Additional Hetero Ring Attached Directly Or Indirectly To The Morpholine Ring By Nonionic Bonding Patents (Class 514/231.5)
  • 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: 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: 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: 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: 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: 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: 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: 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: 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: 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
  • Patent number: 9174969
    Abstract: The subject invention concerns methods and compounds for inhibiting Shp2.
    Type: Grant
    Filed: July 21, 2009
    Date of Patent: November 3, 2015
    Assignee: UNIVERSITY OF SOUTH FLORIDA
    Inventors: Jie Wu, Nicholas J. Lawrence, Said M. Sebti
  • Patent number: 9174960
    Abstract: Dibenzylidene and heterobenzylideneacetone derivatives, related 4-piperidones, related 4-thiopyranones and the corresponding sulfinyl- and sulfonyl-analogues for their use for prophylaxis or treatment of trypanosomiasis and leishmaniasis.
    Type: Grant
    Filed: September 20, 2010
    Date of Patent: November 3, 2015
    Assignee: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Elisabeth Davioud-Charvet, Ingrid Nicole Wenzel, Thomas J. J. Müller, Gilles Hanquet, Don Antoine Lanfranchi, Frédéric Leroux, Thibault Gendron
  • Patent number: 9045441
    Abstract: The present disclosure relates to (thio)morpholine derivatives of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof; with the proviso that the derivative of formula (I) is not 2-(4-ethylphenyl)-4-morpholinoethanol or 4-[4-(2-hydroxyethyl)-2-morpholinyl]benzeneacetonitrile or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the disclosure have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.
    Type: Grant
    Filed: August 27, 2010
    Date of Patent: June 2, 2015
    Assignee: ABBVIE BAHAMAS LIMITED
    Inventors: Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Axel Stoit, Harmen Mons, Eric Ronken, Elizabeth Van Der Kam, Jurjen Frankena, Adrian Hobson
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Patent number: 9029370
    Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, X, Z, Ar, and n are as described in the claims, Ar is phenyl or heteroaryl, selected from the group consisting of 1H-indazole-3yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyrimidine-5-yl, 1H-pyrazole-3-yl, 1H-pyrazole-4-yl and 1H-pyrazole-5-yl; or to a pharmaceutically suitable acid addition salt thereof, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Grant
    Filed: June 1, 2012
    Date of Patent: May 12, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Roger Norcross, Philippe Pflieger
  • Patent number: 9029371
    Abstract: The present invention relates to bisaryl (thio)morpholine derivatives of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof, with the proviso that the derivative of formula (I) is not 2-[4-(4-chlorophenoxy)-2-chlorophenyl]-4 -morpholineethanol. The compounds of the invention have affinity to S1 Preceptors and may be used in the treatment, alleviation or prevention of S1 Preceptor mediated diseases and conditions.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: May 12, 2015
    Assignee: Abbvie B.V.
    Inventors: Wouter I. Iwema Bakker, Raymond Bronger
  • Publication number: 20150105392
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Publication number: 20150057278
    Abstract: Amido compounds are disclosed that have a formula represented by the following: and wherein Cy1, Cy2, 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: Application
    Filed: September 10, 2012
    Publication date: February 26, 2015
    Inventors: Dan Littman, Jun R. Huh, Ruili Huang, Wenwei Huang, Erika E. Englund
  • Publication number: 20150051144
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as hyperlipidemia and also have a beneficial effect on cholesterol.
    Type: Application
    Filed: September 26, 2012
    Publication date: February 19, 2015
    Inventors: Harikishore Pingali, Vrajesh Pandya
  • Publication number: 20150025068
    Abstract: A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 22, 2015
    Inventors: Jessica Martinsson, Katarina Faernegardh, Mattias Joensson, Rune Ringom
  • Publication number: 20150025069
    Abstract: This invention is directed to analogs of 5-(tetradecyloxy)-2-furancarboxylic acid (TOFA) and their use in the treatment of dermatological disorders or conditions characterized by sebaceous gland hyperactivity, such as acne and oily skin, and other dermatological disorders and conditions. This invention is also directed to pharmaceutical compositions comprising analogs of TOFA and a pharmaceutically acceptable excipient for dermatological or oral administration.
    Type: Application
    Filed: October 3, 2014
    Publication date: January 22, 2015
    Inventors: Timothy Scott Daynard, Geoffrey C. Winters, David W.C. Hunt
  • Patent number: 8927589
    Abstract: Compounds of Formulas 1 and 2 where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: January 6, 2015
    Assignee: Allergan, Inc.
    Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
  • Patent number: 8927710
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: January 6, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Publication number: 20150005275
    Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, R3, L, and the subscript m 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, and methods of treatment using the same, for the treatment of cystic fibrosis by administering a compound of the invention.
    Type: Application
    Filed: May 6, 2014
    Publication date: January 1, 2015
    Inventors: Steven Emiel Van der Plas, Oscar Mammoliti, Christel Jeanne Marie Menet, Giovanni Alessandro Tricarico, Ann De De Blieck, Caroline Martine Andrée Marie Joannesse, Hans Kelgtermans, Tom Roger Lisette De Munck
  • Patent number: 8901313
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: December 2, 2014
    Assignee: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti