Nitrogen Bonded Directly To The Pteridine Ring System Patents (Class 544/258)
  • Patent number: 10753942
    Abstract: Disclosed methods for detecting remnant cancer cells in a tissue sample.
    Type: Grant
    Filed: October 3, 2018
    Date of Patent: August 25, 2020
    Assignee: Indicator Systems International, Inc.
    Inventors: Robert M. Moriarty, Richard J. Pariza, David M. White, Gerald F. Swiss
  • Patent number: 10519146
    Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
    Type: Grant
    Filed: May 21, 2018
    Date of Patent: December 31, 2019
    Assignee: Amgen Inc.
    Inventors: Brian Alan Lanman, Jian Chen, Anthony B. Reed, Victor J. Cee, Longbin Liu, David John Kopecky, Patricia Lopez, Ryan Paul Wurz, Thomas T. Nguyen, Shon Booker, Nobuko Nishimura, Youngsook Shin, Nuria A. Tamayo, John Gordon Allen, Jennifer Rebecca Allen
  • Patent number: 10286080
    Abstract: IgA-based Fc-folate conjugates as a treatment for cancer are provided. The conjugates utilize only the Fc portion of IgA to target its receptor on neutrophils (Fc?R1) to elicit antibody-dependent cellular-cytotoxicity (ADCC).
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: May 14, 2019
    Assignee: Wayne State University
    Inventor: Cecilia Speyer
  • Patent number: 9938280
    Abstract: Described herein are methods for making folic acid derivatives, intermediates, pharmaceutical compositions and uses thereof.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: April 10, 2018
    Assignee: Chemic Laboratories, Inc.
    Inventors: Gerald S. Jones, Jr., Joseph P. St. Laurent, Scott A. Goodrich
  • Patent number: 9611227
    Abstract: The present invention provides an antitumor effect potentiator for enhancing antitumor activity of an antitumor agent comprising tegafur in a therapeutically effective amount, gimeracil in an amount effective for enhancing an antitumor effect, and oteracil potassium in an amount effective for inhibiting a side effect. The antitumor effect potentiator comprising at least one member selected from the group consisting of folinic acid and pharmacologically acceptable salts thereof. The present invention also provides a method for enhancing an antitumor effect of an antitumor agent comprising the step of administering to a patient the aforementioned antitumor effect potentiator; and a method for cancer treatment comprising the step of administering to a patient the aforementioned antitumor agent.
    Type: Grant
    Filed: March 11, 2004
    Date of Patent: April 4, 2017
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Junji Uchida, Koyo Shudo
  • Patent number: 9598415
    Abstract: The present invention encompasses compounds of the formula (I) wherein the variables are defined herein which are suitable for the modulation of ROR? and the treatment of diseases related to the modulation of ROR?. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
    Type: Grant
    Filed: September 20, 2016
    Date of Patent: March 21, 2017
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Johanna Bakonyi, Steven Richard Brunette, Delphine Collin, Robert Owen Hughes, Xiang Li, Shuang Liang, Robert Sibley, Michael Robert Turner, Lifen Wu, Qiang Zhang
  • Patent number: 9433624
    Abstract: The present invention is directed to a novel methods and compositions for the therapeutic intervention in hyperphenylalaninemia. More specifically, the specification describes methods and compositions for treating various types of phenylketonurias using compositions comprising BH4. Combination therapies of BH4 and other therapeutic regimens are contemplated.
    Type: Grant
    Filed: November 16, 2011
    Date of Patent: September 6, 2016
    Assignee: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Daniel I. Oppenheimer, Emil D. Kakkis, Fredric D. Price, Alejandro Dorenbaum, Rudolf Moser, Viola Groehn, Thomas Egger, Fritz Blatter
  • Patent number: 9382251
    Abstract: Described herein are methods for making folic acid derivatives, intermediates, pharmaceutical compositions and uses thereof.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: July 5, 2016
    Assignee: CHEMIC LABORATORIES INC.
