Alicyclic Ring Containing Patents (Class 568/329)
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Patent number: 6340774Abstract: 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: GrantFiled: January 31, 2001Date of Patent: January 22, 2002Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Chaitan Khosla, Zhihao Hu, Thomas Marti
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Publication number: 20020007085Abstract: 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 1Type: ApplicationFiled: December 5, 2000Publication date: January 17, 2002Applicant: 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
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Patent number: 6313351Abstract: 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: GrantFiled: September 2, 1999Date of Patent: November 6, 2001Assignee: Honshu Chemical Industry Co., Ltd.Inventors: Norimoto Kiya, Shinsaku Kawasaki, Kenji Ekawa, Kenji Sugiyama, Toyokazu Kitaura
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Publication number: 20010021791Abstract: 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 1Type: ApplicationFiled: December 8, 2000Publication date: September 13, 2001Applicant: 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
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Patent number: 6281250Abstract: The present invention is directed to retinyl ethers, derivatives and analogues and their use in inhibiting breast carcinogenesis or breast cancer cell growth.Type: GrantFiled: April 12, 1999Date of Patent: August 28, 2001Assignee: Southern Research InstituteInventor: Y. Fulmer Shealy
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Patent number: 6258854Abstract: 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: GrantFiled: September 1, 1999Date of Patent: July 10, 2001Assignee: Givaudan Roure ( International ) SAInventors: Denise Anderson, Georg Fráter
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Patent number: 6251833Abstract: 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: GrantFiled: August 31, 1999Date of Patent: June 26, 2001Inventors: Christoph Erdelen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Norbert Mencke, Andreas Turberg
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Publication number: 20010003784Abstract: 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: ApplicationFiled: December 5, 2000Publication date: June 14, 2001Inventors: Andreas Kramer, Christian Knoll, Johann-Peter Melder, Wolfgang Siegel, Gerd Kaibel
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Patent number: 6242641Abstract: 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: GrantFiled: March 22, 1999Date of Patent: June 5, 2001Assignee: Bayer AktiengesellschaftInventors: Manfred Jautelat, Carl Casser, Hanns-Peter Müller, Manfred Hajek
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Patent number: 6239135Abstract: 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: GrantFiled: December 9, 1998Date of Patent: May 29, 2001Assignee: Eli Lilly and CompanyInventors: Daniel Timothy Kohlman, Yao-Chang Xu
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Patent number: 6207852Abstract: 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: GrantFiled: December 23, 1998Date of Patent: March 27, 2001Assignee: Bridge Pharma, Inc.Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen
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Publication number: 20010000038Abstract: 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 1Type: ApplicationFiled: December 1, 2000Publication date: March 15, 2001Inventors: 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
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Patent number: 6172118Abstract: 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: GrantFiled: April 8, 1999Date of Patent: January 9, 2001Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Cornelia J. Forster
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Patent number: 6159988Abstract: 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: GrantFiled: June 29, 1998Date of Patent: December 12, 2000Assignee: Hoeschst AktiengesellschaftInventors: 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
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Patent number: 6150374Abstract: 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: GrantFiled: September 29, 1997Date of Patent: November 21, 2000Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Peter Gerdes, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
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Patent number: 6118017Abstract: 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: GrantFiled: April 8, 1999Date of Patent: September 12, 2000Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Cornelia J. Forster
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Patent number: 6086857Abstract: 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: GrantFiled: September 3, 1998Date of Patent: July 11, 2000Assignee: BASF AktiengesellschaftInventors: Christof Kandzia, Horst Westenfelder, Volker Schehlmann
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Patent number: 6040274Abstract: 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: GrantFiled: March 18, 1997Date of Patent: March 21, 2000Assignee: BASF AktiengesellschaftInventors: 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
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Patent number: 6017470Abstract: 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: GrantFiled: April 12, 1996Date of Patent: January 25, 2000Assignee: The Trustees of Columbia University in the City of New YorkInventors: Thomas J. Katz, Colin P. Nuckolls
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Patent number: 5932765Abstract: 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: GrantFiled: October 22, 1997Date of Patent: August 3, 1999Assignee: Merck Patent Gesellschaft MitInventors: Claude Lardy, Jaques Barbanton, Herve Dumas, Francois Collonges, Phillippe Durbin
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Patent number: 5908944Abstract: 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: GrantFiled: September 30, 1994Date of Patent: June 1, 1999Assignee: Schering AktiengesellschaftInventors: Jurgen Westermann, Klaus Nickisch
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Patent number: 5892098Abstract: 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: GrantFiled: April 15, 1997Date of Patent: April 6, 1999Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
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Patent number: 5840661Abstract: 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: GrantFiled: December 31, 1996Date of Patent: November 24, 1998Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Jacques Dumas, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Andreas Turberg, Norbert Mencke
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Patent number: 5773614Abstract: (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: GrantFiled: September 13, 1996Date of Patent: June 30, 1998Assignee: Bristol-Myers Squibb Co.Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller
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Patent number: 5767288Abstract: 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: GrantFiled: January 5, 1996Date of Patent: June 16, 1998Assignee: California Institute of TechnologyInventors: Ronald S. Rock, Michael H. B. Stowell, Sunney I. Chan
