Additional Hetero Ring Other Than The Six-membered Hetero Rings Patents (Class 514/333)
  • Patent number: 10316020
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: June 11, 2019
    Assignee: Novartis AG
    Inventors: Christopher Adams, Takeru Ehara
  • Patent number: 10307427
    Abstract: The present invention relates to compounds of Formula (I): Wherein variables are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.
    Type: Grant
    Filed: March 21, 2018
    Date of Patent: June 4, 2019
    Assignee: Gilead Sciences, Inc.
    Inventor: Gregory Notte
  • Patent number: 10308629
    Abstract: Compounds of formula (I) as described herein, processes for their production and their use as pharmaceuticals.
    Type: Grant
    Filed: August 1, 2016
    Date of Patent: June 4, 2019
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Keith Graham, Ulrich Klar, Hans Briem, Gerhard Siemeister, Ursula Mönning
  • Patent number: 10155763
    Abstract: The present invention provides a novel 2-pyridyl substituted imidazole derivative, or a pharmaceutically acceptable salt or solvate thereof, which selectively inhibits the transforming growth factor-? (TGF-?) type I receptor (ALK5) and/or the activin type I receptor (ALK4); a pharmaceutical composition comprising same as an active ingredient; and a use of the 2-pyridyl substituted imidazole derivative for the manufacture of a medicament for preventing or treating a disease mediated by ALK5 and/or ALK4 receptors in a mammal.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: December 18, 2018
    Assignee: TIUMBIO CO., LTD.
    Inventors: Ju Young Lee, Keun-Ho Ryu, Jae-Sun Kim, Yong-Hyuk Kim, Dong-Chul Shin, Bong-yong Lee, Sang-hwan Kang, Hyun-Jung Lee, Hoechul Jung, Young Ah Shin, Euisun Park, Jaeseung Ahn, Hun-Taek Kim, Je Ho Ryu
  • Patent number: 10138227
    Abstract: The invention discloses compounds of Formula I, wherein X1, X2, R1, and R2 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.
    Type: Grant
    Filed: May 23, 2017
    Date of Patent: November 27, 2018
    Assignees: AbbVie S.á.r.l., Galapagos NV
    Inventors: Robert J. Altenbach, Andrew Bogdan, Ghjuvanni Petru Diunisu Coti, Marlon D. Cowart, Stephen N Greszler, Hans Kelgtermans, Philip R Kym, Steven Emiel Van der Plas, Xueqing Wang
  • Patent number: 9861621
    Abstract: The present invention provides, inter alia, a composition containing a compound of formula (I): or a pharmaceutically acceptable salt thereof, optionally, in combination with at least one immune checkpoint inhibitor compound. Kits containing the composition, and methods of using the composition for ameliorating or treating the effects of a disease such as a cancer, in a subject, are also provided herein.
    Type: Grant
    Filed: June 28, 2016
    Date of Patent: January 9, 2018
    Assignee: Biomed Valley Discoveries, Inc.
    Inventors: Saurabh Saha, Linping Zhang, Xiaoyan Michelle Zhang
  • Patent number: 9796683
    Abstract: Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-? protein.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: October 24, 2017
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Mark Bock, Ming-Hong Hao, Manav Korpal, Vijay Kumar Nyavanandi, Xiaoling Puyang, Susanta Samajdar, Peter Gerard Smith, John Wang, Guo Zhu Zheng, Ping Zhu
  • Patent number: 9782404
    Abstract: Methods for treatment of disease-induced ataxia and non-ataxic imbalance are disclosed. The methods involve treating a patient with a compound having nicotinic acetylcholine receptor activity.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: October 10, 2017
    Assignee: UNIVERSITY OF SOUTH FLORIDA
    Inventors: Theresa A. Zesiewicz, Kelly L. Sullivan
  • Patent number: 9763925
    Abstract: Disclosed are compounds of formula (I): which are of use in the treatment of bacterial diseases and infections, to compositions containing those compounds and to methods of treating bacterial diseases and infections using the compounds. In particular, the compounds are useful for the treatment of infection with, and diseases caused by, Clostridium difficile.
    Type: Grant
    Filed: March 8, 2016
    Date of Patent: September 19, 2017
    Assignee: SUMMIT THERAPEUTICS PLC
    Inventors: Francis Xavier Wilson, Peter David Johnson, Richard Vickers, Richard Storer, Graham Michael Wynne, Alan Geoffrey Roach, Olivier De Moor, Colin Richard Dorgan, Paul James Davis
  • Patent number: 9751854
    Abstract: The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: November 9, 2016
    Date of Patent: September 5, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Indu T. Bharathan, Chris Blackburn, Jeffrey P. Ciavarri, Jouhara Chouitar, Courtney A. Cullis, Natalie D'Amore, Paul E. Fleming, Kenneth M. Gigstad, Krista E. Gipson, Mario Girard, Yongbo Hu, Janice Lee, Gang Li, Mansoureh Rezaei, Michael D. Sintchak, Francois Soucy, Stephen G. Stroud, Tricia J. Vos, Tzu-Tshin Wong, He Xu, Tianlin Xu, Yingchun Ye
  • Patent number: 9725440
    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 CFTR mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: February 27, 2015
    Date of Patent: August 8, 2017
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Mark Miller, Brian Bear, Jinglan Zhou, Jason McCartney, Peter Grootenhuis
  • Patent number: 9695147
    Abstract: The present invention provides intermediates useful for the synthesis of Perampanel and processes employing said intermediates for preparing Perampanel. The invention also provides processes for making the intermediates, crystalline forms of the intermediates and the use of the crystalline forms for preparing Perampanel.
    Type: Grant
    Filed: July 24, 2014
    Date of Patent: July 4, 2017
    Assignee: TEVA PHARMACEUTICALS INTERNATIONAL GMBH
    Inventor: Marian Buchlovic
  • Patent number: 9643934
    Abstract: A method for preparing a compound of formula k or a salt or solvate thereof, wherein R1 is as defined herein, the method comprising treating a compound of formula j or a salt or solvate thereof, with ammonia, to form the compound of formula k.
    Type: Grant
    Filed: October 14, 2013
    Date of Patent: May 9, 2017
    Assignee: Roche Palo Alto LLC
    Inventors: Charles Alois Dvorak, Keena Lynn Green, Gary R. Lee
  • Patent number: 9463190
    Abstract: Methods for treatment of disease-induced ataxia and non-ataxic imbalance are disclosed. The methods involve treating a patient with a compound having nicotinic acetylcholine receptor activity.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: October 11, 2016
    Assignee: UNIVERSITY OF SOUTH FLORIDA
    Inventors: Theresa A. Zesiewicz, Kelly L. Sullivan
  • Patent number: 9382228
    Abstract: Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: July 5, 2016
    Assignee: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Timothy Malcolm Caldwell, Michael D. Kaufman, William C. Patt, Thiwanka Samarakoon, Lakshminarayana Vogeti, Karen M. Yates
  • Patent number: 9326975
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Grant
    Filed: January 20, 2015
    Date of Patent: May 3, 2016
    Assignees: SUNSHINE LAKE PHARMA CO., LTD, CALITOR SCIENCES, LLC
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Patent number: 9309224
    Abstract: Described are compounds of Formula 1 which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: April 12, 2016
    Assignee: Deciphera Pharmaceuticals, LLC.
    Inventors: Daniel L. Flynn, Timothy Malcolm Caldwell, Thiwanka Samarakoon, Lakshminarayana Vogeti, Michael D. Kaufman, William C. Patt, YuMi Ahn
  • Patent number: 9301953
    Abstract: A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cycloheteroalkenyl Compound are disclosed herein.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: April 5, 2016
    Assignee: Purdue Pharma L.P.
    Inventors: Qun Sun, Kate Xin Wen
  • Patent number: 9289467
    Abstract: A method of treating a degenerative bone condition of a subject includes administering to hematopoietic progenitor cells or osteoclast progenitor cells of the subject at least one agent that substantially reduces the interaction of at least one of C3a or C5a with the C3a receptor (C3aR) and/or C5a receptor (C5aR), a STAT3/IL-6 signaling pathway antagonist, and a combination thereof, the agent being administered to the hematopoietic progenitor cells or osteoclast progenitor cells at an amount effective to inhibit osteoclast differentiation of hematopoietic progenitor cells or osteoclast progenitor cells.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: March 22, 2016
    Assignee: Case Western Reserve University
    Inventors: Feng Lin, James E. Dennis, Zhidan Tu
  • Patent number: 9145373
    Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
    Type: Grant
    Filed: August 9, 2013
    Date of Patent: September 29, 2015
    Assignee: CHDI FOUNDATION, INC.
    Inventors: John Wityak, Leticia M. Toledo-Sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
  • Patent number: 9120785
    Abstract: The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: September 1, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Maria Emilia Di Francesco, Andrew M. Haidle, Ryan D. Otte, John Michael Ellis, Kaleen Konrad Childers, Alan B. Northrup, Liping Wang
  • Patent number: 9062032
    Abstract: [Problem] To provide a compound that has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. [Means for Solution] The present inventors conducted their studies on a compound that has an NPT-IIb inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. As a result, they created an aminoalkyl-substituted N-thienylbenzamide derivative which has NPT-IIb inhibitory action, thereby completing the present invention. The aminoalkyl-substituted N-thienylbenzamide derivative of the present invention has an NPT-IIb inhibitory action and can be used as an agent for preventing and/or treating hyperphosphatemia.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: June 23, 2015
    Assignee: Astellas Pharma Inc.
    Inventors: Masanori Miura, Daisuke Kaga, Susumu Watanuki, Shunichiro Hachiya, Takao Okuda, Ippei Sato, Mai Isomura, Kazuhiro Terai, Yoh Terada
  • Patent number: 9051307
    Abstract: The present invention relates to novel bipyridyl derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: June 9, 2015
    Assignee: Merck Patent GmbH
    Inventors: Guenter Hoelzemann, Dieter Dorsch, Alfred Jonczyk, Christiane Amendt, Frank Zenke
  • Patent number: 9040563
    Abstract: Many GTPases such as Ras, Ral and Rho require post-translational farnestylation or geranylgeranylation for mediating malignant transformation. Dual farnesyltransferase (FT) (FTI) and geranylgeranyltransferase-I (GGT-1) inhibitors (GGTI) were developed as anticancer agents from based on an ethylenediamine scaffold. On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating extensive structure-activity relationship studies. The most potent inhibitor is compound exhibited an in vitro hFTase IC50 value of 25 nM and a whole cell H-Ras processing IC50 value of 90 nM. Several of the inhibitors proved highly selective for hFTase over the related prenyltransferase enzyme geranylgeranyltransferase-I (GGTase-I).
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: May 26, 2015
    Assignees: H. Lee Moffitt Cancer Center and Research Institute, Inc., Yale University
    Inventors: Said M. Sebti, Andrew Hamilton
  • Publication number: 20150141463
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: January 20, 2015
    Publication date: May 21, 2015
    Applicants: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Publication number: 20150133430
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 14, 2015
    Inventors: Qing XU, Zhe LI
  • Publication number: 20150133473
    Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: May 20, 2013
    Publication date: May 14, 2015
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Joseph E. Drumm III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
  • Publication number: 20150126558
    Abstract: To provide crystal polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, which is a useful pharmaceutical, and a production method therefor. Through purification of a corresponding salt, recrystallization, or storage under humidified conditions, three different crystal forms; i.e., crystalline polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile are produced.
    Type: Application
    Filed: July 24, 2013
    Publication date: May 7, 2015
    Applicant: FUJIYAKUHIN CO., LTD.
    Inventors: Yoshiyuki Iwabuchi, Sachiho Miyata, Takahiro Sato, Junichiro Uda, Takamitsu Kandou, Tadashi Inoue, Hiroyuki Nakano
  • Publication number: 20150126496
    Abstract: The invention relates to methods for diagnosis and treatment of autism spectrum disorders, particularly for autism spectrum disorders characterized by increased head size (circumference) and deficits in social behavior.
    Type: Application
    Filed: October 10, 2014
    Publication date: May 7, 2015
    Applicant: Massachusetts Institute of Technology
    Inventors: Damon Theron Page, Mriganka Sur
  • Publication number: 20150126529
    Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 7, 2015
    Inventors: Upender Velaparthi, Peiying Liu
  • 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: 20150119384
    Abstract: The present invention relates to ethynyl derivatives of formula I X, O, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined hereinor to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.
    Type: Application
    Filed: January 6, 2015
    Publication date: April 30, 2015
    Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • 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
  • Patent number: 9017735
    Abstract: Disclosed herein are compositions and methods for treating a psychiatric disorder or symptoms thereof in a patient. The compositions comprise a compound that modulates KCNQ (Kv7) potassium channel activity and the methods include administering an effective amount of the compound that modulates KCNQ (Kv7) potassium channel activity.
    Type: Grant
    Filed: June 3, 2010
    Date of Patent: April 28, 2015
    Assignee: Marquette University
    Inventor: Mohammadhossein Behnam Ghasemzadeh
  • Patent number: 9018234
    Abstract: The present invention relates to novel, fluoro-substituted 2-aryl-3,5-dicyano-4-(1H-indazol-5-yl)-6-methyl-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly Cancer and other proliferative disorders.
    Type: Grant
    Filed: November 8, 2010
    Date of Patent: April 28, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Alexandros Vakalopoulos, Martin Michels, Katja Zimmermann, Nicole Teusch, Mario Lobell, Karen Engel
  • Publication number: 20150111865
    Abstract: An object of the present invention is to provide a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I): (wherein all symbols represent the same meanings as described in the specification), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 23, 2015
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Jun Takeuchi, Masahiro Ikura, Masato Higashino, Maki Iwahashi, Kazuya Hashimura
  • Publication number: 20150111735
    Abstract: A pesticidal composition comprises a pyridine triazole compound of formula I or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, Z, and x are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse
  • Publication number: 20150111900
    Abstract: The present invention relates to compounds described herein Formula (I) and pharmaceutical acceptable salts thereof, which modulate the activity of calcium release-activated calcium (CRAC) channel. The invention also describes the compounds of Formula (I) and pharmaceutical compositions containing such compounds thereof for treating, managing, and/or lessening the severity of diseases, disorders, syndromes or conditions associated with the modulation of calcium release-activated calcium (CRAC) channel.
    Type: Application
    Filed: May 1, 2013
    Publication date: April 23, 2015
    Inventors: Nageswara Rao Irlapati, Zubair Abdul Wajid Shaikh, Vijay Pandurang Karche, Gokul Keruji Deshmukh, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20150111734
    Abstract: A pesticidal composition comprises at least one compounds selected from a compound of formula, or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, Q, Z, L, La, and x are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Yu Zhang, Asako Kubota, Noormohamed M. Niyaz, Thomas Barton, Tony K. Trullinger, Christian T. Lowe, Paul R. LePlae, Ann M. Buysse, Martin J. Walsh, Negar Garizi, Ricky Hunter, Daniel Knueppel
  • Publication number: 20150099750
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: December 1, 2014
    Publication date: April 9, 2015
    Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger
  • 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: 20150099758
    Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 9, 2015
    Applicant: Anvyl LLC
    Inventors: David Putnam, Olivier Dasse
  • Patent number: 8999966
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: April 7, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, Jr.
  • Patent number: 8999971
    Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.
    Type: Grant
    Filed: August 21, 2014
    Date of Patent: April 7, 2015
    Assignee: Aerpio Therapeutics Inc.
    Inventors: Robert Shalwitz, Joseph H. Gardner
  • Patent number: 8993598
    Abstract: The present invention relates to a compound represented by the formula: wherein A is pyridyl group having at least one substituent wherein R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, R4 and R6 are each a hydrogen atom, a halogen atom or a C1-6 alkyl group optionally substituted by halogen, R5 is a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, and R7 is a hydrogen atom or a C1-6 alkyl group optionally substituted by halogen or a salt thereof, or a pharmaceutical composition containing the same.
    Type: Grant
    Filed: October 1, 2013
    Date of Patent: March 31, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Haruyuki Nishida, Yasuyoshi Arikawa, Ikuo Fujimori
  • Publication number: 20150087618
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Application
    Filed: December 2, 2014
    Publication date: March 26, 2015
    Applicant: AbbVie Inc.
    Inventors: Mary E. Bellizzi, David A. Betebenner, Jean C. Califano, William A. Carroll, Daniel D. Caspi, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Yi Gao, Charles W. Hutchins, Douglas K. Hutchinson, Tammie K. Jinkerson, Warren M. Kati, Ryan G. Keddy, Allan C. Krueger, Wenke Li, Dachun Liu, Clarence J. Maring, Mark A. Matulenko, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, John K. Pratt, John T. Randolph, Todd W. Rockway, Kathy Sarris, Michael D. Tufano, Seble H. Wagaw, Rolf Wagner, Kevin R. Woller
  • Publication number: 20150087648
    Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: November 10, 2014
    Publication date: March 26, 2015
    Inventors: Werngard CZECHTIZKY, John WESTON, Nils RACKELMANN, Michael PODESCHWA, Petra ARNDT, Klaus WIRTH, Heinz GOEGELEIN, Olaf RITZELER, Volker KRAFT, Patrice BELLEVERGUE, Gary McCORT
  • 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: 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
  • 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