Additional Chalcogen Bonded Directly To The Lactone Ring Patents (Class 549/292)
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Patent number: 7955824Abstract: The invention provides novel compounds that may be used as intermediates in the preparation of epothilones, epothilone analogs and derivative, as well as new synthetic methods for producing the intermediates and products.Type: GrantFiled: May 9, 2008Date of Patent: June 7, 2011Assignee: Kosan Biosciences IncorporatedInventors: John R. Carney, Yong Li, Hugo Menzella, Ralph C. Reid
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Patent number: 7919522Abstract: Provided is a novel ivermectin derivative and compositions for the treatment or prophylaxis of parasite infestations in mammals or birds which comprise: (A) a pharmaceutically effective amount of a 1-N-phenylpyrazole compound; (B) a pharmaceutically effective amount of an ivermectin derivative of formula (II) wherein: R14 represents —(CH2)s—O—Z wherein, s is 1 or 2; Y represents —CH(OR15)—, —C(?O)— or —C(?NOR15); R15 represents hydrogen, alkyl or phenyl; and R16 represents —CH3 or —CH2CH3; Z is alkyl, alkenyl, alkynyl, acyl, alkylalkoxy, aryl, alkanoyloxy, alkoxycarbonyl, alkenoyl, alkynoyl, or aroyl.Type: GrantFiled: May 3, 2007Date of Patent: April 5, 2011Assignee: Merial LimitedInventors: Mark D. Soll, Albert Boeckh, Natalya Shub
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Publication number: 20110077380Abstract: The present invention relates to a novel carbohydrate lactone, functionalized aliphatic polyesters and copolymers formed therefrom, and processes for the preparation thereof from renewable resources.Type: ApplicationFiled: March 27, 2009Publication date: March 31, 2011Applicant: IMPERIAL INNOVATIONS LIMITEDInventors: Charlotte K. Williams, Molly Morag Stevens, Min Tang
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Patent number: 7902383Abstract: A method of the invention industrially produces heterocyclic mercapto compounds useful as raw materials or intermediates in the synthesis of medicaments or pesticides, or as permanent wave agent, with a high yield and high productivity using easily available starting materials. A heterocyclic mercapto compound represented by Formula (1) (wherein X represents any structure of —O—, —S—, —NH—, and —NR1—; R1 represents any of an alkyl group, alkoxy group and alkoxyalkyl group each having 1 to 6 carbon atoms; Y represents an oxygen atom, a sulfur atom or —NR2—; R2 represents a hydrogen atom or alkyl group having 1 to 6 carbon atoms; and Z1 represents a divalent organic residue having at least one mercapto group) is produced by reacting a metal sulfide or a metal hydrosulfide with a compound represented by Formula (2) (wherein X and Y are as defined in Formula (1); and Z2 represents a divalent organic residue having at least one halogen group) in the presence of a solvent at a pH of 7.0 to 11.0.Type: GrantFiled: May 28, 2007Date of Patent: March 8, 2011Assignee: Showa Denko K.K.Inventors: Shinichi Yorozuya, Hidemasa Aoki
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Publication number: 20110054193Abstract: The present invention relates to a polypeptide with HMG-CoA reductase activity, to its polynucleotide congener and to a method for the production of a statin comprising over expression of said polypeptide.Type: ApplicationFiled: April 28, 2009Publication date: March 3, 2011Inventors: Marco Alexander Van Den Berg, Marcus Hans
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Publication number: 20110021592Abstract: The present invention provides a process for preparing a redispersible powder of nanoparticles of a water-insoluble organic compound, the process including the steps of: (i) preparing an oil-in-water microemulsion comprising a water-insoluble organic compound, a volatile water-immiscible organic solvent, water, and at least one surfactant; and (ii) removing the volatile water-immiscible organic solvent and the water so as to form the redispersible powder comprising said nanoparticles, wherein the nanoparticle are in a particulate form, and wherein the solubility of the water-insoluble organic compound is at least about 5 times greater than the solubility of the water-insoluble organic compound in unprocessed form. Step (i) can further include the addition of co-solvent or polymer.Type: ApplicationFiled: September 16, 2007Publication date: January 27, 2011Inventors: Shlomo Magdassi, Hadas Netivi, Katrin Goshen
