Chalcogen Or Nitrogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/22)
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Patent number: 6020371Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.Type: GrantFiled: December 16, 1997Date of Patent: February 1, 2000Assignee: Agouron Pharmaceuticals, Inc.Inventors: Peter S. Dragovich, Thomas J. Prins, Ru Zhou
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Patent number: 5872121Abstract: A compound of the formula ##STR1## wherein R is a) phenyl; phenyl(C.sub.1 -C.sub.4 alkoxy); phenoxy; or benzyl; the phenyl ring of each substituent being optionally substituted with one or more of halogen, nitro, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 haloalkyl, C.sub.1 -C.sub.8 haloalkoxy, di(C.sub.1 -C.sub.8 alkyl)amino, phenyl or phenoxy; or b) a 5- or 6-membered heterocyclic group comprising 1-3 heteroatoms selected from the group consisting of N, O or S, optionally substituted with one or more of halogen, nitro, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 haloalkyl, C.sub.1 -C.sub.8 haloalkoxy, or di-(C.sub.1 -C.sub.8 alkyl)amino. These compounds and pesticidal compositions prepared therefrom, are useful as plant protecting agents for the control of insects, nematodes, and mites.Type: GrantFiled: August 21, 1997Date of Patent: February 16, 1999Assignee: Uniroyal Chemical Company, Inc.Inventors: Mark Achiel Dekeyser, Paul Thomas McDonald
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3-aryl-tetronic acid derivatives, the production thereof and the use thereof as antiparasitic agents
Patent number: 5830825Abstract: The present invention relates to new 3-aryl-4-hydroxy-.DELTA..sup.3 -dihydrofuranone derivatives of the formula (I) ##STR1## in which A and B together with the carbon atom to which they are bonded form an unsubstituted or substituted 5- to 7-membered ring which is interrupted by at least one hetero atom,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents a number 0, 1, 2 or 3,G represents hydrogen (a) or one of the groups ##STR2## E represents a metal Ion equivalent or an ammonium ion, L represents oxygen or sulphur,M represents oxygen or sulphur andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meanings given in the description, to processes for their preparation, and to their use as pesticides.Type: GrantFiled: June 17, 1997Date of Patent: November 3, 1998Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Gunther Beck, Hermann Hagemann, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wolfram Andersch, Norbert Mencke, Andreas Turberg -
Patent number: 5824484Abstract: The invention provides a method of screening a substance for the ability to effect the formation of a retinoid X receptor homodimer comprising combining the substance and a solution containing retinoid X receptors and determining the presence of homodimer formation. Also provided is a method of screening a substance for an effect on a retinoid X receptor homodimer's ability to bind DNA comprising combining the substance with the homodimer and determining the effect of the compound on the homodimer's ability to bind DNA. A method of inhibiting an activity of a retinoid X receptor heterodimer comprising increasing the formation of a retinoid X receptor homodimer, thereby preventing the retinoid X receptor from forming a heterodimer and preventing the resulting heterodimer activity is also provided. A method of inhibiting an activity of a retinoid X receptor homodimer is also provided.Type: GrantFiled: January 22, 1996Date of Patent: October 20, 1998Assignee: La Jolla Cancer Research FoundationInventors: Magnus Pfahl, Xiao-kun Zhang, Jurgen M. Lehmann, Marcia I. Dawson, James F. Cameron, Peter D. Hobbs, Ling Jong
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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: 5756766Abstract: A composition for optical materials is herein disclosed which comprises the following two components (a) and (b):(a) a component containing at least one of poly isocyanates represented by the formula (1) ##STR1## wherein A is an alkanediyl group or an alkanetetrayl group which may contain a sulfur atom, or a dithianetetrayl group, and the alkanediyl group or the alkanetetrayl group may be substituted by a phenyl group; B is a methylene chain represented by .paren open-st.CH.sub.2 .paren close-st..sub.m (m is an integer of 1 to 4) which may contain a sulfur atom, and B's may be the same or different; and n is an integer of 2 or 4, and(b) a component containing at least one of polythiols having two or more mercapto groups. The composition is useful to provide optical products such as plastic lenses, filters, substrates for recording media and optical fibers which have a very high refractive index and which are excellent in heat resistance.Type: GrantFiled: March 24, 1997Date of Patent: May 26, 1998Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Nobuya Kawauchi, Katsuyoshi Sasagawa, Seiichi Kobayashi
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Patent number: 5744569Abstract: In one-component and two-component polyurethane coating compositions comprising at least one reactive component capable of reacting with polyisocyanates, the reactive component is a compound A) containing an isocyanate group, a urethane, thiourethane or urea group and two capped isocyanate-reactive groups.Type: GrantFiled: June 28, 1996Date of Patent: April 28, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Bruchmann, Hans Renz, Gunter Mohrhardt
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Patent number: 5718845Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.Type: GrantFiled: January 18, 1995Date of Patent: February 17, 1998Assignee: Enichem S.p.A.Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
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Patent number: 5693827Abstract: A method of inhibiting the growth or replication of viruses of the HIV group is disclosed. Also disclosed are compounds useful in the method and pharmaceutical formulations incorporating such compounds. The method involves the use of compounds having the general formula: ##STR1## wherein the substituent groups are as defined in the specification.Type: GrantFiled: June 7, 1995Date of Patent: December 2, 1997Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd/LteeInventors: William Ashley Harrison, Gary Edward Jewell, Ethel Ellen Felauer, Mark Achiel Dekeyser, Dong Dao-Cong, James Anthony McGuiness, Anupama Mishra, Walter Gerhard Brouwer, Derek James McPhee
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Patent number: 5648354Abstract: Novel 1,2-dithiin compounds useful as antifungal or anti-infective agents, as well as methods for their use as such, are described.Type: GrantFiled: February 28, 1995Date of Patent: July 15, 1997Assignee: Shaman Pharmaceuticals, Inc.Inventors: Donald E. Bierer, Jeffrey M. Dener, Joane Litvak, Larisa G. Dubenko
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Patent number: 5621147Abstract: A 1,1,2-trifluoro-2-(trans-4-substituted cyclohexyl)ethylene of the formula (1):R--(A).sub.m --Cy--CF=CF.sub.2 (1)wherein R is a C.sub.1-10 alkyl group, a halogen atom or a cyano group, provided that in the case of the alkyl group, an oxygen atom may be interposed in a carbon-carbon bond of the alkyl group or in a carbon-carbon bond between this alkyl group and A, some of carbon-carbon bonds in the alkyl group may be triple bonds or double bonds, one --CH.sub.2 -- group in the alkyl group may be substituted by a carbonyl group, and some or all of hydrogen atoms in the alkyl group may be substituted by fluorine atoms;Cy is an unsubstituted trans-1,4-cyclohexylene group;A is a trans-1,4-cyclohexylene group, a 1,4-phenylene group or a 1,4-cyclohexenylene group, wherein each of such cyclic groups is unsubstituted or substituted by one or more halogen atoms or cyano groups, one or more =CH-- groups constituting rings of such cyclic groups may be substituted by nitrogen atoms, and one or more --CH.sub.Type: GrantFiled: May 4, 1995Date of Patent: April 15, 1997Assignee: Asahi Glass Company Ltd.Inventors: Osamu Yokokoji, Tamaki Simizu, Seisaku Kumai
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Patent number: 5618943Abstract: Compounds of the formula ##STR1## the symbols have the meaning described in the specification have retinoid-like biological activity.Type: GrantFiled: December 29, 1994Date of Patent: April 8, 1997Assignee: AllerganInventors: Vidyasagar Vuligonda, Alan T. Johnson, Richard L. Beard, Min Teng, Tae K. Song, Harold N. Wong, Roshantha A. Chandraratna
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Patent number: 5583235Abstract: The present invention provides an improved procedure for the preparation of 3,6-disubstituted-1,2-dithiin derivatives, especially unsymmetrical 1,2-dithiins. In addition, the process offers significant process, scaleup, and safety advantages over the previously reported synthetic processes. The compounds synthesized by this new process and described herein are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, Trichophyton rubrum, Candida parapsilosis, Candida tropicalis, or Candida krusei.Type: GrantFiled: March 11, 1994Date of Patent: December 10, 1996Assignee: Shaman Pharmaceuticals, Inc.Inventors: Donald E. Bierer, Jeffrey M. Dener, Thien V. Truong
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Patent number: 5580897Abstract: Novel 1,2-dithiin compounds useful as antifungal or anti-infective agents, as well as methods for their use as such, are described.Type: GrantFiled: February 28, 1995Date of Patent: December 3, 1996Assignee: Shaman Pharmaceuticals, Inc.Inventors: Donald E. Bierer, Patricia Peterli-Roth
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Patent number: 5574000Abstract: Cyclohexenone oxime ethers of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl, A is substituted or unsubstituted C.sub.4 -alkylene or C.sub.4 -alkenylene,X is nitro, cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl and/or phenyl,n is from 0 to 3 or from 1 to 5 when X is halogen,R.sup.2 is C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.4 -alkythio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl or C.sub.5 -C.sub.Type: GrantFiled: November 17, 1994Date of Patent: November 12, 1996Assignee: BASF AktiengesellschaftInventors: Juergen Kast, Dieter Kolassa, Norbert Meyer, Ulrich Schirmer, Albrecht Harreus, Jochen Wild, Karl-Otto Westphalen, Bruno Wuerzer
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Patent number: 5556875Abstract: This invention pertains to a novel group of 1,2-dithiin compounds useful as antiinfective agents, and a novel synthetic process to produce the same. The compounds are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans or Aspergillus fumigatus.Type: GrantFiled: August 24, 1995Date of Patent: September 17, 1996Assignees: Shaman Pharmaceuticals, Inc., The Regents of the University of MichiganInventors: Thien V. Truong, Donald E. Bierer, Jeffrey M. Dener, Richard Hector, Michael S. Tempesta, Bernard Loev, Wu Yang, Masato Koreeda
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Patent number: 5554582Abstract: Cyclohexenone compounds of the formula ##STR1## where R.sup.1 is alkyl of 1 to 4 carbon atoms, alkenyl or alkynyl of 3 or 4 carbon atoms, haloalkenyl of 3 or 4 carbon atoms and 1 to 3 halogen substituents, or is thenyl which is unsubstituted or substituted by halo and/or alkyl, R.sup.2 is alkyl of 1 to 4 carbon atoms, and R.sup.3 is formyl, a radical of the general formula R.sup.4 XCHXR.sup.5, where X is oxygen or sulfur, and R.sup.4 and R.sup.5 are identical or different alkyl, or together denote alkylene of 1 to 4 carbon atoms and which is unsubstituted or substituted by alkyl, alkoxy, alkylthio, hydroxy, halogen, cyano or N,N-dialkylamino, have a good herbicidal action preferably on species from the grass family.Type: GrantFiled: November 30, 1992Date of Patent: September 10, 1996Assignee: BASF AktiengesellschaftInventors: Michael Keil, Ulrich Schirmer, Dieter Kolassa, Juergen Kast, Bruno Wuerzer, Norbert Meyer
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Patent number: 5541323Abstract: Anhydride compounds which contain at least one rodlike mesogenic moiety and at least two anhydride groups per molecule, wherein each of said aromatic anhydride groups is linked to the mesogen via an ester linkage are prepared. These anhydride compounds are useful in curing epoxy resins to provide the cured products with one or more improved properties.Type: GrantFiled: January 18, 1995Date of Patent: July 30, 1996Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5527924Abstract: The present invention provides two basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogs to taxol. Both the intermediates and analogs to taxol may prove to be valuable anticancer agents.Type: GrantFiled: December 5, 1994Date of Patent: June 18, 1996Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, William G. Bornmann, Yves Queneau, Thomas V. Magee, Walter J. Krol
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Patent number: 5508275Abstract: Lipid-selective antioxidants of the formula I(A).sub.a (L)(X).sub.a, (I),in whichA=an antioxidative component,L=a bridging member,X=a lipophilic componenta and a'=independently of one another the numbers 1 or 2.The compounds are used for the protection of lipid-containing substances against oxidation and in pharmaceuticals for the prophylaxis and treatment of diseases in which bioradicals are involved, in particular of coronary, circulatory and vascular diseases.Type: GrantFiled: March 15, 1994Date of Patent: April 16, 1996Assignee: Hoechst AktiengesellschaftInventors: Klaus-Ulrich Weithmann, Gunther Wess, Dirk Seiffge
