Additional -coo- Group Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/321)
  • Patent number: 10260114
    Abstract: The present invention relates in a first aspect to a method of preparing a crystalline lanthanum-carboxylate coordination polymer and the crystalline lanthanum-carboxylate coordination polymer obtained or obtainable by the method. In another aspect of the present invention, also provides a method of detecting a target nucleic acid sequence in a sample.
    Type: Grant
    Filed: May 18, 2017
    Date of Patent: April 16, 2019
    Assignees: MACAU UNIVERSITY OF SCIENCE AND TECHNOLOGY, SOUTHERN MEDICAL UNIVERSITY
    Inventors: Jin-Xiang Chen, Bin Sun, Bao-Ping Xie, Zhi-Hong Jiang, Li-Ping Bai
  • Patent number: 10233196
    Abstract: The present invention relates to the preparation of compounds of formula III: wherein R is alkyl, aryl or benzyl.
    Type: Grant
    Filed: February 28, 2018
    Date of Patent: March 19, 2019
    Assignee: ViiV Healthcare Company
    Inventors: Steven N. Goodman, Huan Wang, Douglas Mans, Matthew Kowalski
  • Patent number: 10174051
    Abstract: The present invention relates to intermediates in the preparation of carbamoylpyridone derivatives, such as compounds of formula (III) and/or compounds of formula (IV): wherein R is alkyl, aryl or benzyl.
    Type: Grant
    Filed: February 28, 2018
    Date of Patent: January 8, 2019
    Assignee: ViiV Healthcare Company
    Inventors: Steven N. Goodman, Huan Wang, Douglas Mans, Matthew Kowalski
  • Publication number: 20150094344
    Abstract: The present invention relates to methods for lowering stroke damages and/or lowering blood pressure in a subject with a stroke in need thereof, comprising administering to the subject an effective amount of a pharmaceutical composition comprising a short acting dihydropyridine compound, preferably clevidipine or a pharmaceutically acceptable salt or ester thereof. Also provided are related medicaments, pharmaceutical compositions, and methods for preparing the medicaments.
    Type: Application
    Filed: March 30, 2012
    Publication date: April 2, 2015
    Applicant: THE MEDICINES COMPANY
    Inventor: Gregory Charles Williams
  • Publication number: 20150044557
    Abstract: A negative electrode active material for a sodium-ion battery includes a compound including an aromatic ring structure and two or more COOX groups in which X is Li or Na, and which are bonded to ends of the aromatic ring structure, the aromatic ring structure including an aromatic heterocyclic ring that contains nitrogen in the ring.
    Type: Application
    Filed: August 12, 2014
    Publication date: February 12, 2015
    Inventor: Hideki Nakayama
  • Publication number: 20140323529
    Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.
    Type: Application
    Filed: April 30, 2014
    Publication date: October 30, 2014
    Applicant: NEKTAR THERAPEUTICS
    Inventors: Zhongxu Ren, Bo-Liang Deng, Jennifer Riggs-Sauthier, Micah Harvey
  • Publication number: 20140315893
    Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi
    Type: Application
    Filed: November 22, 2012
    Publication date: October 23, 2014
    Inventors: Ferenc Fülöp, László Vígh, Zsolt Török, Botond Penke, Ibolya Horváth, Gábor Balogh, Sándor Bernáth, Ákos Hunya
  • Publication number: 20140242606
    Abstract: The present invention relates to a probe for iFRET and use thereof. Specifically, the present invention relates to a novel probe for iFRET, a method for preparing the probe for iFRET, a method for searching a target protein-specific binding site or a molecule having the binding site using the probe for iFRET, and a method for imaging the target protein using the probe for iFRET. The probe for iFRET according to the present invention utilizes an amino acid in a protein as a fluorescent donor, unlike the conventional FRET method. Therefore, only one fluorescent material is used, and its emission wavelength is distinct from the intrinsic fluorescence of the protein. Thus, high specificity and sensitivity are ensured, and the quantity, activity and mechanism of various proteins can be analyzed in an easy and accurate manner.
    Type: Application
    Filed: June 25, 2012
    Publication date: August 28, 2014
    Applicant: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
    Inventors: Sang Jeon Chung, Ju Hwan Kim, Elena Ruchkina, Hyo Jin Kang
  • Publication number: 20140206873
    Abstract: A process for manufacturing 5-chloromethyl-2,3-pyridine dicarboxylic acid anhydrides (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; comprising the steps of (i) reacting a compound of formula (II), wherein the symbols have the meaning given in formula (I), with a chlorinating agent, optionally in the presence of a radical initiator in a solvent selected from halogenated hydrocarbons, and (ii) crystallizing the compound (I) formed in step (i) from a solvent selected from chlorobenzene, 1,2-dichlorobenzene, 1,3-dichlorobenzene, 1,4-dichlorobenzene, dichloroethane, trichloromethane, dichloromethane, toluene, xylenes, ethyl acetate, methyl tert.-butyl ether, and mixtures thereof. Compounds (I) are useful intermediates in the synthesis of herbicidal imidazolinones.
    Type: Application
    Filed: March 20, 2014
    Publication date: July 24, 2014
    Applicant: BASF SE
    Inventors: Frederik MENGES, Joachim GEBHARDT, Michael RACK, Michael KEIL, Rodney F. KLIMA, David CORTES, Robert LEICHT, Helmut ZECH, Jochen SCHROEDER
  • Patent number: 8716319
    Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: May 6, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki
  • Publication number: 20140031557
    Abstract: A method for purification calcium ion channel blocker medicament of dihydropyridine type and pharmaceutically acceptable salts thereof through the ultrasonic crystallization technology and direct preparation of nanoparticles thereof.
    Type: Application
    Filed: April 14, 2012
    Publication date: January 30, 2014
    Applicant: HEFEIBEINIE MEDICAL TECHNOLOGY COMPANY, LTD.
    Inventor: Qiong Chen
  • Patent number: 8629279
    Abstract: A process for manufacturing a 5-formyl-pyridine-2,3-dicarboxylic acid ester (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro and R1, R2 are independently C1-C10-alkyl, comprising the steps of (i) reacting a compound of formula (II), wherein the symbols are as in formula (I), with a nitrosation agent (III) R3—O—N?O (III) wherein R3 is C1-C8-alkyl, in the presence of an alkali metal or alkaline earth metal alcoholates or carbonates in a polar aprotic solvent at a temperature of from ?45 to 40° C., to obtain an oxime compound (IV) where Z, Z1, R1 and R2 are as in formula (I), and (ii) reacting oxime compound (IV) with an aliphatic C1-C10-aldehyde in the presence of a Lewis acid at a temperature in the range of from 0 to 100° C. The compounds of formula (I) are useful intermediates in the synthesis of herbicidal imidazolinones, like imazamox.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: January 14, 2014
    Assignee: BASF SE
    Inventors: Michael Rack, Joachim Gebhardt, Frederik Menges, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schröder
  • Publication number: 20140005233
    Abstract: A composition having clevidipine as an active ingredient is described. The composition includes clevidipine as an active ingredient and an amount of the impurity H168/79 that is no greater than about 1.5%, or where the ratio between clevidipine and H168/79 is equal or above 60 to 1.
    Type: Application
    Filed: June 17, 2013
    Publication date: January 2, 2014
    Applicant: The Medicines Company
    Inventors: Rajeshwar Motheram, Gopal Krishna, Min Ding, Keith Flood, Kornepati Ramakrishna
  • Publication number: 20130324525
    Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: August 6, 2013
    Publication date: December 5, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
  • Publication number: 20130302736
    Abstract: A resist composition including a base material component whose solubility in a developing solution changes by the action of an acid and an acid generator component which generates an acid upon exposure. The acid generator component includes an acid generator that includes a compound containing nitrogen atoms having proton acceptor properties and sites capable of generating an acid upon exposure in the same molecule, the number of the sites being larger than the number of the nitrogen atoms.
    Type: Application
    Filed: April 30, 2013
    Publication date: November 14, 2013
    Applicant: Tokyo Ohka Kogyo Co., Ltd.
    Inventors: Yoshiyuki Utsumi, Yoshitaka Komuro, Tomoyuki Hirano
  • Patent number: 8492413
    Abstract: New compounds of 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type having general formula I wherein R is a lower alkyl group, which is methyl or ethyl R1 and R2 is sodium carboxylate-methyl ester, having synergistic cytotoxic effect combined with 5-fluorouracil.
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: July 23, 2013
    Assignee: JSC Grindeks
    Inventors: Gunars Duburs, Egils Bisenieks, Irina Sestakova, Ivars Kalvinsh, Brigita Vigante, Janis Uldrikis, Ilona Domraceva, Elina Jascenko, Janis Poikans, Imanta Bruvere, Ilmars Stonans
  • Patent number: 8455655
    Abstract: The invention relates to a method and compounds for the preparation of clevidipine butyrate, a very short acting hypertensive calcium antagonist, as well as the synthesis of these compounds useful for the preparation of clevidipine (also known as clevidipine butyrate). Moreover the invention also discloses polymorphic forms of clevidipine butyrate, useful for the preparation of pharmaceutical compositions, and processes to prepare them.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: June 4, 2013
    Assignee: Laboratorios Lesvi, S.L.
    Inventors: Ravindranath Vishnu Newadkar, Anil Purushottam Joshi, Santosh Kumar Singh
  • Publication number: 20130131126
    Abstract: 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type compounds having general formula I wherein R is hydrogen or carboxylate-methyl ester, R1 is sodium carboxylate-methyl ester R2 is methyl, ethyl or sodium carboxyate-methyl ester possessing antiviral efficacy.
    Type: Application
    Filed: July 15, 2011
    Publication date: May 23, 2013
    Applicant: JSC Grindeks
    Inventors: Ilmars Stonans, Ilze Jansone, Indra Jonane-Osa, Egils Bisenieks, Gunars Duburs, Ivars Kalvins, Brigita Vigante, Janis Uldrikis, Imanta Bruvere, Liga Zuka, Janis Poikans, Zaiga Neidere
  • Patent number: 8445688
    Abstract: The present invention relates to a process for preparation of optically pure (S)-amlodipine-L-hemitartrate DMF solvate comprising the steps of treating (R,S) amlodipine base with L-tartaric acid in the presence of dimethyl formamide and a co-solvent. The invention also relates to a process for converting (R) or (S)-amlopidine-L-hemitartrate DMF solvate into their besylates without isolating free chiral amlopidine base after solution.
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: May 21, 2013
    Assignee: Emcure Pharmaceuticals Limited
    Inventors: Milind Moreshwar Gharpure, Baburao Manikrao Bhawal, Prasad Vasudeo Ranade, Rajendra Dagadu Deshmukh, Satish Ramanlal Mehta
  • Patent number: 8436188
    Abstract: Disclosed is a method for the separation of S-(?)-amlodipine from a racemic amlodipine. Featuring the use of inexpensive L-tartaric acid as an optical resolution agent and DMAC as a solvent, the separation method allows the resolution of S-(?)-amlodipine from racemic amlodipine at high yield and to a satisfactory enantiomeric excess and thus is economically favorable and applicable to the mass production of the optical isomer.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: May 7, 2013
    Assignee: CJ Cheiljedang Corporation
    Inventors: Seog Beom Song, Il Hwan Cho, Yong Sik Youn, Dong Kwon Lim
  • Publication number: 20130053573
    Abstract: New triaminophenol compositions and related compounds are disclosed, as are processes for their preparation and for the preparation of novel salts and diacid complexes from such compounds. Polymers prepared from these compositions can be made into high strength fiber, film, and tape and are useful in applications such as protective apparel, aircraft, automotive components, personal electronics, and sports equipment.
    Type: Application
    Filed: December 21, 2010
    Publication date: February 28, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Rajiv Dhawan, Joachim C. Ritter
  • Patent number: 8362263
    Abstract: Disclosed are crystalline S-(?)-amlodipine adipic acid salt anhydrous and a preparation method thereof. The crystalline S-(?)-amlodipine adipic acid salt anhydrous exhibits excellent physical and chemical properties including non-hygroscopicity, solubility, thermal stability, and photostability, and is superior in formulation processability and long-term storage safety.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: January 29, 2013
    Assignee: CJ Cheiljedang Corporation
    Inventors: Il Hwan Cho, Yong Sik Youn, Seog Beom Song, Dong Kwon Lim
  • Publication number: 20120322835
    Abstract: A composition having clevidipine as an active ingredient is described. The composition includes clevidipine as an active ingredient and an amount of the impurity H168/79 that is no greater than about 1.5%, or where the ratio between clevidipine and H168/79 is equal or above 60 to 1.
    Type: Application
    Filed: August 30, 2012
    Publication date: December 20, 2012
    Inventors: Rajeshwar Motheram, Gopal Krishna, Min Ding, Keith Flood, Kornepati Ramakrishna
  • Publication number: 20120322836
    Abstract: Pharmaceutical compositions, and a method of stabilizing pharmaceutical compositions having clevidipine, or any pharmaceutically acceptable salt thereof, as the active ingredient is described. The method includes the slowing down or inhibiting of the oxidation pathway of clevidipine. This can be accomplished by reducing the amount the pharmaceutical composition is exposed to oxygen and/or light during the manufacturing and storing processes. According to this method, oxygen must be removed or replaced, or light must be sufficiently blocked such that light energy cannot reach the active ingredient of the composition, or is reduced to a level that the light-induced oxidation reaction converting clevidipine to H324/78 is minimized, such that the total detectable level of H324/78 in a given composition sample does not exceed about 0.2% on a weight-by-weight basis, or the ratio of clevidipine to H324/78 is equal to or greater than about 450 to 1 on a weight-to-weight basis.
    Type: Application
    Filed: August 30, 2012
    Publication date: December 20, 2012
    Inventors: Gopal Krishna, Rajeshwar Motheram, Min Ding
  • Publication number: 20120108818
    Abstract: The present invention relates to a microwave apparatus, a method or use of the apparatus and a method of carrying out chemical reactions on a continuous basis with the apparatus, wherein the apparatus is particularly suitable for microwave-assisted organic synthesis.
    Type: Application
    Filed: January 26, 2010
    Publication date: May 3, 2012
    Applicant: CAMBREX KARLSKOGA AB
    Inventors: Birger Hagberg, Lars Eklund
  • Patent number: 8163907
    Abstract: A dihydropyridine (DHP) calcium antagonist compound and its preparation method and medical use are related to preparation methods of compounds of general formulas (I) and (II) as shown below and their pharmaceutical salts and applications for treating cardiovascular diseases, and R1 represents a substituted or unsubstituted heterocyclic, aromatic ring or aralkyl group, and the substituent may be C1-C4 alkyl, C1-C4 alkoxyl, halogen, cyano, trifluoromethyl, trifluoromethoxyl, methylthio, nitro, amino or hydroxyl group; R2 represents a C1-C8 alkyl group; R3 and R4 are the same or different, and each represents a hydrogen, halogen, cyano, trifluoromethyl, trifluoromethoxyl, methylthio, nitro or amino group or a C1-C4 alkyl, C1-C4 alkoxyl, C1-C4 alkenyl, or C1-C4 alkinyl group; R5 and R6 are the same or different, and each represents a C1-C4 alkyl group; X represents O, S or a single bond; m=0-6, n=1-6, and m and n are the same or different.
    Type: Grant
    Filed: January 5, 2009
    Date of Patent: April 24, 2012
    Assignee: Cosunter Pharmaceutical Company
    Inventors: Guo-hua Chen, Li Wang
  • Patent number: 8129410
    Abstract: The invention includes benzisoxazole piperidine compositions and methods of using them for modulating sleep.
    Type: Grant
    Filed: April 26, 2006
    Date of Patent: March 6, 2012
    Assignee: Hypnion, Inc.
    Inventors: Daniel Coughlin, James F. White, Kazumi Shiosaki, David G. Hangauer, Michael Solomon, Dale M. Edgar
  • Publication number: 20120022088
    Abstract: New compounds of 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type having general formula I wherein R is a lower alkyl group, which is methyl or ethyl R1 and R2 is sodium carboxylate-methyl ester, having synergistic cytotoxic effect combined with 5-fluorouracil.
    Type: Application
    Filed: March 11, 2010
    Publication date: January 26, 2012
    Applicant: JSC GRINDEKS
    Inventors: Gunars Duburs, Egils Bisenieks, Irina Sestakova, Ivars Kalvinsh, Brigita Vigante, Janis Uldrikis, Ilona Domraceva, Elina Jascenko, Janis Poikans, Imanta Bruvere, Ilmars Stonans
  • Patent number: 8097729
    Abstract: Processes for the purification of lercanidipine hydrochloride are provided which uses a binary system of an alcohol-containing solvent such as methanol and an aliphatic ester-containing solvent such as isopropyl acetate. Processes for the preparation of substantially amorphous lercanidipine hydrochloride are also provided. Also provided is lercanidipine hydrochloride substantially in polymorph form V.
    Type: Grant
    Filed: September 18, 2006
    Date of Patent: January 17, 2012
    Assignee: Glenmark Generics Ltd.
    Inventors: Mangesh Shivram Sawant, Maloyesh Mathuresh Biswas, Mubeen Ahmed Khan, Sukumar Sinha, Nitin Sharad Chandra Pradhan
  • Publication number: 20120004349
    Abstract: The present invention provides a liquid curable epoxy resin composition that has excellent storage stability and curing properties and provides a cured product having excellent properties, particularly, excellent organic solvent resistance. For that purpose, a clathrate containing a carboxylic acid compound and at least one selected from the group consisting of an imidazole compound represented by formula (I), wherein R1 to R4 each represent a hydrogen atom or the like, and 1,8-diazabicyclo[5.4.0]undecene-7 (DBU) is mixed in an epoxy resin. The liquid curable epoxy resin composition uses a liquid epoxy resin or an organic solvent.
    Type: Application
    Filed: March 9, 2010
    Publication date: January 5, 2012
    Inventors: Masami Kaneko, Kazuo Ono, Natsuki Amanokura, Naoyuki Kamegaya
  • Publication number: 20110275825
    Abstract: The invention relates to a method and compounds for the preparation of clevidipine butyrate, a very short acting hypertensive calcium antagonist, as well as the synthesis of these compounds useful for the preparation of clevidipine (also known as clevidipine butyrate). Moreover the invention also discloses polymorphic forms of clevidipine butyrate, useful for the preparation of pharmaceutical compositions, and processes to prepare them.
    Type: Application
    Filed: May 6, 2011
    Publication date: November 10, 2011
    Applicant: LABORATORIOS LESVI, S.A.
    Inventors: RAVINDRANATH VISHNU NEWADKAR, Anil Purushottam Joshi, Santosh Kumar Singh
  • Publication number: 20110245505
    Abstract: A process for manufacturing a 5-formyl-pyridine-2,3-dicarboxylic acid ester (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro and R1, R2 are independently C1-C10-alkyl, comprising the steps of (i) reacting a compound of formula (II), wherein the symbols are as in formula (I), with a nitrosation agent (III) R3—O—N?O (III) wherein R3 is C1-C8-alkyl, in the presence of an alkali metal or alkaline earth metal alcoholates or carbonates in a polar aprotic solvent at a temperature of from ?45 to 40° C., to obtain an oxime compound (IV) where Z, Z1, R1 and R2 are as in formula (I), and (ii) reacting oxime compound (IV) with an aliphatic C1-C10-aldehyde in the presence of a Lewis acid at a temperature in the range of from 0 to 100° C. The compounds of formula (I) are useful intermediates in the synthesis of herbicidal imidazolinones, like imazamox.
    Type: Application
    Filed: December 7, 2009
    Publication date: October 6, 2011
    Applicant: BASF SE
    Inventors: Michael Rack, Joachim Gebhardt, Frederik Menges, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schröder
  • Publication number: 20110224433
    Abstract: A process for manufacturing 5,6-disubstituted-3-pyridylmethyl ammonium bromides (I), wherein Q is a tertiary aliphatic or cyclic, saturated, partially unsaturated or aromatic amine; Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; Y and Y1 are each independently OR1, NR1R2, or when taken together YY1 is —O—, —S— or NR3—; R1 and R2 are each independently hydrogen, C1-C4 alkyl optionally substituted with C1-C4 alkoxy or phenyl optionally substituted with one to three C1-C4 alkyl groups, C1-C4 alkoxy groups or halogen atoms, or phenyl optionally substituted with one to three C1-C4 alkyl groups, C1-C4 alkoxy groups or halogen atoms; R3 is hydrogen or C1-C4 alkyl; comprises the steps of (i) reacting a compound of formula (II), wherein the symbols have the meaning given in formula (I), with bromine in the presence of a radical initiator in a solvent mixture comprising an aqueous phase and an organic phase, where the organic phase comprises a solvent selected from 1,2-dichloroethane,
    Type: Application
    Filed: November 13, 2009
    Publication date: September 15, 2011
    Applicant: BASF SE
    Inventors: Joachim Gebhardt, Frederik Menges, Michael Rack, Michael Keil, Jochen Schroeder, Stefan Orsten, Helmut Zech, David Cortes, Robert Leicht, Tony Yegerlehner, Rodney F. Klima
  • Publication number: 20110224439
    Abstract: A process for manufacturing 5-chloromethyl-2,3-pyridine dicarboxylic acid anhydrides (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; comprising the steps of (i) reacting a compound of formula (II), wherein the symbols have the meaning given in formula (I), with a chlorinating agent, optionally in the presence of a radical initiator in a solvent selected from halogenated hydrocarbons, and (ii) crystallizing the compound (I) formed in step (i) from a solvent selected from chlorobenzene, 1,2-dichlorobenzene, 1,3-dichlorobenzene, 1,4-dichlorobenzene, dichloroethane, trichloromethane, dichloromethane, toluene, xylenes, ethyl acetate, methyl tert.-butyl ether, and mixtures thereof. Compounds (I) are useful intermediates in the synthesis of herbicidal imidazolinones.
    Type: Application
    Filed: November 13, 2008
    Publication date: September 15, 2011
    Inventors: Frederik Menges, Joachim Gebhardt, Michael Rach, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schroeder
  • Publication number: 20110201811
    Abstract: A dihydropyridine (DHP) calcium antagonist compound and its preparation method and medical use are related to preparation methods of compounds of general formulas (I) and (II) as shown below and their pharmaceutical salts and applications for treating cardiovascular diseases, and R1 represents a substituted or unsubstituted heterocyclic, aromatic ring or aralkyl group, and the substituent may be C1-C4 alkyl, C1-C4 alkoxyl, halogen, cyano, trifluoromethyl, trifluoromethoxyl, methylthio, nitro, amino or hydroxyl group; R2 represents a C1-C8 alkyl group; R3 and R4 are the same or different, and each represents a hydrogen, halogen, cyano, trifluoromethyl, trifluoromethoxyl, methylthio, nitro or amino group or a C1-C4 alkyl, C1-C4 alkoxyl, C1-C4 alkenyl, or C1-C4 alkinyl group; R5 and R6 are the same or different, and each represents a C1-C4 alkyl group; X represents O, S or a single bond; m=0-6, n=1-6, and m and n are the same or different.
    Type: Application
    Filed: January 5, 2009
    Publication date: August 18, 2011
    Inventors: Guo-hua Chen, Li Wang
  • Publication number: 20110118199
    Abstract: The present invention relates to the treatment of protozoal diseases by administering cytotoxic and/or cytostatic compounds, in particular those used in anticancer therapy, to patients. In particular, the invention relates to the use of anticancer agents that can penetrate into the CNS for treatment of late stage African sleeping sickness or cerebral malaria.
    Type: Application
    Filed: January 11, 2007
    Publication date: May 19, 2011
    Inventor: Matthias Dormeyer
  • Publication number: 20110098273
    Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.
    Type: Application
    Filed: September 3, 2008
    Publication date: April 28, 2011
    Applicant: Nektar Therapeutics
    Inventors: Zhongxu Ren, Bo-Liang Deng, Jennifer Riggs-Sauthier, Micah Harvey
  • Publication number: 20110087025
    Abstract: The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.
    Type: Application
    Filed: October 15, 2010
    Publication date: April 14, 2011
    Applicant: WILEX AG
    Inventors: Hugo Ziegler, Peter Wikstroem
  • Publication number: 20110040097
    Abstract: Disclosed herein is a novel method for preparing lercanidipine hydrochloride which is highly effective for treating hypertension. The method comprises the steps of reacting 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylic acid with a substituted chlorophosphate derivative to obtain a substituted phosphonoester derivative, and reacting the substituted phosphonoester derivative with 2, N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2-propanol. According to the preparation method, since little by-products are formed, the yield is improved, as compared to cases of conventional methods. In addition, the method involves simple isolation and purification processes of lercanidipine, thus realizing a high-quality product. Furthermore, the method has advantages of low preparation costs, substantial waste-free environmental-friendly process and applicability to industrial mass-production.
    Type: Application
    Filed: June 5, 2007
    Publication date: February 17, 2011
    Applicant: DONGWOO SYNTECH CO., LTD
    Inventors: Young-Deuck Kim, Jae-Yeon Shin
  • Publication number: 20110021783
    Abstract: The present invention relates to a process for preparation of optically pure (S)-amlodipine-L-hemitartrate DMF solvate comprising the steps of treating (R,S) amlodipine base with L-tartaric acid in the presence of dimethyl formamide and a co-solvent. The invention also relates to a process for converting (R) or (S)-amlopidine-L-hemitartrate DMF solvate into their besylates without isolating free chiral amlopidine base after solution.
    Type: Application
    Filed: September 30, 2010
    Publication date: January 27, 2011
    Inventors: Milind Moreshwar GHARPURE, Baburao Manikrao Bhawal, Prasad Vasudeo Ranade, Rajendra Dagadu Deshmukh, Satish Ramanlal Mehta
  • Patent number: 7858801
    Abstract: The present invention relates to a process for preparation of optically pure (S)-amlodipine-L-hemitartrate DMF solvate comprising the steps of treating (R,S) amlodipine base with L-tartaric acid in the presence of dimethyl formamide and a co-solvent. The invention also relates to a process for converting (R) or (S)-amlopidine-L-hemitartrate DMF solvate into their besylates without isolating free chiral amlopidine base after solution.
    Type: Grant
    Filed: October 17, 2005
    Date of Patent: December 28, 2010
    Assignee: Emcure Pharmaceuticals Limited
    Inventors: Milind Moreshwar Gharpure, Baburao Manikrao Bhawal, Prasad Vasudeo Ranade, Rajendra Dagadu Deshmukh, Satish Ramanlal Mehta
  • Publication number: 20100272726
    Abstract: A novel class of hydroxylases is described having the amino acid sequence of SEQ ID NO: 2, 4, 6 and 8, and variants and fragments thereof having HIF hydroxylation activity. The polypeptides of the invention have in particular prolyl hydroxylase activity. An assay method monitors the interaction of the HIF hydroxylase with a substrate. Modulators of HIF hydroxylase are provided for use in the treatment of a condition associated with increased or decreased HIF levels or activity or for the treatment of a condition where it is desirable to modulate HIF levels or activity.
    Type: Application
    Filed: January 12, 2010
    Publication date: October 28, 2010
    Inventors: Patrick Henry Maxwell, Christopher William Pugh, Peter John Ratcliffe, Christopher Joseph Schofield
  • Publication number: 20100267704
    Abstract: This invention pertains to a class of autophagy inducing compounds that treat diseases caused by misfolded protein aggregates and a screening method for identifying these compounds.
    Type: Application
    Filed: October 10, 2008
    Publication date: October 21, 2010
    Applicants: President an Fellows of Harvard Colege, Shangha Institute of Organic Chemistry Chineesse Academy of Sciences
    Inventors: Junying Yuan, Dawei Ma, Lihong Zhang
  • Publication number: 20100261765
    Abstract: The present invention relates to dihydropyridine mineralocorticoid receptor modulating compounds having the structure: and their use in treating cardiovascular events.
    Type: Application
    Filed: December 10, 2008
    Publication date: October 14, 2010
    Inventors: Philip E. Brandish, Mark E. Fraley, James C. Hershey, Justin T. Steen
  • Patent number: 7795439
    Abstract: A method for the in-situ treatment of a pyridine-2,3-dicarboxylic acid ester with an oxidizing agent, such as hydrogen peroxide, to improve product quality is provided. The method for the in-situ removal of impurities from a saponified solution of pyridine-2,3-dicarboxylic acid ester comprises the steps of providing a solution of pyridine-2,3-dicarboxylic acid ester, saponifying the solution with a base to form the corresponding pyridine-2,3-dicarboxylic acid salt, reacting the solution with an oxidizing agent in an amount effective to remove impurities, acidifying the solution with an acid to convert the pyridine-2,3-dicarboxylic acid into the corresponding pyridine-2,3-dicarboxylic acid, and collecting a purified solution comprising pyridine-2,3-dicarboxylic acid. Further provided is a method for the preparation of herbicidal 2-(2-imidazolin-2-yl)nicotinic acids, esters, and salts by using a pyridine-2,3-dicarboxylic acid salt prepared by the above method as an intermediate.
    Type: Grant
    Filed: June 25, 2004
    Date of Patent: September 14, 2010
    Assignee: BASF Aktiengesellschaft
    Inventor: Michael A. Levy
  • Publication number: 20100203135
    Abstract: Methods of forming soft connective tissue compositions such as skin equivalents, compositions made by the methods and their uses.
    Type: Application
    Filed: March 14, 2006
    Publication date: August 12, 2010
    Inventors: Paul Kemp, David Shering, Andrew Shering, Penny Johnson, Damian Marshall
  • Patent number: 7772400
    Abstract: The present invention relates to a method for optical resolution of amlodipines by using isopropanol solvent and optically active O,O?-dibenzoyl tartaric acid as chiral reagent. More particularly, the present invention relates to a method comprising (a) obtaining (R)- or (S)-amlodipine dibenzoyl tartrate salt or solvate thereof by reacting (R,S)-amlodipines with optically active O,O?-dibenzoyl tartaric acid in isopropanol solvent, and (b) treating the (R)- or (S)-amlodipine salt with a base, thus obtaining optically active amlodipine.
    Type: Grant
    Filed: December 2, 2005
    Date of Patent: August 10, 2010
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Jae-Sun Kim, Jin Young Choi, Nam Ho Kim, Nam Kyu Lee
  • Patent number: 7772401
    Abstract: The invention provides a novel process for the preparation of lercanidipine or a pharmaceutical acceptable salt using novel intermediates. Thus, 2,N-dimethyl-N-(3,3-diphenylpropy1)-1-amino-2-propanol is reacted with trimethylsilyl chloride in presence of triethyl amine in methylene chloride to give 2,N-dimethyl-2-(trimethylsilyloxy)-N-(3,3-diphenylpropy1)-1-propanamine, which is then reacted with 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carbonyl chloride for 2 hours and crystallized to obtain lercanidipine hydrochloride.
    Type: Grant
    Filed: October 22, 2009
    Date of Patent: August 10, 2010
    Assignee: Hetero Drugs Limited
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Dandamudi Satish Kumar
  • Publication number: 20100197684
    Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: February 9, 2010
    Publication date: August 5, 2010
    Applicant: Gilead Palo Alto, Inc.
    Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki
  • Publication number: 20100184989
    Abstract: The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.
    Type: Application
    Filed: March 12, 2008
    Publication date: July 22, 2010
    Applicant: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Zhongxu Ren, Wen Zhang, Xuyuan Gu, Franco J. Duarte