Additional Acyclic Nitrogen Or Acyclic Chalcogen In The 6-position Substituent Patents (Class 540/335)
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Publication number: 20120289471Abstract: The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.Type: ApplicationFiled: April 18, 2012Publication date: November 15, 2012Applicant: SIGNATURE R&D HOLDINGS, LLCInventor: V. Ravi Chandran
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Patent number: 7534781Abstract: The invention relates to crystalline amoxicillin trihydrate powder having a bulk density higher than 0.45 g/ml. The invention also relates to a process for preparing crystalline amoxicillin trihydrate powder, said process comprising: crystallizing amoxicillin trihydrate from a solution containing dissolved amoxicillin; separating the crystals from said solution; and drying the separated crystals, resulting in crystalline powder having a bulk density higher than 0.45 g/ml.Type: GrantFiled: March 19, 2004Date of Patent: May 19, 2009Assignee: DSM IP Assets B.V.Inventors: Jan Willem Groenendaal, Everardus Johannus Antonius Maria Leenderts, Thomas Van Der Does
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Patent number: 6103897Abstract: A process for the production of a crystalline salt of amoxicillin utilizing ethanol as a solvent, and crystallizing the salt of amoxicillin in the presence of a salifying compound.Type: GrantFiled: August 3, 1998Date of Patent: August 15, 2000Assignee: Biochemie Gesellschaft m.b.H.Inventors: Joan Cabre, Jose Diago, Asuncion Esteve, Johannes Ludescher
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Patent number: 6013647Abstract: This invention relates to new benzoxazinedione derivatives corresponding to the formula I: ##STR1## wherein R.sup.1 =H or carboxyalkyl, R.sup.2 =H, alkyl or phenyl, and R.sup.3 represents different acid groups derived from amino acids, dipeptides and hydrazones or conjugates thereof with active ingredients, e.g. antibiotics. The compounds may be present as free acids, in the form of their salts or as readily cleavable esters. The compounds according to the invention constitute heterocyclically protected catechol derivatives and are effective as siderophores against gram-negative bacterial strains, particularly against Pseudomonads and strains of E. coli and Salmonella. In the form of their conjugates with active ingredients, e.g. antibiotics (as "siderophore-antibiotic conjugates"), they can transport the latter into bacterial cells and can improve or extend the antibacterial effect thereof, sometimes even in relation to bacterial strains which are resistant to other .beta.-lactams.Type: GrantFiled: March 5, 1998Date of Patent: January 11, 2000Assignee: Gruenenthal GmbHInventors: Lothar Heinisch, Steffen Wittmann, Ute Moellmann, Rolf Reissbrodt
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Patent number: 5599987Abstract: An integrated process for producing cyclohexanone oxime, a caprolactam precursor, is provided wherein isopropanol is utilized to generate the hydrogen peroxide oxidizing agent. The acetone produced as a co-product is recycled back to the secondary alcohol by hydrogenation. Ammoximation of cyclohexanone is performed in the presence of water and an alcohol other than isopropanol such as methanol or t-butyl alcohol.Type: GrantFiled: March 31, 1995Date of Patent: February 4, 1997Assignee: Arco Chemical Technology, L.P.Inventors: Guy L. Crocco, John C. Jubin, Jr., John G. Zajacek
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Patent number: 5451701Abstract: An integrated process for producing cyclohexanone oxime, a caprolactam precursor, is provided wherein a secondary alcohol is utilized to generate the hydrogen peroxide oxidizing agent and as a reaction medium for ammoximation. The ketone produced as a co-product is recycled back to the secondary alcohol by hydrogenation.Type: GrantFiled: June 27, 1994Date of Patent: September 19, 1995Assignee: Arco Chemical Technology, L.P.Inventors: John G. Zajacek, John C. Jubin, Guy L. Crocco
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Patent number: 4918067Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or in-vivo hydrolysable ester thereof: ##STR1## wherein R.sup.1 is a 5 or 6 membered sulphur and/or nitrogen containing heterocyclic group substituted by an optionally protected amino group, with the proviso that R.sup.1 is not 2-aminothiazol-4-yl, and R is hydrogen; optionally substituted C.sub.1-12 alkyl; optionally substituted C.sub.2-12 alkenyl or alkynyl; carbocyclyl; aryl or heterocyclyl.These compounds have antibacterial properties, and therefore are of use in the treatment of bacterial infections in humans and animals caused by a wide range of organizations.Type: GrantFiled: July 22, 1987Date of Patent: April 17, 1990Assignee: Beecham Group p.l.c.Inventors: Brian C. Gasson, Michael J. Pearson
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Patent number: 4877783Abstract: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.Type: GrantFiled: January 24, 1985Date of Patent: October 31, 1989Assignee: Beecham Group p.l.c.Inventor: Peter H. Milner
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Patent number: 4866170Abstract: A stable trihydrate of (2S, 5R, 6R)-6-{(2R)-2-[(2R)-2-amino-3-(N-methylcarbamoyl)propionamido]-2-(p-hydrox yphenyl)acetamido}-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-c arboxylic acid and process for preparing the same are disclosed.Type: GrantFiled: September 18, 1987Date of Patent: September 12, 1989Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Susumu Ohshiro, Masaru Senuma, Mitsuyoshi Wagatsuma
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Patent number: 4801704Abstract: There are presented compounds of the formula ##STR1## wherein R.sub.2, R.sub.3, R.sub.4 and m are as described herein.Type: GrantFiled: May 16, 1988Date of Patent: January 31, 1989Assignee: Hoffman-La Roche Inc.Inventors: Dennis D. Keith, Chung-Chen Wei, Manfred Weigele
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Patent number: 4769325Abstract: 2-(Allenyl)penicillins antibiotics and intermediates thereto are disclosed. A process for making the 2-(allenyl)penicillins and the starting materials for the process are also disclosed.Type: GrantFiled: July 28, 1986Date of Patent: September 6, 1988Inventors: Jack E. Baldwin, Amit Basak