Quinolizines (including Hydrogenated) Patents (Class 514/306)
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Patent number: 11219616Abstract: Methods of treating a dengue virus (DENV) infection in a human subject, comprising administering to the human subject a compound of Formula (I), or pharmaceutical composition comprising a compound of Formula (I): A compound of Formula (I) can be administered within onset of fever to 72 hours of fever onset due to dengue infection and then every 6 to 12 hours until there is an improvement in the infection or between from about 1 day to about 10 days. The methods of the invention can be used to treat primary and secondary DENV1-4 viral infections.Type: GrantFiled: December 23, 2019Date of Patent: January 11, 2022Assignees: 60 Degrees Pharmaceuticals, LLC, National University of Singapore, Singapore Health Services PTE Ltd.Inventors: Geoffrey S. Dow, Subhash Vasudevan, Mark Reid, Glynn Morrish, Cynthia Sung, Abhay Rathore, Satoru Watanabe, Eng Eong Ooi, Jenny Low
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Patent number: 11000516Abstract: Methods of preventing a disease resulting from a dengue virus (DENV) infection in a human subject, comprising administering to the human subject a compound of Formula (I), or pharmaceutical composition comprising a compound of Formula (I); a compound of Formula (I) can be first administered to an asymptomatic human subject followed by subsequent doses administered at least once daily. The methods of the invention can be used to prevent a disease resulting from primary and secondary DENV 1-4 viral infections.Type: GrantFiled: December 9, 2016Date of Patent: May 11, 2021Assignees: 60 Degrees Pharmaceuticals, LLC, National University of Singapore, Singapore Health Services PTE Ltd.Inventors: Subhash Vasudevan, Geoffrey S. Dow, Satoru Watanabe, Eng Eong Ooi, Jenny Low, Kitti Wing Ki Chan
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Patent number: 10407408Abstract: Provided is a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2. The present invention relates to a compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION. The compound has a selective MMP-9 production suppressive action, and is useful as a drug for the prophylaxis and/or treatment of autoimmune diseases such as rheumatoid arthritis and the like, inflammatory bowel diseases (ulcerative colitis, Crohn's disease) or osteoarthritis.Type: GrantFiled: July 8, 2016Date of Patent: September 10, 2019Assignee: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Seigo Ishibuchi, Kunio Saruta, Maiko Hamada, Nobuatsu Matoba, Tetsuji Matsudaira, Maki Seki, Akiko Tarao, Takashi Honjo, Shingo Ogata, Atsushi Kawata, Kenji Morokuma, Naoto Fujie, Yukio Aoyama
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Patent number: 10328061Abstract: The present invention concerns the use of castanospermine or other alpha-glucosidase inhibitors for the treatment or prevention of Zika virus infections. Aspects of the invention include methods for treating or preventing Zika virus infection by administering an alpha-glucosidase inhibitor (e.g., an alpha-glucosidase I inhibitor) to a subject in need thereof; methods for inhibiting a Zika virus infection in a cell in vitro or in vivo; pharmaceutical compositions; packaged dosage formulations; and kits for treating or preventing Zika virus infection.Type: GrantFiled: May 2, 2017Date of Patent: June 25, 2019Assignee: FLORIDA STATE UNIVERSITY RESEARCH FOUNDATION, INC.Inventors: Eric Holmes, Gary Ostrander
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Patent number: 10046005Abstract: A composition and associated method for treating a hepatitis C virus (HCV) infection in a subject who is human being. The composition includes: an anti-viral agent and/or a protease inhibitor; a polymerase inhibitor; one or more viral entry inhibitors; and one or more anti-fibrotic agents and/or anti-hemolytic agents including one or more Polyphenols and/or one or more Thiols. The composition may also include one or more sulfated oligosaccharide or non-anticoagulant glycosaminoglycans (GAGs). The method administers, to the subject, a therapeutic dose of the composition to treat the subject for the HCV infection.Type: GrantFiled: August 11, 2016Date of Patent: August 14, 2018Inventor: Shaker A. Mousa
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Patent number: 9199939Abstract: The present invention is directed to quinoline amide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: December 13, 2010Date of Patent: December 1, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Kelly-Ann S. Schlegel, Zhi-Qiang Yang
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Publication number: 20150141435Abstract: Disclosed herein are compounds of Formula I wherein R1, R2, X, and Y are defined herein. These compounds are type II topoisomerase inhibitors and can be used in methods for treating infections caused by gram-positive pathogens, gram-negative pathogens, and drug-resistant strains thereof.Type: ApplicationFiled: January 7, 2015Publication date: May 21, 2015Inventors: Patrick ROUSSEL, Jutta HEIM, Peter SCHNEIDER, Christian BARTELS, Yaoquan LIU, Glen DALE, Daniel MILLIGAN
