Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Isoquinoline Ring System By Nonionic Bonding Patents (Class 514/310)
  • Patent number: 10357469
    Abstract: Described is a method of diagnosis or prognosis of preeclampsia in a pregnant subject, comprising providing a sample from a pregnant subject and measuring the ratio between the amount of (a) one or both of sFlt-1 and PlGF, and (b) one or both of a breakdown product of heme and a breakdown product of arginine, in the sample. Also described are assay kits and a computer adapted for use in the method. Also described is a method of treating preeclampsia, comprising administering a pharmaceutically effective amount of L-arginine and/or citrulline and an inhibitor of arginase or pharmaceutically acceptable salts thereof. Also described is a method of treating cancer, comprising treating a subject with a therapeutically effective amount of an anti-VEGF compound, L-arginine and an arginase inhibitor.
    Type: Grant
    Filed: February 18, 2016
    Date of Patent: July 23, 2019
    Assignee: ASTON UNIVERSITY
    Inventors: Asif Ahmed, Keqing Wang, Shakil Ahmad
  • Patent number: 10227295
    Abstract: Disclosed are selective histone deactylase inhibitors (HDACi) that having Formula I. Methods of making and using these inhibitors for the treatment of cancer, in particular melanoma are also disclosed.
    Type: Grant
    Filed: September 5, 2017
    Date of Patent: March 12, 2019
    Assignees: H. Lee Moffitt Cancer Center and Research Institute, Inc., Board of Trustees of The University of Illinois
    Inventors: Eduardo M. Sotomayor, Joel A. Bergman, Alan P. Kozikowski, Alejandro V. Villagra, Karrune V. Woan
  • Patent number: 10028944
    Abstract: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
    Type: Grant
    Filed: January 3, 2017
    Date of Patent: July 24, 2018
    Assignee: ACADIA PHARMACEUTICALS INC.
    Inventors: David M. Weiner, Robert E. Davis, Mark R. Brann, Carl-Magnus A. Andersson, Allan K. Uldam
  • Patent number: 9956192
    Abstract: Disclosed are selective histone deactylase inhibitors (HDACi) that having Formula (I). Methods of making and using these inhibitors for the treatment of cancer, in particular melanoma are also disclosed.
    Type: Grant
    Filed: August 8, 2016
    Date of Patent: May 1, 2018
    Assignees: H. Lee Moffitt Cancer Center and Research Institute, Inc., Board of Trustees of The University of Illinois
    Inventors: Eduardo M. Sotomayor, Joel Bergman, Alan Kozikowski, Karrune Veeraprasert Woan, Alejandro V. Villagra
  • Patent number: 9951048
    Abstract: Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: December 6, 2017
    Date of Patent: April 24, 2018
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, Chi Ching Mak, Brian Walter Eastman, Jianguo Cao, Venkataiah Bollu, Gopi Kumar Mittapalli, Chandramouli Chiruta
  • Patent number: 9920011
    Abstract: The present invention relates to methods and compounds for regulating or enhancing erythropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.
    Type: Grant
    Filed: November 19, 2013
    Date of Patent: March 20, 2018
    Assignee: FibroGen, Inc.
    Inventors: Stephen J. Klaus, Christopher J. Molineaux, Thomas B. Neff, Volkmar Guenzler-Pukall, Robert C. Stephenson, Todd W. Seeley, Ingrid Langsetmo Parobok
  • Patent number: 9908890
    Abstract: The compounds of the invention are antagonists of CAR, with specificity for CAR over other proteins including PXR. The disclosed compounds are useful in treating or controlling cell proliferative disorders, in particular oncological disorders, such as cancer. 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: Grant
    Filed: October 16, 2015
    Date of Patent: March 6, 2018
    Assignee: St. Jude Children's Research Hospital
    Inventors: Taosheng Chen, Milu Cherian, Wenwei Lin
  • Patent number: 9889132
    Abstract: Pharmaceutical compositions for topical administration for the treatment of psoriasis are described, containing as active ingredient therapeutically effective quantities of 4,6-dimethyl-N-(3,4,5-trimethoxyphenyl)pyrimidin-2-amine (I) and 2,4-O-(2-furanylmethylene)-1,3,5,6-tetra-O-methyl-D-glucitol combined with suitable excipients and/or diluents.
    Type: Grant
    Filed: July 3, 2015
    Date of Patent: February 13, 2018
    Assignee: SPECIAL PRODUCT'S LINE S.P.A.
    Inventors: Daniele Biagioni, Carlo De Angelis, Lorenzo Scappaticci, Andrea Calcaterra
  • Patent number: 9884840
    Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.
    Type: Grant
    Filed: November 2, 2016
    Date of Patent: February 6, 2018
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
  • Patent number: 9789058
    Abstract: An ophthalmic composition for administration to an eye of a patient for the treatment of an ocular infection. The ophthalmic composition contains an ?-polylysine (?PL) in an amount effective to treat or control or prevent the ocular infection.
    Type: Grant
    Filed: June 18, 2015
    Date of Patent: October 17, 2017
    Assignee: CooperVision International Holding Company, LP
    Inventor: Erwin C. Si
  • Patent number: 9668996
    Abstract: The present technology provides methods for preventing or treating dry eyes in a subject in need thereof. The methods include administering to the subject an effective amount of a composition comprising C16:1n7-palmitoleate, its derivatives, pharmaceutically acceptable salts thereof, or a combination thereof.
    Type: Grant
    Filed: June 4, 2015
    Date of Patent: June 6, 2017
    Assignee: TERSUS LIFE SCIENCES, LLC
    Inventor: Lochlainn O'hAimhirgin
  • Patent number: 9656960
    Abstract: The present invention relates to compounds which are inhibitors of microsomal triglyceride transfer protein and/or apolipoprotein B (Apo B) secretion. These compounds can be useful for the prevention and treatment of various diseases, particularly atherosclerosis and its clinical sequelae, for lowering serum lipids, and related ailments. The invention further relates to pharmaceutical compositions comprising the compounds and to methods of treating diseases, such as hypertriglyceridemia, hyperchylomicronemia, atherosclerosis, obesity, and related conditions using the compounds. A method for decreasing apolipoprotein B (apo B) secretion is also provided.
    Type: Grant
    Filed: March 17, 2015
    Date of Patent: May 23, 2017
    Assignee: Surface Logix, Inc.
    Inventors: Alessandra Bartolozzi, Stewart Campbell, Hope Foudoulakis, Enoch Kim, Paul Sweetnam, Yingfei Yang
  • Patent number: 9593103
    Abstract: The invention provides pyridyl-hydfazones of Formula I, or pharmaceutically acceptable salts, esters, solvates, isprriers and prodrugs thereof as well as pharmaceutical compositions containing these compounds for use in the prophylactic and/or therapeutic treatment of tuberculosis and related diseases, such as, diseases caused by nontuberculous mycobacteria and/or caused by Micobacterium leprae.
    Type: Grant
    Filed: November 20, 2013
    Date of Patent: March 14, 2017
    Assignee: TECNIMEDE SOCIEDADE TECNICO-MEDICINAL S.A.
    Inventors: Ana Lucia Almeida Ferreira, Ana Sofia Lopes, Augusto Eugenio Pardal Filipe, Carlos Caixado, Pedro Filipe Eufrasio Pedroso, Susana Marques De Almeida Pecorelli
  • Patent number: 9586945
    Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: March 7, 2017
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying Wang, Jason Brewer, Anil Vasudevan, Yanbin Lao, Charles Hutchins, Hongyu Zhao, Huan-Qiu Li
  • Patent number: 9566271
    Abstract: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
    Type: Grant
    Filed: November 6, 2015
    Date of Patent: February 14, 2017
    Assignee: ACADIA Pharmaceuticals Inc.
    Inventors: David M. Weiner, Robert E. Davis, Mark R. Brann, Carl-Magnus A. Andersson, Allan K. Uldam
  • Patent number: 9561223
    Abstract: The present invention discloses a method of treating cancer comprising administering an effective amount of an alkaloid, in which the alkaloid is liensinine, isoliensinine, dauricine, cepharanthine, hernandezine or thalidezine and isolated from the traditional Chinese medicinal herbs. The use of the alkaloid in treating neurodegenerative disorder is also disclosed.
    Type: Grant
    Filed: December 31, 2015
    Date of Patent: February 7, 2017
    Assignee: Macau University of Science and Technology
    Inventors: Kam Wai Wong, Yuen Kwan Law, Liang Liu, Jingrong Wang
  • Patent number: 9561220
    Abstract: The present invention discloses a method of treating cancer comprising administering an effective amount of an alkaloid, in which the alkaloid is liensinine, isoliensinine, dauricine, cepharanthine, hernandezine or thalidezine and isolated from the traditional Chinese medicinal herbs. The use of the alkaloid in treating neurodegenerative disorder is also disclosed.
    Type: Grant
    Filed: December 31, 2015
    Date of Patent: February 7, 2017
    Assignee: Macau University of Science and Technology
    Inventors: Kam Wai Wong, Yuen Kwan Law, Liang Liu, Jingrong Wang
  • Patent number: 9492439
    Abstract: Amido compounds are disclosed that have a formula represented by the following: and wherein n1, n2, R1a, R1b, R2, R3, R4, R5, and R6 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.
    Type: Grant
    Filed: March 11, 2011
    Date of Patent: November 15, 2016
    Assignees: New York University, The United States of America, as Represented by the Secretary, Department of Health and Human Services
    Inventors: Dan Littman, Jun R. Huh, Wenwei Huang, Ruili Huang, Erika Elaine Englund
  • Patent number: 9415043
    Abstract: Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog. Compounds described herein include those in which an isoquinoline compound is covalently linked to a prostaglandin or a prostaglandin analog, and those in which an isoquinoline compound and a prostaglandin free acid together form a salt.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: August 16, 2016
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Casey Kopczynski, Cheng-Wen Lin, Jill Marie Sturdivant, Mitchell A. deLong
  • Patent number: 9409858
    Abstract: Disclosed are selective histone deactylase inhibitors (HDACi) that having Formula (I). Methods of making and using these inhibitors for the treatment of cancer, in particular melanoma are also disclosed.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: August 9, 2016
    Assignees: H. Lee Moffitt Cancer Center and Research Institute, Inc., Board of Trustees of the University of Illinois
    Inventors: Eduardo M. Sotomayor, Joel Bergman, Alan Kozikowski, Karrune Veeraprasert Woan, Alejandro V. Villagra
  • Patent number: 9328061
    Abstract: The present invention provides organic molecules and methods thereof for reactions between organoboron reagents and double bonds, such as imines or carbonyls, to stereoselectively provide chiral products including amines and alcohols, entities useful for the preparation of biologically active molecules.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: May 3, 2016
    Assignee: Trustees of Boston College
    Inventors: Amir H. Hoveyda, Daniel L. Silverio, Tatiana Pilyugina, Sebastian Torker, Daniel Robbins
  • Patent number: 9259472
    Abstract: The present invention relates to artificial tear formulations and ophthalmic formulations suitable for drug delivery. The formulations comprise galactomannans such as guar or hydroxypropyl guar and a borate source such as boric acid. The formulations further comprise a cis-diol such as sorbitol that interferes with the cross-linking of galactomannan and borate. Optionally, the formulations are substantially free of divalent cations.
    Type: Grant
    Filed: February 14, 2014
    Date of Patent: February 16, 2016
    Assignee: Alcon Research, Ltd.
    Inventors: Howard Allen Ketelson, David L. Meadows, James W. Davis
  • Patent number: 9192605
    Abstract: This application describes compositions of receptor inhibitors, including typical antipsychotic agents, for example haloperidol, and methods of use for treating clinical signs or symptoms of Parkinson's disease. Furthermore, this application describes compositions and methods to induce supersensitivity in dopamine D2 and other receptors involved in Parkinson's disease as a means of alleviating the clinical signs or symptoms of Parkinson's disease.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: November 24, 2015
    Assignee: CLERA INC.
    Inventor: Philip Seeman
  • Patent number: 9173395
    Abstract: Use of substituted isoquinolinones, isoquinolinediones, isoquinolinetriones and dihydroisoquinolinones of the general formula (I) or their respective salts where the radicals in the general formula (I) correspond to the definitions given in the description, for enhancing stress tolerance in plants to abiotic stress, for strengthening plant growth and/or for increasing plant yield, and selected processes for preparing the compounds mentioned above.
