Plural Nitrogens Bonded Directly To The Tetracyclo Ring System Patents (Class 552/205)
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Publication number: 20100160265Abstract: 7, 8 and 9-substituted tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7, 8 and 9-substituted tetracycline compounds are described.Type: ApplicationFiled: March 9, 2010Publication date: June 24, 2010Applicant: Trustees of Tufts CollegeInventors: Mark L. Nelson, Darrell J. Koza, Glen Rennie
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Publication number: 20100160264Abstract: The present invention relates to the new crystalline solid form VI and VIII of tigecycline and processes for the production of form VI and VIII. It further relates to a new method for preparing Form I and Form III in high polymorphic purity.Type: ApplicationFiled: June 20, 2008Publication date: June 24, 2010Inventors: Josef Wieser, Arthur Pichler, Andreas Hotter
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Publication number: 20100152142Abstract: The present invention provides processes for the preparation of crystalline forms of Tigecycline.Type: ApplicationFiled: December 1, 2008Publication date: June 17, 2010Inventors: Sigalit Levi, Michal Rafilovich, Sofia Gorohovsky-Rosenberg, Slavik Yurkovski, Sergei Fine, Leonid Metsger, Evgeny Tsiperman
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Publication number: 20100113401Abstract: Methods for the synthesis and purification of 9-amino alkyl tetracycline compounds are described.Type: ApplicationFiled: October 29, 2009Publication date: May 6, 2010Applicant: Paratek Pharmaceuticals, Inc.Inventors: Sean Johnston, Tadeusz Warchol
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Publication number: 20100113400Abstract: The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and minocycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.Type: ApplicationFiled: May 28, 2009Publication date: May 6, 2010Applicant: Paratek Pharmaceuticals, Inc.Inventors: Mark L. Nelson, Roger Frechette, Mohamed Y. Ismail, Laura Honeyman, Todd Bowser, Beena Bhatia
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Publication number: 20100075929Abstract: A compound of formula (I):Type: ApplicationFiled: November 24, 2009Publication date: March 25, 2010Applicant: Paratek Pharmaceuticals, Inc.Inventors: Carmen García-Luzón, Juan Carlos Cuevas, Jose M. Fiandor, Araceli Mallo, Mark L. Nelson, Roger Frechette
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Patent number: 7652002Abstract: A compound of formula (I):Type: GrantFiled: December 20, 2006Date of Patent: January 26, 2010Assignee: Paratek Pharmaceuticals, Inc.Inventors: Carmen García-Luzón, Juan Carlos Cuevas, Jose M. Fiandor, Araceli Mallo, Mark L. Nelson, Roger Frechette
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Publication number: 20090325908Abstract: The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.Type: ApplicationFiled: January 9, 2009Publication date: December 31, 2009Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Mohamed Y. Ismail, Todd Bowser, Jimmy Dumornay, Glen Rennie, Gui Liu, Darrell J. Koza, Paul Sheahan, Karen Stapleton, Paul Hawkins, Beena Bhatia, Atul K. Verma, Laura Honeyman, Tadeusz Warchol, David Messersmith
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Publication number: 20090275766Abstract: The invention relates to processes for the preparation of tigecycline (I): a wide spectrum antibiotic belonging to the tetracycline family, in stable amorphous form, by freeze-drying, antisolvent precipitation and nebulization.Type: ApplicationFiled: May 4, 2009Publication date: November 5, 2009Inventors: Giovanni POZZI, Marco Alpegiani, Angelo Bedeschi, Roberta Pizzocaro
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Patent number: 7553828Abstract: The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and minocycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.Type: GrantFiled: February 24, 2004Date of Patent: June 30, 2009Assignee: Paratek Pharmaceuticals, Inc.Inventors: Mark L. Nelson, Roger Frechette, Mohamed Y. Ismail, Laura Honeyman, Todd Bowser, Beena Bhatia
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Publication number: 20090156842Abstract: Methods of synthesizing substituted tetracycline compounds are provided.Type: ApplicationFiled: July 7, 2008Publication date: June 18, 2009Inventors: Farzaneh Seyedi, Tadeusz Warchol, Mark Grier
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Publication number: 20090124583Abstract: 7-substituted tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-substituted tetracycline compounds are described.Type: ApplicationFiled: May 30, 2008Publication date: May 14, 2009Applicant: Trustees of Tufts CollegeInventors: Mark L. Nelson, Darrell Koza
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Publication number: 20090099376Abstract: Methods of preparing and purifying 9-nitrominocycline and 9-aminominocycline and salts thereof used in the process of making tigecycline, are disclosed. In one embodiment, the invention is directed to a method of preparing the compound of formula 1 or a pharmaceutically acceptable salt thereof, comprising: (a) reacting nitric acid with the compound of formula 2, or a salt thereof, to produce a reaction mixture comprising an intermediate; and (b) further reacting the intermediate to form the compound of formula 1, wherein the intermediate is isolated from the reaction mixture, the method further comprising sparging with an inert gas prior to step (a).Type: ApplicationFiled: October 15, 2008Publication date: April 16, 2009Applicant: WyethInventors: Michel Bernatchez, Warren Chew, Sylvain Daigneault, Ernest Palus, Mahmoud Mirmehrabi, Luc Bouchard
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Publication number: 20080234504Abstract: The present invention provides substantially pure intermediates, 9-haloacetomidominocyclines, and process of preparing them that are useful for the preparation of glycylcyclines, specifically Tigecycline.Type: ApplicationFiled: November 30, 2007Publication date: September 25, 2008Inventors: Evgeny Tsiperman, Sofia Gorohovsky, Slavik Yurkovski, Sergei Fine, Tamas Koltai, Judith Aronhime
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Patent number: 7214669Abstract: A treatment for inhibiting microbial or tumor growth is disclosed, which comprises adding to a subject in need of treatment an effective amount of one or more tetracycline derivatives.Type: GrantFiled: October 4, 2002Date of Patent: May 8, 2007Assignee: Tetragenex Pharmaceuticals, Inc.Inventors: Joseph J. Hlavka, Richard J. Ablin
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Patent number: 7208482Abstract: A compound of formula (I):Type: GrantFiled: August 6, 2003Date of Patent: April 24, 2007Assignee: Paratek Pharmaceuticals, Inc.Inventors: Carmen García-Luzón, Juan Carlos Cuevas, Jose M. Fiandor, Araceli Mallo, Mark L. Nelson, Roger Frechette
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Patent number: 7067504Abstract: The present invention is a di-steroidal prodrug of ethinyl estradiol according to formula I:Type: GrantFiled: December 10, 2004Date of Patent: June 27, 2006Assignee: Warner Chilcott Company, Inc.Inventors: John Alexander King, James Keown, James William McIlroy, William Paul Armstrong, Michael Anthony McKervey, Austin McMordie
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Patent number: 7067505Abstract: The present invention is a di-steroidal prodrug of estradiol having the following formula:Type: GrantFiled: December 10, 2004Date of Patent: June 27, 2006Assignee: Warner Chilcott Company, Inc.Inventors: John Alexander King, James Keown, James William McIlroy, William Paul Armstrong, Michael Anthony McKervey, Austin McMordie
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Patent number: 7001918Abstract: A compound of Formula (I): wherein variables R, R1, R2, R3 and A are as defined in theType: GrantFiled: June 1, 2004Date of Patent: February 21, 2006Assignee: Paratek Pharmaceuticals, Inc.Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
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Patent number: 6846939Abstract: The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.Type: GrantFiled: June 29, 2001Date of Patent: January 25, 2005Assignees: Paratek Pharmaceuticals, Inc., Trustees of Tufts CollegeInventors: Mark L. Nelson, Roger Frechette, Peter Viski, Beena Bhatia
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Publication number: 20040224927Abstract: 7-substituted tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-substituted tetracycline compounds are described.Type: ApplicationFiled: April 7, 2004Publication date: November 11, 2004Applicant: Trustees of Tufts CollegeInventors: Mark L. Nelson, Darrell J. Koza
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Publication number: 20040192657Abstract: A compound of formula (I): 1Type: ApplicationFiled: August 6, 2003Publication date: September 30, 2004Inventors: Carmen Garcia-Luzon, Juan Carlos Cuevas, Jose M. Fiandor, Araceli Mallo, Mark L. Nelson, Roger Frechette
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Patent number: 6506740Abstract: The present invention provides new chemically modified 4-dedimethylaminotetracycline compounds that can be substituted at the 7, 8, and/or 9 positions and methods for preparing the 4-dedimethylamino tetracycline compounds. Other tetracycline compounds are the 4-dedimethylaminotetracycline derivatives with an oxime group, NH-Alkyl, or N—NH-Alkyl group at the C4 position. The present invention also provides a method of treating a mammal suffering from conditions or diseases by administering to the mammal an effective amount of the new chemically modified 4-dedimethylamino tetracycline compounds.Type: GrantFiled: May 18, 2000Date of Patent: January 14, 2003Inventors: Robert A. Ashley, Joseph J. Hlavka
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Publication number: 20020103171Abstract: Substituted tetracycline compounds, methods of synthesis, and methods of use are discussed. Tetracyclines useful for treating tetracycline related disorders are also discussed. Intermediates useful for synthesizing other tetracycline compounds are also included.Type: ApplicationFiled: March 30, 2001Publication date: August 1, 2002Inventors: Mark L. Nelson, Stuart B. Levy, Roger Frechette, Todd E. Bowser, Mohamed Y. Ismail
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Patent number: 6165999Abstract: The present invention relates to novel tetracycline derivatives, to intermediates used in their preparation, to pharmaceutical compositions containing them and to their medicinal use.Type: GrantFiled: February 23, 1998Date of Patent: December 26, 2000Assignee: Pfizer IncInventor: Chi Bao Vu
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Patent number: 6028207Abstract: A compound represented by the following formula (I):X--Y--Z (I)where Y is represented by the following formulae: ##STR1## X is a monovalent group of a tetracycline type compounds and Z is a monoent group of a steroid type compound such as estrogen.The compound can concentrate on the bone tissue and has bone resorption inhibition/ossification promotion functions.Type: GrantFiled: July 3, 1997Date of Patent: February 22, 2000Assignees: Iskra Industry Co., Ltd., Institute of Pharmacology, West China University of Medical SciencesInventors: Hu Zheng, Lingling Weng
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Patent number: 5834450Abstract: This invention relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are defined as in the specification and the pharmaceutically acceptable salts of such compounds. Compounds of the formula I exhibit antibiotic activity against a wide range of gram-positive and gram-negative organisms, including organisms that are resistant to tetracycline antibiotics.Type: GrantFiled: July 22, 1996Date of Patent: November 10, 1998Assignee: Pfizer Inc.Inventor: Wei-guo Su
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Patent number: 5675030Abstract: The invention provides a method for selectively extracting a compound of formula I: ##STR1## wherein: R is hydrogen or --NR.sub.3 R.sub.4 ; and when R=--NR.sub.3 R.sub.4, R.sub.3 and R.sub.4 may be the same or different and are selected from hydrogen and straight or branched (C.sub.1 -C.sub.4)alkyl; R.sub.1 and R.sub.2 may be the same or different and are selected from straight or branched (C.sub.1 -C.sub.6)alkyl; from an aqueous mixture containing a compound of Formula I, its C-4 epimer and its oxidative degradation by-products by adding methylene at a concentration of 2-4 ml of methylene chloride per gram of compound of Formula I and at a pH between pH 6.5-8.0; and obtaining an extract containing methylene chloride, a compound of Formula I, and its C-4 epimer, said epimer being present in an amount of less than 3% of the amount of the compound of Formula I.Type: GrantFiled: November 16, 1994Date of Patent: October 7, 1997Assignee: American Cyanamid CompanyInventors: Lalitha Krishnan, Richard A. Leese, Raghavan Krishnan
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Patent number: 5639742Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.1, R.sup.2 and W are defined in the specification. These compounds are useful as antibiotic agents.Type: GrantFiled: August 29, 1994Date of Patent: June 17, 1997Inventors: Ving Jick Lee, Brian Lee Buckwalter, Timothy Claude Barden
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Patent number: 5530117Abstract: The disclosure is drawn to novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds. These compounds are useful to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.Type: GrantFiled: May 31, 1995Date of Patent: June 25, 1996Assignee: American Cyanamid CompanyInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee, Adma A. Ross
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Patent number: 5494903Abstract: The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula ##STR1## wherein R, X, R.sup.5 and R.sup.6 are defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics.Type: GrantFiled: August 4, 1994Date of Patent: February 27, 1996Assignee: American Cyanamid CompanyInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee, Adma A. Ross
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Patent number: 5495018Abstract: The invention provides compounds of the formulas ##STR1## which are useful as intermediates for the preparation of 6-demethyl-6-deotetracycline antibiotic agents.Type: GrantFiled: December 8, 1994Date of Patent: February 27, 1996Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Joseph J. Hlavka, Raymond T. Testa
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Patent number: 5495030Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.1 and Y are defined in the specification. The compounds are useful for the production of 6-demethyl-6-deoxytracycline derivatives.Type: GrantFiled: September 1, 1994Date of Patent: February 27, 1996Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Raymond T. Testa
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Patent number: 5495032Abstract: The invention provides a process for the production of compounds of the formula: ##STR1## wherein, R, R.sup.3, R.sup.4, X and W are defined in the specification in which a compound of the following formula: ##STR2## is reacted with a nucleophile of the formula WH in an inert atmosphere in the presence of a polar-protic or a polar-aprotic solvent. The resulting compounds are useful as antibiotics.Type: GrantFiled: September 27, 1994Date of Patent: February 27, 1996Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Joseph J. Hlavka, Raymond T. Testa
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Patent number: 5488119Abstract: Compounds of formulae I and II ##STR1## wherein D is H or --OR wherein R is phenyl and R.sub.1 to R.sub.4 are H or a substituent such as phenylthio, and one of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is a group of formula III--E-CR.sub.5 =C(R.sub.6).sub.2 (III)or R is substituted by a group of formula III, wherein E is a direct bond or --X-C(O)-- wherein X is a linking group, and R.sub.5 and R.sub.6 are each independently of the other H, halogen, C.sub.1 -C.sub.12 alkyl or C.sub.6 -C.sub.10 aryl, can be polymerised to homopolymers or copolymers. The monomers and polymers are reversible photochromic systems which can be used as color indicators, as photochemically modifiable color filters, or for the optical storage of information.Type: GrantFiled: October 12, 1993Date of Patent: January 30, 1996Assignee: Ciba-Geigy CorporationInventors: Evelyn Fischer-Reimann, Walter Fischer
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Patent number: 5442059Abstract: The invention provides compounds of the formula: ##STR1## wherein R, and R.sup.1 and W are defined in the specification. These compounds are useful as antibiotic agents.Type: GrantFiled: August 13, 1992Date of Patent: August 15, 1995Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Raymond T. Testa
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Patent number: 5430162Abstract: The invention provides compounds of formula ##STR1## wherein X, R and R.sup.1 are defined in the specification. These compounds are useful as antibiotic agents.Type: GrantFiled: March 21, 1994Date of Patent: July 4, 1995Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Joseph J. Hlavka, Raymond T. Testa
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Patent number: 5401729Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.3, R.sup.4 and W are defined in the specification. These compounds are useful as antibiotic agents.Type: GrantFiled: February 24, 1994Date of Patent: March 28, 1995Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Raymond T. Testa
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Patent number: 5386041Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.3, R.sup.4, X and W are defined in the specification. These compounds are useful as antibiotic agents.Type: GrantFiled: February 8, 1994Date of Patent: January 31, 1995Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Joseph J. Hlavka, Raymond T. Testa
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Patent number: 5380888Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.3, R.sup.4 and W are defined in the specification. These compounds are useful as antibiotic agents.Type: GrantFiled: March 2, 1994Date of Patent: January 10, 1995Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Raymond T. Testa
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Patent number: 5371076Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.1, R.sup.2 and W are defined in the specification. These compounds are useful as antibiotic agents.Type: GrantFiled: April 2, 1993Date of Patent: December 6, 1994Assignee: American Cyanamid CompanyInventors: Ving J. Lee, Brian L. Buckwalter, Timothy C. Barden
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Method of producing 7-(substituted)-9-[(substituted glycyl)-amidol]-6-demethyl-6-deoxytetra-cyclines
Patent number: 5284963Abstract: The invention provides a novel method for producing compounds of the formula I: ##STR1## wherein X and R are defined in the specifications. The invention also provides a method for making intermediates useful to produce the compounds of formula I. Utilizing a common intermediate, the novel method efficiently produces compounds of the formula I.Type: GrantFiled: August 13, 1992Date of Patent: February 8, 1994Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee -
Patent number: 5281628Abstract: 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.Type: GrantFiled: October 4, 1991Date of Patent: January 25, 1994Assignee: American Cyanamid CompanyInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
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Patent number: 5248797Abstract: The invention relates to a novel method for producing [4S-(4alpha, 12aalpha)]-9-amino-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3, 10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide, hereinafter called 9-amino-6-demethyl-6-deoxytetracycline, which compound is a valuable intermediate for synthesis of tetracyclines.Type: GrantFiled: August 13, 1992Date of Patent: September 28, 1993Assignee: American Cyanamid CompanyInventor: Phaik-Eng Sum
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Patent number: 4918208Abstract: A process for producing 7-dimethylamino-6-demethyl-6-deoxytetracycline (minocycline) which comprises treating the reaction liquid containing minocycline and formaldehyde with hydroxylamine or urea, the reaction liquid being obtained after reductive methylation of 7-amino-6-demethyl-6-deoxytetracycline by using aldehyde, then subjecting the reaction liquid to an adsorption treatment with a nonionic adsorption resin (adsorbent), and subsequently eluting the intended product adsorbed to the adsorbent.Type: GrantFiled: July 22, 1988Date of Patent: April 17, 1990Assignee: Nippon Kayaku Kabushiki KaishaInventors: Ryoichi Hasegawa, Hiroaki Ohno, Kazuaki Sano, Yoshinori Saito
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Patent number: RE40183Abstract: The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula wherein R, X, R5 and R6 are defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics.Type: GrantFiled: June 3, 2005Date of Patent: March 25, 2008Assignee: Wyeth Holdings CorporationInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee, Adma A. Ross