Alicyclic Ring Containing Patents (Class 568/329)
  • Patent number: 6340774
    Abstract: This invention relates generally to non-steroidal estrogen-receptor (ER) antagonists that are useful as therapeutics in the treatment of advanced stage breast cancer. More particularly, this invention relates to the cloning and heterologous expression of genes encoding ER antagonists. This invention also relates to the use of such expression to overproduce the ER antagonist and analogs thereof.
    Type: Grant
    Filed: January 31, 2001
    Date of Patent: January 22, 2002
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Chaitan Khosla, Zhihao Hu, Thomas Marti
  • Publication number: 20020007085
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1
    Type: Application
    Filed: December 5, 2000
    Publication date: January 17, 2002
    Applicant: Merrell Pharmaceuticals Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Patent number: 6313351
    Abstract: The process for producing alicyclic monoketones (hydroxyphenylcyclohexanone derivatives) according to the present invention comprises hydrogenating substituted bisphenols such as bisphenol A in a solvent in the presence of a palladium/alkali metal catalyst in which palladium and an alkali metal are both supported on a carrier to obtain alicyclic monoketones such as 2-(4-oxocyclohexyl)-2-(4-hydroxyphenyl)propane. The process for producing alicyclic diketones according to the present invention comprises hydrogenating substituted bisphenols such as bisphenol A in a solvent in the presence of a palladium/alkali metal catalyst in which palladium and an alkali metal are both supported on a carrier to obtain alicyclic diketones such as 2,2-bis(4-oxocyclohexyl)propane and 4,4′-bicyclohexanone.
    Type: Grant
    Filed: September 2, 1999
    Date of Patent: November 6, 2001
    Assignee: Honshu Chemical Industry Co., Ltd.
    Inventors: Norimoto Kiya, Shinsaku Kawasaki, Kenji Ekawa, Kenji Sugiyama, Toyokazu Kitaura
  • Publication number: 20010021791
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1
    Type: Application
    Filed: December 8, 2000
    Publication date: September 13, 2001
    Applicant: Merrell Pharmaceuticals Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hax, Duane E. Rudisill, Gianbattista Panzone
  • Patent number: 6281250
    Abstract: The present invention is directed to retinyl ethers, derivatives and analogues and their use in inhibiting breast carcinogenesis or breast cancer cell growth.
    Type: Grant
    Filed: April 12, 1999
    Date of Patent: August 28, 2001
    Assignee: Southern Research Institute
    Inventor: Y. Fulmer Shealy
  • Patent number: 6258854
    Abstract: The invention discloses ketones of formula I: wherein, Y is an optionally substituted alkyl, cycloalkyl, or cycloalkylalkyl, wherein each alkyl group is straight or branched and each alkyl and cycloalkyl group is saturated or unsaturated; R1 is hydrogen or a C1-6 alkyl group that is substituted, saturated or unsaturated, straight or branched; A is a chromophoric substituted aromatic ring or ring system; n is an integer; and with the proviso that formula I is not 2-ethoxy-1-phenyl-ethanone. These compositions are useful for the delivery of organoleptic compounds, especially of flavors, fragrances, masking agents and antimicrobial compounds.
    Type: Grant
    Filed: September 1, 1999
    Date of Patent: July 10, 2001
    Assignee: Givaudan Roure ( International ) SA
    Inventors: Denise Anderson, Georg Fráter
  • Patent number: 6251833
    Abstract: The present invention relates to novel 2-aryl-3-hydroxy-&Dgr;2-cyclopentene-1-one derivatives of the formula (I) in which A, B, D1, D2, G, W, X, Y and Z are each as defined in the description, to processes for their preparation and to their use as herbicides and pesticides.
    Type: Grant
    Filed: August 31, 1999
    Date of Patent: June 26, 2001
    Inventors: Christoph Erdelen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Norbert Mencke, Andreas Turberg
  • Publication number: 20010003784
    Abstract: A process for preparing ketones by so-called “crossed aldol condensation” of a ketone with an aldehyde in the presence of a catalyst system consisting of approximately equimolar amounts of a secondary amine and of a carboxylic acid containing at least 2 C atoms, to form an &agr;,&bgr;-unsaturated ketone, and, where appropriate, subsequent catalytic hydrogenation.
    Type: Application
    Filed: December 5, 2000
    Publication date: June 14, 2001
    Inventors: Andreas Kramer, Christian Knoll, Johann-Peter Melder, Wolfgang Siegel, Gerd Kaibel
  • Patent number: 6242641
    Abstract: The present invention relates to compounds selected from formula I wherein R1, R2, R3 and R4 are the same or different and represent hydrogen, C1, to C6-alkyl, C5 to C6-cycloalkyl, phenyl and halogen, m and n are the same or different and represent the 2, 3, 4 or 5, X, A and B represent carbon and Y1, Y2, Z1 and Z2 are the same or different and represent hydrogen, hydroxyl (OH), amino (NH2), isocyanato (NCO) or 4-hydroxyphenyl.
    Type: Grant
    Filed: March 22, 1999
    Date of Patent: June 5, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Manfred Jautelat, Carl Casser, Hanns-Peter Müller, Manfred Hajek
  • Patent number: 6239135
    Abstract: A series of aryl piperazine compounds of the formula: or the pharmaceutically acceptable salts thereof, are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.
    Type: Grant
    Filed: December 9, 1998
    Date of Patent: May 29, 2001
    Assignee: Eli Lilly and Company
    Inventors: Daniel Timothy Kohlman, Yao-Chang Xu
  • Patent number: 6207852
    Abstract: The present invention relates to smooth muscle spasmolytic agents, pharmaceutical compositions containing them and method of using said compounds and compositions for the treatment of urinary incontinence, gastric hyperactivity (ex. Irritable Bowel Syndrome) and other smooth muscle contractile conditions. More particularly, the present invention relates to certain substituted esters, amides and ketones having smooth muscle relaxing properties while avoiding, on administration to a mammal, adverse side effects such as prominent antimuscarinic, arrhythmogenic and cardiodepressive effects.
    Type: Grant
    Filed: December 23, 1998
    Date of Patent: March 27, 2001
    Assignee: Bridge Pharma, Inc.
    Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen
  • Publication number: 20010000038
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1
    Type: Application
    Filed: December 1, 2000
    Publication date: March 15, 2001
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Patent number: 6172118
    Abstract: This invention relates to ketones, alcohols and amines represented by the likes of of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylethynylcyclobutan-1-one. They are useful as PDE 4 antagonists.
    Type: Grant
    Filed: April 8, 1999
    Date of Patent: January 9, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Cornelia J. Forster
  • Patent number: 6159988
    Abstract: Compounds of formula I, ##STR1## and the physiologically tolerable salts thereof, wherein the substituents R.sub.1 -R.sub.4 have the meanings given in the specifications and show an activity against inflammatory conditions.
    Type: Grant
    Filed: June 29, 1998
    Date of Patent: December 12, 2000
    Assignee: Hoeschst Aktiengesellschaft
    Inventors: Ramachandra Ganapati Naik, Vilas Narayan Mumbaikar, Ravishankar Vasumathy, Aftab Dawoodbhai Lakdawala, Mandakini Bipin Alreja, Bansi Lal, Jurgen Blumbach, Klaus Ulrich Weithmann, Robert Ryder Bartlett, Kalpana Sanjay Joshi, Swati Bal-Tembe, Sadagopan Raghavan
  • Patent number: 6150374
    Abstract: The invention relates to novel substituted cycloalkenes of the formula (I), ##STR1## to a plurality of processes for their preparation, and to novel intermediates and a plurality of processes for their preparation.
    Type: Grant
    Filed: September 29, 1997
    Date of Patent: November 21, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Gayer, Peter Gerdes, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
  • Patent number: 6118017
    Abstract: This invention relates to ketones, alcohols and amines and acids represented by the likes of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylcyanoclobutan-1-one. They are useful as PDE 4 antngionists.
    Type: Grant
    Filed: April 8, 1999
    Date of Patent: September 12, 2000
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Cornelia J. Forster
  • Patent number: 6086857
    Abstract: The invention relates to cinnamylidenecamphor derivatives of the formula (1) ##STR1## where the diene system is in the Z,Z, Z,E, E,Z or E,E configuration and R.sup.1 is H, CH.sub.3,R.sup.2 is C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, NR.sup.3 H, NR.sup.3.sub.2,R.sup.3 is C.sub.1 -C.sub.4 -alkyl,R.sup.4 is H, C.sub.1 -C.sub.6 -alkyl,n is 1, 2,and to its use.
    Type: Grant
    Filed: September 3, 1998
    Date of Patent: July 11, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Christof Kandzia, Horst Westenfelder, Volker Schehlmann
  • Patent number: 6040274
    Abstract: 2- Aroylcyclohexanediones I ##STR1## where X, Y=O or S;Ar=phenyl or heteroaryl in each case having 1-4 substituents: halogen, cyano, nitro, --N.dbd.N--Ph, C.sub.1 -C.sub.4 -alkoxycarbonyl, --N(R.sup.9)--COR.sup.10, --N(R.sup.9)--SO.sub.2 --R.sup.11, --SO.sub.2 --N(R.sup.9)R.sup.10, --S(O).sub.m --R.sup.8 or opt. subst. C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl or C.sub.1 -C.sub.4 -haloalkoxy;two adjacent C atoms of the phenyl or heteroaryl ring can also be bridged by means of a chain --C(R.sup.12).dbd.C(R.sup.13)--C(R.sup.14).dbd.C(R.sup.15)--, --Z.sup.1 --C(R.sup.12).dbd.N--, --Z.sup.1 --N.dbd.C(R.sup.12)--, --Z.sub.1 --C(R.sup.12).dbd.C(R.sup.13)--, --Z.sup.1 --C(R.sup.12).dbd.C(R.sup.13)--C(R.sup.14,R.sup.15)--, --Z.sup.1 --C (R.sup.12,R.sup.13)--C(R.sup.14,R.sup.15)--, --Z.sup.1 --C(R.sup.12,R.sup.13)--C(R.sup.14 R.sup.15)--Z.sup.2 --, --C(R.sup.12,R.sup.13)--Z.sup.1 --C(R.sup.14,R.sup.15)--C(R.sup.16,R.sup.17)--, --Z.sup.1 --N(R.sup.20)--Z.sup.2 --, --Z.sup.1 --Z.sup.
    Type: Grant
    Filed: March 18, 1997
    Date of Patent: March 21, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Jurgen Kast, Marcus Vossen, Wolfgang von Deyn, Stefan Engel, Regina Luise Hill, Uwe Kardorff, Martina Otten, Peter Plath, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
  • Patent number: 6017470
    Abstract: This invention provides a compound having the structure: ##STR1## wherein rings A and B represent independent electron accepting ring systems and wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are the same or different and are H, substituted or unsubstituted, saturated or unsaturated alkyl, alkenyl, cycloalkyl, aryl, or arylalkyl, --SR, --NRR', --OR, --OC(O)R, SC(O)R, --SCR, wherein R and R' are independently substituted or unsubstituted, saturated or unsaturated alkyl, alkenyl, cycloalkyl, aryl, or arylalkyl.This invention also provides thin films comprising a compound having the above structure or suitable derivatives thereof.This invention further provides liquid crystal display devices and non-linear optical devises comprising a compound having the above structure or a suitable derivative thereof.
    Type: Grant
    Filed: April 12, 1996
    Date of Patent: January 25, 2000
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Thomas J. Katz, Colin P. Nuckolls
  • Patent number: 5932765
    Abstract: The present invention relates to the compounds of formula: ##STR1## in which R.sub.1, R.sub.2, R.sub.3, E, A, X, Z, p and n are as defined herein. These compounds are aldose reductase inhibitors.
    Type: Grant
    Filed: October 22, 1997
    Date of Patent: August 3, 1999
    Assignee: Merck Patent Gesellschaft Mit
    Inventors: Claude Lardy, Jaques Barbanton, Herve Dumas, Francois Collonges, Phillippe Durbin
  • Patent number: 5908944
    Abstract: This invention describes a new methylation or ethylation agent containing trimethyl aluminum or dimethyl zinc or triethyl aluminum as methyl or ethyl source, which additionally contains catalytic amounts of one or more copper(I) and/or copper(II) compounds as well as a process for the 1,4-addition of a methyl or ethyl group to an .alpha.,.beta.-unsaturated or an .alpha.,.beta.-double unsaturated ketone or an .alpha.,.beta.-unsaturated aldehyde using the agent according to the invention.By using only catalytic amounts of copper and a CKW (chlorinatedhydrocarbon)-free reaction medium, the new methylation/ethylation agent/process is distinguished by its environmental compatibility and it is, for example, suitable for the production of initial products for the synthesis of biologically effective compounds.
    Type: Grant
    Filed: September 30, 1994
    Date of Patent: June 1, 1999
    Assignee: Schering Aktiengesellschaft
    Inventors: Jurgen Westermann, Klaus Nickisch
  • Patent number: 5892098
    Abstract: This invention relates to derivatives of 3,3-(disubstituted)cyclohexan-1-one monomers and related compounds which are useful for treating allergic and inflammatory diseases.
    Type: Grant
    Filed: April 15, 1997
    Date of Patent: April 6, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
  • Patent number: 5840661
    Abstract: The present invention relates to novel 2-aryl-3-hydroxy-cyclopent-2-en-1-one derivatives of the formula (I) ##STR1## in which X represents halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Y represents hydrogen, halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Z represents halogen, nitro, cyano, alkyl, alkoxy or halogenoalkoxy andA, B, D.sup.1, D.sup.2, G and n have the meaning given in the description,several processes for their preparation and their use as compositions for controlling pests and as herbicides.
    Type: Grant
    Filed: December 31, 1996
    Date of Patent: November 24, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Jacques Dumas, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Andreas Turberg, Norbert Mencke
  • Patent number: 5773614
    Abstract: (1R,trans) Diprotected 3-methylene-1,2-cyclopropanedimethanol is oxidized to an optically active diol ##STR1## which is then cyclized to an orthoester ##STR2## This orthoester is then treated with a Lewis acid catalyst to give the cyclobutanone ##STR3## which is useful as an intermediate in the preparation of the antiviral agent ?1R-(1.alpha.,2.beta.,3.alpha.)!-2-amino-9-?2,3-bis(hydroxymethyl)cyclobut yl!-1,9-dihydro-6H-purin-6-one.
    Type: Grant
    Filed: September 13, 1996
    Date of Patent: June 30, 1998
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller
  • Patent number: 5767288
    Abstract: The invention relates to dithiane adducts of substituted benzoins and substituted benzoins derived therefrom each of which are useful as protecting groups, photolabile linkers, and fluorescent probes.
    Type: Grant
    Filed: January 5, 1996
    Date of Patent: June 16, 1998
    Assignee: California Institute of Technology
    Inventors: Ronald S. Rock, Michael H. B. Stowell, Sunney I. Chan
  • Patent number: 5741476
    Abstract: The invention relates to polyhydric phenol compounds of the general formula ##STR1## wherein R is a hydrogen atom or a saccharide moiety;A and B are hydrogen atoms or form together a C--C bond;R.sub.1 is a hydroxy group and R.sub.2 is a hydrogen atom, orR.sub.1 and R.sub.2 form together an oxygen atom;Z is a hydroxy group, an amino group, a carboxy group or a N-(carboxymethyl)carbamoyl group;X* is a radioactive halogen isotope; andm and n are 0 or 1, with the proviso, that m is 1 if n is 0, and that m is 0 if n is 1.The radiolabelled phenol compounds can be used for diagnosis and therapy.
    Type: Grant
    Filed: June 20, 1995
    Date of Patent: April 21, 1998
    Assignee: Mallinckrodt Medical, Inc.
    Inventor: John Janine Rene Mertens
  • Patent number: 5739376
    Abstract: Fullerene derivatives, methods of preparing the same and methods of using the same, wherein the fullerene derivatives are of the formula I ##STR1##
    Type: Grant
    Filed: October 20, 1995
    Date of Patent: April 14, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Carsten Bingel
  • Patent number: 5728889
    Abstract: A process for preparing a compound of formula (I), where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently hydrogen or C.sub.1-6 alkyl; R.sup.7 is halogen, cyano, NO.sub.2, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.1-4 alkoxy or RaS in which Ra is C.sub.1-4 alkyl; R.sup.8, R.sup.9 and R.sup.10 independently are hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, CN, NO.sub.2, phenoxy or substituted phenoxy; R.sub.b S(O)n Om in which m is 0 or 1, n is 0, 1 or 2 and Rb is C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, phenyl or benzyl, NHCOR.sub.c in which c is C.sub.1-4 alkyl, NRdRe in which Rd and Re independently are hydrogen or C.sub.1-4 alkyl; RfC(O)-- in which Rf is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl or C.sub.1-4 alkoxy; SO.sub.2 NRgRh in which Rg and Rh independently are hydrogen or C.sub.1-4 alkyl; or any two of R.sup.8, R.sup.9 and R.sup.
    Type: Grant
    Filed: June 24, 1997
    Date of Patent: March 17, 1998
    Assignee: Zeneca Limited
    Inventors: Howard Rawlinson, Jonathan William Wiffen, Stephen Martin Brown
  • Patent number: 5639918
    Abstract: (Benzylidene)-azolylmethylcycloalkane or -alkene of formula ##STR1## in which: A and A.sub.1 are hydrocarbon chains of 1 to 3 carbon atoms,R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are hydrocarbon radicals,X is halogen,Y is H or halogen,n=1, 2 or 3,W is --CH.dbd. or --N.dbd..Use as a fungicide.
    Type: Grant
    Filed: September 26, 1994
    Date of Patent: June 17, 1997
    Assignee: Rhone-Poulenc Agrochimie
    Inventors: Jean Hutt, Jacques Mugnier, Alfred Greiner, Regis Pepin
  • Patent number: 5633381
    Abstract: This invention relates to novel (Z,Z), (Z,E) and (E,Z) olefin isomers of substituted benzylidene cycloketones and their pharmaceutically acceptable salts. The compounds of the invention are potent factor Xa inhibitors thereby acting as anticoagulants useful in a number of thrombotic disease states. Pharmaceutical compositions are proposed for the compounds.
    Type: Grant
    Filed: July 5, 1994
    Date of Patent: May 27, 1997
    Assignee: Berlex Laboratories, Inc.
    Inventors: Jerry L. Dallas, William J. Guilford, Sunil K. Koovakkat, Michael M. Morrissey, Kenneth J. Shaw
  • Patent number: 5476876
    Abstract: The subject invention relates to compounds having the structure: ##STR1## wherein (a) X is selected from hydroxy, C.sub.1 to about C.sub.2 alkanoxy, thiol, C.sub.1 to about C.sub.2 alkanylthiol, and halo;(b) R and R' are each independently selected from C.sub.1 to about C.sub.3 straight or branched alkanyl, and C.sub.3 to about C.sub.4 cyclic alkanyl; or R and R' are bonded together to form a C.sub.3 to about C.sub.6 cyclic alkanyl ring, or a C.sub.3 to about C.sub.5 cyclic heteroalkanyl ring having one oxygen or sulfur atom in the ring, the heteroatom not being bonded to the carbon to which X is bonded; and R and R', or the ring formed by them when bonded together, are each, independently, unsubstituted or monosubstituted with a substituent selected from halo, hydroxy, thiol, C.sub.1 to about C.sub.2 alkanoxy, and C.sub.1 to about C.sub.2 alkanylthiol.The subject invention also relates to the pharmaceutical compositions comprising the above compounds, and methods of treating inflammation using the compounds.
    Type: Grant
    Filed: May 24, 1994
    Date of Patent: December 19, 1995
    Assignee: The Procter & Gamble Company
    Inventors: Stanislaw Pikul, Joseph A. Miller, John M. Janusz, Theresa Rosario-Jansen
  • Patent number: 5466721
    Abstract: Provided are compounds having the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are independently selected from the group consisting of a hydrogen atom, an aliphatic group, a hetero-aliphatic group, an aromatic group, and a heterocyclic group, provided that R.sup.1 and R.sup.2 may together form a divalent radical selected from the group consisting of an aliphatic radical and hetero-aliphatic group;each R.sup.3 is independently selected from the group consisting of an aliphatic group, a hetero-aliphatic group, an aromatic group, and a heterocyclic group;R.sup.4 is selected from the group consisting of an aliphatic group, a hetero-aliphatic group, an aromatic group, and a heterocyclic group; andn is an integer from 0 to 5.Also provided are polymerizable compositions containing such compounds and a method of coating a substrate which uses such polymerizable compositions.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: November 14, 1995
    Assignee: Henkel Corporation
    Inventor: Paul E. Share
  • Patent number: 5393917
    Abstract: A process for isolating and purifying oxadimethacrylics of the general formula ICH.sub.2 .dbd.C(A)CH.sub.2 --O--CH.sub.2 C(B).dbd.CH.sub.2 Iwhere A and B are selected from the group consisting of --COOR.sup.1, --COR.sup.1, --CONR.sup.2 R.sup.3 and --CN and R.sup.1, R.sup.2 and R.sup.3 are each defined as follows:R.sup.1 is hydrogen, alkyl, substituted or unsubstituted cycloalkyl or cycloalkylalkyl, hydroxyalkyl, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, substituted or unsubstituted aryl or arylalkyl,R.sup.2 and R.sup.3 are each hydrogen, alkyl, substituted or substituted cycloalkyl or cycloalkylalkyl, substituted or unsubstituted aryl or arylalkyl,comprises precipitating or crystallizing them from their solutions that contain at least one liquid hydrocarbon compound.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: February 28, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Siegmund Besecke, Andreas Deckers, Harald Lauke
  • Patent number: 5387593
    Abstract: Novel piperazinyl- and piperidinyl-cyclohexanols of the following formula are useful as anxiolytic agents and have other psychotropic properties ##STR1##
    Type: Grant
    Filed: February 17, 1994
    Date of Patent: February 7, 1995
    Assignee: Briston-Myers Squibb
    Inventors: Ronald J. Mattson, John D. Catt
  • Patent number: 5384331
    Abstract: 5,6-Dehydronorketamine and derivatives retaining the .alpha.,.beta.-unsaturated carbonyl are disclosed. These end other Michael or Michael-type acceptors and adducts are shown to influence the replication, differentiation or maturation of blood cells, especially platelet progenitor cells. Accordingly, these compounds are used for treatment of thrombocytopenia.
    Type: Grant
    Filed: May 28, 1993
    Date of Patent: January 24, 1995
    Assignee: Genentech, Inc.
    Inventors: Timothy P. Kogan, Todd C. Somers
  • Patent number: 5380900
    Abstract: Disclosed herein is an .alpha.-methylene-cyclopentanone derivative represented by the formula [I] below which is useful as an intermediate for pharmaceuticals and insecticides, especially prostaglandins. Also disclosed herein is a process for producing the derivative advantageously on an industrial scale. ##STR1## where X denotes (.alpha.-OZ, .beta.-H) or (.alpha.-H, .beta.-OZ), with Z representing a protecting group for the hydroxyl group; U denotes (.alpha.-H, .beta.-R.sup.1) or (.beta.-R.sup.1, .alpha.-H); R.sup.1 denotes ##STR2## where R.sup.2 denotes a protected hydroxyl group, a substituted or unsubstituted C.sub.1-15 alkyl group, a substituted or unsubstituted C.sub.2-15 alkenyl group, a substituted or unsubstituted C.sub.2-15 alkynyl group, or a substituted or unsubstituted C.sub.6-15 aryl group; Z' denotes a protecting group for the hydroxyl group; and k is 0 or 1).
    Type: Grant
    Filed: February 12, 1992
    Date of Patent: January 10, 1995
    Assignee: Nissan Chemical Industries, Limited
    Inventors: Fumie Sato, Kazutaka Arai, Katsuaki Miyaji
  • Patent number: 5362915
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is --CH.sub.3 or --CH.sub.2 CH.sub.3 unsubstituted or substituted by 1 to 3 fluorines;X is O or S(O).sub.s where s=0 to 2;R.sub.2 is C.sub.4 -C.sub.6 cyclic alkyl, optionally substituted by one to three methyl groups or one ethyl group; --CH.sub.2 -cyclopentyl, --CH.sub.2 -cyclopropyl, 3-tetrahydrofuranyl, C.sub.1-7 alkyl, CH.sub.3 or CH.sub.2 CH.sub.3 substituted by one to three fluorines;--(CH.sub.2).sub.n COO(CH.sub.2).sub.g CH.sub.3, or (CH.sub.2).sub.n O(CH.sub.2).sub.g CH.sub.3, wherein n is 2 to 4 and g is 0 to 2;R.sub.3 represents a moiety of formula (a); ##STR2## wherein R.sub.4 and R.sub.5 each represent hydrogen or R.sub.4 and R.sub.5 together represent a bond;B represents >C.dbd.O, >C.dbd.S or >CH--R.sub.6 wherein R.sub.6 represents H, OH, C.sub.1-6 alkoxy or C.sub.
    Type: Grant
    Filed: October 2, 1992
    Date of Patent: November 8, 1994
    Assignees: SmithKline Beecham Pharma GmbH, SmithKline Beecham Corporation
    Inventors: Harald Maschler, Siegfried B. Christensen, IV
  • Patent number: 5352678
    Abstract: Certain piperazinyl- and piperidinyl-substituted cyclohexanes have anti-ischemic properties.
    Type: Grant
    Filed: June 25, 1993
    Date of Patent: October 4, 1994
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Ronald J. Mattson, John D. Catt
  • Patent number: 5352822
    Abstract: The present invention discloses pesticidally active compounds of formula (II) ##STR1## or a salt thereof, wherein Q is an monocyclic aromatic ring, or fused bicyclic ring system of which at least one ring is aromatic containing 9 or 10 atoms of which one may be nitrogen and the rest carbon each ring system being optionally substituted, or Q is a dihalovinyl group or a group R.sup.6 --C.tbd.C-- where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; R.sup.2, R.sup.3 , R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; and R.sup.1 is selected from hydrogen and C.sub.1-8 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy and X.sup.1 is hydrogen, fluoro or chloro.
    Type: Grant
    Filed: April 7, 1993
    Date of Patent: October 4, 1994
    Assignee: Roussel Uclaf
    Inventors: Robert J. Blade, George S. Cockerill, John E. Robinson
  • Patent number: 5306695
    Abstract: Compounds of the formula I ##STR1## in which n is 0-6, R.sup.1 is alkyl, haloalkyl, cycloalkyl, halocycloalkyl, phenyl or halogenated phenyl,R.sup.2 is Hal, CN, alkyl, haloalkyl, alkoxy, haloalkoxy, thioalkyl, R.sup.a SO.sub.2 --, R.sup.a SO.sub.2 O--, R.sup.a SO.sub.2 NR.sup.6, R.sup.a and R.sup.b being alkyl or haloalkyl, and R.sup.3 is H, Hal, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio, and R.sup.4 is haloalkyl, are suitable as selective herbicides and as growth regulators. To prepare them, a cyclohexanedione can be reacted a) with a 4-oxy-substituted benzoyl chloride and the resulting enol ether can be rearranged, or b) with a benzoyl cyanide. The benzoyl chloride or benzoyl cyanide required can be obtained from correspondingly substituted toluenes via the carboxylic acid.
    Type: Grant
    Filed: March 4, 1992
    Date of Patent: April 26, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Herbert Stark, Klaus Bauer, Hermann Bieringer
  • Patent number: 5264632
    Abstract: 2,2-Difluorocyclopropyl derivatives of the formula ##STR1## in which R represents alkyl, optionally substituted aryl or optionally substituted aralkyl andX represents hydroxymethyl, 2-hydroxyethyl, isocyanato, amino, amino hydrohalide or a radical of the formula --CO--R.sup.1, whereR.sup.1 represents hydrogen, hydroxyl, alkoxy, alkyl, halogen or amino,are intermediates for fungicides.
    Type: Grant
    Filed: December 8, 1992
    Date of Patent: November 23, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Karl-Rudolf Gassen, Bernd Baasner
  • Patent number: 5254708
    Abstract: The present invention relates to substituted cyclopentanone and cyclohexanone derivatives and substituted cyclopentenone and cyclohexenone derivatives, which are useful as intermediates for pharmaceutical products and agricultural chemicals and especially useful for the synthesis of prostaglandins, and also to a process for producing the same.
    Type: Grant
    Filed: December 14, 1990
    Date of Patent: October 19, 1993
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Fumie Sato, Kazutaka Arai, Katsuaki Miyaji
  • Patent number: 5250732
    Abstract: 5,6-Dehydronorketamine and derivatives retaining the .alpha.,.beta.-unsaturated carbonyl are disclosed. These and other Michael or Michael-type acceptors and adducts are shown to influence the replication, differentiation or maturation of blood cells, especially platelet progenitor cells. Accordingly, these compounds are used for treatment of thrombocytopenia.
    Type: Grant
    Filed: July 18, 1991
    Date of Patent: October 5, 1993
    Assignee: Genentech, Inc.
    Inventors: Timothy P. Kogan, Todd C. Somers
  • Patent number: 5248830
    Abstract: Disclosed are intermediates and a process of making an anticholesterolemic compound of the formula ##STR1## the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 23, 1992
    Date of Patent: September 28, 1993
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: John Ullrich, John R. Regan
  • Patent number: 5248834
    Abstract: Pesticidal compounds of formula II: R.sub.A CR.sub.3 .dbd.CR.sub.4 CHDR.sub.Bin which formula:R.sub.A represents a group ArCR.sub.1 R.sub.2 - in which Ar represents a phenyl or naphthyl group optionally substituted by one or more halogen, alkoxy, haloalkoxy, methylenedioxy, C.sub.1 -C.sub.6 alkyl or haloalkyl groups;R.sub.1 and R.sub.2 together with the carbon to which they are attached represent a C.sub.3 -C.sub.6 cycloalkyl group optionally substituted by one or more halogen atoms or C.sub.1 -C.sub.6 alkyl groups.R.sub.3 and R.sub.4 which may be identical or differ, represent hydrogen halogen or C.sub.1 -C.sub.6 alkyl groups andR.sub.B represents the residue of an alcohol R.sub.B CHDOH in which D is hydrogen or cyano and of which the [1R, cis] 2,2-dimethyl-3-(2,2-dibromovinyl) cyclopropane carboxylic ester is significantly insecticidal,the configuration of R.sub.A and CHDR.sub.
    Type: Grant
    Filed: April 17, 1992
    Date of Patent: September 28, 1993
    Assignee: British Technology Group Limited
    Inventors: Michael Elliott, Norman F. Janes, Bhupinder P. S. Khambay, Ahmet Baydar
  • Patent number: 5245041
    Abstract: A process for the preparation of cyclohexanedione derivatives of the general formula I ##STR1## where R.sup.1 is C.sub.2 -C.sub.8 -alkyl, C.sub.2 -C.sub.8 -alkenyl, C.sub.3 -C.sub.12 -cycloalkyl, C.sub.5 -C.sub.12 -cycloalkyl with 0-4 olefinically unsaturated bonds, C.sub.2 -C.sub.8 -alkylthioalkyl, C.sub.6 -C.sub.12 -bicycloalkyl with 0-3 olefinically unsaturated bonds, unsubstituted or substituted aryl or hetaryl, or a heterocyclic radical of 4 to 7 atoms of which not more than 3 may be hetero-atoms chosen from O, S and N, the radical being saturated or olefinically unsaturated, by reacting an .alpha.,.beta.-unsaturated ketone (II) with a dialkyl malonate in the presence of a base to give the alkoxycarbonylcyclohexenolone or its salt (III) ##STR2## and acylation, hydrolysis and decarboxylation of (III), wherein the .alpha.,.beta.
    Type: Grant
    Filed: December 18, 1991
    Date of Patent: September 14, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Gernot Reissenweber, Winfried Richarz
  • Patent number: 5239110
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is lower-alkanoyl or hydrogen;R.sub.2 and R.sub.3 are the same or different lower-alkyl; or pharmaceutically acceptable acid-addition salts thereof are useful in the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: December 30, 1992
    Date of Patent: August 24, 1993
    Assignee: Sterling Winthrop, Inc.
    Inventors: John P. Mallamo, William F. Michne, Aram Mooradian
  • Patent number: 5231208
    Abstract: The present invention relates to substituted cyclopentanone and cyclohexanone derivatives and substituted cyclopentenone and cyclohexenone derivatives, which are useful as intermediates for pharmaceutical products and agricultural chemicals and especially useful for the synthesis of prostaglandins, and also to a process for producing the same.
    Type: Grant
    Filed: December 14, 1990
    Date of Patent: July 27, 1993
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Fumie Sato, Kazutaka Arai, Katsuaki Miyaji
  • Patent number: 5208353
    Abstract: This invention relates to a process for preparing epoxy esters, and intermediates prepared by this process, in particular, to a process which produces non-racemic epoxy esters which are of use as intermediates in the preparation of pharmaceutical compounds.
    Type: Grant
    Filed: July 15, 1992
    Date of Patent: May 4, 1993
    Assignee: SmithKline Beecham Corp.
    Inventors: Joseph R. Flisak, Paul G. Gassman, Ivan Lantos, Wilford L. Mendelson
  • Patent number: 5200535
    Abstract: The invention provides cyclohexanone derivatives of the general formula ##STR1## in which n represents an integer from 0 to 5; each R represents a halogen atom, nitro, cyano, hydroxyl, alkyl, haloalkyl, alkoxy, haloalkoxy, amino, alkylamino, dialkylamino, alkoxycarbonyl, carboxyl, alkanoyl, alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, alkylamido, cycloalkyl or phenyl group; R.sup.1, R.sup.2 and R.sup.3 independently represent a hydrogen atom or an alkyl group; R.sup.6 and R.sup.7 together represent a single carbon-carbon bond or an epoxy group; and R.sup.8 represents a hydrogen atom or a hydroxyl group; with the proviso that when R.sup.6 and R.sup.7 together represent an epoxy group then R.sup.8 represents a hydrogen atom; and a process for their preparation. Compounds of formula I are useful as intermediates in the preparation of certain fungicidally active cyclopentane derivatives.
    Type: Grant
    Filed: August 19, 1991
    Date of Patent: April 6, 1993
    Assignee: Shell Research Limited
    Inventor: Paul H. Briner