Chalcogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 548/952)
-
Patent number: 7030274Abstract: The present invention relates to an improved process for the production of carbodiimide modified organic isocyanate, preferably a polymethylene polyphenylisocyanate, and most preferably diphenylmethane diisocyanate. This process includes (1) neutralizing acidic impurities in an organic isocyanate, (2) partially carbodiimidizing isocyanate groups of the neutralized organic isocyanate, and (3) terminating the carbodiimidization reaction.Type: GrantFiled: June 17, 2004Date of Patent: April 18, 2006Assignee: Bayer MaterialScience LLCInventors: James William Rosthauser, James Thomas Garrett, Jeffrey S. Bolton
-
Patent number: 6987158Abstract: Polyaddition compounds containing uretdione groups prepared by reacting uretdione polyisocyanates formed from diisocyanates having exclusively secondary- and/or tertiary-attached isocyanate groups with a molar fraction of isocyanurate structures, based on the sum of uretdione groups and isocyanurate groups, of not more than 10%, with compounds reactive towards isocyanates. The polyaddition compounds can be use as a starting component in the preparation of polyurethane plastics, in particular as crosslinkers for heat-crosslinkable powder coating materials. The compounds may be used as starting components in the preparation of moldings and shaped parts, and as starting components in the preparation of coating materials and coatings.Type: GrantFiled: July 3, 2003Date of Patent: January 17, 2006Assignee: Bayer AktiengesellschaftInventors: Hans-Josef Laas, Reinhard Halpaap, Peter Thometzek, Michael Grahl, Hans-Ulrich Meier-Westhues
-
Patent number: 6852865Abstract: Epoxides, aziridines, thiiranes, oxetanes, lactones, lactams and analogous compounds are reacted with carbon monoxide in the presence of a catalytically effective amount of catalyst having the general formula [Lewis acid]z+{[QM(CO)x]w?}y where Q is any ligand and need not be present, M is a transition metal selected from the group consisting of Groups 4, 5, 6, 7, 8, 9 and 10 of the periodic table of elements, z is the valence of the Lewis acid and ranges from 1 to 6, w is the charge of the metal carbonyl and ranges from 1 to 4 and y is a number such that w times y equals z, and x is a number such as to provide a stable anionic metal carbonyl for {[QM(CO)x]w?}y and ranges from 1 to 9 and typically from 1 to 4.Type: GrantFiled: December 2, 2002Date of Patent: February 8, 2005Assignee: Cornell Research Foundation, Inc.Inventors: Geoffrey W. Coates, Yutan D. Y. L. Getzler, Peter Wolczanski, Viswanath Mahadevan
-
Patent number: 6835727Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of Cathepsins K and L. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: August 23, 2002Date of Patent: December 28, 2004Assignees: Merck Frosst Canada & Co., Banyu Pharmaceutical Co., Ltd., Axys Pharmaceuticals, Inc.Inventors: Osamu Okamoto, Jean-Pierre Falgueyret, Renata Marcella Oballa, Petpiboon Prasit, Robert Rydzewski
-
Patent number: 6833453Abstract: Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-halopropanol.Type: GrantFiled: October 17, 2001Date of Patent: December 21, 2004Assignee: Pharmacia & Upjohn CompanyInventors: William R. Perrault, Robert C. Gadwood
-
Patent number: 6831078Abstract: A compound of formula (1) wherein R1 is aryl; and R2 is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and their use in therapy, particularly for the treatment and prophylaxis of CNS disorders such as anxiety and epilepsy.Type: GrantFiled: February 12, 2001Date of Patent: December 14, 2004Assignee: Vernalis Research LimitedInventors: David Reginald Adams, Jon Bentley, Corinna Dagmar Bodkin, Ian Anthony Cliffe, James Edward Paul Davidson, Howard Langham Mansell, Nathaniel Julius Monck, Robin Gerald Shepherd, by Joy Miriam Shepherd
-
Patent number: 6784161Abstract: The present invention relates to a method for the treatment or prevention of Flavivirus infections using nucleoside analogues in a host comprising administering a therapeutically effective amount of a compound having the formula I or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 20, 2001Date of Patent: August 31, 2004Assignee: BioChem Pharma, Inc.Inventors: Hicham Moulay Alaoui Ismaili, Yun-Xing Cheng, Jean-François Lavallée, Arshad Siddiqui, Richard Storer
-
Patent number: 6599894Abstract: There is provided compounds of formula I wherein R1, R2, Y, R3 and R4 have meanings given in the description which are useful as, or as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.Type: GrantFiled: March 16, 2000Date of Patent: July 29, 2003Assignee: AstŕaZeneca ABInventors: Tord Inghardt, Jan-Erik Nyström
-
Patent number: 6590098Abstract: The invention relates to a method of preparing an aliphatic polyisocyanate by conversion of an aliphatic diisocyanate to a polyisocyanates in the presence of a catalyst, wherein the catalyst contains a saline compound having 5 to 97.1 wt. % of a 1,2,3- and/or a 1,2,4-triazolate (calculated as C2N3, molecular weight 66) in the anion, the isocyanates thus prepared and the polyurethane paints and coatings containing them.Type: GrantFiled: May 13, 2002Date of Patent: July 8, 2003Assignee: Bayer AktiengesellschaftInventors: Frank Richter, Reinhard Halpaap, Jürgen Köcher, Hans-Josef Laas
-
Patent number: 6579995Abstract: The present invention is directed to improved processes for phosphorylation and compounds produced by the improved processes. The improved process for phosphorylating complex alcohols comprises the following steps: (a) forming an intimate mixture of one or more complex alcohols and P4O10 at a temperature below 80° C. in the absence of additional solvents; and (b) allowing the intimate mixture to continue to react for a period of time at a temperature below 80° C. until the formation of the dihydrogen form of the phosphorylated complex alcohol is substantially completed.Type: GrantFiled: November 14, 2001Date of Patent: June 17, 2003Assignee: Vital Health Sciences Pty LtdInventor: Simon Michael West
-
Patent number: 6514961Abstract: A compound of formula (1): wherein R1 is aryl; and R2, R3, R4, R5 and R6 which may be the same or different are selected from H, alkyl and aryl; pharmaceutically acceptable addition compounds thereof and the use of the compounds in therapy, particularly for CNS disorders such as anxiety and epilepsy.Type: GrantFiled: March 6, 2002Date of Patent: February 4, 2003Assignee: Vernalis Research LimitedInventors: David Reginald Adams, Ian Anthony Cliffe, Howard Langham Mansell, Nathaniel Julius Monck
-
Patent number: 6509463Abstract: The present invention relates to compounds of the general formula I wherein A is a group of the formula and Z is an O or S atom, to the further processing thereof to form novel sec-amidoalkylcarbonic acid derivatives and to those sec-amidoalkylcarbonic acid derivatives.Type: GrantFiled: August 2, 2000Date of Patent: January 21, 2003Assignee: Ugichem GmbHInventors: Ivar Ugi, Holger Bock, Thomas Lindhorst
-
Patent number: 6489503Abstract: The present invention provides a liquid methylene bis(phenylisocyanate) composition including a high concentration of methylene bis(phenylisocyanate) which has an improved storage stability. The invention further provides a method of making the liquid methylene bis(phenylisocyanate) compositions of the present invention.Type: GrantFiled: November 9, 1999Date of Patent: December 3, 2002Assignee: BASF CorporationInventors: Thirumurti Narayan, Anthony Lunato, Jon S. Speier, David D. Peters, Cynthia Loop, Filip Nevejans
-
Patent number: 6452003Abstract: The present invention provides a process, which includes: partially trimerizing isophorone diisocyanate in the presence of a catalyst having the formula: [R—NX3]⊕Y⊖ wherein R and X are butyl groups and Y− is CH3COO−; or wherein R is a benzyl group, Y− is a carboxylate anion having from 4 to 8 carbon atoms and each X is an alkylene group having from 2 to 3 carbon atoms, wherein the three alkylene groups share a common carbon atom and, together with the N atom in the formula, form a tricyclic structure, and wherein at least one alkyene group has at least one OH group in an &agr; or &bgr; &ggr; position relative to the N atom, to obtain a monomer-containing polyisocyanurate mixture. The present invention also provides a monomer-containing polyisocyanurate mixture made from the above process.Type: GrantFiled: July 6, 2001Date of Patent: September 17, 2002Assignee: Degussa AGInventors: Michael Ewald, Rainer Lomoelder, Stephan Kohlstruk
-
Patent number: 6417373Abstract: New aza azetidinium sulfate compounds are described which can be intermediates in the preparation of azabicyclobutane.Type: GrantFiled: October 19, 1998Date of Patent: July 9, 2002Assignee: The United States of America as represented by Secretary of ArmyInventors: Paritosh R. Dave, Thomas G. Archibald
-
Patent number: 6403573Abstract: The invention relates to a compound having formula (I) wherein A is an optionally unsaturated 5- or 6-membered ring, which may comprise a heteroatom selected from N,O and S and which may be substituted with oxo or (1-6C) alkyl; R1, R2 and R3 are independently H, (1-6C) alkyl, (1-6C) alkoxy,(1-6C) alkoxy-(1-6C) alkyl, carbo(1-6C) alkoxy or halogen; X is O or S; and n is 1 or 2; or a pharmaceutically acceptable salt thereof, with the exception of 3-(naphth-1-yl-oxy)-pyrrolidin and 3-(5,6,7,8-tetrahydro-napth-1-yl-oxy)-pyrrolidin. The compounds of the invention have antidepressant activity and can be used in treating or preventing serotonin-related diseases.Type: GrantFiled: May 30, 2001Date of Patent: June 11, 2002Assignee: Akzo Nobel N.V.Inventors: Dirk Leysen, Johannes Hubertus Wieringa, Christophorus Louis Eduard Broekkamp
-
Patent number: 6403574Abstract: A compound of formula (1), wherein: R1 is aryl; R2 is H, alkyl or aryl; and R3 is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and the use of the compounds in therapy, particularly for the treatment and prophylaxis of CNS disorders such as anxiety and epilepsy.Type: GrantFiled: September 17, 2001Date of Patent: June 11, 2002Assignee: Vernalis Research LimitedInventors: David Reginald Adams, Corinna Dagmar Bodkin, Ian Anthony Cliffe, Howard Langham Mansell, Nathaniel Julius Monck, Robin Gerald Shepherd
-
Patent number: 6380429Abstract: Disclosed is a process for the oxidation of sulfonamides to sulfonyl imines using chromium (IV) dioxide as the oxidant.Type: GrantFiled: September 15, 2000Date of Patent: April 30, 2002Assignee: E. I. du Pont Nemours and CompanyInventor: Eric Maurice Smith
-
Patent number: 6375926Abstract: A human leucocyte elastase (HLE) inhibitor labelled with a detector moiety where the inhibitor is synthetic and has a molecular weight of less than 2000, is useful for the diagnostic imaging of sites of inflammation of infection in vivo, for labelling leucocytes in vitro, or for radiotherapy of rthritis. The HLE inhibitor is preferably a &bgr;-lactam or an azetidinone.Type: GrantFiled: May 16, 2000Date of Patent: April 23, 2002Assignee: Amersham International PLCInventors: Karen Jane Barnes, Gary Robert Bower, Alan Michael Forster, Peter Knox, Marivi Mendizabal, Anthony Eamon Storey
-
Publication number: 20020040016Abstract: The invention relates to a compound having formula (I) wherein A is an optionally unsaturated 5- or 6-membered ring, which may comprise a heteroatom selected from N, O and S and which may be substituted with oxo or (1-6C)alkyl; R1, R2 and R3 are independently H, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkoxy-(1-6C)alkyl, carbo(1-6C)alkoxy or halogen; X is O or S; and n is 1 or 2; or a pharmaceutically acceptable salt thereof, with the exception of 3-(naphth-1-yl-oxy)-pyrrolidin and 3-(5,6,7,8-tetrahydro-napth-1-yl-oxy)-pyrrolidin. The compounds of the invention have antidepressant activity and can be used in treating or preventing serotonin-related diseases.Type: ApplicationFiled: May 30, 2001Publication date: April 4, 2002Inventors: Dirk Leysen, Johannes Hubertus Wieringa, Christophorus Louis Eduard Broekkamp
-
Patent number: 6362359Abstract: The present invention relates to compounds containing modified hydrazide groups and corresponding to formula I wherein R represents the residue obtained by removing the isocyanate groups from a monomeric polyisocyanate, a polyisocyanate adduct or an NCO prepolymer, X represents OR′ or NHR′ and R′ represents a group which is inert to isocyanate groups under the conditions used to form the compound of formula I, R″ represents a divalent, linear or branched aliphatic group containing 2 to 10 carbon atoms, provided that there are at least two carbons between the oxygen atoms wherein the aliphatic group may optionally be substituted by heteroatoms to form ether or ester groups, and n is 2 to 6.Type: GrantFiled: December 1, 2000Date of Patent: March 26, 2002Assignee: Bayer CorporationInventors: Sze-Ming Lee, Karen M. Henderson, Patricia B. Jacobs, Robert A. Sylvester, Douglas A. Wicks
-
Publication number: 20020010343Abstract: The present invention is directed to small molecule inhibitors of the IgE response to allergens which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic.Type: ApplicationFiled: June 14, 2001Publication date: January 24, 2002Inventors: Jagadish C. Sircar, Mark L. Richards, Michael G. Campbell, Michael W. Major
-
Patent number: 6297343Abstract: The present invention relates to polyaddition compounds, which are solid below 40° C. and liquid above 125° C., are prepared by the reaction of an isocyanate component containing uretdione groups with a polyol containing ester and/or carbonate groups, other than hydroxypivalic acid neopentylglycol ester, and have a) an average isocyanate functionality of 2.0 to 8.0 and a content of free isocyanate groups (calculated as NCO; molecular weight=42) of 2.1 to 6.0 wt. %, b) a content of uretdione groups (calculated as C2N2O2; molecular weight=84) of 10 to 19 wt. %, c) a content of urethane groups (calculated as —NH—CO—O; molecular weight=59) of 10 to 17 wt. % and d) a content of ester groups —CO—O (calculated as —CO—O; molecular weight=44) and/or carbonate groups —O—CO—O (calculated as —CO—O; molecular weight=44) of 1 to 17 wt. %.Type: GrantFiled: January 21, 2000Date of Patent: October 2, 2001Assignee: Bayer AktiengesellschaftInventors: Hans-Josef Laas, Ulrich Freudenberg, Reinhard Halpaap, Michael Grahl
-
Patent number: 6180745Abstract: The present invention relates to moisture-curable compositions which have a) a content of (cyclo)aliphatically-bound isocyanate groups (calculated as NCO, MW 42) of 0.2 to 22% by weight and b) a content of succinyl urea groups (calculated as —NH—CO—N—, MW 57) of 0.1 to 14% by weight, and c) an equivalent ratio of (cyclo)aliphatically-bound isocyanate groups to succinyl urea groups of 4:1 to 1:1, wherein the preceding percentages are based on resin solids content of the moisture-curable compositions. The present invention also relates to coating, adhesive or sealing compositions containing these moisture-curable compounds as the binder.Type: GrantFiled: November 8, 1999Date of Patent: January 30, 2001Assignee: Bayer CorporationInventor: Richard R. Roesler
-
Patent number: 6174879Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.Type: GrantFiled: March 17, 1999Date of Patent: January 16, 2001Assignee: University of British ColumbiaInventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
-
Patent number: 6150457Abstract: The present invention relates to compounds containing modified hydrazide groups and corresponding to formula I ##STR1## wherein R represents the residue obtained by removing the isocyanate groups from a monomeric polyisocyanate, a polyisocyanate adduct or an NCO prepolymer,X represents OR' or NHR' andR' represents a group which is inert to isocyanate groups under the conditions used to form the compound of formula I andn has a value of 2 to 6.The present invention also relates to one-component, thermoset coating compositions containing the compounds of formula I and a cross-linking component that is reactive with these compounds. Finally, the present invention relates coatings, sealants and adhesives prepared from these thermoset compositions.Type: GrantFiled: November 23, 1998Date of Patent: November 21, 2000Assignees: Bayer Corporation, Bayer AktiengesellscaftInventors: Sze-Ming Lee, Douglas A. Wicks, Eberhard Koenig, Carol L. Kinney, Karen M. Henderson
-
Patent number: 6121462Abstract: The invention is a process for the modification or substitution of aza suituted azetidines through acylative dealkylation.Type: GrantFiled: September 14, 1998Date of Patent: September 19, 2000Assignee: The United States of America as represented by the Secretary of the ArmyInventor: Dave Paritosh
-
Patent number: 6120699Abstract: The present invention provides a liquid methylene bis(phenylisocyanate) composition including a high concentration of methylene bis(phenylisocyanate) which has an improved storage stability. The invention further provides a method of making the liquid methylene bis(phenylisocyanate) compositions of the present invention.Type: GrantFiled: September 21, 1998Date of Patent: September 19, 2000Assignee: BASF CorporationInventors: Thirumurti Narayan, Anthony Lunato, Jon S. Speier, David D. Peters, Cynthia Loop, Filip Nevejans
-
Patent number: 6107493Abstract: The invention relates to a process for the preparation of cyclic perfluoroalkanebis(sulfonyl)imides and salts thereof.The new compound lithium cyclo-difluoromethanebis(sulfonyl)imide is outstandingly suitable as a conductive salt in non-aqueous electrolytes for lithium secondary batteries.Type: GrantFiled: November 12, 1998Date of Patent: August 22, 2000Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Ludwig Pohl, Volker Hilarius, Peter Sartori, Ralf Jueschke
-
Patent number: 6087379Abstract: A cyclic amine derivative represented by the following formula: ##STR1## wherein R.sup.1 represents a substituted or unsubstituted phenyl group, R.sup.2 represents a substituted of unsubstituted C.sub.1 -C.sub.8 aliphatic acyl group, a substituted or unsubstituted benzoyl group or a C.sub.1 -C.sub.4 alkoxycarbonyl group, and R.sup.3 represents a substituted 3 to 7 membered saturated cyclic amino group which may form a fused ring; or pharmaceutically acceptable salts thereof. The compounds and salts have excellent platelet aggregation inhibitory action. They are useful for the treatment and prevention of such diseases as embolism, thrombosis or arteriosclerosis and for the preparation of pharmaceutical compositions for such uses.Type: GrantFiled: February 25, 1999Date of Patent: July 11, 2000Assignees: Sankyo Company, Limited, Ube Industries, Ltd.Inventors: Fumitoshi Asai, Atsuhiro Sugidachi, Toshihiko Ikeda, Hiroyuki Koike, Teruhiko Inoue, Katsunori Takata, Ryo Iwamura, Jun-ichiro Kita, Kenji Yoneda
-
Patent number: 6063935Abstract: An azetidine derivative is provided which includes 3,3-dihydroxyazetidine represented by Chemical Formula (I) or a salt thereof: ##STR1## A composition containing the azetidine derivative, and a process for producing the azetidine derivative are also provided. The azetidine derivative is a novel compound, and is useful for promoting bifidobacterium divisional multiplication.Type: GrantFiled: February 9, 1999Date of Patent: May 16, 2000Assignee: Toa Pharmaceutical Co., Ltd.Inventors: Takashi Masuda, Taketoshi Arai, Kenji Shiojima, Masanori Sasatsu, Kazuo Masuda, Hajime Hamashima, Genichiro Seo
-
Patent number: 5986092Abstract: The invention relates to a process for the preparation of N-substituted lactams by reaction of a lactam, which is unsubstituted on the nitrogen, with an organic halide in the presence of at least one solid-liquid phase transfer catalyst, such as a quaternary ammonium salt, and of at least one solid inorganic base, such as an alkali metal hydroxide, and in the absence of solvent. By this process, N-substituted lactams are obtained with good yields and high purity. The absence of solvent makes possible a considerable gain in productivity and an improvement in safety and in regard for the environment.Type: GrantFiled: July 8, 1997Date of Patent: November 16, 1999Assignee: SNPEInventors: Michel Denarie, Khann Ly Kok
-
Patent number: 5965565Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: December 11, 1997Date of Patent: October 12, 1999Assignee: Merck & Co., Inc.Inventors: Meng H. Chen, Zhijian Lu, Ravi Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang, Mu Tsu Wu
-
Patent number: 5961878Abstract: The invention relates to non-crystallising, amine-blocked polyisocyanates, to the preparation thereof and to their in one-component polyurethane stoving compositions, in particular for coil-coating applications.Type: GrantFiled: September 2, 1998Date of Patent: October 5, 1999Assignee: Bayer AktiengesellschaftInventors: Eberhard Konig, Karl-Ludwig Noble, Christian Fussel
-
Patent number: 5952354Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholesterol and thus can lower serum cholesterol levels. Compounds of the formula: ##STR1## where Z is ##STR2## or --Ar.sup.1 --(CR.dbd.CR).sub.1-3 --Ar.sup.2, --AR.sup.1 --NR.sup.7 --AR.sup.2 and A is a linking group inhibit the enzymes CEH and/or ACAT (in vitro) and inhibit absorption of cholesterol.Type: GrantFiled: July 21, 1993Date of Patent: September 14, 1999Assignee: American Home Products CorporationInventors: Thomas Joseph Commons, Donald Peter Strike, Christa Marie LaClair
-
Patent number: 5945531Abstract: A polyisocyanate composition, comprising:A) from 55 to 87% by weight of a polyisocyanate which contains uretdione groups;B) from 10 to 30% by weight of blocking agent,C) from 3 to 30% by weight of polyol having more than two hydroxyl groups and/or chain extender having more than two hydroxyl groups, wherein the polyisocyanate contains more than two terminal, partially or fully blocked isocyanate groups and has a molecular weight of from 1000 to 10,000.Type: GrantFiled: December 8, 1997Date of Patent: August 31, 1999Assignee: Huels AktiengesellschaftInventor: Rainer Gras
-
Patent number: 5912314Abstract: A Polyaddition product, containing uretdione groups, which is obtainable by reaction of (A) a diisocyanate mixture which contains uretdione groups and comprises (1) at least 40 mol % to not more than 80 mol % of isophorone diisocyanate containing uretdione groups and (2) not more than 60 mol % and not less than 20 mol % of hexamethylene diisocyanate containing uretdione groups, with (B) a disecondary diamine, in an NCO/NH ratio of 1:0.5 to 1:0.9 at room temperature to 60.degree. C. in a solvent which is inert towards isocyanates.Type: GrantFiled: March 17, 1997Date of Patent: June 15, 1999Assignee: Huels AktiengesellschaftInventor: Elmar Wolf
-
Patent number: 5883093Abstract: The present invention relates to antimicrobial phenyloxazolidinone compounds having a pyrrolidinyl or azetidinyl moiety.Type: GrantFiled: April 23, 1997Date of Patent: March 16, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Douglas K. Hutchinson, Steven J. Brickner, Michael R. Barbachyn, Mikio Taniguchi, Kiyotaka Munesada, Hiroyoshi Yamada
-
Patent number: 5869024Abstract: In accordance with the present invention a novel method and composition for using nonionic contrast media to reduce the risk of clot formation in a diagnostic procedure is disclosed. Novel compositions for such method are also disclosed. The present method comprises employing a triiodinated phenyl contrast agent having a heterocyclic group or a dimeric triiodinated phenyl contrast agent having one or more heterocyclic groups.Type: GrantFiled: June 5, 1992Date of Patent: February 9, 1999Assignee: Bracco International B.V.Inventors: Ramachandran S. Ranganathan, Michael F. Tweedle, Paul W. Wedeking
-
Patent number: 5861429Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is methyl, ethyl, isopropyl or sec-butyl; X is carbonyl or methylene; Z is .dbd.C.dbd.(R.sup.2).sub.2 or .dbd.C.dbd.(CH.sub.2).sub.m, in which R.sup.2 is alkyl, and m is integer of from 2 to 5); n is 0 or 1; R.sup.3 is nitro, amino, alkylamino, dialkylamino, alkoxy, alkoxyalkoxy, or a group (iii), (iv), (v), (vi), (vii), (viii) or (ix): ##STR2## , wherein: R.sup.4 represents: alkyl; substituted alkyl; cycloalkyl having from 3 to 6 carbon atoms; substituted cycloalkyl; alkenyl; alkynyl; carbocyclic aryl; or heterocyclic; R.sup.5 is hydrogen atom or alkyl; R.sup.6 represents: hydrogen; alkyl; or cycloalkyl; R.sup.7 represents: alkyl; cycloalkyl; carbocyclic aryl; or aralkyl; or R.sup.6 and R.sup.7, together with the nitrogen atom to which they are attached, are fuised to form heterocyclic ring; Y is oxygen or sulfur; r is 1, 2 or 3; Q is methylene or carbonyl; R.sup.8 is: alkyl or carbocyclic aryl; R.sup.Type: GrantFiled: September 30, 1996Date of Patent: January 19, 1999Assignee: Sankyo Company, LimitedInventors: Kazuo Sato, Akio Saito, Toshimitsu Toyama
-
Patent number: 5750629Abstract: The present invention relates to a process for preparing pure bis(isocyanatoalkyl)monouretdiones corresponding to formula (I) ##STR1## wherein R represents identical or different, linear or branched alkyl groups having 4 to 9 carbon atoms,by oligomerizing at least a portion of the isocyanate groups of aliphatic diisocyanates in the presence of catalysts which accelerate the dimerization of isocyanate groups, terminating the reaction at the desired degree of oligomerization, removing unreacted excess diisocyanate by extraction or thin film distillation to obtain a distillation residue, subjecting the distillation residue to thin film distillation at a temperature of 160.degree. to 220.degree. C. and a pressure of 0.01 to 1.0 mbar and obtaining bis(isocyanato-alkyl)monouretdiones corresponding to formula (I) as the distillate.Type: GrantFiled: January 23, 1997Date of Patent: May 12, 1998Assignee: Bayer AktiengesellschaftInventors: Hans-Josef Laas, Reinhard Halpaap, Josef Pedain, Klaus Konig
-
Patent number: 5750727Abstract: A polyisocyanate composition, comprising:A) from 55 to 87% by weight of a polyisocyanate which contains uretdione groups;B) from 10 to 30% by weight of blocking agent,C) from 3 to 30% by weight of polyol having more than two hydroxyl groups and/or chain extender having more than two hydroxyl groups, wherein the polyisocyanate contains more than two terminal, partially or fully blocked isocyanate groups and has a molecular weight of from 1000 to 10,000.Type: GrantFiled: February 12, 1996Date of Patent: May 12, 1998Assignee: Huels AktiengesellschaftInventor: Rainer Gras
-
Patent number: 5705522Abstract: A new family of compounds having anti-inflammatory, anti-viral, and brocho-dilating activity having the following linear and cyclic formulas: ##STR1## and compositions of these, which alone, and in combination with reverse transcriptase inhibitors thereby resulting in an additive or synergistic effect, are useful in inhibiting or suppressing viruses including those exhibiting retroviral replication, or in treating viruses including a retrovirus such as HIV in a human cell population and methods of using these compositions, compounds, and salts thereof.Type: GrantFiled: February 13, 1996Date of Patent: January 6, 1998Assignee: Compagnie de Developpement Aguettant S.A.Inventors: Farid Hamedi-Sangsari, Fabienne Nugier, Thierry Vallet, Jacques Grange, Jorge Vila
-
Patent number: 5696256Type: GrantFiled: May 12, 1995Date of Patent: December 9, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Yasuyuki Kando, Hideki Uneme, Isao Minamida
-
Patent number: 5608102Abstract: This invention relates to a method for preparing .beta.-phenylisoserine and analogues thereof having general formula (I) ##STR1## from an aromatic aldehyde and an .alpha.-methylarylamine-S, and through a lactam of general formula (II) as described herein. The acids of general formula (I) (R.dbd.H) may be used to prepare taxane derivatives having remarkable antitumoral and antileukaemic activity.Type: GrantFiled: September 26, 1994Date of Patent: March 4, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Jean-Dominique Bourzat, Alain Commer.cedilla.on
-
Patent number: 5563168Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: June 16, 1995Date of Patent: October 8, 1996Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
-
Patent number: 5536723Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.Type: GrantFiled: October 6, 1994Date of Patent: July 16, 1996Assignee: Brigham & Women's HospitalInventors: Joseph Loscalzo, John Cooke
-
Patent number: 5527926Abstract: In accordance with the present invention a novel method and composition for using nonionic contrast media to reduce the risk of clot formation in a diagnostic procedure is disclosed. Novel compositions for such method are also disclosed. The present method comprises employing a triiodinated phenyl contrast agent having a heterocyclic group or a dimeric triiodinated phenyl contrast agent having one or more heterocyclic groups.Type: GrantFiled: June 6, 1995Date of Patent: June 18, 1996Assignee: Bracco International B.V.Inventors: Ramachandran S. Ranganathan, Radhakrishna K. Pillai
-
Patent number: 5512560Abstract: HIV protease inhibitors containing hydroxypyrrolidine or hydroxypiperidine with one or more basic amines are disclosed.Type: GrantFiled: March 29, 1994Date of Patent: April 30, 1996Assignee: Merck & Co., Inc.Inventors: Byeong M. Kim, Joseph P. Vacca
-
Patent number: 5508372Abstract: The present invention relates to a process for the production of storage stable prepolymers containing free isocyanate groups by reactinga) an organic polyisocyanate component having (cyclo)aliphatically bound isocyanate groups and a maximum functionality of 4.5 withb) one or more hydroxy-functional polyacrylate resins having a content of alcoholic hydroxy groups of 0.05 to 7% by weight at an equivalent ratio of isocyanate groups of component a) to hydroxyl groups of component b) of 3:1 to 40:1, wherein components a) and b) are selected to provide a value B of at most 4 when calculated in accordance with the formula: ##EQU1## wherein F.sub.1 and F.sub.2 represent the NCO and OH functionalities of components a) and b), F.sub.1 representing the component with the lower functionality when the components differ in functionality andval.sub.A /val.sub.I represents the OH/NCO equivalent ratio of components a) and b).Type: GrantFiled: April 19, 1993Date of Patent: April 16, 1996Assignee: Bayer AktiengesellschaftInventors: Martin Brahm, Lutz Schmalstieg, Werner Kubitza, Wieland Hovestadt, Josef Pedain