    Type: Grant
    Filed: July 2, 2012
    Date of Patent: November 3, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jens Frackenpohl, Hans-Joachim Zeiss, I, Ines Heinemann, Lothar Willms, Thomas Mueller, Marco Busch, Pascal Von Koskull-Doering, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills
  • Patent number: 9125939
    Abstract: The pharmaceutical composition of the present invention comprises a carbostyril derivative which is a dopamine-sero-tonin system stabilizer and a mood stabilizer in a pharmaceutically acceptable carrier. The carbostyril derivative may be aripiprazole or a metabolite thereof. The mood stabilizer may include but is not limited to lithium, valproic acid, divalproex sodium, carbamaza-pine, oxcarbamazapine, zonisamide, lamotragine, topiramate, gabapentin, levetiracetam or clonazepam. These compositions are used to treat patients with mood disorders, particularly bipolar disorder with or without psychotic features, mania or mixed episodes. Methods are provided for separate administration of a carbostyril derivative and a mood stabilizer to a patient with a mood disorder.
    Type: Grant
    Filed: May 19, 2004
    Date of Patent: September 8, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Tetsuro Kikuchi, Taro Iwamoto, Tsuyoshi Hirose
  • Patent number: 9079880
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and X 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: June 29, 2011
    Date of Patent: July 14, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: John David Ginn, Daniel Richard Marshall, Robert Sibley, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
  • Patent number: 9072728
    Abstract: This invention relates to methods and materials involved in the treatment of diseases with severe distal colitis component, and more specifically non-fungal and/or non-microbial induced mucositis of the distal intestinal tract. Kits and pharmaceutical compositions for medical treatments also are provided.
    Type: Grant
    Filed: September 20, 2004
    Date of Patent: July 7, 2015
    Assignee: Children's Medical Center Corporation
    Inventors: Paul Rufo, Wayne I. Lencer
  • Publication number: 20150148313
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are Factor VIIa inhibitors which may be used as medicaments.
    Type: Application
    Filed: June 5, 2013
    Publication date: May 28, 2015
    Inventors: Xiaojun Zhang, Peter Glunz, Eldon Scott Priestley, James A. Johnson, Nicholas Ronald Wurtz, Vladimir Ladziata
  • Publication number: 20150148256
    Abstract: A bioluminescence imaging-based high-throughput assay for inhibitors of ABCG2 is described. Compositions of inhibitors of ABCG2 and methods of using ABCG2 inhibitors are also described.
    Type: Application
    Filed: August 21, 2014
    Publication date: May 28, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: MARTIN GILBERT POMPER, YIMAO ZHANG, JOHN LATERRA
  • Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Publication number: 20150119387
    Abstract: The present invention relates to a compound having the structure of Formula I as inhibitor of WNT signal transduction pathways, as well as a composition comprising the compound. Further, the present invention relates to the use of the compound and the method of inhibiting the WNT signal transduction pathways.
    Type: Application
    Filed: June 15, 2012
    Publication date: April 30, 2015
    Applicant: Curegenix Inc.
    Inventor: Songzhou An
  • Publication number: 20150119419
    Abstract: 6-Amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided.
    Type: Application
    Filed: December 26, 2014
    Publication date: April 30, 2015
    Inventors: Mitchell A. deLong, Susan M. Royalty, Jill Marie Sturdivant, Geoffrey Richard Heintzelman
  • Publication number: 20150119418
    Abstract: Provided is a pharmaceutical agent containing a compound represented by General Formula (1), a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein A represents a C1-C3 linear alkylene group, in which one methylene group is optionally substituted with O or S; n represents an integer of from 3 to 5; X1 and X2 each independently represent CH or N; W1 and W2 each independently represent a carboxyl group or a tetrazolyl group; V represents a C1-C8 linear or branched alkylene group, in which one methylene group is optionally substituted with O or S; and R represents a substituted phenyl group, for example.
    Type: Application
    Filed: April 15, 2013
    Publication date: April 30, 2015
    Applicant: TOA EIYO LTD.