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Publication number: 20100317823Abstract: The present invention generally relates to processes for the chemocatalytic conversion of a glucose source to an adipic acid product. The present invention includes processes for the conversion of glucose to an adipic acid product via glucaric acid or derivatives thereof. The present invention also includes processes comprising catalytic oxidation of glucose to glucaric acid or derivative thereof and processes comprising the catalytic hydrodeoxygenation of glucaric acid or derivatives thereof to an adipic acid product. The present invention also includes products produced from adipic acid product and processes for the production thereof from such adipic acid product.Type: ApplicationFiled: June 11, 2010Publication date: December 16, 2010Applicant: RENNOVIA, INC.Inventors: Thomas R. Boussie, Eric L. Dias, Zachary M. Fresco, Vincent J. Murphy, James Shoemaker, Raymond Archer, Hong Jiang
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Publication number: 20100274029Abstract: Provided is a method of preparing a (6R)-3-hexyl-4-hydroxy-6-undecyl-5,6-dihydropyran-2-one, and a (5R)-2-hexyl-5-hydroxy-3-iminohexadecanoate derivative used in said method as an intermediate.Type: ApplicationFiled: October 29, 2008Publication date: October 28, 2010Applicant: HANMI PHARM. CO., LTD.Inventors: Sang Min Yun, Young Ho Moon, Young-Kil Chang, Dong Jin Hong, Ji-Yeon Chang, Moon Sub Lee, Jaeho Yoo, Ji Sook Kim, Cheol Kyung Kim
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Patent number: 7781601Abstract: A method for the production of 6,6,6-trihalo-3,5-dioxohexanic acid esters of formula (I): in addition to the enols thereof and <I>E</I> and <I>Z</I> isomers, wherein X independently represents fluorine, chlorine or bromine and R1 represents alkyl, cycloalkyl, aryl or aralkyl. A method for the production of enol ethers of formula (Ib): and the enols thereof (E and Z isomers) wherein X and R1 have the above-mentioned meanings.Type: GrantFiled: February 28, 2008Date of Patent: August 24, 2010Assignee: BaselInventors: Paul Hanselmann, Wolfgang Wenger
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Patent number: 7772191Abstract: The present invention relates to processes for preparing the compounds of general formula I, wherein the groups R1 and R3 are defined according to claim 1. Furthermore this inventions relates to intermediates obtained in these processes.Type: GrantFiled: May 3, 2006Date of Patent: August 10, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Frank Himmelsbach, Xiao-jun Wang, Wenjun Tang, Xiufeng Sun, Li Zhang, Dhileepkumar Krishnamurthy, Chris Hugh Senanayake, Zhengxu Han
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Publication number: 20100191002Abstract: A controlled nitric acid process employing oxygen and nitric acid as co-oxidants is used to oxidize organic compounds subject to nitric acid oxidation, to their corresponding carboxylic acids. Oxidation of some carbohydrates by this process can produce one or more of their corresponding acid forms. The process is carried out at moderate temperatures, typically in the range of 20° C. to 45° C. in a closed reactor, with oxygen gas being introduced into the reaction chamber as needed in order to sustain the reaction. Computer controlled reactors allow for careful and reproducible control of reaction parameters. Nitric acid can be recovered by a distillation/evaporation process, or by diffusion dialysis, the aqueous solution made basic with inorganic hydroxide, and the residual inorganic nitrate removed using a filtration (nanofiltration) device.Type: ApplicationFiled: April 2, 2010Publication date: July 29, 2010Inventors: Donald E. Kiely, Kirk R. Hash, SR.
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Publication number: 20100183563Abstract: The present invention provides a dentinogenesis inducer and dentinogenesis pulp-capping material, which are effectively used for formation (regeneration) of dentin. The present invention also provides a method of producing odontoblasts useful for dental regenerative therapy and the application of the obtained odontoblasts. The dentinogenesis inducer and the dentinogenesis pulp-capping material of the present invention are both characterized by the use of an HMG-CoA reductase inhibitor as an active ingredient. Additionally, odontoblasts can be produced by culturing cells capable of differentiating into odontoblasts in the presence of the HMG-CoA reductase inhibitor.Type: ApplicationFiled: March 28, 2008Publication date: July 22, 2010Applicant: ORGAN TECHNOLOGIES, INC.Inventors: Takuo Kuboki, Mitsuaki Ono, Wataru Sonoyama, Takuo Fujisawa, Kengo Shimono, Masamitsu Oshima, Yosuke Okamoto
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Publication number: 20100145046Abstract: Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-?-lactones and ?-lactones are disclosed.Type: ApplicationFiled: November 20, 2009Publication date: June 10, 2010Inventors: Geoffrey W. Coates, John W. Kramer
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Publication number: 20100137244Abstract: Chemical syntheses and medical uses of novel modulators of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and diastereomeric mixtures of isomers, individual diastereomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of hypercholesterolemia, dyslipidemia, coronary artery disease, atherosclerosis, metabolic syndrome, a hyperproliferative disease such as colorectal cancer, prostate cancer, and melanoma, a neurodegenerative disease such as cerebral ischemia, Alzheimer's disease, and Parkinson's disease are described.Type: ApplicationFiled: July 12, 2007Publication date: June 3, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100136339Abstract: The invention relates to the preparation of 2-(6-substituted-1,3-dioxane-4-yl)acetic acid derivatives of formula 1, where X stands for a leaving group, and R1, R2, and R3 each independently stand for an alkyl group with 1-3 carbon atoms from 4-hydroxy-6-X-substituted-methyl-tetrahydropyran-2-one compounds, where X is as defined above, with the aid of an acetalization agent, in the presence of an acid catalyst. The invention also relates to the novel compounds of formula 1 as well as salts and acids to be prepared from these, with the OR3 group in formula 1 being replaced by an OY group, where X, R1 and R2 have the meanings defined above and where Y stands for an alkaline (earth) metal or a substituted or unsubstituted ammonium group or stands for hydrogen, and to the novel compounds of formula 2. The products concerned are, after conversion into the t-butyl ester of 2-(6-hydroxymethyl-1,3-dioxane-4-yl)acetic acid, important as intermediary products in the preparation of statins.Type: ApplicationFiled: November 24, 2009Publication date: June 3, 2010Applicant: AstraZeneca UK Ltd.Inventors: Jacob Hermanus Mattheus Hero Kooistra, Hubertus Josephus Marie ZEEGERS, Daniel MINK, Joannes Maria Cornelis Antonius MULDERS
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Patent number: 7678927Abstract: The present invention relates to an improved and industrial friendly process for lactonization to produce compound of the Formula [I], from compound of the Formula [II] in presence of an inorganic compound as a suitable lactonizing agent, preferably alkali metal hydrogen sulfate, and crystallizing the obtained lactone product in a solvent; or treating compound of the Formula [II] in the presence of an inorganic compound preferably alkali metal hydrogen sulfate using phase transfer catalyst in heterogeneous phase followed by crystallizing the obtained lactone product in a solvent.Type: GrantFiled: September 8, 2004Date of Patent: March 16, 2010Assignee: Jubilant Organosys LimitedInventors: Govind Singh, Paramvir Bhadwal, Sanjay Jaiswal, Dinesh R. Panchasara, Rajesh Kumar Thaper, Sushil Kumar Dubey, Jag Mohan Khanna
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Patent number: 7678928Abstract: An improved method for manufacture of simvastatin of formula (I) in high purity. The process for preparation of compound (I) comprises the steps of agitating a compound of formula (II), wherein R is hydrogen, NH4+ or an alkali metal in an organic solvent and in an inert atmosphere at a temperature of between 27° C. to 40° C. in the presence of a weak acid followed by neutralization with an organic base and obtaining compound of formula (I) in high purity and substantially free of impurities through a step of isolation and crystallization.Type: GrantFiled: June 17, 2005Date of Patent: March 16, 2010Assignee: Lupin LimitedInventors: Subhash Rajaram Kadam, Mahendra Raghunath Patil, Madhukar Shaligram Patil, Sachin Arun Sasane
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Publication number: 20100048690Abstract: Antitumoral compounds obtained from a porifera, of the family Raspailiidae, genus Lithoplocamia, species lithistoides, and derivatives thereof are provided.Type: ApplicationFiled: June 15, 2007Publication date: February 25, 2010Applicant: PHARMA MAR, S.A.Inventors: Ma Jesus Martin Lopez, Laura Coello Molinero, Jose Fernando Reyes Benitez, Alberto Rodriguez Vicente, Maria Garranzo Garcia-Ibarrola, Carmen Murcia Perez, Andres Francesch Solloso, Francisco Sanchez Sancho, Maria del Carmen Cuevas Marchante, Rogelio Fernandez Rodriguez
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Publication number: 20090312555Abstract: There is provides a process for the preparation of a compound of formula (7): wherein R is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; provides that R is not a compound of Formula (a): wherein Ra represents an alkyl group, such as a C1-16 alkyl group, and preferably an isopropyl group; Rb represents an aryl group, preferably a 4-fluorophenyl group; Rc represents hydrogen, a protecting group or an alkyl group, such as a C1-16 alkyl group, and preferably a methyl group; and Rd represents hydrogen, a protecting group or a SO2Re group where Re is an alkyl group, such as a C1-16 alkyl group, and preferably a methyl group.Type: ApplicationFiled: November 28, 2005Publication date: December 17, 2009Applicant: NPIL PHARMACEUTICAL (UK) LIMITEDInventors: David John Moody, Jonathan William Wiffen
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Publication number: 20090306412Abstract: Derivatives of drugs are provided, said derivatives comprising the H2S-releasing moiety 4-hydroxythiobenzamide that is either covalently linked to the drug or forms a salt with the drug. The compounds of the present invention exhibit enhanced activity or reduced side effects or both.Type: ApplicationFiled: July 18, 2007Publication date: December 10, 2009Applicant: ANTIBE THERAPEUTICS INC.Inventors: John L. Wallace, Giuseppe Cirino, Vincenzo Santagada, Giuseppe Caliendo
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Patent number: 7566792Abstract: A method for the manufacture of Lovastatin of formula (I) is disclosed. The method comprises of: A. lactonisation of Mevinolinic acid (II) and isolation of impure Lovastatin (I), B. purification of impure Lovastatin (I), C. optionally, repurification of pure Lovastatin (I) from a mixture of alumina and a water miscible solvent.Type: GrantFiled: October 14, 2003Date of Patent: July 28, 2009Assignee: Lupin LimitedInventors: Sanjay Kumar Vaishnav, Bhupendra Harishchandra Thakur, Subhash Rajaram Kadam
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Publication number: 20090187031Abstract: Synthetic methods and intermediates useful in the preparation of lactone containing compounds such as discodermolide and compounds which mimic the chemical or biological activity of discodermolide are provided.Type: ApplicationFiled: February 28, 2008Publication date: July 23, 2009Applicant: The Trustees of The University of PennsylvaniaInventors: Amos B. Smith, III, Thomas J. Beauchamp, Matthew J. LaMarche, Yuping Qiu, Michael D. Kaufman, Hirokazu Arimoto, David R. Jones, Kaoru Kobayashi
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Publication number: 20090186938Abstract: Antitumoral compounds obtained from a porifera, of the family Raspailiidae, genus Lithoplocamia, species lithistoides, and derivatives thereof are provided.Type: ApplicationFiled: June 15, 2007Publication date: July 23, 2009Applicant: PHARMA MAR, S.A.Inventors: Ma Jesus Martin Lopez, Laura Coello Molinero, Jose Fernando Reyes Benitez, Alberto Rodriguez Vicente, Maria Garranzo Garcia-Ibarrola, Carmen Murcia Perez, Andres Francesch Solloso, Francisco Sanchez Sancho, Maria del Carmen Cuevas Marchante, Rogelio Fernandez Rodriguez
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Publication number: 20090171095Abstract: A method of the invention industrially produces heterocyclic mercapto compounds useful as raw materials or intermediates in the synthesis of medicaments or pesticides, or as permanent wave agent, with a high yield and high productivity using easily available starting materials. A heterocyclic mercapto compound represented by Formula (1) (wherein X represents any structure of —O—, —S—, —NH—, and —NR1—; R1 represents any of an alkyl group, alkoxy group and alkoxyalkyl group each having 1 to 6 carbon atoms; Y represents an oxygen atom, a sulfur atom or —NR2—; R2 represents a hydrogen atom or alkyl group having 1 to 6 carbon atoms; and Z1 represents a divalent organic residue having at least one mercapto group) is produced by reacting a metal sulfide or a metal hydrosulfide with a compound represented by Formula (2) (wherein X and Y are as defined in Formula (1); and Z2 represents a divalent organic residue having at least one halogen group) in the presence of a solvent at a pH of 7.0 to 11.0.Type: ApplicationFiled: May 28, 2007Publication date: July 2, 2009Applicant: SHOWA DENKO K.K.Inventors: Shinichi Yorozuya, Hidemasa Aoki
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Publication number: 20090156837Abstract: The present invention relates to a novel process for isolation and recovery of compounds such as biosynthetically produced simvastatin in either lactone form or in the form of its acid salt in high yield and purity, from microbial fermentation broth and isolating the said statin from harvested microbial broth.Type: ApplicationFiled: December 18, 2008Publication date: June 18, 2009Applicant: Themis Medicare LimitedInventors: Dinesh Shantilal PATEL, Sachin Dinesh Patel, Shashikant Prabhudas Kurani, Tapas Barui, Rajneesh Anand, T. Damodar Reddy
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Patent number: 7528265Abstract: Highly pure simvastatin can be prepared economically in a high yield using the method comprising the steps of treating lovastatin with potassium hydroxide dissolved in a mixture of water and methanol to obtain a triol acid; relactonizing the triol acid, and protecting the hydroxy group on the lactone ring; and acylating the resulting compound with 2,2-dimethylbutyryl chloride or 2,2-dimethylbutyryl bromide in the presence of an acylation catalyst in an organic solvent, followed by removing the silyl protecting group on the lactone ring to obtain simvastatin.Type: GrantFiled: December 26, 2002Date of Patent: May 5, 2009Assignee: Hanmi Pharm., Co., Ltd.Inventors: Jaeheon Lee, Taehee Ha, Chulhyun Park, Hoechul Lee, Gwansun Lee, Youngkil Chang
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Publication number: 20090048335Abstract: Preparation of simvastatin.Type: ApplicationFiled: August 15, 2008Publication date: February 19, 2009Inventors: Venkata Naga Mandava, Radha Krishna Singamsetty, Satish Kumar Vujjni, Vadali Ravi Kumar, Thambidurai Marappa Gounder, Dipal Ranjan Bhowmik, S. Venkatesh, Kedar K. Nerurkar
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Publication number: 20090010860Abstract: Disclosed is the use of the compounds of formula wherein Q is —OH; —OR7; —NH2; —NHR7; —NR7R8; or —N?R9; T is —COR5; —CN; or —SO2—(C6-C12)aryl; R1 is hydrogen; —OR7, —SR7; —NHR7; —NR7R8; C1-C22alkyl; C2-C12Alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl, C2-C11heteroaralkyl; C6-C10aryl; or C1-C9heteroaryl; R2 and R3 independently from each other are C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl, C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl; C3-C12cycloheteroalkyl; C2-C11heteroaralkyl, C6-C10aryl; or C1-C9heteroaryl; R4 is cyano; COR7, COOR7; CONH2; CONHR7; CONR7R8; SO2(C6-C12)aryl, C2-C12alk-1-enyl; C3-C12cycloalk-1-enyl; C2-C12alk-1-inyl; C2-C12heteroalkyl, C3-C5heterocycloalkyl, C6-C10aryl; or C1-C9heteroaryl; R5 is —COR7; —COOR7; —OR7; —SR7, —NHR7, —NR7R8; C2-C12alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12alkylphenyl; C1-C12alkoxy-C8-C10aryl; C1-C12heteroalkyl; C2-C11heteroaralkyl; CType: ApplicationFiled: June 20, 2005Publication date: January 8, 2009Inventors: Barbara Wagner, Frank Bienewald, Heinz Wolleb, Olof Wallquist, Bernd Herzog, Thomas Ehlis, Jurg Haase
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Publication number: 20080319211Abstract: Intermediates in the preparation of epothilones and epothilone analogs are provided along with synthetic methods useful in the synthesis of epothilone compounds.Type: ApplicationFiled: May 9, 2008Publication date: December 25, 2008Applicant: KOSAN Biosciences, Inc.Inventors: Yue Chen, Yong Li
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Patent number: 7439046Abstract: The invention relates to a process for the preparation of a 2,4-dideoxyhexose or a 2,4,6-trideoxyhexose from a substituted or unsubstituted carbonyl compound with at least 2 carbon atoms and at least one ?-hydrogen atom and a substituted or unsubstituted aldehyde in the presence of an aldolase and water, the reaction between the substituted or unsubstituted carbonyl compound with at least 2 carbon atoms and at least one ?-hydrogen atom and the substituted or unsubstituted aldehyde being carried out at a carbonyl concentration of at most 6 moles/l of reaction mixture and the final concentration of the 2,4-dideoxyhexose or the 2,4,6-trideoxyhexose being at least 2 mass % of the reaction mixture. The invention also relates to the use of a 2,4-dideoxyhexose or a 2,4,6-trideoxyhexose obtained by means of a process according to the invention in the preparation of a medicine, particularly in the preparation of a statine.Type: GrantFiled: August 17, 2005Date of Patent: October 21, 2008Assignee: DSM IP Assets B.V.Inventors: Joannes Gerardus Kierkels, Daniel Mink, Sven Panke, Franciscus Alphons Lommen, Dennis Heemskerk
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Patent number: 7423162Abstract: The invention relates to a process for the preparation of (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile from 6-X-substituted-methyl-4-hydroxy-tetrahydro-pyran-2-one, wherein X stands for a leaving group, by reacting 6-X-substituted-methyl-4-hydroxy-tetrahydro-pyran-2-one with a cyanide ion in water and by subsequent lowering of the pH to a pH between 0 and 5. (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile and other compounds obtainable from (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile may suitably be used in the preparation of a pharmaceutical preparation, more in particular in the preparation of statins, more in particular in the preparation of Atorvastatine or a salt thereof, for instance its calcium salt. The invention also relates to (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile and other compounds obtainable therefrom.Type: GrantFiled: April 28, 2004Date of Patent: September 9, 2008Assignee: DSM IP Assets B.V.Inventors: Daniel Mink, Wilhelmus Hubertus Joseph Boesten, Michael Wolberg, Natascha Sereinig
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Publication number: 20080214843Abstract: An improved method for manufacture of simvastatin of formula (I) in high purity. The process for preparation of compound (I) comprises the steps of agitating a compound of formula (II), wherein R is hydrogen, NH4+ or an alkali metal in an organic solvent and in an inert atmosphere at a temperature of between 27° C. to 40° C. in the presence of a weak acid followed by neutralization with an organic base and obtaining compound of formula (I) in high purity and substantially free of impurities through a step of isolation and crystallization.Type: ApplicationFiled: June 17, 2005Publication date: September 4, 2008Applicant: Lupin LimitedInventors: Subhash Rajaram Kadam, Mahendra Raghunath Patil, Madhukar Shaligram Patil, Sachin Arun Sasane
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Patent number: 7414074Abstract: Lactones of Formula (I) which are pharmaceutically active in diseases associated with inflammationType: GrantFiled: March 31, 2005Date of Patent: August 19, 2008Assignee: Novartis AGInventors: Josef Gottfried Meingassner, Klaus Thirring
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Publication number: 20080161582Abstract: A method for the production of 6,6,6-trihalo-3,5-dioxohexanic acid esters of formula (I): in addition to the enols thereof and <I>E</I> and <I>Z</I> isomers, wherein X independently represents fluorine, chlorine or bromine and R1 represents alkyl, cycloalkyl, aryl or aralkyl. A method for the production of enol ethers of formula (Ib): and the enols thereof (E and Z isomers) wherein X and R1 have the above-mentioned meanings.Type: ApplicationFiled: February 28, 2008Publication date: July 3, 2008Inventors: Paul Hanselmann, Wolfgang Wenger
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Patent number: 7304091Abstract: The present invention relates to compounds with structures resembling natural statins isolated from Penicillium sp.Type: GrantFiled: December 3, 2002Date of Patent: December 4, 2007Assignee: Myco TeO A/SInventors: Jens Christian Frisvad, Lene Lange, Kirk Schnorr, Steen Stender, Thomas Ostenfeld Larsen
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Patent number: 7214708Abstract: Synthetic discodermolide analogs having utility as antiproliferative agents, having a structure represented by formula A where RA through RE and XA are as defined herein.Type: GrantFiled: October 28, 2005Date of Patent: May 8, 2007Assignee: Kosan Biosciences IncorporatedInventors: Kurt F. Sundermann, Simon James Shaw, Daniel V. Santi
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Patent number: 7205415Abstract: A process for manufacturing simvastatin is provided using novel intermediates. Thus, for example, lovastatin is reacted with methoxyethylamine, alpha methylated 2-methylbutyryl side chain of the amide formed, hydrolyzed and lactonized to produce finally simvastatin of high purity.Type: GrantFiled: January 2, 2004Date of Patent: April 17, 2007Assignee: Hetero Drugs, Ltd.Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
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Patent number: 7189558Abstract: In one aspect, the present invention provides an improved method for the manufacture of Pravastatin sodium salt by fermentation under optimal fermentation parameters using a new strain of Streptomyces flavidovirens.Type: GrantFiled: September 27, 2001Date of Patent: March 13, 2007Assignee: Biocon LimitedInventors: Ramavana Gururaja, Anuj Goel, Madhavan Sridharan, Ramakrishnan Sadhana Melarkode, Madhav Kulkarni, Acharya Poornaprajna, Deepthy Sathyanathan, Sambasivam Ganesh, Shrikumar Suryanarayan
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Patent number: 7151105Abstract: The present invention provides compounds of formula (4), and their pharmaceutically acceptable salts and solvates, which are useful as inhibitors of the Hepatitis C virus (HCV) polymerase enzyme and are also useful for the treatment of HCV infections in HCV-infected mammals. The present invention also provides pharmaceutical compositions comprising compounds of formula (4), their pharmaceutically acceptable salts and solvates. Furthermore, the present invention provides intermediate compounds and methods useful in the preparation of compounds of formula (4).Type: GrantFiled: August 15, 2005Date of Patent: December 19, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Javier Gonzalez, Tanya Michelle Jewell, Hui Li, Angelica Linton, John Howard Tatlock
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Patent number: 7141681Abstract: The invention relates to a continuous process for preparing dihydropyrones of general formula I, wherein the groups R1 and R2 have the meanings described herein.Type: GrantFiled: February 14, 2002Date of Patent: November 28, 2006Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Oliver Meyer, Markus Sauter, Mark Goehlich
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Patent number: 7141602Abstract: Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, Streptomyces, Actinomadura, Micromonospora, some are obtained by treating the fermentation products using the method of chemical synthesis or they are the products of total chemical synthesis. The purity of the active ingredient is an important factor for manufacturing the safe and effective pharmaceutical, especially if the pharmaceutical product must be taken on a longer term basis in the treatment or prevention of high plasma cholesterol. The accumulation of the impurities from the pharmaceuticals of lower purity may cause many side effects during the medical treatment.Type: GrantFiled: October 30, 2003Date of Patent: November 28, 2006Assignee: LEK Pharmaceuticals d.d.Inventors: Rok Grahek, Dusan Milivojevic, Andrej Bastarda
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Patent number: 7101912Abstract: Prodrugs of carbidopa, derivatives of carbidopa prodrugs, methods of making prodrugs of carbidopa and derivatives thereof, methods of using prodrugs of carbidopa and derivatives thereof, and compositions of prodrugs of carbidopa and derivatives thereof are disclosed.Type: GrantFiled: December 8, 2003Date of Patent: September 5, 2006Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Mark A. Gallop, Kenneth C. Cundy, Jianhua Li, Feng Xu, Cindy X. Zhou, Laxminarayan Bhat
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Patent number: 7094912Abstract: A process for the preparation of inhibitors of HMG-CoA reductase, such as simvastatin, from 4-silyloxytetrahydropyran-2-ones with triethylamine trihydrofluoride being used as the desilylation reagent is described. The reaction is performed in organic solvents, a mixture thereof or without solvents. It is characteristic of this reaction that no additional impurities are obtained and that it takes place without the use of additional catalysts and with low excesses of the reagent.Type: GrantFiled: March 17, 2003Date of Patent: August 22, 2006Assignee: KRKA, Tovarna Zdravil, D. D.Inventors: Silvo Zupancic, Dusan Krasovec, Pavel Zupet
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Patent number: 7081347Abstract: A method for assessing aspirin resistance and relative risk of a cardiovascular event in a patient taking aspirin is provided. The concentration of 11-dehydro-thromboxane B2 in a urine sample is measured and compared to a set of standardized quartile concentrations. A concentration of urinary 11-dehydro-thromboxane B2 that falls within the second, third, or fourth quartile is indicative of aspirin resistance and an elevated risk of a recurrent cardiovascular event.Type: GrantFiled: September 24, 2003Date of Patent: July 25, 2006Assignee: McMaster UniversityInventors: Salim Yusuf, Jack Hirsh, John Eikelboom
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Patent number: 7074826Abstract: The present invention concerns esters of R-enantiomers of a non-steroidal anti-inflammatory drug, which is substantially free from the S-enantiomer. The compounds of the invention may be used in treating a disease or illness in a mammal. To this end, a composition comprising a compound mentioned above, or a pharmaceutically acceptable salt thereof where salt formation occurs, is administered to the mammal in an amount sufficient to elicit a chemopreventative effect or a chemoprotective effect or a therapeutic effect or a prophylactic effect.Type: GrantFiled: October 3, 2003Date of Patent: July 11, 2006Assignee: Encore Pharmaceuticals, Inc.Inventors: William J. Wechter, Elaine Benaksas Schwartz
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Patent number: 7038064Abstract: A process of the present invention produces a hydroxylactone by subjecting an unsaturated carboxylic acid having a double bond not conjugated to a carboxyl group or an ester thereof to (i) a reaction with hydrogen peroxide in the presence of a metallic compound containing a metallic element selected from W, Mo, V and Mn or (ii) a reaction with a peroxide containing the metallic element to thereby yield a corresponding hydroxylactone having a hydroxyl group combined with one of carbon atoms constituting the double bond and being cyclized at the other carbon atom position. The metallic compound may be one selected from oxides, oxoacids and salts thereof. The unsaturated carboxylic acid includes, for example, ?,?-unsaturated carboxylic acids, ?,?-unsaturated carboxylic acids, and ?,?-unsaturated carboxylic acids. The process can produce hydroxylactones in high yields at low cost.Type: GrantFiled: July 18, 2001Date of Patent: May 2, 2006Assignee: Diacel Chemical Industries, Ltd.Inventors: Yasutaka Ishii, Tatsuya Nakano, Keizo Inoue
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Patent number: 7026351Abstract: The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.Type: GrantFiled: March 20, 2003Date of Patent: April 11, 2006Assignee: Xenoport, Inc.Inventors: Mark A Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat
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Patent number: 7002017Abstract: The invention relates to a process for preparing the compounds of general formula I by enantioselective hydrogenation of the compounds of formula II in the presence of special hydrogenation catalysts. The invention is characterised by high enantioselectivity, providing easy access to a category of important pharmaceutical compositions, i.e. intermediates for the synthesis of tipranavir.Type: GrantFiled: March 10, 2004Date of Patent: February 21, 2006Assignee: Boehringer Ingelheim International GmbHInventors: Franz Dietrich Klingler, Michael Steigerwald, Richard Ehlenz
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Patent number: 6995277Abstract: The present invention relates to a process for preparing simvastatin, wherein the simvastatin dimer content is controlled. More particularly, the present invention relates to a process for preparing simvastatin having a simvastatin dimer content of about 0.2 to about 0.4% wt. The present invention also relates to a process for preparing simvastatin having a simvastatin dimer content of less than about 0.2% wt. The present invention also discloses a commercial scale process of preparing simvastatin having a specified simvastatin dimer content which is reproducible.Type: GrantFiled: February 11, 2004Date of Patent: February 7, 2006Assignee: Plus Chemicals, B.V.Inventors: Ferenc Korodi, Csaba Szabo, Szabolcs Salyi, Istvan Bodi
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Patent number: 6960573Abstract: Compounds expressed by the following general formula (1), [wherein, R01 and R02 are each independently a hydrogen atom or a protecting group for a hydroxyl group; Z is one out of the following formulae (1-1), (1-2), (1-3), (1-4) and (1-5)]. The compounds can be used as active ingredients of treating agents for inflammatory respiratory diseases, malignant tumors, rheumatoid arthritis, osteoporosis, diabetes mellitus, hypertension, alopecia, acne, psoriasis, dermatitis, hypercalcemia, hypoparathyroidism and metabolic disorder of cartilage.Type: GrantFiled: January 4, 2002Date of Patent: November 1, 2005Assignee: Teijin LimitedInventors: Kazuya Takenouchi, Qingzhi Gao, Kenji Manabe, Ryo Sogawa, Yasuhiro Takano, Seiichi Ishizuka