Ring Nitrogen In The Polycyclo Ring System Patents (Class 546/200)
  • Patent number: 10626101
    Abstract: Solid forms comprising 2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed.
    Type: Grant
    Filed: December 11, 2018
    Date of Patent: April 21, 2020
    Assignee: Celgene Corporation
    Inventors: Ying Li, Hon-Wah Man
  • Patent number: 10590104
    Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.
    Type: Grant
    Filed: November 26, 2018
    Date of Patent: March 17, 2020
    Assignee: Celgene Corporation
    Inventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller
  • Patent number: 10040778
    Abstract: Anhydrous polymorphic form-I of anti cancer drug, Lenalidomide whose chemical name is 3-(4-amino-1-oxo-1,3-dihydro-isoindole-2-yl)-piperidine-2,6-dione, is disclosed. Alternate methods for making anhydrous polymorphic form-I of Lenalidomide are also disclosed.
    Type: Grant
    Filed: July 8, 2015
    Date of Patent: August 7, 2018
    Assignee: NATCO PHARMA LIMITED
    Inventors: Durga Prasad Konakanchi, Buchappa Gongalla, Kotayya Babu Sikha, Chandrasekar Kandaswamy, Kali Satya Bhujanga Rao Adibhatla, Venkaiah Chowdary Nannapaneni
  • Patent number: 9808450
    Abstract: Provided herein are solid forms comprising (a) 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione (Lenalidomide) and (b) a coformer. Pharmaceutical compositions comprising the solid forms and methods for treating, preventing and managing various disorders are also disclosed.
    Type: Grant
    Filed: March 25, 2014
    Date of Patent: November 7, 2017
    Assignee: Celgene Corporation
    Inventors: G. Patrick Stahly, David Jonaitis, Ho-Wah Hui, Kevin J. Klopfer
  • Patent number: 9278931
    Abstract: The present invention provides a compound having a lysine-specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for cancer, and central nervous system diseases, and the like.
    Type: Grant
    Filed: August 8, 2012
    Date of Patent: March 8, 2016
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Naoki Tomita, Shigeo Kajii, Douglas Robert Cary, Daisuke Tomita, Shinichi Imamura, Ken Tsuchida, Satoru Matsuda, Ryujiro Hara, Yusuke Tominari
  • Patent number: 9101620
    Abstract: The present invention provides polymorph of 3-(4-amino-1-oxo-1,3-dihydro-2H-isoindole-2-yl)-piperidine-2,6-dione, and also the preparing methods and pharmaceutical compositions thereof.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: August 11, 2015
    Assignee: Nanjing Cavendish Bio-Engineering Technology Co., Ltd.
    Inventors: Rong Yan, Hao Yang, Yongxiang Xu
  • Publication number: 20150141652
    Abstract: The present invention relates to an improved process for preparing 2-[(2E)-2-fluoro-2-(3-piperidinylidene)ethyl]-1H-isoindole-1,3(2H)-dione, or a salt thereof, which is an intermediate in the synthesis route of the antibacterial compound 7-[(3E)-3-(2-amino-1-fluoroethylidene)-1-piperidinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxo 3-quinolinecarboxylic acid.
    Type: Application
    Filed: September 28, 2012
    Publication date: May 21, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Yolande Lydia Lang, Dominique Paul, Michel Depre
  • Patent number: 9023868
    Abstract: The present application describes deuterium-enriched lenalidomide, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Grant
    Filed: January 24, 2014
    Date of Patent: May 5, 2015
    Assignee: Deuteria Pharmaceuticals, Inc.
    Inventor: Anthony W. Czarnik
  • Publication number: 20150105552
    Abstract: This invention provides enantioenriched heterocyclic enaminone compounds with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): comprising treating a compound of formula (II): with a transition metal catalyst under alkylation conditions.
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Inventors: Brian M. Stoltz, Dennis A. Dougherty, Douglas Duquette, Noah Duffy
  • Publication number: 20150094473
    Abstract: Solid forms comprising crystalline 3-(4-nitro-1-oxoisoindolin-2-yl)piperidine-2,6-dione are disclosed. Compositions comprising the solid forms, methods of making the solid forms and methods of their use are also disclosed.