    Inventors: Gerald S. Jones, Jr., Joseph P. St. Laurent, Scott A. Goodrich
  • Patent number: 9371326
    Abstract: Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, and resolves a racemate intermediate or an intermediate having a low antimer isomerism value by using a chiral resolving reagent, thereby obtaining an intermediate having a high antimer isomerism value. Raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
    Type: Grant
    Filed: December 27, 2012
    Date of Patent: June 21, 2016
    Assignees: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD, ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD, TIANJIN ASYMCHEM PHARMACEUTICAL CO., LTD, ASYMCHEM LABORATORIES (FUXIN) CO., LTD, JILIN ASYMCHEM LABORATORIES CO., LTD
    Inventors: Hao Hong, James Gage, Chaoyong Chen, Jiangping Lu, Yan Zhou, Shuangyong Liu
  • Patent number: 9365573
    Abstract: Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, introduces a chiral center in an asymmetric synthesis manner, in which a tetrahydrofuran solution containing a samarium catalyst is adopted as a catalyst, and obtains a target compound having a high antimer isomerism value by means of selective catalysis. The yield is improved, raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
    Type: Grant
    Filed: December 27, 2012
    Date of Patent: June 14, 2016
    Assignees: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD, ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD, ASYMCHEM LABORATORIES (FUXIN) CO., LTD, JILIN ASYMCHEM LABORATORIES CO., LTD, TIANJIN ASYMCHEM PHARMACEUTICAL CO., LTD.
    Inventors: Hao Hong, James Gage, Chaoyong Chen, Jiangping Lu, Yan Zhou, Shuangyong Liu
  • Patent number: 9254341
    Abstract: The present invention discloses a process for preparing a compound having the formula Including Reacting a compound of the formula 1: with a compound of the formula: in the presence of a polar solvent and trifluoroacetic acid to provide a compound of the formula: or a racemic mixture thereof; and further reacting the compound of the formula: or a racemic mixture thereof; with sodium hydroxide and a compound of the formula: wherein R1 and R2 are as defined above.
    Type: Grant
    Filed: October 4, 2013
    Date of Patent: February 9, 2016
    Inventors: Sumith A. Kularatne, Pravin Gagare, Mohammad Noshi
  • Patent number: 9242989
    Abstract: The present invention encompasses compounds of the formula (I) wherein the variables are defined herein which are suitable for the modulation of ROR? and the treatment of diseases related to the modulation of ROR?. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
    Type: Grant
    Filed: April 10, 2015
    Date of Patent: January 26, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Johanna Bakonyi, Steven Richard Brunette, Delphine Collin, Robert Owen Hughes, Xiang Li, Shuang Liang, Robert Sibley, Michael Robert Turner, Lifen Wu, Qiang Zhang
  • Patent number: 9150982
    Abstract: Disclosed are a crystal form of (6S)-5-methyltetrahydrofolate salt and a method for preparing the same. The crystal form is: Form C of the crystal form of (6S)-5-methyltetrahydrofolate calcium salt, where the X-ray diffraction pattern has diffraction peaks at the 2? angles of 6.3±0.2 and 19.2±0.2; or the crystal form of (6S)-5-methyltetrahydrofolate strontium salt, where the X-ray diffraction pattern has diffraction peaks at the 2? angles of 6.5±0.2 and 22.0±0.2. The crystal form of (6S)-5-methyltetrahydrofolate salt of the present invention has the advantages of excellent physicochemical properties, good stability, high purity, good reproducibility, and being more suitable for production on an industrial scale.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: October 6, 2015
    Assignee: LIANYUNGANG JINKANG HEXIN PHARMACEUTICAL CO. LTD.
