Oxadiazole Ring Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/269.4)
  • Patent number: 10308659
    Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: September 28, 2015
    Date of Patent: June 4, 2019
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Olivier Gavelle, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Roever Stephan, Mark Rogers-Evans, Didier Rombach, Tanja Schulz-Gasch
  • Patent number: 9845316
    Abstract: This invention relates to novel polymorphs of (HO)2NO2(C6H)—(C2N2O)—(C5N)(CH3)2Cl2O, to processes for their preparation, and to pharmaceutical compositions containing said novel polymorphs as active pharmaceutical ingredient.
    Type: Grant
    Filed: February 23, 2015
    Date of Patent: December 19, 2017
    Assignee: BIAL—PORTELA & CA., S.A.
    Inventor: David Alexander Learmonth
  • Patent number: 9630955
    Abstract: There is disclosed a methylated intermediate which may be demethylated to provide an inhibitor of catechol-O-methyltransferase useful in the treatment of Parkinson's disease. Also disclosed are methods of making and using said intermediate.
    Type: Grant
    Filed: July 31, 2015
    Date of Patent: April 25, 2017
    Inventors: Domenico Russo, Laszlo Erno Kiss, Jorge Bruno Reis Wahnon, David Alexander Learmonth, Tibor Eszenyi, Axel Zimmermann, Bjoern Schlummer, Michael Kreis, Klaus Reiter
  • Patent number: 9617250
    Abstract: The invention relates to compounds of the Formula (I), Formula (I) wherein R1 and R2 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: April 11, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Martin Bolli, Cyrille Lescop, Oliver Nayler, Beat Steiner
  • Patent number: 9409898
    Abstract: The present invention relates to compounds described herein Formula (I) and pharmaceutical acceptable salts thereof, which modulate the activity of calcium release-activated calcium (CRAC) channel. The invention also describes the compounds of Formula (I) and pharmaceutical compositions containing such compounds thereof for treating, managing, and/or lessening the severity of diseases, disorders, syndromes or conditions associated with the modulation of calcium release-activated calcium (CRAC) channel.
    Type: Grant
    Filed: May 1, 2013
    Date of Patent: August 9, 2016
    Assignee: LUPIN LIMITED
    Inventors: Nageswara Rao Irlapati, Gokul Keruji Deshmukh, Nilesh Raghunath Khedkar, Kiran Chandrashekhar Kulkarni, Zubair Abdul Wajid Shaikh, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 9399638
    Abstract: The present invention relates to compounds described herein Formula (I) and pharmaceutical acceptable salts thereof, which modulate the activity of calcium release-activated calcium (CRAC) channel. The invention also describes the compounds of Formula (I) and pharmaceutical compositions containing such compounds thereof for treating, managing, and/or lessening the severity of diseases, disorders, syndromes or conditions associated with the modulation of calcium release-activated calcium (CRAC) channel.
    Type: Grant
    Filed: May 1, 2013
    Date of Patent: July 26, 2016
    Assignee: LUPIN LIMITED
    Inventors: Nageswara Rao Irlapati, Zubair Abdul Wajid Shaikh, Vijay Pandurang Karche, Gokul Keruji Deshmukh, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 9126988
    Abstract: There is disclosed a methylated intermediate which may be demethylated to provide an inhibitor of catechol-O-methyltransferase useful in the treatment of Parkinson's disease. Also disclosed are methods of making and using said intermediate.
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: September 8, 2015
    Assignee: BIAL—PORTELA & CA, S.A.
    Inventors: Domenico Russo, Laszlo Erno Kiss, Jorge Bruno Reis Wahnon, David Alexander Learmonth, Tibor Eszenyi, Axel Zimmermann, Bjoern Schlummer, Michael Kreis, Klaus Reiter
  • Publication number: 20150133669
    Abstract: The present invention relates to new processes for the preparation of 2-cyclopentyl-6-methoxy-isonicotinic acid, which is a useful intermediate for the synthesis of pyridine-4-yl derivatives as immunomodulating agent. Moreover, the present invention also relates to new intermediates used in those processes.
    Type: Application
    Filed: May 21, 2013
    Publication date: May 14, 2015
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventor: Gunther Schmidt
  • Publication number: 20150111900
    Abstract: The present invention relates to compounds described herein Formula (I) and pharmaceutical acceptable salts thereof, which modulate the activity of calcium release-activated calcium (CRAC) channel. The invention also describes the compounds of Formula (I) and pharmaceutical compositions containing such compounds thereof for treating, managing, and/or lessening the severity of diseases, disorders, syndromes or conditions associated with the modulation of calcium release-activated calcium (CRAC) channel.
    Type: Application
    Filed: May 1, 2013
    Publication date: April 23, 2015
    Inventors: Nageswara Rao Irlapati, Zubair Abdul Wajid Shaikh, Vijay Pandurang Karche, Gokul Keruji Deshmukh, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20150094337
    Abstract: The present invention provides a heterocyclic group contained amino-methanol derivative, and salt, a preparation method and use thereof, and belongs to the medical field. The heterocyclic group contained amino-methanol derivative and the salt thereof of the present invention are used for preparing medicines for immune suppression and for the treatment of organ transplant rejection, or medicines for treating immune mediated inflammatory diseases, such as multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis.
    Type: Application
    Filed: December 8, 2014
    Publication date: April 2, 2015
    Inventors: Xingmin Zhang, Ensi Wang, Jing Guo, Shengxiu Niu, Zhuolin Dai, Nan Zheng, Liping Ji, Zhenfang Wang, Tie Liang
  • Publication number: 20150072977
    Abstract: New compounds of formula I are described. The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.
    Type: Application
    Filed: November 14, 2014
    Publication date: March 12, 2015
    Inventors: David Alexander LEARMONTH, Laszlo Erno KISS, Pedro Nuno LEAL PALMA, Humberto DOS SANTOS FERREIRA, Patricio Manuel Vieira ARAUJO SOARES DA SILVA
  • Patent number: 8975410
    Abstract: This invention relates to novel polymorphs of (HO)2NO2(C6H)—(C2N2O)—(C5N)(CH3)2Cl2O, to processes for their preparation, and to pharmaceutical compositions containing said novel polymorphs as active pharmaceutical ingredient.
    Type: Grant
    Filed: March 16, 2009
    Date of Patent: March 10, 2015
    Assignee: BIAL—Portela & CA., S.A.
    Inventors: David Alexander Learmonth, Keith Lorimer, Kevin Wayne Meyer, Tibor Eszenyi, Álmosné Kovách
  • Patent number: 8946426
    Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: February 2, 2010
    Date of Patent: February 3, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Henricus Jacobus Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, François Paul Bischoff, Tongfei Wu, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge Maria Aloysius Pieters, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn, Daniel Oehlrich
  • Publication number: 20150011517
    Abstract: The present invention relates to a lupane triterpenoid derivatives and pharmaceutical use thereof, specifically relates to a lupane triterpenoid derivatives of formula (I)˜(III), a pharmaceutical composition and a combination preparation comprising a lupane triterpenoid derivatives or a pharmaceutically acceptable salt thereof in a therapeutically-effective dose, particularly relates to the use in preparation of a medicament for the treatment of HIV-1/AIDS.
    Type: Application
    Filed: January 30, 2013
    Publication date: January 8, 2015
    Inventor: Feng Lu
  • Patent number: 8916594
    Abstract: This invention provides new compounds having NPY Y5 antagonistic activity. The present inventors found that a compound of the formula (I): wherein R1 is substituted or unsubstituted alkyl or the like; p, q and r are each independently 0 or 1; ring A is oxadiazole; and R2 is substituted or unsubstituted alkyl or the like, has NPY Y5 antagonistic activity.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: December 23, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kyohei Hayashi, Yuusuke Tamura, Naoki Omori
  • Patent number: 8907099
    Abstract: New compounds of formula I are described. The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.
    Type: Grant
    Filed: April 9, 2012
    Date of Patent: December 9, 2014
    Assignee: Bial-Portela & Ca, S.A.
    Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto Dos Santos Ferreira, Patricio Manuel Vieira Araújo Soares da Silva
  • Publication number: 20140350057
    Abstract: There is disclosed a methylated intermediate which may be demethylated to provide an inhibitor of catechol-O-methyltransferase useful in the treatment of Parkinson's disease. Also disclosed are methods of making and using said intermediate.
    Type: Application
    Filed: December 12, 2012
    Publication date: November 27, 2014
    Applicant: BIAL - PORTELA & CA, S.A.
    Inventors: Domenico Russo, Laszlo Erno Kiss, Jorge Bruno Reis Wahnon, David Alexander Learmonth, Tibor Eszenyi, Axel Zimmermann, Bjoern Schlummer, Michael Kreis, Klaus Reiter
  • Publication number: 20140343052
    Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent glucose lowering effect. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof: wherein R1 represents a C1-C3 alkyl group, each substituent R2 may be the same or different and may each represent a C1-C3 alkyl group, R3 represents an optionally substituted pyridyl group or the like, R4 and R5, which are the same or different, each represent a C1-C3 alkyl group, R6 and R7, which are the same or different, each represent a C1-C3 alkyl group, and n represents 0 to 3.
    Type: Application
    Filed: May 30, 2014
    Publication date: November 20, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Shigeo YAMANOI, Katsuji KAGECHIKA, Tsuyoshi SONEDA, Yuichi OCHIAI, Hidenori NAMIKI, Fuminao DOI, Madoka HOSHINO, Shoko YOSHIDA
  • Publication number: 20140329797
    Abstract: The present application relates to novel substituted 5-(1,2,4-oxadiazol-5-yl)pyridin-2-ones and 6-(1,2,4-oxadiazol-5-yl)pyridazin-3-ones, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for producing medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: October 16, 2012
    Publication date: November 6, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Unterschemmann
  • Publication number: 20140275133
    Abstract: The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof that are possible useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the above mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).
    Type: Application
    Filed: October 8, 2012
    Publication date: September 18, 2014
    Inventors: Hong Shen, Jason M. Cox, Hong Dong Chu
  • Publication number: 20140249159
    Abstract: The invention relates to compounds of Formula I: wherein Ar1, Ar2, Ar3, L1, L2, Y, Z and v are defined in the specification, and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.
    Type: Application
    Filed: May 16, 2012
    Publication date: September 4, 2014
    Inventors: Noriyuki Kurose, Kayoko Hata, Yasuyoshi Iso, Naoko Yamaguchi, Bin Shao, Laykea Tafesse, Xiaoming Zhou, Jianming Yu
  • Patent number: 8815903
    Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a benzene ring, a pyridine ring, or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; Z represents —C(?O)—NHSO2R6, an acidic 5-membered hetero ring group, or the like; R1 represents a hydrogen atom or the like; R2 represents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: August 26, 2014
    Assignees: Kissei Pharmaceutical Co., Ltd., Kyorin Pharmaceutical Co., Ltd.
    Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
  • Publication number: 20140235673
    Abstract: The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 21, 2014
    Inventors: Zulan Pi, John Llyod, Jennifer X. Qiao, Tammy C. Wang, George O. Tora
  • Publication number: 20140228376
    Abstract: The present invention provides pyridin-oxadiazole/thiadiazole derivatives of Formula I wherein A is N or CR 4a; and (ii) or (iii) which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: September 14, 2012
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: Kamlesh Jagdis Bala, Rebecca Butler, Stephen Paul Collingwood, Edward Charles Hall, Lee Edwards, Darren Mark Legrand, Katrin Spiegel
  • Patent number: 8802858
    Abstract: A compound of formula II in which Z is C or N and the Z ring is optionally further substituted; R1 is H, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl; and R2 is a group selected from (b), (c), and (d):
    Type: Grant
    Filed: July 26, 2010
    Date of Patent: August 12, 2014
    Assignee: Basilea Pharmaceutica AG
    Inventors: Jens Pohlmann, Felix Bachmann
  • Patent number: 8796247
    Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a pyridine ring, a furan ring, or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents —C(?O)—NH—SO2R6, an acidic 5-membered hetero ring group, or the like; R2 represents an optionally substituted phenyl group, an optionally substituted 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], and a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: August 5, 2014
    Assignees: Kissei Pharmaceutical Co., Ltd., Kyorin Pharmaceutical Co., Ltd.
    Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
  • Patent number: 8796253
    Abstract: This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.
    Type: Grant
    Filed: May 8, 2008
    Date of Patent: August 5, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Stephen Boyer, Michael Härter, Philip Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp
  • Patent number: 8791091
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: July 29, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Huji Turdi, Jon J. Hangeland, R. Michael Lawrence, Saleem Ahmad, Wei Meng, Robert Paul Brigance, Pratik Devasthale, Guohua Zhao
  • Patent number: 8791142
    Abstract: The present invention provides oxadiazole pyridine derivatives of Formula (I), their use as medicaments and their use for treating multiple sclerosis and other diseases.
    Type: Grant
    Filed: March 2, 2010
    Date of Patent: July 29, 2014
    Assignee: Merck Serono S.A.
    Inventors: Anna Quattropani, Patrick Gerber, Jerome Dorbais
  • Publication number: 20140187780
    Abstract: The present invention discloses compounds of formula I, II or X, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
    Type: Application
    Filed: December 24, 2013
    Publication date: July 3, 2014
    Applicant: Enanta Pharmaceuticals, Inc.
    Inventors: In Jong Kim, Tongzhu Liu, Jiang Long, Guoqiang Wang, Yao-Ling Qiu, Heejin Kim, Yanchun Wang, Ly Tam Phan, Yat Sun Or
  • Patent number: 8759539
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • Patent number: 8716317
    Abstract: The invention relates to Sulfonamides with heterocycle and oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
    Type: Grant
    Filed: May 22, 2009
    Date of Patent: May 6, 2014
    Assignee: Sanofi
    Inventors: Stefanie Keil, Matthias Urmann, Maike Glien, Hans Matter, Harry Randall Munson, Jr., Ulrike Wendler
  • Patent number: 8697732
    Abstract: The invention relates to novel pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: April 15, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
  • Patent number: 8697733
    Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: June 20, 2013
    Date of Patent: April 15, 2014
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
  • Publication number: 20140081025
    Abstract: The compound represented by formula (IA) or a pharmaceutically acceptable salt thereof is based on orexin (OX) receptor antagonist activity, is useful in the treatment and prevention of illnesses including sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependency, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, pain, gastrointestinal disease, epilepsy, inflammation, immunological disease, endocrinological related disease, and hypertension.
    Type: Application
    Filed: May 8, 2012
    Publication date: March 20, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Ryo Suzuki, Aya Futamura, Masahito Abe, Shuhei Kashiwa, Nobutaka Hattori, Dai Nozawa, Hiroshi Ohta, Yuko Araki
  • Publication number: 20140073634
    Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.
    Type: Application
    Filed: August 23, 2013
    Publication date: March 13, 2014
    Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer Center
    Inventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Joe Marszalek, Gang Liu, Zhijun Kang, Chris Carroll, Timothy McAfoos, Barbara Czako
  • Publication number: 20140073650
    Abstract: Focused library synthesis and medicinal chemistry on an oxadiazole-isopropylamide core proteasome inhibitor provided the lead compound that strongly inhibits CT-L activity. Structure activity relationship studies indicate the amide moiety and two phenyl rings are sensitive toward synthetic modifications. Only para-substitution in the A-ring was important to maintain potent CT-L inhibitory activity. Hydrophobic residues in the A-ring's para-position and meta-pyridyl group at the B-ring significantly improved inhibition. The meta-pyridyl moiety improved cell permeability. The length of the aliphatic chain at the para position of the A-ring is critical with propyl yielding the most potent inhibitor, whereas shorter (i.e. ethyl, methyl or hydrogen) or longer (i.e. butyl, propyl and hexyl) chains demonstrating progressively less potency. Introduction of a stereogenic center next to the ether moiety (i.e.
    Type: Application
    Filed: September 24, 2013
    Publication date: March 13, 2014
    Applicant: H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: Harshani R. Lawrence, Said M. Sebti, Sevil Ozcan
  • Patent number: 8658675
    Abstract: The invention relates to pyridine derivatives of Formula (I), wherein A, R1, R2, R3, and R4 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
    Type: Grant
    Filed: July 15, 2010
    Date of Patent: February 25, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, Cyrille Lescop, Boris Mathys, Keith Morrison, Claus Mueller, Oliver Nayler, Beat Steiner
  • Publication number: 20140051862
    Abstract: This invention provides new compounds having NPY Y5 antagonistic activity. The present inventors found that a compound of the formula (I): wherein R1 is substituted or unsubstituted alkyl or the like; p, q and r are each independently 0 or 1; ring A is oxadiazole; and R2 is substituted or unsubstituted alkyl or the like, has NPY Y5 antagonistic activity.
    Type: Application
    Filed: April 25, 2012
    Publication date: February 20, 2014
    Applicant: Shionogi & Co., Ltd.
    Inventors: Kyohei Hayashi, Yuusuke Tamura, Naoki Omori
  • Publication number: 20140031374
    Abstract: The present invention relates to compounds of formula (I), to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy: Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway and increased presence of nuclear ?-catenin. For example, these may be used in preventing and/or retarding proliferation of tumor cells and metastasis, for example carcinomas such as colon carcinomas.
    Type: Application
    Filed: December 8, 2011
    Publication date: January 30, 2014
    Applicant: OSLO University Hospital, HF
    Inventors: Daniel Holsworth, Jo Waaler, Ondrej Machon, Stefan Krauss, Andrey Edward Voronkov
  • Publication number: 20140024682
    Abstract: This invention relates to novel substituted nitrocatechol derivatives, their use in the treatment of some central and peripheral nervous system disorders and pharmaceutical compositions containing them.
    Type: Application
    Filed: August 30, 2013
    Publication date: January 23, 2014
    Applicant: BIAL - PORTELA & CA, S.A.
    Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto dos Santos Ferreira, Patricio Manuel V. A. Soares da Silva
  • Publication number: 20140018335
    Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a pyridine ring, a furan ring, or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents —C(?O)—NH—SO2R6, an acidic 5-membered hetero ring group, or the like; R2 represents an optionally substituted phenyl group, an optionally substituted 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], and a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.
    Type: Application
    Filed: January 24, 2012
    Publication date: January 16, 2014
    Applicant: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
  • Patent number: 8618139
    Abstract: The present invention relates to novel oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 11, 2011
    Date of Patent: December 31, 2013
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha Bin Im
  • Publication number: 20130338196
    Abstract: Compounds are disclosed that are effective in inhibition of fatty acid amide hydrolase, an enzyme responsible for catabolism of endogenous cannabinoids such as anandamide. The compounds are useful as analgesic compounds and as sleep-inducing compounds, that can be orally administered, and that can have a relatively long duration of effect. Methods of preparation of the compounds are also provided. The compounds are conformationally constrained analogs of heterocyclylketones such as oxazolylketones.
    Type: Application
    Filed: February 3, 2012
    Publication date: December 19, 2013
    Applicant: The Scripps Research Institute
    Inventor: Dale L. Boger
  • Publication number: 20130331416
    Abstract: The invention relates to the use of an oxodiazolyl compound (I) for the preparation of a medicament for the prevention or treatment of central and peripheral nervous system associated disorders, wherein said medicament is administered according to a dosing regimen having a dosing periodicity ranging from about twice a day to about once every other day.
    Type: Application
    Filed: July 25, 2013
    Publication date: December 12, 2013
    Applicant: BIAL - PORTELA & CA, S.A.
    Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto dos Santos Ferreira, Patricio Manuel Vieira Araujo Soares da Silva
  • Publication number: 20130317065
    Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a benzene ring, a pyridine ring, or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; Z represents —C(?O)—NHSO2R6, an acidic 5-membered hetero ring group, or the like; R1 represents a hydrogen atom or the like; R2 represents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.
    Type: Application
    Filed: January 24, 2012
    Publication date: November 28, 2013
    Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
  • Patent number: 8592460
    Abstract: The invention relates to novel amino-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
    Type: Grant
    Filed: February 29, 2008
    Date of Patent: November 26, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jorg Velker
  • Publication number: 20130303514
    Abstract: The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, and R4 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
    Type: Application
    Filed: January 18, 2012
    Publication date: November 14, 2013
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Martin Bolli, Cyrille Lescop, Boris Mathys, Keith Morrison, Claus Mueller, Oliver Nayler, Beat Steiner
  • Patent number: 8580824
    Abstract: The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, R4, R5, and R6 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
    Type: Grant
    Filed: September 6, 2007
    Date of Patent: November 12, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
  • Publication number: 20130296166
    Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.
    Type: Application
    Filed: April 3, 2013
    Publication date: November 7, 2013
    Inventors: Deryck J. Williams, Matt W. Dimmic, William P. Haakenson, Al Wideman, Barry J. Shortt, Tim Cheeseright, Michael J. Crawford