Cyclopentyl-coor, -c-coor Or -c-c-coor Patents (Class 560/122)
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Publication number: 20080319066Abstract: The present invention provides novel jasmonate derivative compounds, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for treatment of cancers, especially mammalian cancers.Type: ApplicationFiled: August 26, 2008Publication date: December 25, 2008Applicant: RAMOT AT TEL-AVIV UNIVERSITY LTD.Inventors: Eliezer FLESCHER, Yoel Kashman, Dorit Reischer, Shiri Shimony
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Publication number: 20080275247Abstract: The present invention relates to novel transition metal complexes of the formula (I) to a process for preparing these transition metal complexes and to the use of the transition metal complexes as catalysts in metathesis reactions.Type: ApplicationFiled: April 24, 2008Publication date: November 6, 2008Inventors: Renat Kadyrov, Anna Szadkowska, Karol Grela, Michal Barbasiewicz
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Patent number: 7442827Abstract: The present invention provide a process that allows the industrially advantageous production of a cyclopentanone-2,3,5-tricarboxylic acid triester. Namely, the present invention provides a process for producing a cyclopentanone-2,3,5-tricarboxylic acid triester represented by the general formula (IV), characterized by comprising: (1) allowing an itaconic acid diester represented by the general formula (I) to react with a metal salt of malonic acid diester represented by the general formula (II) to obtain a reaction mixture containing an adduct represented by the general formula (III); and then (2) allowing said reaction mixture to react with an alcohol or a metal alkoxide, or a mixture thereof: wherein R1, R2, R3, R4, R5, R6, and R7 each independently represents an alkyl group which may have a substituent, and M represents an alkali metal.Type: GrantFiled: May 10, 2005Date of Patent: October 28, 2008Assignee: Kuraray Co., Ltd.Inventors: Takashi Sugioka, Yoshimi Fukunaga
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Publication number: 20080249166Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.Type: ApplicationFiled: June 9, 2008Publication date: October 9, 2008Applicant: Esperion Therapeutics, Inc.Inventors: Jean-Louis Henri Dasseux, Daniela Carmen Oniciu
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Publication number: 20080242859Abstract: The present invention provides compounds which are useful as safe substitutes for the organotin reagent used in coupling reaction for the oxymethylation of aromatic rings, such as alkoxymethylation or hydroxymethylation, with a palladium catalyst and which can dispense with chromatographic purification with silica gel in the production and are suitable for mass production; and compounds applicable even to the oxymethylation of aromatic ring substrates which do not permit coupling reaction by conventional technique or have low reactivity.Type: ApplicationFiled: March 13, 2006Publication date: October 2, 2008Applicant: Eisai R&D Management Co., LtdInventors: Keigo Tanaka, Satoshi Inoue, Daisuke Ito, Norio Murai, Yosuke Kaburagi, Shuji Shirotori, Shuichi Suzuki, Yoshiaki Ohashi
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Publication number: 20080221240Abstract: The present invention generally provides compositions including carbon-containing molecules, and related methods. In some cases, the present invention relates to aromatic molecules comprising functional groups bonded to the aromatic portion of the molecule, including nonplanar portions of the molecules. Methods of the invention may provide the ability to introduce a wide range of functional groups to carbon-containing molecules. In some cases, methods of the invention may be performed using relatively mild reaction conditions, such as relatively low temperature, low pressure, and/or in the absence of strong acids or strong bases. The present invention may provide a facile and modular approach to synthesizing molecules that may be useful in various applications including photovoltaic devices, sensors, and electrodes (e.g., for electrocatalysis).Type: ApplicationFiled: March 7, 2008Publication date: September 11, 2008Applicant: Massachusetts Institute of TechnologyInventors: Timothy M. Swager, Wei Zhang
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Patent number: 7390779Abstract: Odourant compounds selected from compounds having the structure: wherein, R1 and R2 may be independently hydrogen or methyl, and n is an integer 1, 2 or 3 provided that n+ the carbon atoms in R1 and R2 is less than 5, their preparation and their use in fine fragrances and perfume components, wherein the compounds provide a musk characteristic.Type: GrantFiled: May 30, 2002Date of Patent: June 24, 2008Assignee: Givaudan SAInventors: Philip Kraft, Riccardo Cadalbert
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Cyclopentane carboxylate compounds, process and intermediates for preparing the same and use thereof
Patent number: 7388103Abstract: The present invention discloses cyclopentane carboxylate compounds. The 1-hydrocarbyl-2-acyloxy-cyclopentane carboxylates according to the invention have a general formula (I): wherein groups R1, R2 and R3, which are identical or different, are independently selected from the group consisting of linear or branched C1-C20alkyl, C3-C20cycloalkyl, C6-C20aryl, C7-C20alkaryl and C7-C20aralkyl. The present invention also discloses a process as well as intermediate compounds for preparing the compounds of formula (I), and use of the compounds (I) as electron donor in the preparation of catalysts for propylene polymerization.Type: GrantFiled: October 27, 2005Date of Patent: June 17, 2008Assignees: China Petroleum & Chemical Corporation, Beijing Research Institute of Chemical IndustryInventors: Lunjia Xie, Hongbin Du, Zhibiao Hu, Tianyi Zhang, Siyuan Zhao, Xinsheng Wang -
Patent number: 7355064Abstract: Disclosed is an improved method for preparing 15-keto-prostaglandin E derivative. According to the invention, the deprotection of protected hydroxy group required in manufacturing a 15-keto-prostaglandin derivative is conducted under the presence of a phosphoric acid compound.Type: GrantFiled: February 7, 2007Date of Patent: April 8, 2008Assignee: R-Tech Ueno, Ltd.Inventors: Ryu Hirata, Tatsuya Matsukawa
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Publication number: 20080008965Abstract: Novel ester compounds having formulae (1) to (4) wherein A1 is a polymerizable functional group having a carbon-carbon double bond, A2 is oxygen, methylene or ethylene, R1 is a monovalent hydrocarbon group, R2 is H or a monovalent hydrocarbon group, any pair of R1 and/or R2 may form an aliphatic hydrocarbon ring, R3 is a monovalent hydrocarbon group, and n is 0 to 6 are polymerizable into polymers. Resist compositions comprising the polymers as a base resin are thermally stable and sensitive to high-energy radiation, have excellent sensitivity and resolution, and lend themselves to micropatterning with electron beam or deep-UV.Type: ApplicationFiled: July 5, 2007Publication date: January 10, 2008Inventors: Masaki Ohashi, Takeshi Kinsho, Takeru Watanabe
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Patent number: 7285613Abstract: The invention is based on the discovery that certain polyester compounds bearing free-radical curable moieties are useful as b-stageable adhesives for the microelectonic packaging industry.Type: GrantFiled: June 3, 2005Date of Patent: October 23, 2007Assignee: Designer Molecules, Inc.Inventors: Stephen M. Dershem, Farhad G. Mizori
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Patent number: 7253300Abstract: In a process for producing tricyclo[5.2.1.02,6]decane-2-carboxylic acid ester by reacting tricyclo[5.2.1.02,6]deca-3-ene with carbon monoxide and alcohol in the presence of HF, carried out separately are (a) a step in which tricyclo[5.2.1.02,6]deca-3-ene is reacted with carbon monoxide to produce acyl fluoride and (b) a step in which acyl fluoride obtained in the step described above is reacted with alcohol to produce an ester. Also, the reaction conditions at the step (a) described above are selected or a step for carrying out isomerization reaction of tricyclo[5.2.1.02,6]decane-2-carboxylic fluoride obtained at the step (a) is interposed between the step (a) and the step (b). Further, the crude product of tricyclo[5.2.1.02,6]decane-2-carboxylic acid ester thus obtained is subjected to contact treatment with specific glycol in the presence of an acid catalyst and then distilled.Type: GrantFiled: September 17, 2004Date of Patent: August 7, 2007Assignees: Mitsubishi Gas Chemical Company, Inc., Kao CorporationInventors: Mitsuharu Kitamura, Takashi Kojima, Yoshiharu Ataka, Tomoaki Kubota, Kinji Kato, Kazuyuki Fukuda
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Patent number: 7227044Abstract: The present invention relates to a cycloalkanone composition which contains cycloalkanone (1) in an amount of 70 wt % or more based on the composition, wherein the content of a dimer of a cycloalkanone represented by formula (2) is 0.055 or less in terms of weight ratio to the cycloalkanone (1), a process for producing the same, a process for producing a composition containing alkyl acetate (5) by using the cycloalkanone composition, and an alkyl acetate composition obtained by the process wherein n is an integer of 1 or 2, R1 and R2 each represent H, a C1 to C8 alkyl group etc., and R3 represents a C1 to C3 alkyl group.Type: GrantFiled: March 11, 2005Date of Patent: June 5, 2007Assignee: Kao CorporationInventor: Koji Mine
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Patent number: 7166750Abstract: 5-[(4-chlorophenyl)methyl]-2,2-dimethylcyclopentanone is produced by reacting 1-[(4-chlorophenyl)methyl]-3-methyl-2-oxocyclopentanecarboxylic acid methyl ester or 1-[(4-chlorophenyl)methyl]-3-methyl-2-oxocyclopentanecarboxylic acid ethyl ester with sodium hydride and methyl halide, then hydrolyzing the obtained 1-[(4-chlorophenyl)methyl]-3,3-dimethyl-2-oxocyclopentanecarboxylic acid methyl ester or 1-[(4-chlorophenyl)methyl]-3,3-dimethyl-2-oxocyclopentanecarboxylic acid ethyl ester. The process provides 5-[(4-chlorophenyl)methyl]-2,2-dimethylcyclopentanone, an important intermediate of an agricultural or horticultural fungicide, e.g., Metconazole.Type: GrantFiled: August 11, 2000Date of Patent: January 23, 2007Assignee: Kureha CorporationInventors: Kazuhiko Sunagawa, Hajime Hoshi, Shigeru Mizusawa, Nobuyuki Kusano, Satoru Kumazawa
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Patent number: 7132564Abstract: The present invention provides a process for preparing cyclic 1,3-keto esters in the absence of solvent, using solid-state or high viscosity reactors.Type: GrantFiled: October 4, 2005Date of Patent: November 7, 2006Assignee: Bayer Materialscience AGInventors: Christoph Gürtler, Jörg Kirchhoff, Ido Schwarz
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Patent number: 7122678Abstract: The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.Type: GrantFiled: March 11, 2005Date of Patent: October 17, 2006Assignee: Warner-Lambert CompanyInventors: Justin Stephen Bryans, David Christopher Horwell, Andrew John Thorpe, David Juergen Wustrow, Po-Wai Yuen
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Patent number: 7078559Abstract: The present invention relates to a method of producing an acetate derivative represented by the formula (II) by demonocarboxylating dimalonate represented by the formula (I), wherein water is supplied while the concentration of water in a demonocarboxylating reaction solution is controlled to 0.4% by weight or less to run demonocarboxylation: wherein n denotes an integer of 1 or 2, R1 and R2 represent H, a C1-8 alkyl group or the like and R3 represents a C1-3 alkyl group.Type: GrantFiled: July 13, 2004Date of Patent: July 18, 2006Assignee: Kao CorporationInventors: Koji Mine, Hisanori Hagi
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Patent number: 7060840Abstract: The present invention relates to methods for the synthesis of chiral non-racemic products, e.g., enantiomerically-enriched hemiesters, from prochiral starting materials, e.g., meso anhydrides. The present invention also relates to catalysts for the aforementioned methods, and methods for synthesizing these catalysts.Type: GrantFiled: February 13, 2003Date of Patent: June 13, 2006Assignee: Brandeis UniversityInventors: Li Deng, Yonggang Chen, Shikai Tian
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Patent number: 7057077Abstract: A method for producing 2-(alkyl)cycloalkenone and a method for producing alkyl(3-oxo-2-alkylcycloalkyl) acetate and 5-alkyl-5-alkanolide which are useful as flavoring materials and physiologically active substances using the same are provided. A method for producing Compound (2) including the steps of: dehydrating Compound (1) using an acid catalyst until the conversion ratio of dehydration reaction reaches 20 to 90% based on Compound (1), thereby obtaining a mixture containing Compound (1) and Compound (3); and isomerizing Compound (3) while dehydrating the remaining Compound (1), and a method for producing Compound (5) or (6) using obtained Compound (2). (wherein n represents 1 or 2, R1 and R2 each represent H, C1-8 alkyl groups and the like and R3 represents C1-3 alkyl groups).Type: GrantFiled: December 11, 2003Date of Patent: June 6, 2006Assignee: Kao CorporationInventors: Hirotsugu Nishimura, Koji Mine
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Patent number: 7045653Abstract: The invention relates to NEP inhibitors for treating cardiovascular disorders. Preferred NEP inhibitors are compounds of formula (I) wherein R1 is C1–C6alkyl, C1–C6alkoxyC1–C3alkyl or C1–C6alkoxyC1–C6alkoxyC1–C3alkyl; R2 is hydrogen or C1–C6alkyl; L is a three atom linkage selected from —CH2—X—CH2— and —CH2—CH2—X— where the right hand side of the linkage is attached to R3 and where X is oxygen, sulfur or methylene; R3 is phenyl or aromatic heterocyclyl, either of which may be independently substituted by one or more groups selected from: C1–C6alkyl, halo, haloC1–C6alkyl, C1–C6alkoxy, haloC1–C6alkoxy, C1–C6alkylthio, haloC1–C6alkylthio and nitrile; and R4 and R5 are either both hydrogen, or one of R4 and R5 is hydrogen and the other is a biolabile ester-forming group that in the body of a patient is replaced by hydrogen.Type: GrantFiled: December 18, 2003Date of Patent: May 16, 2006Assignee: Pfizer, Inc.Inventors: Kevin Neil Dack, Robert John Maguire
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Patent number: 7038060Abstract: Provided is a novel method of making 2-butyl-3-[[2?(1-trityl-1H-tetrazol-5-yl)biphen-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-ene-4-one, which can be converted to irbesartan. Also provided are methods of making irbesartan.Type: GrantFiled: February 5, 2004Date of Patent: May 2, 2006Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Ben-Zion Dolitzky, Julia Kaftanov, Boris Pertsikov, Igor Rukhman, Gennady Nisnevich
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Patent number: 7022678Abstract: In accordance with the present invention, there is provided pregabalin lactose conjugate compounds. Also provided as part of the present invention is a novel method of central nervous system disorders or diseases including seizure disorders, pain, depression, anxiety, sleep disorders, consumptive disorders, psychosis, tardive dyskinesia, Huntington's disease, or Parkinson's disease in a subject by administering to the subject a pharmaceutically effective amount of a pregabalin lactose conjugate.Type: GrantFiled: January 28, 2002Date of Patent: April 4, 2006Assignee: Warner-Lambert CompanyInventors: Timothy Robert Hurley, Michael James Lovdahl, Brian Tobias
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Patent number: 6909014Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: GrantFiled: September 5, 2003Date of Patent: June 21, 2005Assignee: Esperion Therapeutics, Inc.Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Patent number: 6858650Abstract: The present invention concerns highly pure, crystalline, stable compounds of novel derivatives of 3,3-diphenylpropylamines in the form of their salts, a method for the manufacture and highly pure, stable intermediate products. The method is in particular characterized by regio- and chemoselectivity and high yield. Salts of phenolic monoesters of 3,3-diphenylpropylamines are provided, that are particularly well-suited for use in pharmaceutical formulations. Preferred compounds are R-(+)-2-(3-diisopropylamino-1-phenyl-propyl)-4-hydroxymethylphenylisobutyrate ester hydrogen fumarate and R-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenylisobutyrate ester hydrochloride hydrate. Furthermore, stable, crystalline intermediate products that are essential for obtaining the abovementioned salts are provided. A preferred intermediate product is R-(?)-3-(3-diisopropylamino-phenyl-propyl)-4-hydroxy-benzoic acid methyl ester.Type: GrantFiled: November 15, 2000Date of Patent: February 22, 2005Assignee: Schwarz Pharma AGInventor: Claus Meese
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Patent number: 6825375Abstract: The present invention relates to a 2-fluoro-2-(3-oxobicyclopentyl)acetate derivative represented by the formula (1): The compound according to the present invention is useful for efficient syntheses of 2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acids.Type: GrantFiled: December 17, 2002Date of Patent: November 30, 2004Assignee: Taisho Pharmaceutical Co.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Takeo Taguchi
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Publication number: 20040167351Abstract: A biotechnological method is described for preparing compounds of the general formulas 1Type: ApplicationFiled: February 13, 2004Publication date: August 26, 2004Inventors: Christine Bernegger-Egli, Frank Brux, Jean Paul Roduit, Oleg Werbitzky, Yves Guggisberg
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Patent number: 6770676Abstract: The present invention relates to 2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives represented by the formula: the pharmaceutically acceptable salts thereof, or the hydrates thereof. The compounds of the present invention are useful as a medicament, and in particular, are useful as modulators acting on group 2 metabotropic glutamate receptors, having effects for treating and/or preventing psychiatric disorders such as schizophrenia, anxiety and its associated diseases, depression, bipolar disorder, and epilepsy; and/or neurological diseases such as drug dependence, cognitive disorders, Alzheimer's disease, Huntington's chorea, Parkinson's disease, dyskinesia associated with muscular stiffness, cerebral ischemia, cerebral failure, myelopathy, and head trauma.Type: GrantFiled: December 6, 2002Date of Patent: August 3, 2004Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kosuke Kanuma, Kazunari Sakagami
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Patent number: 6734320Abstract: Novel non-symmetric, partially fluorinated compositions and method of manufacture which are useful as lubricants or as additives to lubricant formulations involving the molecular structure: R1f—F′—R2—F″—R3h where R1f represents a wholly or partially fluorinated organic residue end group, F′ and F″ represent functional linkages which may be alike or different, R2 represents the backbone and R3h represents a non-fluorinated organic residue end group. Such compositions are produced by reacting a mixture of alcohols, mercaptans or amines containing at least one partially fluorinated compound and at least one non-fluorinated compound in the mixture, thus producing the R1f and the R3h residues, with a difunctional organic compound (e.g., diacid, dinitrile, disulfonyl halide, diisocyanate, diisothiocyanate, diphosphoryl halide or dithiophosphoryl halide).Type: GrantFiled: April 30, 2002Date of Patent: May 11, 2004Assignee: E. I. du Pont de Nemours and CompanyInventor: Richard P. Beatty
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Publication number: 20030191182Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells.Type: ApplicationFiled: April 9, 2003Publication date: October 9, 2003Inventors: Gary David Lopaschuk, John Christopher Vederas, Jason R Dyck
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Patent number: 6596898Abstract: A process for preparing compounds represented by the following general formula (I) wherein X represents chlorine atom, bromine atom, or iodine atom, and R includes alkoxy group and amino group which comprises the step of allowing a compound represented by the formula: CH2═CXF react with a compound represented by the formula: N2CHCOR in the presence of a catalyst containing a metal atom such as a transition metal of group 8 together with chiral carboxylic-type or amide-type ligands to preferentially obtain a stereoisomer of the compound of the general formula (I) wherein the stereochemical configuration at the 1-position is S-configurationType: GrantFiled: February 27, 1998Date of Patent: July 22, 2003Assignees: Daiichi Pharmaceutical Co., Ltd., Sumitomo Chemical Co., Ltd.Inventors: Tsutomu Ebata, Toshifumi Akiba, Takanobu Ikeya, Ryuhei Wakita, Mikio Sasaki
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Patent number: 6593489Abstract: 3,4-Disubstituted-1-cyclopentene compounds, in substantially enantiopure form, have the relative stereochemistry according to formula (1A) or (1B) including the opposite enantiomers thereof, wherein R1 is either COOX, wherein X is selected from the group consisting of alkyl, H, and a salt-forming cation, or CH2OH, whererin the hydroxy group is optionally protected; R2 is H or a protecting group; R3 is H or alkyl, and R4 is selected from the group consisting of H, alkoxy, alkyl, aryl, and aralkyl; or, in the case of formula (1A), R2 and R4 are linked to form an oxazolidonone ring. These compounds can be used to prepare a series of complementary stereochemcially varied cyclopentane scaffolds.Type: GrantFiled: September 11, 2000Date of Patent: July 15, 2003Assignee: ChirotechTechnology LimitedInventors: Mark Edward Brennan Smith, Nadine Derrien
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Patent number: 6576786Abstract: The invention relates to a process for preparing substituted cyclopentane derivatives represented by the formula (I) wherein R1, R2, R3, R4, X and Y are as described in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to a process for purifying the compound of formula (Ia) and novel crystalline forms of the compound of formula (Ia).Type: GrantFiled: November 26, 2001Date of Patent: June 10, 2003Assignee: Biocryst Pharmaceuticals Inc.Inventors: Ahmed F. Abdel-Magid, Hans-Ulrich Bichsel, Daniel J. Korey, Gunther G. Laufer, Erja A. Lehto, Sebastiano Mattei, Max Rey, Thomas W. Schultz, Cynthia Maryanoff
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Patent number: 6562861Abstract: Compounds I-III wherein U is CH, O, or S; Z is mono- or di-substituted carbon; R is (CH2)nCO2H, (CH2)nSO3H, (CH2)nPO3H2, (CH2)nNO2, CH(SCH3)3, esters; R1 is H, hydroxyalkyl, aminoalkyl, alkoxyalkyl; RR1 is O; n is 0-4; R2, R3 is H, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkyl; R4 is (CH2)nOH, (CH2)nNH2, substituted alkyl were prepd. as neuraminidase inhibitors. Thus, (1R,3R,4R,1′S)-(−)-(1′-acetylamino-2 ′-ethyl)butyl-4-(aminoimino)methylaminocyclopentan-1-carboxylic acid was prepd. and tested in vitro as neuraminidase inhibitor (IC50<1.mu.M).Type: GrantFiled: May 25, 2000Date of Patent: May 13, 2003Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, John A. Montgomery
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Publication number: 20030069438Abstract: 1Type: ApplicationFiled: June 6, 2002Publication date: April 10, 2003Inventors: Justin Stephen Bryans, David Clive Blakemore, Sophie Caroline Williams
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Patent number: 6518305Abstract: Disclosed are compounds of the formula: which are useful for inhibiting neuraminidases from disease-causing microorganisms, especially, influenza neuraminidase. Also disclosed are compositions and methods for preventing and treating diseases caused by microorganisms having a neuraminidase, processes for preparing the compounds and synthetic intermediates used in these processes.Type: GrantFiled: October 19, 1999Date of Patent: February 11, 2003Assignee: Abbott LaboratoriesInventors: Clarence J. Maring, Yuanwei Chen, David A. Degoey, Vincent L. Giranda, David J. Grampovnik, Yu Gui Gu, Warren M. Kati, Dale J. Kempf, April Kennedy, Allan C. Krueger, Zhen Lin, Darold L. Madigan, Steven W. Muchmore, Hing L. Sham, Kent D. Stewart, Vincent S. Stoll, Minghua Sun, Gary T. Wang, Sheldon Wang, Ming C. Yeung, Chen Zhao
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Patent number: 6503745Abstract: New cyclopentane and cyclopentene compounds are provided along with their use in method for detecting influenza virus.Type: GrantFiled: May 7, 2001Date of Patent: January 7, 2003Assignee: Biocryst Pharmaceuticals, Inc.Inventors: Pooran Chand, Yarlagadda S. Babu, Shanta Bantia
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Patent number: 6500990Abstract: A process for efficiently producing a 2-alkyl-2-cyclopentenone comprising reacting an amine and a hydrogen halide, which are present in a ratio ranging from 1.1:1 to 5:1, with a 2-alkylidene cyclopentanone to carry out an isomerization reaction. A process for producing a jasmonate derivative comprising reacting a 2-alkyl-2-cyclopentenone with a malonic acid diester.Type: GrantFiled: March 13, 2001Date of Patent: December 31, 2002Assignee: Kao CorporationInventors: Takahiro Asada, Yoshiharu Ataka, Junji Koshino
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Patent number: 6495711Abstract: The invention relates to a process for preparing (−)-(1S,4R) N protected 4-amino-2-cylcopentene-1-carboxylate esters represented by the formula (I) wherein R1 and R2 are as described within the specification.Type: GrantFiled: December 18, 2001Date of Patent: December 17, 2002Assignee: BioCryst Pharmaceuticals Inc.Inventors: Max Rey, Gregor Welti, Cynthia Maryanoff
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Patent number: 6458569Abstract: Described is a bioprocess for the high-yield production of food flavor-acceptable jasmonic acid and methyl jasmonate, as well as a novel jasmonic acid isomer produced thereby and organoleptic uses thereof. The process yields at least 5% of the “cis” isomer defined according the structure: (wherein R is hydrogen or methyl) or at least 5% of the “cis” isomer defined according to the structure: (wherein R is hydrogen or methyl). Compositions containing at least 98% of the isomer having the structure: with an optical rotation (&agr;D20) of +58° are novel. Compositions containing at least 98% of the isomer having the structure: with an optical rotation (&agr;D20) of +58° are also novel.Type: GrantFiled: August 22, 2001Date of Patent: October 1, 2002Assignee: International Flavors & Fragrances Inc.Inventors: Mohamad I. Farbood, Robert W. Blocker, Lynda B. McLean, Mark A. Sprecker, Michael P. McLean, Nicolas Kossiakoff, Augustine Yonghwi Kim, Myrna Hagedorn
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Patent number: 6452010Abstract: The present invention provides an improved process for preparing an hydroxycarbamoyl derivative of a carboxylic acid using a hydroxylammonium salt of a carboxylic acid as a reagent.Type: GrantFiled: May 9, 2000Date of Patent: September 17, 2002Assignee: Hoffmann-La Roche Inc.Inventor: Florian Stäbler
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Patent number: 6423865Abstract: The invention relates to compounds with the general formula Y1—A1—M1—A2—Y2 wherein Y1 and Y2 are different from each other and Y1 is an acrylate or methacrylate residue and Y2 is a vinyl ether, epoxy, or azide residue, A1 and A2 are identical or different residues with the general formula CnH2n in which n is a whole number from 0 to 20 and one or more methylene groups can be replaced by oxygen atoms, and M1 has the general formula —R1—X1—R2—X2—R3—X3—R4— wherein R1, R2, R3, and R4 are identical or different doubly bonded residues from the group —O—, —COO—, —CONH—, —CO—, —S—, —C≡C—, —CH═CH—, —CH═N—, —CH2—, —N═N—, and —N═N(O)—, and R2—X2—R3 can also be a C—C bond, and X1, X2, and X3 are identical or different residues from the group 1,4-phenylene, 1,4-cyclohexylenType: GrantFiled: March 1, 2000Date of Patent: July 23, 2002Assignee: DaimlerChrysler AGInventors: Peter Strohriegl, Katja Strelzyk, Andreas Stohr, Petra Grundig, Michael Gailberger, Fritz Dannenhauer, Anne Barth
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Patent number: 6395930Abstract: A method for enhancing the purity of a desired compound comprising: Step (a) treating a crude reaction product which contains at least one desired compound, unreacted starting materials and/or byproducts with at least one bifunctional quenching agent that is capable of selective covalent reaction with unwanted byproducts, or excess reagents; Step (b) allowing the quenching agent to covalently react with unreacted starting materials and/or byproducts to afford a derivatized compound of the quenching agent: and Step (c) isolating the desired compound is described as well as novel quenching agents and methods for their use in the rapid purification of synthetic intermediates and products in synthesis, combinatorial chemistry, and automated organic synthesis.Type: GrantFiled: May 25, 2000Date of Patent: May 28, 2002Assignee: Warner LambertInventor: Sham Nikam
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Publication number: 20020052524Abstract: The invention relates to a process for preparing (−)-(1S,4R) N protected 4-amino-2-cylcopentene-1-carboxylate esters represented by the formula (I) 1Type: ApplicationFiled: December 18, 2001Publication date: May 2, 2002Inventors: Max Rey, Gregor Welti, Cynthia Maryanoff
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Patent number: 6369194Abstract: The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.Type: GrantFiled: November 9, 1998Date of Patent: April 9, 2002Assignee: Yale UniversityInventor: Harry H. Wasserman
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Patent number: 6362361Abstract: This invention relates to peroxyketals derived from cyclic &bgr;-keto esters and use of the same in the curing of resins, such as unsaturated polyester resins. The new peroxyketals were synthesized via an acid catalyzed reaction of cyclic &bgr;-keto esters with aliphatic hydroperoxides.Type: GrantFiled: June 22, 2001Date of Patent: March 26, 2002Assignee: Crompton CorporationInventors: Delphine Nwoko, Michael Wells, Lawrence Bock
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Patent number: 6362166Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.Type: GrantFiled: October 13, 2000Date of Patent: March 26, 2002Assignee: Agouron Pharmaceuticals, Inc.Inventors: Stephen E. Webber, Peter S. Dragovich, Thomas J. Prins, Siegfried H. Reich, Thomas L. Little, Jr., Ethel S. Littlefield, Joseph T. Marakovits, Robert E. Babine, Ted M. Bleckman
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Patent number: 6333180Abstract: Described is a bioprocess for the high-yield production of food flavor-acceptable jasmonic acid and methyl jasmonate, as well as a novel jasmonic acid isomer produced thereby and organoleptic uses thereof. The process yields at least 5% of the “cis” isomer defined according the structure: (wherein R is hydrogen or methyl) or at least 5% of the “cis” isomer defined according to the structure: (wherein R is hydrogen or methyl). Compositions containing at least 98% of the isomer having the structure: with an optical rotation (&agr;D20) of +58° are novel. Compositions containing at least 98% of the isomer having the structure: with an optical rotation (&agr;D20) of +58° are also novel.Type: GrantFiled: December 21, 1999Date of Patent: December 25, 2001Assignee: International Flavors & Fragrances Inc.Inventors: Mohamad I. Farbood, Robert W. Blocker, Lynda B. McLean, Mark A. Sprecker, Michael P. McLean, Nicolas Kossiakoff, Augustine Yonghwi Kim, Myrna Hagedorn
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Patent number: 6333428Abstract: The present invention provides fluorobicyclo[3.1.0]hexane derivatives represented by the formula [wherein R1 and R2 are the same or different and each represents a hydrogen atom, a C1-10 alkyl group, a C3-8 cycloalkyl group or a C3-8 cycloalkyl-C1-5 alkyl group: Y1 and Y2 are the same or different and each represents a hydrogen atom, a C1-10 alkylthio group, a C3-8 cycloalkylthio group, a C3-8 cycloalkyl-C1-5 alkylthio group, a C1-5 alkoxy group, a C3-8 cycloalkoxy group or a C3-8 cycloalkyl-C1-5 alkoxy group; or one represents a hydrogen atom and the other represents a hydroxyl group, a C1-5 alkoxy group, a C3-8 cycloalkoxy group or a C3-8 cycloalkyl-C1-5 alkoxy group; or Y1 and Y2 together represent an oxygen atom or —X(CH2)nX— (X represents an oxygen atom or a sulfur atom: N is 2 or 3)], pharmaceutically acceptable salts thereof, or hydrates thereof.Type: GrantFiled: February 22, 2001Date of Patent: December 25, 2001Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa
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Publication number: 20010051750Abstract: A process for preparing compounds represented by the following general formula (I) wherein X represents chlorine atom or other and R represents alkoxy group, amino group or other, which comprises the step of allowing a compound represented by the formula: CH2═CXF react with a compound represented by the formula: N2CHCOR in the presence of a catalyst containing a metal atom such as a transition metal of group 8 together with chiral carboxylic-type or amide-type ligands to preferentially obtain a stereoisomer of the compound of the general formula (I) wherein the stereochemical configuration at the 1-position is S-configuration 1Type: ApplicationFiled: February 27, 1998Publication date: December 13, 2001Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: TSUTOMU EBATA, TOSHIFUMI AKIBA, TAKANOBU IKEYA, RYUHEI WAKITA, MIKIO SASAKI
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Patent number: 6329429Abstract: GABA analogs such as gabapentin and pregabalin are useful to prevent and treat inflammatory diseases.Type: GrantFiled: October 25, 1999Date of Patent: December 11, 2001Assignee: Warner-Lambert CompanyInventors: Denis Schrier, Charles Price Taylor, Jr., Karin Nanette Westlund High