The Five-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/143)
  • Patent number: 8367665
    Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.
    Type: Grant
    Filed: April 16, 2009
    Date of Patent: February 5, 2013
    Assignee: Karo Bio AB
    Inventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
  • Publication number: 20130025618
    Abstract: The present invention relates to a cationic 4-aminoindole of general formula (I), addition salts thereof with an acid and solvates thereof: in which: R1 is a linear or branched, saturated C2-C20 alkyl radical, substituted and/or interrupted with a cationic radical. The present invention is also directed towards a process for synthesizing this cationic 4-aminoindole, to the compositions, the uses, the hair dyeing processes and the devices using this cationic 4-aminoindole.
    Type: Application
    Filed: December 6, 2010
    Publication date: January 31, 2013
    Inventor: Aziz Fadli
  • Publication number: 20130029970
    Abstract: The present disclosure relates to compounds of formula I useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: July 9, 2010
    Publication date: January 31, 2013
    Applicant: IRONWOOD PHARMACEUTICALS, INC
    Inventors: Kevin Sprott, Jason Rohde, Takashi Nakai, Bo Peng, John Jeffrey Talley
  • Patent number: 8354406
    Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: January 15, 2013
    Assignee: GlaxoSmithKline LLC
    Inventors: Jianghe Deng, Jeffrey K. Kerns, Qi Jin, Guoliang Lin, Xichen Lin, Michael Lindenmuth, Christopher Neipp, Hong Nie, Sonia M Thomas, Katherine L. Widdowson
  • Patent number: 8338416
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Grant
    Filed: March 16, 2007
    Date of Patent: December 25, 2012
    Assignee: Pharmacylics, Inc.
    Inventors: Joseph J. Buggy, Sriram Balasubramanian, Erik Verner, Vincent W. F. Tai, Chang-Sun Lee
  • Publication number: 20120309757
    Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
    Type: Application
    Filed: June 6, 2012
    Publication date: December 6, 2012
    Applicant: SCRIPPS RESEARCH INSTITUTE, THE
    Inventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
  • Patent number: 8324204
    Abstract: A series of 5,6-dihydro-1-benzothiophen-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Grant
    Filed: June 4, 2007
    Date of Patent: December 4, 2012
    Assignee: UCB Pharma SA
    Inventors: Rikki Peter Alexander, Stuart Bailey, Stephen Brand, Daniel Christopher Brookings, Julien Alistair Brown, Alan Findlay Haughan, Natasha Kinsella, Christopher Lowe, Stephen Robert Mack, William Ross Pitt, Marianna Dilani Richard, Andrew Sharpe, Laura Jane Tait
  • Publication number: 20120295884
    Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: January 2, 2012
    Publication date: November 22, 2012
    Applicant: NOVARTIS AG
    Inventors: Eva ALTMANN, Ulrich HOMMEL, Edwige Liliane Jeanne LORTHIOIS, Juergen Klaus MAIBAUM, Nils OSTERMANN, Jean Quancard, Stefan Andreas RANDL, Olivier ROGEL, Oliver SIMIC, Anna VULPETTI, Veronique Stark-Rogel
  • Publication number: 20120295904
    Abstract: The present embodiments relate to compounds with physiological effects, such as the activation of hematopoietic growth factor receptors. The present embodiments also relate to use of the compounds to treat a variety of conditions, diseases and ailments such as hematopoietic conditions and disorders.
    Type: Application
    Filed: October 12, 2010
    Publication date: November 22, 2012
    Applicant: LIGAND PHARMACEUTICALS INC.
    Inventors: Lin Zhi, Andrew R. Hudson, Cornelis A. Van Oeveren, Steven L. Roach, Bijan Pedram, Yixing Shen, Lino J. Valdez, Jillian Basinger, Virginia Heather Sharron Grant, Jason C. Pickens
  • Patent number: 8304411
    Abstract: Disclosed are new dicycloazaalkane derivates represented by general formula (I), preparation processes and pharmaceutical compositions containing them, and the uses for treatment especially for dipeptidyl peptidase inhibitor (DPP-IV), in which each substitute group of general formula (I) is as defined in specification.
    Type: Grant
    Filed: May 20, 2008
    Date of Patent: November 6, 2012
    Assignees: Jiangsu Hansoh Pharmaceutical Co., Ltd., Shanghai Hengrui Pharmaceutical Co. Ltd.
    Inventors: Peng Cho Tang, Zhigang Lin, Hejun Lu, Fuqiang Zhao, Li Li, Fanglong Yang, Jianghong Fu, Lin Wang, Guangyuan Shen, Dongliang Guan
  • Patent number: 8299066
    Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: October 30, 2012
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masahiro Sakagami, Hiroshi Hashizume, Satoru Tanaka
  • Publication number: 20120252801
    Abstract: The present invention relates to a series of novel compounds which have been shown to possess antifungal activity. The invention therefore relates to the new compounds, methods for their preparation, pharmaceutical compositions comprising them and to the compounds for use as a medicament, more in particular antifungal medicament.
    Type: Application
    Filed: December 15, 2010
    Publication date: October 4, 2012
    Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&D
    Inventors: Dorothée Bardiot, Bruno Cammue, Patrick Chaltin, Arnaud Marchand, Karin Thevissen
  • Publication number: 20120225873
    Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
    Type: Application
    Filed: April 13, 2012
    Publication date: September 6, 2012
    Applicant: Myrexis, Inc.
    Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
  • Publication number: 20120202810
    Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.
    Type: Application
    Filed: April 24, 2012
    Publication date: August 9, 2012
    Applicant: Grunenthal GmbH
    Inventors: Bert NOLTE, Wolfgang SHRÖDER, Klaus LINZ, Werner ENGLBERGER, Hans SCHICK, Heinz GRAUBAUM, Birgit ROLOFF, Sigrid OZEGOWSKI, József BÁLINT, Helmut SONNENSCHEIN
  • Publication number: 20120197014
    Abstract: The present invention generally relates to inhibitors of isoprenylcysteine carboxyl methyltransferase (Icmt), in particularly to compounds that inhibit Icmt activity and pharmaceutical compositions thereof. The invention also relates to methods of disease treatment using the same.
    Type: Application
    Filed: July 30, 2010
    Publication date: August 2, 2012
    Inventors: Jo Lene Leow, Mei-Wang Casey, Patrick J. Casey, Mei Lin Go, Kumar Gorla Suresh
  • Patent number: 8232312
    Abstract: The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
    Type: Grant
    Filed: March 14, 2008
    Date of Patent: July 31, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
  • Publication number: 20120178723
    Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: August 11, 2011
    Publication date: July 12, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
  • Publication number: 20120170098
    Abstract: A photochromic chromene compound having an indeno(2,1-f)naphtho(1,2-b)pyran structure as its basic skeleton, an aryl group or a heteroaryl group at the 6-position carbon atom of the structure and an electron donor group having a Hammett constant ?p of not more than ?0.1 at the 7-position carbon atom.
    Type: Application
    Filed: September 15, 2010
    Publication date: July 5, 2012
    Inventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Mitsuyoshi Sando, Kazuhiro Teranishi
  • Publication number: 20120165320
    Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.
    Type: Application
    Filed: June 22, 2010
    Publication date: June 28, 2012
    Applicant: PANACEA BIOTEC LTD.
    Inventors: Rajseh Jain, Sanjay Trehan, Jagattaran Das, Gurmeet Kaur, Sandeep Kanwar, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
  • Patent number: 8207216
    Abstract: Compounds of formula: and pharmaceutically acceptable salts, esters and solvates thereof, where variables are defined in the specification, useful generally as inhibitors of protein kinases and particularly useful for inhibition of GSK-3. Pharmaceutically compositions and medicaments containing a compound of the invention are provided. The invention provides methods of treatment of protein kinase-related disease, disorders or conditions. The invention provides methods of treatment of GSK-3-related diseases, disorders or conditions.
    Type: Grant
    Filed: June 19, 2009
    Date of Patent: June 26, 2012
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Alan P. Kozikowski, Irina Gaysina
  • Publication number: 20120157437
    Abstract: This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A1 represents a nitrogen atom or C—R3d wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R1 represents H or a C1-8 alkyl group; R2 represents H, a halogen, a C1-8 alkoxy group, or an optionally-substituted benzyloxy group; and R3a, R3b and R3c independently represent H, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group.
    Type: Application
    Filed: February 1, 2012
    Publication date: June 21, 2012
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Nobuo MACHINAGA, Shin Ilmura, Yoshiyuki Yoneda, Jun Chiba, Fumihito Muro, Hideko Hoh, Atsushi Nakayama
  • Patent number: 8198274
    Abstract: This application discloses compounds of generic Formula I: or pharmaceutically acceptable salts thereof, wherein A, R1, R2, R3, R4, Q, X, Y, m, p, and q are defined as described herein, useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Grant
    Filed: July 15, 2009
    Date of Patent: June 12, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Eun Kyung Lee, Ryan Craig Schoenfeld, Robert James Weikert
  • Publication number: 20120122839
    Abstract: The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (I) or (Ia) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (I) or (Ia) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.
    Type: Application
    Filed: January 17, 2012
    Publication date: May 17, 2012
    Applicant: Priaxon AG
    Inventors: Christoph BURDACK, Cedric Kalinski, Vladimir Khazak, Gunther Ross, Lutz Weber
  • Patent number: 8168634
    Abstract: A series of thiazole derivatives which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Grant
    Filed: October 16, 2007
    Date of Patent: May 1, 2012
    Assignee: UCB Pharma S.A.
    Inventors: Rikki Peter Alexander, Julien Alistair Brown, Karen Viviane Lucile Crépy, Stephen Robert Mack
  • Publication number: 20120094995
    Abstract: This invention relates to 2-aza-bicyclo[2.2.1]heptane compounds (and salts thereof), the process for making such a compound and pharmaceutical compositions comprising such a compound. The invention also relates to the use of the compounds for modulating the glycine transporter 1 (GlyT1) and for the treatment of psychosis, cognitive disorders, bipolar disorders, depression disorders, anxiety disorders, post-traumatic stress disorders and pain.
    Type: Application
    Filed: January 27, 2010
    Publication date: April 19, 2012
    Applicant: ASTRAZENECA AB
    Inventors: Jeffrey Scott Albert, Donald Andisik, Cristobal Alhambra, Todd Andrew Brugel, Glen E Ernst, William Frietze, Lindsay Hinkley, Jeffrey Gilbert Varnes, Xia Wang, Hui Xiong
  • Publication number: 20120065191
    Abstract: The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to substrates of the FAAH enzyme, and methods of treatment or prevention using the compounds and compositions.
    Type: Application
    Filed: December 23, 2009
    Publication date: March 15, 2012
    Applicant: BIAL - PORTELA & Cª, S.A.
    Inventors: Laszlo Erno Kiss, David Alexander Learmonth, Carla Patrícia da Costa Pereira Rosa, Rita Gusmão de Noronha, Pedro Nuno Leal Palma, Patrício Manuel Vieira Araújo Soares da Silva, Alexander Beliaev
  • Patent number: 8129372
    Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.
    Type: Grant
    Filed: April 20, 2009
    Date of Patent: March 6, 2012
    Assignee: Shionogi & Co., Ltd.
    Inventor: Masahiro Sakagami
  • Patent number: 8119623
    Abstract: The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (I) or (Ia) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (I) or (Ia) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.
    Type: Grant
    Filed: September 15, 2009
    Date of Patent: February 21, 2012
    Assignee: Priaxon AG
    Inventors: Christoph Burdack, Cedric Kalinski, Vladimir Khazak, Gunther Ross, Lutz Weber
  • Publication number: 20120040958
    Abstract: The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: October 24, 2011
    Publication date: February 16, 2012
    Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
  • Publication number: 20120028963
    Abstract: The present invention relates to hydroxamate derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof, the use thereof for preparing pharmaceutical compositions, pharmaceutical compositions containing the same, a method of treating disease using the compositions, and a method for preparing the hydroxamate derivatives.
    Type: Application
    Filed: March 18, 2010
    Publication date: February 2, 2012
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: Sung Sook Lee, Kyung Joo Lee, Chang Sik Lee, Hyun Mo Yang, Do Hoon Kim, Dae Kyu Choi, Ho Jin Choi, Dal Hyun Kim, In Chang Hwang, Mi Jeong Kim, Byeong Hoon Han
  • Publication number: 20120020920
    Abstract: The present invention relates to a fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
    Type: Application
    Filed: February 24, 2011
    Publication date: January 26, 2012
    Applicant: Japan Tobacco Inc.
    Inventors: Ryo Mizojiri, Shintaro Hirashima, Takahiro Oka, Kenta Aoki, Satoru Noji, Izuru Ando, Toshihiro Sato, Yasushi Niwa
  • Publication number: 20120022057
    Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I).
    Type: Application
    Filed: March 16, 2010
    Publication date: January 26, 2012
    Applicant: Schering Corporation
    Inventors: Gang Zhou, Grant Wishart, Pauline C. Ting, Robert G. Aslanian, Nicolas Zorn, Jianhua Cao
  • Publication number: 20120022063
    Abstract: The invention relates to (among other things) oligomer-cannabinoid conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated cannabinoid compounds.
    Type: Application
    Filed: February 6, 2009
    Publication date: January 26, 2012
    Applicant: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, C. Simone Jude-Fishburn, Guy Lalonde
  • Patent number: 8097623
    Abstract: There is provided compounds of formula (I), wherein X1, Q, T, Y, R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.
    Type: Grant
    Filed: December 22, 2005
    Date of Patent: January 17, 2012
    Assignee: Biolipox AB
    Inventors: Benjamin Pelcman, Kristofer Olofsson, Martins Katkevics, Vita Ozola, Edgars Suna, Ivars Kalvins, Peteris Trapencieris, Dace Katkevica, Wesley Schaal
  • Patent number: 8088768
    Abstract: The present invention provides a method for identifying inhibitors of protein kinases and/or protein phosphatases. Methods are also provided for inhibiting protein kinase and/or protein phosphatase activity. Specific non-peptide protein tyrosine kinase and/or protein phosphatase inhibitors are provided. The protein kinase or protein phosphatase inhibitors of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, arthrosclerosis, immune system activity, Type II diabetes, and obesity.
    Type: Grant
    Filed: August 10, 2010
    Date of Patent: January 3, 2012
    Assignee: The Research Foundation of The State University of New York
    Inventors: David G. Hangauer, Jr., Moustafa E. El-Araby, Karen L. Milkiewicz
  • Publication number: 20110312945
    Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed.
    Type: Application
    Filed: October 1, 2009
    Publication date: December 22, 2011
    Inventors: James Jia, Ara Mermerian, Charles Kim, Regina Graul, Joel Moore
  • Publication number: 20110312949
    Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
    Type: Application
    Filed: August 30, 2011
    Publication date: December 22, 2011
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventors: John Paul Kilburn, Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Soren Ebdrup
  • Publication number: 20110311483
    Abstract: Compounds of Formulae I-1 to I-9 are disclosed, which are modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders.
    Type: Application
    Filed: March 29, 2011
    Publication date: December 22, 2011
    Applicant: IRONWOOD PHARMACEUTICALS, INC.
    Inventors: James JIA, Regina GRAUL, Bo PENG, Colleen HUDSON, Joel MOORE, Ara MERMERIAN
  • Publication number: 20110306560
    Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
    Type: Application
    Filed: August 19, 2011
    Publication date: December 15, 2011
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Julian Adams, Yu-Tung Ma, Ross Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
  • Patent number: 8071584
    Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: December 6, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
  • Publication number: 20110281870
    Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Application
    Filed: May 24, 2011
    Publication date: November 17, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Xenia B. Searle, Ming C. Yeung, Stanley DiDomenico, Andrew O. Stewart, Daria Darczak, Michael Schrimpf, Michael J. Rozema
  • Publication number: 20110269668
    Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.
    Type: Application
    Filed: October 13, 2009
    Publication date: November 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alexander Heim-Riether, Shuang Liang, Sabine Schlyer
  • Publication number: 20110263599
    Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.
    Type: Application
    Filed: April 15, 2011
    Publication date: October 27, 2011
    Inventors: Xiaohong Song, Hong Ding, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Cheol-Min Park, Zhi-Fu Tao, Xilu Wang, Aaron R. Kunzer
  • Publication number: 20110230454
    Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.
    Type: Application
    Filed: May 26, 2011
    Publication date: September 22, 2011
    Applicant: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
  • Patent number: 8008298
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1, R, and X are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: August 30, 2011
    Assignee: Roche Palo Alto
    Inventors: Joe Timothy Bamberg, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Alam Jahangir, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, David Bernard Smith, Michael Soth, Hanbiao Yang
  • Publication number: 20110190294
    Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.
    Type: Application
    Filed: April 16, 2009
    Publication date: August 4, 2011
    Inventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
  • Patent number: 7981888
    Abstract: Compounds of Formula I wherein A1, B1, C1, D1, E1, F1 and L1 are as defined herein, which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein, such as leukemia and lymphoma, are disclosed.
    Type: Grant
    Filed: April 16, 2008
    Date of Patent: July 19, 2011
    Assignee: Abbott Laboratories
    Inventors: Xiaohong Song, Hong Ding, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Cheol-Min Park, Zhi-Fu Tao, Xilu Wang, Aaron R. Kunzer
  • Publication number: 20110160207
    Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
    Type: Application
    Filed: March 2, 2011
    Publication date: June 30, 2011
    Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
  • Patent number: 7967906
    Abstract: The invention relates to a method for directly producing fine-particle 1,4-diketopyrrolo[3,4-c]pyrrols of formula (1), wherein R1a, R1b, R2a and R2b independently represent hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, cyano or phenyl, said compounds being characterized by a maximum frequency distribution between 20 and 120 nm. According to the method, nitriles are reacted with succinic acid esters or lactames or enamines in an alkali medium to form a pigment salt, and then protolysis of the pigment alkali salt is carried out. Said method is characterized in that an effective quantity of a pigment dispersant of formula (II) is added during the protolysis of the pigment alkali salt. In formula (II), Q is a radical of an organic pigment from the group of perinone, quinacridone, quinacridonquinone, anthanthrone, indanthrone, dioxazine, diketopyrrolopyrrol, indigo, thioindigo, thiazineindigo, isoindoline, isoindolinone, pyranthrone, isoviolanthrone, flavanthrone or anthrapyrimidine pigments.
    Type: Grant
    Filed: February 20, 2008
    Date of Patent: June 28, 2011
    Assignee: Clariant Finance (BVI) Limited
    Inventor: Matthias Ganschow
  • Patent number: 7964593
    Abstract: The present invention relates to indolone-acetamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as for the treatment of epilepsy, epileptogenesis, seizure disorders and convulsion.
    Type: Grant
    Filed: November 20, 2009
    Date of Patent: June 21, 2011
    Assignee: UCB Pharma, S.A.
    Inventors: Jean-Philippe Starck, Benoit Kenda