Spiro Ring System Containing Patents (Class 514/252.15)
  • Patent number: 11759462
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Grant
    Filed: March 15, 2021
    Date of Patent: September 19, 2023
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • Patent number: 11478476
    Abstract: The present invention is directed to a composition comprising a buspirone metabolite, alone or in combination with a second active ingredient, for use in the treatment of movement disorders.
    Type: Grant
    Filed: June 25, 2015
    Date of Patent: October 25, 2022
    Assignee: CONTERA PHARMA APS
    Inventors: John Bondo Hansen, Mikael S. Thomsen
  • Patent number: 11439627
    Abstract: The present invention relates to a pharmaceutical composition or a kit comprising, a first substance capable of raising intracellular cAMP levels, and a second substance capable of modulating intracellular calcium concentration. Likewise, the present invention relates to methods of treating patients suffering from autism spectrum disorder (ASD) phenotype 1 by administering an effective amount of a substance capable of raising intracellular cAMP levels and, optionally, an effective amount of a substance capable of modulating intracellular calcium concentration.
    Type: Grant
    Filed: December 18, 2020
    Date of Patent: September 13, 2022
    Assignee: Stalicla S.A.
    Inventor: Lynn Durham
  • Patent number: 10946018
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Grant
    Filed: April 16, 2020
    Date of Patent: March 16, 2021
    Assignee: Roivant Sciences GmbH
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • Patent number: 10806703
    Abstract: The present invention relates to a transmucosal administration system to administer quinones, benzoquinones, and especially 1,4-benzoquinones, via the oromucosal route.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: October 20, 2020
    Assignees: LTS Lohmann Therapie-System AG, Santhera Pharmaceuticals (Schweitz) AG
    Inventors: Markus Krumme, Keith Jensen, Judith Dubach-Powell, Rudolf Hausmann
  • Patent number: 10660893
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Grant
    Filed: May 30, 2019
    Date of Patent: May 26, 2020
    Assignee: ROIVANT SCIENCES, GmbH
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • Patent number: 10350208
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Grant
    Filed: May 14, 2018
    Date of Patent: July 16, 2019
    Assignee: Roivant Sciences GmbH
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • Patent number: 10045988
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: August 14, 2018
    Assignee: Roivant Sciences GmbH
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • Patent number: 9750740
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Grant
    Filed: September 28, 2016
    Date of Patent: September 5, 2017
    Assignee: Kanos Pharmaceuticals, Inc.
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren
  • Patent number: 9023834
    Abstract: This invention relates to a pharmaceutical kit containing a lyophilized preparation of a pyrimidine compound described in the specification. Also disclosed is a lyophilization process for making this preparation.
    Type: Grant
    Filed: November 12, 2009
    Date of Patent: May 5, 2015
    Assignee: TaiGen Biotechnology Co., Ltd.
    Inventors: Chi-Feng Yen, Judy Yuan, Chi-Hsin Richard King
  • Publication number: 20150104506
    Abstract: The present invention provides a pharmaceutical formulation for oral administration comprising an agonist of two or more of the 5-HT1B, 5-HT1D and 5-HT1F receptors, such as a triptan, e.g. zolmitriptan, in a matrix constituent with extended release characteristics, and further comprising a 5-HT1A-R agonist, such as buspirone, in a constituent with immediate-release characteristics. The special formulation is particularly well-suited for use in the treatment of movement disorders by combining the two active ingredients in a manner that achieves synergy from both the combination per se and the special release parameters of the pharmaceutical formulation, allowing for ease of administration and reducing the risk of adverse effects of each of the two active ingredients.
    Type: Application
    Filed: April 18, 2013
    Publication date: April 16, 2015
    Applicant: CONTERA PHARMA APS
    Inventors: John Bondo Hansen, Mikael S. Thomsen, Jens D. Mikkelsen, Peter Gudmund Nielsen, Mads Kreilgaard
  • Publication number: 20150099743
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Hui LI, Seiji NUKUI, Stephanie Anne SCALES, Min TENG, Chunfeng YIN
  • Publication number: 20150080393
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Application
    Filed: September 5, 2014
    Publication date: March 19, 2015
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • Publication number: 20140255517
    Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing posttraumatic stress disorder comprising administering a pharmaceutical composition comprising effective amount of an angiotensin-converting enzyme inhibitor to a subject in need thereof. In certain embodiments, the angiotensin-converting enzyme inhibitor is administered in combination with an angiotensin receptor blocker.
    Type: Application
    Filed: March 5, 2014
    Publication date: September 11, 2014
    Applicant: EMORY UNIVERSITY
    Inventors: Kerry J. Ressler, Paul J. Marvar
  • Publication number: 20140243350
    Abstract: The present invention relates to the combined use of compounds which are activators of the KCNQ family potassium ion channels and compounds which are serotonin 5-HT1 receptor agonists. The combined use of KCNQ channel activators and 5-HT1 receptor agonists is useful in the treatment of for example movement disorders. The present invention further relates to pharmaceutical compositions, methods of treatments and kits of parts.
    Type: Application
    Filed: July 5, 2012
    Publication date: August 28, 2014
    Applicant: CONTERA PHARMA APS
    Inventors: John Bondo Hansen, Mikael S. Thomsen
  • Publication number: 20140221385
    Abstract: The present invention relates to the use of 5-HT1 agonists in pharmaceutical compositions, compounds and methods for treatment of movement disorders related to neurological dysfunctions. The invention is particularly relevant for treatment of patients suffering from tardive dyskinesia, Parkinson's disease and associated disorders thereof. Kits of parts comprising the 5-HT1 agonist compounds or pharmaceutical compositions according to the present invention, as well as methods of preparation are also provided by the present invention.
    Type: Application
    Filed: June 1, 2012
    Publication date: August 7, 2014
    Applicant: CONCIT PHARMA APS
    Inventors: John Bondo Hansen, Mikael S. Thomsen, Jens D. Mikkelsen
  • Publication number: 20140024628
    Abstract: The present invention relates to a compound of formula (I), which has valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, processes for stereoselectively preparing these compounds, particularly pharmaceutical formulations suitable for inhalation and their use for the treatment of diseases, particularly tumoral diseases, benign prostatic hyperplasia and diseases of the lungs and airways.
    Type: Application
    Filed: July 17, 2013
    Publication date: January 23, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Markus OSTERMEIER, Peter SIEGER
  • Patent number: 8618097
    Abstract: The present invention provides compounds of Formula (I), including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: July 3, 2008
    Date of Patent: December 31, 2013
    Assignees: Array Biopharma, Inc., Genentech, Inc.
    Inventors: Josef Bencsik, James F. Blake, James M. Graham, Martin F. Hentemann, Nicholas C. Kallan, Ian S. Mitchell, Stephen T. Schlachter, Keith L. Spencer, Dengming Xiao, Rui Xu, Mike Welch, Jun Liang, Brian S. Safina
  • Patent number: 8557796
    Abstract: Substituted 1-oxa-2,8-diaza-spiro[4,5]dec-2-ene compounds and processes for their production, the use thereof for producing pharmaceutical compositions, pharmaceutical compositions containing these compounds and methods of treatment using these compounds.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: October 15, 2013
    Assignee: Gruenenthal GmbH
    Inventors: Heinrich Helmut Buschmann, Guenter Werner Englberger, Tieno Germann, Hagen-Henrich Hennies, Corinna Maul, Bernd Sundermann, Joerg Holenz
  • Publication number: 20130252965
    Abstract: The present invention relates to the use of 5-HT1 agonists in pharmaceutical compositions, compounds and methods for treatment of movement disorders related to neurological dysfunctions. The invention is particularly relevant for treatment of patients suffering from tardive dyskinesia, Parkinson's disease and associated disorders thereof. Kits of parts comprising the 5-HT1 agonist compounds or pharmaceutical compositions according to the present invention, as well as methods of preparation are also provided by the present invention.
    Type: Application
    Filed: October 13, 2011
    Publication date: September 26, 2013
    Applicant: CONCIT PHARMA APS
    Inventors: John Bondo Hansen, Mikael S. Thomsen
  • Patent number: 8445482
    Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: May 21, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
  • Patent number: 8440654
    Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: May 14, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
  • Publication number: 20130045962
    Abstract: The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives. Specifically, the invention is directed to compounds of formula (I): wherein R1, R2 and R3 are defined below and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.
    Type: Application
    Filed: November 6, 2008
    Publication date: February 21, 2013
    Inventors: Donghui Qin, Beth Norton, Xiangmin Liao, Andrew Nicholson Knox, Jinhwa Lee, Yuhong Fang, Jason Christopher Dreabit, Siegfried Benjamin Christensen, IV, Andrew B. Benowitz, Kelly M. Aubart
  • Publication number: 20130005655
    Abstract: A composition comprising doxepin, or a pharmaceutically acceptable salt, or prodrug thereof, and a compound that enhances sleep onset, sleep maintenance or reduces early morning awakenings. These compositions are useful for treating multiple manifestations of insomnia.
    Type: Application
    Filed: September 12, 2012
    Publication date: January 3, 2013
    Applicant: Somaxon Pharmaceuticals, Inc.
    Inventors: Philip Jochelson, Robert Mansbach, Michael Skinner, Neil B. Kavey
  • Publication number: 20120270838
    Abstract: The present invention relates to a compound represented by the following formula (1): wherein W, X, Y, R1, R2, R33, R34, m and n are as defined in the claims, or a pharmacologically acceptable salt thereof.
    Type: Application
    Filed: April 27, 2010
    Publication date: October 25, 2012
    Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHA
    Inventors: Toru Esaki, Yoshikazu Nishimura, Yoshiaki Isshiki, Naoki Okamoto, Yoshiyuki Furuta, Akemi Mizutani, Masateru Ohta, Wayne Wen Lai, Tomoya Kotake
  • Publication number: 20120165331
    Abstract: The invention relates to compounds of the formula I A-D-C(R1)2—B??(I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: December 19, 2011
    Publication date: June 28, 2012
    Inventors: Sangamesh BADIGER, Dirk BEHNKE, Claudia BETSCHART, Vinod CHAUDHARI, Simona COTESTA, Samuel HINTERMANN, Andreas LERCHNER, Fatma LIMAM, Silvio OFNER, Chetan PANDIT, Jürgen WAGNER
  • Patent number: 8193178
    Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.
    Type: Grant
    Filed: September 12, 2008
    Date of Patent: June 5, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
  • Publication number: 20120114670
    Abstract: Disclosed are compositions and methods related to new targets for cancer treatment.
    Type: Application
    Filed: January 23, 2011
    Publication date: May 10, 2012
    Applicant: UNIVERSITY OF ROCHESTER
    Inventors: Hartmut Land, Helene R. McMurray, Erik R. Sampson
  • Publication number: 20120108570
    Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.
    Type: Application
    Filed: January 6, 2012
    Publication date: May 3, 2012
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Miodrag Radulovacki, David W. Carley
  • Publication number: 20120108510
    Abstract: This disclosure provides methods of using compounds that act to increase oxytocin release, including certain melanocortin receptor agonists, for treating or reducing the severity of psychotherapeutic or social disorders such as autism, and in particular the use of these compounds as an adjunct to psychotherapeutic counseling or behavioral therapy.
    Type: Application
    Filed: May 19, 2011
    Publication date: May 3, 2012
    Applicant: EMORY UNIVERSITY
    Inventors: Larry James Young, Meera E. Modi
  • Publication number: 20120077818
    Abstract: Provided herein are methods of and compositions for, treating, preventing and managing various neurological disorders. The methods comprise administering a transnorsertraline in combination with a serotonin receptor IA agonist, antagonist or modulator.
    Type: Application
    Filed: May 12, 2010
    Publication date: March 29, 2012
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Una Campbell, Judith Dunn
  • Publication number: 20110319386
    Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on muscarinic receptor modulation, such as via inhibition of acetylcholine esterase (AChE) activity, alone or in combination with another neurogenic agent to stimulate or activate the formation of new nerve cells.
    Type: Application
    Filed: June 10, 2011
    Publication date: December 29, 2011
    Applicant: BrainCells Inc.
    Inventors: Carrolee Barlow, Todd A. Carter, Kai Treuner, Michael Lee
  • Publication number: 20110301175
    Abstract: The invention provides compounds of formula (1) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFR?, PDGFR?, CSF1R, AbI, BCR-AbI, CSK, JNK1, JNK2, p38, p70S6K, TGF?, SRC, EGFR, trkB, FGFR3. Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2?, BRK, Fms, KDR, c-rapor b-raf kinases.
    Type: Application
    Filed: August 19, 2008
    Publication date: December 8, 2011
    Inventors: Valentina Molteni, Xiaolin Li, Xiaodong Liu, Donatella Chianelli, Juliet Nabakka, Jon Loren, Shuli You
  • Publication number: 20110281860
    Abstract: The present invention relates to the use of quinazoline derivatives, which show EGFR inhibitory activity, for the prevention and/or treatment of virus-induced diseases, preferably virus induced respiratory diseases and exacerbation in chronic airway diseases such as COPD or asthma.
    Type: Application
    Filed: August 13, 2009
    Publication date: November 17, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Birgit Jung
  • Patent number: 8039472
    Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: October 18, 2011
    Assignee: Novartis AG
    Inventors: Gurdip Bhalay, Emma Budd, Graham Charles Bloomfield, Stephen Paul Collingwood, Andrew Dunstan, Lee Edwards, Peter Gedeck, Catherine Howsham, Peter Hunt, Thomas Anthony Hunt, Paul Oakley, Nichola Smith
  • Publication number: 20110224172
    Abstract: Substituted 1-oxa-2,8-diaza-spiro[4,5]dec-2-ene compounds and processes for their production, the use thereof for producing pharmaceutical compositions, pharmaceutical compositions containing these compounds and methods of treatment using these compounds.
    Type: Application
    Filed: May 26, 2011
    Publication date: September 15, 2011
    Applicant: GRUENENTHAL GmbH
    Inventors: Heinrich Helmut BUSCHMANN, Guenter Werner Englberger, Tieno Germann, Hagen-Heinrich Hennies, Corinna Maul, Bernd Sundermann, Joerg Holenz
  • Publication number: 20110112112
    Abstract: The disclosure provides compounds and methods of using Apogossypolone derivatives for treating diseases and disorders. In particular, the disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and provides methods for the preparation of compounds of Formula I; and methods for treating cancer, autoimmune diseases, and inflammation by administering a compound of Formula I.
    Type: Application
    Filed: October 7, 2010
    Publication date: May 12, 2011
    Applicant: Sanford-Burnham Medical Research Institute
    Inventors: Maurizio Pellecchia, Jun Wei
  • Publication number: 20110097305
    Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-me-dialed disorders, such as cancer. The subject compounds arc gem-disubstituted or spimcyclic pyridine, pyrimidine and triazine derivatives.
    Type: Application
    Filed: April 6, 2009
    Publication date: April 28, 2011
    Applicant: AMGEN INC.
    Inventors: Richard V. Connors, Kang Dai, John Eksterowicz, Pingchen Fan, Benjamin Fisher, Jiasheng Fu, Kexue Li, Zhihong Li, Lawrence R. Mcgee, Rajiv Sharma, Xiaodong Wang
  • Publication number: 20110086851
    Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.
    Type: Application
    Filed: May 13, 2009
    Publication date: April 14, 2011
    Inventors: Bernard Golding, Richard Franklin
  • Publication number: 20110059905
    Abstract: Methods for treatment of disease-induced ataxia and non-ataxic imbalance are disclosed. The methods involve treating a patient with a compound having nicotinic acetylcholine receptor activity.
    Type: Application
    Filed: March 31, 2009
    Publication date: March 10, 2011
    Inventors: Theresa A. Zesiewicz, Kelly L. Sullivan
  • Publication number: 20110046148
    Abstract: The present invention relates to spirocyclic heterocycles of general formula (I) the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways, and the preparation thereof.
    Type: Application
    Filed: February 5, 2009
    Publication date: February 24, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank Himmelsbach, Birgit Jung, Ralf Lotz
  • Publication number: 20110014304
    Abstract: The disclosure relates to pharmacotherapy of a psychiatric disorder which is schizophrenia and/or anxiety, wherein schizophrenia includes schizophrenia related disorders such as brief psychotic disorders, delusional disorders, schizoaffective disorders, and schizophreniform disorders, and anxiety includes panic disorders, obsessive-compulsive disorders (OCD), post-traumatic stress disorders (PTSD), social phobia or social anxiety disorders, specific phobia, and generalized anxiety disorders (GAD). The compounds of the disclosure are useful for the treatment of the above psychiatric disorders alone or in combination with other therapeutical agents effective in the treatment of schizophrenia and/or anxiety disorders.
    Type: Application
    Filed: June 15, 2010
    Publication date: January 20, 2011
    Applicant: Newron Pharmaceuticals S.p.A.
    Inventors: Emanuela Izzo, Laura Faravelli, Elena Barbanti, Patricia Salvati
  • Publication number: 20100298305
    Abstract: Disclosed herein are methods of treating a psychiatric disorder, such as a sleep disorder, an anxiety disorder, a mood disorder or a perceptual disturbance. In one example, a method of treating a sleep disorder or anxiety disorder includes selecting a subject with a sleep disturbance or anxiety disorder in the absence of an underlying physical disorder and administering a therapeutically effective amount of tizanidine, thereby reducing or inhibiting a symptom of the sleep disorder or anxiety disorder. In another example, a method of treating a mood disorder or a perceptual disturbance is disclosed. This method includes selecting a subject with a mood disorder or perceptual disturbance and administering a therapeutically effective amount of tizanidine, thereby reducing or inhibiting a symptom of the mood disorder or perceptual disturbance.
    Type: Application
    Filed: November 25, 2009
    Publication date: November 25, 2010
    Inventor: Bruce Capehart
  • Publication number: 20100292216
    Abstract: This invention relates to methods and compositions for treating psychiatric conditions, such as depression.
    Type: Application
    Filed: November 16, 2009
    Publication date: November 18, 2010
    Applicant: ADAMAS PHARMACEUTICALS, INC.
    Inventors: Laurence R. Meyerson, Gregory T. Went, Timothy J. Fultz
  • Publication number: 20100239525
    Abstract: The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: December 30, 2009
    Publication date: September 23, 2010
    Applicant: ArQule, Inc.
    Inventors: Syed M. Ali, Mark A. Ashwell, Sudharshan Eathiraj, Eugene Kelleher, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Rocio Palma, Manish Tandon, David Vensel, Neil Westlund, Hui Wu, Rui-Yang Yang
  • Publication number: 20100216734
    Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use nootropic agents, optionally in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells.
    Type: Application
    Filed: November 19, 2009
    Publication date: August 26, 2010
    Applicant: BrainCells, Inc.
    Inventors: Carrolee Barlow, Todd A. Carter, Andrew Morse, Kai Treuner, Kym I. Lorrain, Dana Gitnick, Jammieson C. Pires
  • Publication number: 20100196286
    Abstract: Methods, devices and kits for treating sleep disorders, anxiety disorders, and developmental disorders, and/or for inducing an arousable state of sedation in a subject, are described. For example, inhalation methods, devices and kits for treating insomnia, anxiety and/or ADHD using one or more ?2-adrenergic agonists such as dexmedetomidine or clonidine are described.
    Type: Application
    Filed: December 1, 2009
    Publication date: August 5, 2010
    Inventors: Thomas A. ARMER, Robert O. Cook, Terry Alfredson, Anthony Sun
  • Publication number: 20100168121
    Abstract: Compositions and methods for treating disorders of the outer retina with compounds with 5-HT1A agonist activity are disclosed.
    Type: Application
    Filed: March 8, 2010
    Publication date: July 1, 2010
    Applicant: ALCON, INC.
    Inventors: Robert J. Collier, JR., Michael A. Kapin, Mark R. Hellberg, Thomas R. Dean
  • Publication number: 20100166674
    Abstract: A pharmaceutical composition for transdermal delivery comprising one or more physiologically active agents; one or more dermal penetration enhancers; and a volatile pharmaceutically acceptable carrier comprising a volatile solvent; and wherein the physiologically active agent and dermal penetration enhancer form an amorphous deposit upon evaporation of the volatile carrier, said amorphous deposit forming a reservoir within the stratum corneum; and (A) wherein the composition has a release rate profile of physiologically active agent so as to provide a ratio of the maximum concentration (Cmax) to the average concentration (Cavg) for the physiologically active agent over the dosage interval within the range of 1 to 10.
    Type: Application
    Filed: December 18, 2009
    Publication date: July 1, 2010
    Inventors: Timothy Matthias Morgan, Nina Frances Wilkins, Kathryn Taci-Jane Klose, Barrie Charles Finnin, Barry Leonard Reed
  • Publication number: 20100166889
    Abstract: The invention provides methods of treating depressive disorders, in particular major depression but other depressive orders also, with prodrug stimulants or analogs including amphetamine prodrugs, methylphenidate prodrugs, and methylphenidate analogs, Such methods of treatment may utilize the prodrug stimulant or analog as monotherapy or, more commonly, as an adjunct to antidepressant medication treatment to augment their effect. The invention includes combination methods of treatment in which an amphetamine prodrug, methylphenidate prodrug, or methylphenidate analog is administered to an individual in need with one or more other active agents, either in separate forms or as a single pharmaceutical formulation. Packaged pharmaceutical compositions containing an amphetamine or methylphenidate prodrug, instructions for using the prodrug to treat certain disorders, and optionally one or more other active agents are provided by the invention.
    Type: Application
    Filed: December 23, 2009
    Publication date: July 1, 2010
    Applicant: LCS GROUP, LLC
    Inventor: Louis Sanfilippo