Purification Or Recovery Patents (Class 540/220)
  • Patent number: 9187482
    Abstract: Disclosed is a compound of formula (I): crystalline forms thereof, and solvates thereof; pharmaceutical compositions comprising a pharmaceutically effective amount of the compound of formula (I), or a crystalline form thereof, or a solvate thereof, and a pharmaceutically acceptable carrier or diluent; and the use of a compound of formula (I), or a crystalline form thereof, or a solvate thereof, for treating a patient suffering from, or subject to, a pathological condition capable of being ameliorated by inhibiting an E1 activating enzyme, particularly NAE, including, e.g., cancer.
    Type: Grant
    Filed: May 13, 2010
    Date of Patent: November 17, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Ian G. Armitage, Reenu Chopra, Martin Ian Cooper, Marianne Langston, Steven P. Langston, Stepan Vyskocil
  • Publication number: 20150005491
    Abstract: A solid DMSO solvate of a compound of formula (I) is described, which is a useful intermediate for preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril.
    Type: Application
    Filed: September 15, 2014
    Publication date: January 1, 2015
    Applicant: Basilea Pharmaceutica AG
    Inventors: Marco Alpegiani, JR., Walter Cabri, Markus Heubes, Davide Longoni, Michael Schleimer
  • Patent number: 8859761
    Abstract: It discloses a novel process for refining cefamandole nafate, comprising: 1) adsorbing cefamandole nafate with strongly acidic ion exchange resin, followed by eluting the resin and collecting the eluate, to provide a primary purified cefamandole acid after concentration under reduced pressure; 2) neutralizing the primary purified cefamandole acid with an aqueous solution of sodium hydroxide or an aqueous solution of basic salt of sodium, followed by adjusting the pH value and filtrating out the insoluble substances with heating, thereby providing a secondary purified aqueous solution of cefamandole nafate; and 3) adding ethanol in a volume ratio between ethanol and water of 4:6 into the aqueous solution, to allow recrystallization under controlling the temperature, to provide a tertiary purified cefamandole nafate. The refined cefamandole nafate product has a purity of no less than 99.5%, mostly no less than 99.6%, with significantly low content of heavy metals.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: October 14, 2014
    Assignee: Hainan Lingkang Pharmaceutical Co., Ltd.
    Inventor: Linggang Tao
  • Patent number: 8853389
    Abstract: The present invention relates to a novel process for refining Cefmetazole sodium, comprising the steps of: 1) dissolving Cefmetazole sodium material in water, and extracting after adding a water-immiscible organic solvent(s), followed by separating the organic phase containing impurities, to provide an aqueous phase containing Cefmetazole sodium; 2) treating by adding an alkoxide of alkali metal or alkaline earth metal into the above aqueous phase, followed by filtrating the precipitate, to provide an aqueous filtrate; and 3) adding ethanol or acetone in the aqueous solution and recrystallizing, followed by centrifuging and washing the resultant crystals, to provide the refined and purified Cefmetazole sodium after drying. The purity of Cefmetazole sodium material can be greatly improved by the process of the present invention.
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: October 7, 2014
    Assignee: Hainan Lingkang Pharmaceutical Co., Ltd.
    Inventor: Linggang Tao
  • Publication number: 20140005381
    Abstract: The present invention relates to a novel process for refining Cefmetazole sodium, comprising the steps of: 1) dissolving Cefmetazole sodium material in water, and extracting after adding a water-immiscible organic solvent(s), followed by separating the organic phase containing impurities, to provide an aqueous phase containing Cefmetazole sodium; 2) treating by adding an alkoxide of alkali metal or alkaline earth metal into the above aqueous phase, followed by filtrating the precipitate, to provide an aqueous filtrate; and 3) adding ethanol or acetone in the aqueous solution and recrystallizing, followed by centrifuging and washing the resultant crystals, to provide the refined and purified Cefmetazole sodium after drying. The purity of Cefmetazole sodium material can be greatly improved by the process of the present invention.
    Type: Application
    Filed: April 14, 2011
    Publication date: January 2, 2014
    Applicant: HAINAN LINGKANG PHARMACEUTICAL CO., LTD.
    Inventor: Linggang Tao
  • Patent number: 8058425
    Abstract: The present invention provides kinase inhibitors of Formula I.
