Additional Hetero Ring Attached Directly Or Indirectly To The Morpholine Ring By Nonionic Bonding Patents (Class 514/231.5)
  • Patent number: 12109219
    Abstract: Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;
    Type: Grant
    Filed: April 15, 2020
    Date of Patent: October 8, 2024
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Jayant Thatte, Anthony C. Blackburn, Sangdon Han, Robert M. Jones, Jae-Kyu Jung, Antonio Garrido Montalban, Biman B. Pal, Jaimie Karyn Rueter, Sonja Strah-Pleynet, Lars Thoresen, Yifeng Xiong, Dawei Yue, Xiuwen Zhu
  • Patent number: 11845811
    Abstract: The present invention provides an improved process for the preparation of Sugammadex sodium of formula (I) having more than 98.5% purity along with less than 1.0% monohydroxy Sugammadex sodium and less than 0.15% any other known or unknown impurities by HPLC.
    Type: Grant
    Filed: September 18, 2019
    Date of Patent: December 19, 2023
    Assignee: NATCO PHARMA LIMITED
    Inventors: Vanga Prabhakar, Baddula Saidulu, Kotte Rajashekar, Peddi Rajasekhara Reddy, Vuppalapati Naga Vasanta Srinivasu, Konduri Srinivasa Krishna Murthy, Budideti Shankar Reddy, Muddasani Pulla Reddy, Nannapaneni Venkaiah Chowdary
  • Patent number: 11813268
    Abstract: Activators of mitofusins and their uses in treatment of diseases and disorders are disclosed.
    Type: Grant
    Filed: October 16, 2018
    Date of Patent: November 14, 2023
    Assignee: Albert Einstein College of Medicine
    Inventors: Evripidis Gavathiotis, Richard N. Kitsis, Nikolaos Biris, Emmanouil Zacharioudakis
  • Patent number: 11731972
    Abstract: Compounds of formula (I), wherein A, R, L, Z, Q1, Q2 and n have the meaning according to the claims, can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
    Type: Grant
    Filed: August 22, 2019
    Date of Patent: August 22, 2023
    Assignee: Asceneuron SA
    Inventors: Anna Quattropani, Santosh S. Kulkarni, Paul Rakesh, Awadut Gajendra Giri
  • Patent number: 11446325
    Abstract: The present invention generally relates to use of single isomer chemically modified cyclodextrins, namely, S-(carboxyalkyl)-thio-cyclodextrin salts in medication used for the prevention or treatment of lysosomal storage diseases. More particularly, the present invention relates to isomer-pure, single isomer hexakis-S-(carboxyalkyl)-hexathio-alpha-cyclodextrin sodium salts, heptakis-S-(carboxyalkyl)-heptathio-beta-cyclodextrin sodium salts and octakis-S-(carboxyalkyl)-octathio-gamma-cyclodextrin sodium salts in medication used for the prevention or treatment of lysosomal storage diseases.
    Type: Grant
    Filed: September 30, 2020
    Date of Patent: September 20, 2022
    Assignee: CYCLOLAB CYCLODEXTRIN RESEARCH AND DEVELOPMENT LABORATORY LTD.
    Inventors: Lajos Szente, István Puskas, Tamas Sohajda
  • Patent number: 11345659
    Abstract: The present disclosure relates to chemical compounds that modulate proteasome activity, pharmaceutical compositions containing such compounds, and use of these compounds and compositions for the treatment of disorders of uncontrolled cellular proliferation such as, for example, a 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: January 30, 2019
    Date of Patent: May 31, 2022
    Assignees: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM, BOARD OF TRUSTEES OF MICHIGAN STATE UNIVERSITY
    Inventors: Maria Gaczynska, Pawel A. Osmulski, Jetze Tepe, Matt Giletto
  • Patent number: 11311524
    Abstract: The present invention provides a pharmaceutical composition containing an inhibitor selected from the group consisting of an EZH1 inhibitor, an EZH2 inhibitor and an EZH1/2 dual inhibitor as an active ingredient, for use in treating HTLV-1-associated myelopathy. The present invention provides a pharmaceutical composition for use in treating HTLV-1-associated myelopathy, containing a 1,3-benzodioxole derivative or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 18, 2018
    Date of Patent: April 26, 2022
    Assignees: DAIICHI SANKYO COMPANY, LIMITED, ST. MARIANNA UNIVERSITY SCHOOL OF MEDICINE
    Inventors: Yoshihisa Yamano, Natsumi Ueda, Kazushi Araki
  • Patent number: 11241381
    Abstract: A treatment process of cyclosporine eye gel, comprising the steps of: adding carbomer to water, stirring thoroughly and homogenizing; after the prepared carbomer base swollen, stirring and homogenizing; cooling the carbomer base after moist heat sterilization, performing vacuum degassing, adjusting the pH of the base to 5.0-9.0 with filtered sodium hydroxide solution; mixing polyoxyl 35 castor oil, cyclosporin A raw material, 1,2-propanediol and water in a suitable ratio, preparing into a clear solution under a water bath at 35 to 45° C., and filtering; mixing the filtrate uniformly with the carbomer base, performing vacuum degassing; performing aseptic filling after another filtration. For the process of the present invention, sterilization and filtration is performed before adding carbomer, which is convenient for industrial production.
    Type: Grant
    Filed: December 25, 2018
    Date of Patent: February 8, 2022
    Assignee: ZHAOKE (GUANGZHOU) OPHTHALMIC DRUG COMPANY LIMITED
    Inventors: Gang Li, Kailei Cao, Xiaoyi Li, Xiangrong Dai, Lei Yin, Juan Ling
  • Patent number: 11208404
    Abstract: Inhibitors of ALCAT1 are described having the general formula: (I). These compounds offer a treatment for aging and age-related diseases.
    Type: Grant
    Filed: March 29, 2018
    Date of Patent: December 28, 2021
    Assignee: PERENNA PHARMACEUTICALS, INC.
    Inventors: Yuguang Shi, Daqing Che, Jonathan Baell, Xiaoyu Liu, Jiasheng Fu
  • Patent number: 11197871
    Abstract: This document provides methods and materials involved in treating cardiovascular conditions such as calcific aortic valve stenosis. For example, methods and materials for using sGC agonists or a combination of sGC agonists and PDE5A inhibitors to reduce calcification of heart valves and/or vessels or to slow progression of aortic sclerosis to calcific aortic valve stenosis are provided.
    Type: Grant
    Filed: December 17, 2019
    Date of Patent: December 14, 2021
    Assignee: Mayo Foundation for Medical Education and Research
    Inventors: Jordan D. Miller, Bin Zhang
  • Patent number: 11052472
    Abstract: A cutting insert includes a rake face configuring one of polygonal surfaces, a seating surface configuring the other one of the polygonal surfaces, and a side surface connecting the rake face and the seating surface to each other. The cutting insert has a cutting edge portion including a main cutting edge located in a side portion of the rake face, a subsidiary cutting edge connected to the main cutting edge, and a corner cutting edge connected to the subsidiary cutting edge and located in a corner portion of the rake face. The side surface includes a flank face and a connection surface which are adjacent to each other in a thickness direction via a boundary line. The connection surface is located on the seating surface side, and is located outside than an extension line of the flank face.
    Type: Grant
    Filed: December 25, 2017
    Date of Patent: July 6, 2021
    Assignee: MOLDINO TOOL ENGINEERING, LTD.
    Inventors: Masashi Noshita, Hayato Takahashi
  • Patent number: 10968180
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.
    Type: Grant
    Filed: June 6, 2019
    Date of Patent: April 6, 2021
    Assignee: Regenacy Pharmaceuticals, LLC
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 10952976
    Abstract: 5-HT receptor agonists are useful in the treatment of a variety of diseases. Provided herein are methods of treating and/or reducing the occurrence of respiratory depression caused by an opioid in a human patient or patient population using a 5-HT receptor agonist, such as, for example, a 5-HT4 agonist (e.g., fenfluramine). Methods of stimulating one or more 5-HT4 receptors in the brain of a patient undergoing treatment with an opioid, wherein the patient is at risk of respiratory depression, by administering a 5-HT4 agonist (e.g., fenfluramine) to a subject in need thereof are provided. Pharmaceutical compositions for use in practicing the subject methods are also provided.
    Type: Grant
    Filed: November 22, 2019
    Date of Patent: March 23, 2021
    Assignee: ZOGENIX INTERNATIONAL LIMITED
    Inventors: Bradley S. Galer, Carl L. Faingold, Parthena Martin
  • Patent number: 10772893
    Abstract: The present invention relates to substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative disease as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: May 8, 2018
    Date of Patent: September 15, 2020
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Lars Wortmann, Ulrich Lücking, Julien Lefranc, Hans Briem, Marcus Koppitz, Knut Eis, Franz Von Nussbaum, Benjamin Bader, Antje Margret Wengner, Gerhard Siemeister, Wilhelm Bone, Philip Lienau, Joanna Grudzinska-Goebel, Dieter Moosmayer, Uwe Eberspächer, Hans Schick
  • Patent number: 10722516
    Abstract: The invention provides a new use of landiolol hydrochloride for persistent reduction of the heart rate during the administration period of landiolol hydrochloride in the treatment of a human suffering from tachycardia, tachyarrhythmia or elevated blood pressure, wherein landiolol hydrochloride is administered at a constant dose of more than 5 ?g/kg/min, specifically of at least 10 ?g/kg/min for a period of at least 2 hours and wherein the heart rate and/or blood pressure of said patient are persistently reduced during the administration period compared to the heart rate and/or blood pressure before treatment and no overshooting effect occurs after termination of said administration.
    Type: Grant
    Filed: April 25, 2014
    Date of Patent: July 28, 2020
    Assignee: AOP ORPHAN PHARMACEUTICALS AG
    Inventor: Günther Krumpl
  • Patent number: 10583111
    Abstract: The present application provides a use of a nitric oxide releasing agent in preparing a medicament, wherein the medicament is used for preventing or treating EGFR inhibition associated epithelial diseases in a subject. The present application further provides a pharmaceutical composition or a kit comprising EGFR inhibitor and nitric oxide releasing agent.
    Type: Grant
    Filed: May 28, 2019
    Date of Patent: March 10, 2020
    Assignee: ONQUALITY PHARMACEUTICALS CHINA LTD.
    Inventors: Shiyi Zhang, Zhaoyu Wu, Chao Liu, Leying Chen, Xin Zhao, Zhehui Gong, Rui Xing, Songxuan Sun, Jie Luo
  • Patent number: 10556894
    Abstract: Novel compounds useful for treating and/or preventing HCMV infections are provided.
    Type: Grant
    Filed: November 9, 2015
    Date of Patent: February 11, 2020
    Assignee: Evrys Bio, LLC
    Inventors: Stacy Remiszewski, Emre Koyuncu, Qun Sun, Lillian Chiang
  • Patent number: 10442871
    Abstract: Novel thioalkylcarboxylate-modified CDs and pharmaceutical compositions comprising these thioalkylcarboxylate-modified CDs are disclosed, as well as methods of using the disclosed thioalkylcarboxylate-modified CDs and pharmaceutical compositions thereof to neutralize or reduce undesired effects or symptoms associated with one or more fentanyl related compounds in a subject in need thereof. The use of the disclosed thioalkylcarboxylate-modified CDs to detect the presence of one or more fentanyl related compounds in a sample is also disclosed, which comprises contacting the sample with said thioalkylcarboxylate-modified CDs or a composition comprising these CDs.
    Type: Grant
    Filed: June 22, 2017
    Date of Patent: October 15, 2019
    Assignee: Lawrence Livermore National Security, LLC
    Inventors: Daniel Joseph Kennedy, Brian P. Mayer, Carlos A. Valdez
  • Patent number: 10434100
    Abstract: Disclosed are methods for treating a meylodysplastic syndrome (MDS) in a subject that involves administering to the subject a therapeutically effective amount of a protein phosphatase 2A (PP2A) inhibitor.
    Type: Grant
    Filed: August 20, 2018
    Date of Patent: October 8, 2019
    Assignee: Lixte Biotechnology, Inc.