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Patent number: 8962842Abstract: Described are a series of 2-pyridone compounds as a potent and selective new class of type II topoisomerase inhibitors with broad-spectrum antimicrobial activity having the general formula (I); where R1, R2, X, and Y are defined herein Such compounds can be used in methods for treating an infection caused by a gram-positive pathogen, a gram-negative pathogen, or a drug-resistant strains thereof.Type: GrantFiled: September 16, 2011Date of Patent: February 24, 2015Assignee: Evolva SAInventors: Patrick Roussel, Jutta Heim, Peter Schneider, Christian Bartels, Yaoquan Liu, Glen Dale, Daniel Milligan
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Patent number: 8946446Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: GrantFiled: April 13, 2012Date of Patent: February 3, 2015Assignee: Phenex Pharmaceuticals AGInventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
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Patent number: 8835461Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: GrantFiled: March 23, 2010Date of Patent: September 16, 2014Assignee: Shionogi & Co., Ltd.Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
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Patent number: 8796256Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: May 24, 2011Date of Patent: August 5, 2014Assignee: Janssen Pharmaceutica NVInventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
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Publication number: 20140094450Abstract: The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R?, R?, R??, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: September 19, 2013Publication date: April 3, 2014Applicant: SANOFIInventors: Stephanie HACHTEL, Paulus WOHLFART, John WESTON, Marco MUELLER, Elisabeth DEFOSSA, Katharina MERTSCH, Jian-Hui WENG, Robert Alan BINNIE, Farid ABDUL-LATIF, William Jerome BOCK, Armin WALSER
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Patent number: 8623891Abstract: Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of Formulas (1) and (2) wherein the variables have the meaning disclosed in the specification.Type: GrantFiled: March 4, 2008Date of Patent: January 7, 2014Assignee: Allergan, Inc.Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
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Publication number: 20130310357Abstract: Provided herein are azolyl urea compounds for treatment of CSF-1R kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: May 26, 2011Publication date: November 21, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventor: Gang Liu
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Patent number: 8586570Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.Type: GrantFiled: April 27, 2011Date of Patent: November 19, 2013Assignee: Massachusetts Institute of TechnologyInventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
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Publication number: 20130296228Abstract: Novel compositions and methods of reducing microbial resistance to antimicrobial agents and treating infections are disclosed. In particular, compositions and methods of inhibiting efflux pump activity, treating infection and methods of enhancing antimicrobial activity of antimicrobial agents are provided.Type: ApplicationFiled: April 22, 2013Publication date: November 7, 2013Inventors: Mahesh Vithalbhai PATEL, Sachin Subhash Bhagwat, Mohammad Alam Jafri
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Patent number: 8546425Abstract: Conjugates of antifolates, releasable linkers, and drugs, and pharmaceutical compositions containing them are described. The conjugates are useful for treating diseases arising from pathogenic cell populations. Methods for treating such diseases are also described.Type: GrantFiled: September 17, 2009Date of Patent: October 1, 2013Assignees: Purdue Research Foundation, Endocyte, Inc.Inventors: Christopher Paul Leamon, Iontcho Radoslavov Vlahov, Philip Stewart Low
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Publication number: 20130245035Abstract: Described are a series of 2-pyridone compounds as a potent and selective new class of type II topoisomerase inhibitors with broad-spectrum antimicrobial activity having the general formula (I); where R1, R2, X, and Y are defined herein Such compounds can be used in methods for treating an infection caused by a gram-positive pathogen, a gram-negative pathogen, or a drug-resistant strains thereof.Type: ApplicationFiled: September 16, 2011Publication date: September 19, 2013Applicant: EVOLVA SAInventors: Patrick Roussel, Jutta Heim, Peter Schneider, Christian Bartels, Yaoquan Liu, Glen Dale, Daniel Milligan
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Publication number: 20130172335Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: February 22, 2013Publication date: July 4, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8450313Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: GrantFiled: May 22, 2012Date of Patent: May 28, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Patent number: 8399480Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: April 2, 2009Date of Patent: March 19, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
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Patent number: 8389720Abstract: The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. 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 the neuropeptide S receptor is involved.Type: GrantFiled: November 3, 2009Date of Patent: March 5, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: James C. Barrow, Mark T. Bilodeau, Christopher D. Cox, John C. Hartnett, Nathan R. Kett, Yiwei Li, Peter J. Manley, Jeffrey Melamed, William D. Shipe, B. Wesley Trotter, Amy Zartman
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Patent number: 8357686Abstract: The invention relates to aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description as well as to pharmaceutical compositions and medical treatments employing these compounds.Type: GrantFiled: June 23, 2009Date of Patent: January 22, 2013Assignee: Sanofi-Aventis Deutschland GmbHInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Petra Lennig
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Patent number: 8357692Abstract: Methods of reducing bone loss and treating degenerative bone diseases such as osteoporosis are disclosed. The methods comprise administration of an agent that inhibits signaling through the IL-17 pathway, such as an antibody or a quinazolinone analogue such as halofuginone.Type: GrantFiled: June 17, 2011Date of Patent: January 22, 2013Assignee: Washington UniversityInventors: Steven L. Teitelbaum, Carl J. DeSelm
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Patent number: 8334316Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: GrantFiled: February 9, 2009Date of Patent: December 18, 2012Assignee: ACEA Biosciences, Inc.Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
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Patent number: 8278323Abstract: Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.Type: GrantFiled: May 11, 2009Date of Patent: October 2, 2012Assignee: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec, Allan James Goodman
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Patent number: 8278322Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.Type: GrantFiled: July 28, 2006Date of Patent: October 2, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: M. Katharine Holloway, Nigel J. Liverton, John A. McCauley, Michael T. Rudd, Joseph P. Vacca, Steven W. Ludmerer, David B. Olsen
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Patent number: 8268894Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.Type: GrantFiled: November 11, 2010Date of Patent: September 18, 2012Assignees: The United States of America as Represented by the Secretary, Department of Health and Human Services, Sequella, Inc.Inventors: Marina Nikolaevna Protopopova, Elena Bogatcheva, Leo Einck, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III
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Publication number: 20120232071Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20120232076Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: November 15, 2010Publication date: September 13, 2012Inventors: Scott D. Kuduk, Ronald K. Chang
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Patent number: 8258135Abstract: The present invention is directed to spiropiperidine compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: October 15, 2008Date of Patent: September 4, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Ronald K. Chang, Scott D. Kuduk
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Patent number: 8247415Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: April 2, 2009Date of Patent: August 21, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
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Patent number: 8232265Abstract: Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.Type: GrantFiled: October 10, 2006Date of Patent: July 31, 2012Assignee: Board of Trustees of the University of AlabamaInventors: Robin D. Rogers, Daniel T. Daly, Richard P. Swatloski, Whitney L. Hough, James Hilliard Davis, Jr., Marcin Smiglak, Juliusz Pernak, Scott K. Spear
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Patent number: 8202910Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis. In certain embodiments, the present invention comprises compositions comprising novel substituted ethylene diamine compounds further comprising antitubercular agents such as rifampicin, isoniazid, pyrazinamide and ethambutol.Type: GrantFiled: October 22, 2008Date of Patent: June 19, 2012Assignee: Sequella, Inc.Inventors: Marina Nikolaena Protopopova, Leo Einck, Boris Nikonenko, Ping Chen
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Patent number: 8178520Abstract: The present invention relates to macrocyclic compounds of formula (I): wherein W, n, R1, Ra, Rb, R3, R4, M, Z, ring A and ring B are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.Type: GrantFiled: May 11, 2007Date of Patent: May 15, 2012Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpAInventors: Maria Emilia Di Francesco, Emanuela Nizi, Paola Pace, Vincenzo Summa
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Patent number: 8173672Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: March 11, 2009Date of Patent: May 8, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco
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Patent number: 8163741Abstract: The invention relates to therapeutic use of aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description.Type: GrantFiled: June 23, 2009Date of Patent: April 24, 2012Assignee: Sanofi-Aventis Deutschland GmbHInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Petra Lennig
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Publication number: 20120095010Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.Type: ApplicationFiled: December 22, 2011Publication date: April 19, 2012Inventors: John R. Carson, Ellen Codd, Christine M. Razler, Andrea Works, Mark McDonnell, James J. McNally
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Patent number: 8143273Abstract: The present invention relates to a compound of formula I-A or I-B wherein X, R1, R2 and R3 are defined herein; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. The compounds of formulas I-A and I-B are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors, suitable in the treatment of neurological and neuropsychiatric disorders.Type: GrantFiled: June 16, 2011Date of Patent: March 27, 2012Assignee: Hoffman-La Roche Inc.Inventors: Sabine Kolczewski, Emmanuel Pinard
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Patent number: 8119640Abstract: The present disclosure provides for compounds, pharmaceutical preparations, kits and methods for the inhibition of the Hh pathway and the alleviation of cancer and developmental disorders associated with the Hh pathway.Type: GrantFiled: February 12, 2009Date of Patent: February 21, 2012Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: James K. Chen, Joel M. Hyman, Cory A. Ocasio
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Publication number: 20110311519Abstract: Methods of reducing bone loss and treating degenerative bone diseases such as osteoporosis are disclosed. The methods comprise administration of an agent that inhibits signaling through the IL-17 pathway, such as an antibody or a quinazoline analogue such as halofuginone.Type: ApplicationFiled: June 17, 2011Publication date: December 22, 2011Applicant: Washington UniversityInventors: Steven L. Teitelbaum, Carl J. DeSelm
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Publication number: 20110301192Abstract: The present invention provides compounds that inhibit cyclin kinase inhibitor p21, such as compounds of formula I. The present invention also provides compositions including compounds of Formula I and a pharmaceutically acceptable excipient. In addition, the present invention provides methods of inhibiting cyclin kinase inhibitor p21 and of treating cancer.Type: ApplicationFiled: September 29, 2009Publication date: December 8, 2011Applicant: The regents of the University of CaliforniaInventors: Robert Weiss, See-Hyoung Park, Kit S. Lam, Ruiwu Liu
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Publication number: 20110294780Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
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Publication number: 20110274648Abstract: The present disclosure relates to 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: November 4, 2010Publication date: November 10, 2011Inventors: Rico Lavoie, John A. Bender, Zhong Yang, Makonen Belema, Omar D. Lopez, Qi Chen, Gan Wang, Piyasena Hewawasam
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Publication number: 20110183959Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.Type: ApplicationFiled: January 25, 2011Publication date: July 28, 2011Inventors: Meng-Hsin Chen, James B. Doherty, Robert Tynebor, Swaminathan R. Natarajan, Zhen Li, Soumya P. Sahoo
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Publication number: 20110178122Abstract: The present invention is directed to quinolizidinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: September 29, 2009Publication date: July 21, 2011Inventors: Scott D. Kuduk, Christina Ng Di Marco
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Publication number: 20110160238Abstract: This invention relates to octahydroquinolizines for pharmaceutical use with the following formula: (I), X=H, F; R=Methyl, Ethyl, nPropyl, nButyl.Type: ApplicationFiled: June 29, 2009Publication date: June 30, 2011Applicant: 55PHARMA DRUG DISCOVERY & DEVELOPMENT AGInventors: Immanuel Adorjan, Leonhardt Bauer, Klaus Frobel, Clemens Fuernsinn
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Patent number: 7915287Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: December 19, 2007Date of Patent: March 29, 2011Assignee: Amgen Inc.Inventors: Steven Bellon, Shon Booker, Noel D'Angelo, Julie Germain, Jean-Christophe Harmange, Tae-Seong Kim, Matthew Lee, Longbin Liu, Mark H. Norman, Elizabeth Rainbeau, Ning Xi, Shimin Xu
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Patent number: 7897634Abstract: This invention relates to compounds of the formulas (1), (2) and (3) having pharmacological activity, to compositions containing these compounds, and to methods of treatment employing the compounds and compositions.Type: GrantFiled: January 30, 2007Date of Patent: March 1, 2011Assignee: Athersys, Inc.Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
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Publication number: 20110046145Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: March 11, 2009Publication date: February 24, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco