The Two Cyclos Share At Least Three Ring Members (i.e., Bridged) Patents (Class 549/363)
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Publication number: 20150104437Abstract: The present invention relates to methods of the treatment and diagnosis of bone mineral density related disorders. More particularly, the present invention relates to a method of diagnosing or predicting a hone mineral density related disease, or a risk of a bone mineral density related disease, in a subject, which method comprises detecting a mutation in the TBXAS1 gene, wherein the presence of said mutation is indicative of a bone mineral density related disease or of a risk of a bone mineral density related disease. The invention also relates to a compound selected in the group consisting of a thromboxane synthase (TXAS) encoding polynucleotide, a TXAS, thromboxane A2 or an analog thereof for treating or preventing a disease associated with an increased bone mineral density (e.g., Ghosal hematodiaphyseal dysplasia syndrome).Type: ApplicationFiled: December 19, 2014Publication date: April 16, 2015Inventors: Valerie Cormier-Daire, Arnold Munnich
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Publication number: 20150060732Abstract: An object is to provide a liquid crystal compound satisfying at least one of physical properties such as a high stability to heat and light, a high clearing point, a low minimum temperature of a liquid crystal phase, a small viscosity, a suitable optical anisotropy, a large dielectric anisotropy, a suitable elastic constant and an excellent compatibility with other liquid crystal compounds, a liquid crystal composition containing the compound, and a liquid crystal display device including the composition. A solution is a compound represented by formula (1). In formula 1, R1 is alkyl having 1 to 10 carbons, for example; ring A1 and ring A2 are independently 1,4-cyclohexylene or 1,4-phenylene; Z1 and Z2 are independently a single bond or —CF2O—; L1 and L2 are halogen; and a is 1 or 2.Type: ApplicationFiled: August 27, 2014Publication date: March 5, 2015Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATIONInventors: Yasuyuki GOTOH, Masakazu YANO
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Publication number: 20140296541Abstract: A compound is provided that is useful for, among other things, preparing water-soluble polymer derivatives bearing a terminal N-succinimidyl ester.Type: ApplicationFiled: June 12, 2014Publication date: October 2, 2014Inventor: Antoni Kozlowski
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Publication number: 20140203209Abstract: An object is to provide a liquid crystal compound satisfying at least one of physical properties such as a high stability to heat, light and so forth, a high clearing point, a low minimum temperature of a liquid crystal phase, a small viscosity, a suitable optical anisotropy, a large dielectric anisotropy, a suitable elastic constant and an excellent compatibility with other liquid crystal compounds, a liquid crystal composition containing the compound, and a liquid crystal display device including the composition. A solution is the compound represented by formula (1): wherein, in formula (1), for example, R1 is alkyl having 1 to 10 carbons; ring A1 and ring A2 are independently 1,4-cyclohexylene or 1,4-phenylene; Z1 and Z2 are independently a single bond or —CF2O—; L1 and L2 are halogen; and a is 1 or 2.Type: ApplicationFiled: January 21, 2014Publication date: July 24, 2014Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATIONInventors: Yasuyuki GOTOH, Kenji HIRATA
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Publication number: 20140145113Abstract: A liquid crystal compound having high stability to heat, light and so forth, a high clearing point, a low minimum temperature of a liquid crystal phase, small viscosity, suitable optical anisotropy, large dielectric anisotropy, a suitable elastic constant and excellent compatibility with other liquid crystal compounds, a liquid crystal composition containing the compound, and a liquid crystal display device including the composition. The compound is represented by formula (1-1): wherein, for example, R1 is hydrogen, halogen or alkyl having 1 to 20 carbons; ring A1, ring A2, ring A3, ring A4 and ring A5 are independently 1,4-cyclohexylene or 1,4-phenylene; Z1, Z2, Z3 and Z4 are independently a single bond, —(CH2)2—, —CH?CH— or —CF?CF—: and a, b, c and d are independently 0 or 1, and a sum of a, b, c and d is one or more.Type: ApplicationFiled: November 26, 2013Publication date: May 29, 2014Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATIONInventors: Tomohiro YANO, Junichi YAMASHITA
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Publication number: 20140021407Abstract: The invention is to provide a liquid crystal compound having a large dielectric anisotropy, a high voltage holding ratio and stability to heat, light and so forth, maintaining a nematic phase in a wide temperature range, having a suitable optical anisotropy and an excellent compatibility with other liquid crystal compounds, particularly, to provide a liquid crystal compound having a large dielectric anisotropy. The invention provides compound (1): In the formula, for example, R1 is alkyl having 1 to 20 carbons; ring A1, ring A2, ring A3, ring A4, ring A5 and ring A6 are independently 1,4-cyclohexylene or 1,4-phenylene; Z1, Z2, Z3, Z4, Z5, Z6 and Z7 are independently a single bond, —(CH2)2—, —COO—, —OCO—, —CF2O—, —OCF2— or —CH?CH—; X1 is fluorine, —CF3 or —OCF3; and Y1 and Y2 are independently hydrogen or fluorine.Type: ApplicationFiled: March 7, 2012Publication date: January 23, 2014Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATIONInventor: Tokifumi Masukawa
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Patent number: 8563779Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.Type: GrantFiled: July 19, 2011Date of Patent: October 22, 2013Assignee: Bayer CropScience AGInventors: Hartmut Ahrens, Andreas Van Almsick, Elmar Gatzweiler, Dieter Feucht, Isolde Haeuser-Hahn, Stefan Lehr, Christopher Hugh Rosinger
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Publication number: 20130078272Abstract: Antifungal compounds, an antifungal compound extracted from Epicoccum purpurascens, also known as Epicoccum nigrum, methods of producing the antifungal compounds, isolates and compositions comprising the antifungal compounds, and methods of using the antifungal compounds.Type: ApplicationFiled: December 9, 2010Publication date: March 28, 2013Applicant: Auckland UniServices LimitedInventor: Silas Granato Villas-Boas
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Publication number: 20110098488Abstract: Oxidation of organic substrates by means of singlet oxygen, in which organic substrates which react with 1O2 are admixed with 10-70% H2O2 in an organic solvent in the presence of a molybdate LDH catalyst modified by ethylene glycol, polyethylene glycol or polyol, and the catalytic decomposition of H2O2 to water and 1O2 is then followed by the oxidation to the corresponding oxidation products, and also modified molybdate LDH catalysts.Type: ApplicationFiled: March 18, 2006Publication date: April 28, 2011Inventors: Dirk De Vos, Pierre Jacobs, Joos Wahlen, Paul Alsters, Walther Jary
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Patent number: 7531657Abstract: A method for preparing a compound represented by the following general formula (5) where, n is an integer of 0 to 3; and Y represents a protecting group for an amino group, the method including the steps of reacting a compound represented by the following general formula (3) where n and Y are as described above, with a silylating agent, and subsequently reacting it with P (?O) T3, where T represents a halogen atom, and further with ammonia.Type: GrantFiled: December 16, 2002Date of Patent: May 12, 2009Assignee: Nippon Kayaku Kabushiki KaishaInventors: Masashi Nagai, Hiroko Yamazaki, Keiichirou Yamamoto, Masatoshi Abe
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Publication number: 20090023926Abstract: The present invention provides a compound of the formula: (IIa); having a reactive functional group M, capable of reacting with a biopolymer, BP, having at least one group capable of reacting with M to form a covalent linkage, to provide a biopolymer derivative of the formula: (IIIa). The biopolymer derivatives of the invention have enhanced ionisability with respect to free 10 biopolymer (Bp) enabling improved analysis of the biopolymer using mass spectrometry. The invention further provides specific examples of compounds formula (IIa), e.g. compounds of formula: (IIa-2a) and (IIa-58a).Type: ApplicationFiled: September 22, 2005Publication date: January 22, 2009Inventors: Edwin Mellor Southern, Vladimir Korshun, Mikhail Sergeevich Shchepinov
