Bicyclo Ring System Which Is Indole (including Hydrogenated) Patents (Class 546/201)
  • Patent number: 10392364
    Abstract: Disclosed herein is an improved process for preparation of Lenalidomide and crystalline polymorphic forms thereof.
    Type: Grant
    Filed: August 11, 2015
    Date of Patent: August 27, 2019
    Assignee: AVRA LABORATORIES PVT. LTD.
    Inventors: Ramakrishna Rao, Ramadevi Nandipati, Ravi Gooda, Mukesh Padmakar Shewalkar, Venkat Vasantrao Bhadke
  • Patent number: 10300105
    Abstract: The present invention relates to particulate forms of anamorelin monohydrochloride or a composition comprising anamorelin monohydrochloride having controlled chloride content, preferably isolated in an amorphous and/or fine particulate state, processes for making the particulate forms, and pharmaceutical compositions comprising the particulate forms.
    Type: Grant
    Filed: April 26, 2018
    Date of Patent: May 28, 2019
    Assignees: ONO PHARMACEUTICAL CO., LTD, HELSINN HEALTHCARE SA
    Inventors: Shin-itsu Kuwabe, Takehiko Yanagimachi, Hideyuki Yoshiyama, Seemon Pines, Eleanor de Groot, Silvina Garcia Rubio, Peter Manini
  • Patent number: 10246414
    Abstract: The present invention relates to novel heterocyclic derivatives which are allosteric modulators of cannabinoid receptor 1 (CB1) and which are useful for the treatment or prevention of neurological and psychiatric disorders associated with endocannabinoid dysfunction and diseases in which the CB1 subtype of cannabinoid receptor is involved; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.
    Type: Grant
    Filed: January 26, 2017
    Date of Patent: April 2, 2019
    Assignee: Northeastern University
    Inventors: Ganeshsingh A. Thakur, Pushkar M. Kulkarni
  • Patent number: 10239909
    Abstract: The present disclosure relates to new compounds and their use as fluorescent labels. The compounds may be used as fluorescent labels for nucleotides in nucleic acid sequencing applications. The labels are advantageous due to their long Stokes shifts.
    Type: Grant
    Filed: May 23, 2016
    Date of Patent: March 26, 2019
    Assignee: Illumina Cambridge Limited
    Inventors: Nikolai Romanov, Xiaolin Wu
  • Patent number: 10047068
    Abstract: The problem addressed by the present invention is to provide a novel method for separating and purifying pure enantiomer of lenalidomide. Pure enantiomer of lenalidomide can be separated and purified by using, as the mobile phase, an organic solvent selected from the group consisting of aprotic solvents, secondary alcohols, and mixtures thereof.
    Type: Grant
    Filed: May 21, 2015
    Date of Patent: August 14, 2018
    Assignee: Shiseido Company, Ltd.
    Inventors: Yosuke Tojo, Masashi Mita, Wolfgang Lindner
  • Patent number: 10017492
    Abstract: Provided are an isoindoline derivative, intermediate, preparation method, pharmaceutical composition and use thereof. The isoindoline derivative and the pharmaceutical composition thereof can regulate the production or activity of immunological cytokines, thus effectively treating cancer and inflammatory disease.
    Type: Grant
    Filed: August 27, 2015
    Date of Patent: July 10, 2018
    Assignee: KANGPU BIOPHARMACEUTICALS, LTD.
    Inventors: Chuansheng Ge, Wen-Cherng Lee, Baisong Liao, Lei Zhang
  • Patent number: 9981002
    Abstract: The present invention relates to particulate forms of anamorelin monohydrochloride or a composition comprising anamorelin monohydrochloride having controlled chloride content, preferably isolated in an amorphous and/or fine particulate state, processes for making the particulate forms, and pharmaceutical compositions comprising the particulate forms.
    Type: Grant
    Filed: April 21, 2016
    Date of Patent: May 29, 2018
    Assignees: HELSINN HEALTHCARE SA, ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shin-itsu Kuwabe, Takehiko Yanagimachi, Hideyuki Yoshiyama, Seemon Pines, Eleanor de Groot, Silvina Garcia Rubio, Peter Manini
  • Patent number: 9956261
    Abstract: The present invention relates to particulate forms of anamorelin monohydrochloride or a composition comprising anamorelin monohydrochloride having controlled chloride content, preferably isolated in an amorphous and/or fine particulate state, processes for making the particulate forms, and pharmaceutical compositions comprising the particulate forms.
    Type: Grant
    Filed: April 21, 2016
    Date of Patent: May 1, 2018
    Assignees: HELSINN HEALTHCARE SA, ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shin-itsu Kuwabe, Takehiko Yanagimachi, Hideyuki Yoshiyama, Seemon Pines, Eleanor De Groot, Silvina Garcia Rubio, Peter Manini
  • Patent number: 9872883
    Abstract: The present invention relates to particulate forms of anamorelin monohydrochloride or a composition comprising anamorelin monohydrochloride having controlled chloride content, preferably isolated in an amorphous and/or fine particulate state, processes for making the particulate forms, and pharmaceutical compositions comprising the particulate forms.
    Type: Grant
    Filed: April 21, 2016
    Date of Patent: January 23, 2018
    Assignees: HELSINN HEALTHCARE SA, ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shin-itsu Kuwabe, Takehiko Yanagimachi, Hideyuki Yoshiyama, Seemon Pines, Eleanor De Groot, Silvina Garcia Rubio, Peter Manini
  • Patent number: 9643950
    Abstract: The invention in one embodiment is directed to solid forms of {S-3-(4-Amino-1-oxo-isoindolin-2-yl)(piperidine-3,4,4,5,5-d5)-2,6-dione}, including an anhydrous crystalline form, two hydrates, and an amorphous form. The invention in one embodiment is directed to methods of preparation of the solid forms.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: May 9, 2017
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Joanna A. Bis, David H. Igo
  • Patent number: 9567339
    Abstract: The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Grant
    Filed: June 26, 2014
    Date of Patent: February 14, 2017
    Assignee: AbbVie Inc.
    Inventors: Dominique Bonafoux, Heather M. Davis, Kristine E. Frank, Michael M. Friedman, J. Martin Herold, Michael Z. Hoemann, Raymond Huntley, Augustine Osuma, George Sheppard, Gagandeep K. Somal, Jennifer Van Camp, Stacy A. Van Epps, Anil Vasudevan, Grier A. Wallace, Lu Wang, Lu Wang, Zhi Wang, Noel S. Wilson, Xiangdong Xu
  • Patent number: 9522899
    Abstract: The present invention discloses methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2,6-dioxopiperidine and intermediates thereof, namely, the synthesis of compounds of the Formula (I), with each substitutional group defined in the patent specification. Owing to the advantages of high productivity, little influence to the environment and material accessibility, the methods of the present invention is suitable for industrial production.
    Type: Grant
    Filed: June 15, 2015
    Date of Patent: December 20, 2016
    Assignees: NANJIAN CAVENDISH BIO-ENGINEERING TECHNOLOGY CO., LTD
    Inventors: Rong Yan, Hao Yang, Yongxiang Xu
  • Patent number: 9216966
    Abstract: The present disclosure relates to novel indole and tetrahydroindole core compounds useful for the treatment of disorders associated with a defect in vesicular transport (e.g., axonal transport).
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: December 22, 2015
    Inventor: John Manfredi
  • Patent number: 9045482
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: June 2, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
  • Publication number: 20150139905
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 21, 2015
    Inventors: Dinesh Chimmanamada, Weiwen Ying
  • Publication number: 20150133659
    Abstract: The present invention relates to millepachine ((E)-1-(5-methoxy-2,2-dimethyl-2H-chromen-8-yl)-3-(4-methoxyphenyl)prop-2-en-1-one) and its analogues. The present invention provides methods for preparing these compounds, pharmaceutical compositions including these compounds, and methods of treating diseases utilizing pharmaceutical compositions including these compounds.
    Type: Application
    Filed: May 25, 2012
    Publication date: May 14, 2015
    Applicant: Sichuan University
    Inventors: Lijuan Chen, Yuquan Wei
  • Publication number: 20150133422
    Abstract: The present invention embodiments relate to compound of Formula I or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates in certain embodiments to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates in certain embodiments to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates in certain embodiments to a process for manufacturing compounds of Formula I.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 14, 2015
    Inventors: Stefano Crosignani, Sandra Cauwenberghs, Frederik Deroose
  • Patent number: 9029548
    Abstract: The invention relates to fatty acid lenalidomide derivatives; compositions comprising an effective amount of a fatty acid lenalidomide derivative; and methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid lenalidomide derivative.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: May 12, 2015
    Assignee: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu, Amal Ting
  • Patent number: 9018231
    Abstract: The present invention relates to novel sulfone compounds as 5-HT6 receptor ligands of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. These compounds are useful in the treatment/prevention of various disorders that are related to 5-HT6 receptor functions.
    Type: Grant
    Filed: March 24, 2010
    Date of Patent: April 28, 2015
    Assignee: Suven Life Sciences Limited
    Inventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Rama Sastri Kambhampati, Rajesh Kumar Badange, Veena Reballi, Anil Kashinath Chindhe, Rambabu Namala, Mohamad Sadik Abdulhamid Mulla, Ishtiyaque Ahmad, Renny Abraham, Venkateswarlu Jasti
  • Publication number: 20150112067
    Abstract: The disclosure encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, having less steps and improved yields as compared to previous synthetic methods for making these compounds, which are CGRP receptor antagonists, useful for the treatment of migraine. Conditions for an amide bond formation between an acid and amine include for example reacting the compounds of Formulae B (after salt break) and C with an amide coupling reagent and optionally an additive and an acid and/or a base in a non-reactive solvent.
    Type: Application
    Filed: March 13, 2013
    Publication date: April 23, 2015
    Inventors: Frank Chen, Carmela Molinaro, W. Peter Wuelfing, Nobuyushi Yasuda, Jianguo Yin, Yong-Li Zhong, Joseph Lynch, Teresa Andreani
  • Patent number: 9006276
    Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: April 14, 2015
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
  • Patent number: 9006268
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Grant
    Filed: June 6, 2011
    Date of Patent: April 14, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John S. Debenham, Jinlong Jiang, Christina B. Madsen-Duggan, Dong-Ming Shen
  • Publication number: 20150099709
    Abstract: The present invention relates to a use of a compound having ghrelin receptor agonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for treatment of diseases including achlorhydria in which abnormal gastric acid secretion is involved. In addition, the present invention relates to the method of treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agents. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound of the present invention or a pharmaceutically acceptable salt thereof for the treatment of said diseases.
    Type: Application
    Filed: May 27, 2013
    Publication date: April 9, 2015
    Inventors: Nobuyuki Takahashi, Masaki Sudo, Kaoru Shimada, Hiroaki Wakabayashi
  • Publication number: 20150099746
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 9, 2015
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
  • Patent number: 9000175
    Abstract: The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I).
    Type: Grant
    Filed: November 24, 2011
    Date of Patent: April 7, 2015
    Assignee: Lupin Limited
    Inventors: Rajesh Thotapally, Onkar Gangaram Kachi, Atish Harishchandra Rodge, Ashok Bhau Pathak, Bhavana Shrirang Kardile, Milind Dattatraya Sindkhedkar, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 8999994
    Abstract: The present invention relates to a compound of formula (I): wherein: R1 and R2 are selected from among H and C1-C10 alkyl; R3 is selected from among H, —OR4, N, —CN, —C(O)R4, —C(O)OR4, —C(O)NR4R5, —C?NR4, —OC(O)R4, —NR4R5, —NR4C(O)R5, —NO2, —N?CR4R5, halogen and C1-C10 alkyl, wherein R4 and R5 are selected from among H, alkyl, alkenyl, cycloalkyl and aryl; X, Y, Z1, Z2 and Z3 are selected independently from among CH and N; A is selected from among (CH2)n, NH, O and CO, wherein n is an integer between 1 and 6, to the procedure for the obtainment of said compounds, to a pharmaceutical composition comprising said compound, and to the use thereof in the treatment of a neurodegenerative disease, more particularly treatment of Alzheimer's or Parkinson's disease.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: April 7, 2015
    Assignees: Consejo Superior de Investigaciones Cientificas, Universitat Autonoma de Barcelona, Universidad de Barcelona
    Inventors: Abdelouahid Samadi, José Luis Marco Contelles, Irene Bolea Tomás, Francisco Javier Luque Garriga, Mercedes Unzeta López
  • Patent number: 9000005
    Abstract: The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: April 7, 2015
    Assignee: ArQule, Inc.
    Inventors: Yoshitaka Nakamura, Jo Ooyama
  • Publication number: 20150090936
    Abstract: Provided herein are heptamethine cyanine dyes having a large Stokes shift, and the salts and conjugates thereof. Also provided are methods of using and making such large Stokes shift dyes as fluorescence resonance energy transfer (FRET) acceptors or donors.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 2, 2015
    Inventors: Yi-Zhen HU, Hee Chol KANG
  • Publication number: 20150087628
    Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
    Type: Application
    Filed: April 10, 2013
    Publication date: March 26, 2015
    Inventors: Jonathan Ostrem, Ulf Peters, Kevan M. Shokat
  • Publication number: 20150072934
    Abstract: The present invention relates to particulate forms of anamorelin monohydrochloride or a composition comprising anamorelin monohydrochloride having controlled chloride content, preferably isolated in an amorphous and/or fine particulate state, processes for making the particulate forms, and pharmaceutical compositions comprising the particulate forms.
    Type: Application
    Filed: November 12, 2014
    Publication date: March 12, 2015
    Applicants: Ono Pharmaceutical Co., Ltd., Helsinn Healthcare SA
    Inventors: Shin-itsu Kuwabe, Takehiko Yanagimachi, Hideyuki Yoshiyama, Marcia Philipson, Eleanor De Groot, Silvina Garcia Rubio, Peter Manini
  • Publication number: 20150057248
    Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.
    Type: Application
    Filed: September 1, 2014
    Publication date: February 26, 2015
    Applicant: The Board of Regents of The University of Texas System
    Inventors: Jia Zhou, Haijun Chen, Kenneth M. Johnson, Cheng Z. Wang
  • Patent number: 8946265
    Abstract: The present invention relates to improved processes for preparing 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione (I) (lenalidomide) and its intermediate 3-(1-oxo-4-nitro-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione. The present invention further relates to improved processes for preparing lenalidomide crystalline form A, use of said crystalline form A as an active pharmaceutical ingredient or as an intermediate in the preparation of further crystalline or amorphous forms of lenalidomide, compositions comprising lenalidomide crystalline form A and their use in the treatment of disease.
    Type: Grant
    Filed: March 1, 2010
    Date of Patent: February 3, 2015
    Assignee: Generics [UK] Limited
    Inventors: Vinayak Govind Gore, Vinay Kumar Shukla, Shreyas Shrikant Bhandari, Suresh Hasbe
  • Patent number: 8940784
    Abstract: This invention relates to novel analogs of the DNA-binding alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
    Type: Grant
    Filed: February 2, 2007
    Date of Patent: January 27, 2015
    Assignee: Syntarga B.V.
    Inventors: Patrick Henry Beusker, Franciscus Marinus Hendrikus de Groot, Lutz F. Tietze, Felix Major, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker
  • Publication number: 20150018310
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: September 29, 2014
    Publication date: January 15, 2015
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone, Julie Wurster
  • Publication number: 20150011557
    Abstract: The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.
    Type: Application
    Filed: September 7, 2012
    Publication date: January 8, 2015
    Applicant: Merck Patent GmbH
    Inventors: Kai Schiemann, Wolfgang Staehle, Michael Busch, Dirk Wienke, Oliver Poeschke, Christa Burger
  • Patent number: 8927550
    Abstract: Disclosed are CCR1 receptor antagonists of the formula (I) wherein Ar1, Ar2, R1-R3, X and L are disclosed herein. Also disclosed are compositions, methods of making and using compounds of the formula (I).
    Type: Grant
    Filed: October 21, 2010
    Date of Patent: January 6, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Brian Nicholas Cook, Daniel Kuzmich
  • Publication number: 20150005279
    Abstract: The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: June 26, 2014
    Publication date: January 1, 2015
    Applicant: ABBVIE INC.
    Inventors: Dominique Bonafoux, Heather M. Davis, Kristine E. Frank, Michael M. Friedman, J. Martin Herold, Michael Z. Hoemann, Raymond Huntley, Augustine Osuma, George Sheppard, Gagandeep K. Somal, Jennifer Van Camp, Stacy A. Van Epps, Anil Vasudevan, Grier A. Wallace, Lu Wang, Lu Wang, Zhi Wang, Noel S. Wilson, Xiangdong Xu
  • Publication number: 20150005346
    Abstract: The present invention relates to novel heterocyclic derivatives which are allosteric modulators of cannabinoid receptor 1 (CB1) and which are useful for the treatment or prevention of neurological and psychiatric disorders associated with endocannabinoid dysfunction and diseases in which the CB1 subtype of cannabinoid receptor is involved; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.
    Type: Application
    Filed: July 3, 2014
    Publication date: January 1, 2015
    Inventors: Ganeshsingh A. THAKUR, Pushkar M. KULKARNI
  • Patent number: 8921559
    Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: December 30, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui, Xuqing Zhang
  • Patent number: 8912199
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: December 16, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
  • Publication number: 20140364393
    Abstract: The present invention is directed to novel piperidinyl-carboxamide derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders.
    Type: Application
    Filed: December 5, 2012
    Publication date: December 11, 2014
    Inventors: Shyh-Ming Yang, Gee-Hong Kuo, Micheal D. Gaul, Thomas A. Rano
  • Publication number: 20140364610
    Abstract: The present invention relates to certain heteroaromatic compounds of Formula (Ia), or pharmaceutically acceptable salts thereof, and uses of such compounds in the treatment of synucleopathies.
    Type: Application
    Filed: August 21, 2014
    Publication date: December 11, 2014
    Inventors: Eliezer MASLIAH, Edward M. ROCKENSTEIN, Wolfgang WRASIDLO, Igor Flint TSIGELNY
  • Patent number: 8907097
    Abstract: This disclosure is directed to pyrido[4,3-b]indoles having rigid moieties. The compounds in one embodiment are pyrido[4,3-b]indoles having an unsaturated hydrocarbon moiety. The compounds in another embodiment are pyrido[4,3-b]indoles having a cycloalkyl, cycloalkenyl or heterocyclyl moiety. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: October 30, 2009
    Date of Patent: December 9, 2014
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sarvajit Chakravarty
  • Publication number: 20140343001
    Abstract: The present invention encompasses compounds having general formula (I) able to inhibit the lactate production (lactic acid) involved in the angiogenesis of tumoral tissues, in the glycolytic metabolic process of tumoral cells, of immune system cells in asthmatic diseases, in vascular cells in the pulmonary hypertension, in the treatment of chronic back pain or hyperoxaluria, and in the process by which the parasites protozoan causing malaria obtain most of the necessary energy.
    Type: Application
    Filed: December 19, 2012
    Publication date: November 20, 2014
    Applicant: Universita di Pisa
    Inventors: Filippo Minutolo, Marco Macchia, Carlotta Granchi, Valeria Di Bussolo, Gino Giannaccini, Antonio Lucacchini, Paul J. Hergenrother, Emilia C. Calvaresi
  • Publication number: 20140343037
    Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Inventors: Kenneth He Huang, Jeron Eaves, Gunnar Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
  • Patent number: 8889716
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: November 18, 2014
    Assignee: CHDI Foundation, Inc.
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas MacDonald, John Wityak
  • Patent number: 8883395
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: November 11, 2014
    Assignee: International Business Machines Corporation
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Patent number: 8877780
    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: Grant
    Filed: May 30, 2008
    Date of Patent: November 4, 2014
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Roger Shen-Chu Chen, Alexander L. Ruchelman, Hon-Wah Man, Weihong Zhang, Ehab M. Khalil
  • Patent number: 8877932
    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: March 8, 2010
    Date of Patent: November 4, 2014
    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: 8877923
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: November 4, 2014
    Assignee: Allergan, Inc.
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone