Additional Hetero Ring Containing Patents (Class 546/187)
  • Patent number: 10584136
    Abstract: Aluminum chloride is separated from a silane mixture containing aluminum chloride by reacting the aluminum chloride with a compound reactive therewith which forms an ionic liquid or solid, and separating the ionic liquid or solid from the now-purified silane.
    Type: Grant
    Filed: April 3, 2017
    Date of Patent: March 10, 2020
    Assignee: WACKER CHEMIE AG
    Inventors: Andreas Bockholt, Konrad Mautner
  • Patent number: 10202362
    Abstract: This present disclosure is directed to compounds of formula (I): where R1a, R3, Y, and Z are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions including the compounds described herein and methods of preparing the compounds described herein are also provided.
    Type: Grant
    Filed: December 11, 2017
    Date of Patent: February 12, 2019
    Assignee: Celtaxsys, Inc.
    Inventors: Kurt Roinestad, William Guilford, Tom Kirkland, Lopa Bhatt, Eric Springman
  • Patent number: 9409884
    Abstract: The disclosure relates particularly to certain carboxamide, sulfonamide and amine compounds and pharmaceutical compositions thereof, and to methods of treating and ameliorating disorders and conditions related to the adiponectin pathway, sphingolipid metabolism, oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. In certain embodiments, the compounds have the structures (I-1), (2-I) and (3-I) in which the variables are as described herein.
    Type: Grant
    Filed: January 31, 2013
    Date of Patent: August 9, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, David Carroll, Simon Shaw, Hitoshi Yasumichi
  • Patent number: 9353092
    Abstract: The present disclosure provides compositions and methods for the synthesis and use of croconaine compounds. The disclosed compounds are easily prepared from croconic acid. A halothiophene is reacted with an alkanolamine, the resulting aminothiophene is modified by appending a desired functional group to the hydroxyl group, and the modified aminothiophene is reacted with croconic acid to form the final compound. Applications of such croconaine compounds include photothermal imaging, photothermal therapy, light-activated drug release, and tissue welding.
    Type: Grant
    Filed: June 21, 2014
    Date of Patent: May 31, 2016
    Assignee: University of Notre Dame du Lac
    Inventor: Bradley Smith
  • Patent number: 9029531
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: May 12, 2015
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
  • Patent number: 9023854
    Abstract: The present invention relates to novel 5-halogen-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.
    Type: Grant
    Filed: December 5, 2008
    Date of Patent: May 5, 2015
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilfried Braje, Thorsten Oost, Astrid Netz, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Andrea Hager-Wernet
  • Publication number: 20150111888
    Abstract: The present invention provides a small compound targeting at TACC3. The present invention further provides a drug, particularly, an anticancer agent, comprising the small compound targeting at TACC3. A compound represented by the general formula (I) or a pharmaceutically acceptable salt, solvate, or ester derivative thereof binds to TACC3 and inhibits cell growth. Thus, these compounds can be used as drugs, particularly, anticancer agents.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 23, 2015
    Inventors: Ryoji Yao, Hiroyuki Osada, Yasumitsu Kondoh
  • Patent number: 8987303
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: March 24, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Publication number: 20150079028
    Abstract: Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.
    Type: Application
    Filed: August 5, 2013
    Publication date: March 19, 2015
    Applicant: SUNSHINE LAKE PHARMA CO., LTD
    Inventors: Yingjun Zhang, Jaincun Zhang, Hongming Xie, Qingyun Ren, Yumei Tan, Huichao Luo
  • Patent number: 8980921
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: March 17, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Publication number: 20150065490
    Abstract: Compounds of formula I in free or salt or solvate form, wherein X has the meaning indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ?2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Application
    Filed: November 6, 2014
    Publication date: March 5, 2015
    Applicant: NOVARTIS AG
    Inventors: Bernard CUENOUD, Robin Alec FAIRHURST, Roger John TAYLOR, David BEATTIE
  • Patent number: 8962845
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, and X are defined herein. Also disclosed are pharmaceutical compositions and methods related to use of these compounds.
    Type: Grant
    Filed: September 25, 2012
    Date of Patent: February 24, 2015
    Assignee: National Health Research Institutes
    Inventors: Kak-Shan Shia, Chun-Ping Chang, Yu-Sheng Chao
  • Publication number: 20150045553
    Abstract: Provided are novel compounds that are useful in the prevention or treatment of such diseases as dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, epilepsy, central convulsion, obesity, diabetes mellitus, hyperlipidemia, narcolepsy, idiopathic hypersomnia, behaviorally induced insufficient sleep syndrome, sleep apnea syndrome, circadian rhythm disorder, parasomnia, sleep related movement disorder, insomnia, depression, or allergic rhinitis, or pharmaceutically acceptable salts of such compounds.
    Type: Application
    Filed: December 27, 2012
    Publication date: February 12, 2015
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Toshio Nakamura, Seiji Masuda
  • Patent number: 8952004
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R3, A, B, X, and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: January 5, 2011
    Date of Patent: February 10, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: John David Ginn, Ronald John Sorcek, Michael Robert Turner, Di Wu, Frank Wu
  • Publication number: 20150025056
    Abstract: The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.
    Type: Application
    Filed: October 3, 2014
    Publication date: January 22, 2015
    Applicant: Incyte Corporation
    Inventors: Yun-Long Li, Jincong Zhuo, David M. Burns, Wenqing Yao, Ravi Kumar Jalluri
  • Publication number: 20150011754
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: September 17, 2014
    Publication date: January 8, 2015
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
  • Publication number: 20150005501
    Abstract: The present disclosure provides compositions and methods for the synthesis and use of croconaine compounds. The disclosed compounds are easily prepared from croconic acid. A halothiophene is reacted with an alkanolamine, the resulting aminothiophene is modified by appending a desired functional group to the hydroxyl group, and the modified aminothiophene is reacted with croconic acid to form the final compound. Applications of such croconaine compounds include photothermal imaging, photothermal therapy, light-activated drug release, and tissue welding.
    Type: Application
    Filed: June 21, 2014
    Publication date: January 1, 2015
    Applicant: University of Notre Dame du Lac
    Inventor: Bradley Smith
  • 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: 20140378471
    Abstract: The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.
    Type: Application
    Filed: September 9, 2014
    Publication date: December 25, 2014
    Inventors: Astrid Netz, Thorsten Oost, Herve Geneste, Wilfried Braje, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
  • Publication number: 20140378429
    Abstract: The disclosure relates particularly to certain carboxamide, sulfonamide and amine compounds and pharmaceutical compositions thereof, and to methods of treating and ameliorating disorders and conditions related to the adiponectin pathway, sphingolipid metabolism, oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. In certain embodiments, the compounds have the structures (I-1), (2-I) and (3-I) (The chemical formulas should be inserted here) in which the variables are as described herein.
    Type: Application
    Filed: January 31, 2013
    Publication date: December 25, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, David Carroll, Simon Shaw, Hitoshi Yasumichi
  • Patent number: 8916555
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: December 23, 2014
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
  • 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
  • Patent number: 8907098
    Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, Y1, Y2, V, W, n, m and o have the meanings given herein, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.
    Type: Grant
    Filed: November 18, 2010
    Date of Patent: December 9, 2014
    Assignee: MERCK PATENT GmbH
    Inventors: Frank Stieber, Dirk Wienke
  • Publication number: 20140349989
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and complications associated with these diseases and disorders.
    Type: Application
    Filed: December 20, 2013
    Publication date: November 27, 2014
    Applicant: ALZHEIMER'S INSTITUTE OF AMERICA
    Inventors: Dange Vijay Kumar, Paul M. Slattum, Kraig M. Yager, Mark D. Shenderovich, Rajendra Tangallapally, Se-Ho Kim
  • Publication number: 20140349918
    Abstract: The present invention relates to xanthone analogs. Such compounds may be used in the treatment of bacterial infections.
    Type: Application
    Filed: September 10, 2012
    Publication date: November 27, 2014
    Applicants: Singapore Health Services Pte Ltd., Agency for Science, Technology and Research
    Inventors: Hanxun Zou, Lakshminiarayan Rajanmani, Lei Zhou, Chang Chui Charles Tang, Jun Jie Koh, Tiang Hwee Donald Tan, Chandra Verma, Roger W. Beuerman, Shouping Liu, Saraswathi Padmanabhan
  • Publication number: 20140343074
    Abstract: The present invention relates to novel substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-related disorders.
    Type: Application
    Filed: March 14, 2014
    Publication date: November 20, 2014
    Inventors: Katja Jantos, Wilfred Braje, Herve Geneste, Andreas Kling, Liliane Unger, Berthold Behl, Marcel van Gaalen, Wilfried Hornberger, Loic Laplanche, Silke Weber
  • Publication number: 20140341851
    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: Application
    Filed: April 4, 2014
    Publication date: November 20, 2014
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: YAO-LING QIU, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Xuri Gao, Bin Wang, Yat Sun Or
  • Publication number: 20140343075
    Abstract: The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.
    Type: Application
    Filed: July 30, 2014
    Publication date: November 20, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Kai SCHIEMANN, Melanie SCHULTZ, Wolfgang STAEHLE
  • Patent number: 8889670
    Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: November 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell
  • Publication number: 20140336168
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 13, 2014
    Inventor: AbbVie Inc.
  • Publication number: 20140336165
    Abstract: Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.
    Type: Application
    Filed: November 14, 2012
    Publication date: November 13, 2014
    Inventors: Takeshi Hondo, Keita Nakanishi, Tatsuya Niimi, Masaichi Warizaya, Ichiji Namatame, Katsuya Harada
  • Publication number: 20140330010
    Abstract: Provided are novel compounds that are useful in the prevention or treatment of such diseases as dementia, Alzheimer's disease, attention-deficient hyperactivity disorder, schizophrenia, epilepsy, central convulsion, obesity, diabetes mellitus, hyperlipidemia, narcolepsy, idiopathic hypersomnia, behaviorally induced insufficient sleep syndrome, sleep apnea syndrome, circadian rhythm disorder, parasomnia, sleep related movement disorder, insomnia, and depression, or allergic rhinitis, or pharmaceutically acceptable salts of such compounds.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 6, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Toshio Nakamura, Seiji Masuda
  • Publication number: 20140329803
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.
    Type: Application
    Filed: November 16, 2012
    Publication date: November 6, 2014
    Inventors: Miles Congreve, Giles Brown, Julie Cansfield, Benjamin Tehan
  • Patent number: 8877778
    Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, x, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: November 4, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • Publication number: 20140323458
    Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.
    Type: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Inventors: Jason Allan Wiles, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Venkat Gadhachanda, Avinash Phadke, Milind Deshpande, Dawei Chen
  • Patent number: 8871770
    Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: February 3, 2014
    Date of Patent: October 28, 2014
    Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
  • Publication number: 20140314669
    Abstract: The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (PET) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body. More particularly, the invention relates to small nonpeptide, high-affinity, specific-binding glycoprotein 11b/IIIa antagonists for imaging of thrombi.
    Type: Application
    Filed: August 17, 2012
    Publication date: October 23, 2014
    Applicant: PIRAMAL IMAGING SA
    Inventors: Markus Berger, Martin Kruger, Jessica Lohrke, Michael Reinhardt, Holger Siebeneicher
  • Publication number: 20140315914
    Abstract: The present invention relates to novel carbamate-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.
    Type: Application
    Filed: April 14, 2014
    Publication date: October 23, 2014
    Inventors: Astrid Netz, Thorsten Oost, Hervé Geneste, Wilfried Braje, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
  • Publication number: 20140315893
    Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi
    Type: Application
    Filed: November 22, 2012
    Publication date: October 23, 2014
    Inventors: Ferenc Fülöp, László Vígh, Zsolt Török, Botond Penke, Ibolya Horváth, Gábor Balogh, Sándor Bernáth, Ákos Hunya
  • Publication number: 20140315918
    Abstract: The present invention relates to novel substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-related disorders.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Inventors: Katja Jantos, Wilfred Braje, Herve Geneste, Andreas Kling, Liliane Unger, Berthold Behl, Marcel van Gaalen, Wilfried Hornberger, Loic Laplanche, Silke Weber
  • Patent number: 8865702
    Abstract: Disclosed are compounds of the formula I wherein A, Y, R1, R2, R3, R4 and R5 are defined, suitable for treating diseases and symptoms of diseases caused at least to some extent by stimulation of bradykinin-B1 receptors, the preparation thereof and the use thereof.
    Type: Grant
    Filed: July 23, 2008
    Date of Patent: October 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Iris Kauffmann-Hefner, Angelo Ceci, Henri Doods, Norbert Hauel, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
  • Publication number: 20140309193
    Abstract: There are provided inter alia compounds of formula (I) wherein R1, R2, R3, R4a and R4b are as defined in the specification and their use in therapy, especially in the treatment of bacterial (e.g. pneumococcal) infections.
    Type: Application
    Filed: December 5, 2012
    Publication date: October 16, 2014
    Inventors: Peter William Andrew, Rana Lonnen, Mafalda Pires Damaso, Fritz-Frieder Frickel, Simon Christopher Hirst, Mark William Davies, Daniel Hamza
  • Patent number: 8859776
    Abstract: The present invention provides a compound of Formula 1 as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
    Type: Grant
    Filed: October 5, 2010
    Date of Patent: October 14, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Stephane L. Bogen, Yao Ma, Yaolin Wang, Brian Robert Lahue, Latha G. Nair, Manami Shizuka, Matthew Ernst Voss, Margarita Kirova-Snover, Weidong Pan, Yuan Tian, Bheemashankar A. Kulkarni, Craig R. Gibeau, Yuan Liu, Giovanna Scapin, Diane Rindgen, Ronald J. Doll, Timothy J. Guzi, Danny J. Hicklin, Amin Nomeir, Gerald W. Shipps, Jr., Malcolm MacCoss
  • Patent number: 8859557
    Abstract: The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.
    Type: Grant
    Filed: August 21, 2012
    Date of Patent: October 14, 2014
    Assignee: Abbott GmbH & Co. KG
    Inventors: Astrid Netz, Thorsten Oost, Herve Geneste, Wilfried Martin Braje, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Andrea Hager-Wernet
  • Patent number: 8853205
    Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or CB2 cannabinoid receptors. Aspects disclose hetero pyrrole analogs acting as CB1 and/or CB 1 receptor antagonists, having selectivity for the CB 1 or CB2 receptor, acting as neutral antagonists, acting preferentially on CB 1 receptors located in the peripheral nervous system, and/or acting as nitric oxide donors. Pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect are also disclosed.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: October 7, 2014
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Venkata Kiran Vemuri
  • Publication number: 20140296289
    Abstract: Thiazolyl oxime ethers and hydrazones of the formula (I), in which the symbols A, L1, L2, Y, W, X, R1, R2, R3, R4, R5, R6 and R7 have the meanings given in the description, and also agrochemically active salts thereof, and their use for controlling phytopathogenic harmful fungi, and also methods for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
    Type: Application
    Filed: February 28, 2014
    Publication date: October 2, 2014
    Applicant: Bayer CropScience AG
    Inventors: Pierre CRISTAU, Nicola Rahn, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann, Arnd Voerste, Jürgen Benting
  • Publication number: 20140296235
    Abstract: Compounds having formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds having formula (I), methods of treatment comprising compounds having formula (I), and methods of inhibiting the PARP enzyme comprising compounds having formula (I).
    Type: Application
    Filed: April 11, 2014
    Publication date: October 2, 2014
    Inventors: Thomas D. Penning, Sheela A. Thomas, Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Vincent L. Giranda
  • Patent number: 8846675
    Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.
    Type: Grant
    Filed: May 3, 2012
    Date of Patent: September 30, 2014
    Assignee: Cymabay Therapeutics, Inc.
    Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
  • Publication number: 20140275068
    Abstract: The present invention provides neuronal gap junction blocking compounds according to formula (I) or a hydrate, solvate, or pharmaceutically acceptable salt thereof: wherein the integers Q, R2, A, R1, Z1, Z2, and Z3 are as defined in claim 1. The compounds are useful for the treatment or prevention of a range of conditions including, e.g., migraine, epilepsy, non-epileptic seizures, brain injury, and cardiovascular disease.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Proximagen Limited
    Inventors: Edward Savory, Daniel Hill, Oldrich Kocian
  • Publication number: 20140275110
    Abstract: The present invention relates to novel amidomethyl-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.
    Type: Application
    Filed: April 11, 2014
    Publication date: September 18, 2014
    Inventors: Thorsten Oost, Astrid Netz, Hervé Geneste, Wilfried Braje, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch