Tricyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/586)
  • Patent number: 9399641
    Abstract: A compound with the formula I wherein: R2 is of formula II where Q is selected from OH, SH and NRN, and RN is selected from H, methyl and ethyl, as well as drug-linkers and drug-conjugates made from this compound.
    Type: Grant
    Filed: September 20, 2012
    Date of Patent: July 26, 2016
    Assignee: MEDIMMUNE LIMITED
    Inventor: Philip Wilson Howard
  • Patent number: 9266894
    Abstract: A compound with the formula I wherein: R2 is of formula II where Q is selected from OH, SH and NRN, and RN is selected from H, methyl and ethyl, as well as drug-linkers and drug-conjugates made from this compound.
    Type: Grant
    Filed: September 20, 2012
    Date of Patent: February 23, 2016
    Assignee: MEDIMMUNE LIMITED
    Inventor: Philip Wilson Howard
  • Patent number: 8999969
    Abstract: The present invention relates to anti-RSV compounds of Formula (I) and methods for use of the compounds in the treatment and prevention of RSV infection.
    Type: Grant
    Filed: July 7, 2010
    Date of Patent: April 7, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Richard L. Mackman, David Sperandio, Hai Yang
  • Publication number: 20140286899
    Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.
    Type: Application
    Filed: November 18, 2013
    Publication date: September 25, 2014
    Applicant: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Patent number: 8835421
    Abstract: The present invention provides a compounds of general formula (8), (11) and (14), useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepine hybrids of general formula (8), (11) and (14).
    Type: Grant
    Filed: October 31, 2008
    Date of Patent: September 16, 2014
    Assignee: Council of Scientific and Industrial Research
    Inventors: Ahmen Kamal, Pogula Praveen Kumar, Bobburi Naga Seshadri, Kokkonda Sreekanth
  • Publication number: 20140206672
    Abstract: 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: Application
    Filed: March 19, 2014
    Publication date: July 24, 2014
    Applicant: ABT Holding Company
    Inventors: L. Nathan Tumey, David C. Bom, Youssef L. Bennani, Michael J. Robarge
  • Patent number: 8779154
    Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: September 25, 2007
    Date of Patent: July 15, 2014
    Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen
  • Publication number: 20140194411
    Abstract: 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 benzazepine 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: Application
    Filed: December 23, 2013
    Publication date: July 10, 2014
    Applicant: ABT Holding Company
    Inventors: Mike Robarge, John Harrington, David Gerrish, John Mecom
  • Publication number: 20140163012
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described.
    Type: Application
    Filed: October 31, 2013
    Publication date: June 12, 2014
    Applicant: Albany Molecular Research, Inc.
    Inventors: Matthew D. SURMAN, Emily E. FREEMAN, Peter R. GUZZO, Alan J. HENDERSON, Mark HADDEN
  • Patent number: 8716276
    Abstract: 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: Grant
    Filed: January 12, 2011
    Date of Patent: May 6, 2014
    Assignee: Athersys, Inc.
    Inventors: L. Nathan Tumey, David C. Bom, Youssef L. Bennani, Michael J. Robarge
  • Publication number: 20130302282
    Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.
    Type: Application
    Filed: October 21, 2011
    Publication date: November 14, 2013
    Applicant: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Patent number: 8546379
    Abstract: 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: Grant
    Filed: September 14, 2012
    Date of Patent: October 1, 2013
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Brian Smith, Jeffrey Smith
  • Publication number: 20130190293
    Abstract: This disclosure is directed to tetracyclic pyrido[4,3-b]indole and pyrido[3,4-b]indoles. 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: Application
    Filed: February 18, 2011
    Publication date: July 25, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130184256
    Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: March 5, 2013
    Publication date: July 18, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Henning PRIEPKE, Georg DAHMANN, Kai GERLACH, Roland PFAU, Wolfgang WIENEN, Annette SCHULER-METZ, Sandra HANDSCHUH, Herbert NAR
  • Publication number: 20130167930
    Abstract: The invention relates to compounds of general formula IIIa and their use in optoelectronic components.
    Type: Application
    Filed: December 29, 2011
    Publication date: July 4, 2013
    Applicant: Heliatek Gmbh
    Inventors: Dirk Hildebrandt, Gunter Mattersteig, Olga Gerdes, Serge Vetter, Andre Weiss
  • Patent number: 8367657
    Abstract: 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: Grant
    Filed: June 16, 2004
    Date of Patent: February 5, 2013
    Assignee: 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
  • Publication number: 20130012495
    Abstract: 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: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Inventors: Brian Smith, Jeffrey Smith
  • Publication number: 20120196846
    Abstract: The present invention relates to anti-RSV compounds of Formula (I) and methods for use of the compounds in the treatment and prevention of RSV infection.
    Type: Application
    Filed: July 7, 2010
    Publication date: August 2, 2012
    Applicant: Gilead Sciences, Inc.
    Inventors: Richard L. Mackman, David Sperandio, Hai Yang
  • Publication number: 20120184531
    Abstract: The present invention relates to benzofuro[3,2-c]pyridine and azepine analogs as serotonin sub-type 6 (5-HT6) modulators, pharmaceutical compositions including these compounds, methods of preparation, and use thereof. These compounds are useful in the treatment of central nervous system disorders including obesity, metabolic syndrome, cognition, schizophrenia, attention deficit hyperactivity disorder, bipolar disorder, rare and orphan diseases, and sleep disorders. The subject compounds have the structure of formula (I) with the substituents being described herein.
    Type: Application
    Filed: January 18, 2012
    Publication date: July 19, 2012
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Peter R. GUZZO, Alan J. HENDERSON, Matthew ISHERWOOD, Chong Yew LEE, Animesh GHOSH, He ZHAO
  • Patent number: 8202858
    Abstract: The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.
    Type: Grant
    Filed: August 24, 2005
    Date of Patent: June 19, 2012
    Assignee: Vantia Limited
    Inventors: Andrzej Roman Batt, Martin Lee Stockley, Michael Bryan Roe, Celine Marguerite Simone Heeney, Andrew John Baxter, Peter Hudson, Rachel Handy
  • Publication number: 20120095075
    Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells.
    Type: Application
    Filed: August 16, 2011
    Publication date: April 19, 2012
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah MANOHARAN, Kallanthottathil G. Rajeev, David Butler, Narayanannair K. Jayaprakash, Muthusamy Jayaraman, Laxman Eltepu
  • Patent number: 8133992
    Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.
    Type: Grant
    Filed: January 29, 2009
    Date of Patent: March 13, 2012
    Assignee: Exelixis, Inc.
    Inventors: Richard Martin, Tie-Lin Wang, Brenton T. Flatt, Xiao-Hui Gu, Ronald Griffith
  • Publication number: 20120040966
    Abstract: The compounds provided herein are suitable for inhibiting a virus in a patient and for treating a patient suffering from a viral infection such as an influenza virus. Also provided is a method for screening of compounds for use in treating and preventing viral infections. The assay screens compounds for activity against an influenza virus by measuring the cytopathogenic effect (CPE) of the compound on influenza infected-cells using percent cell viability as the end point.
    Type: Application
    Filed: December 28, 2009
    Publication date: February 16, 2012
    Applicant: Southern Research Institute Office of Commercialization and Intellectual Prop
    Inventors: Joseph A. Maddry, Bill Severson, Colleen B. Jonsson, James W. Noah, Diana L. Noah, Xi Chen
  • Patent number: 8039620
    Abstract: Crystalline forms of Varenicline Tosylate: are provided, along with processes for preparing those crystalline forms of Varenicline Tosylate, and processes for obtaining high purity Varenicline base using Varenicline Tosylate.
    Type: Grant
    Filed: May 21, 2009
    Date of Patent: October 18, 2011
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Suhail Ahmad, Vinod Kumar Kansal, Maytal Piran, Zvi Harel
  • Publication number: 20110190268
    Abstract: The present invention provides a compounds of general formula (8), (11) and (14), useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo [2,1-c][1,4]benzodiazepine hybrids of general formula (8), (11) and (14).
    Type: Application
    Filed: October 31, 2008
    Publication date: August 4, 2011
    Inventors: Ahmed Kamal, Pogula Praveen Kumar, Bobburi Naga Seshadri, Kokkonda Sreekanth
  • Patent number: 7989444
    Abstract: Compounds of formula (I) wherein A is a 5 or 6 membered heteroaromatic ring or a 5 or 6 membered heterocyclic ring, and which are useful for treating mental disorders such as schizophrenia are set out herein.
    Type: Grant
    Filed: May 31, 2005
    Date of Patent: August 2, 2011
    Assignee: Glaxo Group Limited
    Inventors: Giorgio Bonanomi, Federica Damiani, Gabriella Gentile, Dieter Wolfgang Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco, Silvia Terreni
  • Patent number: 7977329
    Abstract: 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: Grant
    Filed: November 14, 2006
    Date of Patent: July 12, 2011
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Jeffrey Smith, Brian Smith
  • Patent number: 7951796
    Abstract: The invention relates to compounds according to general formula (1) and/or their enantiomers, diastereomers as well as their pharmaceutically compatible salts, and to the use thereof for producing a medicament suited for treating diseases associated with misfolded proteins.
    Type: Grant
    Filed: February 28, 2006
    Date of Patent: May 31, 2011
    Inventors: Carsten Korth, Ralf Klingenstein, Stefan Löber, Peter Gmeiner
  • Publication number: 20110124630
    Abstract: 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: Application
    Filed: December 18, 2008
    Publication date: May 26, 2011
    Inventors: Naofumi Mukaida, Hiroyuki Ishibashi, Tsuyoshi Taniguchi
  • Publication number: 20110118199
    Abstract: The present invention relates to the treatment of protozoal diseases by administering cytotoxic and/or cytostatic compounds, in particular those used in anticancer therapy, to patients. In particular, the invention relates to the use of anticancer agents that can penetrate into the CNS for treatment of late stage African sleeping sickness or cerebral malaria.
    Type: Application
    Filed: January 11, 2007
    Publication date: May 19, 2011
    Inventor: Matthias Dormeyer
  • Publication number: 20110112072
    Abstract: 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: Application
    Filed: January 12, 2011
    Publication date: May 12, 2011
    Inventors: L. Nathan Tumey, David C. Bom, Youssef L. Bennani, Michael J. Robarge
  • Patent number: 7893051
    Abstract: 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: Grant
    Filed: January 17, 2007
    Date of Patent: February 22, 2011
    Assignee: Athersys, Inc.
    Inventors: L. Nathan Tumey, David C. Bom, Youssef L. Bennani, Michael J. Robarge
  • Patent number: 7875712
    Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; ?between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.
    Type: Grant
    Filed: September 23, 2008
    Date of Patent: January 25, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
  • Publication number: 20100317848
    Abstract: The present invention relates to a process for the manufacturing of substituted 3-amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) and their precursors in high optical purity to the precursors of the synthesis of substituted S-Amino-tetrahydrofuran-S-carboxylic acid amides of general formula (I) in high optical purity, and to the tautomers, enantiomers, diastereomers, mixtures and salts of substituted 3-amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) in high optical purity, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: December 21, 2007
    Publication date: December 16, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Zhengxu Han, Kai Gerlach, Dhileepkumar Krishnamurthy, Burkhard Matthes, Herbert Nar, Roland Pfau, Henning Priepke, Annette Schuler-Metz, Chris H. Senanayake, Peter Sieger, Wenjun Tang, Wolfgang Wienen, Yibo Xu, Nathan K. Yee
  • Publication number: 20100267695
    Abstract: [Problems] To provide a compound which is useful as an NMDA receptor antagonist. [Means for Solution] The present inventors have studied a compound having an NMDA receptor antagonistic action, and confirmed that the fused indane compound of the present invention has an excellent NMDA receptor antagonistic action, thereby completed the present invention. The fused indane compound of the present invention has an excellent NMDA receptor antagonistic action and can be used as a prophylactic and/or therapeutic agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, intractable depression, attention deficit hyperactivity disorder, migraines, or the like.
    Type: Application
    Filed: November 26, 2008
    Publication date: October 21, 2010
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Satoshi Hayashibe, Shingo Yamasaki, Nobuyuki Shiraishi, Hiroaki Hoshii, Takahiko Tobe
  • Publication number: 20100204207
    Abstract: Compounds of Formula (I): wherein n, m, p, q, Y, R1, R2, R3a, R3b, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed.
    Type: Application
    Filed: April 20, 2010
    Publication date: August 12, 2010
    Inventors: Xinchao Chen, Christopher Lawrence Cioffi, Sean Richard Dinn, Ana Maria Escribano, Maria Carmen Fernandez, Todd Fields, Robert Jason Herr, Nathan Bryan Mantlo, Eva Maria Martin De La Nava, Ana Isabel Mateo Herranz, Saravanan Parthasarathy, Xiaodong Wang
  • Publication number: 20100190772
    Abstract: The present invention generally relates to compounds and pharmaceutical compositions containing the compounds. More specifically, compounds of the present invention are hexahydroazepinoindole and octahydroazepinoindole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).
    Type: Application
    Filed: April 1, 2010
    Publication date: July 29, 2010
    Inventors: Youssef L. Bennani, Michael J. Robarge, David C. Bom, Norbert Varga, Lawrence N. Tumey
  • Publication number: 20100173893
    Abstract: A process for preparing a compound of the formula IA or IB: wherein R is alkyl, aminoalkyl, halogenalkyl, aralkyl, cycloalkyl, cycloalkylalkyl, alkoxy, phenyl or substituted phenyl or pyridyl group; the term alkyl means carbon chain, straight or branched, containing from 1 to 18 carbon atoms; the term halogen represents fluorine, chlorine, bromine or iodine; the term cycloalkyl represents a saturated alicyclic group with 3 to 6 carbon atoms; the term aryl represents unsubstituted phenyl group or phenyl substituted by alkoxy, halogen or nitro group, the process comprising asymmetric hydrogenation of a compound of the formula II: wherein R has the same meanings as above, using a chiral catalyst and a source of hydrogen.
    Type: Application
    Filed: April 11, 2007
    Publication date: July 8, 2010
    Inventors: Bing Yu, Wenge Li, David Alexander Learmont
  • Publication number: 20100173824
    Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular, compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.
    Type: Application
    Filed: August 4, 2009
    Publication date: July 8, 2010
    Applicant: EXELIXIS, INC.
    Inventors: Brett Busch, Brenton T. Flatt, Xiao-Hui Gu, Richard Martin, Raju Mohan, Tie-Lin Wang, Jason H. Wu
  • Patent number: 7727980
    Abstract: This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds.
    Type: Grant
    Filed: January 31, 2006
    Date of Patent: June 1, 2010
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Lin Zhi, Cornelis Arjan Van Oeveren
  • Publication number: 20100105894
    Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.
    Type: Application
    Filed: June 9, 2009
    Publication date: April 29, 2010
    Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafuml Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
  • Publication number: 20100087420
    Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.
    Type: Application
    Filed: December 4, 2009
    Publication date: April 8, 2010
    Applicant: ALANTOS PHARMACEUTICALS HOLDINGS, INC.
    Inventors: Christian Gege, Carine Chevrier, Matthias Schneider, Harald Bluhm, Matthias Hochgürtel, Hongbo Deng, Brian M. Gallagher, JR., Irving Sucholeiki, Arthur G. Taveras
  • Patent number: 7691844
    Abstract: The invention is directed to nonpeptide substituted benzodiazepines of Formula I, wherein A, X, n, R1, R2, R3, R4, R5, a and b are as described in the specification, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.
    Type: Grant
    Filed: October 16, 2006
    Date of Patent: April 6, 2010
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Robert H. K. Chen, Min A. Xiang
  • Publication number: 20100048536
    Abstract: The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the ?v?3 integrin receptor, and pharmaceutical preparations comprising these compounds.
    Type: Application
    Filed: March 3, 2009
    Publication date: February 25, 2010
    Inventors: Herve Geneste, Andreas Kling, Arnulf Lauterbach, Claudia Isabella Graef, Thomas Subkoski, Wilfried Hornberger
  • Publication number: 20100029616
    Abstract: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters and prodrugs thereof, pharmaceutical compositions containing compounds of formula (I) and the use of said compounds and compositions as urotensin II receptor antagonists.
    Type: Application
    Filed: July 31, 2009
    Publication date: February 4, 2010
    Inventors: William A. Kinney, Diane K. Luci, Bruce E. Maryanoff, Shyamali Ghosh, Edward C. Lawson
  • Patent number: 7625888
    Abstract: The present invention is directed to novel fused triazole derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. 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 dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: December 1, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Ann E. Weber, Wallace T. Ashton
  • Publication number: 20090215736
    Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.
    Type: Application
    Filed: September 23, 2008
    Publication date: August 27, 2009
    Applicant: Vertex Pharmaceuticals, Incorporated
    Inventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
  • Publication number: 20090131406
    Abstract: The present invention relates to cripowellins and synthetic derivatives thereof for treating diseases of man and also, in particular, to their use for preparing a medicament for treating cancer or other proliferative disorders in man and animal. Furthermore, the present invention relates to novel cripowellin derivatives and processes for their preparation.
    Type: Application
    Filed: June 13, 2006
    Publication date: May 21, 2009
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Horst-Peter Antonicek, Robert Velten, Peter Jeschke
  • Publication number: 20090131408
    Abstract: The present invention relates to novel aza-thia-benzoazulene derivatives of formula I as defined in the claims, their preparation, the use of these novel compounds for the preparation of pharmaceutical compositions, the use of these novel compounds and compositions for managing arthritis and arthritis-related conditions as well as in the treatment of pain in animals and humans. More particularly, the present invention relates to pharmaceutical, preferably veterinary compositions and methods for reducing inflammation and pain associated with acute inflammation of body parts, particularly joints, due to injury or due to arthritic conditions or other disease conditions.
    Type: Application
    Filed: February 21, 2007
    Publication date: May 21, 2009
    Inventors: Pietro Bollinger, Mahavir Prashad, Bernhard Riss, Janet Dawson King, Peter C. Hiestand, Yugang Liu, Jonathan King, Vincent Schmid, Friedrich Schuerch
  • Publication number: 20090069282
    Abstract: The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
    Type: Application
    Filed: May 15, 2008
    Publication date: March 12, 2009
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Dirk Stenkamp, Stephan Georg Mueller, Gerald Juergen Roth, Thorsten Lehmann-Lintz, Klaus Rudolf, Philipp Lustenberger, Kirsten Arndt, Ralf R. H. Lotz, Martin Lenter