    Inventors: Kazuhiro Uemoto, Yoshimichi Sato, Naoki Okada, Emiko Iimori, Masayuki Kageyama
  • Patent number: 9012473
    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: Grant
    Filed: March 21, 2014
    Date of Patent: April 21, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
  • Patent number: 9006442
    Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: April 14, 2015
    Assignee: Lupin Limited
    Inventors: Sanjeev Anant Kulkarni, Sachin Madan, Nirmal Kumar Jana, Prashant Vitthalrao Tale, Narasimha Murthy Cheemala, Sachin Jaysing Mahangare, Prashant Popatrao Vidhate, Chaitanya Prabhakar Kulkarni, Sapana Suresh Patel, Amolsing Dattu Patil, Seema Prabhakar Zade, Rohan Mahadev Shinde, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 8980915
    Abstract: The present invention relates to compounds which are inhibitors of microsomal triglyceride transfer protein and/or apolipoprotein B (Apo B) secretion. These compounds can be useful for the prevention and treatment of various diseases, particularly atherosclerosis and its clinical sequelae, for lowering serum lipids, and related ailments. The invention further relates to pharmaceutical compositions comprising the compounds and to methods of treating diseases, such as hypertriglyceridemia, hyperchylomicronemia, atherosclerosis, obesity, and related conditions using the compounds. A method for decreasing apolipoprotein B (apo B) secretion is also provided.
    Type: Grant
    Filed: April 19, 2006
    Date of Patent: March 17, 2015
    Assignee: Surface Logix, Inc.
    Inventors: Alessandra Bartolozzi, Stewart Campbell, Hope Foudoulakis, Enoch Kim, Paul Sweetnam, Yingfei Yang
  • Patent number: 8980916
    Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: March 17, 2015
    Assignees: Merck Sharp & Dohme Corp., Mochida Pharmaceutical Co., Ltd.
    Inventors: Matthew Voss, Hiroki Sone, Samuel Chackalamannil, Munetaka Ohkouchi
  • Patent number: 8980914
    Abstract: This therapeutic agent for chronic obstructive pulmonary disease comprises, an active ingredient, at least one of a 7-aminoquinolinone derivative represented by the general formula (I): wherein R1 represents a hydrogen atom or an alkyl group; R2 and R3 each represents a group selected from a hydrogen atom, an acyl group, an alkyl group and an alkenyl group; and R4 and R5 each represents a group selected from a hydrogen atom, an acyl group, an alkyl group, an alkenyl group and an aralkyl group, and its physiologically acceptable salt.
    Type: Grant
    Filed: July 27, 2004
    Date of Patent: March 17, 2015
    Assignee: Mariposa Health Limited
    Inventors: Hidetsugu Takagaki, Yasuo Aoki, Mitsuteru Ishiwara, Nobuaki Mizutani
  • Patent number: 8975275
    Abstract: The invention relates to the use of chemotherapeutic agents for the production of a medicament for the topical and/or local treatment of diseases caused by bacteria and/or for prophylaxis in humans or animals.
    Type: Grant
    Filed: December 22, 2000
    Date of Patent: March 10, 2015
    Assignee: Bayer Innovation GmbH
    Inventors: Hans-Herrmann Schulz, Günther Schlimbach
  • Publication number: 20150057279
    Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Publication number: 20150057288
    Abstract: A pest control method for honeybee parasitic pests has been found, which is highly safe to honeybees and demonstrates excellent pest control effects against honeybee parasitic pests by using a honeybee parasitic pest control agent containing at least one of a compound represented by Formula (I) and acid addition salts thereof.
    Type: Application
    Filed: November 10, 2014
    Publication date: February 26, 2015
    Applicant: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Ryo HORIKOSHI, Masaaki MITOMI
  • Patent number: 8957075
    Abstract: The present invention provides inhibitors of O-GIcNAc transferase. Typically, the inhibitors are quinolinone-6-sulfonamides. The invention also provides pharmaceutical compositions thereof and methods for using the same in diabetes and complications thereof, neurodegenerative diseases, cancers, autoimmune diseases, and inflammatory diseases.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: February 17, 2015
    Assignee: President and Fellows of Harvard College
    Inventors: Suzanne Walker Kahne, Michael Block Lazarus, Benjamin J. Gross
  • Patent number: 8933096
    Abstract: The invention provides a compound of formula (I): or a salt or prodrug thereof, wherein R1, R4-R8, R10, R2?-R6?, W, and A have any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as antibacterial agents.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: January 13, 2015
    Assignees: Rugers, The State University of New Jersey, University of Medicine and Dentistry of New Jersey
    Inventors: Edmond J. Lavoie, Ajit Parhi, Daniel S. Pilch
  • Patent number: 8921393
    Abstract: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: December 30, 2014
    Assignee: ACADIA Pharmaceuticals Inc.
    Inventors: David M. Weiner, Robert E. Davis, Mark R. Brann, Carl-Magnus A. Andersson, Allan K. Uldam
  • Publication number: 20140364393
    Abstract: The present invention is directed to novel piperidinyl-carboxamide derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders.
    Type: Application
    Filed: December 5, 2012
    Publication date: December 11, 2014
    Inventors: Shyh-Ming Yang, Gee-Hong Kuo, Micheal D. Gaul, Thomas A. Rano
  • Patent number: 8895582
    Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: November 25, 2014
    Assignee: Cytokinetics, Inc.
    Inventors: Xiangping Qian, Chihyuan (Grace) Chuang, Pu-Ping Lu, Bing Yao, Qing (Kevin) Lu, Hong Jiang, Wenyue Wang, Bradley P. Morgan, David J. Morgans, Jr.
  • Publication number: 20140343036
    Abstract: The invention provides novel compounds having the general formula: wherein A, R1 and R2 are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Applicant: GENENTECH, INC.
    Inventors: Huifen Chen, Terry Crawford, Steven R. Magnuson, Chudi Ndubaku, Lan Wang
  • Publication number: 20140343095
    Abstract: Methods of using a 15-oxysterol, e.g., 15-ketocholestene (15-KE), 15-ketocholestane (15-KA), and/or 15-hydroxy-cholestene (15-HC), as a biomarker to monitor disease progression in multiple sclerosis (MS), and methods of treating secondary progressive MS (SPMS) using inhibitors of poly(ADP ribose) polymerase-1 (PARD-1).
    Type: Application
    Filed: August 1, 2014
    Publication date: November 20, 2014
    Inventors: Howard Weiner, Francisco J. Quintana, Mauricio Farez
  • Patent number: 8889676
    Abstract: The invention relates to 3-ureidoisoquinolin-8-yl derivatives of formula I wherein R1 is alkyl, haloalkyl or cyclopropyl; R2 is H, halogen, pyridazin-4-yl, pyrimidin-5-yl or an optionally substituted pyridin-3-yl, pyridin-4-yl or phenyl group; R3 is alkyl, alkynyl, aminoalkyl, carbamoylalkyl, methylcarbamoylalkyl, alkoxy, haloalkoxy, alkynyloxy, (4-hydroxybut-2-yn-1-yl)oxy, (4-aminobut-2-yn-1-yl)oxy, dimethylaminoalkoxy, carbamoylalkoxy, alkylamino, cycloalkyl, cycloalkylalkyl, cycloalkylalkoxy, hydroxyalkyl, hydroxyalkoxy, alkoxyalkyl, alkoxyalkoxy, carboxyalkyl, carboxyalkoxy, alkoxycarbonylalkoxy, aryl, heteroaryl, benzyl, benzyloxy, 2-cyanoethoxy, 2,3-dihydroxypropoxy, 3,4-dihydroxybutoxy, —CH2Ra, —CH2CH2Rb, —(CH2)n—C(O)O—Rd, —(CH2)n—N(Rc)C(O)O—Rd, —O—(CH2)n—N(Rc)C(O)O—Rd, —(CH2)n—Re or —O—(CH2)n—Re; Ra is cyano, acetylamino or N,N-dimethylamino; Rb is cyano or carbamoyl; Rc is H or methyl; Rd is alkyl; Re is pyrrolidin-1-yl, piperidin-1-yl, piperidin-3-yl, morpholin-1-yl, 2-oxopyrrolidin-1-yl, 5-ox
    Type: Grant
    Filed: March 28, 2012
    Date of Patent: November 18, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Markus Gude, Christian Hubschwerlen, Philippe Panchaud
  • Patent number: 8889712
    Abstract: There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
    Type: Grant
    Filed: June 19, 2013
    Date of Patent: November 18, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Heidi L. Perez, Erik M. Stang, Kyoung S. Kim