    Type: Application
    Filed: February 20, 2013
    Publication date: April 2, 2015
    Inventors: Ying Li, Jean Xu, Kevin J. Klopfer
  • Publication number: 20150064623
    Abstract: A novel compound having satisfactory sensitivity (base generating performance), a photosensitive resin composition containing the compound as a photo-initiator, and a cured product of the composition are provided. Specifically, a compound represented by general formula (1) (compound (1)), a photosensitive resin composition containing (A) a photo-initiator including at least one compound (1) and (B) a photosensitive resin are provided. Preferred are the compound (1) in which R1 is an unsubstituted or substituted C6-C20 aromatic hydrocarbon group, the compound (1) in which at least one of R5, R6, R7, R8, R9, R10, and R11 is nitro, and the compound (1) in which n is 0. The symbols in general formula (1) are as defined in the description.
    Type: Application
    Filed: March 5, 2013
    Publication date: March 5, 2015
    Inventors: Takeo Oishi, Koichi Kimijima, Nobuhide Tominaga, Hirokatsu Shinano, Daisuke Sawamoto
  • Publication number: 20150065498
    Abstract: The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: May 11, 2012
    Publication date: March 5, 2015
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Zhi-Qiang Yang, Youheng Shu, Daniel Pitts
  • Patent number: 8962835
    Abstract: Certain imidazopyrazines of Formula (I): or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: February 24, 2015
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford
  • Publication number: 20150045362
    Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.
    Type: Application
    Filed: August 25, 2014
    Publication date: February 12, 2015
    Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford
  • Patent number: 8952166
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: July 25, 2013
    Date of Patent: February 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Fa-Xiang Ding, Shuzhi Dong, Jessica Frie, Xin Gu, Jinlong Jiang, Alexander Pasternak, Haifeng Tang, Zhicai Wu, Yang Yu, Takao Suzuki
  • Publication number: 20150025089
    Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.
    Type: Application
    Filed: October 6, 2014
    Publication date: January 22, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Waldemar PFRENGLE, Thorsten PACHUR, Thomas NICOLA, Adil DURAN
  • Patent number: 8933095
    Abstract: Compounds of Formula I: wherein X, Y, Z, R1, R2, R3, R4 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.
    Type: Grant
    Filed: October 31, 2013
    Date of Patent: January 13, 2015
    Assignee: Pfizer Inc.
    Inventors: Amy Beth Dounay, Laura Ann McAllister, Vinod Dipak Parikh, Suobao Rong, Patrick Robert Verhoest
  • Patent number: 8927725
    Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein A, B and D are each oxygen or sulfur, provided that least one of A, B and D is sulfur; and R1-R8 are each independently hydrogen, hydroxyl, acyl, substituted acyl, acyloxy, substituted acyloxy, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryl, substituted aryl, amino, substituted amino, halogen, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, substituted heteroaryl, or a thio-containing group.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: January 6, 2015
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Nigel H. Greig, Weiming Luo, David Tweedie, Harold W. Holloway, Qian-Sheng Yu, Edward J. Goetzl
  • Publication number: 20150005303
    Abstract: This invention relates to 5-substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Application
    Filed: September 18, 2014
    Publication date: January 1, 2015
    Inventors: George W. MULLER, Roger Shen-Chu CHEN, Alexander L. RUCHELMAN
  • Publication number: 20140364615
    Abstract: An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.
    Type: Application
    Filed: June 9, 2014
    Publication date: December 11, 2014
    Applicant: GE HEALTHCARE LIMITED
    Inventors: HARRY JOHN WADSWORTH, DENNIS O'SHEA, JOANNA PASSMORE, WILLIAM TRIGG, AMANDA EWAN, BO SHAN
  • Publication number: 20140315889
    Abstract: The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 23, 2014
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: Yuntae Kim, Changsik Lee, Hyun-mo Yang, Hojin Choi, Jaeki Min, Soyoung Kim, Dal-Hyun Kim, Nina Ha, Jung-Min Kim, Hyojin Lim, Eunhee Ko
  • Publication number: 20140296229
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4, A1 and A2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Application
    Filed: March 26, 2014
    Publication date: October 2, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Harald ENGELHARDT, Davide GIANNI, Andreas MANTOULIDIS, Christian SMETHURST
  • Publication number: 20140296291
    Abstract: The invention relates to novel crystalline forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione, including a novel urea cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel gallic acid cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel propyl gallate cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; and a novel L-tartaric acid cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione. The preparation and characterization of the novel crystalline forms according to various embodiments of the invention are described. The invention also relates to pharmaceutical compositions containing the novel crystalline forms, and the therapeutic use of the novel crystalline forms.
    Type: Application
    Filed: June 7, 2012
    Publication date: October 2, 2014
    Inventors: Scott L. Childs, Shreenivas R. Lingireddy, Nathan Barishansky
  • Publication number: 20140288300
    Abstract: Disclosed is a drug-fluorophore complex for specific detection of tumor cells. Specifically, the drug-fluorophore complex includes a tumor cell-targeting drug penetrating tumor cells and non-tumor cells at different rates or levels, and a fluorescent substance chemically bonded to the tumor cell-targeting drug. The drug-fluorophore complex enables specific imaging of tumor cells only with high accuracy in a very simple manner without causing cytotoxicity.
    Type: Application
    Filed: July 8, 2013
    Publication date: September 25, 2014
    Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Kwang Meyung KIM, Ick Chan KWON, Sang Yoon KIM, Ju Hee RYU, Eun Sung JUN, In San KIM
  • Patent number: 8841325
    Abstract: Provided herein are methods of restoring vitamin D sensitivity in tumor cells that are vitamin D resistant. Also provided are methods of treating, preventing or managing cancer using an immunomodulatory compound in combination with a vitamin D agent. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods provided herein are also disclosed.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: September 23, 2014
    Assignee: Celgene Corporation
    Inventors: Carole Brosseau, Justin Blake Bartlett, Angus George Dalgleish, Kay Winifred Colston, Christine Galustian
  • Publication number: 20140275114
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ralf ANDERSKEWITZ, Marc GRUNDL, Gerd MORSCHHAEUSER, Thorsten OOST, Alexander PAUTSCH
  • Publication number: 20140256950
    Abstract: The present invention provides new processes for the preparation of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds which are useful, for example, for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-?. The invention can provide improved and/or efficient processes for the commercial production of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds, including, but not limited to, unsubstituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione.
    Type: Application
    Filed: April 29, 2014
    Publication date: September 11, 2014
    Applicant: Celgene Corporation
    Inventors: Chuansheng Ge, George W. Muller, Roger Chen, Manohar Tukaram Saindane
  • Publication number: 20140256700
    Abstract: The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: February 26, 2014
    Publication date: September 11, 2014
    Inventors: Michael A. Poss, David R. Tortolani, Dharmpal S. Dodd, Christopher P. Mussari, John S. Tokarski, Ashvinikumar V. Gavai, Yufen Zhao, George V. Delucca, Daniel O'Malley, Derek J. Norris, Patrice Gill, Claude A. Quesnelle, Wen-Ching Han
  • Patent number: 8802675
    Abstract: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.
    Type: Grant
    Filed: January 31, 2010
    Date of Patent: August 12, 2014
    Assignees: Technion Research and Development Foundation Ltd, Yeda Research and Development Company Ltd.
    Inventors: Moussa B. H. Youdim, Mati Fridkin, Hailin Zheng
  • Publication number: 20140221427
    Abstract: Provided herein are pomalidomide, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.
    Type: Application
    Filed: June 20, 2012
    Publication date: August 7, 2014
    Applicant: CELGENE CORPORATION
    Inventors: George W. Muller, Hon-Wah Man
  • Publication number: 20140187584
    Abstract: Substituted 2-(2,6-dioxopiperidin-3-yl)phthalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl)isoindolines are disclosed. The compounds are useful, for example, in reducing the levels of TNF? in a mammal.
    Type: Application
    Filed: January 15, 2014
    Publication date: July 3, 2014
    Applicant: Celgene Corporation
    Inventors: George W. MULLER, David I STIRLING, Roger Shen-Chu CHEN
  • Patent number: 8765738
    Abstract: Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: July 1, 2014
    Assignee: Incuron, LLC
    Inventors: John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
  • Patent number: 8754107
    Abstract: The present invention is directed to novel aminopyrrolidines of formula I pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined herein. The compounds of formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: June 17, 2014
    Assignee: AbbVie Inc.
    Inventors: Dawn M. George, Richard W. Dixon, Michael Friedman, Adrian D. Hobson, Biqin Li, Lu Wang, Xiaoyun Wu, Neil Wishart
  • Publication number: 20140142141
    Abstract: The present application describes deuterium-enriched lenalidomide, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: January 24, 2014
    Publication date: May 22, 2014
    Applicant: DEUTERIA PHARMACEUTICALS, INC.
    Inventor: Anthony W. CZARNIK
  • Patent number: 8722905
    Abstract: Disclosed is a dye, having a chemical formula: wherein each R1 is independently selected from hydrogen, —(CxH2x+1), —(CyH2y)—S—(CxH2x+1), or —(CyH2y)—N(CxH2x+1)2; Ar1 is wherein each R2 is independently selected from —(CxH2x+1), —(CxH2x)—S—(CxH2x+1), or (CxH2x)—N(CxH2x+1)2; Ar2 is wherein each R3 is independently selected from hydrogen, —(CxH2x+1), —(CyH2y)—S—(CxH2x+1), or —(CyH2y)—N(CxH2x+1)2; X is sulfur, oxygen, selenium, or N—R4, and R4 is —(CxH2x+1); m is in integer of 1 to 4; x is an integer of 1 to 20; and y is an integer of 0 to 20. The dye can be applied to a photoelectric conversion device.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: May 13, 2014
    Assignee: Industrial Technology Research Institute
    Inventors: Yao-Shan Wu, Yung-Liang Tung, Jen-An Chen, Chun-Guey Wu, Jheng-Ying Li
  • Patent number: 8716292
    Abstract: The present invention relates to riminophenazines having heteroaromatic substitutions, including those with 2-heteroaryl-amino substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments. A general representation of the 2-(heteroaryl)amino-riminophenazines is shown below.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: May 6, 2014
    Assignee: Global Alliance for TB Drug Development
    Inventors: Kai Liu, Christopher B. Cooper, Haihong Huang, Chun Li, Binna Liu, Yang Liu, Zhenkun Ma, Jingbin Wang, Dali Yin, Dongfeng Zhang, Gang Zhang, Hao Zhang
  • Patent number: 8716314
    Abstract: Provided herein are thalidomide, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: May 6, 2014
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man
  • Publication number: 20140121245
    Abstract: Anhydrous polymorphic form-I of anti cancer drug, Lenalidomide whose chemical name is 3-(4-amino-1-oxo-1,3-dihydro-isoindole-2-yl)-piperidine-2,6-dione, is disclosed. Alternate methods for making anhydrous polymorphic form-I of Lenalidomide are also disclosed.
    Type: Application
    Filed: January 9, 2014
    Publication date: May 1, 2014
    Applicant: Natco Pharma Limited
    Inventors: Durga Prasad Konakanchi, Buchappa Gongalla, Kotayya Babu Sikha, Chandrasekar Kandaswamy, Kali Satya Bhujanga Rao Adibhatla, Venkaiah Chowdary Nannapaneni
  • Publication number: 20140113890
    Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.
    Type: Application
    Filed: December 23, 2013
    Publication date: April 24, 2014
    Applicant: ACHILLION PHARMACEUTICALS, INC.
    Inventors: Avinash Phadke, Dawei Chen, Venkat Gadhachanda, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Atul Agarwal, Ha Young Kim, Shuoming Li, Cuixian Liu, Suoming Zhang, Milind Deshpande
  • Publication number: 20140113935
    Abstract: This invention relates to N-methylaminomethyl-isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Application
    Filed: December 30, 2013
    Publication date: April 24, 2014
    Applicant: Celgene Corporation
    Inventors: George W. MULLER, Roger Shen-Chu Chen
  • Patent number: 8697877
    Abstract: The present invention relates to novel oxyindole derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the motilin receptor (GPR38).
    Type: Grant
    Filed: March 1, 2010
    Date of Patent: April 15, 2014
    Assignee: RaQualia Pharma Inc.
    Inventors: Masaki Sudo, Yasuhiro Iwata, Yoshimasa Arano, Madoka Jinno, Masashi Ohmi, Hirohide Noguchi
  • Patent number: 8686153
    Abstract: The present invention relates to acid addition salts of lenalidomide, wherein said acid has a pKa lower than 1, preferably selected from hydrochloric acid, hydrobromic acid, methane sulfonic acid, ethane sulfonic acid, benzene sulfonic acid and p-toluenesulfonic acid, to processes for their making, and use in medicine, and to purification of lenalidomide base.
    Type: Grant
    Filed: August 12, 2009
    Date of Patent: April 1, 2014
    Assignee: Synthon B.V.
    Inventor: Jacobus Theodorus Henricus Van Eupen
  • Publication number: 20140073669
    Abstract: Provided are 4?-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Application
    Filed: November 18, 2013
    Publication date: March 13, 2014
    Inventors: Alexander L. RUCHELMAN, George W. Muller, Hon-Wah Man, Roger Shen-Chu Chen
  • Patent number: 8669276
    Abstract: The present application describes deuterium-enriched lenalidomide, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Grant
    Filed: September 9, 2012
    Date of Patent: March 11, 2014
    Assignee: Deuteria Pharmaceuticals, Inc.
    Inventor: Anthony W. Czarnik
  • Patent number: 8648067
    Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: February 11, 2014
    Assignees: Cephalon, Inc., Teva Sante
    Inventors: Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek D. Dunn, Greg A. Hostetler, Robert L. Hudkins, Brigitte Lesur, Babu G. Sundar, Allison L. Zulli, Christophe Yue
  • Patent number: 8642772
    Abstract: Piperidine compounds and pharmaceutically useful salts thereof, a pharmaceutical composition including an effective amount of the racemic or enantiomerically enriched piperidine compounds to treat gastrointestinal diseases, and a method of treating gastrointestinal diseases in a mammal are provided.
    Type: Grant
    Filed: October 9, 2009
    Date of Patent: February 4, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Coo-Min Chung, Hyung-Jin Jun, Jin-Sung Kim, Hui-Ho Kim, Hye-Kyung Min, Yong-Gil Kim, Jong-Gil Choi, Hongwook Kim
  • Publication number: 20130274291
    Abstract: The present application describes 3?-deutero-pomalidomide, deuterated derivatives thereof, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: June 10, 2013
    Publication date: October 17, 2013
    Inventor: Sheila DEWITT
  • Publication number: 20130245067
    Abstract: The present application describes deuterium-enriched lenalidomide, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: September 9, 2012
    Publication date: September 19, 2013
    Applicant: DEUTERIA PHARMACEUTICALS, INC.
    Inventor: Anthony W. Czarnik
  • Patent number: 8518972
    Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: August 27, 2013
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
  • Patent number: 8513285
    Abstract: There are disclosed racemic or enantiomerically enriched 3- or 4-substituted piperidine compounds represented by the following structural formula (I): or any of their isomers, or pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions containing the subject compounds. The subject compounds are useful for the treatment of diseases of the central nervous system, particularly depression, anxiety and pain disorder.
    Type: Grant
    Filed: January 19, 2012
    Date of Patent: August 20, 2013
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Ki-Ho Lee, Chun-Eung Park, Kyung-Hyan Min, Yong-Je Shin, Yu-Jin Shin, Hae-Jeong Yoon, Won Kim, Eun-Ju Ryu