    Type: Grant
    Filed: May 4, 2011
    Date of Patent: November 15, 2011
    Assignee: Eli Lilly and Company
    Inventors: Thomas Albert Engler, Timothy Paul Burkholder, Joshua Ryan Clayton, Clive Gideon Diefenbacher, Kelly Wayne Furness, James Robert Henry, Yihong Li, Sushant Malhotra, Angela Lynn Marquart, Johnathan Alexander McLean, David Mendel, Jon Kevin Reel, Brian Raymond Berridge, Charles Edward Ruegg, John Morris Sullivan
  • Publication number: 20110137026
    Abstract: A solid DMSO solvate of a compound of formula (I) is described, which is a useful intermediate for preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril.
    Type: Application
    Filed: April 14, 2009
    Publication date: June 9, 2011
    Applicant: BASILEA PHARMACEUTICA AG
    Inventors: Marco Alpegiani, Walter Cabri, Markus Heubes, Davide Longoni, Michael Schleimer
  • Patent number: 7893254
    Abstract: A process for preparing 7-amino-3-[(E/Z)-2-(4-methylthiazol-5-yl)vinyl]-3-cephem-4-carboxylic acid of the formula (1) and an alkali metal salt thereof, said acid and said salt being improved in the content of 7-amino-3-[(Z)-2-(4-methylthiazol-5-yl)vinyl]-3-cephem-4-carboxylic acid of the formula (2) or an alkali metal salt thereof, the process being characterized in that an aqueous solution of an alkali metal salt of 7-amino-3-[(E/Z)-2-(4-methylthiazol-5-yl)vinyl]-3-cephem-4-carboxylic acid of the formula (1) is treated with a high porous polymer and/or active carbon as added thereto.
    Type: Grant
    Filed: June 3, 2005
    Date of Patent: February 22, 2011
    Assignees: Otsuka Chemical Co., Ltd., Meiji Seika Kaisha Ltd.
    Inventors: Yoichi Nishioka, Masahiro Ito, Yutaka Kameyama
  • Patent number: 7759483
    Abstract: A 3-alkenylcephem compound of the formula (1) wherein R1 is benzyl or phenoxymethyl, R2, R3 and R4 are alike or different and are each a hydrogen atom, C1-10 alkyl, C4-8 cycloalkyl or aryl C1-3 alkyl substituted or unsubstituted with C1-4 alkyl, R2 and R3, when taken together, form a group —(CH2)lXm(CH2)n— substituted or unsubstituted with C1-4 alkyl at an optional position, X is an oxygen atom or group —N(R5)—, l is 0 to 3, m is 0 or 1, n is an integer of 2 to 4, R5 is a hydrogen atom or C1-4 alkyl.
    Type: Grant
    Filed: June 2, 2005
    Date of Patent: July 20, 2010
    Assignee: Otsuka Chemical Co., Ltd.
    Inventors: Yoichi Nishioka, Koichi Sorajo, Yutaka Kameyama
  • Patent number: 7560545
    Abstract: The invention relates to a method for obtaining cefotetan acid substantially free of tautomer, by treating crude cefotetan with Al3+ ions which cause the tautomer to precipitate. The precipitate is eliminated by filtration to provide a solution from which practically tautomer-free cefotetan is obtained.
    Type: Grant
    Filed: May 12, 2006
    Date of Patent: July 14, 2009
    Assignee: ACS Dobfar S.p.A.
    Inventors: Maurizio Zenoni, Antonio Manca, Riccardo Monguzzi
  • Patent number: 7544677
    Abstract: The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: June 9, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, Nicholas D. P. Cosford, John C. Hartnett, Yiwei Li, Jun Liang, Peter J. Manley, Lou Anne Neilson, Tony Siu, Zhicai Wu
  • Patent number: 7507813
    Abstract: A novel process for the preparation of amorphous cefuroxime axetil particles and the amorphous cefuroxime axetil particles therefrom are disclosed in the invention. Specifically, the invention is implemented by means of antisolvent recrystallization to prepare the cefuroxime axetil in an amorphous form; particularly, the amorphous ultrafine or even nanosized cefuroxime axetil with a controllable particle size and a narrow particle size distribution. The cefuroxime axetil according to the invention can used to enhance bioavailability, since it is in an amorphous form and has a controllable particle size and a narrow particle size distribution.
