Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 514/321)
  • Patent number: 10336771
    Abstract: The present invention provides compounds that modulate protein function, to restore protein homeostasis, including cytokine, CK1?, GSPT1, aiolos, and/or ikaros activity, and cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions, including in combination with other cytokine and inflammatory mediators, are provided. Methods of treatment, amelioration, or prevention of diseases, disorders, or conditions associated with a protein, such as diseases, disorders, and conditions associated with cytokines, including inflammation, fibromyalgia, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, inflammatory bowel diseases, Crohn's disease, ulcerative colitis, uveitis, inflammatory lung diseases, chronic obstructive pulmonary disease, Alzheimer's disease, and cancer, are provided.
    Type: Grant
    Filed: June 18, 2018
    Date of Patent: July 2, 2019
    Assignee: BioTheryX, Inc.
    Inventors: Kyle W. H. Chan, Paul E. Erdman, Leah Fung, Frank Mercurio, Robert Sullivan, Eduardo Torres
  • Patent number: 10265296
    Abstract: Methods for the treatment of systemic disorders treatable with mast cell stabilizers, including mast cell related disorders, are provided.
    Type: Grant
    Filed: August 5, 2016
    Date of Patent: April 23, 2019
    Assignee: RESPIVANT SCIENCES GMBH
    Inventors: William Gerhart, Pravin Soni, Robert Craig Armstrong
  • Patent number: 10212930
    Abstract: Grease-like compositions are provided for repelling insects and preventing undesirable behavior in hoofed animals. The compositions utilize nontoxic mineral, synthetic, or vegetable oil based gels containing silica, clay, urea, polytetrafluoroethylene, or metallic soap thickeners and capsaicin.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: February 26, 2019
    Assignee: Pacific Tech Industries, Inc.
    Inventors: Richard Numata, Ryan Willey
  • Patent number: 10085446
    Abstract: Grease-like compositions are provided for repelling rodents. The compositions utilize nontoxic mineral, synthetic, or vegetable oil based gels containing silica, clay, urea, polytetrafluoroethylene, or metallic soap thickeners and capsaicin.
    Type: Grant
    Filed: June 23, 2017
    Date of Patent: October 2, 2018
    Assignee: Pacific Tech Industries, Inc.
    Inventors: Richard Numata, Ryan Willey
  • Patent number: 10076581
    Abstract: The present invention relates to deuterated and optionally detectably labeled compounds of formula (I) and formula (V): and salts thereof, wherein R1, R2, A, and X10-X19 have any of the values defined in the specification. Also included are pharmaceutical compositions comprising such compounds and salts, and methods of using such compounds and salts as imaging agents.
    Type: Grant
    Filed: January 26, 2016
    Date of Patent: September 18, 2018
    Assignee: Genentech, Inc.
    Inventors: Jan Marik, Joseph P. Lyssikatos, Simon Williams
  • Patent number: 10071989
    Abstract: The present invention relates to substituted cinnamamide derivatives, the method for preparing thereof and the use thereof. Each of said derivatives has a structure of formula (I). The method for preparing the substituted cinnamamides and their derivatives of the present invention is also disclosed. Substituted piperonal derivatives are selected as starting materials to prepare the substituted cinnamamide derivatives of the present invention by Wittig reaction and acid-amine condensation reaction. Further, a use of the present compounds in preventing and treating depressive-type mental diseases is disclosed.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: September 11, 2018
    Assignee: TASLY PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Xiaohui Ma, Yuanpeng Jin, Min Han, Shuiping Zhou, Wangyi Zhou, Xuejun Luo, Guocheng Wang, Lulu Yan, Lanlan Zhang, Yonghong Zhu
  • Patent number: 10040804
    Abstract: The present invention provides compounds that modulate protein function, to restore protein homeostasis, including cytokine, CK1?, GSPT1, aiolos, and/or ikaros activity, and cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions, including in combination with other cytokine and inflammatory mediators, are provided. Methods of treatment, amelioration, or prevention of diseases, disorders, or conditions associated with a protein, such as diseases, disorders, and conditions associated with cytokines, including inflammation, fibromyalgia, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, inflammatory bowel diseases, Crohn's disease, ulcerative colitis, uveitis, inflammatory lung diseases, chronic obstructive pulmonary disease, Alzheimer's disease, and cancer, are provided.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: August 7, 2018
    Assignee: Biotheryx, Inc.
    Inventors: Kyle W. H. Chan, Paul E. Erdman, Leah Fung, Frank Mercurio, Robert Sullivan, Eduardo Torres
  • Patent number: 10034872
    Abstract: Methods of treating, preventing and/or managing multiple myeloma are disclosed. Specific methods encompass the administration of an immunomodulatory compound, e.g., lenalidomide or pomalidomide with an anti-CS1 antibody, e.g., elotuzumab in patients who have received autologous stem cell transplantation.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: July 31, 2018
    Assignee: Celgene Corporation
    Inventors: Anjan Thakurta, Mohamed Hussein, Christian Jacques
  • Patent number: 9907302
    Abstract: Grease-like compositions are provided for repelling insects and preventing undesirable behavior in hoofed animals. The compositions utilize nontoxic mineral, synthetic, or vegetable oil based gels containing silica, clay, urea, polytetrafluoroethylene, or metallic soap thickeners and capsaicin.
    Type: Grant
    Filed: August 5, 2016
    Date of Patent: March 6, 2018
    Assignee: Pacific Tech Industries, Inc.
    Inventors: Richard Numata, Ryan Willey
  • Patent number: 9833447
    Abstract: This invention relates to 4-{[4-({([4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]-oxy}methyl)piperidin-1-yl]methyl}tetrahydro-2H-pyran-4-carboxylic acid for use in therapeutic treatment of the human body. In particular, it relates to the compound having selective 5-HT4 receptor agonism, which is useful for treating gastroparesis, or preventing or delaying the onset or the progression of gastroparesis.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: December 5, 2017
    Assignee: RAQUALIA PHARMA INC.
    Inventors: Nobuyuki Takahashi, Toshinori Yamamoto, Kaoru Shimada, Hirohide Noguchi
  • Patent number: 9738773
    Abstract: Among other things the invention provides novel flame-retardant compounds useful for increasing the flame retardance of polymers.
    Type: Grant
    Filed: August 7, 2015
    Date of Patent: August 22, 2017
    Assignee: Central Michigan University
    Inventors: Bob A. Howell, Yoseph G. Daniel
  • Patent number: 9718854
    Abstract: The invention provides compounds of formula (I) with substituents as specified in claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac.
    Type: Grant
    Filed: March 20, 2012
    Date of Patent: August 1, 2017
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ramesh Kaul, Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Kun Liu, Harold G. Selnick, Zhongyong Wei, Changwei Mu, Yaode Wang, Xiaona Wang
  • Patent number: 9706774
    Abstract: Grease-like compositions are provided for repelling rodents. The compositions utilize nontoxic mineral, synthetic, or vegetable oil based gels containing silica, clay, urea, polytetrafluoroethylene, or metallic soap thickeners and capsaicin.
    Type: Grant
    Filed: January 7, 2016
    Date of Patent: July 18, 2017
    Assignee: Pacific Tech Industries, Inc.
    Inventors: Richard Numata, Ryan Willey
  • Patent number: 9676764
    Abstract: A compound having the structure according to formula III wherein: X is NH or S; R1 is H or (1C-4C)alkyl; R2 is (1C-4C)alkyl, phenyl or a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, which alkyl, phenyl or aromatic ring is optionally substituted with one or more groups selected from (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, phenyloxy, phenylthio, halogen, or nitro; R3 and R4 are each independently H, (1C-6C)alkyl, (2C-6C) alkenyl, (2C-6C)alkynyl, cyano, (3C-6C)cycloalkyl, phenyl, a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, a monocyclic non-aromatic ring having one or more N-, O- or S-atoms in the ring, each optionally substituted with hydroxyl, (1C-4C)alkoxy, phenyl, cycloalkyl, piperidyl, piperazinyl, furyl, thienyl, pirazinyl, pyrrolyl, 2H-pyrrolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyrrolidonyl, pyrrolinyl, imidazolinyl, imidazolyl, a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring,
    Type: Grant
    Filed: July 22, 2016
    Date of Patent: June 13, 2017
    Assignees: Compound Handling B.V., Stichting Katholieke Universiteit
    Inventors: Onno Van Hooij, Jacobus Antonius Schalken, Hendrik Engelbertus Vietor, Dennis Patrick Piet, Petrus Emmanuel Marie Maas, Johann Heinrich Tijhuis, Sirik Deerenberg, Nanda Elisabeth Sprenkels, Siu Ha Tang
  • Patent number: 9624172
    Abstract: The present invention provides novel polymorphs of Lomitapide, process for their preparation and pharmaceutical compositions comprising them. The present invention also provides a novel polymorph of Lomitapide mesylate, process for its preparation and pharmaceutical compositions comprising it.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: April 18, 2017
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Jambula Mukunda Reddy, Bandi Vamsi Krishna
  • Patent number: 9446038
    Abstract: A method and composition for treating serotonin receptor-mediated conditions.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: September 20, 2016
    Assignee: Vanda Pharmaceuticals, Inc.
    Inventors: Mihael H. Polymeropoulos, Paolo Baroldi, Curt Wolfgang
  • Patent number: 9371387
    Abstract: Disclosed is a pharmaceutical composition for the prevention or treatment of ischemic heart diseases, comprising as an active ingredient an inhibitor which acts to restrain mononuclear phagocyte system cells from synthesizing or releasing AGE-albumin, which induces the apoptosis of cardiomyocytes upon the onset of the ischemic heart disease. Also, a method is provided for screening an inhibitor against the AGE-albumin synthesis or release of mononuclear phagocyte system cells. Inhibitory or suppressive of AGE-albumin-induced cell death, the pharmaceutical composition comprising as an active ingredient an inhibitor against the AGE-albumin synthesis or release of mononuclear phagocyte system cells can be applied to the prevention or treatment of a wide spectrum of ischemic heart diseases including myocardial infarction.
    Type: Grant
    Filed: November 12, 2012
    Date of Patent: June 21, 2016
    Assignee: GACHON UNIVERSITY OF INDUSTRY-ACADEMIC COOPERATION FOUNDATION
    Inventors: Bong Hee Lee, Kyung Hee Byun
  • Patent number: 9364470
    Abstract: The present invention provides methods and compositions for treating hyperlipidemia and/or hypercholesterolemia comprising administering to the subject an effective amount of an MTP inhibitor to inhibit hyperlipidemia and/or hypercholesterolemia in said subject, wherein said administration comprises an escalating series of doses of the MTP inhibitor. In some embodiments the method comprises administering at least three step-wise, increasing dosages of the MTP inhibitor to the subject. In some embodiments, the method further comprises the administration of one or more other lipid modifying compounds.
    Type: Grant
    Filed: December 4, 2015
    Date of Patent: June 14, 2016
    Assignee: The Trustees of the University of Pennsylvania
    Inventor: Daniel J. Rader
  • Patent number: 9364497
    Abstract: The invention relates to treatments of cognitive disorders e.g. Mild Cognitive Disorder comprising the use of agents which are capable of lowering homocysteine levels in a subject, preferably a human subject. Aspects of the invention relate to a method of treating such disorders comprising administering one or more B vitamins e.g. folic acid, Vitamin B6 and/or Vitamin B12 or derivatives thereof.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: June 14, 2016
    Assignee: Isis Innovation Limited
    Inventors: Anthony David Smith, Helga Margareta Refsum
  • Patent number: 9351962
    Abstract: The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators.
    Type: Grant
    Filed: January 16, 2015
    Date of Patent: May 31, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Fredrick Van Goor, Mark Miller, Jason McCartney, Jinglan Zhou, Vijayalaksmi Arumugam
  • Patent number: 9258997
    Abstract: Grease-like compositions are provided for repelling rodents. The compositions utilize nontoxic mineral, synthetic, or vegetable oil based gels containing silica, clay, urea, polytetrafluoroethylene, or metallic soap thickeners and capsaicin.
    Type: Grant
    Filed: December 11, 2014
    Date of Patent: February 16, 2016
    Assignee: Pacific Tech Industries, Inc.
    Inventors: Richard Numata, Ryan Willey
  • Patent number: 9211290
    Abstract: The invention relates to solid dispersions containing paroxetine mesylate. One solid dispersion contains amorphous paroxetine mesylate and a methacrylic acid-methyl methacrylate copolymer, where the weight ratio of paroxetine mesylate to polymer ranges from about 30:70 to about 90:10. Another solid dispersion contains amorphous paroxetine mesylate and a -vinylpyrrolidone/vinylacetate copolymer (PVP-VA), where the weight ratio of paroxetine mesylate to copolymer ranges from about 30:70 to about 50:50. An amorphous solid dispersion of the invention may have a single glass transition temperature. An amorphous solid dispersion is stable for at least 48 hours at 60° C. and 75% relative humidity. A further embodiment of the invention relates to pharmaceutical compositions of paroxetine mesylate comprising a solid dispersion of the invention and at least one pharmaceutically acceptable excipient.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: December 15, 2015
    Assignee: NOVEN THERAPEUTICS, LLC
    Inventors: David A. Engers, Yonglai Yang, Stephan Parent, Travis Houston, Bruce Charles Friedman
  • Patent number: 9187463
    Abstract: The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms (Polymorph Form I or Polymorph Form II), and to processes for the preparation of, compositions containing and to uses of, such polymorph forms.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: November 17, 2015
    Assignee: RAQUALIA PHARMA INC.
    Inventors: Toyoharu Numata, Hirohide Noguchi, Nobuaki Waizumi, Takashi Kojima
  • Patent number: 9161913
    Abstract: The present invention provides a stabilized pharmaceutical suspension of carisbamate for pediatric and adult use. More particularly, the suspension is stabilized with hypromellose (HPMC) to prevent crystal growth of the suspended particles and to prevent re-crystallization of the drug product with change in polymorphic form.
    Type: Grant
    Filed: August 9, 2012
    Date of Patent: October 20, 2015
    Assignee: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Roger Embrechts, Cedric De Leersnijder
  • Patent number: 9067889
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases, gastrointestinal diseases and respiratory diseases.
    Type: Grant
    Filed: August 31, 2012
    Date of Patent: June 30, 2015
    Assignee: Amakem NV
    Inventors: Jo Alen, Sandro Boland, Arnaud Pierre Jean Bourin, Olivier Defert, Dirk Leysen
  • Publication number: 20150148329
    Abstract: Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1A2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent.
    Type: Application
    Filed: June 24, 2013
    Publication date: May 28, 2015
    Inventors: Allen B. Reitz, Garry Robert Smith
  • Publication number: 20150133444
    Abstract: The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 14, 2015
    Inventors: Venumadhav Janganati, Narsimha Reddy Penthala, Peter A. Crooks, Craig T. Jordan
  • Publication number: 20150133465
    Abstract: The invention provides compounds of formula (I): wherein R1-R3, n, and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: Edmond J. LaVoie, Ajit Parhi, Daniel S. Pilch, Yongzheng Zhang, Malvika Kaul
  • Publication number: 20150133499
    Abstract: This invention relates to novel pharmaceutical compositions comprising a therapeutically effective amount of a slow-release formulation of 5-hydroxytryptophan (5-HTP) and a serotonin-enhancing compound. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating CNS disorders, including depressive disorders, bipolar disorders, anxiety disorders, obesity and pain.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 14, 2015
    Inventors: Jacob Pade Ramsoe Jacobsen, Brian Frostrup
  • Patent number: 9029357
    Abstract: The present patent application concerns new ligands of the H4-receptor, their process of preparation and their therapeutic use.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: May 12, 2015
    Assignee: Bioprojet
    Inventors: Isabelle Berrebi-Bertrand, Xavier Billot, Thierry Calmels, Marc Capet, Denis Danvy, Stéphane Krief, Olivier Labeeuw, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Philippe Robert, Jean-Charles Schwartz
  • Publication number: 20150125441
    Abstract: The present invention provides methods of treating and pharmaceutical compositions useful for treating a mood disorder or depressive symptoms associated with pain, inducing analgesia and treating pain in a subject by administering a pharmaceutically effective amount of an agent capable of one or more of increasing GluA1 level, expression, concentration, or biological activity, increasing calcium permeable AMPA (? amino-3-hydroxy-5-methylisoxazole-4-propionic acid) receptor (CPAR) level, expression, concentration, or biological activity or potentiating a CPAR current. The agent may be an AMPA potentiator or ampakine. The agent may increase AMPA receptor currents by slowing the deactivation of open channels and may be, for instance, 2-pyrrolidinone, 4-[2-(phenylsulfonylamino)ethylthio]-2,6-difluorophenoxyacetamide (PEPA) or LY451646. The agent may also be a protein, RNA or DNA product.
    Type: Application
    Filed: May 24, 2013
    Publication date: May 7, 2015
    Applicant: New York University
    Inventors: Jing Wang, Edward Ziff
  • Patent number: 9024038
    Abstract: Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: May 5, 2015
    Assignee: Purdue Research Foundation
    Inventors: Arun K. Ghosh, Bruno D. Chapsal, Hiroaki Mitsuya, Cuthbert D. Martyr
  • Publication number: 20150119366
    Abstract: Pharmaceutical compositions of the invention comprise alkylated imino sugars derivatives having a disease-modifying action in the treatment of diseases associated with glucosidase activity that include Viral hemorrhagic fevers, and any other diseases involving glucosidase activity.
    Type: Application
    Filed: March 27, 2013
    Publication date: April 30, 2015
    Inventors: Yanming Du, Xiaodong Xu, Hong Ye, Jinhong Chang, Timothy M. Block
  • Publication number: 20150119380
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.
    Type: Application
    Filed: December 28, 2012
    Publication date: April 30, 2015
    Inventors: Matthew G. Woll, Guangming Chen, Soongyu Choi, Amal Dakka, Song Huang, Gary Mitchell Karp, Chang-Sun Lee, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Sergey Paushkin, Hongyan Qi, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Emmanuel Pinard, Hasane Ratni
  • Publication number: 20150119383
    Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.
    Type: Application
    Filed: June 5, 2014
    Publication date: April 30, 2015
    Inventors: Barry S. Fogel, William D. Kerns, Kei-Lai Fong, San-Laung Chow, Edward Lin, David Wong
  • Patent number: 9018213
    Abstract: Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and clambering symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: April 28, 2015
    Assignees: Huazhong University of Science & Technology, NHWA Pharma. Corporation
    Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Xin Liu, Song Zhao, Bifeng Liu, Minquan Yu, Yinli Qiu
  • Publication number: 20150105354
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicants: MERCK SHARP & DOHME CORP., PHARMACOPEIA, LLC
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, JR., John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
  • Publication number: 20150099731
    Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 me
    Type: Application
    Filed: May 5, 2014
    Publication date: April 9, 2015
    Applicant: University of Kentucky
    Inventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
  • Patent number: 8999972
    Abstract: The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, and depression. This invention could also be used for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: April 7, 2015
    Assignee: Neuronascent, Inc.
    Inventor: Judith Kelleher-Andersson
  • Publication number: 20150093458
    Abstract: A nutritional supplement for increasing cognitive functioning. The supplement includes a flavonoid such as luteolin and a labdane diterpene such as forskolin. The supplement can also include one or any combination of L-phenylalanine, L-carnitine, acetyl-L-carnitine, and vitamin B6. Artichoke extract can be used as a source of luteolin. Methods of using the nutritional supplements to increase cognitive functioning are also included.
    Type: Application
    Filed: September 27, 2014
    Publication date: April 2, 2015
    Inventor: Justin SHER
  • Publication number: 20150094304
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 2, 2015
    Inventors: SARA SABINA HADIDA RUAH, PETER DIEDERIK JAN GROOTENHUIS, FREDRICK F. VAN GOOR, JINGLAN ZHOU, BRIAN RICHARD BEAR, MARK THOMAS MILLER, JASON MC CARTNEY, MEHDI MICHEL DJAMEL NUMA
  • Patent number: 8993575
    Abstract: The present invention belongs to the medicinal chemistry field, and specifically discloses a [1,3,4]oxadiazole derivative with the structure of general formula (I) and pharmaceutically acceptable salt thereof. The compound can be used to prepare a medicine for preventing or treating a disease of the central nervous system.
    Type: Grant
    Filed: April 1, 2012
    Date of Patent: March 31, 2015
    Assignees: Huazhong University of Science & Technology, NHWA Pharma Corporation
    Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Bifeng Liu, Xiaojun Feng, Song Zhao, Shicheng Liu, Minquan Yu, Yu Lan, Yinli Qiu
  • Patent number: 8987250
    Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: March 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
  • Patent number: 8987299
    Abstract: Compounds of formula (I) described herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: March 24, 2015
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Fabio Rancati, Ian Linney
  • Publication number: 20150080364
    Abstract: Provided herein are carbamate compounds which may be useful in the treatment of for example, pain, solid tumors and/or obesity.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 19, 2015
    Applicants: Abide Therapeutics, Inc., The Scripps Research Insititute
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Dong-Hui Wang, Olivia Weber, Benjamin F. Cravatt, Micah J. Niphakis, Armand Cognetta, Jae Won Chang
  • Publication number: 20150080380
    Abstract: This invention relates to novel therapeutic uses for compounds which are inverse agonists of the H3 receptor. In particular this invention relates to therapeutic use of these compounds in the treatment of Multiple Sclerosis.
    Type: Application
    Filed: January 15, 2013
    Publication date: March 19, 2015
    Inventors: Hongtao Lu, Rong Wang
  • Patent number: 8980913
    Abstract: Compounds of formula (I) defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: March 17, 2015
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Fabio Rancati, Ian Linney, Chris Knight, Wolfgang Schmidt
  • Publication number: 20150072958
    Abstract: Various embodiments of the present invention relate to, among other things, compounds and methods of using those compounds to treat an HIV infection. The compounds of the various embodiments of the present invention provide, among other things, therapeutic agents having enhanced penetration capability across the blood-brain barrier, such that they can enter the CNS to treat an HIV-1 infection in the CNS.
    Type: Application
    Filed: September 10, 2014
    Publication date: March 12, 2015
    Inventors: Arun K. Ghosh, Hiroaki Mitsuya, Sofiya Yashchuk
  • Publication number: 20150073019
    Abstract: A compound having the structure according to formula III wherein: X is NH or S; R1 is H or (1C-4C)alkyl; R2 is (1C-4C)alkyl, phenyl or a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, which alkyl, phenyl or aromatic ring is optionally substituted with one or more groups selected from (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, phenyloxy, phenylthio, halogen, or nitro; R3 and R4 are each independently H, (1C-6C)alkyl, (2C-6C) alkenyl, (2C-6C)alkynyl, cyano, (3C-6C)cycloalkyl, phenyl, a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, a monocyclic non-aromatic ring having one or more N-, O- or S-atoms in the ring, each optionally substituted with hydroxyl, (1C-4C)alkoxy, phenyl, cycloalkyl, piperidyl, piperazinyl, furyl, thienyl, pirazinyl, pyrrolyl, 2H-pyrrolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyrrolidonyl, pyrrolinyl, imidazolinyl, imidazolyl, a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, whereb
    Type: Application
    Filed: March 5, 2013
    Publication date: March 12, 2015
    Inventors: Onno Van Hooij, Jacobus Antonius Schalken, Hendrik Engelbertus Viëtor, Dennis Patrick Piet, Petrus Emmanuel Marie Maas, Johann Heinrich Tijhuis, Sirik Deerenberg, Nanda Elisabeth Sprenkels, Siu Ha Tang
  • Publication number: 20150065490
    Abstract: Compounds of formula I in free or salt or solvate form, wherein X has the meaning indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ?2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Application
    Filed: November 6, 2014
    Publication date: March 5, 2015
    Applicant: NOVARTIS AG
    Inventors: Bernard CUENOUD, Robin Alec FAIRHURST, Roger John TAYLOR, David BEATTIE