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Patent number: 5741476Abstract: 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: GrantFiled: June 20, 1995Date of Patent: April 21, 1998Assignee: Mallinckrodt Medical, Inc.Inventor: John Janine Rene Mertens
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Patent number: 5739376Abstract: Fullerene derivatives, methods of preparing the same and methods of using the same, wherein the fullerene derivatives are of the formula I ##STR1##Type: GrantFiled: October 20, 1995Date of Patent: April 14, 1998Assignee: Hoechst AktiengesellschaftInventor: Carsten Bingel
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Patent number: 5728889Abstract: 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: GrantFiled: June 24, 1997Date of Patent: March 17, 1998Assignee: Zeneca LimitedInventors: Howard Rawlinson, Jonathan William Wiffen, Stephen Martin Brown
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Patent number: 5639918Abstract: (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: GrantFiled: September 26, 1994Date of Patent: June 17, 1997Assignee: Rhone-Poulenc AgrochimieInventors: Jean Hutt, Jacques Mugnier, Alfred Greiner, Regis Pepin
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Patent number: 5633381Abstract: 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: GrantFiled: July 5, 1994Date of Patent: May 27, 1997Assignee: Berlex Laboratories, Inc.Inventors: Jerry L. Dallas, William J. Guilford, Sunil K. Koovakkat, Michael M. Morrissey, Kenneth J. Shaw
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Patent number: 5476876Abstract: 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: GrantFiled: May 24, 1994Date of Patent: December 19, 1995Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Joseph A. Miller, John M. Janusz, Theresa Rosario-Jansen
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Patent number: 5466721Abstract: 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: GrantFiled: June 13, 1994Date of Patent: November 14, 1995Assignee: Henkel CorporationInventor: Paul E. Share
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Patent number: 5393917Abstract: 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: GrantFiled: December 16, 1993Date of Patent: February 28, 1995Assignee: BASF AktiengesellschaftInventors: Siegmund Besecke, Andreas Deckers, Harald Lauke
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Patent number: 5387593Abstract: Novel piperazinyl- and piperidinyl-cyclohexanols of the following formula are useful as anxiolytic agents and have other psychotropic properties ##STR1##Type: GrantFiled: February 17, 1994Date of Patent: February 7, 1995Assignee: Briston-Myers SquibbInventors: Ronald J. Mattson, John D. Catt
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Patent number: 5384331Abstract: 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: GrantFiled: May 28, 1993Date of Patent: January 24, 1995Assignee: Genentech, Inc.Inventors: Timothy P. Kogan, Todd C. Somers
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Patent number: 5380900Abstract: 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: GrantFiled: February 12, 1992Date of Patent: January 10, 1995Assignee: Nissan Chemical Industries, LimitedInventors: Fumie Sato, Kazutaka Arai, Katsuaki Miyaji
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Patent number: 5362915Abstract: 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: GrantFiled: October 2, 1992Date of Patent: November 8, 1994Assignees: SmithKline Beecham Pharma GmbH, SmithKline Beecham CorporationInventors: Harald Maschler, Siegfried B. Christensen, IV
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Patent number: 5352678Abstract: Certain piperazinyl- and piperidinyl-substituted cyclohexanes have anti-ischemic properties.Type: GrantFiled: June 25, 1993Date of Patent: October 4, 1994Assignee: Bristol-Myers Squibb Co.Inventors: Ronald J. Mattson, John D. Catt
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Patent number: 5352822Abstract: 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: GrantFiled: April 7, 1993Date of Patent: October 4, 1994Assignee: Roussel UclafInventors: Robert J. Blade, George S. Cockerill, John E. Robinson
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Patent number: 5306695Abstract: 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: GrantFiled: March 4, 1992Date of Patent: April 26, 1994Assignee: Hoechst AktiengesellschaftInventors: Herbert Stark, Klaus Bauer, Hermann Bieringer
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Patent number: 5264632Abstract: 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: GrantFiled: December 8, 1992Date of Patent: November 23, 1993Assignee: Bayer AktiengesellschaftInventors: Karl-Rudolf Gassen, Bernd Baasner
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Patent number: 5254708Abstract: 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: GrantFiled: December 14, 1990Date of Patent: October 19, 1993Assignee: Nissan Chemical Industries, Ltd.Inventors: Fumie Sato, Kazutaka Arai, Katsuaki Miyaji
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Patent number: 5250732Abstract: 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: GrantFiled: July 18, 1991Date of Patent: October 5, 1993Assignee: Genentech, Inc.Inventors: Timothy P. Kogan, Todd C. Somers
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Patent number: 5248830Abstract: 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: GrantFiled: June 23, 1992Date of Patent: September 28, 1993Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: John Ullrich, John R. Regan
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Patent number: 5248834Abstract: 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: GrantFiled: April 17, 1992Date of Patent: September 28, 1993Assignee: British Technology Group LimitedInventors: Michael Elliott, Norman F. Janes, Bhupinder P. S. Khambay, Ahmet Baydar
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Patent number: 5245041Abstract: 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: GrantFiled: December 18, 1991Date of Patent: September 14, 1993Assignee: BASF AktiengesellschaftInventors: Gernot Reissenweber, Winfried Richarz
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Patent number: 5239110Abstract: 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: GrantFiled: December 30, 1992Date of Patent: August 24, 1993Assignee: Sterling Winthrop, Inc.Inventors: John P. Mallamo, William F. Michne, Aram Mooradian
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Patent number: 5231208Abstract: 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: GrantFiled: December 14, 1990Date of Patent: July 27, 1993Assignee: Nissan Chemical Industries, Ltd.Inventors: Fumie Sato, Kazutaka Arai, Katsuaki Miyaji
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Patent number: 5208353Abstract: 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: GrantFiled: July 15, 1992Date of Patent: May 4, 1993Assignee: SmithKline Beecham Corp.Inventors: Joseph R. Flisak, Paul G. Gassman, Ivan Lantos, Wilford L. Mendelson
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Patent number: 5200535Abstract: 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: GrantFiled: August 19, 1991Date of Patent: April 6, 1993Assignee: Shell Research LimitedInventor: Paul H. Briner