Having Chalcogen, Carbonyl, Or Thiocarbonyl Bonded Directly To The 4-position Substituent Nitrogen Patents (Class 536/28.51)
  • Patent number: 8975393
    Abstract: This invention relates to a process of synthesizing a ?-nucleoside compound of formula (I): wherein R1 is alkyl, aryl, cycloalkyl, heteroaryl, or heterocycloalkyl. The process includes reacting a compound of formula (II): with a compound of formula (III): wherein R1 is as defined above and X is chloride, bromide, iodide, methanesulfonate, triflate, p-toluenesulfonate, trifluoroacetate, 4-nitrophenoxy, or N-succinimidyloxy, in a solvent and in the presence of a base.
    Type: Grant
    Filed: January 8, 2013
    Date of Patent: March 10, 2015
    Assignee: PharmaEssentia Corp.
    Inventors: Ko-Chung Lin, Chungsun Chien
  • Patent number: 8956613
    Abstract: The present invention provides compounds according to formula I: and pharmaceutically acceptable salts thereof. For compounds of formula I, R1 and R2 are independently selected from the group consisting of H, —C(?O)—(CH2)2-aryl, and —C(?O)—(CH2)n—C(?O)—NH-aryl. The subscript n is from 2 to 6. R3 is selected from the group consisting of H and —C(?O)—O—R4; and R4 is selected from the group consisting of alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, arylalkyl, substituted arylalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, heteroalkyl and substituted heteroalkyl. Compounds are provided wherein at least one of R1 and R2 is other than H. Pharmaceutical compositions, methods for inhibiting the growth of cancer cells, and methods for the treatment of cancer are also provided.
    Type: Grant
    Filed: November 12, 2013
    Date of Patent: February 17, 2015
    Assignee: BoYen Therapeutics, Inc.
    Inventor: Laurence I. Wu
  • Publication number: 20150005251
    Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection, with a nucleoside, a nucleotide and an analog thereof.
    Type: Application
    Filed: June 24, 2014
    Publication date: January 1, 2015
    Inventors: Natalia Dyatkina, Guangyi Wang, Leonid Beigelman, Vivek Kumar Rajwanshi
  • Publication number: 20140378673
    Abstract: Provided is a prodrug of 2-nitro-1-imidazolepropionic acid and a therapeutically active organic compound having on the molecule an amino group, a cyclic amino group or a hydroxyl group, particularly a prodrug in which the therapeutically active organic compound is selected from among antitumor agents. The prodrug cleaves specifically under hypoxic conditions in vivo to exhibit the inherent therapeutic activity.
    Type: Application
    Filed: February 13, 2013
    Publication date: December 25, 2014
    Inventors: Yukio Nagasaki, Yutaka Ikeda, Hikaru Hisano
  • Patent number: 8884001
    Abstract: The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2; (ii) converting said compound of formula 682-2? into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2?-cyano-2?-deoxy-N4-palmitoyl-1-?-D-arabmofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.
    Type: Grant
    Filed: May 8, 2009
    Date of Patent: November 11, 2014
    Assignee: Cyclacel Limited
    Inventors: Gavin Wood, Robert Westwood, Tsuyoshi Murofushi, Eiji Numagami, Takashi Takita
  • Publication number: 20140235568
    Abstract: The present invention relates to the field of medical technology, and in particular relates to a kind of gemcitabine amide derivative with a novel structure. The new compounds of the present invention are very active with regard to many tumour cells such as human lung cancer, colon cancer, breast cancer and liver cancer etc., and therefore can be used for preparing anti-tumour drugs. In addition, these compounds also have anti-viral activity. Also disclosed are a preparation method for the compounds, a pharmaceutical composition containing the compounds and the use thereof in preparing drugs against tumours and viruses etc.
    Type: Application
    Filed: September 26, 2012
    Publication date: August 21, 2014
    Inventors: Yunlong Song, Zhiyu Shao
  • Publication number: 20140235566
    Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV, HCV, Norovirus, Saporovirus, cytomegalovirus (CMV), herpes viruses (HSV-1, HSV-2), Dengue virus, Yellow fever, or HBV in human patients or other animal hosts. The compounds are certain N4-hydroxycytidine nucleosides derivatives, modified monophosphate and phosphonates prodrugs analogs, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1, HIV-2, HCV, Norovirus, Saporovirus, cytomegalovirus (CMV), herpes viruses (HSV-1, HSV-2), Dengue virus, Yellow fever, and HBV.
    Type: Application
    Filed: October 29, 2013
    Publication date: August 21, 2014
    Applicants: Emory University, RFS Pharma, LLC
    Inventors: Franck Amblard, Steven J. Coats, Raymond F. Schinazi
  • Publication number: 20140221304
    Abstract: The present invention relates to 5?-Substituted Nucleoside Analogs of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, Z, R1, R2, R3 and R3? are as defined herein. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Analog, and methods of using the 5?-Substituted Nucleoside Analogs for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: July 10, 2012
    Publication date: August 7, 2014
    Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Kevin X. Chen
  • Publication number: 20140134160
    Abstract: The present invention provides compounds according to formula I: and pharmaceutically acceptable salts thereof. For compounds of formula I, R1 and R2 are independently selected from the group consisting of H, —C(?O)—(CH2)2-aryl, and —C(?O)—(CH2)n—C(?O)—NH-aryl. The subscript n is from 2 to 6. R3 is selected from the group consisting of H and —C(?O)—O—R4; and R4 is selected from the group consisting of alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, arylalkyl, substituted arylalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, heteroalkyl and substituted heteroalkyl. Compounds are provided wherein at least one of R1 and R2 is other than H. Pharmaceutical compositions, methods for inhibiting the growth of cancer cells, and methods for the treatment of cancer are also provided.
    Type: Application
    Filed: November 12, 2013
    Publication date: May 15, 2014
    Applicant: BoYen Therapeutics, Inc.
    Inventor: Laurence I. Wu
  • Publication number: 20140128339
    Abstract: The present invention relates to 2?-Methyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3, are as defined herein. The present invention also relates to compositions comprising at least one 2?-Methyl Substituted Nucleoside Derivative, and methods of using the 2?-Methyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: October 15, 2013
    Publication date: May 8, 2014
    Inventors: Vinay Girijavallabhan, Stephane Bogen, Quang T. Truong, Ping Chen, Angela Kerekes, Frank Bennett, Sara Esposite, Qingmei Hong, Ian Davies
  • Publication number: 20140094426
    Abstract: Amphiphilic prodrugs of general formula A-X are disclosed, wherein A is a biologically active agent or may be metabolized to a biologically active agent; and X is R, or up to three R moieties attached to a linker, Y1, Y2 or Y3. Self-assembly of the amphiphilic prodrugs into reverse lyotropic phases, particularly hexagonal, cubic and sponge, is disclosed.
    Type: Application
    Filed: November 8, 2013
    Publication date: April 3, 2014
    Inventors: Calum John Drummond, Sharon Marie Sagnella, Minoo Jalili Moghaddam, Xiaojuan Gong
  • Patent number: 8653048
    Abstract: Prodrugs based on gemcitabine structure shown in formula (I) as well as their synthetic method and application are disclosed in the present invention, wherein the definitions for the groups of a, b, c, d, E, Z and V are described in the specification. By modifying the N4 group, the solubility, the bioavailability and the organ specificity of the prodrugs are improved. Therefore, the fast metabolism problem is overcome for the produced prodrugs compounds. Intestinal toxicity induced by gemcitabine is decreased. Thereby, the prodrugs can be delivered by oral administration in clinics and further improve their anti-tumor, anti-cancer, anti-infection and diffusion preventing capability, and can also specifically act on liver or colon. The synthetic method is simple and adapted to industrial production.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: February 18, 2014
    Assignee: Sanlugen Pharmatech Ltd.
    Inventors: Xiaoxia Xue, Gang Li, Changjun Sun, Wenbao Li
  • Publication number: 20140046021
    Abstract: The molecular structures of metal-salen complexes which exerts pharmacological effects are clarified and the metal-salen complexes having such molecular structures and their derivatives are provided. A metal-salen complex compound is characterized in that a metal atom part in each of multiple molecules of the metal-salen complex or its derivative is multimerized via water.
    Type: Application
    Filed: January 19, 2012
    Publication date: February 13, 2014
    Applicants: IHI CORPORATION
    Inventors: Yoshihiro Ishikawa, Haruki Eguchi
  • Patent number: 8609864
    Abstract: The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.
    Type: Grant
    Filed: January 7, 2010
    Date of Patent: December 17, 2013
    Assignee: Purdue Pharmaceutical Products, L.P.
    Inventors: Yu Chen, Yi Chen
  • Patent number: 8603999
    Abstract: Amphiphilic prodrugs of general formula A-X are disclosed, wherein A is a biologically active agent or may be metabolised to a biologically active agent; and X is selected from the group consisting of R, or up to three R moieties attached to a linker, Y1, Y2 or Y3, wherein R is selected from a group consisting of alkyl, alkenyl, alkynyl, branched alkyl, branched alkenyl, branched alkynyl, substituted alkyl, substituted alkenyl and substituted alkynyl groups and their analogues; Y1 is a linker group which covalently attached to an R group at one site and is attached to A at a further independent site; Y2 is a linker group which is covalently attached to two R groups at two independent sites and is attached to A at a further independent site; and Y3 is a linker group which is covalently attached to three R groups at three independent sites and is attached to A at a further independent site.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: December 10, 2013
    Assignee: Commonwealth Scientific and Industrial Research Organisation
    Inventors: Calum John Drummond, Sharon Marie Sagnella, Minoo Jalili Moghaddam, Xiaojuan Gong
  • Publication number: 20130184451
    Abstract: This invention relates to a process of synthesizing a ?-nucleoside compound of formula (I): wherein R1 is alkyl, aryl, cycloalkyl, heteroaryl, or heterocycloalkyl. The process includes reacting a compound of formula (II): with a compound of formula (III): wherein R1 is as defined above and X is chloride, bromide, iodide, methanesulfonate, triflate, p-toluenesulfonate, trifluoroacetate, 4-nitrophenoxy, or N-succinimidyloxy, in a solvent and in the presence of a base.
    Type: Application
    Filed: January 8, 2013
    Publication date: July 18, 2013
    Applicant: PharmaEssentia Corp.
    Inventor: PharmaEssentia Corp.
  • Patent number: 8361988
    Abstract: The present invention comprises compounds useful as antiviral or antitumor agents. The compounds comprise nucleotide analogues that comprise tetrahydrofuranyl or tetrahydrothienyl moeities with quaternary centers at the 3? position. The nucleotide analogues can be used to inhibit cancer or viruses. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting diseases or conditions associated with cancers and viruses. Thus, the present invention also comprising pharmaceutical formulations comprising the compounds and methods of using the compounds and formulations to inhibit viruses or tumors and treat, prevent, or inhibit the foregoing diseases.
    Type: Grant
    Filed: January 17, 2008
    Date of Patent: January 29, 2013
    Assignee: Institut de Recherches Cliniques de Montreal
    Inventor: Yvan Guindon
  • Patent number: 8334364
    Abstract: [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a high therapeutic effect at a low dose. [Means For Solving Problems] Disclosed is a high molecular weight derivative of a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the carboxyl group in the side chain is bound to a hydroxyl group in the nucleoside derivative via an ester bond. Also disclosed is a method for producing the high molecular weight derivative.
    Type: Grant
    Filed: November 1, 2007
    Date of Patent: December 18, 2012
    Assignee: Nipon Kayaku Kabushiki Kaisha
    Inventors: Keiichiro Yamamoto, Kazutoshi Takashio
  • Publication number: 20120258891
    Abstract: The present disclosure relates to photoactivable protecting groups containing a diarylsulfide chromophore, a method for the synthesis thereof and their use as photoactivable protecting groups using maskless photolithography based array synthesis.
    Type: Application
    Filed: March 29, 2012
    Publication date: October 11, 2012
    Applicant: NIMBLEGEN SYSTEMS GMBH
    Inventor: Klaus-Peter Stengele
  • Publication number: 20120232029
    Abstract: Embodiments of the invention are to compounds, methods, and compositions for use in the treatment of viral infections. More specifically embodiments of the invention are 2?,4?-substituted nucleoside compounds useful for the treatment of viral infections, such as HIV, HCV, and HBV infections.
    Type: Application
    Filed: December 13, 2011
    Publication date: September 13, 2012
    Applicant: Pharmasset, Inc.
    Inventors: MICHAEL JOSEPH SOFIA, Jinfa Du
  • Publication number: 20120190639
    Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
    Type: Application
    Filed: April 30, 2010
    Publication date: July 26, 2012
    Applicant: UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEE
    Inventors: Steven Albert Everett, Saraj Ulhaq
  • Patent number: 8227594
    Abstract: Disclosed are nucleosides which are useful in diagnosing and treating viral infections, for example, infections caused by hepatitis B virus (HBV), and herpes viruses including Epstein Barr virus.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: July 24, 2012
    Inventors: Rakesh Kumar, Babita Agrawal, D. Lorne J. Tyrrell
  • Publication number: 20120184724
    Abstract: A nucleoside monomer that is protected by a thionocarbamate protecting group and contains one or more 2H, 13C, or 15N isotopes in the ribose and/or base part is provided, as well as a method for making a polynucleotide that uses the same. Also provided is a polynucleotide synthesis method that employs a diamine to deprotect a protected polynucleotide.
    Type: Application
    Filed: December 28, 2011
    Publication date: July 19, 2012
    Applicant: AGILENT TECHNOLOGIES, INC.
    Inventors: Agnieszka B. Sierzchala, Brian Phillip Smart, Douglas J. Dellinger, Geraldine Dellinger, Joel Myerson, Zoltan Timar
  • Patent number: 8202985
    Abstract: Nucleotide monomers, polynucleotides, methods of making each, and methods of deprotecting each, are disclosed. An embodiment of the nucleotide monomer, among others, includes a nucleotide monomer having a heterobase protecting group selected from structures I through III as described herein. An embodiment of the polynucleotide, among others, includes a plurality of nucleotide moieties having a heterobase protecting group selected from one of structures I through III as described herein.
    Type: Grant
    Filed: March 23, 2006
    Date of Patent: June 19, 2012
    Assignees: Agilent Technologies, Inc., The Regents of the University of Colorado
    Inventors: Douglas J. Dellinger, Zoltan Timar, Agnieszka Sierzchala, Geraldino Dellinger, Marvin H. Caruthers
  • Publication number: 20120149888
    Abstract: The present invention relates to synthesis, purification and methods to obtain high purity novel 2?-arabino-O-methyl nucleosides and the corresponding phosphoramidites of various arabinonucleoside bases and introduction of such units into defined sequence synthetic DNA and RNA. Various synthetic oligonucleotides, such as HIV integrase inhibitor 14-mer and thrombin binding oligonucleotide, thrombin-1, bearing ara-2?-omethyl modification have been synthesized. It is anticipated the oligonucleotides incorporating these monomers will exhibit biological activities related to antisense approach approach, design of better SiRNA's, diagnostic agents. Similarly, it is anticipated that oligonucleotides incorporating such novel nucleosides will be useful to develop therapeutic candidates designing stable G-quadruplexes and Aptamers for oligonucleotide structure, folding topology, evaluation of biochemical properties and design and develop as therapeutic agents.
    Type: Application
    Filed: February 23, 2010
    Publication date: June 14, 2012
    Inventors: Suresh C. Srivastava, Divya Pandey, Naveen P. Srivastava, Alok Srivastava
  • Patent number: 8193339
    Abstract: This invention relates to a process of stereoselectively synthesizing a ?-nucleoside compound of formula (I): wherein R1, R2, and B are as defined in the specification; each of R3 and R4, independently, is H or fluoro. The process includes reacting, in the presence of a transition metal salt, a tetrahydrofuran compound of formula (II): wherein R1, R2, and L are as defined in the specification, with a nucleobase derivative; and each of R3 and R4, independently, is H or fluoro.
    Type: Grant
    Filed: November 6, 2008
    Date of Patent: June 5, 2012
    Assignee: Pharmaessentia Corp.
    Inventors: Chi-Yuan Chu, Wei-Der Lee, Wensen Li, Chan Kou Hwang
  • Patent number: 8188222
    Abstract: [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a higher therapeutic effect at a lower dose. [Means for Solving Problems] Disclosed is a high molecular weight derivative a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the nucleoside derivative is bound to the carboxyl group in the side chain of the high molecular weight compound via a highly hydrophobic linker.
    Type: Grant
    Filed: November 6, 2007
    Date of Patent: May 29, 2012
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Keiichiro Yamamoto, Kazutoshi Takashio
  • Publication number: 20110301114
    Abstract: Amphiphilic prodrugs of general formula A-X are disclosed, wherein A is a biologically active agent or may be metabolised to a biologically active agent; and X is selected from the group consisting of R, or up to three R moieties attached to a linker, Y1, Y2 or Y3, wherein R is selected from a group consisting of alkyl, alkenyl, alkynyl, branched alkyl, branched alkenyl, branched alkynyl, substituted alkyl, substituted alkenyl and substituted alkynyl groups and their analogues; Y1 is a linker group which covalently attached to an R group at one site and is attached to A at a further independent site; Y2 is a linker group which is covalently attached to two R groups at two independent sites and is attached to A at a further independent site; and Y3 is a linker group which is covalently attached to three R groups at three independent sites and is attached to A at a further independent site Self-assembly of the amphiphilic prodrugs into reverse lyotropic phases, particularly hexagonal, cubic and sponge, is discl
    Type: Application
    Filed: December 4, 2009
    Publication date: December 8, 2011
    Inventors: Calum John Drummond, Sharon Marie Sangella, Minoo Jalili Moghaddam, Xiaojuan Gong
  • Patent number: 8058260
    Abstract: The present disclosure provides 2?-C-methyl-ribofuranosyl cytidine prodrugs, methods of making 2?-C-methyl-ribofuranosyl cytidine prodrugs, pharmaceutical compositions of 2?-C-methyl-ribofuranosyl cytidine prodrugs, and methods of using 2?-C-methyl-ribofuranosyl cytidine prodrugs and pharmaceutical compositions thereof to treat viral diseases such as hepatitis C.
    Type: Grant
    Filed: May 22, 2007
    Date of Patent: November 15, 2011
    Assignee: XenoPort, Inc.
    Inventor: Mark A. Gallop
  • Publication number: 20110275590
    Abstract: The present invention relates to conjugates of a drug and an amino acid or an amino acid derivative or analog, pharmaceutical compositions that include the conjugates and methods of use thereof. In particular, the present invention relates to conjugates of anti-proliferative drugs and asparagine and glutamine and analogs thereof as compositions for treatment of cancer, and conjugates of imaging agent carriers and amino acids for the diagnosis of tumors and metastases.
    Type: Application
    Filed: June 20, 2011
    Publication date: November 10, 2011
    Inventors: Stela Gengrinovitch, Esther Izakovich
  • Publication number: 20110269706
    Abstract: The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.
    Type: Application
    Filed: January 7, 2010
    Publication date: November 3, 2011
    Applicant: Northlake Biosciences LLC
    Inventors: Yu Chen, Yi Chen
  • Publication number: 20110224422
    Abstract: The present invention relates to substantially pure capecitabine and processes for the preparation thereof.
    Type: Application
    Filed: May 25, 2011
    Publication date: September 15, 2011
    Applicants: DR. REDDY'S LABORATORIES LTD., DR. REDDY'S LABORATORIES, INC.
    Inventors: Rajasekhar Kadaboina, Sekhar Munaswamy Nariyam, Veerender Murki, Raghupati Rama Vinjamuri, Srinivas Benda, Shravan Kumar Komati, Nageshwar Gunda
  • Publication number: 20110224421
    Abstract: The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2; (ii) converting said compound of formula 682-2? into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2?-cyano-2?-deoxy-N4-palmitoyl-1-?-D-arabmofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.
    Type: Application
    Filed: May 8, 2009
    Publication date: September 15, 2011
    Applicant: CYCLACEL LIMITED
    Inventors: Gavin Wood, Robert Westwood
  • Publication number: 20110178284
    Abstract: A protective group represented by the following general formula (I) (the oxygen atom attached with * represents oxygen atom of 2?-hydroxyl group of a ribonucleoside, a ribonucleotide or a derivative thereof; R1 and R2 both represent hydrogen atom, or represent a halogen atom, a C1-6 alkyl group, or a C1-6 halo-substituted alkyl group; R3 and R4 represent hydrogen atom, a halogen atom, a C1-6 alkyl group, or a C1-6 halo-substituted alkyl group; and R5 and R6 represent a halogen atom, a C1-6 halo-substituted alkyl group, cyano group, nitro group, or the like), which is stable under the reaction conditions of the nucleic acid synthetic cycles and has little steric hindrance, and can be removed under mild conditions using fluoride ions as a base.
    Type: Application
    Filed: September 15, 2010
    Publication date: July 21, 2011
    Applicant: CHIRALGEN, LTD.
    Inventors: Takeshi WADA, Mamoru SHIMIZU
  • Publication number: 20110123457
    Abstract: A therapeutic agent formed of a magnetic resonance imaging tracer conjugated with a chemotherapeutic agent. The therapeutic agents can be used in measuring drug delivery to a target tissue. The therapeutic agents allow for therapeutic MRI, in which 19F MRI techniques are used to detect, monitor, evaluate, and/or adjust chemotherapeutic drug dosage levels in a patient or a targeted tissue thereof.
    Type: Application
    Filed: December 17, 2010
    Publication date: May 26, 2011
    Inventor: Yihua Yu
  • Patent number: 7935681
    Abstract: 4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C (HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: May 3, 2011
    Assignee: Medivir AB
    Inventors: Nils-Gunnar Johansson, Genaidy Kalyanov, Joseph Armstrong Martin, David Bernard Smith, Anna Winqvist
  • Publication number: 20110021769
    Abstract: A process for making a capecitabine or its derivative comprising (a) reacting a compound of the formula (II): wherein each of R1 and R2 independently represents a hydroxyl protecting group, with an acylating agent of formula (III): X—C(?O)—R3, wherein X is an acyl activating group in an organic solvent to produce an acylated compound; (b) deprotecting the acylated compound to obtain the compound of formula (I); and (c) purifying the compound of formula (I) with a solvent.
    Type: Application
    Filed: July 21, 2010
    Publication date: January 27, 2011
    Inventors: Tsung-Cheng Hu, Hong-Tsung Huang
  • Patent number: 7851599
    Abstract: The invention refers to the use of L19IL2 for treatment of pancreatic cancer. In another embodiment, the invention relates to a combination (i) of a fusion protein, comprising an Interleukin 2 part and an antibody part, specifically recognizing the extra domain B of fibronectin (ED-B-fibronectin), and (ii) gemcitabine.
    Type: Grant
    Filed: April 4, 2007
    Date of Patent: December 14, 2010
    Assignee: Philogen S.p.A.
    Inventors: Andreas Menrad, Hans Dietrich Menssen, Karola Wagner
  • Publication number: 20100298550
    Abstract: It is an object of the present invention to provide a process for producing 1,2,3-tri-O-acetyl-5-deoxy-ribofuranose in an industrially appropriate manner. The present invention provides a process for producing a 1,2,3-tri-O-acetyl-5-deoxy-ribofuranose which comprises hydrogenating a compound represented by the formula (1) or formula (2) in the presence of a metal catalyst: wherein P1 and P2 independently represent a hydrogen atom or an acyl group, OP1 and OP2 may together form an acetal group, and R represents a hydrogen atom, an alkyl group, an aryl group, an aralkyl group, or an acyl group; wherein X1 represents Br or I, P3 and P4 independently represent a hydrogen atom or an acyl group, and R represents a hydrogen atom, an alkyl group, an aryl group, an aralkyl group, or an acyl group.
    Type: Application
    Filed: October 3, 2008
    Publication date: November 25, 2010
    Applicant: API CORPORATION
    Inventors: Tomoko Maeda, Hisatoshi Uehara, Naoki Harada, Manabu Katsurada, Mitsuharu Sano
  • Publication number: 20100249395
    Abstract: The present invention relates to a method for preparing capecitabine and a method for preparing a ?-anomer-rich trialkyl carbonate compound used therein, and a highly pure capecitabine can be efficiently prepared with a high yield by the method of the present invention using the ?-anomer-rich trialkyl carbonate compound as an intermediate.
    Type: Application
    Filed: November 7, 2008
    Publication date: September 30, 2010
    Applicant: HANMI PHARM. CO., LTD.
    Inventors: Jaeheon Lee, Gha-Seung Park, Weon Ki Yang, Jin Hee Kim, Cheol Hyun Park, Yong-Hoon An, Yoon Ju Lee, Young-Kil Chang, Gwan Sun Lee
  • Publication number: 20100240883
    Abstract: New prodrugs are derived from highly water soluble parent drugs that exist as primary or secondary amines in their parent form. Lipophilic carrier groups are bonded to the parent drug via an amide linkage with additional linker elements between the amide group and the carrier group.
    Type: Application
    Filed: March 17, 2010
    Publication date: September 23, 2010
    Inventors: Nian Wu, Brian Charles Keller
  • Patent number: 7776838
    Abstract: The subject invention discloses compounds, compositions and methods for treatment and prevention of toxicity due to chemotherapeutic agents and antiviral agents. Disclosed are acylated derivatives of non-methylated pyrimidine nucleosides. These compounds are capable of attenuating damage to the hematopoietic system in animals receiving antiviral or antineoplastic chemotherapy.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: August 17, 2010
    Assignee: Wellstat Therapeutics Corporation
    Inventors: Reid W. von Borstel, Michael K. Bamat
  • Patent number: 7772208
    Abstract: A method for the treatment or prevention of Flaviviridae infections, in particular, hepatitis C virus infection, in a host, and in particular, a human, is provided that includes administering an effective amount of a ?-L- or ?-D-2?,3?-dideoxynucleoside or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable diluent or excipient.
    Type: Grant
    Filed: January 8, 2008
    Date of Patent: August 10, 2010
    Assignees: Pharmasset, Inc., Leland Stanford Junior University, Emory University
    Inventors: Raymond Schinazi, Robert Striker, Junxing Shi
  • Patent number: 7772207
    Abstract: A first aspect of the invention relates to a combination comprising a CDK inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof. A second aspect of the invention relates to a pharmaceutical product comprising a CDK inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a CDK inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, to a subject.
    Type: Grant
    Filed: December 3, 2004
    Date of Patent: August 10, 2010
    Assignee: Cyclacel Limited
    Inventors: Simon Richard Green, Roger Neil Sleigh
  • Publication number: 20100130734
    Abstract: There is provided processes for the preparation of capecitabine and intermediates thereof.
    Type: Application
    Filed: April 17, 2008
    Publication date: May 27, 2010
    Applicants: DR. REDDY'S LABORATORIES LTD., DR. REDDY'S LABORATORIES, INC.
    Inventors: Raghavendracharyulu Venkata Palle, Anant Madhavrao Marathe, Srinivas Aluru, Ramesh Bochha, Rajasekhar Kadaboina, Sekhar Munaswamy Nariyam, Anil Patri
  • Patent number: 7691827
    Abstract: The present invention relates to the gemcitabine prodrug 1-(2,2-difluoro-2-deoxy-?-D -ribofuranosyl)-4-(2-propyl-1-oxopentyl)aminopyrimidin-2-one useful as an oral drug for the treatment of cancer.
    Type: Grant
    Filed: November 30, 2005
    Date of Patent: April 6, 2010
    Assignee: Eli Lilly and Company
    Inventors: David Michael Bender, David Michael Remick
  • Patent number: 7691826
    Abstract: A polysialic acid compound is reacted with a hetero-bifunctional reagent to introduce a pendant functional group for site-specific conjugation to sulfhydryl groups, for instance side chains of cysteine units in drugs, drug delivery systems, proteins or peptides. The functional group is, for instance, an N-maleimide group.
    Type: Grant
    Filed: August 12, 2004
    Date of Patent: April 6, 2010
    Assignee: Lipoxen Technologies Limited
    Inventors: Dale Howard Hreczuk-Hirst, Sanjay Jain, Peter Laing, Gregory Gregoriadis, Ioannis Papaioannou
  • Publication number: 20100062996
    Abstract: This invention relates to certain unsaturated fatty acid derivatives of therapeutically active 1,3-dioxolane nucleoside analogues and to pharmaceutical formulations containing them. The said derivatives are referred to as “Compounds of formula (I)” herein. Compounds of formula (I) can be used in the treatment of a cancerous disease. Treatment of both solid tumours and haematological cancers such as leukaemias, lymphomas and multiple myelomas are included.
    Type: Application
    Filed: December 7, 2006
    Publication date: March 11, 2010
    Applicant: CLAVIS PHARMA AS
    Inventors: Finn Myhren, Marit Liland Sandvold, Steinar Hagen, Ole Henrik Eriksen
  • Patent number: 7666856
    Abstract: 4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C (HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process.
    Type: Grant
    Filed: October 10, 2007
    Date of Patent: February 23, 2010
    Assignee: Medivir AB
    Inventors: Nils-Gunnar Johansson, Genadiy Kalyanov, Joseph Armstrong Martin, David Bernard Smith, Anna Winqvist
  • Patent number: 7645745
    Abstract: Compounds having the formula I wherein R1 is as herein defined are Hepatitis C virus NS5b polymerase inhibitors.
    Type: Grant
    Filed: April 4, 2007
    Date of Patent: January 12, 2010
    Assignee: Roche Palo Alto LLC
    Inventor: Keshab Sarma