The Additional Hetero Ring Is Attached Indirectly To The Morpholine Ring By An Acyclic Chain Having A Hetero Atom As A Chain Member Patents (Class 514/237.2)
  • Patent number: 9274117
    Abstract: The use of SIRT7 (sirtuin 7) as a marker for diagnosis of liver cancer is described. The disclosure variously relates to a liver cancer diagnostic marker including SIRT7 gene, a liver cancer diagnostic composition, a kit and microarray including the same, and a method of diagnosing liver cancer using the same. Also described is a method for screening a substance capable of treating liver cancer by inhibiting the expression of SIRT7 gene or protein, and a composition for preventing or treating liver cancer, which includes such substance. The disclosure further relates to the use of SIRT7 gene as a cancer diagnostic marker and the anticancer use of inhibition of SIRT7 expression, as well as the use of the specific miRNA to regulate the cell cycle and inhibit tumor growth by the expression of SIRT7 gene.
    Type: Grant
    Filed: December 21, 2013
    Date of Patent: March 1, 2016
    Assignee: CATHOLIC UNIVERSITY INDUSTRY ACADEMIC
    Inventors: Suk-Woo Nam, Jeong-Kyu Kim
  • Patent number: 9140691
    Abstract: A diagnostic test and method is provided comprising mixing blood or another biological fluid sample with a test compound and spotting the blood on filter paper for subsequent analysis of the effect of the test compound on the blood. The biological fluid can be a cerebrospinal fluid, a peritoneal fluid, a cyst fluid, an amniotic fluid, a lavage fluid, a saliva, a cell extract or a tissue extract. The compound is chosen among an amino acid, a peptide, a protein, a carbohydrate, an oligosaccharide, a polysaccharide, a glycoprotein, a lipid, a lipoprotein, a glycosaminoglycan, a hormone, a steroid, a vitamin, a low molecular weight synthetic or natural compound which influences the blood to cause an alteration of its composition, e.g., a toxin, allergen, autoantigen, bacterial protein or polysaccharide, viral protein, fungal protein or polysaccharide, parasitic protein or polysaccharide, bacterial lipopolysaccharide or any other compound relevant to diseases.
    Type: Grant
    Filed: November 30, 2007
    Date of Patent: September 22, 2015
    Assignee: Statens Serum Institut
    Inventors: Gunnar Houen, David Hougaard, Kristin Skogstrand, Charlotte Svaerke Jørgensen
  • Patent number: 9079859
    Abstract: The present invention provides methods for inhibiting growth and proliferation of HIF pathway proficient cells by administering GLUT1 inhibitors of the invention to HIF pathway proficient cells.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: July 14, 2015
    Assignees: AUCKLAND UNISERVICES LIMITED, THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY, RUGA CORPORATION
    Inventors: John Irwin, Patrick Sutphin, Denise Chan, Sandra Turcotte, Amato Giaccia, Edwin Lai, Olga Razorenova, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Raymond Tabibiazar
  • Patent number: 9018206
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: April 28, 2015
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Publication number: 20150111879
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 24, 2014
    Publication date: April 23, 2015
    Applicants: CURIS, INC., GENENTECH, INC.
    Inventors: Janet L. GUNZNER, Daniel P. SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
  • Publication number: 20150105393
    Abstract: The present invention relates to amide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 16, 2015
    Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Mikio Morita
  • Patent number: 8980907
    Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: March 17, 2015
    Assignee: The Regents of the University of Michigan
    Inventors: James R. Baker, Jr., Xue-min Cheng, Abraham F. L. Van Der Spek, Baohua Mark Huang, Thommey P. Thomas
  • Publication number: 20150065507
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 5, 2015
    Applicant: Glaxo Group Limited
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Publication number: 20150038484
    Abstract: The present invention relates to indole and indazole compounds of Formula (I) that activate 5? adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Applicant: PFIZER INC.
    Inventors: Samit Bhattacharya, Kimberly Cameron, Matthew Dowling, Dilinie Fernando, David Ebner, Kevin Filipski, Daniel Kung, Esther Lee, Aaron Smith, Meihua Tu
  • Publication number: 20150038492
    Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.
    Type: Application
    Filed: August 12, 2014
    Publication date: February 5, 2015
    Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
  • Publication number: 20150018341
    Abstract: The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.
    Type: Application
    Filed: December 28, 2012
    Publication date: January 15, 2015
    Applicant: CENTAURUS BIOPHARMA CO., LTD.
    Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Rong Yu, Wei Hu, Na Zhao, Yong Peng, Hong Luo, Yongxin Han
  • Publication number: 20150011553
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Application
    Filed: July 3, 2014
    Publication date: January 8, 2015
    Inventors: Ulrich GÖRGENS, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
  • Publication number: 20150005296
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Application
    Filed: September 18, 2014
    Publication date: January 1, 2015
    Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, JR.
  • Publication number: 20140357612
    Abstract: Compounds active on protein kinases and methods for regulating protein kinase pathways are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: May 29, 2014
    Publication date: December 4, 2014
    Inventors: Chao Zhang, Klaus-Peter Hirth, Prabha N. Ibrahim, Marika Nespi, Songyuan Shi, Wayne Spevak, Gaston G. Habets, Betsy Burton
  • Publication number: 20140357599
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
  • 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
  • Patent number: 8889635
    Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: November 18, 2014
    Assignee: The Regents of The University of Michigan
    Inventors: James R. Baker, Jr., Xue-min Cheng, Abraham F. L. Van Der Spek, Baohua Mark Huang, Thommey P. Thomas
  • Patent number: 8889665
    Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R3 and L are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: November 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ioannis Sapountzis, Peter Ettmayer, Christian Klein, Andreas Mantoulidis, Steffen Steurer, Irene Waizenegger
  • Publication number: 20140336158
    Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
    Type: Application
    Filed: July 25, 2014
    Publication date: November 13, 2014
    Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
  • Publication number: 20140336153
    Abstract: The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particularly FabI inhibitors. Formula (I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
    Type: Application
    Filed: November 29, 2012
    Publication date: November 13, 2014
    Inventors: Mohamed Takhi, Subramanya Hosahalli, Sunil Kumar Panigrahi, Muni Kumar Mahadari, Chandrashekar Reddy Kottam, Noorsaadah Abd Rahman, Rohana Yusof
  • Publication number: 20140336193
    Abstract: The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Inventors: Donald W. Landry, Shi-Xian Deng, Stevan Pecic, Kirsten Alison Rinderspacher
  • Publication number: 20140323412
    Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 30, 2014
    Inventors: Bronislava Gedulin, Michael Grey, Niall O'Donnell
  • Publication number: 20140323486
    Abstract: The present invention provides a compound of the following formula, racemates, enantiomers and salts thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
    Type: Application
    Filed: December 21, 2012
    Publication date: October 30, 2014
    Inventors: Edward Malcolm Tyndall, Lloyd George Czaplewski, Colin William Gordon Fishwick, Andrew Ian Yule, Jeffrey Peter Mitchell, Kelly Helen Anderson, Gary Robert William Pitt
  • 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
  • Publication number: 20140301999
    Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.
    Type: Application
    Filed: June 23, 2014
    Publication date: October 9, 2014
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
  • Publication number: 20140288076
    Abstract: The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Applicant: NOVARTIS AG
    Inventors: Paul A. Barsanti, Cheng Hu, Jeff Jin, Robert Keyes, Robert Kucejko, Xiaodong Lin, Yue Pan, Keith B. Pfister, Martin Sendzik, James Sutton, Lifeng Wan
  • Publication number: 20140271734
    Abstract: Provided herein are methods of treating or ameliorating Barrett's esophagus by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Provided herein are methods of treating or ameliorating gastroesophageal reflux disease (GERD) by administering to an individual in need thereof a therapeutically effective amount of an ASBTI or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating symptoms or complications associated with Barrett's esophagus or GERD comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Inventors: Bronislava GEDULIN, Michael GREY, Niall O'DONNELL, Bradley T. KELLER
  • Publication number: 20140275016
    Abstract: Described are compounds of Formula 1 which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Timothy Malcolm Caldwell, Thiwanka Samarakoon, Lakshminarayana Vogeti, Michael D. Kaufman, William C. Patt, YuMi Ahn
  • Publication number: 20140275090
    Abstract: Provided herein are methods of treating or ameliorating primary sclerosing cholangitis and inflammatory bowel disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating primary sclerosing cholangitis comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Lumena Pharmaceuticals, Inc.
    Inventors: Bronislava GEDULIN, Michael GREY, Niall O'DONNELL, Bradley T. KELLER
  • 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
  • Publication number: 20140256728
    Abstract: The present invention relates to the use of predominantly known pyridyl carboxamide derivatives as nematicides, compositions containing such compounds and methods for the control of nematodes.
    Type: Application
    Filed: October 29, 2012
    Publication date: September 11, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jörg Nico Greul, Heiko Rieck, Christian Paulitz, Matthias Riedrich, Ralf Dunkel, Arianna Martelletti, Alexander Sudau, Peter Lösel, Olga Malsam, Arnd Voerste, Hans-Georg Schwarz, Ulrich Görgens, Kerstin Ilg, Michael Maue, Pierre-Yves Coqueron, Philippe Desbordes, Philippe Meresse, Stephanie Gary, Pierre Cristau, David Bernier
  • Publication number: 20140243341
    Abstract: Antiviral protease inhibitors, including peptidyl aldehydes, peptidyl ?-ketoamides, peptidyl bisulfite salts, and peptidyl heterocycles, are disclosed, along with related antiviral compounds, and methods of using the same to treat or prevent viral infection and disease. The compounds possess broad-spectrum activity against viruses that belong to the picornavirus-like supercluster, which include important human and animal pathogens including noroviruses, enteroviruses, poliovirus, foot-and-mouth disease virus, hepatitis A virus, human rhinovirus (cause of common cold), human coronavirus (another cause of common cold), transmissible gastroenteritis virus, murine hepatitis virus, feline infectious peritonitis virus, and severe acute respiratory syndrome coronavirus.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 28, 2014
    Inventors: Kyeong-Ok Chang, Yunjeong Kim, William C. Groutas, Duy Hua, Linda J. Saif
  • Publication number: 20140235642
    Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: AMGEN INC.
    Inventors: James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Holger Monenschein, Thomas T. Nguyen, Nobuko Nishimura, Wenge Zhong
  • Publication number: 20140221334
    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: April 10, 2014
    Publication date: August 7, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Juan-Miguel Jimenez, Guy William Bemis, Francois Maltais, Tiansheng Wang, Ronald Marcellus Alphonsus Knegtel, Christopher John Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Paul Mortimore
  • Patent number: 8778941
    Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: July 15, 2014
    Assignee: AMGEN Inc.
    Inventors: James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Holger Monenschein, Thomas T. Nguyen, Nobuko Nishimura, Wenge Zhong
  • Patent number: 8741894
    Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: June 3, 2014
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Garrett Thomas Potter, Jared Andrew Forrester
  • Publication number: 20140148458
    Abstract: The present invention relates to a heterocyclic compound of the general formula (I) and their use and preparation, methods of making the compounds, compositions containing at least one of said compounds, and methods of treatment using at least one compound.
    Type: Application
    Filed: January 31, 2014
    Publication date: May 29, 2014
    Inventors: Sean Colm Turner, Margaretha Henrica Maria Bakker, Kent D. Stewart
  • Publication number: 20140135304
    Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors.
    Type: Application
    Filed: June 7, 2011
    Publication date: May 15, 2014
    Applicant: SUVEN LIFE SCIENCES LIMITED
    Inventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Ramasastri Kambhampati, Amol Dinakar Deshpande, Adi Reddy Dwarampudi, Narasimhareddy Gangadasari, Sangram Keshari Saraf, Vishwottam Nagaraj Kandikere, Pradeep Jayarajan, Ishtiyaque Ahmad, Mohmadsadik Abdulhamid Mulla, Venkateswarlu Jasti
  • Publication number: 20140135329
    Abstract: The present invention provides pyridine and pyrazine derivatives 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: June 20, 2013
    Publication date: May 15, 2014
    Inventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
  • Publication number: 20140128397
    Abstract: The present invention provides methods for inhibiting growth and proliferation of HIF pathway proficient cells by administering GLUT1 inhibitors of the invention to HIF pathway proficient cells.
    Type: Application
    Filed: January 20, 2012
    Publication date: May 8, 2014
    Inventors: John Irwin, Patrick Sutphin, Denise Chan, Sandra Turcotte, Amato Giaccia, Edwin Lai, Olga Razorenova, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Raymond Tabibiazar
  • Patent number: 8716288
    Abstract: The present invention relates to a novel pharmaceutical composition of benproperine derivatives for preventing and treating angiogenesis-related diseases. The benproperine derivatives and pharmaceutically acceptable salts thereof according to the present invention inhibit cancer cell migration and the angiogenesis of vascular endothelial cells, and therefore can be effectively used not only as an anticancer agent, but also as an agent for preventing and treating diseases caused by abnormal angiogenesis, such as diabetic retinopathy and corneal transplant rejection.
    Type: Grant
    Filed: May 10, 2013
    Date of Patent: May 6, 2014
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Byoung Mog Kwon, Dong Cho Han, Dae Seop Shin, Young Min Han
  • Publication number: 20140121210
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor.
    Type: Application
    Filed: January 8, 2014
    Publication date: May 1, 2014
    Applicant: HELSINN HEALTHCARE SA
    Inventors: Silvina GARCIA RUBIO, Claudio PIETRA, Claudio GIULIANO, Zhigang LI
  • Publication number: 20140100224
    Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.
    Type: Application
    Filed: June 26, 2013
    Publication date: April 10, 2014
    Applicants: The University of North Carolina at Chapel Hill, U.S. Government represented by the Department of Veterans Affairs, The Regents of the University of California
    Inventors: Frank M. Longo, Stephen M. Massa
  • Publication number: 20140100212
    Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 10, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Xialing Guo, Zhen Zhu
  • Publication number: 20140080770
    Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 17, 2013
    Publication date: March 20, 2014
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi MIYAZAKI, Junko OKABE, Kosuke YASUDA, Iwao TAKAMURO, Osamu SAKURAI, Tetsuya YANAGIDA, Yutaka HISADA
  • Patent number: 8673912
    Abstract: This invention relates to three crystalline forms of N-[3-fluoro-4-((6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl|oxy)phenyl]-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide. Compound (I), designated as Form A, Form B, and Form C. The invention provides methods for treatment of cancer by exploiting the modulation of protein kinase activity. The invention also provides pharmaceutical compositions containing a crystalline form of Compound (I) and a pharmaceutically acceptable excipient.
    Type: Grant
    Filed: July 16, 2010
    Date of Patent: March 18, 2014
    Assignee: Exelixis, Inc.
    Inventors: Hilary Cannon, David Igo, Tri Tran
  • Publication number: 20140057916
    Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thorsten OOST, Dennnis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
  • Publication number: 20140057882
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and the treatment of certain conditions such as COPD.
    Type: Application
    Filed: October 8, 2013
    Publication date: February 27, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Elisabetta ARMANI, GABRIELE AMARI, LAURA CARZANIGA, CARMELIDA CAPALDI, ORIANA ESPOSITO, GINO VILLETTI, RENATO DE FANTI
  • Publication number: 20140051686
    Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: July 11, 2013
    Publication date: February 20, 2014
    Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
  • Patent number: RE45323
    Abstract: Object of the present invention are novel substituted compounds of the formula 1, wherein A, R1, R2, R3 and R4 are defined as in the description. Another object of the present invention is to provide antagonists of CCR3, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 7, 2014
    Date of Patent: January 6, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Marc Grundl, Horst Dollinger, Riccardo Giovannini, Christoph Hoenke, Matthias Hoffmann, Jan Kriegl, Domnic Martyres, Georg Rast, Peter Seither