Chalcogen And A Carbocyclic Ring Bonded Directly At 4-position Patents (Class 546/217)
  • Patent number: 10023535
    Abstract: The present invention refers to a process for the preparation of 1-(2-halogen-ethyl)-4-piperidinecarboxylic acid ethyl esters, in particular of 1-(2-chloroethyl)-4 piperidinecarboxylic acid ethyl ester, a versatile synthesis intermediate, particularly useful as an intermediate compound in the synthesis of umeclidinium.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: July 17, 2018
    Assignee: OLON S.P.A.
    Inventors: Giorgio Bertolini, Corrado Colli, Aldo Bianchi, Federica Colombo, Stefano Maiorana, Filippo Nisic
  • Publication number: 20140329746
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
    Type: Application
    Filed: July 16, 2014
    Publication date: November 6, 2014
    Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
  • Publication number: 20140235631
    Abstract: The present invention relates to efflux inhibitor compositions and methods of using these agents for treating conditions where the activity of efflux transporter proteins (e.g., Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP)) inhibit effective delivery of a therapeutic agent to a target tissue (e.g., brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, and/or stem cells).
    Type: Application
    Filed: July 26, 2013
    Publication date: August 21, 2014
    Inventors: Antonius Martinus Gustave Bunt, Olaf van Tellingen
  • Publication number: 20140179665
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Application
    Filed: December 9, 2013
    Publication date: June 26, 2014
    Inventors: George D. Hartman, Osvaldo A. Flores
  • Patent number: 8633226
    Abstract: The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: January 21, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventor: Joseph B. Santella
  • Patent number: 8623867
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: January 7, 2014
    Assignees: Merck Sharp & Dohme Corp., Pharmacopeia Drug Discovery, Inc.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey H. Lowrie, Kurt W. Saionz, Suresh D. Babu
  • Patent number: 8609849
    Abstract: Pharmaceutical compositions of the invention include hydroxylated sulfamide derivatives having a disease-modifying action in the treatment of diseases associated with excitotoxicity and accompanying oxidative stress that include epilepsy, Alzheimer's disease, and any neurodegenerative disease involving glutamate toxicity.
    Type: Grant
    Filed: November 29, 2011
    Date of Patent: December 17, 2013
    Assignees: Fox Chase Chemical Diversity Center, Inc., Advanced Neural Dynamics, Inc.
    Inventors: Garry Robert Smith, Douglas E. Brenneman, Allen B. Reitz, Yan Zhang, Yanming Du
  • Publication number: 20130310399
    Abstract: An insecticidal acaricidal and nematicidal composition of formula I Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; the ring is a 6 membered aromatic ring or is a 5 or 6 membered heteroaromatic ring; Z and provided that both are not N; R1, R2, R3, R3a, R4, R8 and Ra are specified organic groups and n and p are independently 0, 1, 2, 3 or 4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.
    Type: Application
    Filed: July 24, 2013
    Publication date: November 21, 2013
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Peter Maienfisch, Louis-Pierre Molleyres, Jerome Cassayre, Fredik Cederbaum, Camilla Corsi, Thomas Pitterna
  • Patent number: 8580965
    Abstract: Substituted sulfonamide compounds with bradykinin receptor (B1R) modulating activity; processes for the preparation thereof, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or inhibit pain and/or other disorders and/or disease states.
    Type: Grant
    Filed: October 16, 2007
    Date of Patent: November 12, 2013
    Assignee: Gruenenthal GmbH
    Inventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
  • Patent number: 8536198
    Abstract: The present application describes modulators of MIP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.
    Type: Grant
    Filed: July 23, 2008
    Date of Patent: September 17, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joseph B. Santella, John Hynes, Daniel S. Gardner
  • Patent number: 8501782
    Abstract: The present application describes modulators of MIP-1? of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.
    Type: Grant
    Filed: July 23, 2008
    Date of Patent: August 6, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Daniel S. Gardner, John V. Duncia, John Hynes, T.G. Murali Dhar, Percy H. Carter, Joseph B. Santella
  • Publication number: 20130178444
    Abstract: The present application describes prodrugs of the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed.
    Type: Application
    Filed: March 5, 2013
    Publication date: July 11, 2013
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8410139
    Abstract: The present application describes prodrugs of the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed.
    Type: Grant
    Filed: October 4, 2010
    Date of Patent: April 2, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: John Hynes, Percy H. Carter, Lyndon A. M. Cornelius, T.G. Murali Dhar, John V. Duncia, Satheesh Nair, Joseph B. Santella, Jayakumar S. Warrier, Hong Wu
  • Patent number: 8362255
    Abstract: A process for the manufacture of (un)substituted phenylsulfanylphenyl-piperidines comprising the use of benzyl as N-piperidine protecting group is disclosed.
    Type: Grant
    Filed: March 2, 2009
    Date of Patent: January 29, 2013
    Assignee: H. Lundbeck A/S
    Inventors: Michael Rock, Sebastian Brandes
  • Publication number: 20130023564
    Abstract: The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed.
    Type: Application
    Filed: September 27, 2012
    Publication date: January 24, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8299098
    Abstract: The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: October 30, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventor: Joseph B. Santella
  • Publication number: 20120270885
    Abstract: The use of a compound of formula I Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; the ring is a 6 membered aromatic ring or is a 5 or 6 membered heteroaromatic ring; Z and Z? are provided that both are not N; R1, R2, R3, R3a, R4, R8 and Ra are specified organic groups and n and p are independently 0, 1, 2, 3 or 4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.
    Type: Application
    Filed: February 10, 2012
    Publication date: October 25, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Peter Maienfisch, Louis-Pierre Molleyres, Jérôme Cassayre, Fredrik Cederbaum, Camilla Corsi, Thomas Pitterna
  • Publication number: 20120149733
    Abstract: The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed.
    Type: Application
    Filed: June 15, 2011
    Publication date: June 14, 2012
    Inventors: Robert J. Cherney, John V. Duncia, Daniel S. Gardner, Joseph B. Santella, Zhongyu Wang
  • Patent number: 8012955
    Abstract: The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R1, R2, R3, R4, T, n, w and x are as described herein. In certain embodiments of the invention, a compound of the present invention activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: September 6, 2011
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Jiaxin Yu, Hui Hong, Sambaiah Thota, Xiang Xu, Ihab S. Darwish
  • Patent number: 7989630
    Abstract: P-glycoprotein transporter (P-gp) acts as a pump at the blood-brain barrier to exclude a wide range of xenobiotics (e.g., toxins, drugs, etc.) from the brain and is also expressed in a tumor in response to exposure to established or prospective chemotherapeutics (a phenomenon known as multidrug resistance). This invention concerns the preparation and use of radiotracers for imaging P-gp function in vitro and in vivo. Radiotracers of the present invention are avid substrates for P-gp and have structures based on N-Desmethyl-loperamide.
    Type: Grant
    Filed: April 30, 2008
    Date of Patent: August 2, 2011
    Assignee: National Institutes of Health Represented by the Secretary of the Department of Health and Human Services, National Institutes of Health
    Inventors: Victor W. Pike, Robert B. Innis, Sami S. Zoghbi, Neva Lazarova
  • Publication number: 20110178068
    Abstract: The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X?. In one embodiment, the present invention provides a prodrug compound of Formula I: where R1-R5 are defined in the written description of the invention.
    Type: Application
    Filed: December 23, 2010
    Publication date: July 21, 2011
    Applicant: Alkermes, Inc.
    Inventors: Orn Almarsson, Laura Cook Blumberg, Julius F. Remenar
  • Publication number: 20110054178
    Abstract: A process for the manufacture of (un)substituted phenylsulfanylphenyl-piperidines comprising the use of benzyl as N-piperidine protecting group is disclosed.
    Type: Application
    Filed: March 2, 2009
    Publication date: March 3, 2011
    Applicant: H. LUNDBECK A/S
    Inventors: Michael Rock, Sebastian Brandes
  • Publication number: 20100267704
    Abstract: This invention pertains to a class of autophagy inducing compounds that treat diseases caused by misfolded protein aggregates and a screening method for identifying these compounds.
    Type: Application
    Filed: October 10, 2008
    Publication date: October 21, 2010
    Applicants: President an Fellows of Harvard Colege, Shangha Institute of Organic Chemistry Chineesse Academy of Sciences
    Inventors: Junying Yuan, Dawei Ma, Lihong Zhang
  • Patent number: 7812035
    Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
    Type: Grant
    Filed: December 11, 2002
    Date of Patent: October 12, 2010
    Assignee: Sepracor Inc.
    Inventors: Heike Radeke, Liming Shao
  • Patent number: 7812159
    Abstract: The present invention relates to processes for preparing aromatic ether compounds that are modulators of glucose metabolism and therefore useful in the treatment of metabolic disorders such as diabetes and obesity.
    Type: Grant
    Filed: January 9, 2006
    Date of Patent: October 12, 2010
    Assignee: Arena Pharamaceuticals, Inc.
    Inventors: Tawfik Gharbaoui, John R. Fritch, Ashwin M. Krishnan, Beverly Wolgast Throop, Naomi S. Kato
  • Publication number: 20100256163
    Abstract: The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho,meta-disubstituted phenyl)-1-alkypiperidines and piperazines. wherein R1, R2, R3 and X are as defined.
    Type: Application
    Filed: June 14, 2010
    Publication date: October 7, 2010
    Inventors: Clas Sonesson, Lars Swanson, Nicholas Ross Waters
  • Publication number: 20100191475
    Abstract: Materials, methods and a computer system are provided which facilitate the identification and characterization of modulators of potassium ion channels, particularly the HERG channel.
    Type: Application
    Filed: March 4, 2010
    Publication date: July 29, 2010
    Inventors: Scott Perschke, Ming Liu
  • Publication number: 20100168080
    Abstract: The present invention relates to novel morpholine, oxazapane and piperidine derivatives that act as ligands for CC chemokine receptors, such as CCR1. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
    Type: Application
    Filed: December 16, 2009
    Publication date: July 1, 2010
    Inventors: Uttam KHAMRAI, Sumit Kumar Karak, Matthew Ronsheim, Ashis Kumar Saha
  • Publication number: 20100144657
    Abstract: The present invention relates to new phenylpiperidine modulators of opioid ?-receptors, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: December 8, 2009
    Publication date: June 10, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Publication number: 20100105736
    Abstract: A compound having the general formula wherein A is selected from the group consisting of to the formation of a compound of the general formula (1) and a compound of the general formula (2) respectively, and pharmaceutically acceptable salts thereof, wherein R1 is a member selected from the group consisting of CF3, OSO2CF3, OSO2CH3, SOR4, SO2R4, COR4, CN, OR4, NO2, CONHR4, 3-thiophene, 2-thiophene, 3-furane, 2-furane, F, Cl, Br and I, wherein R4 is as defined below; R2 is a member selected from the group consisting of H, F, Cl, Br, I, CN, CF3, CH3, OCH3, OH, NH2, SOmCF3, O(CH2)mCF3, SO2N(R4)2, CH?NOR4, COCOOR4, COCOON(R4)2, (C1-C8)alkyl, (C3-C8)cykloalkyl, CH2OR4, CH2(R4)2, NR4SO2CF3, NO2, at phenyl at positions 2, 4, 5 or 6, wherein x and R4 are as defined below; R3 is a member selected from the group consisting of hydrogen, CF3, CH2CF3, (C1-C8)alkyl, (C3-C8)cykloalkyl, (C4-C9)cycloalkylmethyl, (C2-C8)alkenyl, (C2-C8)alkynyl, 3,3,3-tri-fluoropropyl, 4,4,4-trifluorobutyl, CH2SCH3, CH2CH2OCH3,
    Type: Application
    Filed: April 14, 2008
    Publication date: April 29, 2010
    Applicant: NSAB, Filial af NeuroSearch Sweden Ab, Sverige
    Inventor: Håkan V. Wikström
  • Patent number: 7700587
    Abstract: Haloperidol analogs that conforms to the structural formulae: wherein: R is H, or —(CH2)n—OH, n is an integer from 0 to 2, and A is a heterocyclic bridging group, consisting essentially of carbon and at least one nitrogen atom, which effectively maintains the distance between the moieties connected thereby such that the compound (1) is incapable of metabolizing to BCPP+ like species, (2) has an affinity for the D2 receptor subtype of 15<D2<250 and (3) functions as a dopamine receptor antagonist, or the structural formulae: wherein: R1 is H, or —(CH2)n—OH, n is an integer from 0 to 2, B is an aza- or diaza-bicyclo group, which effectively maintains the distance between the moieties connected thereby such that the compound is incapable of metabolizing to BCPP+ like species; and Z is —CH— or N; and pharmaceutically acceptable salts, esters, derivatives, metal complexes, conjugates and prodrugs thereof.
    Type: Grant
    Filed: September 7, 2004
    Date of Patent: April 20, 2010
    Assignee: Florida A&M University
    Inventors: Seth Y. Ablordeppey, Donald M. N. Sikazwe
  • Patent number: 7645754
    Abstract: The subject invention provides compounds having the structure: wherein, R1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(?O)NRaRb, —NRaRb, —NRaC(?O)NRaRb, —NRaC(?O)ORa, —OC(?O)NRaRb, or —NHC(?O) Ra; R2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(?O)NRaRb, —NRaRb, —NRaC(?O)NRaRb, —NRaC(?O)ORa, —OC(?O)NRaRb, or —NHC(?O)Ra, or R1, R2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH2)2OH or —CH2C(?O)OH; R3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C1-C15)alkyl, (C1-C15)alkoxy, or —NRaRb; R4 is hydrogen or substituted or unsubstituted (C1-C15)alkyl; R5 is —(CH2)mOR6, —CHNOR7, —C(?O)NR8R9, —(CH2)mC(?O)OR10, —(CH2)kC(?O)NR11R12; wherein R6 is a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl
    Type: Grant
    Filed: June 19, 2007
    Date of Patent: January 12, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Arlindo Castelhano, Bryan McKibben, Arno Steinig
  • Publication number: 20100004289
    Abstract: The present invention relates to a central nervous system-acting substituted butyrophenones. These compounds are useful in antipsychotic medications for psychosis, including schizophrenia, but especially for L-DOPA-induced psychosis, while having low or no risk of eliciting extrapyramidal side effects, hyperprolactinemia or tardive dyskinesia.
    Type: Application
    Filed: May 1, 2006
    Publication date: January 7, 2010
    Applicant: CLERA INC.
    Inventor: Philip Seeman
  • Publication number: 20090326010
    Abstract: The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed.
    Type: Application
    Filed: June 24, 2009
    Publication date: December 31, 2009
    Inventor: Joseph B. Santella
  • Publication number: 20090274624
    Abstract: P-glycoprotein transporter (P-gp) acts as a pump at the blood-brain barrier to exclude a wide range of xenobiotics (e.g., toxins, drugs, etc.) from the brain and is also expressed in a tumor in response to exposure to established or prospective chemotherapeutics (a phenomenon known as multidrug resistance). This invention concerns the preparation and use of radiotracers for imaging P-gp function in vitro and in vivo. Radiotracers of the present invention are avid substrates for P-gp and have structures based on N-Desmethyl-loperamide.
    Type: Application
    Filed: April 30, 2008
    Publication date: November 5, 2009
    Inventors: Victor W. Pike, Robert B. Innis, Sami S. Zoghbi, Neva Lazarova
  • Patent number: 7579474
    Abstract: The present invention relates to compounds having therapeutic effects against disorders in the central nervous system, and in particular substituted hydroxypiperidines of the formula 1: wherein R1, R2, and R3 are as defined herein.
    Type: Grant
    Filed: December 7, 2006
    Date of Patent: August 25, 2009
    Assignee: NSAB, Filial AF Neurosearch AB, Sverige
    Inventors: Clas Sonesson, Lars Swanson, Nicholas Waters
  • Patent number: 7560459
    Abstract: The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy. The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.
    Type: Grant
    Filed: November 2, 2005
    Date of Patent: July 14, 2009
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Ahmed Abdel-Magid, Cynthia Maryanoff, Steven Mehrman, Allen B. Reitz, Bruce Maryanoff
  • Publication number: 20090017489
    Abstract: The present invention relates to a composition for modulating the activation of Nurr1, the composition comprising an agonist or an antagonist of a dopamine D2 receptor, methods for modulating the activation of Nurr1 by the dopamine D2 receptor, a method and composition for treating Nurr1-related diseases using the dopamine D2 receptor, and methods for screening a modulator of a dopamine D2 receptor of a test compound. Accordingly, the activation of Nurr1 can be modulated by treating the dopaminergic neurons with the agonist or the antagonist of the dopamine D2 receptor, thereby enhancing or inhibiting generation of the dopaminergic neurons.
    Type: Application
    Filed: June 22, 2006
    Publication date: January 15, 2009
    Applicant: Korea University Industry And Academy Cooperation Foundation
    Inventors: Ja hyun Baik, Sung yul Kim
  • Patent number: 7473692
    Abstract: The present invention relates to new D3 dopamine receptor subtype selectice ligands of formula (I) to pharmacological compositions containing the same and to their use in therapy and/or prevention of psychoses (e.g. schizophrenia, schizo-affective disorders, etc), drug (e.g. alcohol, cocaine and nicotine, opioids etc.) abuse, cognitive impairment accompanying schizophrenia, mild-to-moderate cognitive deficits, amnesia, eating disorders (e.g. bulimia nervosa, etc.), attention deficit disorders, hyperactivity disorders in children, psychotic depression, mania, paranoid and delusional disorders, dyskinetic disorders (e.g. Parkinson's diseases, neuroleptic induced Parkinson's dissases, tardive dyskinesias) anxiety, sexual dysfunction, sleep disorders, emesis, aggression, autism, pain ophthalmological diseases (e.g. glaucoma etc.).
    Type: Grant
    Filed: September 25, 2002
    Date of Patent: January 6, 2009
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: János Galambos, Katalin Nógrádi, Éva Ágainé Csongor, György Miklós Keserü, István Vágó, György Domány, Béla Kiss, István Gyertyán, István Laszlovszky, Judit Laszy
  • Publication number: 20080139564
    Abstract: Certain substituted phenyl propyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.
    Type: Application
    Filed: November 14, 2007
    Publication date: June 12, 2008
    Inventors: John M. Keith, Jennifer M.B. Miller, Emily M. Stocking
  • Publication number: 20080113922
    Abstract: Compounds and pharmaceutical compositions comprising them are disclosed that may be useful for the treatment of diseases and disorders such as diabetes and obesity.
    Type: Application
    Filed: September 27, 2007
    Publication date: May 15, 2008
    Inventors: Bryce Alden Harrison, Spencer David Kimball, Ross Mabon, David Brent Rawlins
  • Patent number: 7338965
    Abstract: The invention relates to substituted piperidine, piperazine, morpholine and thiomorpholine compounds useful in the treatment of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers. One embodiment of the invention relates to compounds having the structure: where Z is CR or N, and R1, R2 and R3 are as described in the specification.
    Type: Grant
    Filed: November 19, 2002
    Date of Patent: March 4, 2008
    Assignees: Pharmacia & Upjohn Company, Elan Pharmaceuticals, Inc.
    Inventors: Joseph B. Moon, Shon R. Pulley, Daniel H. Rich, David L. Brown, Barbara Jagodzinska, Varghese John, John Jacobs
  • Patent number: 7129228
    Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.
    Type: Grant
    Filed: January 7, 2004
    Date of Patent: October 31, 2006
    Assignee: Sepracor Inc.
    Inventors: Gregory D. Cuny, Liming Shao, James R. Hauske, Michele L. R. Heffernan, Brian M. Aquila, Xinhe Wu, Fengjiang Wang, Thomas D. Bannister
  • Patent number: 7060713
    Abstract: The present invention provides compounds having formula (II): wherein X, n, R1–R12 are defined herein, or a pharmaceutically acceptable salt thereof. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound represented by formula (II) and a pharmaceutically acceptable carrier or excipient. The invention further provides a method for treating cancer comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound represented by formula (II).
    Type: Grant
    Filed: March 18, 2005
    Date of Patent: June 13, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kyungjin Kim, Emily Aijun Liu, Steven Gregory Mischke
  • Patent number: 6987111
    Abstract: The invention relates to the discovery that pamoate salts of haloperidol and aripiprazole result in a good to superior long acting and/or extended release profile. Thus, in one aspect of the invention, the invention includes pamoate salts of haloperidol or aripiprazole. Preferably, the pamoate salt is characterized by a ratio of haloperidol to pamoate of 1:1 or 2:1. The pamoate salt can be crystalline, such as a needle or a dense crystal, such as described in the Figures. The invention further relates to methods of treating an individual in need thereof comprising administering a pharmaceutical composition comprising a pamoate salt of haloperidol and aripiprazole.
    Type: Grant
    Filed: August 6, 2003
    Date of Patent: January 17, 2006
    Assignee: Alkermes Controlled Therapeutics, II
    Inventors: Kristyn Greco, James Wright
  • Patent number: 6958352
    Abstract: Compounds, compositions and methods for altering insulin secretion, particularly in the context of treatment of subjects having, or suspected of being at risk for having, diabetes mellitus. The compounds have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein W1, W2, X, R1, R2, R3, R4, m and n are defined herein.
    Type: Grant
    Filed: February 10, 2003
    Date of Patent: October 25, 2005
    Assignee: SmithKline Beecham Corporation
    Inventors: Yazhong Pei, Soumitra S. Ghosh, Ian William James
  • Patent number: 6953801
    Abstract: Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
    Type: Grant
    Filed: May 21, 2002
    Date of Patent: October 11, 2005
    Assignee: Neurogen Corporation
    Inventors: Alan Hutchison, Linda M. Gustavson, John M. Peterson, Dario Doller, Timothy M. Caldwell, Taeyoung Yoon, Wallace C. Pringle, Yiping Shen, Cheryl Steenstra
  • Patent number: 6946478
    Abstract: The invention provides compounds of general formula wherein R1, m, Q, T, n, R2, R3, V, W, X and R4 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: January 9, 2003
    Date of Patent: September 20, 2005
    Assignee: AstraZeneca AB
    Inventors: Andrew Baxter, Stephen Brough, Nicholas Kindon, Thomas McInally, Bryan Roberts, Stephen Thom
  • Patent number: 6916833
    Abstract: The present invention provides compounds having formula (I): and formula (II): wherein X, n, and R1-R12 are defined herein, or a pharmaceutically acceptable salt thereof. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound represented by formula (I) or (II) and a pharmaceutically acceptable carrier or excipient. The invention further provides a method for treating cancer comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound represented by formula (I) or (II).
    Type: Grant
    Filed: March 4, 2004
    Date of Patent: July 12, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kyungjin Kim, Emily Aijun Liu, Steven Gregory Mischke
  • Patent number: 6838470
    Abstract: A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate: wherein R1 to R4 independently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, R5 represents H, optionally substituted alkyl, aryl, or aralkyl group, E1 represents O, S, or —NR6, where R6 represents H, an optionally substituted alkyl, aryl, or aralkyl group, E2 represents O, S, or —NR7, where R7 represents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when E1 represents O or S, E2 does not represent O or S, which has an action of suppressing the cytotoxic Ca2+ overload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.
    Type: Grant
    Filed: December 31, 2002
    Date of Patent: January 4, 2005
    Assignee: Daiichi Suntory Pharma Co., Ltd.
    Inventors: Hirokazu Annoura, Kyoko Nakanishi, Shigeki Tamura