At Least Three Hetero Rings Containing Patents (Class 544/364)
  • Patent number: 9630959
    Abstract: The disclosure relates to Compounds of Formula (I) and pharmaceutically acceptable derivatives thereof, where R1, R4, R8, R9, and m are as defined herein, compositions comprising an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, pain associated with osteoarthritis, osteoarthritis, UI, an ulcer, IBD, and IBS, comprising administering to an animal in need thereof an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof.
    Type: Grant
    Filed: February 8, 2016
    Date of Patent: April 25, 2017
    Assignees: Purdue Pharma L.P., Shionogi & Co., Ltd.
    Inventors: Shigeru Ando, Noriyuki Kurose, Laykea Tafesse
  • Patent number: 9580404
    Abstract: The invention relates to compounds of the general formula (I), wherein the variable have the meanings as indicated in the claims, or a physiologically acceptable salt thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling endoparasites in warm-blooded animals.
    Type: Grant
    Filed: May 17, 2016
    Date of Patent: February 28, 2017
    Assignee: Novartis Tiergesundheit AG
    Inventors: Noelle Gauvry, Francois Pautrat
  • Patent number: 9273043
    Abstract: The disclosure relates to Compounds of Formula (I) and pharmaceutically acceptable derivatives thereof, where R1, R4, R8, R9, and m are as defined herein, compositions comprising an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, pain associated with osteoarthritis, osteoarthritis, UI, an ulcer, IBD, and IBS, comprising administering to an animal in need thereof an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: March 1, 2016
    Assignees: Purdue Pharma L.P., Shionogi & Co., Ltd.
    Inventors: Noriyuki Kurose, Laykea Tafesse
  • 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
  • Patent number: 9040522
    Abstract: The present invention provides compounds of the formula: which are useful as inhibitors of PHD and pharmaceutical compositions thereof.
    Type: Grant
    Filed: March 26, 2014
    Date of Patent: May 26, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jason W. Brown, Melinda Davis, Anthony Ivetac, Benjamin Jones, Andre A. Kiryanov, Jon Kuehler, Marion Lanier, Joanne Miura, Sean Murphy, Xiaolun Wang
  • Publication number: 20150139905
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 21, 2015
    Inventors: Dinesh Chimmanamada, Weiwen Ying
  • Patent number: 9034875
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: May 19, 2015
    Assignee: ABBVIE INC.
    Inventors: George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Andrew J. Souers, Zhi-Fu Tao, Gary T. Wang, Le Wang, Robert Mantei, Todd M. Hansen
  • Patent number: 9034874
    Abstract: The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: May 19, 2015
    Assignee: NOVARTIS AG
    Inventors: Yves Auberson, Mark Gary Bock, Dario Braga, Marco Curzi, Stephanie Kay Dodd, Stefano Luca Giaffreda, Haiyang Jiang, Piotr Karpinski, Thomas J. Troxler, Tielin Wang, Xiaoyang Wang, Xuechun Zhang
  • Patent number: 9029356
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 12, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Publication number: 20150126515
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.
    Type: Application
    Filed: January 25, 2013
    Publication date: May 7, 2015
    Applicant: PTC Therapeutics, Inc.
    Inventors: Guangming Chen, Amal Dakka, Gary Mitchell Karp, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Marla L. Weetall, Ellen Welch, Xin Zhao
  • Publication number: 20150126522
    Abstract: This invention relates to novel substituted benzamides according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
    Type: Application
    Filed: May 15, 2013
    Publication date: May 7, 2015
    Applicant: GlaxoSmithKline LLC
    Inventors: Joelle Lorraine Burgess, Celine Duquenne, Steven David Knight, William Henry Miller, Kenneth Allen Newlander, Sharad Kumar Verma
  • Patent number: 9024033
    Abstract: The present invention is related to a use of aminopyridine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyridine derivatives useful for the preparation of a pharmaceutical foimulation for the inhibition of malaria parasite proliferation.
    Type: Grant
    Filed: January 17, 2011
    Date of Patent: May 5, 2015
    Assignee: MMV Medicines for Malaria Venture
    Inventors: Michael John Witty, David Hardick
  • Patent number: 9023854
    Abstract: The present invention relates to novel 5-halogen-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.
    Type: Grant
    Filed: December 5, 2008
    Date of Patent: May 5, 2015
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilfried Braje, Thorsten Oost, Astrid Netz, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Andrea Hager-Wernet
  • Publication number: 20150119380
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.
    Type: Application
    Filed: December 28, 2012
    Publication date: April 30, 2015
    Inventors: Matthew G. Woll, Guangming Chen, Soongyu Choi, Amal Dakka, Song Huang, Gary Mitchell Karp, Chang-Sun Lee, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Sergey Paushkin, Hongyan Qi, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Emmanuel Pinard, Hasane Ratni
  • Publication number: 20150119395
    Abstract: The present invention relates to novel triazole Hsp90 inhibitors that possess significant inhibitory activity against Hsp90, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders. Furthermore, pharmaceutical compositions, including combination products, are also provided in the present application. Further provided are methods of using the pharmaceutical compositions and/or combination products.
    Type: Application
    Filed: April 4, 2013
    Publication date: April 30, 2015
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying
  • Publication number: 20150111879
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 24, 2014
    Publication date: April 23, 2015
    Applicants: CURIS, INC., GENENTECH, INC.
    Inventors: Janet L. GUNZNER, Daniel P. SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
  • Patent number: 9012479
    Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R11, R12, R13, Q, Z, and p are as described herein. Compounds of the present invention are useful for the treatment of cancers.
    Type: Grant
    Filed: October 7, 2013
    Date of Patent: April 21, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Jerry Leroy Adams, Thomas H. Faitg, Neil W. Johnson, Hong Lin, Xin Peng
  • Publication number: 20150105550
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicants: CURIS, INC., GENENTECH, INC.
    Inventors: Janet L. GUNZNER, Daniel SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
  • Publication number: 20150105388
    Abstract: This invention relates to new carboxamide-substituted heteroaryl-pyrazoles, method for their production, their use for the treatment and/or prophylaxis of diseases, as well as their use for the production of pharmaceutical agents for the treatment and/or prophylaxis of diseases, in particular retroviral diseases, in humans and/or animals.
    Type: Application
    Filed: November 29, 2012
    Publication date: April 16, 2015
    Applicant: AICURIS GMBH & CO. KG
    Inventors: Steffen Wildum, Burkhard Klenke, Astrid Wendt
  • Publication number: 20150105397
    Abstract: The present inventions relate to substituted piperazine derivatives of general formula (I) and to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various medical conditions related to glycine transporter-1 (GlyT1).
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Christoph HOENKE, Riccardo GIOVANNINI, Uta LESSEL, Holger ROSENBROCK, Bernhard SCHMID
  • Patent number: 9006276
    Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: April 14, 2015
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
  • Publication number: 20150099761
    Abstract: 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1-carboxylic acid (4-chloro-pyridin-3-yl)-amide is described, which is useful as a FAAH modulator. 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1-carboxylic acid (4-chloro-pyridin-3-yl)-amide may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). A method of synthesizing 4-(2,2-difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1-carboxylic acid (4-chloro-pyridin-3-yl)-amide is also disclosed.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 9, 2015
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: John M. Keith, Jing Liu
  • Publication number: 20150099736
    Abstract: Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1-C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, —N(R11)—R12, -Alk-N(R11)—R12, —O-Alk-N(R11)—R12, —C(?O)OH, carboxy-(C1-C3)-alkyl, or —C(?O)—NH—R13; Alk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(?O)—N(—R16)— or —N(—R17)—C(?O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substitu
    Type: Application
    Filed: November 10, 2014
    Publication date: April 9, 2015
    Inventors: Stephen Stokes, Nicolas Foloppe, Andrea Fiumana, Martin Drysdale, Simon Bedford, Paul Webb
  • Publication number: 20150099746
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 9, 2015
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
  • Patent number: 8999981
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: April 7, 2015
    Assignees: Pfizer Inc., Pfizer Products Inc.
    Inventors: Iriny Botrous, Yufeng Hong, Hui Li, Kevin Kun-Chin Liu, Seiji Nukui, Min Teng, Eileen Valenzuela Tompkins, Chunfeng Yin
  • Patent number: 8993574
    Abstract: The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof; wherein: R1, R2, R3, R4, R5, R6, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
    Type: Grant
    Filed: April 23, 2009
    Date of Patent: March 31, 2015
    Assignee: F2G Ltd
    Inventors: Graham Edward Morris Sibley, Robert Downham, Lloyd James Payne, Derek Law, Jason David Oliver, Mike Birch, Gareth Morse Davies, Patricia Suling Davies
  • Patent number: 8993779
    Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
  • Patent number: 8993575
    Abstract: The present invention belongs to the medicinal chemistry field, and specifically discloses a [1,3,4]oxadiazole derivative with the structure of general formula (I) and pharmaceutically acceptable salt thereof. The compound can be used to prepare a medicine for preventing or treating a disease of the central nervous system.
    Type: Grant
    Filed: April 1, 2012
    Date of Patent: March 31, 2015
    Assignees: Huazhong University of Science & Technology, NHWA Pharma Corporation
    Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Bifeng Liu, Xiaojun Feng, Song Zhao, Shicheng Liu, Minquan Yu, Yu Lan, Yinli Qiu
  • Publication number: 20150087635
    Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Application
    Filed: December 4, 2014
    Publication date: March 26, 2015
    Inventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
  • Patent number: 8987276
    Abstract: The present invention is concerned with novel substituted triazolyl piperazine and triazolyl piperidine derivatives of Formula (I) wherein R1, R2, R3, R4a, R4b, R5, X, Y1, Y2, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: March 24, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Francois Paul Bischoff, Adriana Ingrid Velter, Sven Franciscus Anna Van Brandt, Didier Jean-Claude Berthelot
  • Patent number: 8987250
    Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: March 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
  • Publication number: 20150080383
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 19, 2015
    Inventors: Tianle Yang, Gary Mitchell Karp, Hongyan Qi
  • Patent number: 8981084
    Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, Y, Q, X, B and L are as defined herein, and methods of making and using the same.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: March 17, 2015
    Assignee: Tempero Pharmaceuticals, Inc.
    Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
  • Publication number: 20150072976
    Abstract: Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.
    Type: Application
    Filed: April 11, 2013
    Publication date: March 12, 2015
    Inventors: Amato Giaccia, Edwin Lai, Olga Razorenova, Denise Chan, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Ray Tabibiazar, Po-wai Yuen
  • Publication number: 20150065477
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 5, 2015
    Inventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Möller, Wilfried Hornberger, Gisela Backfisch, Yanbin Lao, Marjoleen Nijsen
  • Publication number: 20150065519
    Abstract: This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.
    Type: Application
    Filed: August 28, 2014
    Publication date: March 5, 2015
    Inventors: Sarvajit Chakravarty, Roopa Rai, Son Minh Pham, Brahmam Pujala, Ramniwas Jangir, Rambabu Guguloth, Vijay Kumar Sharma
  • Publication number: 20150065483
    Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl 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.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
  • Publication number: 20150065500
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: September 11, 2014
    Publication date: March 5, 2015
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
  • Patent number: 8962607
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: February 24, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Peter J Connolly, Christopher Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark M McDonnell, Philip M Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Publication number: 20150050237
    Abstract: The present invention relates to the field of anti-mycobacterial therapeutics, in particular the treatment of tuberculosis, especially including pulmonary multidrug-resistant tuberculosis (MDR-TB), with applications in extensively drug-resistant tuberculosis (XDR-TB) and extremely drug-resistant tuberculosis (XXDR-TB), preferably in combination therapy.
    Type: Application
    Filed: March 13, 2013
    Publication date: February 19, 2015
    Inventors: Vasu Nair, Maurice O. Okello, Machhindra G. Gund, Byung I. Seo, Pankajkumar R. Singh, Naveen K. Mangu
  • Publication number: 20150051208
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R3 and X1 through X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Application
    Filed: August 11, 2014
    Publication date: February 19, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Harald ENGELHARDT, Laetitia MARTIN, Christian SMETHURST
  • Publication number: 20150051194
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Patent number: 8957215
    Abstract: The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.
    Type: Grant
    Filed: April 23, 2012
    Date of Patent: February 17, 2015
    Assignee: Navidea Biopharmaceuticals, Inc.
    Inventors: Ylva Gravenfors, Catrin Jonasson, Jonas Malmstrom, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Strom, David Wensbo
  • 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: 20150045347
    Abstract: Compounds having the following formula: (I) wherein: A is an optionally substituted triazole, or a stereoisomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.
    Type: Application
    Filed: January 11, 2013
    Publication date: February 12, 2015
    Inventors: Dharmpal S. Dodd, Christopher P. Mussari, Rajeev S. Bhide, Satheesh Kesavan Nair, Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Sistla, William J. Pitts, John Hynes
  • Publication number: 20150045362
    Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.
    Type: Application
    Filed: August 25, 2014
    Publication date: February 12, 2015
    Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford
  • Patent number: 8952004
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R3, A, B, X, and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: January 5, 2011
    Date of Patent: February 10, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: John David Ginn, Ronald John Sorcek, Michael Robert Turner, Di Wu, Frank Wu
  • Publication number: 20150031661
    Abstract: The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Application
    Filed: March 24, 2014
    Publication date: January 29, 2015
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
  • 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
  • Patent number: 8940894
    Abstract: The present invention relates to an industrial process of preparing pharmaceutical compounds having the formula I: which are useful as certain tyrosine kinase inhibitors and more particularly as c-kit and bcr-abl inhibitors. The groups R1 and R2, identical or different, represent each a hydrogen, halogen atom, an alkyl, an alkoxy, a trifluoromethyl, an amino, an alkylamino, a dialkylamino, a solubilising group; m is 0-5 and n is 0-4; the group R3 represents an aryl or an heteroaryl group as described in claims herein.
    Type: Grant
    Filed: May 10, 2013
    Date of Patent: January 27, 2015
    Assignee: AB Science
    Inventors: Alain Moussy, Philippe Reginault, Francois Bellamy, Anne Lermet