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Patent number: 6894176Abstract: Certain multi-substituted dibenzylidene sorbitol acetals having electron withdrawing groups as constituents and electron donating groups on the other such that the compounds are asymmetric in structure and are dipolar in nature are provided. Polymer compositions comprising such compounds, are also contemplated which may be utilized within, as merely examples, food or cosmetic containers and packaging. These inventive asymmetric dipolar dibenzylidene sorbitol acetals are also useful as gelling agents for water and organic solvents, particularly those used in the preparation of antiperspirant gel sticks.Type: GrantFiled: November 1, 2002Date of Patent: May 17, 2005Assignee: Milliken & CompanyInventors: Darin L. Dotson, Brian M. Burkhart, John D. Anderson, Jeffrey R. Jones, Shawn R. Sheppard
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Patent number: 6864282Abstract: 9,11-Cycloendoperoxide derivatives of biologically active prostaglandin analogs, and particularly of the ocular hypotensive drugs Bimatoprost, Latanaprost, Unoprostone, Travoprost and prostaglandin H2 1-ethanolamide or of structurally closely related analogs, are pro-drugs which hydrolyze under physiological conditions to provide prostaglandin analogues that are capable of providing sustained ocular and other in vivo concentrations of the respective drugs. The compounds of the invention have the formula shown below where the variables have the meaning defined in the specification.Type: GrantFiled: August 5, 2002Date of Patent: March 8, 2005Assignee: Allergan, Inc.Inventors: Kah-Hiing John Ling, Wu Yang, Jinsong Ni, Haiqing Yuan, Diane D. S. Tang-Liu
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Patent number: 6734238Abstract: Plastic additives which are useful as nucleating agents and which are especially useful for improving the optical properties of polymeric materials are provided. More particularly, this invention relates to certain alkyl (or alkoxy) substituted fluoro-benzylidene sorbitol acetals and polymer compositions thereof which may be utilized within, as merely examples, food or cosmetic containers and packaging. These inventive fluorinated and alkylated benzylidene sorbitol acetals are also useful as gelling agents for water and organic solvents, particularly those used in the preparation of antiperspirant gel sticks.Type: GrantFiled: January 7, 2003Date of Patent: May 11, 2004Assignee: Milliken & CompanyInventors: John D. Anderson, Nathan A. Mehl
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Publication number: 20030171423Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.Type: ApplicationFiled: January 7, 2003Publication date: September 11, 2003Inventors: John W. Erickson, Michael Eissenstat, Abelardo Silva, Sergei Gulnik
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Patent number: 6593479Abstract: The invention pertains to a coating composition comprising a first compound comprising at least one bicyclo- or spiro-orthoester group and a second compound comprising at least two hydroxyl-reactive groups. The invention also comprises a process for curing the present coating composition. More particularly, the latent hydroxyl groups of the bicyclo- or spiro-orthoester groups have to be deblocked and reacted with the hydroxyl-reactive groups of the second compound if the present coating composition is to be cured. Further, a process for making bicyclo-orthoester compounds from the corresponding oxetane compound is described, as are polymers comprising at least one bicyclo- or spiro-orthoester group.Type: GrantFiled: August 22, 2001Date of Patent: July 15, 2003Assignee: Akzo Nobel N.V.Inventors: Keimpe Jan van den Berg, Klaus Hobel, Huig Klinkenberg, Arie Noomen, Josephus Christiaan van Oorschot