    Inventors: Zheqing Wang, Yongzhi Cheng, Heng Huang, Huizhen Li
  • Patent number: 9029344
    Abstract: The disclosure provides linked purine pterin compounds and analogs thereof that are novel HPPK inhibitors. The HPPK inhibitors described herein are compounds and the pharmaceutically acceptable salts thereof of general Formula I The variables, e.g. A1 to A3, R1 to R4, L1, L2, B1, and B2 are described herein. Compounds and salts of Formula I bind to HPPK with high affinity and specificity. Pharmaceutical compositions containing an HPPK inhibitor of Formula I and methods of treating a bacterial infection in a patient by providing one or more HPPK inhibitors of Formula I to the patient are also provided. Processes and intermediates useful for preparing compounds of Formula I are also provided. Methods of using the disclosed compounds to guide the development of additional novel anti-bacterial agents are also provided.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: May 12, 2015
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Genbin Shi, Gary X. Shaw, Xinhua Ji
  • Publication number: 20150126508
    Abstract: Provided are a pteridine ketone derivative used as an EGFR, BLK, and FLT3 inhibitor and applications thereof. Specifically, provided are a compound of the following formula I, a pharmaceutical composition containing the compound of the formula I, and use of compound in preparing medicine for treating diseases mediated by EGFR, BLK, or FLT3 or inhibiting EGFR, BLK, and FLT3.
    Type: Application
    Filed: April 2, 2013
    Publication date: May 7, 2015
    Inventors: Honglin Li, Yufang Xu, Zhenjiang Zhao, Xiaofeng Liu, Wei Zhou, Fang Bai, Mengzhu Xue, Lei Zhang, Youli Zhang
  • Publication number: 20150125390
    Abstract: The present invention is directed towards new 18F-folate/antifolate analogue radiopharmaceuticals, wherein the phenyl group within folate structures has been replaced by an 18F-heterocycle, their precursors, a method of their preparation, as well as their use in diagnosis of a cell or population of cells expressing a folate-receptor and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.
    Type: Application
    Filed: May 8, 2013
    Publication date: May 7, 2015
    Applicant: MERCK & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Mueller, Simon Mensah Ametamey, Thomas Betzel, Viola Groehn
  • Publication number: 20150126502
    Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 7, 2015
    Inventors: Robert A. GALEMMO, Dean R. ARTIS, Xiaocong Michael YE, Danielle Aubele, Anh TRUONG, Simeon BOWERS, Roy K. Hom, Yong-Liang ZHU, R. Jeffrey NEITZ, Jennifer SEALY, Marc ADLER, Paul BEROZA, John P. ANDERSON
  • Publication number: 20150119405
    Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
    Type: Application
    Filed: October 23, 2014
    Publication date: April 30, 2015
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Neil Bifulco, Jr., Lucian V. DiPietro, Brian L. Hodous, Chandrasekhar V. Miduturu
  • Publication number: 20150119573
    Abstract: Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, and resolves a racemate intermediate or an intermediate having a low antimer isomerism value by using a chiral resolving reagent, thereby obtaining an intermediate having a high antimer isomerism value. Raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
    Type: Application
    Filed: December 27, 2012
    Publication date: April 30, 2015
    Inventors: Hao Hong, James Gage, Chaoyong Chen, Jiangping Lu, Yan Zhou, Shuangyong Liu
  • Publication number: 20150119574
    Abstract: To provide a method for producing sepiapterin, lactoylpterin or tetrahydrolactoylpterin. Sepiapterin, lactoylpterin and tetrahydrolactoylpterin are produced at high yield through the following reaction scheme.
    Type: Application
    Filed: May 7, 2013
    Publication date: April 30, 2015
    Applicant: SHIRATORI PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi Yoshino, Taichi Komoda, Yuichi Shiro, Shunichi Murata, Shizuaki Murata, Yasuhiro Kuroda
  • Publication number: 20150105555
    Abstract: Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, introduces a chiral center in an asymmetric synthesis manner, in which a tetrahydrofuran solution containing a samarium catalyst is adopted as a catalyst, and obtains a target compound having a high antimer isomerism value by means of selective catalysis. The yield is improved, raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
    Type: Application
    Filed: December 27, 2012
    Publication date: April 16, 2015
    Inventors: Hao Hong, James Gage, Chaoyong Chen, Jiangping Lu, Yan Zhou, Shuangyong Liu
  • Publication number: 20150080368
    Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Applicant: VERASTEM, INC.
    Inventors: Michael Joseph Luzzio, Kevin Daniel Freeman-Cook, Samit Kumar Bhattacharya, Matthew Merrill Hayward, Catherine Angela Hulford, Christopher Lowell Autry, Xumiao Zhao, Jun Xiao, Kendra Louise Nelson
  • Publication number: 20150065708
    Abstract: The present invention relates to a compound [4-(2-amino-10-methyl-4-oxo-6,7,8,9-tetrahydro-4a,7-cycloimino-pyrimido[4,5-b][1,4]diazepine-5(4H)-yl)benzoyl]-glutamate (JK12A for short) with the structure in Formula I. The present invention also relates to the crystal form and salt of the compound JK12A, and preparation method and applications thereof. The compound JK12A of the present invention can be used to prepare drugs as an active ingredient for medicament or food additives.
    Type: Application
    Filed: April 9, 2013
    Publication date: March 5, 2015
    Inventors: Yongzhi Cheng, Zhi Cheng, Min Zhou, Zhaojun Wang, Huizhen Li, Shenggang Fan
  • Publication number: 20150030669
    Abstract: The present invention is directed to carrier systems comprising ether-lipids conjugated to one or more bioactive ligands and exposed on the surface of the carrier system for use in targeted delivery and/or antigen display systems. Optionally one or more further bioactive agents may be encapsulated or embedded within or attached to or adsorbed onto the carrier system. The present invention is further directed to methods of their preparation and their uses in medical applications, such as targeted delivery of bioactive agents to specific tissues or cells and antigen display systems for the study, diagnosis, and treatment of traits, diseases and conditions that respond to said bioactive agents.
    Type: Application
    Filed: March 11, 2013
    Publication date: January 29, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Michael Wilhelm Platscher, Raymond Behrendt, Viola Groehn, Simone Rachel Hoertner, Marco Silvio Passafaro, Finn Bauer
  • Publication number: 20150018357
    Abstract: Disclosed are a crystal form of (6S)-5-methyltetrahydrofolate salt and a method for preparing the same. The crystal form is: Form C of the crystal form of (6S)-5-methyltetrahydrofolate calcium salt, where the X-ray diffraction pattern has diffraction peaks at the 2? angles of 6.3±0.2 and 19.2±0.2; or the crystal form of (6S)-5-methyltetrahydrofolate strontium salt, where the X-ray diffraction pattern has diffraction peaks at the 2? angles of 6.5±0.2 and 22.0±0.2. The crystal form of (6S)-5-methyltetrahydrofolate salt of the present invention has the advantages of excellent physicochemical properties, good stability, high purity, good reproducibility, and being more suitable for production on an industrial scale.
    Type: Application
    Filed: December 17, 2012
    Publication date: January 15, 2015
    Inventors: Zheqing Wang, Yongzhi Cheng, Heng Huang, Huizhen Li
  • Publication number: 20140315911
    Abstract: Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven or mediated at least in part by RSK. This Abstract is not limiting of the invention.
    Type: Application
    Filed: November 12, 2012
    Publication date: October 23, 2014
    Inventors: Meizhong Jin, Mridula Kadalbajoo, An-Hu Li, Mark J. Mulvihill, Kam W. Siu, Arno G. Steinig, Jing Wang
  • Publication number: 20140315220
    Abstract: Disclosed are conjugates that can bind to one or more site on cancer cell surface, for example, surface proteins, compound specific receptors and carbohydrates that comprise the surface of specific cell types. The disclosed conjugates can thereby serve as indicators identifying the presence of cancerous tissue.
    Type: Application
    Filed: July 20, 2012
    Publication date: October 23, 2014
    Applicant: GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION
    Inventors: Chaofeng Dai, Binghe Wang, Lifang Wang, Yong Chu
  • Publication number: 20140316132
    Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
    Type: Application
    Filed: July 1, 2014
    Publication date: October 23, 2014
    Inventors: Manoj C. Desai, Randal L. Halcomb, Paul Hrvatin, Hon Chung Hui, Ryan McFadden, Paul A. Roethle, Hong Yang
  • Patent number: 8865716
    Abstract: The present invention relates to spiroheterocycl-dihydropyrimidines, their use as modulators of ?-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with ?-secretase and/or its substrate and therefore modulate the formation of A? peptides.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: October 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Christian Eickmeier, Kai Gerlach, Niklas Heine, Alexander Weber, Ulrike Gross
  • Publication number: 20140294733
    Abstract: The present invention relates to dendrimer synthesis. Specifically, the present invention relates to dendrimer compositions (e.g., scaffolds) capable of copper-free click conjugation for use in the synthesis of functionalized dendrimers, and methods of use of the same.
    Type: Application
    Filed: November 20, 2012
    Publication date: October 2, 2014
    Inventors: James R. Baker, JR., Baohua M. Huang, Thommey P. Thomas
  • Publication number: 20140271482
    Abstract: The present disclosure relates to compounds that are useful as near-infrared fluorescence probes, wherein the compounds include i) a pteroyl ligand that binds to a target receptor protein, ii) a dye molecule, and iii) a linker molecule that comprises an amino acid or derivative thereof. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds.
    Type: Application
    Filed: August 26, 2013
    Publication date: September 18, 2014
    Applicant: Purdue Research Foundation
    Inventors: Philip S. Low, Sumith A. Kularatne, Sakkarapalayam M. Mahalingam
  • Publication number: 20140275533
    Abstract: Methods of synthesis and compositions of use for compounds that are useful as near-infrared fluorescence probes, wherein the compounds include i) a pteroyl ligand that binds to a target receptor protein, ii) a dye molecule, and iii) a linker molecule that comprises an amino acid or derivative thereof.
    Type: Application
    Filed: October 4, 2013
    Publication date: September 18, 2014
    Applicant: On Target Laboratories, LLC
    Inventors: Sumith A. Kularatne, Pravin Gagare, Mohammad Noshi
  • Publication number: 20140271476
    Abstract: The present disclosure relates to compounds that are useful as near-infrared fluorescence probes, wherein the compounds include i) a pteroyl ligand that binds to a target receptor protein, ii) a dye molecule, and iii) a linker molecule that comprises an amino acid or derivative thereof. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: Purdue Research Foundation
    Inventors: Sumith A. Kularatne, Sakkarapalayam M. Mahalingam, Philip S. Low
  • Publication number: 20140249154
    Abstract: Pharmaceutical compositions of the invention are presented which comprise substituted aminothiazoles derivatives. The substituted aminothiazoles derivatives have a disease-modifying action in the treatment of diseases associated with unregulated cell growth. Such diseases include cancers such as hepatocellular carcinoma, and viral infections from a hepatitis virus.
    Type: Application
    Filed: October 4, 2012
    Publication date: September 4, 2014
    Inventors: Andrea Cuconati, Xiaodong Xu, Timothy M. Block
  • Patent number: 8809527
    Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: August 19, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Manoj C. Desai, Randall L. Halcomb, Paul Hrvatin, Hon Chung Hui, Ryan McFadden, Paul A. Roethle, Hong Yang
  • Publication number: 20140187559
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Application
    Filed: December 26, 2013
    Publication date: July 3, 2014
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventor: Chandrasekhar V. Miduturu
  • Publication number: 20140179761
    Abstract: The present invention provides targeting lipids of structure L100-linker-L101??(CI), where L100 is a lipid, lipophile, alkyl, alkenyl or alkynyl, L101 is a ligand or —CH2CH2(OCH2CH2)pO(CH2)qCH2-ligand, p is 1-1000, and q is 1-20. In addition, the invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo.
    Type: Application
    Filed: October 22, 2013
    Publication date: June 26, 2014
    Applicant: Tekmira Pharmaceuticals Corporation
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Jayaprakash K. Narayanannair, Muthusamy Jayaraman
  • Patent number: 8754212
    Abstract: A process for the preparation of the stable, amorphous calcium salt of (6S)—N(5)-methyl-5,6,7,8-tetrahydrofolic acid of the formula V, and a stable, amorphous calcium salt of (6S)—N(5)-methyl-5,6,7,8-tetrahydrofolic acid of the formula V are provided.
    Type: Grant
    Filed: August 14, 2012
    Date of Patent: June 17, 2014
    Assignee: Cerbios-Pharma S.A.
    Inventors: Raffella Manzotti, Moreno Morosoli
  • Publication number: 20140148433
    Abstract: The present application relates to novel bicyclic azaheterocycles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: August 31, 2011
    Publication date: May 29, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Lars Bärfacker, Stefan Weigand
  • Publication number: 20140121185
    Abstract: Novel compounds and pharmaceutical compositions thereof for the treatment and/or prevention of cancer and precancerous conditions, inflammation-related disorders, pain and fever.
    Type: Application
    Filed: September 23, 2013
    Publication date: May 1, 2014
    Applicant: MEDICON PHARMACEUTICALS, INC.
    Inventor: Basil RIGAS
  • Patent number: 8691822
    Abstract: Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.
    Type: Grant
    Filed: September 14, 2010
    Date of Patent: April 8, 2014
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Peng Cho Tang, Nong Zhang, Baolei Zhang, Weimin Wang, Hao Zheng, Lin Wu
  • Publication number: 20140088100
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Application
    Filed: July 11, 2013
    Publication date: March 27, 2014
    Applicant: BLUEPRINT MEDICINES
    Inventors: Neil Bifulco, JR., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu
  • Publication number: 20140081022
    Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
    Type: Application
    Filed: November 25, 2013
    Publication date: March 20, 2014
    Inventors: Manoj C. Desai, Randall L. Halcomb, Paul Hrvatin, Hon Chung Hui, Ryan McFadden, Paul A. Roethle, Hong Yang
  • Publication number: 20140073761
    Abstract: Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and/or treating diseases and disease states caused by pathogenic cell populations.
    Type: Application
    Filed: March 5, 2013
    Publication date: March 13, 2014
    Applicant: ENDOCYTE, INC.
    Inventor: ENDOCYTE, INC.
  • Patent number: 8669258
    Abstract: Embodiments of the invention are directed to the treatment of gastroparesis by administering sepiapterin.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: March 11, 2014
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Pankaj J. Pasricha, Pandu R. R. Gangula
  • Publication number: 20140058063
    Abstract: The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.
    Type: Application
    Filed: March 5, 2013
    Publication date: February 27, 2014
    Applicant: ENDOCYTE, INC.
    Inventors: Iontcho R. Vlahov, Christopher P. Leamon, Matthew A. Parker, Stephen J. Howard, Hari Krishna R. Santhapuram, Apparao Satyam, Joseph A. Reddy
  • Publication number: 20140050775
    Abstract: Disclosed are compounds, compositions and methods for systemic and local delivery of biologically active molecules.
    Type: Application
    Filed: March 8, 2013
    Publication date: February 20, 2014
    Applicant: Egen, Inc.
    Inventors: Gregory Slobodkin, Richard Congo, Majed Matar, Jason Fewell, Khursheed Anwer, Brian Jeffery Sparks
  • Patent number: 8633202
    Abstract: The present invention relates to stable crystalline (6S)—N(5)-formyl-5,6,7,8-tetrahydrofolic acid, commonly referred to as levofolinic acid, in essentially pure 6S diastereomeric form, and to a process for its preparation.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: January 21, 2014
    Assignee: GMT Fine Chemicals SA
    Inventor: Pascal Jequier
  • Patent number: 8629142
    Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: January 14, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Manoj C. Desai, Randall L. Halcomb, Paul Hrvatin, Hon Chung Hui, Ryan McFadden, Paul A. Roethle, Hong Yang
  • Patent number: 8618106
    Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: December 31, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steve Durrant