Bicyclo Ring System Which Is Isoindole (including Hydrogenated) Patents (Class 546/277.1)
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Patent number: 11261178Abstract: The present disclosure relates to novel compounds, pharmaceutical compositions containing such compounds, and their use in prevention and treatment of cancer and related diseases and conditions.Type: GrantFiled: June 22, 2020Date of Patent: March 1, 2022Assignee: Accutar Biotechnology Inc.Inventors: Jie Fan, Yimin Qian, Wei He, Ke Liu
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Patent number: 11192898Abstract: The present disclosure provides compounds represented by Formula I-A: A1-L1-B1 I-A and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein A1, B1, and L1 are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a condition or disorder responsive to degradation of MDM2 protein such as cancer.Type: GrantFiled: April 6, 2017Date of Patent: December 7, 2021Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Yangbing Li, Jiuling Yang, Angelo Aguilar, Bing Zhou, Jiantao Hu, Fuming Xu, Rohan Rej, Xin Han
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Patent number: 9896443Abstract: Compounds of formula (1a) and pharmaceutically acceptable salts, solvates, and hydrates thereof and related methods of modulatin perforin activity on a cell: wherein Ring A is selected from a 6-10 membered aryl, 5-6 membered cycloalkyi, 5-6 membered heteroaryl or 5-6 membered heterocyclyl, wherein the heteroaryl and heterocyclyl rings comprise at least one heteroatom selected from N, O or S; and wherein the aryl, cycloalkyi, heteroaryl or heterocyclyl rings are optionally substituted with 1 to 3 substituents selected from halo, nitro, —C1-Cealkyl, —C1-Ceaminoalkyl, —C1-C6hydroxyalkyl, -haloC1-C6alkyl, —C1-C6alkoxyl, -haloC1—C<aIkoxyl, heteroaryl, aryl, hydroxyl, —C(0)Ci-C6alkyl, —OC(0)Ci-C6alkyl, —CH2OC(O)CrC6alkyl, —C(O)OC1, —C6alkyI, —NHC(O)C1, —C6alkyl, —NHS(O)2C1-C6alkyl, —S(O)2C1-C6alkyl, —S(O)2NH2, and —C(O)NJJ; Ring B is a 6-10 membered arylene or a 5-6 membered heteroarylene comprising at least one heteroatom selected from N, 0 or S; and wherein the aryl or heteroaryl is optionally, substituted witType: GrantFiled: August 21, 2013Date of Patent: February 20, 2018Assignee: Peter MacCallum Cancer InstituteInventors: Julie Ann Spicer, William Alexander Denny, Christian Karl Miller, Patrick David O'Connor, Kristiina Huttunen, Joseph A. Trapani, Geoff Hill, Kylie Alexander
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Publication number: 20150126485Abstract: The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.Type: ApplicationFiled: May 9, 2013Publication date: May 7, 2015Applicant: Novartis AGInventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
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Publication number: 20150111890Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof,that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: ApplicationFiled: April 19, 2013Publication date: April 23, 2015Inventors: Lisa A. Hasvold, Dachun Liu, Chang Hoon Park, John K. Pratt, George S. Sheppard, Le Wang
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Publication number: 20150025046Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: X is —O—, —N(R), —C(R8)(R9) or —C(O)—; and Y is —O—, —N(R), —C(R8)(R9) or —C(O)— and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ACS, secondary prevention of myocardial infarction or stroke, or PAD.Type: ApplicationFiled: February 27, 2013Publication date: January 22, 2015Inventors: Mihir Mandal, Timothy A. Blizzard, Helen Chen, Harry Chobanian, Yan Guo, Barbara Pio, Zhicai Wu, Tesfaye Biftu, William J. Greenlee, Johnny Zhaoning Zhu
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Patent number: 8916605Abstract: The present application relates to the use of one or more compounds of Formula (I) or pharmaceutically acceptable solvates or prodrugs thereof, for treating cancer or for treating or preventing a viral infection.Type: GrantFiled: March 2, 2010Date of Patent: December 23, 2014Inventor: William G. Tucker
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Patent number: 8912199Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: October 21, 2013Date of Patent: December 16, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
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Patent number: 8846928Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.Type: GrantFiled: November 1, 2011Date of Patent: September 30, 2014Assignee: Portola Pharmaceuticals, Inc.Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
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Publication number: 20140288084Abstract: In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: October 28, 2012Publication date: September 25, 2014Applicant: VANDERBILT UNIVERSITYInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Woods, Corey R. Hopkins, Bruce J. Melancon, Michael S. Poslusney, Darren W. Engers
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Publication number: 20140228360Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.Type: ApplicationFiled: December 20, 2013Publication date: August 14, 2014Applicant: Epizyme, Inc.Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof
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Patent number: 8796313Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating glucokinase mediated disorders. More particularly, the compounds of the present invention are glucokinase modulators useful for treating disorders including, but not limited to, type II diabetes.Type: GrantFiled: October 30, 2006Date of Patent: August 5, 2014Assignee: Janssen Pharmaceutica N.V.Inventors: Joseph Dudash, Philip Rybczynski, Maud Urbanski, Amy Xiang, Roxanne Zeck, Xiaoyan Zhang, Yongzheng Zhang
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Publication number: 20140179686Abstract: The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.Type: ApplicationFiled: February 25, 2014Publication date: June 26, 2014Applicant: Gruenenthal GmbHInventors: Jeewoo LEE, Hyung Chul Ryu, Robert FRANK, Gregor BAHRENBERG, Jean DE VRY, Thomas CHRISTOPH, Derek John SAUNDERS, Klaus SCHIENE, Bernd SUNDERMANN
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Patent number: 8759333Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.Type: GrantFiled: March 13, 2013Date of Patent: June 24, 2014Assignee: Janssen Pharmaceutica NVInventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
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Patent number: 8748582Abstract: The present invention relates generally to affinity ligands and chemical affinity ligand-matrix conjugates for use as chromatographic adsorbents and methods which utilize the adsorbents in the purification of proteins by affinity chromatography. The affinity ligand-matrix conjugates of the present invention comprise ligands of general formula (I): wherein m represents an integer from 0-2, n represents an integer from 0-6, p represents an integer from 0-4, R1 represents H or C1-3 alkyl, R2 is an optional substituent, and X is the position at which the ligand is immobilized, optionally via a linker.Type: GrantFiled: October 15, 2010Date of Patent: June 10, 2014Assignee: Monash UniversityInventors: Milton T W Hearn, Anjali Makarand Bhagwat, William Roy Jackson, Simon John Mountford
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Patent number: 8748426Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of the compounds or their pharmaceutical compositions, to a mammal in need thereof.Type: GrantFiled: December 30, 2010Date of Patent: June 10, 2014Assignee: Piramal Enterprises LimitedInventors: Ravindra Dnyandev Jadhav, Rajiv Sharma
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Patent number: 8722708Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6?R7?); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7? are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.Type: GrantFiled: June 12, 2006Date of Patent: May 13, 2014Assignees: Merck Sharp & Dohme Inc., Pharmacopeia Drug Discovery, Inc.Inventors: Andrew Stamford, Guoqing Li, William Greenlee, Zhaoning Zhu, Brian McKittrick, Robert Mazzola, Ying Huang, Tao Guo, Thuy X. H. Le, Gang Qian, Yuefei Shao
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Patent number: 8664214Abstract: The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I and variables defined herein.Type: GrantFiled: March 25, 2011Date of Patent: March 4, 2014Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Wilfried Braje, Katja Jantos, Hervé Geneste, Mario Mezler, Margaretha Henrica Maria Bakker, Jayne Froggett
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Publication number: 20140038936Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: May 7, 2013Publication date: February 6, 2014Inventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Anne-Laure Grillot, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Jingrong Cao, Upul Keerthi Bandarage, Suganthini S. Nanthakumar
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Publication number: 20140024807Abstract: Novel conjugates and immunogens derived from lenalidomide and antibodies generated by these immunogens are useful in immunoassays for the quantification and monitoring of thalidomide and lenalidomide in biological fluids.Type: ApplicationFiled: March 28, 2013Publication date: January 23, 2014Applicant: Saladax Biomedical Inc.Inventors: Salvatore J. Salamone, Jodi Blake Courtney, Alexander Volkov, Howard Sard, Vishnumurthy Hegde
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Patent number: 8598181Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: July 2, 2010Date of Patent: December 3, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
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Patent number: 8586609Abstract: The invention relates to aryl-substituted polycyclic amines of 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 containing them and to methods of treatment using them.Type: GrantFiled: July 29, 2010Date of Patent: November 19, 2013Assignee: Sanofi-Aventis Deutschland GmbHInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Petra Lennig
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Publication number: 20130302378Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.Type: ApplicationFiled: July 8, 2013Publication date: November 14, 2013Inventors: Viswajanani J. SATTIGERI, Venkata P. PALLE, Manoj Kumar KHERA, Ranadheer REDDY, Manoj Kumar TIWARI, Ajay SONI, Abdul Rehman Abdul RAUF, Sony JOSEPH, Arpita MUSIB, Sunanda G. DASTIDAR, Punit Kumar SRIVASTAVA
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Publication number: 20130295141Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.Type: ApplicationFiled: July 8, 2013Publication date: November 7, 2013Inventors: Viswajanani J. SATTIGERI, Venkata P. PALLE, Manoj Kumar KHERA, Ranadheer REDDY, Manoj Kumar TIWARI, Ajay SONI, Abdul Rehman Abdul RAUF, Sony JOSEPH, Arpita MUSIB, Sunanda G. DASTIDAR, Punit Kumar SRIVASTAVA
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Publication number: 20130281450Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula I.Type: ApplicationFiled: March 12, 2013Publication date: October 24, 2013Inventors: John K. Pratt, Dachun Liu, Chang H. Park, George S. Sheppard, Lisa A. Hasvold, Le Wang
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Patent number: 8541450Abstract: The invention relates to enantiomerically pure 3-(phthalimido)piperidines and processes for preparing enantiomerically pure 3-(phthalimido)piperidines.Type: GrantFiled: March 30, 2009Date of Patent: September 24, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Waldemar Pfrengle, Thorsten Pachur
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Publication number: 20130196967Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R7, A and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: January 29, 2013Publication date: August 1, 2013Inventors: Alessandra BARTOLOZZI, Zhidong CHEN, Jonathon Alan DINES, Ho Yin LO, Pui Leng LOKE, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
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Publication number: 20130143863Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, A1, A2, A3, A4, A5 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful, for example, as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.Type: ApplicationFiled: November 29, 2012Publication date: June 6, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130028843Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.Type: ApplicationFiled: October 10, 2012Publication date: January 31, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Patent number: 8344160Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R4, R5, R3, R3a, W, D, R2a, R2b and R2c are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression, anxiety or intestinal inflammation, by administration of a therapeutically effective dose of a compound according to Formula I.Type: GrantFiled: October 8, 2009Date of Patent: January 1, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Guohua Zhao, William N. Washburn, James J. Mignone
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Publication number: 20120322801Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.Type: ApplicationFiled: March 4, 2011Publication date: December 20, 2012Applicant: Amakem NVInventors: Dirk Leysen, Olivier Defert, Nadzeya Kaval, Petra Blom, Sandro Boland
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Patent number: 8324384Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: February 3, 2010Date of Patent: December 4, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Songnian Lin, Xibin Liao, Edward Metzger, Emma R. Parmee, Sheryl D. Debenham
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Publication number: 20120289505Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.Type: ApplicationFiled: December 30, 2010Publication date: November 15, 2012Inventors: Ravindra Dnyandev Jadhav, Rajiv Sharma
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Patent number: 8309596Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.Type: GrantFiled: June 26, 2008Date of Patent: November 13, 2012Assignee: Novartis AGInventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Andreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
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Publication number: 20120269724Abstract: The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled metal complexes, particularly tissues, organs, or tumors which express certain receptors to which the compounds or complexes of the invention have an affinity. The present invention also relates to methods of treating cancer, particularly those cancer lines which express certain receptors to which the compounds or complexes of the invention have an affinity. In yet another embodiment, the present invention provides methods of imaging and/or inhibiting receptors or neuroreceptors using compounds or complexes of the invention which have an affinity for the receptor or neuroreceptor to be imaged and/or inhibited.Type: ApplicationFiled: December 13, 2011Publication date: October 25, 2012Applicant: President and Fellows of Harvard CollegeInventors: Ashfaq Mahmood, Alun G. Jones, Naengnoi Limpa-Amara, Yijie Peng, Zeynep Akgun
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Publication number: 20120258947Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: April 18, 2012Publication date: October 11, 2012Applicant: Grunenthal GmbHInventors: Sven KÜHNERT, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
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Publication number: 20120259094Abstract: The present invention relates generally to affinity ligands and chemical affinity ligand-matrix conjugates for use as chromatographic adsorbents and methods which utilise the adsorbents in the purification of proteins by affinity chromatography. The affinity ligand-matrix conjugates of the present invention comprise ligands of general formula (I): wherein m represents an integer from 0-2, n represents an integer from 0-6, p represents an integer from 0-4, R1 represents H or C1-3 alkyl, R2 is an optional substituent, and X is the position at which the ligand is immobilized, optionally via a linker.Type: ApplicationFiled: October 15, 2010Publication date: October 11, 2012Inventors: Milton TW Hearn, Anjali Makarand Bhagwat, William Roy Jackson, Simon John Mountford
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Patent number: 8232299Abstract: The present invention relates to compounds that are suitable for treatment of disease states and influence cellular vesicular systems, especially the formation and/or function of lipid droplets, said compound having the general formula I (I) wherein X are each independently hydrogen, halogen, —C1-20-alkyl, —C2-20-alkenyl, —C2-20-alkinyl, —C5-6-cykloalkyl, aryl, aralkyl, adamantyl, heterocyclic, hydroxyl, hydroxyalkyl, Or —N—(R1, R2) group; n is 0, 1, 2, 3, or 4; R1 and R2 may each be independently hydrogen, straight or branching alkyl, cyclo-alkyl, aryl, aralkyl, heterocyclic group, wherein each is un-substituted or halogen substituted; or R1 and R2 together with the nitrogen in between them form a 5 or 6 member ring; A is a single bond, —O—, —S—, —CH2-, or —NH—; Y is O or S; Z is O or S; R? and R? are each independently methyl, ethyl, isopropyl, isobuthyl, sec-butyl or terc-butyl; with the restriction that: X(n) cannot all be fluorine, and A be a single bond, and Y, as well as Z be O, and R?, as well as R? bType: GrantFiled: June 20, 2008Date of Patent: July 31, 2012Assignee: Avidin Kft.Inventors: Laszlo Puskas, Liliana Feher, Eszter Molnar
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Publication number: 20120157497Abstract: The compounds shown by their structural formulas in the specification have analgesic and or immunostimulant activity in mammals.Type: ApplicationFiled: March 1, 2012Publication date: June 21, 2012Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
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Publication number: 20120122854Abstract: The invention is concerned with novel carbocyclyl fused cyclic amines of formula (I) wherein A, X1 to X3, Y1 to Y3, Z, R1, R2, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.Type: ApplicationFiled: January 11, 2012Publication date: May 17, 2012Inventors: Markus Boehringer, Katrin Groebke Zbinden, Wolfgang Haap, Narendra Panday, Fabienne Ricklin, Martin Stahl, Petra Schmitz
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Publication number: 20120122842Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. Disclosed are compounds which inhibit the activity of ROCK, compositions containing the compounds and methods of treating diseases during which ROCK is expressed.Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: Abbott LaboratoriesInventors: Michael L. Curtin, Bryan K. Sorensen, Howard R. Heyman, Richard F. Clark, Kevin R. Woller, Omar J. Shah, Michael Michaelides, Chris Tse, Anil Vasudevan, Helmut Mack, Todd M. Hansen, Ramzi Sweis, Marina A. Pliushchev
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Patent number: 8153664Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: GrantFiled: October 2, 2007Date of Patent: April 10, 2012Assignee: Schering CorporationInventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
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Patent number: 8153638Abstract: Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy.Type: GrantFiled: August 23, 2010Date of Patent: April 10, 2012Assignee: AstraZeneca ABInventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James R. Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
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Publication number: 20120083495Abstract: Compounds useful for the treatment of spinal muscular atrophy or other uses, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced by mutation or frameshift.Type: ApplicationFiled: December 5, 2011Publication date: April 5, 2012Applicants: SCIENCE APPLICATIONS INTERNATIONAL INC. (SAIC), ALBANY MOLECULAR RESEARCH, INC., DEPARTMENT OF HEALTH AND HUMAN SERVICESInventors: Jill Heemskerk, Keith D. Barnes, John M. McCall, Graham Johnson, David Fairfax, Matthew Robert Johnson
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Patent number: 8143288Abstract: Compounds having the structure of formula I are described. The compounds can inhibit hepatitis C virus (HCV) replication, and in particular can inhibit the function of the HCV NS5A protein.Type: GrantFiled: June 5, 2006Date of Patent: March 27, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Michael Serrano-Wu, Makonen Belema, Lawrence B. Snyder, Nicholas A. Meanwell, Denis R. St. Laurent, Ramesh Kakarla, Van N. Nguyen, Yuping Qiu, Xuejie Yang, John E. Leet, Min Gao, Donald R. O'Boyle, II, Julie A. Lemm, Fukang Yang
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Publication number: 20120065396Abstract: The present invention relates to an amide compound or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition comprising the same. The inventive amide compound facilitates bone formation and inhibits bone loss, and is therefore useful for preventing and treating bone disorders such as osteoporosis, osteodystrophy, bone fracture, periodontal disease, Paget's disease, bone metastasis, and rheumatoid arthritis.Type: ApplicationFiled: May 14, 2010Publication date: March 15, 2012Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Jung Nyoung Heo, Bum Tae Kim, Hyuk Lee, Sung Youn Chang, Zang Hee Lee, Seong Hwan Kim, Hyun-Mo Ryoo
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Publication number: 20120046315Abstract: The invention relates to non-crystalline lenalidomide in the form of a storage-stable intermediate, i.e. preferably amorphous lenalidomide together with a surface stabiliser in the form of a stable intermediate or a storage-stable intermediate, containing lenalidomide and matrix material, wherein the lenalidomide is present in the form of a solid solution (i.e. molecularly disperse). The invention further relates to methods of producing stable amorphous or molecularly disperse lenalidomide and pharmaceutical formulations containing stable amorphous or molecularly disperse lenalidomide. In a second aspect, the invention advantageously relates to dry-processing methods for lenalidomide, especially amorphous and disperse lenalidomide.Type: ApplicationFiled: November 13, 2009Publication date: February 23, 2012Inventors: Katrin Rimkus, Frank Muskulus, Sandra Brueck, Jana Paetz
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Patent number: 8119624Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: GrantFiled: October 27, 2010Date of Patent: February 21, 2012Assignee: Pfizer Inc.Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukui, Ru Zhou
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Publication number: 20120040950Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: December 21, 2010Publication date: February 16, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, JR., Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Suganthini S. Nanthakumar, Jingrong Cao, Upul Keerthi Bandarage, Anne-Laure Grillot
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Patent number: 8110681Abstract: Compounds of Formula (I) or (II) useful for the treatment of spinal muscular atrophy or other uses, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced by mutation or frameshift.Type: GrantFiled: March 13, 2007Date of Patent: February 7, 2012Assignees: The United States of America as represented by the Secretary, Department of Health and Human Services, Albany Molecular Research, Inc., Science Applications International Inc. (SAIC)Inventors: Jill Heemskerk, Keith D. Barnes, John M. McCall, Graham Johnson, David Fairfax, Matthew Robert Johnson