    Type: Grant
    Filed: July 22, 2005
    Date of Patent: March 24, 2009
    Assignees: Nanomaterials Technology Pte Ltd., Beijing University of Chemical Technology
    Inventors: Jianfeng Chen, Jie Zhong, Zhigang Shen, Jiyao Zhang
  • Publication number: 20080287673
    Abstract: The present invention provides an improved process for the preparation of high assayed cefdinir. Thus, crude cefdinir is added to water at 25-30° C. and then 18% hydrochloric acid is slowly added to form a clear solution. The solution is cooled to ?5° C. and stirred for 5 minutes at ?5° C. to +5° C. Then temperature of the mass is raised to 35-38° C., stirred for 15 minutes at the same temperature. To the reaction mass eno carbon is added at 35-38° C. and stirred for 30 minutes at 35-38° C. Then the contents are filtered on hiflo bed and washed with water. The filtrate is then cooled to 25° C., the pH is slowly adjusted to 2.6 with saturated sodium bicarbonate solution and stirred for 60 minutes at 25-30° C. Filtered the solid, washed with water and dried at 40° C. under vacuum to give high assayed cefdinir.
    Type: Application
    Filed: June 15, 2005
    Publication date: November 20, 2008
    Inventor: Bandk PARTHASARADHI REDDY
  • Patent number: 7045618
    Abstract: The present invention relates to an improved and cost effective process for the industrial manufacture of cefpodoxime proxetil. More specifically, the present invention relates to the preparation of cefpodoxime proxetil of high purity and yield. The process comprises a) dissolving impure cefpodoxime proxetil or adding a solution containing cefpodoxime proxetil into a polar organic solvent or mixture(s) thereof, optionally reducing the solvent by concentration, and adding into a non-polar organic solvent or mixture(s) thereof to precipitate the solid; and b) dissolving the solid obtained from the above step into water-miscible polar organic solvent, optionally reducing the solvent by concentration, adding it into water to obtain the pure cefpodoxime proxetil.
    Type: Grant
    Filed: February 27, 2002
    Date of Patent: May 16, 2006
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Yatendra Kumar, Kaptan Singh, Rakesh Kumar Arora
  • Patent number: 6949641
    Abstract: The novel intermediate compound crystalline 7-[2-(2-fomylaminothiazol-4-yl)-2 -(Z)-(methoxyimino)acetamido]-3-methoxymethyl-3-cephem-4-carboxylic acid-1 -(isopropoxy/crystallization of cefpodoxime proxetil. The crystallization process comprises dissolving or suspending the intermediate in the presence of a nitrile or a ketone or mixtures thereof; at a ratio of 1 gm of the intermediate to 2-15 ml nitrile; or at a ratio of 1 gm of the intermediate to 3-15 ml ketone; in the presence of 5-80 ml water; and thereafter isolating the intermediate in crystalline form and converting the intermediate by splitting off the formyl group from the amino group attached to the thiazolyl group, to obtain the desired product cefpodoxime proxetil, in the form of a diastereoisomeric mixture in a ratio of B/(A+B) of 0.5 to 0.6.
    Type: Grant
    Filed: October 31, 2001
    Date of Patent: September 27, 2005
    Assignee: Sandoz AG
    Inventors: Julia Greil, Johannes Ludescher, Klaus Totschnig, Siegfried Wolf
  • Patent number: 6835829
    Abstract: Processes for the depletion of 7-ADCA in mixtures of vinyl-ACA with 7-ADCA via novel salts of vinyl-ACA or via chromatography.
    Type: Grant
    Filed: January 21, 2003
    Date of Patent: December 28, 2004
    Assignee: Sandoz GmbH
    Inventors: Johannes Ludescher, Werner Veit
  • Patent number: 6803460
    Abstract: A method for the recovery of an N-substituted cephalosporanic acid compound of general formula (I), wherein R2 is selected from the group consisting of adipyl (1,4-dicarboxybutane), succinyl, glutaryl, adipyl, pimelyl, suberyl, 2-carboxyethyithio)acetyl, 3-carboxyethylthio)propionyl, higher alkyl saturated and higher alkyl unsaturated dicarboxylic acids, from a complex mixture comprising in addition to the compound of general formula (I) 6-aminopenicillanic acid (6-APA) and optionally one or more N-substituted penicillanic acid compounds, comprising the steps of: (a) acidifying the complex mixture to a pH below 6.5 and maintaining the mixture below said pH at a temperature of between 10° C. and 150° C.; and/or (b) contacting the complex mixture with a carbon dioxide source; and (c) recovering the cephalosporanic acid compound of formula (I) from the mixture obtained after steps (a) and/or (b).
