Chalcogen And A Carbocyclic Ring Bonded Directly At 4-position Patents (Class 546/217)
-
Patent number: 10023535Abstract: 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: GrantFiled: October 22, 2015Date of Patent: July 17, 2018Assignee: OLON S.P.A.Inventors: Giorgio Bertolini, Corrado Colli, Aldo Bianchi, Federica Colombo, Stefano Maiorana, Filippo Nisic
-
Publication number: 20140329746Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: ApplicationFiled: July 16, 2014Publication date: November 6, 2014Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
-
Publication number: 20140235631Abstract: 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: ApplicationFiled: July 26, 2013Publication date: August 21, 2014Inventors: Antonius Martinus Gustave Bunt, Olaf van Tellingen
-
Publication number: 20140179665Abstract: 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: ApplicationFiled: December 9, 2013Publication date: June 26, 2014Inventors: George D. Hartman, Osvaldo A. Flores
-
Patent number: 8633226Abstract: 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: GrantFiled: September 27, 2012Date of Patent: January 21, 2014Assignee: Bristol-Myers Squibb CompanyInventor: Joseph B. Santella
-
Patent number: 8623867Abstract: 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: GrantFiled: September 11, 2012Date of Patent: January 7, 2014Assignees: 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: 8609849Abstract: 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: GrantFiled: November 29, 2011Date of Patent: December 17, 2013Assignees: 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: 20130310399Abstract: 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: ApplicationFiled: July 24, 2013Publication date: November 21, 2013Applicant: SYNGENTA PARTICIPATIONS AGInventors: Peter Maienfisch, Louis-Pierre Molleyres, Jerome Cassayre, Fredik Cederbaum, Camilla Corsi, Thomas Pitterna
-
Patent number: 8580965Abstract: 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: GrantFiled: October 16, 2007Date of Patent: November 12, 2013Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
-
Patent number: 8536198Abstract: 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: GrantFiled: July 23, 2008Date of Patent: September 17, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Joseph B. Santella, John Hynes, Daniel S. Gardner
-
Patent number: 8501782Abstract: 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: GrantFiled: July 23, 2008Date of Patent: August 6, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Daniel S. Gardner, John V. Duncia, John Hynes, T.G. Murali Dhar, Percy H. Carter, Joseph B. Santella
-
Publication number: 20130178444Abstract: 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: ApplicationFiled: March 5, 2013Publication date: July 11, 2013Inventor: Bristol-Myers Squibb Company
-
Patent number: 8410139Abstract: 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: GrantFiled: October 4, 2010Date of Patent: April 2, 2013Assignee: Bristol-Myers Squibb CompanyInventors: 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: 8362255Abstract: A process for the manufacture of (un)substituted phenylsulfanylphenyl-piperidines comprising the use of benzyl as N-piperidine protecting group is disclosed.Type: GrantFiled: March 2, 2009Date of Patent: January 29, 2013Assignee: H. Lundbeck A/SInventors: Michael Rock, Sebastian Brandes
-
Publication number: 20130023564Abstract: 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: ApplicationFiled: September 27, 2012Publication date: January 24, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
-
Patent number: 8299098Abstract: 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: GrantFiled: June 24, 2009Date of Patent: October 30, 2012Assignee: Bristol-Myers Squibb CompanyInventor: Joseph B. Santella
-
Publication number: 20120270885Abstract: 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: ApplicationFiled: February 10, 2012Publication date: October 25, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Peter Maienfisch, Louis-Pierre Molleyres, Jérôme Cassayre, Fredrik Cederbaum, Camilla Corsi, Thomas Pitterna
-
Publication number: 20120149733Abstract: 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: ApplicationFiled: June 15, 2011Publication date: June 14, 2012Inventors: Robert J. Cherney, John V. Duncia, Daniel S. Gardner, Joseph B. Santella, Zhongyu Wang
-
Patent number: 8012955Abstract: 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: GrantFiled: December 21, 2007Date of Patent: September 6, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Jiaxin Yu, Hui Hong, Sambaiah Thota, Xiang Xu, Ihab S. Darwish
-
Patent number: 7989630Abstract: 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: GrantFiled: April 30, 2008Date of Patent: August 2, 2011Assignee: National Institutes of Health Represented by the Secretary of the Department of Health and Human Services, National Institutes of HealthInventors: Victor W. Pike, Robert B. Innis, Sami S. Zoghbi, Neva Lazarova
-
Publication number: 20110178068Abstract: 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: ApplicationFiled: December 23, 2010Publication date: July 21, 2011Applicant: Alkermes, Inc.Inventors: Orn Almarsson, Laura Cook Blumberg, Julius F. Remenar
-
Publication number: 20110054178Abstract: A process for the manufacture of (un)substituted phenylsulfanylphenyl-piperidines comprising the use of benzyl as N-piperidine protecting group is disclosed.Type: ApplicationFiled: March 2, 2009Publication date: March 3, 2011Applicant: H. LUNDBECK A/SInventors: Michael Rock, Sebastian Brandes
-
Publication number: 20100267704Abstract: 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: ApplicationFiled: October 10, 2008Publication date: October 21, 2010Applicants: President an Fellows of Harvard Colege, Shangha Institute of Organic Chemistry Chineesse Academy of SciencesInventors: Junying Yuan, Dawei Ma, Lihong Zhang
-
Patent number: 7812035Abstract: 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: GrantFiled: December 11, 2002Date of Patent: October 12, 2010Assignee: Sepracor Inc.Inventors: Heike Radeke, Liming Shao
-
Patent number: 7812159Abstract: 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: GrantFiled: January 9, 2006Date of Patent: October 12, 2010Assignee: Arena Pharamaceuticals, Inc.Inventors: Tawfik Gharbaoui, John R. Fritch, Ashwin M. Krishnan, Beverly Wolgast Throop, Naomi S. Kato
-
Publication number: 20100256163Abstract: 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: ApplicationFiled: June 14, 2010Publication date: October 7, 2010Inventors: Clas Sonesson, Lars Swanson, Nicholas Ross Waters
-
Publication number: 20100191475Abstract: 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: ApplicationFiled: March 4, 2010Publication date: July 29, 2010Inventors: Scott Perschke, Ming Liu
-
Publication number: 20100168080Abstract: 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: ApplicationFiled: December 16, 2009Publication date: July 1, 2010Inventors: Uttam KHAMRAI, Sumit Kumar Karak, Matthew Ronsheim, Ashis Kumar Saha
-
Publication number: 20100144657Abstract: The present invention relates to new phenylpiperidine modulators of opioid ?-receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 8, 2009Publication date: June 10, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
-
Publication number: 20100105736Abstract: 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: ApplicationFiled: April 14, 2008Publication date: April 29, 2010Applicant: NSAB, Filial af NeuroSearch Sweden Ab, SverigeInventor: Håkan V. Wikström
-
Patent number: 7700587Abstract: 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: GrantFiled: September 7, 2004Date of Patent: April 20, 2010Assignee: Florida A&M UniversityInventors: Seth Y. Ablordeppey, Donald M. N. Sikazwe
-
Patent number: 7645754Abstract: 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, heteroarylType: GrantFiled: June 19, 2007Date of Patent: January 12, 2010Assignee: OSI Pharmaceuticals, Inc.Inventors: Arlindo Castelhano, Bryan McKibben, Arno Steinig
-
Publication number: 20100004289Abstract: 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: ApplicationFiled: May 1, 2006Publication date: January 7, 2010Applicant: CLERA INC.Inventor: Philip Seeman
-
Publication number: 20090326010Abstract: 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: ApplicationFiled: June 24, 2009Publication date: December 31, 2009Inventor: Joseph B. Santella
-
Publication number: 20090274624Abstract: 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: ApplicationFiled: April 30, 2008Publication date: November 5, 2009Inventors: Victor W. Pike, Robert B. Innis, Sami S. Zoghbi, Neva Lazarova
-
Patent number: 7579474Abstract: 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: GrantFiled: December 7, 2006Date of Patent: August 25, 2009Assignee: NSAB, Filial AF Neurosearch AB, SverigeInventors: Clas Sonesson, Lars Swanson, Nicholas Waters
-
Patent number: 7560459Abstract: 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: GrantFiled: November 2, 2005Date of Patent: July 14, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Ahmed Abdel-Magid, Cynthia Maryanoff, Steven Mehrman, Allen B. Reitz, Bruce Maryanoff
-
Publication number: 20090017489Abstract: 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: ApplicationFiled: June 22, 2006Publication date: January 15, 2009Applicant: Korea University Industry And Academy Cooperation FoundationInventors: Ja hyun Baik, Sung yul Kim
-
Patent number: 7473692Abstract: 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: GrantFiled: September 25, 2002Date of Patent: January 6, 2009Assignee: 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: 20080139564Abstract: 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: ApplicationFiled: November 14, 2007Publication date: June 12, 2008Inventors: John M. Keith, Jennifer M.B. Miller, Emily M. Stocking
-
Publication number: 20080113922Abstract: 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: ApplicationFiled: September 27, 2007Publication date: May 15, 2008Inventors: Bryce Alden Harrison, Spencer David Kimball, Ross Mabon, David Brent Rawlins
-
Patent number: 7338965Abstract: 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: GrantFiled: November 19, 2002Date of Patent: March 4, 2008Assignees: 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: 7129228Abstract: 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: GrantFiled: January 7, 2004Date of Patent: October 31, 2006Assignee: 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: 7060713Abstract: 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: GrantFiled: March 18, 2005Date of Patent: June 13, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Kyungjin Kim, Emily Aijun Liu, Steven Gregory Mischke
-
Patent number: 6987111Abstract: 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: GrantFiled: August 6, 2003Date of Patent: January 17, 2006Assignee: Alkermes Controlled Therapeutics, IIInventors: Kristyn Greco, James Wright
-
Patent number: 6958352Abstract: 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: GrantFiled: February 10, 2003Date of Patent: October 25, 2005Assignee: SmithKline Beecham CorporationInventors: Yazhong Pei, Soumitra S. Ghosh, Ian William James
-
Patent number: 6953801Abstract: 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: GrantFiled: May 21, 2002Date of Patent: October 11, 2005Assignee: Neurogen CorporationInventors: Alan Hutchison, Linda M. Gustavson, John M. Peterson, Dario Doller, Timothy M. Caldwell, Taeyoung Yoon, Wallace C. Pringle, Yiping Shen, Cheryl Steenstra
-
Patent number: 6946478Abstract: 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: GrantFiled: January 9, 2003Date of Patent: September 20, 2005Assignee: AstraZeneca ABInventors: Andrew Baxter, Stephen Brough, Nicholas Kindon, Thomas McInally, Bryan Roberts, Stephen Thom
-
Patent number: 6916833Abstract: 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: GrantFiled: March 4, 2004Date of Patent: July 12, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Kyungjin Kim, Emily Aijun Liu, Steven Gregory Mischke
-
Arylpiperidinopropanol and arylpiprazinopropanol derivatives and pharmaceuticals containing the same
Patent number: 6838470Abstract: 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: GrantFiled: December 31, 2002Date of Patent: January 4, 2005Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Hirokazu Annoura, Kyoko Nakanishi, Shigeki Tamura