Tetracyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos (e.g., Rifamycin S, Etc.) Patents (Class 540/458)
  • Patent number: 10815309
    Abstract: This invention describes a method of conjugating a cell binding agent such as an antibody with an effector group (e.g., a cytotoxic agent) or a reporter group (e.g., a radionuclide), whereby the reporter or effector group is first reacted with a bifunctional linker and the mixture is then used without purification for the conjugation reaction with the cell binding agent. The method described in this invention is advantageous for preparation of stably-linked conjugates of cell binding agents, such as antibodies with effector or reporter groups. This conjugation method provides in high yields conjugates of high purity and homogeneity that are without inter-chain cross-linking and inactivated linker residues.
    Type: Grant
    Filed: February 1, 2019
    Date of Patent: October 27, 2020
    Assignee: IMMUNOGEN, INC.
    Inventors: Brenda A. Kellogg, Rajeeva Singh, Ravi V. Chari
  • Patent number: 9120818
    Abstract: The present invention relates to macrolactam compounds, intermediates useful in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing and modifying macrolactams. One use of the compounds and methods described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. An example of an HCV inhibitory compound that can be synthesized using the procedures described herein is Compound A and derivative thereof.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: September 1, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Cheng Chen, Jongrock Kong, Guy Humphrey, Sarah Dolman, Hongmei Li, Matthew T. Tudge, Kelvin Yong, Bangping Xiang, Michael Zacuto
  • Publication number: 20150118307
    Abstract: Embodiments relate to Rifaximin polymorphic, salt, and hydrate forms, methods of producing polymorphic forms and to their use in medicinal preparations and to therapeutic methods using them.
    Type: Application
    Filed: May 27, 2014
    Publication date: April 30, 2015
    Applicant: SALIX PHARMACEUTICALS, LTD
    Inventors: Stephan D. Parent, Lisa Lynn McQueen, Patricia Andres, Paul Schields, Yiduo Wu, Fei Ding, Jared Peters Smit
  • Patent number: 9012441
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Grant
    Filed: January 9, 2014
    Date of Patent: April 21, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-Hung Chou, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
  • Publication number: 20140356376
    Abstract: The invention provides anti-wall teichoic acid antibodies and antibiotic conjugates thereof, and methods of using the same.
    Type: Application
    Filed: May 30, 2014
    Publication date: December 4, 2014
    Applicant: GENENTECH, INC.
    Inventors: Eric J. Brown, Martine Darwish, John Flygare, Wouter Hazenbos, Byoung Chul Lee, Sophie M. Lehar, Sanjeev Mariathasan, John Hiroshi Morisaki, Thomas H. Pillow, Leanna Staben, Richard Vandlen, Klaus Koefoed, Magnus Strandh, Peter S. Andersen
  • Publication number: 20140356375
    Abstract: The invention provides anti-wall teichoic acid antibodies and antibiotic conjugates thereof, and methods of using the same.
    Type: Application
    Filed: May 22, 2014
    Publication date: December 4, 2014
    Applicant: GENENTECH, INC.
    Inventors: Eric J. Brown, Martine Darwish, John Flygare, Wouter Hazenbos, Byoung Chul Lee, Sophie M. Lehar, Sanjeev Mariathasan, John Hiroshi Morisaki, Thomas H. Pillow, Leanna Staben, Richard Vandlen, Klaus Koefoed, Magnus Strandh, Peter S. Andersen
  • Patent number: 8871753
    Abstract: The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are JAK/ALK inhibitors useful in the treatment of JAK/ALK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
    Type: Grant
    Filed: April 23, 2009
    Date of Patent: October 28, 2014
    Assignee: Incyte Corporation
    Inventors: Andrew Paul Combs, Richard B. Sparks, Eddy W. Yue, Hao Feng, Michael Jason Bower, Wenyu Zhu
  • Patent number: 8846734
    Abstract: Diazonamide analogs having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders, and related pharmaceutical compositions are provided.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: September 30, 2014
    Assignee: Joyant Pharmaceuticals, Inc.
    Inventors: Qi Wei, Ming Zhou, Xiaoming Xu, Charles Caldwell, Susan Harran, Lai Wang
  • Patent number: 8592469
    Abstract: Diazonamide analogs having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders, and related pharmaceutical compositions are provided.
    Type: Grant
    Filed: April 15, 2012
    Date of Patent: November 26, 2013
    Assignee: Joyant Pharmaceuticals, Inc.
    Inventors: Qi Wei, Ming Zhou, Xiaoming Xu, Charles Caldwell, Susan Harran, Lai Wang
  • Patent number: 8524691
    Abstract: The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
    Type: Grant
    Filed: August 10, 2009
    Date of Patent: September 3, 2013
    Assignee: The Medicines Company
    Inventors: Evelyne Dietrich, Ranga Reddy, Kelly Tanaka, Ting Kang, Yanick LaFontaine, Adel Rafai Far
  • Patent number: 8404664
    Abstract: The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
    Type: Grant
    Filed: August 11, 2006
    Date of Patent: March 26, 2013
    Assignee: Targanta Therapeutics, Inc.
    Inventors: Yannick Stephane Rose, Stephane Ciblat, Ting Kang, Adel Rafai Far, Evelyne Dietrich, Yanick Lafontaine, Ranga Reddy
  • Patent number: 8357687
    Abstract: Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein Y, R1, R2, R4 and n have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: January 22, 2013
    Assignee: Tibotec Pharmaceuticals
    Inventors: David Craig Mc Gowan, Sandrine Marie Helene Vendeville, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri
  • Patent number: 8338422
    Abstract: The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to certain indolin-2-ones and aza-indolin-2-ones which possess anti-tumor activity and are accordingly useful in methods of treatment of the human or animal body, in particular such compounds are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: December 25, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gaston Stanislas Marcella Diels, Marc Gustaaf Celine Verdonck, Peter Jacobus Johannes Antonius Buijnsters, Kristof Van Emelen
  • Patent number: 8334311
    Abstract: Indoline compounds having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders are provided.
    Type: Grant
    Filed: July 25, 2011
    Date of Patent: December 18, 2012
    Assignee: Joyant Pharmaceuticals, Inc.
    Inventors: Gunnar James Hanson, Qi Wei, Charles Caldwell, Ming Zhou, Lai Wang, Susan Harran
  • Publication number: 20120316228
    Abstract: The present invention relates to oral pharmaceutical compositions with controlled and/or programmed release containing at least one active ingredient having antimicrobial and/or anti-infectious activity for the treatment of infections of the large intestine, in particular the colon.
    Type: Application
    Filed: August 22, 2012
    Publication date: December 13, 2012
    Applicant: COSMO TECHNOLOGIES LIMITED
    Inventors: Mauro AJANI, Roberta BOZZELLA, Giuseppe CELASCO, Roberto VILLA
  • Patent number: 8318731
    Abstract: The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are polo-like kinase (PLKs) inhibitors useful for the treatment of disease states mediated by PLK, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: November 27, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gaston Stanislas Marcella Diels, Peter Ten Holte, Eddy Jean Edgard Freyne, Thierry Andre Regis Grand-Perret, Kristof Van Emelen, Werner Constant Johan Embrechts, Pascal Ghislain André Bonnet
  • Patent number: 8211891
    Abstract: The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: July 3, 2012
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yonghua Gai, Dong Liu, Joel D. Moore, Yat Sun Or, Zhe Wang
  • Publication number: 20110312903
    Abstract: Methods for fluorinating organic compounds are described herein.
    Type: Application
    Filed: November 20, 2009
    Publication date: December 22, 2011
    Inventors: Tobias Ritter, Takeru Furuya, PingPing Tang
  • Publication number: 20110263534
    Abstract: The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
    Type: Application
    Filed: August 11, 2006
    Publication date: October 27, 2011
    Inventors: Yannick Stephane Rose, Stephane Ciblat, Ting Kang, Adel Rafai Far, Evelyne Dietrich, Yanick Lafontaine, Ranga Reddy
  • Patent number: 7989482
    Abstract: Indoline compounds having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders are provided.
    Type: Grant
    Filed: April 29, 2009
    Date of Patent: August 2, 2011
    Assignee: Joyant Pharmaceuticals, Inc.
    Inventors: Gunnar James Hanson, Qi Wei, Charles Caldwell, Ming Zhou, Lai Wang, Susan Harran
  • Patent number: 7799793
    Abstract: Compounds of the formula: where X and Y are each independently H, halo, or C1-C6 straight or branched chain substituted or unsubstituted alkyl.
    Type: Grant
    Filed: April 25, 2008
    Date of Patent: September 21, 2010
    Assignee: Medtronic, Inc.
    Inventor: William V. Ferris, Jr.
  • Patent number: 7781422
    Abstract: Compounds of the formula (I): wherein A, B, D, M, Ar, W, X, Y, Z and R1 are as defined herein, are useful in the prevention and treatment of hepatitis C infections. The compounds, their preparation, pharmaceutical compositions containing them and their use in medicine are disclosed.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: August 24, 2010
    Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpA
    Inventors: Ian Stansfield, Uwe Koch, Joerg Habermann, Frank Narjes
  • Publication number: 20100168129
    Abstract: New compounds belonging to the structural formula (I) are described. in which R1, R2, A, Y and X are specified in the description, useful in the treatment of cholestasis and substantially devoid of antibacterial activity. The synthesis process of said compounds, the pharmaceutical compositions containing them and their use in therapy are also described.
    Type: Application
    Filed: July 17, 2008
    Publication date: July 1, 2010
    Inventors: Mario Brufani, Luciano Cellai, Barbara Bartolini, Ilaria Medici, Bianca Maria Lagrasta
  • Patent number: 7678791
    Abstract: Substituted rifamycin derivatives in which a nitroimidazole, nitrothiazole or nitrofuran pharmacophore is covalently bonded to a rifamycin, methods of using the rifamycin derivatives, and pharmaceutical compositions containing the rifamycin derivatives are disclosed. Methods of synthesizing these substituted rifamycin derivatives are also disclosed. The rifamycin derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: March 16, 2010
    Assignee: Cumbre IP Ventures, L.P.
    Inventors: Charles Z. Ding, In Ho Kim, Jiancheng Wang, Zhenkun Ma, Yafei Jin, Keith D. Combrink, Genliang Lu, A. Simon Lynch
  • Publication number: 20100029669
    Abstract: The present invention is directed to novel 3-(substituted ethyl) rifamycin derivatives, pharmaceutical compositions containing them and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes.
    Type: Application
    Filed: July 14, 2009
    Publication date: February 4, 2010
    Inventors: Mark J. MACIELAG, Manomi A. Tennakoon
  • Patent number: 7547692
    Abstract: The present invention features rifamycin analogs and methods of using these compounds to treat a variety of microbial infections.
    Type: Grant
    Filed: December 14, 2006
    Date of Patent: June 16, 2009
    Assignee: ActivBiotics Pharma, LLC
    Inventors: John H. van Duzer, Arthur F. Michaelis, William B. Geiss, Douglas G. Stafford, Joseph Raker, Xiang Y. Yu, James M. Siedlecki, Yingfei Yang
  • Patent number: 7488726
    Abstract: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3?-hydroxy analogs, 5?-halo and/or alkoxy analogs, and various 4?- and/or 6?-substituents that incorporate a cyclic amine moiety.
    Type: Grant
    Filed: November 2, 2006
    Date of Patent: February 10, 2009
    Assignee: ActivBiotics Pharma, LLC
    Inventors: John H. Van Duzer, James M. Siedlecki, Xiang Y. Yu
  • Patent number: 7473366
    Abstract: The invention relates to a process for the recovery of a macrolide in substantial pure form including: a) treating an impure or crude macrolide with water immiscible solvent to form a mixture, b) optionally concentrating the mixture, c) treating with ammonia gas to phase out impurities, d) separating impurities, e) optionally concentrating a phase containing the macrolide, f) loading on silica gel chromatography, optionally reversed phase or pretreated with silver, and eluting the macrolide, g) affording the macrolide in the substantially pure form, h) optional repetition of steps f and g to afford the macrolide in the substantially pure form. The macrolide is preferably tacrolimus, immunomycin or sirolimus.
    Type: Grant
    Filed: December 5, 2003
    Date of Patent: January 6, 2009
    Assignee: BioCon Limited
    Inventors: Nitin Sopanrao Patil, Rakesh Mendhe, Anand Prakash Khedkar, Ramakrishnan Melarkode, Ramavana Gururaja
  • Publication number: 20080268010
    Abstract: Compounds of the formula: where X and Y are each independently H, halo, or C1-C6 straight or branched chain substituted or unsubstituted alkyl.
    Type: Application
    Filed: April 25, 2008
    Publication date: October 30, 2008
    Applicant: MEDTRONIC, INC.
    Inventor: William V. Ferris
  • Publication number: 20080139577
    Abstract: Substituted rifamycin derivatives in which a nitroimidazole, nitrothiazole or nitrofuran pharmacophore is covalently bonded to a rifamycin, methods of using the rifamycin derivatives, and pharmaceutical compositions containing the rifamycin derivatives are disclosed. Methods of synthesizing these substituted rifamycin derivatives are also disclosed. The rifamycin derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.
    Type: Application
    Filed: July 12, 2007
    Publication date: June 12, 2008
    Applicant: Cumbre Pharmaceuticals Inc.
    Inventors: Charles Z. Ding, In Ho Kim, Jiancheng Wang, Zhenkun Ma, Yafei Jin, Keith D. Combrink, Genliang Lu, A. Simon Lynch
  • Patent number: 7368565
    Abstract: The present invention discloses a one-step process for the production of cytotoxic conjugates of maytansinoids and cell binding agents. Maytansinoids having a disulfide linker that bears a reactive moiety are linked to cell binding agents, such as antibodies, without prior modification of the cell binding agent. These conjugates are useful as therapeutic agents which are delivered specifically to target cells and are cytotoxic.
    Type: Grant
    Filed: June 5, 2002
    Date of Patent: May 6, 2008
    Assignee: Immunogen Inc.
    Inventors: Ravi V. J. Chari, Wayne C. Widdison
  • Patent number: 7342011
    Abstract: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3?-hydroxy analogs, 4?- and/or 6? halo and/or alkoxy analogs, and various 5? substituents that incorporate a cyclic amine moiety.
    Type: Grant
    Filed: August 11, 2004
    Date of Patent: March 11, 2008
    Assignee: ActivBiotics, Inc.
    Inventors: John H. van Duzer, Arthur F. Michaelis, William B. Geiss, Douglas G. Stafford, Joseph Raker
  • Patent number: 7300924
    Abstract: The invention is related to phosphorus substituted anti-infective compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: April 26, 2004
    Date of Patent: November 27, 2007
    Assignee: Gilead Sciences, Inc.
    Inventors: Constantine G. Boojamra, Aesop Cho, William J. Watkins
  • Patent number: 7271165
    Abstract: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3?-hydroxy analogs, 4?- and/or 6? halo and/or alkoxy analogs, and various 5? substituents that incorporate a cyclic amine moiety.
    Type: Grant
    Filed: December 22, 2004
    Date of Patent: September 18, 2007
    Assignee: ActivBiotics, Inc.
    Inventors: John H. van Duzer, Arthur F. Michaelis, William B. Geiss, Douglas G. Stafford, Joseph Raker, Xiang Y. Yu, James M. Siedlecki, Yingfei Yang
  • Patent number: 7226931
    Abstract: Rifamycin derivatives having the following structure of general formula I (both hydroquinone and corresponding quinone (C1-C4) forms): or its salts, hydrates or prodrugs thereof; wherein a preferred R1 comprises hydrogen or acetyl and a prefered R2 comprises hydrogen, methyl or other lower alkyls; wherein asterik (*) denotes the carbon bearing the chiral center, wherein absolute configuration is assigned as R or S. Methods of preparation of the aforementioned rifamycin derivatives are also described. The compounds exhibit antimicrobial activities, including activities against drug-resistant microorganisms.
    Type: Grant
    Filed: July 21, 2005
    Date of Patent: June 5, 2007
    Assignee: Cumbre Pharmaceuticals Inc.
    Inventors: Charles Z. Ding, Zhenkun Ma, Jing Li, Susan Harran, Yong He, Keith P. Minor, In Ho Kim, Jamie C. Longgood, Yafei Jin, Keith D. Combrink
  • Patent number: 7220738
    Abstract: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3?-hydroxy analogs, and/or various fused ring systems with the benzene ring at the 4?,5? or 5?,6? positions.
    Type: Grant
    Filed: December 9, 2004
    Date of Patent: May 22, 2007
    Assignee: ActivBiotics, Inc.
    Inventors: John H. van Duzer, Arthur F. Michaelis, William B. Geiss, Douglas G. Stafford, Xiang Y. Yu, James M. Siedlecki, Yingfei Yang
  • Patent number: 7220357
    Abstract: Provided is a method of purifying a macrolide, especially tacrolimus, that includes loading macrolide onto a bed of sorption resin and elting with a suitable eluent such as a combination of water and tetrahydrofuran.
    Type: Grant
    Filed: July 26, 2004
    Date of Patent: May 22, 2007
    Assignee: Teva Gyógyszergyár Zártkörúen Múkó´dó´Résvénytársaság
    Inventors: Vilmos Keri, Zoltan Czövek, Andrea Csorvasi, Ferenc Rantal
  • Patent number: 7122525
    Abstract: The invention features a method of delivering a drug to a diseased cell by linking the drug to a rifamycin derivative, compositions that include drug-rifamycin conjugates of the invention, and methods for treating disease using those compositions.
    Type: Grant
    Filed: November 21, 2002
    Date of Patent: October 17, 2006
    Assignee: ActivBiotics, Inc.
    Inventors: Arthur F. Michaelis, Hawkins V. Maulding, Chalom Sayada, Congxiang Zha
  • Publication number: 20030195181
    Abstract: Laulimalide compounds, intermediates thereto and methods for their preparation, and methods for their use in the treatment of diseases characterized by cellular hyperproliferation.
    Type: Application
    Filed: February 10, 2003
    Publication date: October 16, 2003
    Inventors: Gary Ashley, Brian Metcalf
  • Publication number: 20030166924
    Abstract: Provided is a method for obtaining a macrolide, especially tacrolimus, from biomatter.
    Type: Application
    Filed: February 12, 2003
    Publication date: September 4, 2003
    Inventors: Vilmos Keri, Lajos Deak, Csaba Szabo
  • Patent number: 6476036
    Abstract: Sodium salt of 3-(4-cinnamyl-1-piperazinyl)-iminomethyl rifamycin SV was synthesized. The compound shows high activity against Gram-positive and Gram-negative microorganims, Mycobacterium tuberculosis (including atypical and rifampicin resistant) and may be used in the medical practice. The sodium salt has formula (II). The process for preparation of the sodium salt consists of reacting equimolar quantities of 3-(4-cinnamyl-1-piperazinyl)-iminomethyl rifamycin SV and sodium ascorbate with addition of 30% methanol solution of sodium methylate, followed by filtration and removement of the solvent by distillation under reduced pressure. The compound can also be obtained from the sodium salt of 3-formil rifamycin SV, which is reacting with N1-amino-N4-cinnamypiperazin in medium of inert solvent at room temperature.
    Type: Grant
    Filed: July 20, 2001
    Date of Patent: November 5, 2002
    Inventors: Roumiana Gueorguieva Konstantinova, Kiril Asenov Ninov, Velitchka Ilieva Dimova, Anka Veltcheva Evstatieva
  • Patent number: 6441163
    Abstract: The present invention discloses a one-step process for the production of cytotoxic conjugates of maytansinoids and cell binding agents. Maytansinoids having a disulfide linker that bears a reactive moiety are linked to cell binding agents, such as antibodies, without prior modification of the cell binding agent. These conjugates are useful as therapeutic agents which are delivered specifically to target cells and are cytotoxic.
    Type: Grant
    Filed: May 31, 2001
    Date of Patent: August 27, 2002
    Assignee: Immunogen, Inc.
    Inventors: Ravi V. J. Chari, Wayne C. Widdison
  • Patent number: 6413964
    Abstract: The present invention is directed to peptidomimetic macrocyclic compounds of the formula A: wherein W is a heterocycle, V is a heterocycle or aryl moiety and Z1 is a suitably substituted aryl or heterocycle moiety. The instant compounds inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: July 2, 2002
    Inventors: S. Jane deSolms, Suzanne C. MacTough, Anthony W. Shaw
  • Patent number: 6410534
    Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: June 25, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Ian M. Bell, Douglas C. Beshore, Theresa M. Williams
  • Patent number: 5952320
    Abstract: Macrocyclic compounds of formula ##STR1## are potent inhibitors of matrix metalloproteinase and are useful in the treatment of diseases in which matrix metalloproteinase play a role. Also disclosed are matrix metalloproteinase inhibiting compositions and a method of inhibiting matrix metalloproteinase in a mammal.
    Type: Grant
    Filed: December 17, 1997
    Date of Patent: September 14, 1999
    Assignee: Abbott Laboratories
    Inventors: Steven K. Davidsen, Douglas H. Steinman, George S. Sheppard, Lianhong Xu, James H. Holms, Yan Guo, James B. Summers, Alan S. Florjancic, Michael R. Michaelides
  • Patent number: 5786350
    Abstract: Rifamycin antibiotic derivatives of formulae (I) and (Ia) bearing at the position 36 a substituent selected from (C.sub.1 -C.sub.8)alkyl, halo, hydroxy, (C.sub.1 -C.sub.4)acyloxy, (C.sub.1-C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkylamino, di(C.sub.1-C.sub.4)alkylamino and substituted 4-oxo-3-pyridinyl carbonyloxy of formula (1) obtained by reacting rifamycin with suitably substituted malonic acid. The compounds of the invention are antimicrobial agents mainly active against gram positive bacteria and fastidious gram negative bacteria showing the considerable antimicrobial activity against the rifamypicin resistant microbial strains.
    Type: Grant
    Filed: January 31, 1997
    Date of Patent: July 28, 1998
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Emilio Occelli, Sergio Lociuro, Romeo Ciabatti, Maurizio Denaro
  • Patent number: 5654421
    Abstract: Automatic dishwashing detergent compositions, comprising particular quaternary-substituted bleach activators, are provided. More specifically, the invention relates to granular automatic dishwashing detergents which provide enhanced cleaning/bleaching benefits through the selection of quaternary-substituted bleach activators having specific features, such as caprolactam or valerolactam leaving groups and/or the ability to form particular cationic aliphatic peracid structures in solution. Preferred automatic dishwashing compositions comprise amylase enzymes. Included are preferred activator compounds and methods for washing tableware in domestic automatic dishwashing appliances using the activators.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 5, 1997
    Assignee: The Procter & Gamble Company
    Inventors: Lucille Florence Taylor, Mark Robert Sivik, Alan David Willey, James Charles Theophile Burckett-St. Laurent, Frederick Anthony Hartman
  • Patent number: 5378837
    Abstract: The present invention relates to a new one-pot process for preparing 2'-(diethylamino)rifamycin P and its 25-desacetyl derivative which consists in cyclizing 3-bromorifamycin S or its 25-desacetyl derivative, dissolved in dimethylformamide, with 1,1-diethylthiourea and reducing, without isolation, the obtained 1,2-quinonimine intermediate with a mild reducing agent.
    Type: Grant
    Filed: October 8, 1993
    Date of Patent: January 3, 1995
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Gianbattista Panzone, Anacleto Gianantonio
  • Patent number: 5306715
    Abstract: A solid rifapentine hydrohalide useful for anti-bacterial purposes.
    Type: Grant
    Filed: January 8, 1991
    Date of Patent: April 26, 1994
    Assignee: Gruppo Lepetit SpA
    Inventors: Emilio Occelli, Marino Nebuloni, Bruno Cavalleri
  • Patent number: RE39151
    Abstract: The present invention provides a process for the preparation and purification of thiol-containing maytansinoids comprising the steps of: (1) reductive hydrolysis of a maytansinoid C-3 ester with a reducing agent selected from the group consisting lithium trimethoxyaluminum hydride (LiAl (OMe)3H), lithium triethoxyaluminum hydride (LiAl(OEt)3H), lithium tripropoxyaluminum hydride (LiAl (OPr)3H), sodium trimethoxyaluminum hydride (NaAl (OMe)3H), sodium triethoxyaluminum hydride (NaAl(OEt)3H) and sodium tripropoxyaluminum hydride (NaAl(OPr)3H) to yield a maytansinol; (2) purifying the maytansinol to remove side products when present; (3) esterifying the purified maytansinol with a carboxylic acid to yield a mixture of an L- and a D-aminoacyl ester of maytansinol; (4) separating the L-aminoacyl ester of maytansinol from the reaction mixture in (3); (5) reducing the L-aminoacyl ester of maytansinol to yield a thiol-containing maytansinoid; and (5) purifying the thiol-containing maytansinoid.
    Type: Grant
    Filed: April 10, 2003
    Date of Patent: June 27, 2006
    Assignee: Immunogen, Inc.
    Inventors: Ravi Vankeepuram Jagannatha Chari, Wayne Charles Widdison