Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 514/214.02)
  • Patent number: 11370802
    Abstract: The present invention relates to a compound of formula (I) wherein Ar is (II) or (II); R is CH3 or OCH3; or a pharmaceutically acceptable acid addition salt or a corresponding enantiomer thereof. The compounds are modulators of ?-secretase (A ?42) and may be useful for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis-Dutch type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
    Type: Grant
    Filed: January 21, 2019
    Date of Patent: June 28, 2022
    Assignee: Hoffmann-La Roche, Inc.
    Inventor: Hasane Ratni
  • Patent number: 11352369
    Abstract: Provided are a series of novel pyridine or pyrimidine derivatives which inhibit CDK9 and may be useful for the treatment of hyperproliferative diseases. In particular the compounds are of use in the treatment of proliferative disease such as cancer including hematological malignancies such as acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia, diffuse large B cell lymphoma, Burkitt's lymphoma, follicular lymphoma and solid tumors such as breast cancer, lung cancer, neuroblastoma and colon cancer.
    Type: Grant
    Filed: July 17, 2020
    Date of Patent: June 7, 2022
    Assignee: ASTRAZENECA AB
    Inventors: Bernard Barlaam, Christopher De Savi, Janet Hawkins, Alexander Hird, Michelle Lamb, Kurt Pike, Melissa Vasbinder
  • Patent number: 11084800
    Abstract: Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.
    Type: Grant
    Filed: August 29, 2019
    Date of Patent: August 10, 2021
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, Joel Charles Barrish, William Greenlee, Kyle J. Eastman
  • Patent number: 11077118
    Abstract: This invention provides a method for treating anxiety-related disorder or impulse control disorder, regulating food intake, attenuating food cravings, or treating anger and/or violence and disorders associated therewith in a patient, comprising administering to the patient in need thereof a therapeutically effective amount of ibogaine, ibogaine derivative, or a pharmaceutically acceptable salt and/or solvate thereof.
    Type: Grant
    Filed: March 9, 2017
    Date of Patent: August 3, 2021
    Assignee: DEMERX, INC.
    Inventor: Emeline Maillet
  • Patent number: 10941147
    Abstract: The present invention relates to a compound of formula I, 1-1 or 1-2 wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy, or lower alkoxy substituted by halogen; R1 may be different if n=2 or 3 n is 1, 2 or 3 Ar is a six membered heteroaryl group, selected from wherein R2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R3 is hydrogen or halogen; or to a pharmaceutically active acid addition salt thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
    Type: Grant
    Filed: October 30, 2017
    Date of Patent: March 9, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bjoern Bartels, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Hasane Ratni, Michael Reutlinger, Jérôme Charles Sarie, Greta Vastakaite
  • Patent number: 10928728
    Abstract: Compounds of the Formula (I), (II) and (III) wherein Ar is for example phenylene, biphenyleneor naphthylene, all of which are unsubstituted or substituted by C1-C4-alkyl, C2-C4-alkenyl, CN, OR11, SR11, CH 2OR11, COOR12, CONR12R13 or halogen; R1, R2, R7 and R8 independently of one another other are hydrogen or C1-C6-alkyl; R3 and R5 together and R4 and R6 together form a C2-C6-alkylene bridge which is unsubstituted or substituted by one ore more C1-C4-alkyl; R11 is hydrogen or C1-C6-alkyl; R12 and R13 independently of one another for example are hydrogen, phenyl, C1-C18-alkyl, C1-C18-alkyl which is interrupted by one or more O; n is 1-10; X is O, S or NR10; A and A1 are suitable linking groups; are suitable as photolatent bases.
    Type: Grant
    Filed: January 26, 2018
    Date of Patent: February 23, 2021
    Assignee: BASF SE
    Inventors: Kurt Dietliker, Katharina Misteli, Katia Studer, Tunja Jung, Lother Alexander Engelbrecht
  • Patent number: 10857129
    Abstract: The present invention relates to a vasopressin receptor 1B (V1B) antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in patients showing an elevated arginine vasopressin (AVP) level and/or an elevated copeptin level. The present invention further relates to a method for predicting the treatment response to a V1B antagonist in patients with depressive symptoms and/or anxiety symptoms.
    Type: Grant
    Filed: August 15, 2019
    Date of Patent: December 8, 2020
    Assignee: B.R.A.H.M.S GMBH
    Inventor: Florian Holsboer
  • Patent number: 10758533
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: January 2, 2019
    Date of Patent: September 1, 2020
    Assignee: NOVARTIS AG
    Inventors: Atwood Kim Cheung, Donovan Noel Chin, Natalie Dales, Aleem Fazal, Timothy Brian Hurley, John Kerrigan, Gary O'Brien, Lei Shu, Robert Sun, Moo Je Sung
  • Patent number: 10720584
    Abstract: Provided are: a charge-transporting varnish that contains a charge-transporting substance comprising an oligoaniline derivative represented by formula (1), a charge transporting substance that does not contain fluorine atoms, and an organic solvent; and an organic electroluminescent element including a thin film obtained from the varnish. (In the formula: R1 represents a hydrogen atom or an alkyl group that may be substituted; R2 to R10 each independently represent a hydrogen atom, a halogen atom, a nitro group, a cyano group, or an alkyl group, alkenyl group, alkynyl group, aryl group or heteroaryl group that may be substituted; A represents a prescribed fluorine atom-containing substituent; and k represents an integer from 1 to 20.
    Type: Grant
    Filed: May 25, 2016
    Date of Patent: July 21, 2020
    Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Toshiyuki Endo, Taichi Nakazawa
  • Patent number: 10591487
    Abstract: Disclosed is a angiogenesis inhibition determining method using MALDI mass spectrometry, and more particularly, relate to a method for detecting whether small molecules are bound with a target protein and for measuring a binding distribution between the small molecules and the target protein by comparing a result of MALDI mass spectrometry with a result of immunofluorescence of the small molecules, which are used as drugs, for the target protein, and for determining as angiogenesis is inhibited in a portion overlapping with a portion where the drug small molecules are present after the MALDI mass spectrometry in the cell or in the biosample including organelles and a portion where the target protein is present after immunofluorescence, as well as for detecting presence or absence and a distribution state of small molecules used as drugs in a sample by using MALDI mass spectrometry.
    Type: Grant
    Filed: October 25, 2016
    Date of Patent: March 17, 2020
    Assignee: Industry-Academic Cooperation Foundation, Yonsei University
    Inventors: Ho Jeong Kwon, Yonghyo Kim, György Marko-Varga
  • Patent number: 10561638
    Abstract: Provided are methods of treating patients suffering from or susceptible to at least one symptom of abuse of, dependence on, or withdrawal from at least one substance with Compound A. Also provided are methods of treating at least one phase of substance dependence on at least one substance in patients and certain methods of treating at least one phase of cocaine dependence in patients.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: February 18, 2020
    Assignee: Biotie Therapies, Inc.
    Inventors: Tom Woiwode, Mark Moran, Lesley Pickford
  • Patent number: 10463661
    Abstract: The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X1, X6, X8, Q1, Q2, Q3, Q4, Q5, Q6, Ring A, Ring B, W, W?, R2, R3, R, R?, m, n and q are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.
    Type: Grant
    Filed: August 3, 2018
    Date of Patent: November 5, 2019
    Assignee: BOEHRINGER INGELHEIM ANIMAL HEALTH USA INC.
    Inventors: Alan Long, Srinivas Reddy Gurrala
  • Patent number: 10081647
    Abstract: The present invention relates to Phosphate Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R1, R2, R3, R4, R5, R9 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Phosphate Substituted Quinolizine Derivative, and methods of using the Phosphate Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: March 25, 2016
    Date of Patent: September 25, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tao Yu, Sherman T. Waddell, John A. McCauley, Thomas H. Graham, Hong Li, Izzat Raheem, Jay A. Grobler
  • Patent number: 10071102
    Abstract: Described herein is a method of administering mirtazapine via the parenteral route to treat the decrease or loss of appetite and/or other disorders induced by undernutrition in cats.
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: September 11, 2018
    Assignee: VIRBAC
    Inventors: Karine De Mari, Annaele Sanquer
  • Patent number: 10023557
    Abstract: Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting plasma kallikrein. Furthermore, the subject compounds and compositions are useful for the treatment of diseases wherein the inhibition of plasma kallikrein inhibition has been implicated, such as angioedema and the like.
    Type: Grant
    Filed: June 30, 2016
    Date of Patent: July 17, 2018
    Assignee: LIFESCI PHARMACEUTICALS, INC.
    Inventors: Andrew McDonald, Shawn Qian
  • Patent number: 9951076
    Abstract: Provided are compounds having formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as disclosed herein, or a pharmaceutically salt thereof. Pharmaceutical compositions comprising the compounds and methods of their use, for instance in treating senility, senile confusion, psychoses, psychoneuroses when anxiety and nervous tension were present, cerebral arteriosclerosis, nausea, depression, fatigue, debilitation, mild behavioral disorders, irritability, emotional instability, antisocial attitudes, anxiety, vertigo or incontinence, or symptom thereof, or in improving cognitive function in individuals, for instance, in individuals with Down syndrome and other conditions, are also provided.
    Type: Grant
    Filed: August 24, 2016
    Date of Patent: April 24, 2018
    Assignee: Balance Therapeutics, Inc.
    Inventor: Lyndon Lien
  • Patent number: 9918948
    Abstract: The present invention relates to methods for the treatment or prevention of symptoms associated with post-traumatic stress disorder, and related pharmaceutical compositions. Of particular interest are pharmaceutical compositions comprising a very low dose of cyclobenzaprine, alone, or in combination with an alpha-1-adrenergic receptor antagonist, a beta-adrenergic antagonist, an anticonvulsant, a selective serotonin reuptake inhibitor or a serotonin-norepinephrine reuptake inhibitor.
    Type: Grant
    Filed: November 18, 2010
    Date of Patent: March 20, 2018
    Assignee: TONIX PHARMA HOLDINGS LIMITED
    Inventors: Seth Lederman, Herbert Harris
  • Patent number: 9862719
    Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.
    Type: Grant
    Filed: July 21, 2015
    Date of Patent: January 9, 2018
    Assignee: Gruenenthal GmbH
    Inventors: Claudia Hinze, Otto Aulenbacher, Bernd Sundermann, Stefan Oberboersch, Elmar Friderichs, Werner Englberger, Babette-Yvonne Koegel, Klaus Linz, Hans Schick, Helmut Sonnenschein, Birgitta Henkel, Valerie Sarah Rose, Michael Jonathan Lipkin
  • Patent number: 9845329
    Abstract: A method for producing a pyrrolopyrimidine ring-containing tricyclic compound represented by Formula (1) or a salt thereof. The method comprising the steps of: (I) reacting an organoborane reagent with a compound represented by Formula (2) or a salt thereof, and (II) performing an intramolecular cyclization reaction of the reaction product of step (I) in the presence of a zerovalent palladium catalyst and an alkali metal hydroxide.
    Type: Grant
    Filed: February 21, 2014
    Date of Patent: December 19, 2017
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Takao Uno, Tadashi Shimamura
  • Patent number: 9789119
    Abstract: Provided herein are methods, drug formulations, and dosing regimens for improving cognitive function in a normal or cognitively impaired subject. For instance, methods provided herein comprise administering a GABAA receptor antagonist so that peak concentration of the GABAA receptor antagonist occurs when the subject is asleep.
    Type: Grant
    Filed: January 30, 2015
    Date of Patent: October 17, 2017
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Craig C. Garner, H Craig Heller, Damien Colas, Daniel Z. Wetmore
  • Patent number: 9783535
    Abstract: This invention relates noribogaine derivatives, compositions and methods of use thereof.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: October 10, 2017
    Inventors: Deborah C. Mash, Richard D. Gless, Robert M. Moriarty
  • Patent number: 9765040
    Abstract: [Problem] Provided is a pharmaceutical, in particular, a pharmaceutical composition which is useful for the treatment of pain. [Means for Solution] The present inventors have made extensive studies using model animals with pain for the purpose of providing a therapeutic agent for pain. As a result, they have found that 11?-hydroxydehydrogenase type 1 (11?-HSD1) inhibitor, in particular, a triazole compound having a cyclic group at the 3-position (or 5-position) of a triazole ring has a good effect of ameliorating chronic pain. That is, according to the present invention, a pharmaceutical composition comprising an 11?-HSD1 inhibitor, in particular, the triazole compound of the present invention, as an active ingredient, is useful for the treatment of pain (particularly, neuropathic pain or fibromyalgia).
    Type: Grant
    Filed: September 6, 2011
    Date of Patent: September 19, 2017
    Assignee: Astellas Pharma Inc.
    Inventors: Tetsuo Kiso, Mina Tsukamoto
  • Patent number: 9758526
    Abstract: An object to be achieved by the present invention is to provide a novel compound having EGFR inhibitory effects and cell growth inhibitory effects, as well as a medication useful for the prevention and/or treatment of cancer based on the EGFR inhibitory effects. The present invention provides a compound represented by Formula (I) below, or a salt thereof.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: September 12, 2017
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Takao Uno, Katsumasa Nonoshita, Tadashi Shimamura
  • Patent number: 9701686
    Abstract: Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
    Type: Grant
    Filed: July 29, 2015
    Date of Patent: July 11, 2017
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Teresa Disingrini, Sergio Mantegani, Mario Varasi
  • Patent number: 9663523
    Abstract: The present invention relates to BET-protein-inhibitory, in particular BRD4-inhibitory 5-aryltriazoloazepines of the general formula (I) in which R1, R2, R3 and R4 have the meanings given for the general formula (I), to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for neoplastic disorders. The present invention further relates to the use of BET protein inhibitors in viral infections, in neurodegenerative disorders, in inflammatory diseases, in atherosclerotic disorders and in male fertility control.
    Type: Grant
    Filed: September 25, 2013
    Date of Patent: May 30, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Norbert Schmees, Joachim Kuhnke, Bernard Haendler, Roland Neuhaus, Pascale Lejeune, Stephan Siegel, Martin Krüger, Amaury Ernesto Fernandez-Montalvan, Hermann Künzer, Daniel Gallenkamp
  • Patent number: 9650386
    Abstract: An object to be achieved by the present invention is to provide a novel compound having EGFR inhibitory effects and cell growth inhibitory effects, as well as a medication useful for the prevention and/or treatment of cancer based on the EGFR inhibitory effects. The present invention provides a compound represented by Formula (I) below, or a salt thereof.
    Type: Grant
    Filed: August 22, 2014
    Date of Patent: May 16, 2017
    Assignee: Taiho Pharmaceutical Co., Inc.
    Inventors: Takao Uno, Katsumasa Nonoshita, Tadashi Shimamura
  • Patent number: 9650385
    Abstract: The present invention relates to novel polymorphic forms of alcaftadine, processes of preparing novel polymorphic forms of alcaftadine and pharmaceutical compositions thereof.
    Type: Grant
    Filed: June 27, 2016
    Date of Patent: May 16, 2017
    Assignee: Enaltec Labs Pvt. Ltd.
    Inventors: Sivakumar Bobba Venkata, Eswara Rao Kodali, Girish Bansilal Patel, Sanjay Dashrath Vaidya, Alok Pramod Tripathi
  • Patent number: 9611252
    Abstract: Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting plasma kallikrein. Furthermore, the subject compounds and compositions are useful for the treatment of diseases wherein the inhibition of plasma kallikrein inhibition has been implicated, such as angioedema and the like.
    Type: Grant
    Filed: February 11, 2016
    Date of Patent: April 4, 2017
    Assignee: LIFESCI PHARMACEUTICALS, INC.
    Inventors: Andrew McDonald, Shawn Qian
  • Patent number: 9591978
    Abstract: This invention is directed to a method for pre-screening an opioid-addicted patient to determine the patient's tolerance for a therapeutic dose of noribogaine.
    Type: Grant
    Filed: February 17, 2015
    Date of Patent: March 14, 2017
    Assignee: DEMERX, INC.
    Inventor: Lawrence Friedhoff
  • Patent number: 9586954
    Abstract: This invention relates generally to prodrugs of noribogaine. This invention also relates to pharmaceutical compositions comprising the prodrugs of noribogaine as well as method of treating pain, addiction and/or stress using such compounds and/or pharmaceutical compositions.
    Type: Grant
    Filed: April 21, 2014
    Date of Patent: March 7, 2017
    Assignee: DEMERX, INC.
    Inventor: Deborah C. Mash
  • Patent number: 9427440
    Abstract: Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1, R2, R4, R5, R6 and R7 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: August 30, 2016
    Assignee: Janssen Sciences Ireland UC
    Inventors: Sandrine Marie Helene Vendeville, Pierre Jean-Marie Bernard Raboisson, Tse-I Lin, Abdellah Tahri, Katie Ingrid Eduard Amssoms
  • Patent number: 9409913
    Abstract: The present invention relates to novel polymorphic forms of alcaftadine, processes of preparing novel polymorphic forms of alcaftadine and pharmaceutical compositions thereof.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: August 9, 2016
    Assignee: ENALTEC LABS PRIVATE LIMITED
    Inventors: Sivakumar Bobba Venkata, Eswara Rao Kodali, Girish Bansilal Patel, Sanjay Dashrath Vaidya, Alok Pramod Tripathi
  • Patent number: 9364483
    Abstract: The present invention concerns a premix composition for feeding cattle, comprising: a) a premix carrier having an overall particle size comprised between 300 and 400 ?m, b) zilpaterol, and c) a surface agent. The present invention is also related to a method of increasing the rate of weight gain in cattle, comprising the administration to the cattle of feed additives consisting of a premix composition such as described, over a period of at least two weeks.
    Type: Grant
    Filed: June 20, 2014
    Date of Patent: June 14, 2016
    Assignee: LABORATORIOS VIRBAC
    Inventors: Jose Manuel Monroe Monroy, Luis Gerardo Estrella Parraga, Laurent Angeli
  • Patent number: 9359381
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: June 7, 2016
    Assignee: Novartis AG
    Inventors: Mahbub Ahmed, Alexander Ashall-Kelly, Louisa Gueritz, Jeffrey McKenna, Joseph McKenna, Simon Mutton, Rakesh Parmar, Jon Shepherd, Paul Wright
  • Patent number: 9260391
    Abstract: The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I.
    Type: Grant
    Filed: August 7, 2009
    Date of Patent: February 16, 2016
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Yuli Xie, Shixian Deng, Donald W. Landry, Paul Harris, Antonella Maffei
  • Patent number: 9255101
    Abstract: The present patent application concerns new ligands of the H4-receptor, their process of preparation and their therapeutic use.
    Type: Grant
    Filed: June 5, 2013
    Date of Patent: February 9, 2016
    Assignee: BIOPROJET
    Inventors: Isabelle Berrebi-Bertrand, Xavier Billot, Thierry Calmels, Marc Capet, Stéphane Krief, Olivier Labeeuw, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Philippe Robert, Jean-Charles Schwartz
  • Patent number: 9199985
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?1B—The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.
    Type: Grant
    Filed: February 17, 2012
    Date of Patent: December 1, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty
  • Patent number: 9187471
    Abstract: This disclosure is directed to tetracyclic pyrido[4,3-b]indole and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: November 17, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Patent number: 9051343
    Abstract: Disclosed herein are phosphate esters of noribogaine and dihydronoribogaine, and esters and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the methods of their use, including in the treatment of addiction and/or pain.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: June 9, 2015
    Assignee: DEMERX, INC.
    Inventors: Richard D. Gless, Jr., Robert M. Moriarty
  • Patent number: 9045481
    Abstract: This invention relates noribogaine derivatives, compositions and methods of use thereof.
    Type: Grant
    Filed: January 29, 2013
    Date of Patent: June 2, 2015
    Assignee: DEMERX, INC.
    Inventors: Deborah C. Mash, Richard D. Gless, Jr., Robert M. Moriarty
  • Publication number: 20150148336
    Abstract: The invention provides methods for selecting and administering antidepressant medications to a patient based upon the patient's combination genotype and phenotype for a panel of genes.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 28, 2015
    Inventors: David A. Mrazek, Dennis J. O'Kane, John L. Black
  • Patent number: 9040519
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: May 26, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Patent number: 9040520
    Abstract: Stable noribogaine salt ansolvates are useful for preparing pharmaceutical compositions and for alleviating nociceptive pain in a patient. Such ansolvates can be prepared by slurrying solvated forms, preferably MeOH solvated noribogaine hydrochloride in EtOH/water.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: May 26, 2015
    Assignee: DemeRx, Inc.
    Inventors: Richard D. Gless, Jr., William C. Schinzer
  • Publication number: 20150132258
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 14, 2015
    Inventor: George D. Hartman
  • Publication number: 20150099015
    Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.
    Type: Application
    Filed: November 24, 2014
    Publication date: April 9, 2015
    Inventor: Guochuan Emil TSAI
  • Patent number: 8993559
    Abstract: The present invention relates to a method of treating obesity in a subject by administering to the subject a compound having the formula: wherein n is from 0 to 8; R1 is CH2OH, CH(OH)R5, CH2OR5, CO2R5, C(O)NH2, C(O)NHR5, C(O)NR5R6, C(O)NHNH2, C(O)NHNHR5, C(O)NHNR5R6, C(O)NR5NH2, C(O)NR5NHR6, C(O)NR5NR6R7, C(O)NHNH(C(O)R5), C(O)NHNR5(C(O)R6), C(O)NR5NH(C(O)R6), C(O)NR5NR6(C(O)R7), CN, or C(O)R5; R2 is H, unsubstituted or substituted alkyl, YH, YR8, YR8R9, YR8YR9YR10, YC(O)R8, C(O)YR8, C(O)NH2, C(O)NHR8, C(O)NR8R9, NH2, NHR8, NR8R9, NHC(O)R8, or NR8C(O)R9; R3 and R4 are the same or different and are selected from the group consisting of H, halogens, unsubstituted or substituted alkyl, OH, OR10, NH2, NHR10, NR10R11, NHC(O)R10, or NR10C(O)R11; R5, R6, R7, R8, R9, R10, and R11 are the same or different and are selected from the group consisting of H, unsubstituted alkyl, substituted alkyl, unsubstituted aryl and substituted aryl; R12 is selected from the group consisting of H, unsubstituted alkyl, and substitu
    Type: Grant
    Filed: January 27, 2009
    Date of Patent: March 31, 2015
    Assignee: Albany Medical College
    Inventors: Stanley D. Glick, Isabelle M. Maisonneuve, Olga D. Taraschenko
  • Publication number: 20150087633
    Abstract: Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.
    Type: Application
    Filed: December 1, 2014
    Publication date: March 26, 2015
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald D. Payan, Sylvia Braselmann
  • Publication number: 20150080376
    Abstract: The present invention relates to novel polymorphic forms of alcaftadine, processes of preparing novel polymorphic forms of alcaftadine and pharmaceutical compositions thereof.
    Type: Application
    Filed: November 14, 2013
    Publication date: March 19, 2015
    Applicant: Enaltec Labs Pvt. Ltd.
    Inventors: Sivakumar Bobba Venkata, Eswara Rao Kodali, Girish Bansilal Patel, Sanjay Dashrath Vaidya, Alok Pramod Tripathi
  • Publication number: 20150072964
    Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of agitation, aggressive behaviors, posttraumatic stress disorder or impulse control disorders.
    Type: Application
    Filed: April 14, 2013
    Publication date: March 12, 2015
    Inventors: Sharon Mates, Robert Davis, Kimberly Vanover, Lawrence Wennogle
  • Publication number: 20150051192
    Abstract: A method of preventing drug use relapse by administering an effective amount of an ?3?4 nicotinic antagonist to a mammal after an initial period of drug use, and preventing a relapse of drug use. A method of preventing drug use relapse due to cue inducement by administering an effective amount of an ?3?4 nicotinic antagonist to a mammal after an initial period of drug use, and preventing a relapse of drug use during cue inducement. A method of preventing drug use relapse due to cue inducement by modulating the dopaminergic mesolimbic pathway by blocking ?3?4 nicotinic receptors in the habenulo-interpeduncular pathway and the basolateral amygdala of a mammal after an initial period of drug use, and preventing a relapse of drug use during cue inducement. A method of preventing drug use relapse by preventing a relapse of drug use during cue inducement.
    Type: Application
    Filed: March 25, 2013
    Publication date: February 19, 2015
    Inventors: Stanley D. Glick, James E. Polston