Spiro Patents (Class 544/230)
  • Patent number: 9657018
    Abstract: Compounds, processes for their preparation, pharmaceutical compositions containing such compounds and their use in treating therapeutic conditions, in particular conditions mediated by the action of ligands on the FP, DP, EP1, EP4, IP, DP1, FP and TP prostaglandin (PG) receptors thereby providing a general anti-inflammatory response.
    Type: Grant
    Filed: May 11, 2016
    Date of Patent: May 23, 2017
    Assignee: ALLERGAN, INC.
    Inventors: Jose L. Martos, David F. Woodward, Jenny W. Wang, Steven Dabbs, Jussi J. Kangasmetsa
  • Patent number: 9512122
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Grant
    Filed: September 1, 2015
    Date of Patent: December 6, 2016
    Assignee: Karos Pharmaceuticals, Inc.
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • Patent number: 9365569
    Abstract: Compounds, processes for their preparation, pharmaceutical compositions containing such compounds and their use in treating therapeutic conditions, in particular conditions mediated by the action of ligands on the FP, DP, EP1, EP4, IP, DP1, FP and TP prostaglandin (PG) receptors thereby providing a general anti-inflammatory response.
    Type: Grant
    Filed: January 27, 2015
    Date of Patent: June 14, 2016
    Assignee: ALLERGAN, INC.
    Inventors: Jose L. Martos, David F. Woodward, Jenny W. Wang, Steven Dabbs, Jussi J. Kangasmetsa
  • Patent number: 9199994
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Grant
    Filed: September 5, 2014
    Date of Patent: December 1, 2015
    Assignee: Karos Pharmaceuticals, Inc.
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren
  • Patent number: 9045500
    Abstract: The present invention relates to compounds represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.
    Type: Grant
    Filed: October 8, 2014
    Date of Patent: June 2, 2015
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: Lawrence Wayne Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh B. Singh, Yajun Zheng
  • Publication number: 20150148330
    Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 28, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • Publication number: 20150148327
    Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: June 17, 2013
    Publication date: May 28, 2015
    Applicant: Merck Canada Inc.
    Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
  • Publication number: 20150148340
    Abstract: The present application relates to novel bicyclically substituted uracil derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 28, 2015
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Chantal Fürstner, Jens Ackerstaff, Alexander Straub, Heinrich Meier, Hanna Tinel, Katja Zimmermann, Adrian Tersteegen, Dmitry Zubov, Raimund Kast, Jens Schamberger, Martina Schäfer, Kirsten Börngen
  • Publication number: 20150141396
    Abstract: The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases.
    Type: Application
    Filed: July 3, 2013
    Publication date: May 21, 2015
    Applicant: Ares Trading S.A.
    Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Patrick Gerber, Mathilde Muzerelle
  • Publication number: 20150141643
    Abstract: The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound.
    Type: Application
    Filed: July 14, 2014
    Publication date: May 21, 2015
    Inventors: Kouki FUCHINO, R. Richard GOEHRING, Akira MATSUMURA, Bin SHAO, Yoshiyuki TAODA, Naoki TSUNO, John William Frank WHITEHEAD, Jiangchao YAO
  • Publication number: 20150132352
    Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).
    Type: Application
    Filed: May 2, 2013
    Publication date: May 14, 2015
    Inventors: Hongmin Sun, Bryan Yestrepsky, David Ginsburg, Scott D. Larsen
  • Publication number: 20150133428
    Abstract: The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 14, 2015
    Inventors: Upender Velaparthi, Chetan Padmakar Darne, Peiying Liu, Mark D. Wittman, Bradley C. Pearce, Erika M. V. Araujo, Bireshwar Dasgupta, Jalathi Surendran Nair, Sakthi Kumaran Janakiraman, Chandrasekhar Reddy Rachamreddy, Mettu Mallikarjuna Rao, Arul Mozhi Selvan Subbiah Karuppiah, Bandreddy Subba Reddy, Pulicharla Nagalakshmi, Rajesh Onkardas Bora, Shilpa Holehatti Maheshwarappa, Selvakumar Kumaravel, Dibakar Mullick, Ramesh Sistla
  • Publication number: 20150125535
    Abstract: Described herein is certain crystalline forms of Compound 3, as well as pharmaceutical compositions employing the crystalline forms. Also provided are particles (e.g., nanoparticles) comprising such crystalline forms or pharmaceutical compositions. In certain examples, the particles are mucus penetrating particles (MPPs). The present invention further relates to methods of treating or preventing diseases using crystalline forms or pharmaceutical compositions.
    Type: Application
    Filed: October 31, 2014
    Publication date: May 7, 2015
    Inventors: Elizabeth Enlow, Mint Ngoc Nguyen, Winston Ong
  • Publication number: 20150126513
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Christine Hiu-Tung Chen, Donovan Noel Chin, Lucian V. DiPietro, Jianmei Fan, Mark G. Palermo, Michael David Shultz, Bakary-Barry Toure
  • Publication number: 20150126491
    Abstract: Compounds of the formula I: or a pharmaceutical salt thereof, wherein X, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 7, 2015
    Applicant: Genentech, Inc.
    Inventors: Monique Bodil van Niel, Andrew Cridland, Benjamin Fauber, Alberto Gobbi, Christopher Hurley, David Hurst, Jonathan Killen, Robert Maxey, Stuart Ward
  • Publication number: 20150119379
    Abstract: The present invention relates to certain 2-(2,4,5-substituted-anilino)pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exon19 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.
    Type: Application
    Filed: December 19, 2014
    Publication date: April 30, 2015
    Applicant: AstraZeneca AB
    Inventors: Sam Butterworth, Maurice Raymond Verschoyle Finlay, Richard Andrew Ward, Heather Marie Redfearn, Chandrasekhara Reddy Chintakuntla, Claudio Edmundo Chuaqui, Vasantha Krishna Kadambar, Andiappan Murugan
  • Publication number: 20150119404
    Abstract: The invention relates to spiro derivatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.
    Type: Application
    Filed: May 22, 2013
    Publication date: April 30, 2015
    Applicant: CONVERGANCE PHARMACEUTICALS LIMITED
    Inventors: Gerard M.P. Giblin, David T. Macpherson, David R. Witty, Steven J. Stanway
  • Patent number: 9018214
    Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: April 28, 2015
    Assignee: Astex Therapeutics Limited
    Inventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
  • Publication number: 20150111871
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. 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.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 23, 2015
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Publication number: 20150111876
    Abstract: A sulfur-containing bicyclic compound having a PAM action of GABAB, and it use for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease. A pharmaceutical composition for preventing and/or treating schizophrenia, cognitive impairment associated with schizophrenia (CIAS), cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, Charcot-Marie-Tooth disease, or the like, which has a positive allosteric modulator (PAM action) of GABAB.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Applicant: Astellas Pharma Inc.
    Inventors: Nobuyuki Shiraishi, Hiroaki Hoshii, Wataru Hamaguchi, Eriko Honjo, Tomofumi Takuwa, Yuji Kondo, Takayuki Goto
  • Publication number: 20150105368
    Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 2, 2014
    Publication date: April 16, 2015
    Applicant: ASTEX THERAPEUTICS LTD
    Inventors: Gordon SAXTY, Christopher William MURRAY, Valerio BERDINI, Gilbert Ebai BESONG, Christopher Charles Frederick HAMLETT, Christopher Norbert JOHNSON, Steven John WOODHEAD, Michael READER, David Charles REES, Laurence Anne MEVELLEC, Patrick René ANGIBAUD, Eddy Jean Edgard FREYNE, Tom Cornelis Hortense GOVAERTS, Johan Erwin Edmond WEERTS, Timothy Pietro Suren PERERA, Ronaldus Arnodus Hendrika Joseph GILISSEN, Berthold WROBLOWSKI, Jean Fernand Armand LACRAMPE, Alexandra PAPANIKOS, Oliver Alexis Georges QUEROLLE, Elisabeth Thérèse Jeanne PASQUIER, Isabelle Noëlle Constance PILATTE, Pascal Ghislain André BONNET, Werner Constant Johan EMBRECHTS, Rhalid AKKARI, Lieven MEERPOEL
  • Publication number: 20150105374
    Abstract: The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases.
    Type: Application
    Filed: September 19, 2014
    Publication date: April 16, 2015
    Inventors: Markus FOLLMANN, Johannes-Peter STASCH, Gorden REDLICH, Nils GRIEBENOW, Dieter LANG, Frank WUNDER, Walter HÜBSCH, Niels LINDNER, Alexandros VAKALOPOULOS, Adrian TERSTEEGEN
  • Publication number: 20150099730
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.
    Type: Application
    Filed: September 6, 2013
    Publication date: April 9, 2015
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Peter J. Connolly
  • Publication number: 20150099738
    Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
    Type: Application
    Filed: June 30, 2014
    Publication date: April 9, 2015
    Inventors: Mark L. BEHNKE, Alfredo C. CASTRO, Lawrence K. CHAN, Catherine A. EVANS, Louis GRENIER, Michael J. GROGAN, Yves LEBLANC, Tao LIU, Stephane PELUSO, Daniel A. SNYDER, Thomas T. TIBBITTS
  • Publication number: 20150099737
    Abstract: The invention is directed to novel pyrrolopyrimidine compounds of formula (1) wherein R1, R2y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Applicant: NOVARTIS AG
    Inventors: Christopher Thomas BRAIN, Young Shin CHO, John William GIRALDES, Bharat LAGU, Julian Roy LEVELL, Michael Joseph LUZZIO, Lawrence Blas PEREZ, Yaping WANG, Fan YANG
  • Publication number: 20150080393
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Application
    Filed: September 5, 2014
    Publication date: March 19, 2015
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • Patent number: 8980878
    Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
    Type: Grant
    Filed: April 17, 2013
    Date of Patent: March 17, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Dustin Siegel, David Sperandio, Hai Yang, Michael Sangi, Jay P. Parrish, Hon Chung Hui
  • Patent number: 8981112
    Abstract: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: March 17, 2015
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer-Ingelheim International GmbH
    Inventors: Yuri Bukhtiyarov, Salvacion Cacatian, Lawrence Wayne Dillard, Cornelia Dorner-Ciossek, Klaus Fuchs, Lanqi Jia, Deepak S. Lala, Angel Morales-Ramos, Jonathan Reeves, Suresh B. Singh, Shankar Venkatraman, Zhenrong Xu, Jing Yuan, Yi Zhao, Yajun Zheng, Georg Rast
  • Publication number: 20150073136
    Abstract: The present invention relates to pyrazinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: November 17, 2014
    Publication date: March 12, 2015
    Inventors: Stephen Brough, Richard Evans, Timothy Jon Luker, Piotr Raubo
  • Patent number: 8969325
    Abstract: Disclosed herein are compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein X1, L, Rx, Ry, G, Z, A, m, n, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: March 3, 2015
    Assignee: AbbVie Inc.
    Inventors: Michael J. Dart, Philip R. Kym, Eric A. Voight, Anurupa Shrestha, Jerome F. Daanen, Tammie K. Jinkerson, Ryan G. Keddy, Sridhar Peddi, Arthur Gomtsyan, Michael E. Kort, Gregory A. Gfesser, Kevin R. Woller, Derek W. Nelson
  • Patent number: 8969336
    Abstract: Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: March 3, 2015
    Assignees: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.
    Inventors: Itsuro Shimada, Kazuo Kurosawa, Takahiro Matsuya, Kazuhiko Iikubo, Yutaka Kondoh, Akio Kamikawa, Hiroshi Tomiyama, Yoshinori Iwai
  • Patent number: 8962596
    Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
    Type: Grant
    Filed: April 11, 2011
    Date of Patent: February 24, 2015
    Assignee: Array BioPharma Inc.
    Inventors: Laurence E. Burgess, Mark Laurence Boys, Robert D. Groneberg, Darren M. Harvey, Timothy Kercher, Christopher F. Kraser, Ellen Laird, Eugene Tarlton, Qian Zhao, Lily Huang
  • Patent number: 8957069
    Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted bromopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R3 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, wherein R2 and R3 do not exist when carbon atoms respectively adjacent to R2: and R3 form a double bond, and there is n
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: February 17, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Taiichi Ohra
  • Publication number: 20150038506
    Abstract: The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), neurodegenerative diseases (e.g., Alzheimer's disease), metabolic diseases (e.g. diabetes), neurodevelopmental disorders (e.g. autism), or psychiatric disorders (e.g. schizophrenia or anxiety)) as well as methods of treating these diseases.
    Type: Application
    Filed: October 17, 2014
    Publication date: February 5, 2015
    Applicants: Agency for Science, Technology and Research, University of Basel
    Inventors: Kassoum Nacro, Stephane Baudouin, Peter Scheiffele
  • Publication number: 20150034938
    Abstract: A compound for an organic optoelectronic device, an organic light emitting diode including the same, and a display device including the organic light emitting diode are disclosed and the compound for an organic optoelectronic device represented by the following Chemical Formula 1 or 2 provides an organic light emitting diode having life-span characteristics due to excellent electrochemical and thermal stability, and high luminous efficiency at a low driving voltage.
    Type: Application
    Filed: September 12, 2014
    Publication date: February 5, 2015
    Inventors: Dong-Min KANG, Hyun-Jung KIM, Chang-Ju SHIN, Jong-Woo WON, Nam-Heon LEE, Soo-Young JEONG, Ho-Kuk JUNG, Mi-Young CHAE
  • Publication number: 20150038460
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Application
    Filed: October 16, 2014
    Publication date: February 5, 2015
    Applicant: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A.G.N. Montalbetti
  • Publication number: 20150038707
    Abstract: Methods for preventing pest infestations are disclosed. In some embodiments, the methods for preventing infestations involve use of pyrethroid insecticides or the stereoisomers or salts thereof.
    Type: Application
    Filed: September 19, 2013
    Publication date: February 5, 2015
    Inventors: Kevin M. Belyk, Edward Cleator, Shen-Chun Kuo, Peter Emmanuel Maligres, Bangping Xiang, Nobuyoshi Yasuda, Jianguo Yin
  • Publication number: 20150031693
    Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of Fragile X syndrome.
    Type: Application
    Filed: November 2, 2012
    Publication date: January 29, 2015
    Applicant: AFRAXIS HOLDINGS, INC.
    Inventors: John C. Mckew, Wenwei Huang, David Campbell, Sergio G. Durön, Mark Behnke, Min Shen
  • Publication number: 20150031674
    Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, Re, n, r, s and t are as defined herein and which compounds are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
    Type: Application
    Filed: July 25, 2014
    Publication date: January 29, 2015
    Applicant: GENENTECH, INC.
    Inventors: Joachim Rudolph, Lewis J. Gazzard, James J. Crawford, Chudi Ndubaku, Joy Drobnick, Wendy Lee
  • Publication number: 20150031691
    Abstract: The present invention relates to compounds represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.
    Type: Application
    Filed: October 8, 2014
    Publication date: January 29, 2015
    Inventors: Lawrence Wayne Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh B. Singh, Yajun Zheng
  • Publication number: 20150031541
    Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as a pesticides.
    Type: Application
    Filed: February 27, 2013
    Publication date: January 29, 2015
    Applicant: Syngenta Participations AG
    Inventors: Clemens Lamberth, Sarah Sulzer-Mosse, Fredrik Cedarbaum, Jayant Umarye, Ravindra Sonawane
  • Publication number: 20150025058
    Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupus
    Type: Application
    Filed: January 22, 2013
    Publication date: January 22, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Carl Deutsch, Daniel Kuhn, Tatjana Ross, Lars Burgdorf
  • Publication number: 20150025070
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: January 22, 2015
    Applicant: Novartis AG
    Inventors: Atwood Kim Cheung, Donovan Noel Chin, Jianmei Fan, Karen Marie Miller-Moslin, Michael David Shultz, Troy D. Smith, Ronald Charles Tomlinson, Bakary-Barry Toure, Michael Scott Visser
  • Publication number: 20150018309
    Abstract: In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: February 23, 2013
    Publication date: January 15, 2015
    Inventors: Craig W Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, James C. Tarr, James M. Salovich
  • Publication number: 20150018345
    Abstract: The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(?O)OR7 or C1-4 alkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(?O)R7, C(?O)OR7, C(?O)NR8R9, C1-4 alkyl, wherein said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with C1-4 alkyl or C(?O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ?CH2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are independently hydrogen or C1-4 alkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically accep
    Type: Application
    Filed: February 20, 2013
    Publication date: January 15, 2015
    Inventors: Morten Dahl Sørensen, Romano Di Fabio, Alfonso Pozzan, Maria Pia Catalani, Haakon Bladh, Jakob Felding
  • Patent number: 8933070
    Abstract: Provided herein are methods, uses and compositions for treating a patient with cancer wherein the cancer is characterized by a PTEN gene mutation. In particular embodiments, the methods comprise administering to the patient a composition comprising a therapeutically effective amount of a PLK4 antagonist, and identifying a patient that is likely to be responsive to PLK4 antagonist therapy, if PTEN gene mutation is present.
    Type: Grant
    Filed: July 4, 2011
    Date of Patent: January 13, 2015
    Assignee: University Health Network
    Inventors: Guohua Pan, Jacqueline M. Mason, Xin Wei, Miklos Feher
  • Publication number: 20150011461
    Abstract: Heteroaryl pyridone and aza-pyridone amide compounds of Formula I are provided, and various substituents including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 8, 2015
    Applicant: GENENTECH, INC.
    Inventors: James John Crawford, Wendy Lee, Wendy B. Young
  • Patent number: 8927715
    Abstract: This invention relates to novel compounds of the Formula (I*), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
    Type: Grant
    Filed: August 24, 2007
    Date of Patent: January 6, 2015
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Salvacion Cacatian, Wei He, Robert Simpson, Zhenrong Xu, Wei Zhao
  • Publication number: 20150005289
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.
    Type: Application
    Filed: February 8, 2013
    Publication date: January 1, 2015
    Inventors: Hongyan Qi, Soongyu Choi, Amal Dakka, Gary Mitchell Karp, Jana Narasimhan, Nikolai Naryshkin, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Matthew G. Woll, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Luke Green, Emmanuel Pinard, Hasane Ratni
  • Publication number: 20150005304
    Abstract: The invention relates to pyran spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: January 15, 2013
    Publication date: January 1, 2015
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Vijayalaksmi Arumugam, Michael Paul Deninno, Bryan A. Frieman, Edward Adam Kallel, Mark Thomas Miller, Johnny Uy, Jinglan Zhou