    Type: Grant
    Filed: September 24, 2002
    Date of Patent: October 12, 2004
    Assignee: DSM IP Assets B.V.
    Inventors: Ilco Adrainus Lambertus Antonius Boogers, Emilius Johannes Albertus Xaverius Van De Sandt, Dick Schipper
  • Publication number: 20040092734
    Abstract: The present invention relates to an improved and cost effective process for the industrial manufacture of cefpodoxime proxetil. More specifically, the present invention relates to the preparation of cefpodoxime proxetil of high purity and yield.
    Type: Application
    Filed: December 18, 2003
    Publication date: May 13, 2004
    Inventors: Yatendra Kumar, Kaptan Singh, Rakesh Kumar Arora
  • Publication number: 20030153747
    Abstract: Processes for the depletion of 7-ADCA in mixtures of vinyl-ACA with 7-ADCA via novel salts of vinyl-ACA or via chromatography.
    Type: Application
    Filed: January 21, 2003
    Publication date: August 14, 2003
    Inventors: Johannes Ludescher, Werner Veit
  • Patent number: 6602999
    Abstract: A novel process for the production of an improved amorphous form of cefpodoxime proxetil [(6R-[6&agr;,7&bgr;(Z))]-7-{E(2-Amino-4-thiazolyl)(methoxyimino)acetyl]amino]-3-(methoxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid-1-[[(1-methylethoxy)carboxylic acid-1-[[(1-methylethoxy)carbonyl]oxy]ethyl ester, is described.
    Type: Grant
    Filed: May 21, 2002
    Date of Patent: August 5, 2003
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Yatendra Kumar, Rakesh Kumar Arora, Kaptan Singh
  • Publication number: 20030139595
    Abstract: A method for the recovery of an N-substituted cephalosporanic acid compound of general formula (I), wherein R2 is selected from the group consisting of adipyl (1,4-dicarboxybutane), succinyl, glutaryl adipyl, pimelyl, suberyl, 2-carboxyethyithio)acetyl, 3-carboxyethylthio)propionyl, higher alkyl saturated and higher alkyl unsaturated dicarboxylic acids, from a complex mixture comprising in addition to the compound of general formula (I) 6-aminopenicillanic acid (6-APA) and optionally one or more N-substituted penicillanic acid compounds, comprising the steps of: (a) acidifying the complex mixture to a pH below 6.5 and maintaining the mixture below said pH at a temperature of between 10° C. and 150° C.; and/or (b) contacting the complex mixture with a carbon dioxide source; and (c) recovering the cephalosporanic acid compound of formula (I) from the mixture obtained after steps (a) and/or (b).
    Type: Application
    Filed: September 24, 2002
    Publication date: July 24, 2003
    Inventors: Ilco Adrianus Lambertus Antonius Boogers, Emilius Johannes Albertus Xaverius Van De Sandt, Dick Schipper
  • Patent number: 6552185
    Abstract: A method for the recovery of a compound formula (I) from a complex mixture, comprising the steps of: (a) acidifying the complex mixture to a pH below 6.5 and maintaining the mixture below said pH at a temperature of between 50° C. and 130° C.; and/or (b) contacting the complex mixture with a carbon dioxide source; and (c) subjecting the mixture obtained after steps (a) and/or (b) to chromatography to obtain the compound of formula (I).
    Type: Grant
    Filed: November 16, 2000
    Date of Patent: April 22, 2003
    Assignee: DSM N.V.
    Inventors: Ilco Adrianus Lambertus Antonius Boogers, Emilius Johannes Albertus Xaverius Van De Sandt, Dick Schipper
  • Patent number: 6504026
    Abstract: Process for preparing ceftiofur having formula I: in the form of the sodium salt.
    Type: Grant
    Filed: November 20, 2001
    Date of Patent: January 7, 2003
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Andreas Berger, Martin Decristoforo, Johannes Ludescher, Herbert Schleich
  • Patent number: 6489470
    Abstract: A process for increasing the diastereoisomeric ratio (B/A+B), wherein B is the more apolar and A is the more polar of two diastereoisomers, of a mixture of diastereoisomers of a compound of formula the diastereoisomers being with respect to the carbon atom marked with a star in formula I, comprising treating a mixture of diastereoisomers of a compound of formula I with alcohol and water and isolating the precipitated compound of formula I in an increased diastereoisomeric ratio (B/A+B) of 0.5 to 0.6.
    Type: Grant
    Filed: August 21, 2000
    Date of Patent: December 3, 2002
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Julia Greil, Johannes Ludescher, Klaus Totschnig, Siegfried Wolf
  • Patent number: 6350869
    Abstract: Cefdinir in the form of a salt with dicyclohexylamine, a process for its production and its use in the purification of impure cefdinir.
    Type: Grant
    Filed: September 27, 1999
    Date of Patent: February 26, 2002
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Hubert Sturm, Siegfried Wolf, Johannes Ludescher
  • Publication number: 20020004079
    Abstract: A process for extracting a compound or composition of matter from a raw material containing that compound or composition as a constituent part is described. The process comprises the steps of (1) contacting a sample of the raw material with an extraction solvent comprising a C1-4 (hydro)fluorocarbon alone or with a co-solvent, and (2) separating the solvent liquor thus obtained containing the extract from the raw material. The process may be used to extract natural products, such as flavored or aromatic oils, and biologically active compounds, such as pesticides and pharmaceuticals.
    Type: Application
    Filed: April 26, 2001
    Publication date: January 10, 2002
    Inventors: Richard Llewellyn Powell, Timothy James Noakes
  • Publication number: 20010044533
    Abstract: Processes for the depletion of 7-ADCA in mixtures of vinyl-ACA with 7-ADCA via novel salts of vinyl-ACA or via chromatography.
    Type: Application
    Filed: June 13, 2001
    Publication date: November 22, 2001
    Inventors: Johannes Ludescher, Werner Veit
  • Publication number: 20010037019
    Abstract: Processes for the depletion of 7-ADCA in mixtures of vinyl-ACA with 7-ADCA via novel salts of vinyl-ACA or via chromatography.
    Type: Application
    Filed: May 25, 2001
    Publication date: November 1, 2001
    Inventors: Johannes Ludescher, Werner Veit
  • Patent number: 6288223
    Abstract: There can be produced, at a high selectivity and in a high yield, the Z-isomer of a 7-N-unsubstituted or substituted-amino-3-[2-(4-substituted or unsubstituted-thiazol-5-yl) vinyl]-3-cephem-4-carboxylic acid or an ester thereof having the general formula (IV) wherein R1 denotes a hydrogen atom, a mono-valent amino-protecting group or a 2-(2-N-protected or unprotected aminothiazol-4-yl)- 2-alkoxyiminoacetyl group, R2 denotes a hydrogen atom, or R1 and R2 as taken together mean one di-valent amino-protecting group, R3 denotes a hydrogen atom, pivaloyloxymethyl group or a carboxyl-protecting group and R8 denotes an alkyl group and so on, by a process comprising reacting a 7-N-unsubstituted or substituted-amino-3-[(tri-substituted-phosphoranylidene) methyl]-3-cephem-4-carboxylic acid or an ester thereof having the general formula (I) wherein R1, R2 and R3 each have the same meanings as defined above, and R4 denotes a lower alryl group or an aryl group, with
    Type: Grant
    Filed: February 18, 2000
    Date of Patent: September 11, 2001
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Yumiko Okada, Masamichi Sukegawa, Tatsuo Watanabe, Hiroyuki Iwasawa, Yasushi Murai, Katsuharu Iinuma
  • Patent number: 6284888
    Abstract: A process for purification of vinyl-ACA of formula from a mixture of vinyl-ACA and 7-ADCA of formula is provided. The process comprises a) producing a mixture of a salt of vinyl-ACA and a salt of 7-ADCA in a solvent in which the salt of 7-ADCA has a higher solubility than the salt of vinyl-ACA, and b) subjecting the mixture to crystallization to obtain a precipitate of the salt of vinyl-ACA. A process of purifying vinyl-ACA from a mixture of vinyl-ACA and 7-ADCA via chromatography, particularly adsorption chromatography is also provided.
    Type: Grant
    Filed: May 9, 2000
    Date of Patent: September 4, 2001
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Johannes Ludescher, Werner Veit
  • Patent number: 6172221
    Abstract: A back extraction process in which beta-lactam antibiotics or clavulanic acid is extracted from an organic solvent phase into an aqeous medium phase, using a mixing region in which the phases are mixed rapidly under high turbulence and shear stress.
    Type: Grant
    Filed: August 27, 1997
    Date of Patent: January 9, 2001
    Assignee: SmithKline Beecham p.l.c.
    Inventor: Simon Ruddick
  • Patent number: 6100393
    Abstract: Process for purifying 7-substituted aminodeacetoxycephalosporins through the use of filter membranes. A process for purification by ultrafiltration and/or nanofiltration with a cut-off for molecular weights over 10,000 Dalton and preferably over 2000 Dalton is described. For example cephalosporin-G of increased purity, represented by a 6-8% increase in the HPLC titre, with a reduction of 50% in absorbance, is obtained using this technique. The invention makes it possible for the purified products to be used directly in the synthesis of other antibiotic compounds without the need for intermediate isolation.
    Type: Grant
    Filed: February 25, 1998
    Date of Patent: August 8, 2000
    Assignee: Antibioticos, S.A.
    Inventors: Juan Francisco Lopez Ortiz, Oscar Ferrero Barruego, Emiliano Gonzalez de Prado, Alejandro Vitaller Alba, Francisco Salto Maldonado
  • Patent number: 5874571
    Abstract: The disclosed process is for the recovery of cephalexin from a mixture containing cephalexin and 7-aminodesacetoxy cephalosporanic acid (7-ADCA), wherein a mixture of cephalexin and 7-ADCA, with a pH higher than 7, which apart from any solid cephalexin being present is homogeneous at a pH between 7 and 8.5, is subjected to a pH modification until a pH lower than 7.8 is reached, and the solid substance is recovered. The disclosed process is particularly suited for application to a reaction mixture obtained after the enzymatic acylation reaction of 7-ADCA with a phenylglycine derivative as an acylation agent. Pure cephalexin can thus be recovered in a simple manner.
    Type: Grant
    Filed: July 31, 1997
    Date of Patent: February 23, 1999
    Assignee: Chemferm V.O.F.
    Inventors: Wilhelmus H. J. Boesten, Eric C. Roos, Wilhelmus J. J. van den Tweel
  • Patent number: 5739324
    Abstract: A process for preparing cyclic lactams by reacting amino carbonitriles with water in liquid phase in the presence of heterogeneous catalysts based on titanium dioxide, zirconium oxide, cerium oxide and aluminum oxide.
    Type: Grant
    Filed: May 16, 1996
    Date of Patent: April 14, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Eberhard Fuchs, Tom Witzel
  • Patent number: 5693790
    Abstract: The preparation of a novel crystalline cefaclor and the conversion of such a product to cefaclor monohydrate are described. The new intermediate cefaclor is a particular crystalline form and possesses the same antibiotic properties as cefaclor monohydrate.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: December 2, 1997
    Assignee: Biochimica Opos Spa
    Inventors: Marco Da Col, Leone Dall'Asta, Irene Resta
  • Patent number: 5686588
    Abstract: A stoichiometric acid moiety transfer reaction for the preparation of an acid salt of an amine compound is disclosed. The acid moiety transfer reaction provides amine acid salts of high purity and having crystalline structure of uniform size and shape.
    Type: Grant
    Filed: August 16, 1995
    Date of Patent: November 11, 1997
    Inventor: Seo Hong Yoo
  • Patent number: 5589593
    Abstract: The preparation of a novel crystalline cefaclor and the conversion of such a product to cefaclor monohydrate are described. The new intermediate cefaclor is a particular crystalline form and possesses the same antibiotic properties as cefaclor monohydrate.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 31, 1996
    Assignee: Biochimica Opos SpA
    Inventors: Marco Da Col, Leone Dall'Asta, Irene Resta
  • Patent number: 4973685
    Abstract: Heteroannellated penicillins and cephalosporins of the formula ##STR1## in which R.sup.
    Type: Grant
    Filed: September 28, 1988
    Date of Patent: November 27, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunter Schmidt, Karl G. Metzger, Hans-Joachim Zeiler
  • Patent number: 4820833
    Abstract: There is described a product which is a highly pure substantially amorphous form of cefuroxime axetil (cefuroxime 1-acetoxyethyl ester) which is stable, which has increased absorption via the gastro-intestinal tract and has a correspondingly high level of bioavailability on oral or rectal administration.Methods of preparing the product are also described which involve the recovery of the product from a solution thereof. A preferred method is the use of spray drying techniques, though roller drying, solvent precipitation or freeze-drying are also described.Also disclosed are pharmaceutical compositions containing the product and methods for its use in medicine.
    Type: Grant
    Filed: December 4, 1986
    Date of Patent: April 11, 1989
    Assignee: Glaxo Group Limited
    Inventors: Harold A. Crisp, John C. Clayton, Leonard G. Elliott, Edward M. Wilson
  • Patent number: 4775751
    Abstract: The crystalline ethanol or methanol solvates of cephalexin hydrochloride are isolated in high yield from solutions of cephalexin hydrochloride in substantially anhydrous ethanol or methanol, respectively, by adding miscible C.sub.5 -C.sub.6 alkanes after initiating solvate crystallization. Ethanol or methanol solutions of cephalexin hydrochloride can be prepared by adding gaseous HCl to the respective alcohol slurries of cephalexin monohydrate or the novel crystalline ethanolate or desolvated ethanolate. Alternatively, the cephalexin bis-DMF solvate-derived cephalexin hydrochloride isopropanolate can be used to prepare the crystalline hydrochloride monohydrate in accordance with the disclosed improved method.
    Type: Grant
    Filed: June 3, 1985
    Date of Patent: October 4, 1988
    Assignee: Eli Lilly & Company
    Inventor: Lawrence J. McShane
  • Patent number: 4727070
    Abstract: The antibiotic 7-[D-2-amino-2-(4-hydroxyphenyl)acetamido]-3-[(Z)-1-propenyl]ceph-3-em-4-c arboxylic acid (BMY-28100) forms imidazolidinone derivatives on reaction with ketones. These derivatives are useful in pharmaceutical dosage forms and as intermediates for separation thereof from mixtures containing the [(E)-1-propenyl]isomer of the antibiotic.
    Type: Grant
    Filed: November 25, 1985
    Date of Patent: February 23, 1988
    Assignee: Bristol-Myers Company
    Inventors: Murray A. Kaplan, Michael W. Lovell, Joseph B. Bogardus
  • Patent number: 4719287
    Abstract: The extraction of water soluble antibiotics containing a phenolic or carboxylic group from an aqueous solution or fermentation broth using a N--C.sub.8 --C.sub.14 alkyl pyrrolidone extractant and the process involving the extraction of said antibiotic.
    Type: Grant
    Filed: February 12, 1987
    Date of Patent: January 12, 1988
    Assignee: GAF Corporation
    Inventors: Robert B. Login, Ratan K. Chaudhuri
  • Patent number: 4684641
    Abstract: 7.alpha.-Hydroxyamino-7.beta.-[2-substituted-2-(acylamino)acetamido]-cephal osporin antibiotics, pharmaceutically-acceptable salts and in vivo hydrolyzable esters thereof, a method of treating susceptible infections therewith, and intermediates therefor.
    Type: Grant
    Filed: June 27, 1985
    Date of Patent: August 4, 1987
    Assignee: Pfizer Inc.
    Inventors: Colin W. Greengrass, David W. T. Hoople, Thomas T. Howarth
  • Patent number: 4668782
    Abstract: An anhydrous crystalline, or crystalline hemihydrate, monohydrate or trihydrate of cephalosporin derivative of (6R,7R)-7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxy-iminoacetoamido]-3(1-qui nuclidiniummethyl)-3-cephem-4-carboxylate. These crystalline materials can maintain outstanding stability for a very long period of time and afford excellent practical uses as pharmaceutical compounds.
    Type: Grant
    Filed: December 17, 1985
    Date of Patent: May 26, 1987
    Assignee: Teijin Limited
    Inventors: Yataro Ichikawa, Eishin Yoshisato, Toshiaki Harada, Hiroshi Imai, Yoji Suzuki