    Inventors: Alan F. List, David A. Sallman, John S. Kovach
  • Patent number: 10420836
    Abstract: This disclosure relates to methods of immunization comprising administering an effective amount of an immunogenic composition comprising an antigen or vaccine and an adjuvant disclosed herein to a subject in need thereof. In certain embodiments, the adjuvant is 1,8-dihydroxy-9,10-dihydroanthracen-9-one or derivative thereof. In certain embodiments, the adjuvant is N-(3,5-bis-trifluoromethyl-phenyl)-5-chloro-2-hydroxy-benzamide or derivatives thereof. In certain embodiments, the adjuvant is a fullerene or derivatives thereof, e.g., Fullerene-C60. In certain embodiments, the disclosure relates to compositions and devices comprising adjuvants disclosed herein.
    Type: Grant
    Filed: October 10, 2016
    Date of Patent: September 24, 2019
    Assignee: Emory University
    Inventors: Ioanna Skountzou, Nicole Brock, Elena Vassilieva, Richard Compans
  • Patent number: 10385031
    Abstract: Provided herein are compounds of Formula II, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity
    Type: Grant
    Filed: November 22, 2017
    Date of Patent: August 20, 2019
    Assignee: REGENACY PHARMACEUTICALS, LLC
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 10328064
    Abstract: The present invention relates to compounds, pharmaceutical compositions and formulations that have a structure (I). The compounds comprise a heterocyclic ring where W, X, Y, and Z generally and independently are S, N or C with the proviso that at least 2 of these positions in the ring are other than carbon. A pyridine or a substituted pyridine A ring and a phenyl or a substituted phenyl B ring are covalently bonded to the heterocyclic ring. Further provided are methods for treating a metabolic disorder, cell proliferative disease, reducing body weight or increasing thermogenesis during weight loss with the compounds of structure as described or pharmaceutically acceptable salt or stereoisomer thereof or both.
    Type: Grant
    Filed: December 23, 2015
    Date of Patent: June 25, 2019
    Assignee: FGH BIOTECH, INC.
    Inventors: Motonari Uesugi, Joel Huff
  • Patent number: 10208046
    Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, which may be useful as medicaments such as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies and the like, and the like. The present invention relates to a compound represented by the formula (I) wherein ring A is an optionally substituted 5- or 6-membered ring; R is a C1-6 alkyl group substituted by 1 to 5 halogen atoms; and X is —CH? or —N?, or a salt thereof.
    Type: Grant
    Filed: May 15, 2015
    Date of Patent: February 19, 2019
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiro Sugimoto, Kenichiro Shimokawa, Takuto Kojima, Hiroki Sakamoto, Ikuo Fujimori, Minoru Nakamura, Masami Yamada, Masataka Murakami, Makoto Kamata, Shinkichi Suzuki
  • Patent number: 10189804
    Abstract: It is an object of the present invention to provide an excellent method for producing an excellent therapeutic agent. The solution of the present invention is as shown in the following scheme: wherein R1 represents a C1-C6 alkyl group, R2 represents a C1-C6 alkyl group, and R3 represents a C1-C6 alkyl group.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: January 29, 2019
    Assignee: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Masayuki Murakami, Yuichi Aki, Daisuke Fukatsu, Kenichi Kimura, Makoto Michida, Koji Hamaoka
  • Patent number: 10166238
    Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and their use for the treatment of cancer.
    Type: Grant
    Filed: June 17, 2015
    Date of Patent: January 1, 2019
    Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.
    Inventors: Heike Keilhack, Sarah K. Knutson, Danielle Johnston Blackwell, Larisa Reyderman, Lone Ottesen
  • Patent number: 10111881
    Abstract: Described herein are pharmaceutical compositions capable of inhibiting vesicle formation and methods of treatment or prophylactic administration of these pharmaceutical compositions to treat pathogenic infections.
    Type: Grant
    Filed: April 4, 2017
    Date of Patent: October 30, 2018
    Assignee: Texas Biomedical Research Institute
    Inventors: Robert Andrew Davey, Manu Anantpadma
  • Patent number: 10106516
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Grant
    Filed: August 4, 2016
    Date of Patent: October 23, 2018
    Assignee: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Patent number: 10071094
    Abstract: Disclosed are methods for treating a myelodysplastic syndrome (MDS) in a subject that involves administering to the subject a therapeutically effective amount of a protein phosphatase 2A (PP2A) inhibitor.
    Type: Grant
    Filed: July 23, 2015
    Date of Patent: September 11, 2018
    Inventors: Alan F. List, David A. Sallman, John S. Kovach
  • Patent number: 10072008
    Abstract: The present invention relates to compounds having pharmacological activity towards the sigma (?) receptor, and more particularly to spiro-isoquinoline-3,4?-piperidine compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Grant
    Filed: April 27, 2016
    Date of Patent: September 11, 2018
    Assignee: ESTEVE PHARMACEUTICALS S.A.
    Inventor: Carmen Almansa-Rosales
  • Patent number: 10023561
    Abstract: Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Grant
    Filed: May 16, 2017
    Date of Patent: July 17, 2018
    Assignee: Zafgen, Inc.
    Inventors: James E. Vath, Robert Zahler
  • Patent number: 9981960
    Abstract: The present invention relates to a novel pyrrolidine compound having melanocortin receptor agonist activity or a pharmaceutically acceptable salt thereof, and to pharmaceutical applications thereof. The present invention relates to a pyrrolidine derivative represented by formula [I], wherein ring A represents an optionally substituted aryl group or the like; R1 represents an optionally substituted alkyl group or the like; R2 represents a halogen atom or the like; and R3 is an alkyl group substituted with an optionally substituted aryl group or the like, and R4 is a hydrogen atom or the like; or R3 and R4 are terminally attached to each other, and together with the nitrogen atom to which they are attached, form an optionally substituted nitrogen-containing aliphatic heterocyclic ring that may partially contain a double bond; or to a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 28, 2015
    Date of Patent: May 29, 2018
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Yasuo Yamamoto, Atsushi Sato, Kenji Morokuma, Hiroaki Shitama, Takashi Adachi, Masahiko Miyashiro
  • Patent number: 9902725
    Abstract: The present invention provides novel compounds of formula (I) that are modulators of RORgamma. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the modulation of RORgamma has therapeutic effects, for instance in autoimmune diseases, autoimmune-related diseases, inflammatory diseases, fibrotic diseases, or cholestatic diseases.
    Type: Grant
    Filed: December 22, 2015
    Date of Patent: February 27, 2018
    Assignee: Genfit
    Inventors: Jean-Francois Delhomel, Robert Walczak, Zouher Majd, Emilie Pihan, Pascal Bonnet, Enrico Perspicace
  • Patent number: 9879096
    Abstract: The present invention provides a process for the preparation of sugammadex sodium involving the step of: reacting 6-perdeoxy-6-per-halo-gamma-cyclodextrin with 3-mercapto propionic acid in the presence of alkali metal alkoxide in an organic solvents. The invention also provides a process for purifying the sugammadex or its pharmaceutically acceptable salts using water and organic solvents.
    Type: Grant
    Filed: April 8, 2013
    Date of Patent: January 30, 2018
    Assignee: NEULAND LABORATORIES LIMITED
    Inventors: Ponnaiah Ravi, Praveenkumar Neela, Batthini Guruswamy, Sribhashyam Ravikanth, Uppala Manikya Rao
  • Patent number: 9879002
    Abstract: Isolated or pure compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including but not limited to psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing an isolated or pure compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: January 30, 2018
    Assignee: Omeros Corporation
    Inventors: Jennifer Lynn Gage, Kevin L. Harbol, Raghuram Bommagani, Durga Varaprasad Botla, Laxma Reddy Karnati, Satyamurthi Narayanan
  • Patent number: 9850238
    Abstract: The present invention is directed to a pure enantiomer of 1-(5-(4-chloro-3, 5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, in particular, (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone. The present invention is also directed a crystal structure of (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, a pharmaceutical composition of (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, a method of inhibiting PDE10 with (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, and a process and particular individual intermediates used in the production of (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone.
    Type: Grant
    Filed: October 12, 2016
    Date of Patent: December 26, 2017
    Assignee: Omeros Corporation
    Inventors: Neil S. Cutshall, Kenneth M. Ferguson, Charles Prince Zuta
  • Patent number: 9849098
    Abstract: A method for treating a respiratory injury or disease comprising: administering to a patient in need of treatment a pharmaceutical composition comprising a compound of general Formula I: or salt, ester, solvate, hydrate, or prodrug thereof; wherein: x is an integer from 1 to 10; A and B are each, independently, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-6alkyl, C3-7 heterocycloalkyl, C3-7 heterocycloalkyl-C1-6 alkyl, C6-10aryl, C6-10aryl-C1-6alkyl, C3-9 heteroaryl, or C3-9heteroaryl-C1-6alkyl; and n and p are each, independently, integers from 1 to 10; and a pharmaceutically acceptable carrier, excipient, or diluent.
    Type: Grant
    Filed: December 9, 2014
    Date of Patent: December 26, 2017
    Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education, The United States of America as represented by the Department of Veterans Affairs
    Inventors: Beibei Chen, Rama Mallampalli
  • Patent number: 9776991
    Abstract: The present invention relates to compounds of the formula (I), wherein R1, R2, R3, R4 and X have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They are highly potent and selective soluble epoxide hydrolase inhibitors and are suitable, for example, for the therapy and prophylaxis of renal failure, diabetic nephropathy, type 2 diabetes mellitus, cardiovascular diseases, inflammatory diseases or could show beneficial effects in pain, dyslipidemia, atherosclerosis wound healing and stroke. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    Type: Grant
    Filed: December 2, 2014
    Date of Patent: October 3, 2017
    Assignee: SANOFI
    Inventors: Maria Mendez-Perez, Kristin Breitschopf, Katrin Lorenz, Hartmut Strobel, Li-hsing Wang, Alexander Schiffer, Jochen Goerlitzer
  • Patent number: 9709572
    Abstract: Embodiments of probes for selectively detecting compounds having a thiol group and an amino group, e.g., cysteine and/or homocysteine, are disclosed, along with methods and kits for detecting the compounds in neutral media with the probes. The probes have a structure according to the general formula where R1-R4 independently are hydrogen hydroxyl, halogen, thiol, thioether, lower aliphatic, or lower alkoxy, x is an integer from 0 to 4, and each R5 independently is halogen, hydroxyl, thiol, thioether, lower aliphatic, or lower alkoxy. Embodiments of the disclosed probes are capable of undergoing condensation/cyclization reactions with cysteine and/or homocysteine. Cysteine and/or homocysteine can be selectively detected and identified by determining fluorescence emission of the probes at characteristic wavelengths.
    Type: Grant
    Filed: November 24, 2015
    Date of Patent: July 18, 2017
    Assignee: Portland State University
    Inventors: Robert Strongin, Xiaofeng Yang
  • Patent number: 9682965
    Abstract: Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Grant
    Filed: November 17, 2016
    Date of Patent: June 20, 2017
    Assignee: Zafgen, Inc.
    Inventors: James E. Vath, Robert Zahler
  • Patent number: 9670157
    Abstract: The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R1 to R3, R5 to R9, A, P, V, W, X, Y and Z are as defined herein.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: June 6, 2017
    Assignee: Kalvista Pharmaceuticals Limited
    Inventors: Christine Elizabeth Allan, Andrzej Roman Batt, Rebecca Louise Davie, Hannah Joy Edwards, David Michael Evans, Stephen John Pethen
  • Patent number: 9657058
    Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
    Type: Grant
    Filed: January 7, 2015
    Date of Patent: May 23, 2017
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Kevin D. Shenk, Francesco Parlati, Han-jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
  • Patent number: 9597318
    Abstract: The invention provides compounds of formula (I) wherein X is O or S; R1 is H, OH, SH, nitro, NH2, NHC1-6alkyl, N(C1-6alkyl)2, halo, haloC1-6alkyl, CN, C1-6-alkyl, OC1-6alkyl, C1-6alkylCOOH, C1-6alkylCOOC1-6alkyl, C2-6-alkenyl, C3-10cycloalkyl, C6-10aryl, C1-6alkylC6-10aryl, heterocyclyl, heteroaryl, CONH2, CONHC1-6alkyl, CON(C1-6alkyl)2, OCOC1-6alkyl, or is an acidic group, such as a group comprising a carboxyl, phosphate, phosphinate, sulfate, sulfonate, or tetrazolyl group; R2 is as defined for R1 or R1 and R2 taken together can form a 6-membered aromatic ring optionally substituted by up to 4 groups R5; R3 is H, halo (preferably fluoro), or CHal3 (preferably CF3); each R5 is defined as for R1; V1 is a covalent bond, —O—, or a C1-20alkyl group, or C2-20-mono or multiply unsaturated alkenyl group; said alkyl or alkenyl groups being optionally interrupted by one or more heteroatoms selected from O, NH, N(C1-6 alkyl), S, SO, or SO2; M1 is absent or is a C5-10 cyclic group or a C5-15 aromatic group; and R
    Type: Grant
    Filed: October 4, 2010
    Date of Patent: March 21, 2017
    Assignee: Avexxin AS
    Inventors: George Kokotos, Berit Johansen, Victoria Magrioti, Michael Tsakos
  • Patent number: 9573918
    Abstract: The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.
    Type: Grant
    Filed: May 8, 2013
    Date of Patent: February 21, 2017
    Assignee: Zafgen, Inc.
    Inventors: Robert Zahler, James E. Vath
  • Patent number: 9573930
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.
    Type: Grant
    Filed: January 5, 2016
    Date of Patent: February 21, 2017
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 9555040
    Abstract: Provided herein are methods of administering N-(5-tert-butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea, or a pharmaceutically acceptable salt or solvate thereof, to human patients, including a specific patient population. Specifically, dosing, dosing schedules or dosing regimens are provided herein. Methods of treating proliferative diseases or FLT-3 mediated diseases in humans are also provided.
    Type: Grant
    Filed: September 17, 2014
    Date of Patent: January 31, 2017
    Assignee: Ambit Biosciences Corporation
    Inventors: Robert E. Corringham, Joyce K. James, Patrick B. O'Donnell
  • Patent number: 9556120
    Abstract: The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
    Type: Grant
    Filed: November 26, 2014
    Date of Patent: January 31, 2017
    Assignee: Athenex, Inc.
    Inventors: David G. Hangauer, Jr., Debasis Patra, Jeremy A. Cody, Grant J. Palmer, Paul K. Isbester, Jonathon Salsbury
  • Patent number: 9549935
    Abstract: This invention provides methods and compositions for treating or preventing migraine headache and/or symptoms thereof in a subject. The method comprises administering to the subject in need thereof a therapeutically effective amount of noribogaine, noribogaine derivative, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 17, 2015
    Date of Patent: January 24, 2017
    Assignee: DEMERX, INC.
    Inventor: Holger Weis
  • Patent number: 9527876
    Abstract: Provided are prodrugs of a bicyclic substituted pyrimidine type PDE-5 inhibitors, pharmaceutically acceptable salts or stereoisomers thereof. Also provided are methods for preparing these prodrug compounds, pharmaceutical preparations, and pharmaceutical compositions, as well as a use of these compounds, pharmaceutical preparations and pharmaceutical compositions in the manufacture of medicaments for treatment and/or prophylaxis of sexual dysfunction and lower urinary tract symptoms.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: December 27, 2016
    Assignee: Xuanzhu Pharma Co., Ltd.
    Inventors: Chutian Shu, Yongqian Wu
  • Patent number: 9498475
    Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R7, R6, X and Y have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Grant
    Filed: September 24, 2015
    Date of Patent: November 22, 2016
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Andreas Goutopoulos, Thomas E. Richardson, Jiezhen Li, Brian H. Heasley, Pandi Bharathi
  • Patent number: 9295256
    Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: March 29, 2016
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Seitz, Jurgen Benting, Ulrike Wachendorff-Neumann