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Patent number: 5502073Abstract: Compounds of the formula (I) ##STR1## which contain between 10 and 27 carbon atoms, and wherein m and n are independently selected from 0, 1 and 2; R.sup.2a is hydrogen, methyl, or ethyl; R.sup.2b is acetylene or contains between 3 and 18 carbon atoms and is a group R.sup.7, wherein R.sup.7 is a C.sub.1-13 non-aromatic hydrocarbyl group, optionally substituted by a cyano or C.sub.1-4 carbalkoxy group and/or by one or two hydroxy groups and/or by one to five halo atoms which are the same or different and/or by one to three groups R.sup.8 which are the same or different and each contain one to four hetero atoms, which are the same or different and are chosen from oxygen, sulphur, nitrogen and silicon, 1 to 10 carbon atoms and optionally 1 to 6 fluoro or chloro atoms or R.sup.2b is a 6-membered aromatic ring substituted by cyano and/or by one to three groups R.sup.8 and/or by a group --C.tbd.CH, --C.tbd.C-R.sup.7 or C.tbd.C-halo and/or by one to five halo atoms and/or by one to three C.sub.Type: GrantFiled: February 23, 1994Date of Patent: March 26, 1996Assignees: The Wellcome Foundation, The Regents of the University of CaliforniaInventors: John E. Casida, Michael Elliott, David A. Pulman
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Patent number: 5484872Abstract: The present invention provides a cyclic sulfide compound represented by a general formula (I) ##STR1## (where R.sup.1 represents --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --O--CH.sub.2 --, --CH.sub.2 --O--, or --CH.sub.2 --S--). According to this invention, a novel cyclic sulfide compound which gives high refractive index and high Abbe number can be obtained. The polymerizable compositions for manufacturing optical products with this compound as their main component can be readily molded into plastic lenses which give superhigh refractive indices and high Abbe numbers or those which give high refractive indices and high Abbe number with low sp.grs. in addition thereto. The castings obtained from said polymerizable compositions are useful as plastic lenses for glasses, manifesting optical uniformity and being excellent in processability, transparency, and thermal, impact and light resistance.Type: GrantFiled: March 14, 1995Date of Patent: January 16, 1996Assignee: Daiso Co., Ltd.Inventors: Hiroyuki Kanesaki, Tetsuyuki Saika, Masafumi Mikami
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Patent number: 5463081Abstract: The invention relates to novel intermediates for the preparation of a certain group of novel phenylsulfonylurea herbicides, which herbicides are particularly advantageous for use in crop protection. The novel intermediate compounds are of the formula II ##STR1## and of the formula VI, ##STR2## as defined in the specification and claims. The intermediate compounds may be used to prepare herbicidal and plant growth regulating compounds of the formula I or salts thereof: ##STR3## as defined in the specification. The herbicides so obtained are particularly suitable for selectively controlling weeds.Type: GrantFiled: September 21, 1993Date of Patent: October 31, 1995Assignee: Hoechst AktiengesellschaftInventors: Oswald Ort, Klaus Bauer, Hermann Bieringer
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Patent number: 5446173Abstract: The present invention provides a cyclic sulfide compound represented by a general formula (I) ##STR1## (where R.sup.1 represents --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --O--CH.sub.2 --, --CH.sub.2 --O--, or --CH.sub.2 --S--). Polymerizable compositions for manufacturing optical products with this compound as their main component can be readily molded into plastic lenses which give superhigh refractive indices and high Abbe numbers or those which give high refractive indices and high Abbe number with low sp.grs. in addition thereto. The castings obtained from said polymerizable compositions are useful as plastic lenses for glasses, manifesting optical uniformity and being excellent in processability, transparency, and thermal, impact and light resistance. Further these polymerizable resin compositions are usable preferably as such optical products as prisms, optical fibers, optical disc substrates, color filters, or infrared absorption filters.Type: GrantFiled: March 23, 1993Date of Patent: August 29, 1995Assignee: Daiso Co., Ltd.Inventors: Hiroyuki Kanesaki, Tetsuyuki Saika, Masafumi Mikami
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Patent number: 5405968Abstract: Methine dyes with a polyketo group I ##STR1## where A is ##STR2## R.sup.1 is a 5- or 6-membered cycloaliphatic radical which contains one or two hetero atoms from the group --NR.sup.4 --, --O-- and --S-- and which may be fused to an isoaromatic or heteroaromatic group, R.sup.2 and R.sup.3 are identical or different C.sub.1 -C.sub.10 -alkyl groups or together one of the radicals R.sup.1, and m and n are identical or different integers from 0 to 3, are useful as drugs, for producing singlet oxygen, as sensitizers in electrophotographic layers and for photopolymerizations and as laser light sensitive dyes in optical recording media; also novel triketo- and tetraketomethine dyes.Type: GrantFiled: September 27, 1993Date of Patent: April 11, 1995Assignee: BASF AktiengesellschaftInventors: Bernhard Albert, Knut Kessel, Hans-Dieter Martin, Stefan Silber
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Patent number: 5403938Abstract: This invention relates-to a polythiol compound and an optical material therefrom. Having a rigid 1,4-dithian ring which increases the refractive index and Abbe's number, the polythiol compound used for the production of an optical material imparts the optical material with high heat resistance and excellent mechanical properties as well as excellent optical properties.Type: GrantFiled: June 8, 1993Date of Patent: April 4, 1995Assignee: Hoya CorporationInventors: Tsuyoshi Ohkubo, Chau Nguyen, Reisuke Okada
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Patent number: 5302727Abstract: Compounds of the formula ##STR1## wherein R is a residue of the formula ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X, Y and Z are as described, with the exception of rac-N-(3,4-dimethoxyphenethyl)-2-(3,4-dimethoxyphenyl)-.beta.,N-dimethyl-m -dithiane-2-propanamine, as well as their acid addition salts, in particular for use in eliminating cytostatic resistance in tumor treatment and chloroquine resistance in malaria.Type: GrantFiled: July 15, 1992Date of Patent: April 12, 1994Assignee: Hoffmann-La Roche Inc.Inventors: James F. Eliason, Henri Ramuz, Franz A. Kaufmann-Schmid, deceased
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Patent number: 5296611Abstract: Propenals of formula: ##STR1## in which formula R is H or a C.sub.1 -C.sub.4 thioalkyl radical, the dithiane ring being at the cis position in relation to the aldehyde function when R is H and at the trans position when R is a thioalkyl radical. The invention also relates to two processes for the preparation of these propenals.Type: GrantFiled: June 12, 1992Date of Patent: March 22, 1994Assignee: L'OrealInventors: Guy Solladie, Valerie Berl, Jean Maignan
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Patent number: 5264455Abstract: X is hydrogen or --S(O).sub.m --R.sup.1 and Y is hydrogen or S(O).sub.n --R.sup.2, except that X and Y are not both hydrogen, or one of X and Y is --S--alkyl--SH and the other is hydrogen; ##STR2## and the remaining symbols are as defined in the specification.Type: GrantFiled: July 1, 1991Date of Patent: November 23, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: Ravi K. Varma, Jeffrey O. Saunders, Sam T. Chao, Eric M. Gordon, Dinos P. Santafianos
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Patent number: 5260310Abstract: Novel compounds of the formula ##STR1## wherein Q, R.sup.1 and R.sup.2 are described herein, are disclosed along with pharmaceutical compositions, methods of use, and process for producing compounds of formula I which starts from the corresponding .beta.-hydroxycarboxylic acids.Type: GrantFiled: August 12, 1992Date of Patent: November 9, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Romano Derungs, Hans P. Marki, Henri Stalder, Andre Szente
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Patent number: 5250505Abstract: Cyclohexenone oxime ethers I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl, A is unsubstituted or substituted C.sub.3 -C.sub.6 -alkynylene, Z is unsubstituted or substituted phenyl an unsubstituted or substituted 6-membered or 7-membered saturated or monounsaturated or diunsaturated heterocyclic structure having one or two hetero atoms selected from the group consisting of oxygen and sulfer, and their agriculturally useful salts and esters of C.sub.1 -C.sub.10 -carboxylic acids and inorganic acids, are suitable as herbicides.Type: GrantFiled: May 8, 1991Date of Patent: October 5, 1993Assignee: BASF AktiengesellschaftInventors: Juergen Kast, Norbert Meyer, Ulf Misslitz, Albrecht Harreus, Thomas Kuekenhoehner, Harald Bang, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
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Patent number: 5227398Abstract: Hepatopathy improvers contain as an effective ingredient one or more of benzodioxole derivatives represented by the following formula: ##STR1## wherein A means a particular N- or S-containing group. Most of these benzodioxole derivatives are novel.Type: GrantFiled: November 26, 1991Date of Patent: July 13, 1993Assignee: Tsumura & Co.Inventors: Masayuki Kimura, Shouichi Nishida, Shigefumi Takeda, Kunio Hosaka
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Patent number: 5202348Abstract: This invention pertains to a novel group of Thiarubrine substances and closely related derivatives, useful as antifungal and antibiotic agents.Type: GrantFiled: August 17, 1990Date of Patent: April 13, 1993Assignee: The University of British ColumbiaInventors: G. H. Neil Towers, Reimer C. Bruening, Felipe Balza, Zyta A. Abramowski, Isabel Lopez-Bazzochi
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Patent number: 5126347Abstract: Isomeric derivatives of 2',3'-dideoxyadenosine and 2',3'-dideoxyguanosine wherein the adenine or guanine base is attached to the 1' position of the iso-dideoxysugar residue by the 9-N position, the novel intermediates used in the synthesis of these compounds, and a method for treating a subject infected with a retrovirus by administering the compounds of the invention.Type: GrantFiled: February 13, 1989Date of Patent: June 30, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Donna M. Huryn, Steve Yik-Kai Tam, Manfred Weigele
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Patent number: 5098928Abstract: The ketenedithioacetal derivatives of formula (I) have a potent hypolipidemic and anti-arteriosclerotic effect and are useful for prophylaxis and treatment of arteriosclerosis or hyperlipidemia.Type: GrantFiled: October 25, 1990Date of Patent: March 24, 1992Assignee: Nihon Nohyaku Co., Ltd.Inventors: Masashi Nagamine, Kunikazu Hiraga, Atsushi Sakai, Matazaemon Uchida
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Patent number: 5093502Abstract: A process for the preparation of novel 14.alpha., 17.alpha.-dihydroxy-17.beta.-substituted steroids by reacting 14.alpha.-hydroxy-17-oxo-steroids with metal organic compounds and the use of the said novel steroids in the production of 14.alpha., 17.alpha.-methylenedioxy-pregnane derivatives.Type: GrantFiled: February 16, 1990Date of Patent: March 3, 1992Assignee: Akzo N.V.Inventors: Peter M. Smid, Willem J. Van Zoest, Pieter G. Weber, Arthur F. Marx
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Patent number: 5093370Abstract: A quaternary ammonium having a muscle relaxation activity compound represented by the formula (I): ##STR1## wherein R.sub.1 represents a methylene, a lower alkylenoxy, a lower alkenylene, a lower alkynylene, --CO--, --COO--, a lower alkylene carbonyloxy, --CH(OR.sub.5)--, a lower alkylenecarbonyl, a hydroxy lower alkylene, --O--, --S--, --SO--, or --SO.sub.2 --; R.sub.2 represents a hydrogen atom, a hydroxy lower alkyl, an aldehyde, a lower alkyl carbonyl, --NO.sub.2, or --NHR.sub.6 ; R.sub.3 represents a hydrogen atom of a group --R.sub.1 --(CH.sub.2).sub.a --[CH(CH.sub.2 A)--CH.sub.2 ].sub.b --A; R.sub.4 represents an anion; R.sub.5 and R.sub.6 represent a hydrogen atom or a acetyl; A represents a quaternary ammonium group; a represents an integer of 1 to 8; b represents 0 or 1; m represents an integer of 1 to 4; and (Z) represents a trivalent benzene ring, a trivalent naphthalene ring, a trivalent diphenyl or a trivalent ethane radical.Type: GrantFiled: April 9, 1990Date of Patent: March 3, 1992Assignee: Tobishi Yakuhin Kogyo Kabushiki KaishaInventors: Masayasu Kimura, Kenji Naito, Osamu Sakuma, Tadashi Morita
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Patent number: 5089629Abstract: A compound represented by formula (I): ##STR1## wherein wherein R represents a straight chain alkyl group having from 1 to 9 carbon atoms; ##STR2## represents ##STR3## X represents a hydrogen atom or a fluorine atom; and ##STR4## has a trans (equatorial-equatorial) configuration, is disclosed. The compound of formula (I) exhibits a nematic phase in the vicinity of room temperature or in a temperature range higher than room temperature and has a small optical anisotropy and a positive dielectric anisotropy and is, therefore, useful in preparing a liquid crystal display cell excellent in viewing-angle characteristics.Type: GrantFiled: August 13, 1990Date of Patent: February 18, 1992Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Yasuyuki Tanaka, Haruyoshi Takatsu, Kiyohumi Takeuchi, Yuuji Tamura
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Patent number: 5072046Abstract: This invention relates to a process for producing bis-[aminophenyl ketones] and the resulting compositions which are suitable for the preparation of engineering polymers, e.g., polyimides, polyurethanes and a host of other resinous materials. The bis-[aminophenyl ketones] are formed by reacting 2 moles of a nitrophenyl acid halide with an aromatic bridging composition having at least two hydrogen atoms of sufficient reactivity to undergo acylation reactions whereby nitrophenyl ketone groups are attached to the aromatic bridging group. The resulting bis-[nitrophenyl ketones] then are converted to the amine by hydrogenation or by double nucleophilic displacement with an aminophenol.The invention also relates to polyimides and polyamides prepared from such bis-[aminophenyl ketones].Type: GrantFiled: October 2, 1989Date of Patent: December 10, 1991Assignee: Air Products and Chemicals, Inc.Inventors: William F. Burogyne, Jr., Mark D. Conner, Michael E. Ford, Thomas A. Johnson
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Patent number: 5064848Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.Type: GrantFiled: May 4, 1990Date of Patent: November 12, 1991Assignee: Eisai Co., Ltd.Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
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Patent number: 5022914Abstract: Cyclohexenone oxime ethers of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl,A is substituted or unsubstituted C.sub.4 -alkylene or C.sub.4 -alkenylene,X is nitro, cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl and/or phenyl,n is from 0 to 3 or from 1 to 5 when X is halogen,R.sup.2 is C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl or C.sub.5 -C.sub.Type: GrantFiled: October 31, 1989Date of Patent: June 11, 1991Assignee: BASF AktiengesellschaftInventors: Juergen Kast, Dieter Kolassa, Norbert Meyer, Ulrich Schirmer, Albrecht Harreus, Jochen Wild, Karl-Otto Westphalen, Bruno Wuerzer
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Patent number: 5001144Abstract: Disclosed are novel 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof.Phamaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.Type: GrantFiled: April 17, 1990Date of Patent: March 19, 1991Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: John R. Regan, Kent W. Neuenschwander
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Patent number: 4988459Abstract: Optically active oxirane-2-carboxylic acid esters with a mesogenic molecular component suitable as dopants in liquid-crystal mixtures. They result in liquid-crystalline ferroelectric phases with short switching times and in electroclinic phases with large electroclinic coefficients. A further advantage lies in the fact that they induce a helix with a very small pitch so that they are also suitable for helix compensation in LC mixtures.Type: GrantFiled: May 26, 1988Date of Patent: January 29, 1991Assignee: Hoechst AktiengesellschaftInventors: Gunter Scherowsky, Jurgen Gay, Hans-Rolf Dubal, Claus Escher, Wolfgang Hemmerling, Ingrid Muller, Dieter Ohlendorf, Rainer Wingen
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Patent number: 4987132Abstract: A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity.Type: GrantFiled: August 16, 1988Date of Patent: January 22, 1991Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Toshiyasu Mase, Hiromu Hara, Hitoshi Nagaoka, Takumi Takahashi, Takeshi Suzuki, Kenichi Tomioka, Toshimitsu Yamada
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Patent number: 4985411Abstract: The present invention provides compounds of the formula (I): ##STR1## wherein m and n are independently selected from 0, 1 or 2, ##STR2## R is selected from hydrogen, methyl or ethyl; R.sup.1 is selected from C.sub.1-4 hydrocarbyl substituted by one to five halo atoms, and a group --C.tbd.C--R.sup.9 wherein R.sup.9 is a group S(O).sub.w --R.sup.10 wherein R.sup.10 is trifluoromethyl, methyl or ethyl and w is 0, 1 or 2 or R.sup.9 is a C.sub.3-5 aliphatic group or an aliphatic group containing up to 5 carbon atoms atoms substituted by C.sub.1-4 alkoxy, C.sub.2-6 alkoxyalkoxy, C.sub.1-8 acyloxy, halo or hydroxy, a group COR.sup.11 wherein R.sup.11 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or a group NR.sup.12 R.sup.13 wherein R.sup.12 and R.sup.13 are independently selected from hydrogen, methyl or ethyl, or R.sup.9 is SiR.sup.14 R.sup.15 R.sup.16 wherein R.sup.14 to R.sup.16 are the same or different and each is a C.sub.1-4 aliphatic group or R.sup.14 and R.sup.15 are C.sub.1-4 aliphatic groups and R.sup.Type: GrantFiled: November 29, 1989Date of Patent: January 15, 1991Assignees: The Wellcome Foundation Ltd., The Regents of the University of CaliforniaInventors: John E. Casida, Michael Elliott
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Patent number: 4925590Abstract: Derivatives of 4-cyano-2,3-difluorophenol of the formula I ##STR1## wherein R.sup.1 is an alkyl group which has 1-12 C atoms and in which one or two CH.sub.2 groups can also be replaced by --O--, --CO--, --CO--O-- and/or --CH.dbd.CH--, no two 0 atoms being directly attached to one another,A.sup.1 and A.sup.2 independently of one another are each 1,4-phenylene which is unsubstituted or substituted by one or two F atoms, and in which one or two CH groups can also be replaced by N, or trans-1,4-cyclohexylene in which one or two non-adjacent CH.sub.2 groups can also be replaced by 0 atoms and/or S atoms,Z is --CO--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, OCH.sub.2 --, --CH.sub.2 O, --C.tbd.C-- or a single bond,m is 0, 1 or 2 andQ is --CO-- or --CH.sub.2 --.Type: GrantFiled: March 9, 1989Date of Patent: May 15, 1990Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Volker Reiffenrath, Joachim Krause, Andreas Wachtler, Georg Weber, Ulrich Finkenzeller
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Patent number: 4898986Abstract: Disclosed is a novel inosose compound represented by the general formula: ##STR1## wherein X.sup.1 and X.sup.2 are both halogen; X.sup.1 is hydrogen and X.sup.2 is halogen; or X.sup.1 is --SQ.sup.1 and X.sup.2 is --SQ.sup.2 (each of Q.sup.1 and Q.sup.2 is lower alkyl or Q.sup.1 and Q.sup.2 may form lower alkylene), R.sup.1 is a protective group for hydroxyl and Y is .dbd.O, .dbd.N--Z (Z is hydroxyl which may be protected) or ##STR2## (A is hydrogen or an amine residue), particularly to the compound wherein the symbol Y is oxygen.The inosose compound is useful as intermediates for production of valiolamine and the N-substituted derivatives thereof, which have potent .alpha.-glucosidase inhibiting activities and are useful as preventives or therapeutics for symptoms of hyperglycemia and various diseases derived therefrom in human and animals, such as diabetes, obesity and hyperlipemia.Type: GrantFiled: August 31, 1987Date of Patent: February 6, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Satoshi Horii, Hiroshi Fukase
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Patent number: 4889939Abstract: Compounds suitable for being used as lubricants, having general formula:(I) RO--(C.sub.3 F.sub.6 O).sub.m --(CFXO).sub.n --CFX--L, or(II) R"CFXO--(C.sub.3 F.sub.6 O).sub.x (CFXO).sub.y --(C.sub.2 F.sub.4 O).sub.z --CFX--L, whereR=--CF.sub.3, --C.sub.2 F.sub.5, --C.sub.3 F.sub.7X=F, --CF.sub.3R"=F, --CF.sub.3, --C.sub.2 F.sub.5m=an integer from 3 to 100n=a finite integer, or =zero, wherefore m+n ranges from 3 to 100, provided that, if n is finite, m/n ranges from 5 to 20 and R is preferably =CF.sub.3, if n=zero, R is preferably --C.sub.2 F.sub.5 or --C.sub.3 F.sub.7x=a finite integer, or =zeroy, z=finite integers, such that x+y+z ranges from 5 to 200, while (x+z)/y ranges from 5 to 0.5, provided that when x=zero, z/y ranges from 1 to 0.5 and y+z ranges from 5 to 200 n while X is preferably F, and R"=LL=group Y-Z, where:Y=--CH.sub.2 O--, --CH.sub.2 --OCH.sub.2, --CF.sub.2, --CF.sub.Type: GrantFiled: April 11, 1988Date of Patent: December 26, 1989Assignee: Montedison S.p.A.Inventors: Gerardo Caporiccio, Ezio Strepparola, Mario A. Scarati
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Patent number: 4877779Abstract: Novel compounds and their salts are disclosed having the Formulas: ##STR1## wherein: R.sub.1 is hydrogen, phenyl, 9H-fluoren-9-yl, 10,11-dihydro-5H-dibenzo [a,d]cyclohepten-5-yl, 5H-dibenzo[a,d]cyclohepten-5-yl, 1,2,3,4-tetrahydro-1-naphthyl, 9H-xanthen-9-yl, 9H-thioxanthen-9-yl, 2-chloro-9H-thioxanthen-9-yl, 4H-chromanyl, diphenylmethyl, phenylcycloalkylmethyl wherein the bridgehead methylene may optionally be substituted with a hydroxy group and any of the phenyl or benzo-fused rings may be substituted with one or more R.sub.5 groups wherein R.sub.5 is selected from halogen, trifluoromethyl, lower alkyl, hydroxy or lower alkoxy groups; andR.sub.2 and R.sub.3, which may be the same or different, are hydrogen, lower alkyl, phenylalkyl (C.sub.1 -C.sub.5), wherein the phenyl ring may be substituted with one or more R.sub.5 groups or NR.sub.2 R.sub.Type: GrantFiled: May 17, 1988Date of Patent: October 31, 1989Assignee: Marion Laboratories, Inc.Inventors: Waclaw J. Rzeszotarski, Maria E. Guzewska, John P. Carter, Theodore C. Adams, Andrea C. Dupont, Carl Kaiser
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Patent number: 4855213Abstract: Polymethine dyes are disclosed containing an acidic electron accepting terminal nucleus comprised of an isocyano group. The dyes are useful as spectral sensitizers in ultravioilet responsive imaging compositions.Type: GrantFiled: April 20, 1988Date of Patent: August 8, 1989Assignee: Eastman Kodak CompanyInventor: Margaret E. Logan