium salt of formula I ##STR1## in which R.sup.1 and R.sup.3 are the same or different and stand for aliphatic groups having from 1 to 30 carbon atoms, optionally substituted aryl groups, optionally substituted aralkyl groups, and/or optionally substituted heteroaryl groups,R.sup.2 represents hydrogen, the hydroxymethylene group --CH.sub.2 OH or the hydroxy-hydroxymethylene-methylidyne group --CH(OH)(CH.sub.2 OH), andR.sup.4 denotes hydrogen, a halogen atom, a nitro or cyano group, an aliphatic group having from 1 to 30 carbon atoms, an optionally substituted aryl group, an optionally substituted aralkyl group, an optionally substituted heteroaryl group, an alkoxy group --OR.sup.5, a thioether group --SR.sup.6, an amino group --NR.sup.7 R.sup.
Type:
Grant
Filed:
December 11, 1995
Date of Patent:
December 17, 1996
Assignee:
BASF Aktiengesellschaft
Inventors:
Joaquim H. Teles, Johann-Peter Melder, Eugen Gehrer, Wolfgang Harder, Klaus Ebel, Carsten Groening, Regina Meyer
Abstract: An indoline product obtained by oxidizing at least one compound of formula (I), ##STR1## wherein R.sub.1 and R.sub.3 independently represent a hydrogen atom or a C.sub.1-4 alkyl grouping; R.sub.2 represents a hydrogen atom, a C.sub.1-4 alkyl grouping, a carboxyl grouping or C.sub.1-4 alkoxycarbonyl; R.sub.4 is a hydrogen atom, a C.sub.1-4 alkyl grouping, hydroxyl, C.sub.1-4 alkoxy, C.sub.1-10 amino or alkylamino, or halogen; R.sub.5 is a hydrogen atom, a hydroxyl grouping, C.sub.1-4 alkoxy or amino; with the proviso that at least one of the radicals R.sub.4 or R.sub.5 is a hydroxyl, alkoxy or amino grouping, and that when R.sub.5 is an amino grouping, R.sub.4 is not an alkylamino radical; R.sub.4 and R.sub.5 may also form a C.sub.1-2 alkylenedioxy ring and are in positions 5 and 6; and corresponding salts thereof. Said product may be used in cosmetics as make-up for the hair, eyebrows, eyelashes, nails, etc., and/or skin.
Type:
Grant
Filed:
December 29, 1993
Date of Patent:
December 10, 1996
Assignee:
L'Oreal
Inventors:
Alain Lagrange, Herv e Andrean, Alex Junino