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Patent number: 6555696Abstract: Certain multi-substituted dibenzylidene sorbitol acetals having electron withdrawing groups as constituents and electron donating groups on the other such that the compounds are asymmetric in structure and are dipolar in nature are provided. Polymer compositions comprising such compounds, are also contemplated which may be utilized within, as merely examples, food or cosmetic containers and packaging. These inventive asymmetric dipolar dibenzylidene sorbitol acetals are also useful as gelling agents for water and organic solvents, particularly those used in the preparation of antiperspirant gel sticks.Type: GrantFiled: March 23, 2001Date of Patent: April 29, 2003Assignee: Milliken & CompanyInventors: Darin L. Dotson, Brian M. Burkhart, John D. Anderson, Jeffrey R. Jones, Shawn R. Sheppard
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Patent number: 6518302Abstract: Compounds represented by general formula (I) wherein X represents OH or OSO3H; and R represents a substituent other than OH which allows, after leaving, the induction of unsaturated bonds into the 3- and 4-positions of 3,6-anhydrogalactose or its sulfated derivative, and/or a substituent showing a tissue-specific affinity.Type: GrantFiled: July 20, 2001Date of Patent: February 11, 2003Assignee: Takara Shuzo Co., Ltd.Inventors: Eiji Kobayashi, Tuo-Ping Li, Tatsuji Enoki, Takanari Tominaga, Hiroaki Sagawa, Ikunoshin Kato
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Patent number: 6500964Abstract: This invention relates to a process for preparing alditol acetals, such as dibenzylidene sorbitols, monobenzylidene sorbitols, and the like, through the reaction of unsubstituted or substituted benzaldehydes with alditols (such as sorbitol, xylitol, and ribitol) in the presence of a mineral acid and at least one surfactant having at least one pendant group of 6 carbon chains in length. Such a reaction provides a cost-effective, relatively safe procedure that provides excellent high yields of alditol acetal product. Furthermore, such a specific reaction is also the best known procedure for the production of certain compounds which can be easily separated from other formed isomers. Additionally, such a procedure facilitates the production of certain asymmetric alditol acetal compounds and compositions in acceptable yields as well. Such alditol acetals are useful as nucleating and clarifying agents for polyolefin formulations and articles, as one example.Type: GrantFiled: March 23, 2001Date of Patent: December 31, 2002Assignee: Milliken & CompanyInventors: John G. Lever, Darin L. Dotson, John D. Anderson, Jeffrey R. Jones, Shawn R. Sheppard
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Patent number: 6476240Abstract: This invention relates to a monomer shown by the general formula [1] (wherein X′ is a cyclic hydrocarbon residue containing polymerizable double bond(s), which may have a substituent, Z is a spacer or a direct bond and R is a substituted alkyl or alkenyl group having one or two protected hydroxyl groups as substituent) and a polymer containing a segment derived from the above monomer. The said polymer is useful for a resist composition, etc. utilized in the production of semiconductor elements, etc. and the said monomer is useful as a starting material for the polymer, and a resist composition using the said polymer can remarkably advantageously be used as a resist material for ArF excimer laser beams which has been considered to be a valuable technology for exposure belonging to the coming generation.Type: GrantFiled: October 16, 2001Date of Patent: November 5, 2002Assignee: Wako Pure Chemical Industries, Ltd.Inventor: Motoshige Sumino
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Patent number: 6166065Abstract: 2,3-Dioxabicyclo[3.3.1]nonane derivatives, carrying, at position 4, a sulfur-containing functionality selected from the group consisting of sulfonyl, sulfinyl and sulfenyl, adhered to C(4) vie methylene group, represented by structural formula (A) wherein: X is hydrogen, hydroxy, alkoxy, optionally substituted by alkoxy or acyloxy, aralkoxy optionally substituted by alkoxy or aryloxy, and M is hydrogen, hydroxy, alkoxy, alkenyloxy, acyloxy, optionally substituted by acyl or acyloxy, aralokoxy, arylalkenyloxy, oxalyloxy substituted by alkoxy, di(alkyl)amino or alkyl(aryl)amino, di(aralalkyl)amino or carbonyloxy substituted by arloxy, di(alkyl)amino, di(aralkyl)amino and alkyl(aryl)amino; or X and M together represent a carbon-carbon bond or an oxygen atom; L is hydrogen or L and M together represent a carbon-carbon bond; and either Z is a radical R--S(=O).sub.n -- and Y is hydrogen, or Y is R--S(=O).sub.Type: GrantFiled: May 11, 2000Date of Patent: December 26, 2000Assignees: Yeda Research and Development Co., Ltd., Johns Hopkins UniversityInventors: Mario Bachi, Gary H. Posner, Edward Korshin
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Patent number: 5817692Abstract: The present invention relates to novel biologically-active organic peroxides and to novel uses of both known and new organic peroxides. More specifically, this invention details organic endoperoxides having antiparasitic activity, methods for their preparation and methods for treating malaria and cerebral toxoplasmic encephalitis with the organic endoperoxides.Type: GrantFiled: August 22, 1996Date of Patent: October 6, 1998Assignee: The Johns Hopkins UniversityInventor: Gary H. Posner
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Patent number: 5672718Abstract: The present invention relates to novel N-phenylacetamino nitriles of the general formula (I), ##STR1## in which R.sup.1 represents hydrogen, or represents alkyl, alkenyl, cycloalkyl, aryl or heterocyclyl which are in each case optionally substituted, andR.sup.2 represents hydrogen, or represents alkyl which is optionally substituted, orR.sup.1 and R.sup.2, together with the carbon atom to which they are bonded, represent cycloalkyl or heterocyclyl which are in each case optionally substituted,R.sup.3 represents halogen, alkyl or alkoxy,R.sup.4 represents hydrogen, halogen, alkyl, halogenoalkyl or alkoxy,R.sup.5 represents halogen, alkyl or alkoxy, andm represents a number 0, 1, 2 or 3, processes for their preparation and their use for the preparation of agents for controlling pests.Type: GrantFiled: November 15, 1995Date of Patent: September 30, 1997Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Gunther Beck
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Patent number: 5606037Abstract: This invention relates to a naphthoquinone derivatives, to processes and to intermediates for preparing these derivatives, to pharmaceutical composition and to the use of these derivatives as antitumor agents in mammals.Type: GrantFiled: March 10, 1995Date of Patent: February 25, 1997Assignee: BioChem Pharma Inc.Inventors: Giorgio Attardo, Tibor Breining, Marc Courchesne, Serge Lamothe, Jean-Fran.cedilla.ois Lavall ee, Dieu Nguyen, Rabindra Rej, Yves St-Denis, Wuyi Wang, Yao-Chang Xu, France Barbeau, Elaine Lebeau, Jean L. Kraus
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Patent number: 5506262Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthetase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.Type: GrantFiled: November 10, 1993Date of Patent: April 9, 1996Assignee: Merck & Co., Inc.Inventors: Robert M. Burk, William H. Parsons, John J. Acton, III, Gregory D. Berger, Tesfaye Biftu, Robert L. Bugianesi, Yuan-Ching P. Chiang, Claude Dufresne, Narindar N. Girotra, Robert W. Marquis, Jr., Chan-Hwa Kuo, Sandra P. Plevyak, Mitree M. Ponpipom, Lori L. Whiting, James D. Bergstrom, Conrad Santini
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Patent number: 5468771Abstract: A compound of structural formula ##STR1## having antihypercholesterolemic utility is produced by culturing a Streptomyces sp.Type: GrantFiled: February 2, 1994Date of Patent: November 21, 1995Assignee: Merck & Co., Inc.Inventors: Magda M. Gagliardi, Shieh-Shung T. Chen, Byron H. Arison, George M. Garrity, Leeyuan Huang, John G. MacConnell, Raymond F. White
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Patent number: 5409950Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom, a hydroxyl group or a group selected from --OCOCH.dbd.CHCH(CH.sub.3)(CH.sub.2).sub.3 CH.sub.3, --OCOCH.dbd.CHC(CH.sub.3).dbd.CHCH(CH.sub.3)--CH.sub.2 CH.sub.3, or --OCO--X--CH.sub.2 CH(CH.sub.3)CH.sub.2 CH.sub.3 [where X is --CH.dbd.CHCH(CH.sub.3)--, --CH.sub.2 CH(OH)CH(CH.sub.3)--, --CH.dbd.CHC(OH)(CH.sub.3)--, --CH.sub.2 CH(OH)CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH(CH.sub.3)--)];R.sub.2 represents a hydrogen atom or a hydroxyl group;R.sub.3 represents a group selected from --C(.dbd.CH.sub.2)CH(OR.sub.7)CH(CH.sub.3)CH.sub.2 Ph (where R.sub.7 is a hydrogen atom or an acetyl group), --C(CH.sub.3).dbd.CHCH(CH.sub.2 R.sub.8)CH.sub.2 Ph (where R.sub.8 is a hydrogen or a hydroxyl group), --C(CH.sub.2 OH).dbd.CHCH(CH.sub.3)CH.sub.2 Ph, --C(.dbd.CH.sub.2)CH(OH)CH(CH.sub.2 OH)CH.sub.2 Ph, --C(.dbd.CH.sub.2)CH(NHCOCH.sub.3)CH(CH.sub.3)CH.sub.2 Ph, --C(CH.sub.2 NHCOCH.sub.3).dbd.CHCH(CH.sub.3)CH.sub.2 Ph or ##STR2## R.sub.4, R.Type: GrantFiled: October 26, 1993Date of Patent: April 25, 1995Assignee: Glaxo Group LimitedInventors: Michael J. Dawson, Allan Baxter, Robert M. Tait, Nigel S. Watson, David Noble, Alan Shuttleworth, Howard G. Wildman, Michael V. Hayes
