Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The Additional Six-membered Hetero Ring (e.g., Nicotinic Acid, Etc.) Patents (Class 544/365)
  • Patent number: 10322115
    Abstract: Methods for treating non-systemic deficiencies associated with diabetes using 2-amino substituted nicotinamides or their pharmaceutically acceptable salts.
    Type: Grant
    Filed: September 12, 2017
    Date of Patent: June 18, 2019
    Assignee: Neuralstem, Inc.
    Inventor: Karl K. Johe
  • Patent number: 9572807
    Abstract: Although it is known that certain benzylpiperazine-aminopyridines or open chain forms thereof are effective in stimulating neural growth in in vitro tests, it has now been surprisingly found that administering these compounds in a dosage range of 10 mg/day-130 mg/day over 25-35 days is effective in treating Major Depressive Disorder (MDD) such that statistically significant results can be obtained with samples of only six subjects.
    Type: Grant
    Filed: June 15, 2015
    Date of Patent: February 21, 2017
    Assignee: Neuralstem, Inc.
    Inventor: Karl K. Johe
  • Patent number: 9481649
    Abstract: The invention describes an improved synthesis for piperazine derivatized with nicotinic acid and a benzyl moiety. The product compounds are useful for treatment of neurological conditions.
    Type: Grant
    Filed: December 9, 2015
    Date of Patent: November 1, 2016
    Assignee: NEURALSTEM, INC.
    Inventors: Sripathy Venkatraman, Syed Mahmood, Bingidimi I. Mobele, Olga Lapina, Kellie Vercoe, Ying Li, Jonathan Salsbury, Mark McLaws
  • Publication number: 20150148352
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of angina and cardiovascular conditions may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of chronic aneurysm, angina, atherosclerosis, cerebrovascular accident (stroke), cerebrovascular disease, congestive heart failure, coronary artery disease, myocardial infarction (heart attack), peripheral vascular disease, aortic dissection, aortic stenosis, arrhythmia (irregular heartbeat), atrial fibrillation, cardiomyopathy, chest pain, claudication, congenital heart disease.
    Type: Application
    Filed: July 21, 2013
    Publication date: May 28, 2015
    Inventor: Mahesh Kandula
  • Publication number: 20150141397
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Application
    Filed: August 5, 2014
    Publication date: May 21, 2015
    Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. McMahon, Jay Powers, Sreenivas Punna, Ju Yang
  • Publication number: 20150133467
    Abstract: Provided is a screening method with which it is possible to determine the cause of a decrease or an increase in the amount of a target protein that is expressed by a cell. One or a plurality of embodiments include: conducting cultivation that includes bringing an assay cell into contact with a test substance, and measuring a relative amount (A) of the target protein in relation to an internal standard; conducting cultivation in which an assay cell is not brought into contact with a test substance, and measuring a relative amount (B) in relation to an internal standard; comparing the relative amount (A) and the relative amount (B); and, based on the comparison, selecting a candidate substance that induces instability and/or stability in the target protein.
    Type: Application
    Filed: June 6, 2013
    Publication date: May 14, 2015
    Applicant: KYOTO UNIVERSITY
    Inventors: Masatoshi Hagiwara, lsao Kii, Takamitsu Hosoya, Yuto Sumida, Suguru Yoshida
  • Patent number: 9018376
    Abstract: The invention relates to various new polymorphic forms of manidipine and pharmaceutically acceptable salts thereof. The invention also relates to processes for the preparation of the polymorphic forms of manidipine and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: April 28, 2015
    Assignee: Cipla Limited
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Maruti Ganpati Ghagare
  • Publication number: 20150087635
    Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Application
    Filed: December 4, 2014
    Publication date: March 26, 2015
    Inventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
  • Patent number: 8987248
    Abstract: The invention relates to novel substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular disorders and tumor disorders.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: March 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Mario Jeske, Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Kersten Matthias Gericke
  • Publication number: 20150080365
    Abstract: This invention relates to certain heteroaryl compounds for use as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of helminth infections and the treatment of parasitosis 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 pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 19, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Publication number: 20150080351
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Solomon Ungashe, John J. Wright, Andrew Pennell, Zheng Wei
  • Publication number: 20150050237
    Abstract: The present invention relates to the field of anti-mycobacterial therapeutics, in particular the treatment of tuberculosis, especially including pulmonary multidrug-resistant tuberculosis (MDR-TB), with applications in extensively drug-resistant tuberculosis (XDR-TB) and extremely drug-resistant tuberculosis (XXDR-TB), preferably in combination therapy.
    Type: Application
    Filed: March 13, 2013
    Publication date: February 19, 2015
    Inventors: Vasu Nair, Maurice O. Okello, Machhindra G. Gund, Byung I. Seo, Pankajkumar R. Singh, Naveen K. Mangu
  • Publication number: 20150005315
    Abstract: Provided are compounds represented by the formula: where R, Y3, R1, R2, R3, R4, R6, G, R7, E1, E2, A, B, W, X, Y and Z are as defined herein.
    Type: Application
    Filed: December 10, 2012
    Publication date: January 1, 2015
    Applicant: RESEARCH TRIANGLE INSTITUTE
    Inventors: Frank I. Carroll, James B. Thomas, Hernan A. Navarro, S. Wayne Mascarella, Scott P. Runyon, Chunyang Jin, Chad M. Kormos
  • Publication number: 20140371195
    Abstract: The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Marc Labelle, Thomas Boesen, Mukund Mehrotra, Qasim Khan, Farman Ullah
  • Publication number: 20140315912
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor. (I).
    Type: Application
    Filed: July 18, 2011
    Publication date: October 23, 2014
    Inventors: Gregori J. Morriello, Harvey R. Wendt, Scott D. Edmondson
  • Publication number: 20140309192
    Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts, solvates, and hydrates thereof: that are useful in methods of treatment and alleviation of diseases and disorders of the heart, brain, kidney, immune, and reproductive system resulting from ischemia, or reperfusion subsequent to ischemia, and any downstream complication(s) related thereto. The present invention further relates to methods of treatment and alleviation of diseases and disorders of the vasculature resulting from vasoconstriction or hypertension and any downstream complication(s) resulting from elevated blood pressure and/or reduced tissue perfusion.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 16, 2014
    Inventors: Thuy-Anh Tran, Anthony C. Blackburn, Bryan A. Kramer, Maiko Nagura, Carleton R. Sage, Young-Jun Shin, Ning Zou
  • Publication number: 20140309228
    Abstract: The present disclosure provides substituted pyridine and pyrimidine compounds of Formula (I): A1-X-A2-Z-R1 (I) and the pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein A, X, A, Z, and R are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Application
    Filed: October 30, 2012
    Publication date: October 16, 2014
    Applicant: Purdue Pharma L.P.
    Inventor: John J. Engel
  • Patent number: 8859546
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, A, B, Z, n, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: October 14, 2014
    Assignee: AbbVie Inc.
    Inventors: Anil Vasudevan, Thomas D. Penning, Marina Pliushchev
  • Patent number: 8853218
    Abstract: The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the GPR38 receptor.
    Type: Grant
    Filed: April 2, 2009
    Date of Patent: October 7, 2014
    Assignee: Glaxo Group Limited
    Inventors: Darren Jason Mitchell, Jonathan Thomas Seal, Mervyn Thompson, Susan Marie Westaway, Samantha Louisa Brown
  • Patent number: 8835419
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: September 16, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. MacMahon, Jay Powers, Sreenivas Punna, Ju Yang
  • Publication number: 20140256711
    Abstract: Disclosed are an anti-angiogenic compound, represented by Chemical Formula I, or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutically acceptable composition including the same. Because the compound of Chemical Formula I potently suppresses the angiogenesis, the compound of Chemical Formula I is applicable to the prevention and treatment of diseases caused by aberrant activity of vascular endothelial growth factor, and available as an anti-angiogenic agent.
    Type: Application
    Filed: July 27, 2012
    Publication date: September 11, 2014
    Applicant: Boryung Pharmaceutical Co., Ltd.
    Inventors: Ji Han Kim, Je Hak Kim, Joon Kwang Lee, Hahn-Sun Jung, Nam Seok Han, Yong Park, Seung-Hoon Kang, Hee Jin Jeong, Kyung-Tae Lee, Hye Eun Choi, Yong Ha Chi, Joo Han Lee, Soo Heui Paik
  • Patent number: 8815866
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: January 9, 2013
    Date of Patent: August 26, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Francois Maltais, Guy W. Bemis, Tiansheng Wang, Juan-Miguel Jimenez, Luca Settimo, Stephen Young, Dean Boyall, Damien Fraysse, Christopher John Davis
  • Publication number: 20140200225
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 17, 2014
    Applicant: ORION CORPORATION
    Inventors: Rajeev GOSWAMI, Anil Kumar VUPPALA, Ramesh VELUDANDI, Ramesh SISTLA, Chakshusmathi GHADIYARAM, Muralidhara RAMACHANDRA
  • Patent number: 8759352
    Abstract: The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R1 is (C1-8)alkyl, (C3-8)cycloalkyl or (C3-8)cycloalkyl(C1-3)alkyl, each of which may be substituted by hydroxy, cyano or halogen; R2 represents 1 or 2 optional halogens; R3 is (C1-6)alkyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5- or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholester
    Type: Grant
    Filed: August 26, 2009
    Date of Patent: June 24, 2014
    Assignees: Merck Sharp & Dohme B.V., Pharmacopeia LLC.
    Inventors: Andrew John Cooke, David Jonathan Bennett, Andrew Stanley Edwards, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Koc-Kan Ho, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer
  • Publication number: 20140163017
    Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 19, 2013
    Publication date: June 12, 2014
    Applicant: UNIVERSITY OF UTAH
    Inventors: Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
  • Patent number: 8722930
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: May 13, 2014
    Assignee: Orion Corporation
    Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
  • Publication number: 20140121213
    Abstract: In general, the present invention relates to uses of voltage-gated sodium channel blocker compounds, which include corresponding precursors, intermediates, monomers and dimers, corresponding pharmaceutical compositions, compound preparation and treatment methods for respiratory and respiratory tract diseases. In particular, the present invention also relates to methods and uses for treatment of respiratory or respiratory tract diseases, which comprises administering to a subject in need thereof an effective amount of a compound of the present invention.
    Type: Application
    Filed: July 3, 2012
    Publication date: May 1, 2014
    Inventors: Jeffrey Charles Boehm, Roderick S. Davis, Jeffrey Kerns, Guoliang Lin, Robert D. Murdoch, Hong NIE
  • Publication number: 20140107105
    Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Application
    Filed: December 18, 2013
    Publication date: April 17, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
  • Publication number: 20140093513
    Abstract: The invention relates to new methods of modulating cholesterol by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) with fatty acid derivatives; and new methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid derivative. The present invention is also directed to fatty acid bioative derivatives and their use in the treatment of metabolic diseases.
    Type: Application
    Filed: May 24, 2013
    Publication date: April 3, 2014
    Applicant: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Chi B. Vu
  • Patent number: 8664223
    Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: March 4, 2014
    Assignee: Janssen Pharmaceutica N.V
    Inventors: Laurence Françoise Bernadette Marconnet-Decrane, Sandrine Françoise Dominique Gaurrand, Patrick René Angibaud
  • Publication number: 20140038979
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: October 14, 2013
    Publication date: February 6, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristof VAN EMELEN, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noelle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviene Van Heusden
  • Patent number: 8637520
    Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: January 28, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
  • Publication number: 20130345211
    Abstract: The invention relates to substituted pyridine compounds of Formula I: (I) or a pharmaceutically acceptable salt, prodrug, or solvate thereof wherein A1, X, A2, R1a, R1b, R1c, G, and z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: July 15, 2011
    Publication date: December 26, 2013
    Applicant: Purdue Pharma L.P.
    Inventors: Donald J. Kyle, Chiyou Ni, Minnie Park, Laykea Tafesse
  • Publication number: 20130317041
    Abstract: The present invention relates to benzylpiperazine derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the preparation of medicaments suitable for the treatment of gastrointestinal disorders.
    Type: Application
    Filed: August 5, 2013
    Publication date: November 28, 2013
    Applicant: Glaxo Group Limited
    Inventors: Christopher Norbert JOHNSON, David Timothy MacPherson, Steven James Stanway, Geoffrey Stemp, Mervin Thompson, Susan Marie Westaway
  • Publication number: 20130303526
    Abstract: The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, A1, A2, E, G, Z1, and Z2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: September 16, 2011
    Publication date: November 14, 2013
    Applicant: Purdue Pharma L.P.
    Inventors: Chiyou NI, Bin Shao, Laykea Tafesse, Jiangchao Yao, Jianming Yu, Xiaoming Zhou
  • Publication number: 20130267702
    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: Application
    Filed: March 13, 2013
    Publication date: October 10, 2013
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Publication number: 20130267701
    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: Application
    Filed: March 13, 2013
    Publication date: October 10, 2013
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Publication number: 20130252957
    Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.
    Type: Application
    Filed: December 28, 2012
    Publication date: September 26, 2013
    Applicant: ELAN PHARMACEUTICALS, INC.
    Inventors: Ying-Zi Xu, Shendong Yuan, David Wone, Andrei Konradi
  • Patent number: 8536183
    Abstract: The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.
    Type: Grant
    Filed: August 7, 2012
    Date of Patent: September 17, 2013
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: Paul John Beswick, Alister Campbell, Andrew Cridland, Robert James Gleave, Jag Paul Heer, Neville Hubert Nicholson, Lee William Page, Sadie Vile
  • Patent number: 8530478
    Abstract: The present invention relates to novel piperazine derivatives (I); to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.
    Type: Grant
    Filed: July 15, 2009
    Date of Patent: September 10, 2013
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: Paul John Beswick, Alister Campbell, Andrew Peter Cridland, Robert James Gleave, Jag Paul Heer, Neville Hubert Nicholson, Lee William Page, Sadie Vile
  • Publication number: 20130210811
    Abstract: Provided are picolinamide and pyrimidine-4-carboxamide compounds, a method for preparing the same, a pharmaceutical composition containing the same, and a medical use using the compound as an agent for preventing, regulating, and treating diseases related to regulation of glucocorticoids by using selective inhibitory activity of the compound for an 11?-HSD1 enzyme. The picolinamide and pyrimidine-4-carboxamide compounds of the present invention are selective inhibitors of human-derived 11?-HSD1 enzymes, and are useful in an agent for preventing, regulating, and treating diseases related to glucocorticoid regulation in which human-derived 11?-HSD1 enzymes are involved, for example, metabolic syndromes such as, type 1 and type 2 diabetes, diabetes later complications, latent autoimmune diabetes adult (LADA), insulin tolerance syndromes, obesity, impaired glucose tolerance (IGT), impaired fasting glucose (IFG), damaged glucose tolerance, dyslipidemia, atherosclerosis, hypertension, etc.
    Type: Application
    Filed: May 4, 2011
    Publication date: August 15, 2013
    Applicant: SK CHEMICALS CO., LTD.
    Inventors: Je Ho Ryu, Shin Ae Kim, Keun Ho Ryu, Jae Sun Kim, Nam Ho Kim, Hye Young Han, Yong Hyuk Kim, Won-No Youn, Yoon-Jung Lee, Hyun Joo Son, Bong-Yong Lee, Sung Hoon Park, Ju Young Lee, Hyun Jung Lee, Hoe Chul Jung, Young Ah Shin, Jung A Lee, Bo Ram Lee, Joon Ho Sa
  • 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
  • Publication number: 20130203987
    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: Application
    Filed: March 13, 2013
    Publication date: August 8, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventor: Rigel Pharmaceuticals, Inc.
  • Publication number: 20130190488
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Application
    Filed: December 12, 2012
    Publication date: July 25, 2013
    Applicant: Abbott Laboratories
    Inventor: Abbott Laboratories
  • Publication number: 20130172315
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Application
    Filed: November 30, 2012
    Publication date: July 4, 2013
    Applicant: ChemoCentryx, Inc.
    Inventor: ChemoCentryx, Inc.
  • Publication number: 20130164259
    Abstract: The present invention relates to 1,4-Substituted Piperazine Derivatives, compositions comprising one or more 1,4-Substituted Piperazine Derivatives, and methods of using the 1,4-Substituted Piperazine Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: December 20, 2010
    Publication date: June 27, 2013
    Inventors: Cliff C. Cheng, Xiaohua Huang, Gerald W. Shipps, JR.
  • Publication number: 20130143898
    Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: January 10, 2012
    Publication date: June 6, 2013
    Applicant: JANSSEN PHARMACEUTICA N.V.
    Inventors: Laurence Françoise Bernadette MARCONNET-DECRANE, Sandrine Françoise Dominique Gaurrand, Patrick René Angibaud
  • Publication number: 20130137704
    Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
    Type: Application
    Filed: January 22, 2013
    Publication date: May 30, 2013
    Applicant: Addex Pharma, SA
    Inventor: Addex Pharma, SA
  • Publication number: 20130137703
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: January 9, 2013
    Publication date: May 30, 2013
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20130131079
    Abstract: The present invention is directed to a compound of formula (I) for use in a method to treat or ameliorate amyloid or tau pathologies, such as Alzheimer's disease, or symptoms thereof. The invention is also directed to new compounds of formula (I), of subformula (II), (III), (IV), or (V).
    Type: Application
    Filed: May 23, 2011
    Publication date: May 23, 2013
    Applicant: FAES FARMA, S.A.
    Inventors: Francisco Ledo Gómez, Ana Muñoz Muñoz, Carmen Pumar Durán