The Hetero Ring Is Four-membered Patents (Class 549/510)
  • Patent number: 10314809
    Abstract: Application of Derivatives of Clostridium ghonii, especially in the application of Derivatives of Clostridium ghonii MW-DCG-HNCv-18 in preparation of medicines for treating non-small cell lung carcinoma. It also discloses a medicine combining the Derivatives of Clostridium ghonii MW-DCG-HNCv-18 strain with Docetaxel as the active ingredients. According to the invention, the MW-DCG-HNCv-18 strain is found to have specific inhibition effect on non-small cell lung carcinoma for the first time, the inhibition effect on the non-small cell lung carcinoma is significantly superior to that of other known similar strains, and through screening, the MW-DCG-HNCv-18 strain is found to have more prominent inhibition effect on non-small cell lung carcinoma when combined with Docetaxel injection.
    Type: Grant
    Filed: July 8, 2015
    Date of Patent: June 11, 2019
    Assignee: SHANDONG XINCHUANG BIOTECHNOLOGY CO., LTD.
    Inventors: Laitian Xing, Yong Wang, Mingqian Wei, Yanqiu Xing, Lianlian Li, Lichao Xing, Guangxia Deng, Hong Meng, Tao Huang, Dongxia Yang
  • Patent number: 10149911
    Abstract: This pharmaceutical composition contains a hydroxamic acid derivative, or a salt thereof, and a solubilizer, said hydroxamic acid derivative being selected from among (2S)-2-((4-((4-((1S)-1,2-dihydroxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N-hydroxy-N?,2-dimethylmalonamide, 2S)-2-((4-((4-((1R)-1,2-dihydroxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N-hydroxy-N?,2-dimethylmalonamide, and (2S)-N-hydroxy-2-((4-((4-((1S)-1-hydroxy-2-methoxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N?,2-dimethylmalonamide. The pharmaceutical composition demonstrates strong antibacterial activity, has excellent solubility in water, and is useful as a drug.
    Type: Grant
    Filed: September 11, 2015
    Date of Patent: December 11, 2018
    Assignee: TOYAMA CHEMICAL CO., LTD.
    Inventors: Tatsuya Honda, Yuko Suzumura, Tomoya Kato, Yu Koseki, Kohei Ono
  • Patent number: 9815806
    Abstract: The present invention provides an improved process for the preparation of 4?-acetoxy-2?-benzoyloxy-5?,20-epoxy-1?,13?-dihydroxy-7?,10?-dimethoxy-9-oxo-11-taxene (7?,10?-dimethoxy-10-deacetoxybaccatin III). The present invention also provides a novel process for the preparation of cabazitaxel.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: November 14, 2017
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Adulla Venkat Narsimha Reddy, Bandi Vamsi Krishna
  • Patent number: 9802951
    Abstract: The present invention relates to a novel chemical compound for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents.
    Type: Grant
    Filed: July 25, 2013
    Date of Patent: October 31, 2017
    Assignee: Tapestry Pharmaceuticals, Inc.
    Inventors: James D. McChesney, Gilles H. Tapolsky, David Lloyd Emerson, John Marshall, Michael Kurman, Manuel R. Modiano
  • Patent number: 9586919
    Abstract: The present invention relates to a new anhydrous crystalline form of Cabazitaxel of formula (I), designated as form H. A further object of the present invention is a processes for the preparation of the above mentioned form H by recrystallization of Cabazitaxel from a mixture of decanoyl- and octanoyl triglycerides or from glycerol trioctanoate. Form H of Cabazitaxel is useful for the preparation of Cabazitaxel, Cabazitaxel salts, and polymorphic forms thereof. It is also particularly useful as a medicament, especially for the treatment of cancers.
    Type: Grant
    Filed: October 9, 2014
    Date of Patent: March 7, 2017
    Assignee: INDENA S.P.A.
    Inventors: Walter Cabri, Daniele Ciceri, Luca Domenighini, Andrea Gambini, Federico Peterlongo
  • Patent number: 9487496
    Abstract: The present invention relates to a novel process for preparation of cabazitaxel (I) starting from 10-Deacetyl baccatin or derivative that involves methylation of 7, 10 —OH groups. Also provided is a novel process using chiral bis-lactam linker for the synthesis of cabazitaxel.
    Type: Grant
    Filed: October 31, 2013
    Date of Patent: November 8, 2016
    Assignee: Intas Pharmaceuticals Limited
    Inventors: Mettilda Lourdusamy, Ioan Iosif Radu, Rahul Chandrashayi Saxena, Raghvendra Jayantibhai Patel, Sandeep Bachubhai Shah
  • Patent number: 9434740
    Abstract: The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.
    Type: Grant
    Filed: July 8, 2014
    Date of Patent: September 6, 2016
    Assignee: ODONATE THERAPEUTICS, LLC
    Inventors: John K. Thottathil, Raymond P. Warrell
  • Patent number: 9402824
    Abstract: Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G? or Formula M?: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.
    Type: Grant
    Filed: January 23, 2015
    Date of Patent: August 2, 2016
    Assignee: Tapestry Pharmaceuticals, Inc.
    Inventors: Jan Zygmunt, James Ferrara, James D. McChesney
  • Patent number: 9403785
    Abstract: The present invention provides a non-solvated amorphous form of (2?,5?,7?,10?,13?)-4-acetoxy-13-({(2R,3S)-3[ (tert-butoxy carbonyl) amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate or Cabazitaxel (I), and process for preparation thereof. The present application also provides a non-solvated amorphous form of (2?,5?,7?,10?,13?)-4-acetoxy-13-({(2R,3S)-3[ (tert-butoxy carbonyl) amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate or Cabazitaxel (I) having an XRPD pattern as per FIG. 1, and IR spectrum as per FIG. 3 and is useful as an active pharmaceutical in a pharmaceutical composition comprising thereof and has anti-cancer activity.
    Type: Grant
    Filed: December 26, 2012
    Date of Patent: August 2, 2016
    Assignee: SHILPA MEDICARE LIMITED
    Inventors: Vimal Kumar Shrawat, Prashant Purohit, Rafiuddin Dr, Vinod Kumar Singh, Akshay Kant Chaturvedi
  • Patent number: 9394266
    Abstract: The invention relates to solid state forms of Cabazitaxel and processes for preparing the solid state forms. The invention further relates to pharmaceutical compositions and formulations comprising one or more of the solid state forms.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: July 19, 2016
    Assignee: Ivax International GmBh
    Inventors: Pavel Vraspir, Alexandr Jegorov, Roman Gabriel, Ales Gavenda
  • Patent number: 9284327
    Abstract: The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: March 15, 2016
    Assignee: GFV, LLC
    Inventors: John K. Thottathil, Raymond P. Warrell
  • Patent number: 9133152
    Abstract: A process for the preparation of 10-deacetyl-7,10-bis-trichloroacetylbaccatine III with HPLC purity higher than 99% and free from 2-debenzoyl-2-pentenoylbaccatine III by purification of 10-deacetyl-7,10-bis-trichloroacetylbaccatineIII followed by alkaline hydrolysis of the protecting groups in position 7 and 10.
    Type: Grant
    Filed: April 7, 2006
    Date of Patent: September 15, 2015
    Assignee: INDENA S.P.A.
    Inventors: Bruno Gabetta, Andrea Gambini
  • Patent number: 9127208
    Abstract: The present invention is related to a thermal extract of a plant material and methods of extraction thereof. The method of producing a thermal extract from a plant starting material by means of a thermal extraction of the starting material wherein the improvement consists in requiring smaller amounts of costly and/or toxic organic solvents for the extraction and partitioning steps.
    Type: Grant
    Filed: April 2, 2007
    Date of Patent: September 8, 2015
    Assignee: Pharmatherm Chemicals, Inc.
    Inventors: David Boulard, Robert G. Graham, Barry Freel
  • Patent number: 9119877
    Abstract: The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase II inhibitor, an inhibitor of a growth factor or of a growth factor receptor, an antimitotic agent, a proteasome inhibitor, an inhibitor of an anti-apoptotic protein and an antibody directed against a cell surface protein, wherein the active ingredients are present in each case in lice form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.
    Type: Grant
    Filed: November 17, 2010
    Date of Patent: September 1, 2015
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Dario Ballinari, Antonella Ciavolella, Enrico Pesenti, Alessia Montagnoli
  • Patent number: 9078929
    Abstract: The present invention relates to ?-polylysine conjugates, in particular conjugates of ?-polylysine with compounds carrying carboxyl groups, and to the preparation and use thereof for targeting of the kidney.
    Type: Grant
    Filed: July 9, 2010
    Date of Patent: July 14, 2015
    Assignee: Merck Patent GmbH
    Inventors: Armin Kuebelbeck, Gregor Larbig, Walter Mier, Barbro Beijer, Uwe Haberkorn
  • Patent number: 9062018
    Abstract: A crystalline from of 13-[(N-tert-butoxycarbonyl)-2?-O-hexanoyl-3-phenylisoserinyl]-10-deacetylbaccatin III.
    Type: Grant
    Filed: October 27, 2011
    Date of Patent: June 23, 2015
    Assignee: Indena S.p.A
    Inventors: Daniele Ciceri, Andrea Gambini, Maurizio Ricotti, Nicola Sardone
  • Publication number: 20150141673
    Abstract: The present invention relates to a novel crystalline polymorph form W of cabazitaxel and to method for the preparation thereof.
    Type: Application
    Filed: November 15, 2013
    Publication date: May 21, 2015
    Inventors: Honghai Song, Xingfeng Wang, Song Lin
  • Publication number: 20150141674
    Abstract: The present invention relates to the field of medical chemistry, and discloses a preparing method for three crystal forms of cabazitaxel, that is, crystalline form J of cabazitaxel esterate, crystalline form G of cabazitaxel hydrate and crystalline form I of cabazitaxel, and a novel crystalline form of cabazitaxel. The novel crystalline form of cabazitaxel according to the invention has good stability and good solubility in commonly used solvents, and is easy to be preserved and is stable under treatment during preparation of dosage forms, thus could be used for the preparation of a medicament for treating prostate cancer.
    Type: Application
    Filed: July 18, 2013
    Publication date: May 21, 2015
    Inventors: Jing Li, Quanxing Yao
  • Publication number: 20150125741
    Abstract: A secondary battery includes: a cathode; an anode; and non-aqueous electrolytic solution including a cyclic ether compound that includes a skeleton and one or more substituent groups introduced into the skeleton. The skeleton includes one or more four-or-more-membered oxygen-containing rings. The one or more substituent groups each are a monovalent group represented by Formula (1). —X—O—R??(1) (X is one of a divalent chain saturated hydrocarbon group, a halide group thereof, and nothing. R is one of a monovalent chain saturated hydrocarbon group, etc. At least one of one or more Rs includes one or more of the monovalent chain unsaturated hydrocarbon group, the monovalent cyclic unsaturated hydrocarbon group, the monovalent oxygen-containing cyclic unsaturated hydrocarbon group, the halide group thereof, and the monovalent group obtained by bonding two or more thereof, and includes a carbon-carbon multiple bond (one of —C?C— and —C?C—) bonded to an ether bond (—O—).
    Type: Application
    Filed: October 24, 2014
    Publication date: May 7, 2015
    Inventors: Toru ODANI, Tadahiko KUBOTA
  • Publication number: 20150119589
    Abstract: This invention relates to methods for making oxetan-3-ylmethanamines having the formula (I) wherein R1? and R2? are as defined herein. The methods of the invention provide the compounds of formula (I) in high yields and under conditions amenable for large-scale commercial production.
    Type: Application
    Filed: May 1, 2013
    Publication date: April 30, 2015
    Inventors: Magnus Carl Arne Eriksson, Suresh R. Kapadia, Jonathan Timothy Reeves, Xingzhong Zeng
  • Publication number: 20150110805
    Abstract: Numerous diseases have been linked to the production of effector cells. The present invention relates to the realization that effector cells are cycling in these diseases. In addition, the present invention relates to the determination that regulator cells are cycling in degenerative diseases. Based on these realizations, the present invention provides methods for treating conditions such as autoimmune diseases, degenerative diseases, and graft-versus-host disease. The present invention also relates to methods of determining when therapy should be administered to a patient.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventors: Martin Leonard Ashdown, Luisa Maria Ashdown
  • Patent number: 9012665
    Abstract: The present invention is directed to an amorphous form of cabazitaxel, which can be prepared by dissolving a solid form of cabazitaxel in an organic solvent, and removing the organic solvent to dryness. The amorphous form of cabazitaxel is characterized by DSC as in FIG. 1 and/or X-ray powder diffraction pattern as in FIG. 2.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: April 21, 2015
    Assignee: Yung Shin Pharm. Ind. Co., Ltd.
    Inventors: Liang-Rern Kung, Yi-Ting Hung, Tung-Shen Fang, Po-Wei Chang, Tsang-Miao Huang
  • Patent number: 9000193
    Abstract: The present invention discloses a process for the preparation of 4-acetoxy-2?-benzoyloxy-5?,20-epoxy-1-hydroxy-7?,10?-dimethoxy-9-oxotax-11-en-13?-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate Cabazitaxel (I).
    Type: Grant
    Filed: November 5, 2014
    Date of Patent: April 7, 2015
    Assignee: Fresenius Kabi Oncology Limited
    Inventors: Saswata Lahiri, Nitin Gupta, Abul Azim, Nilendu Panda, Bhuwan Bhaskar Mishra, Sunil Sanghani
  • Patent number: 8993790
    Abstract: Provide is an oxetane-ring containing (meth) acrylic ester compound which can give, through polymerization, a cured article being highly flexible or thermally stable. The oxetane-ring-containing (meth) acrylic ester compound is represented by formula (1) below, in which R1 represents a hydrogen atom or an alkyl group; R2 represent a hydrogen atom or a methyl group; and “A” represent either a linear alkylene group represented by following formula (a1) or a branched-chain alkylene group represented by following formula (a2).
    Type: Grant
    Filed: November 5, 2010
    Date of Patent: March 31, 2015
    Assignee: Daicel Corporation
    Inventors: Tamaki Son, Kiyoshi Ikura
  • Patent number: 8981040
    Abstract: Provided is a cationically polymerizable resin which is rapidly cured upon irradiation with light and forms a cured product excellent in flexibility and thermal stability. The cationically polymerizable resin is obtained through radical polymerization of an oxetane-ring-containing (meth)acryloyl compound represented by following Formula (1) alone or in combination with another radically polymerizable compound. In the formula, R1 represents hydrogen atom or methyl group; R2 represents hydrogen atom or an alkyl group; and “A” represents a linear or branched chain alkylene group having 2 to 20 carbon atoms.
    Type: Grant
    Filed: January 24, 2011
    Date of Patent: March 17, 2015
    Assignee: Daicel Corporation
    Inventors: Naoko Araki, Yoshinori Funaki, Kiyoharu Tsutsumi, Tomoaki Mahiko
  • Publication number: 20150073159
    Abstract: The invention relates to solid state forms of Cabazitaxel, and processes for preparation, via novel synthetic intermediates, thereof, and formulations comprising one or more of the solid state forms of Cabazitaxel.
    Type: Application
    Filed: November 19, 2014
    Publication date: March 12, 2015
    Inventors: Ondrej SIMO, Pavel VRASPIR, Tomas HOLAS, Alexandr JEGOROV, Roman GABRIEL
  • Publication number: 20150072969
    Abstract: The present invention relates to phenyl alkanoic acid derivatives (the compounds of Formula (I)); and their isotopic forms, stereoisomeric and tautomeric forms and mixtures thereof in all ratios, or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, prodrugs, polymorphs, N-oxides, S-oxides or carboxylic acid isosteres thereof. The invention also relates to processes for the preparation of compounds of Formula (I) and pharmaceutical compositions comprising one or more of the compounds of Formula (I). The said compounds and the pharmaceutical composition function as GPR (G-protein coupled receptor) agonists, particularly as GPR40 agonists, and are useful in the treatment of diseases or conditions mediated by GPR40. The present invention further relates to a method of treatment of diseases or conditions mediated by GPR40 comprising administering to a subject in need thereof a therapeutically effective amount of the compounds of Formula (I).
    Type: Application
    Filed: February 27, 2013
    Publication date: March 12, 2015
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Sanjay Kumar, Rajiv Sharma, Vishal Ashok Mahajan, Sangameshwar Prabhakar Sawargave
  • Publication number: 20150072396
    Abstract: Low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations for modifying biomolecules is provided. Compositions, methods, and kits relating to low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations are also provided.
    Type: Application
    Filed: March 1, 2012
    Publication date: March 12, 2015
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Kyle Gee, Upinder Singh, Scott Grecian, Scott Clarke
  • Publication number: 20150065516
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: October 29, 2014
    Publication date: March 5, 2015
    Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Halyan Wang
  • Publication number: 20150057458
    Abstract: Process for the production of a chemical compound from a carbon dioxide starting material, comprising the steps of a) providing a feed stream consisting mainly of carbon dioxide; b) electrolysing in an electrolysis stage the carbon dioxide in the feed stream to a first gas stream containing carbon monoxide and a second gas stream containing oxygen, wherein the molar ratio between carbon monoxide and oxygen is about 1:0.5 in an electrolysis stage; c) adjusting the composition of the first gas stream or the second gas stream or both gas streams to include carbon dioxide, either by operating at less than full conversion of CO2 or by sweeping one or both gas streams with a gas containing CO2 or by at some stage between the electrolysis cell and the oxidative carbonylation reactor diluting one or both gas streams with a gas containing CO2; all while maintaining an overall molar ratio of carbon monoxide to oxygen of about 1:0.
    Type: Application
    Filed: April 11, 2013
    Publication date: February 26, 2015
    Applicant: Haldor Topsøe A/S
    Inventors: Niels Christian Schjødt, John Bøgild Hansen, Claus Friis Pedersen
  • Patent number: 8962870
    Abstract: Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G? or Formula M?: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: February 24, 2015
    Assignee: Tapestry Pharmaceuticals, Inc.
    Inventors: Jan Zygmunt, James Ferrara, James D. McChesney
  • Patent number: 8962871
    Abstract: A 4-benzyl-1-methyl-6-oxabicyclo[3,2,0]heptane derivative is manufactured by reducing, in the presence of both a halogenating agent and a hydride-type reducing agent, a methylene moiety bound to a sulfonyloxy group in a compound represented by General Formula (II).
    Type: Grant
    Filed: November 5, 2012
    Date of Patent: February 24, 2015
    Assignee: Kureha Corporation
    Inventor: Hisashi Kanno
  • Publication number: 20150051269
    Abstract: The present invention relates to a hydrophobic drug delivery conjugate, to which cyclodextrin, poly(maleic anhydride), and a hydrophobic drug are bonded, and to a pharmaceutical composition comprising the hydrophobic drug delivery conjugate as an active ingredient. The hydrophobic drug delivery conjugate according to the present invention can effectively control the release rate and the delivery rate of a hydrophobic drug by regulating the physicochemical bonding and/or composition of the cyclodextrin, poly(maleic anhydride), and hydrophobic drug, and can also increase the effect of the drug by significantly increasing the solubility of the hydrophobic drug. Further, the present invention can enable the type of the hydrophobic drug to be varied, as well as a peptide having target directivity to be introduced into a surface of the conjugate, such that the present invention can be applied to the treatment of various diseases in addition to cancer treatment.
    Type: Application
    Filed: March 12, 2013
    Publication date: February 19, 2015
    Inventors: Won Jong Kim, Ran Namgung, Byung Heon Lee, In San Kim, Allan Hoffman
  • Publication number: 20150050713
    Abstract: Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.
    Type: Application
    Filed: July 25, 2014
    Publication date: February 19, 2015
    Inventors: Michael P. Malakhov, Fang Fang
  • Publication number: 20150038564
    Abstract: The invention relates to solid state forms of Cabazitaxel and processes for preparing the solid state forms. The invention further relates to pharmaceutical compositions and formulations comprising one or more of the solid state forms.
    Type: Application
    Filed: March 7, 2013
    Publication date: February 5, 2015
    Inventors: Pavel Vraspir, Alexandr Jegorov, Roman Gabriel, Ales Gavenda
  • Publication number: 20150005517
    Abstract: Disclosed is a method of crystallizing a taxane comprising combining the taxane and methylene chloride to obtain a solution and adding an anti-solvent to the solution to obtain a crystalline taxane, wherein the anti-solvent is selected from the group consisting of hexane and heptane.
    Type: Application
    Filed: February 24, 2014
    Publication date: January 1, 2015
    Applicant: Phyton Holdings LLC
    Inventors: James H. Johnson, T.G. Sambandam, Barry J. Hand, Christopher D. Howe, Roland R. Franke, Brian A. Bucher, John S. Juchum, Rex T. Gallagher, Marc A. Plante, Edward M. Desimone, III, Dong S. Yang
  • Publication number: 20150005487
    Abstract: The present invention relates to a sorbent comprising a solid support material, the surface of which comprises a residue of a general formula (I), wherein the residue is attached via a covalent single bond to a functional group on the surface of either the bulk solid support material itself or of a polymer film on the surface of the solid support material. Furthermore, the present invention relates to the use of the sorbent according to the invention for the purification of organic molecules, in particular pharmaceutically active compounds, preferably in chromatographic application.
    Type: Application
    Filed: September 17, 2012
    Publication date: January 1, 2015
    Applicant: INSTRACTION GMBH
    Inventors: Markus Arendt, Björn Degel, Thomas Schwarz, Gerhard Stumm, Martin Welter
  • Patent number: 8921411
    Abstract: The invention relates to solid state forms of Cabazitaxel, and processes for preparation, via novel synthetic intermediates, thereof, and formulations comprising one or more of the solid state forms of Cabazitaxel. The present invention further provides pharmaceutical compositions comprising one or more of the solid state forms of Cabazitaxel, and a method of treating hormone-refractory prostate cancer.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: December 30, 2014
    Assignee: Plus Chemicals SA
    Inventors: Ondrej Simo, Pavel Vraspir, Tomas Holas, Alexandr Jegorov, Roman Gabriel
  • Publication number: 20140371474
    Abstract: The invention provides new cabazitaxel isoserine ester intermediates and new synthetic methods, and a preparation method for the anti-tumour drugs cabazitaxel, docetaxel and paclitaxel from the new cabazitaxel isoserine intermediates.
    Type: Application
    Filed: October 19, 2012
    Publication date: December 18, 2014
    Applicant: Shanghai Bioman Phama Limited
    Inventors: Yunman Zheng, Tianhui Xu, Ragina Naidu
  • Patent number: 8912212
    Abstract: The present disclosure relates in part to pharmaceutical compositions comprising polymeric nanoparticles having certain glass transition temperatures. Other aspects of the invention include methods of making such nanoparticles.
    Type: Grant
    Filed: September 27, 2013
    Date of Patent: December 16, 2014
    Assignee: BIND Therapeutics, Inc.
    Inventors: Stephen E. Zale, Greg Troiano, Mir Mukkaram Ali, Jeff Hrkach, James Wright
  • Patent number: 8912229
    Abstract: The present application discloses new taxane analogs, intermediates and methods for producing them. The present application is also directed to pharmaceutical formulations comprising abeo-taxanes and methods of treating cancer with the abeo-taxanes.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: December 16, 2014
    Assignee: Arbor Therapeutics, LLC
    Inventors: James D. McChesney, John T. Henry, Sylesh Venkataraman, Mahesh Kumar Gundluru
  • Patent number: 8905997
    Abstract: Disclosed herein are therapeutic compositions for treating and preventing diseases such as neointimal hyperplasia (NIH), where the compositions comprise a therapeutic particle that has a localized association with a blood vessel and a therapeutic agent, such as an anti-NIH agent. Methods of use of the therapeutic compositions are also disclosed.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: December 9, 2014
    Assignee: BIND Therapeutics, Inc.
    Inventors: Amy Grayson, Stephen E. Zale, David Dewitt
  • Publication number: 20140356417
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Application
    Filed: June 12, 2014
    Publication date: December 4, 2014
    Inventors: Peter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Patent number: 8901327
    Abstract: The present invention discloses a process for the preparation of 4-acetoxy-2?-benzoyloxy-5?,20-epoxy-1-hydroxy-7?,10?-dimethoxy-9-oxotax-11-en-13?-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate Cabazitaxel (I).
    Type: Grant
    Filed: September 24, 2012
    Date of Patent: December 2, 2014
    Assignee: Fresenius Kabi Oncology Limited
    Inventors: Saswata Lahiri, Nitin Gupta, Abul Azim, Nilendu Panda, Bhuwan Bhaskar Mishra, Sunil Sanghani
  • Publication number: 20140350273
    Abstract: The present invention relates to the compound of formula (I): which may be in the form of an anhydrous base, a hydrate or a solvate, for its use for the treatment of pediatric cancers.
    Type: Application
    Filed: August 7, 2014
    Publication date: November 27, 2014
    Inventors: Sidhu S. SUKHVINDER, Patricia VRIGNAUD
  • Publication number: 20140350272
    Abstract: The invention relates to anhydrides, solvates and ethanol hetero-solvates and hydrates of dimethoxy docetaxel or (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate of 4-acetoxy-2?-benzoyloxy-5?,20-epoxy-1-hydroxy-7?, 10?-dimethoxy-9-oxo-tax-11-ene-13?-yle, and to the preparation thereof.
    Type: Application
    Filed: August 6, 2014
    Publication date: November 27, 2014
    Inventors: Pascal BILLOT, Marielle DUFRAIGNE, Hagit ELMALEH, Alexandre GIULIANI, Fabrice MANGIN, Patricia RORTAIS, Lionel ZASKE
  • Patent number: 8895589
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: November 25, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Chris Allen Broka, Ronald Charles Hawley
  • Publication number: 20140343133
    Abstract: The present invention relates to a novel crystalline ethyl acetate solvate form of cabazitaxel or 4?-acetoxy-2?-benzoyloxy-5?,20-epoxy-1?-hydroxy-7?,10?-dimethoxy-9-oxo-11-taxen-13?-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate and process for preparing the same.
    Type: Application
    Filed: June 11, 2014
    Publication date: November 20, 2014
    Inventors: Eric DIDIER, Nicolas TREMAUDEUX, Lionel ZASKE
  • Publication number: 20140336246
    Abstract: The present invention provides a non-solvated amorphous form of (2?,5?,7?,10?,13?)-4-acetoxy-13-({(2R,3S)-3[ (tert-butoxy carbonyl) amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate or Cabazitaxel (I), and process for preparation thereof. The present application also provides a non-solvated amorphous form of (2?,5?,7?,10?,13?)-4-acetoxy-13-({(2R,3S)-3[ (tert-butoxy carbonyl) amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate or Cabazitaxel (I) having an XRPD pattern as per FIG. 1, and IR spectrum as per FIG. 3 and is useful as an active pharmaceutical in a pharmaceutical composition comprising thereof and has anti-cancer activity.
    Type: Application
    Filed: December 26, 2012
    Publication date: November 13, 2014
    Applicant: SHILPA MEDICARE LIMITED
    Inventors: Vimal Kumar Shrawat, Prashant Purohit, Rafiuddin Dr, Vinod Kumar Singh, Akshaykant Chaturvedi
  • Patent number: 8877759
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: September 4, 2012
    Date of Patent: November 4, 2014
    Assignee: Vertex Pharnaceuticals Incorporated
    Inventors: Jean-Damien Charrier, David Kay, Somhairle MacCormick, Pierre-Henri Storck, Joanne Pinder, Michael Edward O'Donnell, Ronald Marcellus Alphonsus Knegtel, Stephen Clinton Young, Philip Michael Reaper, Steven John Durrant, Heather Clare Twin, Christopher John Davis