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Patent number: 5369125Abstract: This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer.Type: GrantFiled: March 19, 1993Date of Patent: November 29, 1994Assignee: Merck & Co., Inc.Inventors: Gregory D. Berger, James D. Bergstrom, Tesfaye Biftu, Robert L. Bugianesi, Robert M. Burk, Narindar N. Girotra, C. H. Kuo, William H. Parsons, Mitree M. Ponpipom, Lori L. Whiting
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Patent number: 5359096Abstract: New cholesterol lowering compounds are formed from the photochemical treatment of the zaragozic acids.Type: GrantFiled: November 20, 1992Date of Patent: October 25, 1994Assignee: Merck & Co., Inc.Inventors: Laszlo R. Treiber, Byron H. Arison, Shieh-Shung T. Chen, George A. Doss, Leeyuan Huang, John G. MacConnell
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Patent number: 5332814Abstract: Process for the preparation of racemic compounds of the formula I ##STR1## or enantiomers thereof, in which B is the radical of a nucleic base from the series comprising purine, a purine analogue or a pyridine analogue, and R is H or a protective group R.sub.1, by reactinga) a compound of the formula II or enantiomer thereof ##STR2## with a compound of the formulae X--CO--X, X--CS--X, X--SO--X, X--SO.sub.2 --X, R.sub.2 --NCO, R.sub.3 R.sub.4 N--C(O)--R.sub.5, X.sub.2 P--R.sub.6 or X.sub.2 P(O)--R.sub.6, in which X is a leaving group, R.sub.2 is, for example, C.sub.1 -C.sub.18 alkyl, R.sub.3 and R.sub.4 are, for example, H or C.sub.1 -C.sub.18 alkyl, R.sub.5 is, for example, H or C.sub.1 -C.sub.12 alkyl, and R.sub.6 is, for example, C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.12 alkoxy, to give a compound of the formula III or enantiomers thereof ##STR3## in which Y is the groups --C(O)--, --C(S)--, --SO--, --SO.sub.2 --, R.sub.2 NH--CH.dbd., R.sub.3 R.sub.4 N--CR.sub.5 .dbd., R.sub.6 P.dbd. and R.sub.6 (O)P.Type: GrantFiled: October 30, 1992Date of Patent: July 26, 1994Assignee: Ciba-Geigy CorporationInventor: Heinz Moser
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Patent number: 5326783Abstract: This invention is directed to compounds of formula (I) which are novel C3- or C5-acyl sulfonamide, carboxamic acid or tetrazolyl analogs of the Zaragozic acids. These compounds inhibit the enzyme squalene synthase and are useful as cholesterol lowering agents.Type: GrantFiled: January 19, 1993Date of Patent: July 5, 1994Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Chan-Hwa Kuo, Conrad Santini
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Patent number: 5322855Abstract: Zaragozic acids isolated from a culture of MF5465 have been subjected to photoreaction, then derivatized at the 4-keto position. The resulting derivatives are active as squalene synthetase inhibitors and are useful in the treatment of hypercholesterolemia.Type: GrantFiled: November 24, 1992Date of Patent: June 21, 1994Assignee: Merck & Co., Inc.Inventors: Laszlo R. Treiber, Doss, George A., Byron H. Arison
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Patent number: 5310949Abstract: New Zaragozic acids have been isolated from a culture of MF5465. These compounds and their derivatives are active as squalene synthetase inhibitors and are useful in the treatment of hypercholesterolemia.Type: GrantFiled: September 2, 1992Date of Patent: May 10, 1994Assignee: Merck & Co., Inc.Inventors: Claude Dufresne, Prakash S. Masurekar, Leslie A. Ferrell, Deborah L. Zink, Margaret S. Sosa
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Patent number: 5302604Abstract: Compounds of Structural Formula (I) ##STR1## are produced by directed biosynthesis. These compounds are squalene synthetase inhibitors and thus useful as cholesterol lowering agents, antifungal agents and cancer treatment agents.Type: GrantFiled: October 6, 1992Date of Patent: April 12, 1994Assignee: Merck & Co., Inc.Inventors: Kevin M. Byrne, Shieh-Shung T. Chen, Louis Kaplan, John G. MacConnell, Brian R. Petuch, Raymond F. White, Byron H. Arison
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Patent number: 5298272Abstract: A sugar substitute which is identified as N-(L)-aspartyl-1-(1'-aminoethyl)-4-methyl-2,6,7-trioxabicyclo[2,2,2]octane . The compound is a bridged carboxylic ortho ester which has an intense sweet taste and is suitable for use as a sugar substitute.Type: GrantFiled: December 2, 1992Date of Patent: March 29, 1994Assignee: The Regents of the University of CaliforniaInventors: Murray Goodman, Yeong S. Oh
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Patent number: 5294638Abstract: Pharmacologically active compounds corresponding to the general formula I: ##STR1## wherein m represents 1-4,n represents 2-5,R.sup.1 is hydrogen or lower alkyl,R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, andR.sup.3 is hydrogen, lower alkyl, lower alkoxy or halogen, orR.sup.2 and R.sup.3 are linked to adjacent carbon atoms and together form an alkylenedioxy group with 1-2 carbon atoms,R.sup.4 represents a saturated monocyclic or bicyclic hydrocarbon radical derived from terpenes and having 10 or 11 hydrocarbon atoms, andZ represents oxygen, an N--R.sup.5 group, wherein R.sup.5 is lower alkyl, or if R.sup.4 is a dihydronopyl radical, Z may also be sulfur,and their acid addition salts.Type: GrantFiled: January 19, 1993Date of Patent: March 15, 1994Assignee: Kali-Chemie Pharma GmbHInventors: Insa Hell, Ulf Preuschoff, Hermann Kraehling, Samuel David, Ivan Ban, Marie-Odile Christen
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Patent number: 5294627Abstract: Compounds of Structural Formula (I) ##STR1## are produced by directed biosynthesis. These compounds are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer.Type: GrantFiled: August 27, 1992Date of Patent: March 15, 1994Assignee: Merck & Co., Inc.Inventors: Bryon H. Arison, Shieh-Shung T. Chen, Raymond F. White, Brian R. Petuch
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Patent number: 5283256Abstract: This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer. This invention also relates to a process for obtaining compounds of structural formula (I).Type: GrantFiled: July 22, 1992Date of Patent: February 1, 1994Assignee: Merck & Co., Inc.Inventors: Claude Dufresne, Josep Guarro, Leeyuan Huang, Yu L. Kong, Russell B. Lingham, Maria S. Meinz, Keith C. Silverman, Sheo B. Singh
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Patent number: 5278320Abstract: Compounds of Structural Formula (I) ##STR1## are produced by chemical modification of directed biosynthesis products. These compounds are squalene synthetase inhibitors and thus useful as cholesterol lowering agents, antifungal agents and cancer treatment agents.Type: GrantFiled: September 11, 1992Date of Patent: January 11, 1994Assignee: Merck & Co., Inc.Inventor: Richard L. Monaghan
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Patent number: 5274157Abstract: Compounds of the formula Ib ##STR1## in which R.sub.1 and R.sub.2 independently of one another are linear or branched C.sub.1 -C.sub.12 alkyl, cycloalkyl having 5 to 8 ring carbon atoms, phenylalkyl having 1 to 4 C atoms in the alkylene group, the cyclic radicals being unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, or R.sub.1 and R.sub.2 independently of one another are --SiR.sub.4 R.sub.5 R.sub.6 in which R.sub.4, R.sub.5 and R.sub.6 independently of one another are C.sub.1 -C.sub.12 alkyl, phenyl, benzyl, or phenyl or benzyl, each of which is substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, and R.sub.3 is a bridging member which, together with the radical --OCH--CH.sub.2 --CHO-- to which it is bonded, forms a 6- to 8-membered ring. These compounds are valuable intermediates for the preparation of carbacyclic nucleosides of the natural and unnatural series and of the racemates.Type: GrantFiled: October 30, 1992Date of Patent: December 28, 1993Assignee: Ciba-Geigy CorporationInventor: Heinz Moser
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Patent number: 5270332Abstract: This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents. The compounds also exhibit antifungal activity and are inhibitors of farnesyl-protein transferase.Type: GrantFiled: August 21, 1992Date of Patent: December 14, 1993Assignee: Merck & Co., Inc.Inventors: Shieh-Shung T. Chen, Leeyuan Huang, John G. MacConnell, Jon D. Polishook, Raymond F. White
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Patent number: 5264593Abstract: This invention relates to compounds of structural formula ##STR1## which are inhibitors of squalene synthase and useful as cholesterol lowering agents.Type: GrantFiled: January 15, 1993Date of Patent: November 23, 1993Assignee: Merck & Co., Inc.Inventor: Laszlo R. Treiber
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Patent number: 5262435Abstract: A new Zaragozic acid analog has been isolated from a culture of MF5453. The compound and its derivatives are active as squalene synthetase inhibitors and are useful in the treatment of hypercholesterolemia.Type: GrantFiled: February 10, 1992Date of Patent: November 16, 1993Assignee: Merck & Co., Inc.Inventors: Henry Joshua, Guy H. Harris
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Patent number: 5260332Abstract: New Zaragozic acids have been isolated from a culture of MF5465. These compounds and their derivatives are active as squalene synthetase inhibitors and are useful in the treatment of hypercholesterolemia.Type: GrantFiled: February 7, 1992Date of Patent: November 9, 1993Assignee: Merci & Co., Inc.Inventor: Claude Dufresne
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Patent number: 5258401Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.Type: GrantFiled: September 10, 1992Date of Patent: November 2, 1993Assignee: Merck & Co., Inc.Inventors: Gregory D. Berger, Robert W. Marquis, Jr., Albert J. Robichaud, Edward M. Scolnick
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Patent number: 5256689Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents and as inhibitors of squalene synthase.Type: GrantFiled: October 26, 1992Date of Patent: October 26, 1993Assignee: Merck & Co., Inc.Inventor: Yuan-Ching P. Chiang
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Patent number: 5241104Abstract: Optically active mono-esters of dicarboxylic acid of the formula III: ##STR1## being useful as intermediates for preparing optically active natural products or medicines; asymmetric synthesis process for preparing thereof being characterized by the reaction of an acid anhydride with an (R)- or (S)-arylacetic acid derivative; and the key substances therefor are also claimed.Type: GrantFiled: June 23, 1992Date of Patent: August 31, 1993Assignee: Shionogi & Co., Ltd.Inventors: Mitsuaki Ohtani, Takaharu Matsuura
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Patent number: 5204333Abstract: The present invention provides compounds of the formula (I): ##STR1## wherein R is a phenyl group, substituted fluorine atoms formulations containing them and their use in controlling pest infestation.Type: GrantFiled: February 24, 1992Date of Patent: April 20, 1993Inventors: John P. Larkin, John B. Weston, Ian H. Smith, Christopher J. Palmer, John E. Casida
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Patent number: 5200513Abstract: To produce doxorubicin and its analogues methyl 3alpha, 5alpha-dihydroxy-5beta-(trimethylsilylethynyl)-2alpha-nitromethylcyclohexa ne-1beta-carboxylate acetonide is condensed with 1,4-dihydro-4,4,5-trimethoxy-1-oxonaphthalene in the presence of 1,8-diazabicyclo-[5.4.0]undec-7-ene in an aprotic solvent to produce 3-[ (2beta-carbomethoxy-4beta-ethynyl-4alpha, 6alpha-(di-O-isopropylidenyl)cyclohexanyl-1-yl]-nitromethyl-4,4,5-trimetho xy-1-oxo-1,2,3,4-tetrahydronaphthalene; which is cyclized to produce 9beta-ethynyl-12-hydroxy-7alpha,9alpha-(di-O-isopropylidenyl)-6-nitro-4,5, 5-trimethoxy-5,5a,6,6a,7,8,9,10,10a,11-decahydro -11-naphthacenone. The decahydro-11-naphthacenone is converted to 7alpha-9alpha,(di-O-isopropyl-idenyl)-4,5-dimethoxy-9beta-ethynyl-12-hydro xy-6-nitro-6,6a,7,8,9,10,10a,11-octahydro-11, -naphthacenone.Type: GrantFiled: June 22, 1990Date of Patent: April 6, 1993Assignee: Board of Regents, University of Nebraska-LincolnInventor: Desmond M. S. Wheeler
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Patent number: RE37087Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: June 20, 1991Date of Patent: March 6, 2001Assignee: Schering AktiengesellschaftInventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles