Spiro Patents (Class 514/212.02)
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Patent number: 8575149Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.Type: GrantFiled: September 14, 2012Date of Patent: November 5, 2013Assignee: Arena Pharmaceuticals, Inc.Inventors: Jeffrey Smith, Brian Smith
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Patent number: 8575148Abstract: This invention concerns spiro azepane-ox-azolidinones as voltage gated Kv1.3 potassium channel blockers, pharmaceutical compositions containing these compounds, methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in the treatment of diabetes, psoriasis, obesity, transplant rejection and inflammatory neuropathies, including T-cell mediated autoimmune diseases such as rheumatoid arthritis and multiple sclerosis. The compounds have formula (1): wherein R1, R2, (R3)n, and (R4)m have the meanings given in the specification.Type: GrantFiled: December 10, 2009Date of Patent: November 5, 2013Assignee: Abbott Healthcare Products B.V.Inventors: Pieter Smid, Michael Mlinaric, Konrad F. Koehler, Sara Nuñez Garcia, Elmar Wegener, Josephus H. M. Lange
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Patent number: 8546379Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.Type: GrantFiled: September 14, 2012Date of Patent: October 1, 2013Assignee: Arena Pharmaceuticals, Inc.Inventors: Brian Smith, Jeffrey Smith
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Patent number: 8546378Abstract: The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.Type: GrantFiled: March 12, 2012Date of Patent: October 1, 2013Assignee: Arena Pharmaceuticals, Inc.Inventors: Dominic P. Behan, Brian M. Smith, Christina Bjenning
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Publication number: 20130231327Abstract: Substituted spiro-amide compounds corresponding to formula I in which R5 through R8, D, X, Y and Z have defined meanings, processes for preparing such spiro-amide compounds, pharmaceutical compositions containing such compounds, and methods of using such spiro-amide compounds for treating and/or inhibiting disorders or disease states mediated at least in part by the bradykinin 1 receptor.Type: ApplicationFiled: April 15, 2013Publication date: September 5, 2013Applicant: Gruenenthal GmbHInventor: Gruenenthal GmbH
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Publication number: 20130225558Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: February 18, 2011Publication date: August 29, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Publication number: 20130131042Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.Type: ApplicationFiled: August 12, 2011Publication date: May 23, 2013Applicant: Merck Sharp & Dohme Corp.Inventors: Joseph L. Duffy, Jianming Bao, Debra L. Ondeyka, Sriram Tyagarajan, Patrick Shao, Feng Ye, Revathi Katipally, Aaron Zwicker, Edward C. Sherer, Michael A. Plotkin, Remond Moningka, Zahid Hussain, Harold B. Wood, Feroze Ujjainwalla, F. Anthony Romero, Paul E. Finke, Yi Zang, Weiguo Liu
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Patent number: 8399453Abstract: The invention relates to organic compounds which have interesting pharmaceutical properties. In particular, the compounds are useful in the treatment and/or prevention of infections such as those caused by Plasmodium falciparum, Plasmodium vivax, Plasmodium malariae, Plasmodium ovale, Trypanosoma cruzi and parasites of the Leishmania genus such as, for example. Leishmania donovani. The invention also relates to pharmaceutical compositions containing the compounds, as well as processes for their preparation.Type: GrantFiled: July 19, 2011Date of Patent: March 19, 2013Assignee: Novartis AGInventors: Shi Hua Ang, Philipp Krastel, Seh Yong Leong, Liying Jocelyn Tan, Wei Lin Josephine Wong, Bryan K. S. Yeung, Bin Zou
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Publication number: 20130065883Abstract: There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3, and/or Flt3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.Type: ApplicationFiled: February 18, 2011Publication date: March 14, 2013Applicant: Centro Nacional de Investigaceiones Oncologicas (CNIO)Inventors: Joaquin Pastor Fernández, Julen Oyarzabal Santamarina, Carl-Gustaf Pierre Saluste, Carmen Blanco Aparicio, Rosa Maria Alvarez Escobar, Virginia Rivero Buceta
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Publication number: 20130065881Abstract: There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description (and which compounds are optionally substituted as indicated in the description), and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease. There is also provided combinations comprising the compounds of formula (I).Type: ApplicationFiled: December 31, 2010Publication date: March 14, 2013Applicant: CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICASInventors: Joaquin Pastor Fernandez, Francisco Javier Ramos Lima, Ana Isabel Hernandez Higueras, Sonia Martinez Gonzalez, Jose Ignacio Martin Hernando, Carl-Gustave Pierre Saluste, Esther Gonzalez Cantalapiedra, Carmen Blanco Aparicio, Antonio Rodriguez Hergueta, Ana Maria Garcia Collazo, Antonio Salgado Serrano, Beatriz Noya Marino
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Patent number: 8367657Abstract: The present invention provides processes and intermediates for the preparation of 3-benzazepines and salts thereof which can be useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.Type: GrantFiled: June 16, 2004Date of Patent: February 5, 2013Assignee: Arena Pharmaceuticals, Inc.Inventors: Beverly L. Wolgast, Charles A. Gilson, III, Shelley Aytes, Scott A. Estrada, Dipanjan Sengupta, Brian Smith, Ulrich Weigl, Heidedore Jlsabeth Rey-Papina
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Publication number: 20130012495Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Inventors: Brian Smith, Jeffrey Smith
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Publication number: 20120302540Abstract: The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.Type: ApplicationFiled: May 24, 2012Publication date: November 29, 2012Inventors: Ameet Vijay Ambarkhane, Gurdip Bhalay, Martin Beckett, James Dale, Ahmed Hamadi, Alessandro Mazzacani, Jeffrey McKenna, Christopher Thomson
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Publication number: 20120283243Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: ApplicationFiled: July 11, 2012Publication date: November 8, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Lewis R. Makings, Miguel Garcia-Guzman Blanco, Dennis J. Hurley, Ioana Drutu, Gabriel Raffai, Daniele M. Bergeron, Akiko Nakatani, Andreas P. Termin, Alina Silina
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Patent number: 8304407Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.Type: GrantFiled: March 7, 2012Date of Patent: November 6, 2012Assignee: Array BioPharma Inc.Inventors: George A. Doherty, Charles Todd Eary, Robert D. Groneberg, Zachary Jones
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Publication number: 20120277192Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: ApplicationFiled: December 15, 2010Publication date: November 1, 2012Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
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Patent number: 8299058Abstract: The use of a compound of formula I, wherein Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; R?, R2, R3, R4, R8 and Ra are specified organic groups and p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2, 3, 4, 5 or 6; provided that when p is 2 then q is not 2; p+q is 1, 2, 3, 4, 5 or 6; or salts or N-oxides thereof or compositions containing them and their using in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.Type: GrantFiled: December 9, 2004Date of Patent: October 30, 2012Assignee: Syngenta Crop Protection LLCInventors: Jérôme Cassayre, Louis-Pierre Molleyres, Peter Maienfisch, Fredrik Cederbaum
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Publication number: 20120270838Abstract: 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: ApplicationFiled: April 27, 2010Publication date: October 25, 2012Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Toru Esaki, Yoshikazu Nishimura, Yoshiaki Isshiki, Naoki Okamoto, Yoshiyuki Furuta, Akemi Mizutani, Masateru Ohta, Wayne Wen Lai, Tomoya Kotake
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Publication number: 20120258949Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C1-C6 alkyl, optionally substituted by C3-C8 cycloalkyl, C6-C10 aryl or hetero(C2-C9)aryl; (CO)R2; (SO2)R3; C3-C8 cycloalkyl; C6-C10 aryl; or hetero(C2-C9)aryl; R1 is halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; Y is CH2 or NR4; Z is C?R5; and R2, R3, R4, and R5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.Type: ApplicationFiled: April 13, 2012Publication date: October 11, 2012Applicant: DAC S.r.I.Inventors: Mario Varasi, Florian Thaler, Raffaella Amici, Agnese Abate, Maria Carmela Fulco, Saverio Minucci, Ciro Mercurio
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Patent number: 8273734Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.Type: GrantFiled: June 14, 2012Date of Patent: September 25, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Brian Smith, Jeffrey Smith
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Publication number: 20120230951Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: March 8, 2012Publication date: September 13, 2012Inventors: Muzaffar Alam, Steven Joseph Berthel, John A. Brinkman, Ronald Charles Hawley, Hongju Li, Wylie Solang Palmer, Sherrie Pietranico-Cole, Ramakanth Sarabu, Mark Smith, Sung-Sau So, Lin Yi, Yansheng Zhai, Qiang Zhang, Shu-Hai Zhao
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Patent number: 8207158Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.Type: GrantFiled: May 27, 2011Date of Patent: June 26, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Brian Smith, Jeffrey Smith
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Publication number: 20120157428Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.Type: ApplicationFiled: December 2, 2011Publication date: June 21, 2012Applicant: CONSTELLATION PHARMACEUTICALS, INC.Inventors: Brian K. Albrecht, James E. Audia, Alexandre Côté, Victor S. Gehling, Jean-Christophe Harmange, Michael C. Hewitt, Yves LeBlanc, Christopher G. Naveschuk, Alexander M. Taylor, Rishi G. Vaswani
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Publication number: 20120156219Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.Type: ApplicationFiled: February 22, 2012Publication date: June 21, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
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Patent number: 8153623Abstract: Compounds of formula (I), pharmaceutical compositions thereof, and methods for treatment using the same.Type: GrantFiled: August 4, 2010Date of Patent: April 10, 2012Assignee: Convergence Pharmaceuticals LimitedInventors: Giuseppe Alvaro, David Amantini, Markus Bergauer, Francesca Bonetti, Roberto Profeta
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Patent number: 8153622Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.Type: GrantFiled: August 17, 2006Date of Patent: April 10, 2012Assignee: Array BioPharma Inc.Inventors: George A. Doherty, C. Todd Eary, Robert D. Groneberg, Zachary Jones
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Patent number: 8153621Abstract: The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.Type: GrantFiled: December 21, 2005Date of Patent: April 10, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Dominic P. Behan, Brian M. Smith, Christina Bjenning
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Publication number: 20120083484Abstract: The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer.Type: ApplicationFiled: September 30, 2011Publication date: April 5, 2012Inventors: Alfredo Castro, Michael J. Grogan, Andre Lescarbeau, Martin Tremblay
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Publication number: 20120077802Abstract: Provided herein are spiro-cyclic compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: June 9, 2010Publication date: March 29, 2012Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
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Publication number: 20120065190Abstract: Compounds of formula I: (wherein variables A1, m, R1, R2, R3, R4 and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: ApplicationFiled: December 14, 2007Publication date: March 15, 2012Inventors: Ian M. Bell, Harold G. Selnick
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Patent number: 8110567Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.Type: GrantFiled: February 4, 2010Date of Patent: February 7, 2012Assignee: H. Lundbeck A/SInventors: Thomas Ruhland, Garrick Paul Smith, Benny Bang-Andersen, Ejner Knud Moltzen, Kim Andersen, Ask Puschl
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Publication number: 20120015934Abstract: The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer.Type: ApplicationFiled: May 6, 2011Publication date: January 19, 2012Inventors: Alfredo C. Castro, Michael J. Grogan, Andre Lescarbeau, Martin R. Tremblay
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Publication number: 20110306595Abstract: The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: February 20, 2010Publication date: December 15, 2011Inventors: Kun Liu, Shawn J. Stachel, Craig A. Coburn, Thomas G. Steele, Richard Soll, Hao Wu, Xuanjin Peng, Yaxian Cai, Xiaoxiang Du, Jian Li
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Publication number: 20110294785Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.Type: ApplicationFiled: August 21, 2009Publication date: December 1, 2011Applicant: The Trustees of the University of PennsylvaniaInventors: William F. DeGrado, Jun Wang
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Publication number: 20110275613Abstract: The invention relates to organic compounds which have interesting pharmaceutical properties. In particular, the compounds are useful in the treatment and/or prevention of infections such as those caused by Plasmodium falciparum, Plasmodium vivax, Plasmodium malariae, Plasmodium ovale, Trypanosoma cruzi and parasites of the Leishmania genus such as, for example. Leishmania donovani. The invention also relates to pharmaceutical compositions containing the compounds, as well as processes for their preparation.Type: ApplicationFiled: July 19, 2011Publication date: November 10, 2011Applicant: NOVARTIS AGInventors: Shi Hua ANG, Philipp KRASTEL, Seh Yong LEONG, Liying Jocelyn TAN, Wei Lin Josephine WONG, Bryan K.S. YEUNG, Bin ZOU
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Publication number: 20110245224Abstract: The present invention relates to compounds of Formula (I); to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.Type: ApplicationFiled: October 13, 2009Publication date: October 6, 2011Inventors: Kevin Barvian, Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
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Publication number: 20110237569Abstract: This invention concerns Spiro azepane-ox-azolidinones as voltage gated Kv1.3 potassium channel blockers, pharmaceutical compositions containing these compounds, methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in the treatment of diabetes, psoriasis, obesity, transplant rejection and inflammatory neuropathies, including T-cell mediated autoimmune diseases such as rheumatoid arthritis and multiple sclerosis. The compounds have formula (1): wherein R1, R2, (R3)n, and (R4)m have the meanings given in the specification.Type: ApplicationFiled: December 10, 2009Publication date: September 29, 2011Applicant: ABBOTT HEALTHCARE PRODUCTS B.V.Inventors: Pieter Smid, Michael Mlinaric, Konrad F. Koehler, Sara Nunez Garcia, Elmar Wegener, Josephus H.M. Lange
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Publication number: 20110218186Abstract: Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the ? opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other ? opioid receptor-mediated conditions.Type: ApplicationFiled: April 29, 2011Publication date: September 8, 2011Applicant: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec, Guo-Hua Chu
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Publication number: 20110178064Abstract: In one aspect, the present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to method for their preparation.Type: ApplicationFiled: July 16, 2008Publication date: July 21, 2011Applicant: ASTRAZENECA R&DInventors: Gregory Steven Basarab, Jacques Dumas, Pamela Hill
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Patent number: 7977329Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.Type: GrantFiled: November 14, 2006Date of Patent: July 12, 2011Assignee: Arena Pharmaceuticals, Inc.Inventors: Jeffrey Smith, Brian Smith
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Publication number: 20110136778Abstract: A compound of the following general formula [I]: wherein each symbol has the same meaning as defined herein, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical use of the same in treating organ transplant rejection, graft versus host reaction after transplantation, autoimmune disease, allergic disease and chronic myeloproliferative disease.Type: ApplicationFiled: July 30, 2010Publication date: June 9, 2011Applicant: JAPAN TOBACCO INC.Inventors: Satoru Noji, Makoto Shiozaki, Tomoya Miura, Yoshinori Hara, Hiroshi Yamanaka, Katsuya Maeda, Akimi Hori, Masafumi Inoue, Yasunori Hase
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Publication number: 20110124630Abstract: An objective of the invention is to provide a compound effective for prevention and/or treatment of cancer. The invention relates to a compound according to by formula I, or a salt, solvate or physiologically functional derivative thereof, and a composition for prevention and/or treatment of cancer comprising the same as an active ingredient: wherein R1 to R6, x, and y are as defined in the description.Type: ApplicationFiled: December 18, 2008Publication date: May 26, 2011Inventors: Naofumi Mukaida, Hiroyuki Ishibashi, Tsuyoshi Taniguchi
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Publication number: 20110105470Abstract: The present invention provides novel tricyclic spiro-oxathiine naphthoquinone derivatives, a synthetic method for making the derivatives, and the use of the derivatives to induce cell death and/or to inhibit proliferation of cancer or precancerous cells. The naphthoquinone derivatives of the present invention are related to the compound known as ?-lapachone (3,4-dihydro-2,2-dimethyl-2H-naphtho(1,2-b)pyran-5,6-dione).Type: ApplicationFiled: January 11, 2011Publication date: May 5, 2011Applicant: ArQule, Inc.Inventors: Mark A. Ashwell, Manish Tandon, Jean-Marc Lapierre, Syed Ali, David Vensel, Chiang J. Li
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Publication number: 20110053911Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.Type: ApplicationFiled: March 13, 2009Publication date: March 3, 2011Inventors: Raffaele Ingenito, Philip Jones, Laura Llauger Bufi, Jesus Maria Ontoria Ontoria, Rita Scarpelli
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Patent number: 7893051Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are thiophenyl and pyrrolyl azepine compounds. These compounds are serotonin receptor (5-HT2c) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT2c) is desired (e.g. addiction, anxiety, depression, obesity, and others).Type: GrantFiled: January 17, 2007Date of Patent: February 22, 2011Assignee: Athersys, Inc.Inventors: L. Nathan Tumey, David C. Bom, Youssef L. Bennani, Michael J. Robarge
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Publication number: 20110034437Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.Type: ApplicationFiled: May 18, 2010Publication date: February 10, 2011Applicant: Infinity Pharmaceuticals, Inc.Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
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Publication number: 20110021500Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2, R3 and R4 are defined as in the description, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, their use and processes for preparing them.Type: ApplicationFiled: November 21, 2008Publication date: January 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
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Publication number: 20110009384Abstract: The present invention provides an agent for the prophylaxis or treatment of diabetes, which has a superior hypoglycemic action, and is associated with a fewer side effects such as body weight gain and the like. The resent invention relates an agent for the prophylaxis or treatment of diabetes, which comprises a compound represented by wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.Type: ApplicationFiled: February 5, 2008Publication date: January 13, 2011Inventors: Taisuke Tawaraishi, Hiroshi Imoto, Nobuo Cho
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Patent number: 7858635Abstract: The present invention relates to spiro compounds of formula XX as modulators of muscarinic receptors, wherein R1, R2, R3, Z1, Z2, L, G, n, m, t and p are defined herein. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: GrantFiled: December 22, 2006Date of Patent: December 28, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Lewis R. Makings, Miguel Garcia-Guzman Blanco, Dennis J. Hurley, Ioana Drutu, Gabriel Raffai, Daniele M. Bergeron, Akiko Nakatani, Andreas P. Termin, Alina Silina
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Publication number: 20100324022Abstract: Compounds of formula (I), pharmaceutical compositions thereof, and methods for treatment using the same.Type: ApplicationFiled: August 4, 2010Publication date: December 23, 2010Applicant: GLAXO GROUP LIMITEDInventors: Giuseppe Alvaro, David Amantini, Markus Bergauer, Francesca Bonetti, Roberto Profeta