Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 546/175)
  • Patent number: 9447044
    Abstract: The present invention relates to thioaryl derivatives of Formula 1 as defined in the specification, a method for preparing the same, a pharmaceutical composition comprising the same and use thereof. The thioaryl derivatives of Formula 1 according to the present invention promote GLP-1 formation in the gastrointestinal tract and improve insulin resistance in macrophages, pancreas cells, etc. due to anti-inflammatory action, and can accordingly be effectively used for preventing or treating diabetes, complications of diabetes, inflammation, obesity, non-alcoholic fatty liver, steatohepatitis or osteoporosis.
    Type: Grant
    Filed: November 5, 2013
    Date of Patent: September 20, 2016
    Assignee: LG LIFE SCIENCES LTD.
    Inventors: Young Kwan Kim, Myoung Yeol Kim, Sang Yun Park, Ok Ku Park, Vasily Artemov, Sang Dae Lee, Hyun Woo Joo, Eun Sil Choi
  • Patent number: 9290485
    Abstract: The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: March 22, 2016
    Assignee: NOVARTIS AG
    Inventors: Trixi Brandl, Stefanie Flohr, Sebastian Kopec, Julie Lachal, Christian Markert, Kenji Namoto, Perle Nganga, Bernard Pirard, Martin Renatus, Richard Sedrani, Thomas Zoller
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Patent number: 9024021
    Abstract: The present invention relates to novel diarylacetylene hydrazide compounds of formula (I) or pharmaceutically acceptable salt thereof, as tyrosine kinase inhibitors, the process for their preparation, and to the use of the compounds of formula (I) in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders related to tyrosine kinases, in warm-blooded animals.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: May 5, 2015
    Assignee: Sun Pharma Advanced Research Company Ltd.
    Inventors: Prabal Sengupta, Hemant Ashvinbhai Chokshi, Chetan Surjitsingh Puri, Sabbirhusen Yusufbhai Chimanwala, Varun Anilkumar Mehta, Dipali Manubhai Desai, Trinadha Rao Chitturi, Rajamannar Thennati
  • Publication number: 20150105366
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 16, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings, William Moore Jones, Steven Goldberg
  • Patent number: 9000010
    Abstract: The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: April 7, 2015
    Assignee: Sanofi
    Inventors: Ahmed Abouabdellah, Antoine Ravet
  • Patent number: 8993612
    Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: March 31, 2015
    Assignee: Rhizen Pharmaceuticals SA
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Kanthikiran V S Varanasi, Gayatri Swaroop Merikapudi, Swaroop Kumar V. S. Vakkalanka
  • Patent number: 8993561
    Abstract: The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: March 31, 2015
    Assignee: Sanofi
    Inventor: Alain Pellet
  • Publication number: 20150072974
    Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.
    Type: Application
    Filed: May 9, 2013
    Publication date: March 12, 2015
    Inventors: Phillip G. Jones, Robert Lew, Kerry L. Spear, Linghong Xie
  • Publication number: 20150018334
    Abstract: The present invention relates to aryl pyrazoles, and pharmaceutically acceptable salts thereof. The aryl pyrazoles of the present invention are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the aryl pyrazoles of the present invention, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: July 14, 2014
    Publication date: January 15, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Asitha ABEYWARDANE, John BROADWATER, Steven Richard BRUNETTE, Thomas Martin KIRRANE, JR., Hossein RAZAVI, Robert SIBLEY, Lana Louise SMITH KEENAN, Qiang ZHANG
  • Publication number: 20150018388
    Abstract: The present invention relates to the identification of compounds and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided compounds.
    Type: Application
    Filed: December 11, 2013
    Publication date: January 15, 2015
    Inventors: Richard B. Silverman, Yinan Zhang
  • Publication number: 20150018333
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: July 14, 2014
    Publication date: January 15, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Asitha ABEYWARDANE, John BROADWATER, Hidenori TAKAHASHI
  • 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: 20140378668
    Abstract: A new and versatile class of cyclic diazodicarboxamides that reacts efficiently and selectively with phenols and the phenolic side chain of tyrosine through an Ene-like reaction is reported. This mild aqueous tyrosine ligation reaction works over a broad pH range and expands the repertoire of aqueous chemistries available for small molecule, peptide, and protein modification. The tyrosine ligation reactions are shown to be compatible with the labeling of native enzymes and antibodies in buffered aqueous solution. This reaction provides a novel synthetic approach to bispecific antibodies. This reaction will find broad utility in peptide and protein chemistry and in the chemistry of phenol-containing compounds.
    Type: Application
    Filed: June 25, 2014
    Publication date: December 25, 2014
    Inventors: Carlos F. Barbas, III, Hitoshi Ban, Julia Gavrilyuk
  • Publication number: 20140369961
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy F. Stanton, Eric B. Sjogren
  • Publication number: 20140364608
    Abstract: The present invention provides a pesticide comprising an aryloxyacetamide compound represented by formula (IV) (wherein in formula (IV), R1a represents an alkyl group or the like, R2 to R5 independently represents an alkyl group, X represents a halogen atom or the like, n represents an integer of 0 to 5, Z represents an oxygen atom or a sulfur atom) or salt thereof as an active ingredient.
    Type: Application
    Filed: February 12, 2013
    Publication date: December 11, 2014
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Hironori Furukawa, Daisuke Hanai, Tetsuo Tamai, Yasuyuki Shiinoki
  • Patent number: 8901119
    Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: December 2, 2014
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
  • Publication number: 20140343065
    Abstract: 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.
    Type: Application
    Filed: May 12, 2014
    Publication date: November 20, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Riccardo GIOVANNINI, Yunhai CUI, Henri DOODS, Marco FERRARA, Stefan JUST, Raimund KUELZER, Iain LINGARD, Rocco MAZZAFERRO, Klaus RUDOLF
  • Publication number: 20140315944
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.
    Type: Application
    Filed: March 11, 2014
    Publication date: October 23, 2014
    Inventors: Jillian Basinger, James Breitenbucher, Graeme Freestone, Varsha Gupta, Alan Kaplan, Chi-Ching Mak, Benjamin Pratt, Vincent Santora, Dipanjan Sengupta, Lino Valdez
  • Patent number: 8865736
    Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: October 21, 2014
    Assignee: Biota Scientific Pty Ltd
    Inventors: David Ryall Brown, Ian Collins, Lloyd George Czaplewski, David John Haydon
  • Publication number: 20140309210
    Abstract: A compound of formula I: stereoisomers or a pharmaceutically acceptable salt thereof, wherein X, X1, X2, X3, R1, R2, R3, R4, R5 and R6 are described herein, compositions including the compounds and methods of making and using the compounds for the treatment of diseases.
    Type: Application
    Filed: February 12, 2014
    Publication date: October 16, 2014
    Applicant: Genentech, Inc.
    Inventors: Jason Burch, Richard A. Goldsmith, Daniel Fred Ortwine, Richard Pastor, Zhonghua Pei
  • Publication number: 20140243368
    Abstract: The present invention is directed to piperidinyl alkyne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the piperidinyl alkyne compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: October 19, 2012
    Publication date: August 28, 2014
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Patent number: 8815901
    Abstract: The invention relates to compounds of formula (I) wherein the substituents are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.
    Type: Grant
    Filed: August 8, 2013
    Date of Patent: August 26, 2014
    Assignee: Novartis AG
    Inventors: Pascal Furet, Diana Graus Porta, Vito Guagnano
  • Publication number: 20140228360
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: August 14, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof
  • Publication number: 20140221657
    Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.
    Type: Application
    Filed: April 7, 2014
    Publication date: August 7, 2014
    Applicant: PRISM BioLab Corporation
    Inventors: Hiroyuki Kouji, Yuji Kogami, Takenao Odagami
  • Publication number: 20140219995
    Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.
    Type: Application
    Filed: July 13, 2012
    Publication date: August 7, 2014
    Applicant: MICROBIOTIX, INC.
    Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams, Matthew Torhan
  • Publication number: 20140221322
    Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).
    Type: Application
    Filed: November 5, 2013
    Publication date: August 7, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Selerstad
  • Publication number: 20140179925
    Abstract: Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of Formulas 1 and 2 wherein the variables have the meaning disclosed in the specification
    Type: Application
    Filed: December 18, 2013
    Publication date: June 26, 2014
    Applicant: Allergan, Inc.
    Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
  • Patent number: 8729063
    Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: May 20, 2014
    Assignee: Incyte Corporation
    Inventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taishing Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
  • Publication number: 20140134235
    Abstract: The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.
    Type: Application
    Filed: October 14, 2013
    Publication date: May 15, 2014
    Applicant: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima BARUAH, Dibyendu DE, Ish Kumar KHANNA, Sivaram PILLARISETTI, Santanu MAITRA, Christopher W. ALEXANDER, Jennepalli SREENU, Indu Dagar, Shanavas Alikunju
  • Patent number: 8716265
    Abstract: The present invention relates to substituted 4-qinolinemethanols and pharmaceutical compositions thereof and methods of using the same for treating of malaria, tuberculosis, and other infectious diseases.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: May 6, 2014
    Assignee: Jenrin Discovery, Inc.
    Inventors: John F. McElroy, Robert J. Chorvat, David Nugiel
  • Publication number: 20140088077
    Abstract: The invention relates to substituted tetrahydronaphthalenes and derivatives thereof, and also to the physiologically compatible salts and physiologically functional derivatives thereof, to preparation thereof, to medicaments comprising at least one inventive substituted tetrahydronaphthalene or derivative thereof, and to the use of the inventive substituted tetrahydronaphthalenes and derivatives thereof as medicaments.
    Type: Application
    Filed: December 3, 2013
    Publication date: March 27, 2014
    Applicant: SANOFI
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Torsten Haack, Petra Lennig
  • 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
  • Publication number: 20140066412
    Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).
    Type: Application
    Filed: November 6, 2013
    Publication date: March 6, 2014
    Inventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Selerstad
  • Patent number: 8653070
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: February 18, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Yat Sun Or
  • Publication number: 20140045890
    Abstract: Compounds of the general formula (I) wherein the substituents are as defined in claim 1, are useful as fungicides.
    Type: Application
    Filed: March 28, 2012
    Publication date: February 13, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Guillaume Berthon, Fiona Kessabi Murphy, Renaud Beaudegnies, Clemens Lamberth, Laura Quaranta, Stephan Trah
  • Patent number: 8618302
    Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.
    Type: Grant
    Filed: January 6, 2011
    Date of Patent: December 31, 2013
    Inventors: Joseph P. Errico, Benjamin Mugrage, Ignatius Turchi, Matthew Sills, Jane Ong, John Allocco, Pam Wines
  • Patent number: 8586739
    Abstract: Substituted bicyclic heteroaryls having the general structure: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: November 19, 2013
    Assignee: Amgen Inc.
    Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian S. Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer L. Seganish, Youngsook Shin, Dawei Zhang
  • Publication number: 20130296557
    Abstract: The present invention relates to novel diarylacetylene hydrazide compounds of formula (I) or pharmaceutically acceptable salt thereof, as tyrosine kinase inhibitors, the process for their preparation, and to the use of the compounds of formula (I) in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders related to tyrosine kinases, in warm-blooded animals
    Type: Application
    Filed: January 23, 2012
    Publication date: November 7, 2013
    Applicant: SUN PHARMA ADVANCED RESEARCH COMPANY LTD.
    Inventors: Prabal Sengupta, Hemant Ashvinbhai Chokshi, Chetan Surjitsingh Puri, Sabbirhusen Yusufbhai Chimanwala, Varun Anilkumar Mehta, Dipali Manubhai Desai, Trinadha Rao Chitturi, Rajamannar Thennati
  • Publication number: 20130245008
    Abstract: The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.
    Type: Application
    Filed: November 18, 2011
    Publication date: September 19, 2013
    Applicant: SANOFI
    Inventor: Alain Pellet
  • Publication number: 20130225591
    Abstract: The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.
    Type: Application
    Filed: September 14, 2010
    Publication date: August 29, 2013
    Inventors: Michelle R. Machacek, Sean P. Ahearn, Eric Romeo, Tony Siu, Stephanie Chichetti, Gabriela de Almeida, Alexey A. Rivkin
  • Publication number: 20130225567
    Abstract: 5-alkynyl-pyridine of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R5 have the meanings given in the claims and in the specification.
    Type: Application
    Filed: February 19, 2013
    Publication date: August 29, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Ulrich REISER, Gerd BADER, Walter SPEVAK, Andreas STEFFEN, Alastair L. PARKES
  • 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
  • Publication number: 20130217727
    Abstract: The present invention relates to fungicidal 1-(heterocyclic carbonyl)-2-substituted pyrrolidines and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.
    Type: Application
    Filed: October 20, 2011
    Publication date: August 22, 2013
    Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Hiroyuki Hadano, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
  • Patent number: 8507509
    Abstract: Compounds of the general formula (I), wherein the substituents are as defined in claim 1, are useful as fungicides.
    Type: Grant
    Filed: September 3, 2008
    Date of Patent: August 13, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Fiona Murphy Kessabi, Hans-Georg Brunner, Renaud Beaudegnies, Laura Quaranta, Fredrik Cederbaum, Jayant Umarye
  • Publication number: 20130203768
    Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: September 28, 2011
    Publication date: August 8, 2013
    Inventors: Michael Berger, Christopher Kern, Marko Eck, Jörg Schröder
  • Patent number: 8481532
    Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: July 9, 2013
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • Patent number: 8481534
    Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.
    Type: Grant
    Filed: June 25, 2009
    Date of Patent: July 9, 2013
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • Patent number: 8476255
    Abstract: Provided herein are novel, stilbene like compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, metabolites, prodrugs, solvates, pharmaceutically acceptable salts and compositions thereof. These compounds can inhibit HDACs and are useful as a therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, etc.
    Type: Grant
    Filed: October 8, 2008
    Date of Patent: July 2, 2013
    Assignee: Orchid Chemicals & Pharmaceuticals Limited
    Inventors: Sridharan Rajagopal, Virendra Kachhadia, Thanasekaran Ponpandian, Abdul Raheem Keeri, Umamaheswari Mani, Suresh Rathinasamy, Praveen Rajendran, Kamaraj Mani, Balaji Ramachandran, Punthalir Narayanaswamy, Sriram Rajagopal
  • Publication number: 20130136794
    Abstract: Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.
    Type: Application
    Filed: April 21, 2011
    Publication date: May 30, 2013
    Applicant: PEKING UNIVERSITY
    Inventors: Runtao Li, Zemei Ge, Jingrong Cui, Xingyl Sun, Zhongqing Wang, Xu Yan