1,3-diazoles (including Hydrogenated) Patents (Class 546/272.7)
  • Patent number: 10308636
    Abstract: The compound represented by the general formula: wherein ring A is benzene which may be substituted and the like; ring B is benzene which may be substituted and the like; X is a single bond and the like; Y is alkyl which may be substituted and the like; Z is CR1 or nitrogen atom; R1 is hydrogen and the like; R2 is alkyl which may be substituted and the like or a pharmaceutically acceptable salt thereof is useful as a prevention/treatment agent of obesity, diabetes, and the like.
    Type: Grant
    Filed: August 29, 2016
    Date of Patent: June 4, 2019
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Kunio Saruta, Norimitsu Hayashi, Osamu Sakurai, Hiroaki Sawamoto, Eri Ooboki
  • Patent number: 10093664
    Abstract: Disclosed herein are compounds which inhibit the kinase activity of dual leucine zipper (DLK) kinase (MAP3K12), pharmaceutical compositions, and methods of treatment of DLK-mediated diseases, such as neurological diseases that result from traumatic injury to central nervous system and peripheral nervous system neurons (e.g. stroke, traumatic brain injury, spinal cord injury), or that result from a chronic neurodegenerative condition (e.g. Alzheimer's disease, frontotemporal dementia, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, spinocerebellar ataxia, progressive supranuclear palsy, Lewy body disease, Kennedy's disease, and other related conditions), from neuropathies resulting from neurological damage (chemotherapy-induced peripheral neuropathy, diabetic neuropathy, and related conditions) and from cognitive disorders caused by pharmacological intervention (e.g. chemotherapy induced cognitive disorder, also known as chemobrain).
    Type: Grant
    Filed: December 8, 2017
    Date of Patent: October 9, 2018
    Assignee: Board of Regents, The University of Texas System
    Inventors: Michael J. Soth, Gang Liu, Kang Le, Jason Cross, Philip Jones
  • Patent number: 9018233
    Abstract: The invention relates to diaminoaryl derivatives substituted by carbamate, salts thereof and a pesticidal composition containing the same, which exhibit superior pest control effects against various insect pests of insect species, in particular against moths such as the diamondback moth or Spodoptera litura.
    Type: Grant
    Filed: May 7, 2013
    Date of Patent: April 28, 2015
    Assignees: Kyung Nong Corporation, Korea Research Institute of Chemical Technology
    Inventors: Sung Youn Chang, Jung Nyoung Heo, Hyuk Lee, Hwan Jung Lim, Bum Tae Kim, Joo Kyung Kim, Jong-Kwan Kim
  • Publication number: 20150099762
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Application
    Filed: December 9, 2014
    Publication date: April 9, 2015
    Inventors: Hilary Schenck EIDAM, Kaushik RAHA, Zhen GONG, Huiping Amy GUAN, Chengde WU, Haiying YANG, Haiyu YU, Zhiliu ZHANG, Mui CHEUNG
  • Publication number: 20150087644
    Abstract: The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 26, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Christian Lerner
  • Patent number: 8987305
    Abstract: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: March 24, 2015
    Assignee: Aptose Biosciences Inc.
    Inventors: Raed H. Al-Qawasmeh, Aiping H. Young, Mario Huesca, Yoon S. Lee
  • Publication number: 20150038517
    Abstract: This invention relates to modulation of the ?7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a salt thereof: wherein R1 is imidazolyl, pyridinyl or pyrimidinyl, any of which is optionally substituted by one group independently selected from C1-3alkyl and C1-3alkoxy.
    Type: Application
    Filed: August 7, 2014
    Publication date: February 5, 2015
    Inventor: Kevin Dinnell
  • Patent number: 8927709
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: January 6, 2015
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • 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
  • Patent number: 8906941
    Abstract: The present invention relates to novel carboxamide compounds and their use as 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 and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds. The carboxamide compounds are compounds of the general formula I in which W—R2 is selected from and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: December 9, 2014
    Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: Andreas Kling, Helmut Mack, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Patent number: 8906943
    Abstract: Methods and small molecule compounds for smoking and CNS disease harm reduction are provided. One example of a class of compounds that may be used is represented by the compound having the structure IA or IB in the form of free base or a pharmaceutically acceptable salt, hydrate or solvate thereof.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: December 9, 2014
    Inventor: John R. Cashman
  • Publication number: 20140336377
    Abstract: The present invention relates to arylamide 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: October 18, 2011
    Publication date: November 13, 2014
    Applicant: RAQUALIA PHARMA INC.
    Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Yoshimasa Arano, Mikio Morita
  • Publication number: 20140315893
    Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi
    Type: Application
    Filed: November 22, 2012
    Publication date: October 23, 2014
    Inventors: Ferenc Fülöp, László Vígh, Zsolt Török, Botond Penke, Ibolya Horváth, Gábor Balogh, Sándor Bernáth, Ákos Hunya
  • Patent number: 8865906
    Abstract: The present invention relates to a process for the preparation of a compound of the formula I, which comprises reacting a compound of the formula IV with an oxalic acid diester and to novel intermediate compounds used therein.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: October 21, 2014
    Assignee: Sanofi
    Inventors: Kai Rossen, Volker Kraft, Hermut Wehlan, Antony Bigot, Veronique Crocq-Stuerga
  • Patent number: 8846012
    Abstract: Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor is represented by general formula (1) (excluding clotrimazole) and/or a pharmacologically acceptable salt thereof. In the formula, A1, A2 and A3 are independently selected from a hydrogen atom, an aryl group which may have a substituent, and an aromatic heterocyclic group which may have a substituent.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: September 30, 2014
    Assignee: Pola Chemical Industries Inc.
    Inventors: Kouji Yokoyama, Makoto Kimura, Masashi Tamai, Yuko Saitoh, Tomomi Kato, Yu Ikeda
  • Publication number: 20140275057
    Abstract: The present invention relates to compounds and composition for inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
    Type: Application
    Filed: September 2, 2011
    Publication date: September 18, 2014
    Inventors: Kenneth W. Bair, Timm Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
  • Publication number: 20140275111
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Hilary Schenck EIDAM, Kaushik Raha, Zhen Gong, Huiping Guan, Chengde Wu, Haiying Yang, Haiyu Yu, Zhiliu Zhang, Mui CHEUNG
  • Patent number: 8809378
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: August 19, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger, Gary D. Gustafson
  • Patent number: 8796314
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, CY, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: January 28, 2010
    Date of Patent: August 5, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Zhan Shi, Irache Visiers, Tricia J. Vos, Stepan Vyskocil
  • Patent number: 8796272
    Abstract: The present invention relates to novel compounds of formula [I] or pharmaceutically acceptable salts thereof: The compounds of the present invention are useful in the prevention or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (e.g., generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, acute stress disorder), depression, drug dependence, spasm, tremor, pain, Parkinson's disease, attention deficit hyperactivity disorder, bipolar disorder, eating disorder, or sleep disorders, which is based on the glycine uptake-inhibiting action.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: August 5, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Minoru Moriya, Hiroshi Ohta, Shuji Yamamoto, Kumi Abe, Yuko Araki, Xiang-Min Sun, Daisuke Wakasugi
  • Patent number: 8785489
    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: Grant
    Filed: October 13, 2009
    Date of Patent: July 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Asitha Abeywardane, Bennett Farmer, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
  • Patent number: 8759332
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: June 24, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Publication number: 20140155407
    Abstract: The present invention relates to compounds which selectively inhibit CYP11B1. Preferably, the compounds of the present invention do not substantially inhibit CYP11B2. Moreover, the compounds of the present invention do not substantially inhibit CYP17 and/or CYP19, either. Amongst other applications of the compounds of the present invention, they can be used for the treatment of Cushing's syndrome or metabolic disease.
    Type: Application
    Filed: October 21, 2011
    Publication date: June 5, 2014
    Inventors: Rolf Hartmann, Ulrike Hille, Christina Zimmer, Carsten A. Vock, Qingzhong Hu
  • Publication number: 20140148461
    Abstract: The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Application
    Filed: November 22, 2013
    Publication date: May 29, 2014
    Inventors: Hervé GENESTE, Sean Colm TURNER, Michael OCHSE, Karla DRESCHER, Lawrence A. BLACK, Katja JANTOS
  • Patent number: 8729271
    Abstract: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: May 20, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Minoru Moriya, Akito Yasuhara, Kazunari Sakagami, Hiroshi Ohta, Kumi Abe, Shuji Yamamoto, Yuko Araki, Hiroki Urabe, Xiang-Min Sun
  • Patent number: 8703103
    Abstract: Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion. Synthesis of the novel compounds and their use to form BST films is also contemplated.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: April 22, 2014
    Assignee: Air Products and Chemicals, Inc.
    Inventors: John Anthony Thomas Norman, Melanie K. Perez, Moo-Sung Kim
  • Patent number: 8691847
    Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: April 8, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song
  • Patent number: 8673955
    Abstract: Imidazole derivatives of formula (I): wherein R1, R2a, R2b, A, V and W are as defined in the description, as inhibitors of fructose-1,6-bisphosphatase, their preparation process and their use in the prevention or treatment of diabetes, and other diseases where the inhibition of gluconeogenesis, control of blood glucose levels, reduction in glycogen stores, or reduction in insulin levels is beneficial and diseases related to the insulin resistance syndrome.
    Type: Grant
    Filed: July 19, 2006
    Date of Patent: March 18, 2014
    Assignee: Merck Patent GmbH
    Inventors: Denis Carniato, Gérard Moinet, Gérard Botton, Annick Arbellot De Vacqueur, Annick Audet
  • Patent number: 8653111
    Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: February 18, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Jörg Keldenich, Metin Akbaba, Mario Jeske
  • Patent number: 8648200
    Abstract: The present invention provides compounds of the formula below: where A, X and R1-R6 are as described herein, a pharmaceutical salt thereof, and a pharmaceutical composition containing this compound; methods of treating pain associated with osteoarthritis using one of the compounds or a pharmaceutically acceptable salt thereof, and processes for preparing the compounds.
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: February 11, 2014
    Assignee: Eli Lilly and Company
    Inventors: Norman Earle Hughes, Bryan Hurst Norman, Timothy Andrew Woods
  • Publication number: 20140024665
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Application
    Filed: June 5, 2013
    Publication date: January 23, 2014
    Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
  • Patent number: 8629279
    Abstract: A process for manufacturing a 5-formyl-pyridine-2,3-dicarboxylic acid ester (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro and R1, R2 are independently C1-C10-alkyl, comprising the steps of (i) reacting a compound of formula (II), wherein the symbols are as in formula (I), with a nitrosation agent (III) R3—O—N?O (III) wherein R3 is C1-C8-alkyl, in the presence of an alkali metal or alkaline earth metal alcoholates or carbonates in a polar aprotic solvent at a temperature of from ?45 to 40° C., to obtain an oxime compound (IV) where Z, Z1, R1 and R2 are as in formula (I), and (ii) reacting oxime compound (IV) with an aliphatic C1-C10-aldehyde in the presence of a Lewis acid at a temperature in the range of from 0 to 100° C. The compounds of formula (I) are useful intermediates in the synthesis of herbicidal imidazolinones, like imazamox.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: January 14, 2014
    Assignee: BASF SE
    Inventors: Michael Rack, Joachim Gebhardt, Frederik Menges, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schröder
  • Publication number: 20130317027
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 28, 2013
    Applicant: Myrexis, Inc.
    Inventors: J. Adam Willardsen, Jeffrey W. Lockman, Brett R. Murphy, Weston R. Judd, In Chul Kim, Se-Ho Kim, Daniel Feodore Zigar, Kraig M. Yager, Tracey C. Fleischer, Ryan T. Terry-Lorenzo, J. Jay Boniface, Daniel P. Parker, Ian A. McAlexander, Matthew Gregory Bursavich, David M. Dastrup, Christophe Hoarau, David A. Gerrish, Paul R. Sebahar, Dange Vijay Kumar
  • Publication number: 20130310375
    Abstract: The present invention relates to compositions and methods for modulating the Wnt signaling pathway.
    Type: Application
    Filed: July 22, 2013
    Publication date: November 21, 2013
    Applicant: IRM LLC
    Inventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
  • 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: 20130261128
    Abstract: This is to provide a continuous arycyclic compound having a DGAT1 inhibitory activity, and useful for prophylaxis and/or treatment of obesity or hyperlipidemia caused by obesity, hypertriglyceridemia, lipid metabolism disorder, fatty liver, hypertension, arteriosclerosis, diabetes, etc., as well as to provide a DGAT1 inhibitor comprising the continuous arycyclic compound or a pharmaceutically acceptable salt thereof as an effective ingredient. Disclosed is the continuous arycyclic compound is represented by the formula: wherein the substituents in the formula are the same as defined in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 16, 2011
    Publication date: October 3, 2013
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Osamu Sakurai, Kunio Saruta, Norimitsu Hayashi, Takashi Goi, Kenji Morokuma, Hidekazu Tsujishima, Hiroaki Sawamoto, Hiroaki Shitama, Ritsuo Imashiro
  • Patent number: 8536185
    Abstract: Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: September 17, 2013
    Assignee: Cayman Chemical Company, Incorporated
    Inventors: Gregory W. Endres, Pil Heui Lee, Kirk Lang Olson, James Bernard Kramer, Fred Lawrence Ciske, Stephen Douglas Barrett
  • Publication number: 20130237502
    Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.
    Type: Application
    Filed: March 5, 2013
    Publication date: September 12, 2013
    Inventors: Michael Curtis, Brian A. Duclos, Richard A. Ewin, Paul D. Johnson, Timothy Allen Johnson, Rajendran Vairagoundar, Denis Billen, Richard M. Goodwin, Andrea K. Haber-Stuk, Graham M. Kyne, Susan M. K. Sheehan
  • Patent number: 8518975
    Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: August 27, 2013
    Assignee: Merck Sharp + Dohme Corp.
    Inventors: Robert G. Aslanian, Xianhai Huang, Anandan Palani, Jun Qin, Wei Zhou, Xiaohong Zhu, Robert D. Mazzola, Jr., Pawan Dhondi, William J. Greenlee
  • Patent number: 8501786
    Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: March 23, 2009
    Date of Patent: August 6, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Bart Harper, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
  • Patent number: 8501747
    Abstract: In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of ÿ2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ÿ2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: February 11, 2008
    Date of Patent: August 6, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Manuel de lera Ruiz, Kevin D. McCormick, Christopher W. Boyce, Robert G. Aslanian, Younong Yu, Pietro Mangiaracina, Junying Zheng, Michael Y. Berlin, Stephanie Louise Ciesla, Chia-Yu Huang, Bo Liang
  • Publication number: 20130196971
    Abstract: This invention relates to the use of imidazole, triazole, and tetrazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of imidazoles, triazoles, and tetrazoles in the treatment of cancer.
    Type: Application
    Filed: September 15, 2011
    Publication date: August 1, 2013
    Inventors: Christopher Joseph Aquino, Dennis Heyer, Terence John Kiesow, David Lee Musso, Cynthia A. Parrish
  • Publication number: 20130196985
    Abstract: The heterocyclic alkynyl benzene compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in preparing drugs for preventing or treating tumors. The compounds can overcome the clinically induced resistance against Gleevec.
    Type: Application
    Filed: June 3, 2011
    Publication date: August 1, 2013
    Applicant: Guangzzhou Institute of Biomedicine and Health, Chineses Academy of Sciences
    Inventors: Ke Ding, Deping Wang, Duanqing Pei, Zhang Zhang, Mengjie Shen, Kun Luo, Yubing Feng
  • Patent number: 8492387
    Abstract: The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: February 18, 2009
    Date of Patent: July 23, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Ivory D. Hills, Craig A. Coburn, Samuel L. Graham, Keith P. Moore, Philippe G. Nantermet, Hemaka A. Rajapakse, Shawn J. Stachel, Hong Zhu
  • Patent number: 8481548
    Abstract: The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3 and R4 are described hereinabove. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognititve disorders and memory deficits, as well as chronic and acute pain.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: July 9, 2013
    Assignee: Hoffman-La Roche Inc.
    Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
  • Publication number: 20130172310
    Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Application
    Filed: September 12, 2012
    Publication date: July 4, 2013
    Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
  • Publication number: 20130165464
    Abstract: This invention provides compounds of formula IB: and also provides compounds of formulas ID, IIB, VB, and IIC: wherein HY, R1, R2, G5, G6, G7, G8, and G9 are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: December 20, 2012
    Publication date: June 27, 2013
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventor: MILLENNIUM PHARMACEUTICALS, INC.
  • Patent number: 8450326
    Abstract: Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: May 28, 2013
    Assignee: Cayman Chemical Company, Incorporated
    Inventors: Gregory W. Endres, Pil Heui Lee, Kirk Lang Olson, James Bernard Kramer, Fred Lawrence Ciske, Stephen Douglas Barrett
  • Publication number: 20130123234
    Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: December 20, 2012
    Publication date: May 16, 2013
    Applicants: EISAI R&D MANAGEMENT CO., LTD., EPIZYME, INC.
    Inventors: EPIZYME, INC., EISAI R&D MANAGEMENT CO., LTD.
  • Publication number: 20130109684
    Abstract: The present disclosure provides a series of compounds which exhibit isoform selective inhibition of GRP94, a homologue of Hsp90 that is localized to the endoplasmic recticulum. Through GRP94 inhibition, these compounds are likely to manifest anti-cancer, anti-inflammatory, anti-metastasis, and immunosuppressive activities, as well as utility in the treatment of neurodegenerative diseases, and diabetes.
    Type: Application
    Filed: April 6, 2012
    Publication date: May 2, 2013
    Applicant: University of Kansas
    Inventors: Brian S.J. Blagg, Adam S. Duerfeldt