Two Of The Cyclos Share At Least Three Ring Members Or A Ring Member Is Shared By Three Of The Cyclos (e.g., Bridged, Peri-fused, Etc.) Patents (Class 540/520)
  • Patent number: 10669286
    Abstract: A series of substituted fused pentacyclic benzimidazole derivatives, and analogues thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: June 2, 2020
    Assignees: UCB Biopharma SRL, Sanofi
    Inventors: Michael Louis Robert Deligny, Jag Paul Heer
  • Patent number: 9045487
    Abstract: The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
    Type: Grant
    Filed: May 8, 2014
    Date of Patent: June 2, 2015
    Assignee: PFIZER INC.
    Inventors: Patricia Ann Basford, Anthony Michael Campeta, Adam Gillmore, Matthew Cameron Jones, Eleftherios Kougoulos, Suman Luthra, Robert Walton
  • Patent number: 8980879
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R6, Y1, Y2, A1, A2, A3, and A4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: March 17, 2015
    Assignee: AbbVie Inc.
    Inventors: Dachun Liu, John Pratt, Le Wang, Lisa A. Hasvold, Andrew Bogdan
  • Publication number: 20150065703
    Abstract: Disclosed are a new method for synthesizing 7-membered fused heterocycles and compounds synthesized by the new method. The method involves a dual activation strategy using an N-heterocyclic carbene catalyst as a first Lewis base and another second Lewis base. Compounds synthesized by the disclosed method may include new benzoxopinone compounds, as well as benzoxepane compounds and benzoazepinone compounds that optionally may be derived from the disclosed benzoxopinone compounds.
    Type: Application
    Filed: August 22, 2014
    Publication date: March 5, 2015
    Applicant: Northwestern University
    Inventors: Karl A. Scheidt, Javier Izquierdo Ferrer
  • Publication number: 20140275034
    Abstract: A method for repelling blood-sucking and biting insects, ticks and mites involving treating an object or area with a blood-sucking and biting insects, ticks and mites repelling effective amount of camphor lactams, verbenone lactams, dolicholactams, dolicholactone, and their precursors, and mixtures thereof, and optionally a carrier.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 18, 2014
    Inventors: Kamlesh R. Chauhan, Bheema R. Paraselli
  • Publication number: 20140256710
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R6, Y1, Y2, A1, A2, A3, and A4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: March 11, 2014
    Publication date: September 11, 2014
    Inventors: Dachun Liu, John Pratt, Le Wang, Lisa A. Hasvold, Andrew Bogdan
  • Publication number: 20140243318
    Abstract: The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Applicant: Pfizer Inc.
    Inventors: Patricia Ann Basford, Anthony Michael Campeta, Adam Gillmore, Matthew Cameron Jones, Eleftherios Kougoulos, Suman Luthra, Robert Walton
  • Publication number: 20140228353
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 14, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvvajit Chakravarty
  • Patent number: 8754072
    Abstract: The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: June 17, 2014
    Assignee: Pfizer Inc.
    Inventors: Patricia Ann Basford, Anthony Michael Campeta, Adam Gillmore, Matthew Cameron Jones, Eleftherios Kougoulos, Suman Luthra, Robert Walton
  • Patent number: 8710047
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: April 29, 2014
    Assignee: Albany Molecular Research, Inc.
    Inventors: David D. Manning, Christopher L. Cioffi
  • Patent number: 8710046
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: June 30, 2010
    Date of Patent: April 29, 2014
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter R. Guzzo, David D. Manning, William Earley
  • Patent number: 8691808
    Abstract: The present disclosure provides compounds having affinity for the M2 proton channel, useful for the treatment of viral infections such as influenza, which are of the Formula (I): wherein R1, R2, and Y are as defined herein. Methods of preparing the compounds, pharmaceutical compositions containing the compounds, and methods of using the compounds in the treatment of viral infections such as influenza are also provided.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: April 8, 2014
    Assignee: Influmedix, Inc.
    Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
  • Publication number: 20130317007
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: April 11, 2013
    Publication date: November 28, 2013
    Applicant: Reata Pharmaceuticals, Inc.
    Inventors: Eric ANDERSON, Xin JIANG, Melean VISNICK
  • Patent number: 8501729
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: August 6, 2013
    Assignee: Albany Molecular Research, Inc.
    Inventors: David D. Manning, Christopher Lawrence Cioffi
  • Publication number: 20130144053
    Abstract: The present invention relates to improved processes for preparing lactam morphinans. The processes generally transform keto-morphinans to seven-membered lactam morphinans using a hydroxyamine sulfonic acid reagent and proceed in high yield and with good selectivity.
    Type: Application
    Filed: December 5, 2012
    Publication date: June 6, 2013
    Applicant: Mallinckrodt LLC
    Inventor: Mallinckrodt LLC
  • Patent number: 8440820
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: May 14, 2013
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
  • Publication number: 20130053365
    Abstract: Provided are inhibitors of poly(ADP-ribose)polymerase according to Formula (M): where A, B, Y, Z, D, E, R1, R2, R3, and R4 are as defined herein. Also described are pharmaceutical compositions, methods of preparing, and methods of using a compound of Formula M to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
    Type: Application
    Filed: August 29, 2012
    Publication date: February 28, 2013
    Applicant: BioMarin Pharmaceutical, Inc.
    Inventors: Bing Wang, Daniel Chu
  • Publication number: 20120295886
    Abstract: The present disclosure provides compounds having affinity for the M2 proton channel, useful for the treatment of viral infections such as influenza, which are of the Formula (I): wherein R1, R2, and Y are as defined herein. Methods of preparing the compounds, pharmaceutical compositions containing the compounds, and methods of using the compounds in the treatment of viral infections such as influenza are also provided.
    Type: Application
    Filed: May 18, 2012
    Publication date: November 22, 2012
    Applicant: INFLUMEDIX, INC.
    Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
  • Publication number: 20120270857
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: June 30, 2010
    Publication date: October 25, 2012
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Peter R. Guzzo, David D. Manning, William Earley
  • Publication number: 20120271046
    Abstract: The present invention relates to 7-membered nitrogen-containing heterocyclic compounds and methods of making the same. Using a novel aza-[4+3] cycloaddition reaction, the 7-membered heterocyclic compounds are synthesized by reacting a first reactant and a second reactant. Exemplary first reactants and second reactants include ?-halohydroxamates and dienes, respectively.
    Type: Application
    Filed: April 19, 2012
    Publication date: October 25, 2012
    Inventor: Christopher S. Jeffrey
  • Publication number: 20120230951
    Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: March 8, 2012
    Publication date: September 13, 2012
    Inventors: Muzaffar Alam, Steven Joseph Berthel, John A. Brinkman, Ronald Charles Hawley, Hongju Li, Wylie Solang Palmer, Sherrie Pietranico-Cole, Ramakanth Sarabu, Mark Smith, Sung-Sau So, Lin Yi, Yansheng Zhai, Qiang Zhang, Shu-Hai Zhao
  • Patent number: 8173802
    Abstract: Provided is a method for producing a piperidin-4-one derivative useful as an intermediate for agricultural chemicals or pharmaceutical products. A piperidin-4-one derivative represented by formula (III-a) or formula (III-b) is produced by reacting a cyclic bis(aminol)ether compound represented by formula (I) and an acetone derivative represented by formula (II) in the presence of at least one substance selected from the group consisting of protonic acids, Lewis acids, acid halides and dialkyl sulfuric acids.
    Type: Grant
    Filed: October 10, 2007
    Date of Patent: May 8, 2012
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Hirohito Oooka, Yasushi Shibata, Hiroki Inoue, Tsutomu Imagawa
  • Patent number: 8124600
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: May 28, 2009
    Date of Patent: February 28, 2012
    Assignee: Albany Molecular Research, Inc.
    Inventors: David D. Manning, Christopher Lawrence Cioffi
  • Publication number: 20110281845
    Abstract: The present disclosure relates to XIAP inhibitor compounds of the formula I.
    Type: Application
    Filed: June 15, 2011
    Publication date: November 17, 2011
    Applicant: NOVARTIS AG
    Inventors: Zhuoliang CHEN, Mark G. PALERMO, Sushil K. SHARMA, Troy SMITH, Christopher S. STRAUB, Run-Ming D. WANG, Yaping WANG, Leigh ZAWEL
  • Patent number: 8008289
    Abstract: The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs).
    Type: Grant
    Filed: August 10, 2005
    Date of Patent: August 30, 2011
    Assignee: Cambridge Enterprise Limited
    Inventors: David J. Grainger, David John Fox
  • Patent number: 8008288
    Abstract: The invention provides compounds, compositions, and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, for the preparation of a medicament intended to treat an inflammatory disorder wherein y is any integer from 1 to 8; z is any integer from 1 to 8; with the proviso that y and z cannot both equal 1; X is —C —(Y)k—(R1)n or SO2—(Y)k—(R1)n; k is 0 or 1; Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or Y is a cycloalkenyl or polycycloalkenyl group.
    Type: Grant
    Filed: August 10, 2005
    Date of Patent: August 30, 2011
    Assignee: Cambridge Enterprise Limited
    Inventors: David J. Grainger, David John Fox
  • Patent number: 7947677
    Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, D2, E1, E2, E3, E4, E5, G1, G2, J, K, T, U, V, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: November 14, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Steven N. Gallicchio, C. Blair Zartman, Harold G. Selnick
  • Patent number: 7915402
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: April 20, 2009
    Date of Patent: March 29, 2011
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
  • Publication number: 20110053911
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.
    Type: Application
    Filed: March 13, 2009
    Publication date: March 3, 2011
    Inventors: Raffaele Ingenito, Philip Jones, Laura Llauger Bufi, Jesus Maria Ontoria Ontoria, Rita Scarpelli
  • Publication number: 20100093997
    Abstract: The fluorinated derivatives of catharanthine according to the invention respond to the general formula I: in which: the dotted line expresses the possibility of the presence of a double bond when the substitution —X is absent or else a single bond when —X designates a substitution for a group: H, OR, NR?R?, SR, or a halogen atom with R, R? and R? designating independently of one another a hydrogen atom or a linear or branched alkyl group in C1 to C6, R1, R2 and R3 represent independently of one another an atom of hydrogen, of fluorine or a methylated group, on the condition nevertheless that at least one of the radicals R1 and R2 represents an atom of fluorine, and n=1 or 2.
    Type: Application
    Filed: September 20, 2007
    Publication date: April 15, 2010
    Applicants: Pierre Fabre Medicament, COMMISSARIAT A L'ENERGIE ATOMIQUE
    Inventors: Lionel Moisan, Sébastien Comesse, Emerson Giovanelli, Bernard Rousseau, Eric Doris, Paul Hellier
  • Patent number: 7696192
    Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R5c, m and n are defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: September 6, 2005
    Date of Patent: April 13, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Steven N. Gallicchio, Craig A. Stump, Cory R. Theberge, Joseph P. Vacca, C. Blair Zartman, Xufang Zhang
  • Publication number: 20100056777
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: April 20, 2009
    Publication date: March 4, 2010
    Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
  • Patent number: 7550588
    Abstract: Disclosed are novel homotropane compounds with CNS activity. These compounds can be used for alleviating symptoms of CNS disorders.
    Type: Grant
    Filed: March 12, 2007
    Date of Patent: June 23, 2009
    Assignee: The Research Foundation of State University of New York
    Inventor: Huw M. L. Davies
  • Publication number: 20090105219
    Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, D2, E1, E2, E3, E4, E5, G1, G2, J, K, T, U, V, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Application
    Filed: November 14, 2006
    Publication date: April 23, 2009
    Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Steven N. Gallicchio, C. Blair Zartman, Harold G. Selnick
  • Publication number: 20080214511
    Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R5c, m and n are defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Application
    Filed: September 6, 2005
    Publication date: September 4, 2008
    Applicant: MERCK & CO., INC.
    Inventors: Ian M. Bell, Steven N. Gallicchiro, Craig A. Stump, Cory R. Theberge, Joseph P. Vacca, C. Blair Zartman, Xufang Zhang
  • Publication number: 20080161283
    Abstract: The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs).
    Type: Application
    Filed: August 10, 2005
    Publication date: July 3, 2008
    Applicant: CAMBRIDGE ENTERPRISE LIMITED
    Inventors: David J. Grainger, David John Fox
  • Patent number: 7393953
    Abstract: Polymeric derivatives of indoles such as are disclosed. Methods of making and using the same as well as related polymeric conjugates are also disclosed.
    Type: Grant
    Filed: March 31, 2003
    Date of Patent: July 1, 2008
    Assignee: Enzon, Inc.
    Inventors: Hong Zhao, Richard B. Greenwald
  • Patent number: 7365196
    Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: April 29, 2008
    Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.
    Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
  • Patent number: 7323562
    Abstract: This invention relates to a new and convergent route to small molecule inhibitors of poly(ADP-ribose) polymerase, such as 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, via a key Sonogashira coupling reaction and a CuI-promoted indole formation.
    Type: Grant
    Filed: September 21, 2005
    Date of Patent: January 29, 2008
    Assignees: Agouron Pharmaceuticals, Inc., Cancer Research Technology Ltd.
    Inventors: Chunrong Ma, Naresh Nayyar, Nebojsa Slobodan Stanković
  • Patent number: 7268126
    Abstract: The present invention relates to novel polymorphic and amorphous forms of a phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
    Type: Grant
    Filed: September 21, 2005
    Date of Patent: September 11, 2007
    Assignees: Agouron Pharmaceuticals, Inc., Cancer Research Technology Ltd.
    Inventors: Jia Liu, Naresh Nayyar, Ming Guo, Zhen-Ping Wu, Bennett Chaplin Borer, Aparna Nadig Srirangam, Mark Bryan Mitchell, Yi Li, Jan-Jon Chu
  • Patent number: 6977298
    Abstract: Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. As cancer therapeutics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation.
    Type: Grant
    Filed: December 3, 2004
    Date of Patent: December 20, 2005
    Assignees: Agouron Pharmacetucals, Inc., Cancer Research Campaign Technology Limited
    Inventors: Stephen Evan Webber, Stacie S. Canan-Koch, Jayashree Tikhe, Lars Henrik Thoresen
  • Patent number: 6958330
    Abstract: Disclosed are polycyclic ?-amino-?-caprolactams and related compounds which are useful as synthetic intermediates in the preparation of inhibitors of ?-amyloid peptide release and/or its synthesis.
    Type: Grant
    Filed: June 14, 2001
    Date of Patent: October 25, 2005
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly and Company
    Inventors: James E. Audia, Thomas E. Mabry, Jeffrey A. Nissen, Stacey L. McDaniel, Warren J. Porter
  • Publication number: 20040157826
    Abstract: The invention relates to novel heterocyclic compounds of general formula (I), and their salts with a base or an acid: 1
    Type: Application
    Filed: December 4, 2003
    Publication date: August 12, 2004
    Applicant: AVENTIS PHARMA S.A.
    Inventors: Maxime Lampilas, Branislav Musicki, Michel Klich, David Alan Rowlands
  • Patent number: 6630472
    Abstract: Compounds that inhibit the peptidyl-prolyl isomerase (rotamase) enzyme activity of the FK-506 binding protein (FKBP) and compositions comprising these compounds are described. The FKBP-inhibiting compounds have a bicyclic [3.3.1], [4.3.1] or polycyclic azaamide nucleus. Pharmaceutical compositions containing such compounds help stimulate the outgrowth of neurites in nerve cells and augmenting nerve regeneration. Methods of treating nerve cells with such compositions are useful to promote repair of neuronal damage caused by disease and physical trauma.
    Type: Grant
    Filed: July 16, 1999
    Date of Patent: October 7, 2003
    Assignee: Pfizer Inc
    Inventors: Susumu Katoh, Hiroshi Kawakami, Hiroki Tada, Maria Angelica Linton, Vincent Kalish, John Howard Tatlock, Jesus Ernesto Villafranca
  • Patent number: 6608175
    Abstract: Certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases, are prepared in various embodiments using Grignard reagents and alkyllithium reagents and various aldehydes to make oxadiazole, thiadiazole and triazole peptoid alcohols, which are then oxidized to the desired keto products.
    Type: Grant
    Filed: November 16, 2001
    Date of Patent: August 19, 2003
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Publication number: 20030153550
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Application
    Filed: October 7, 2002
    Publication date: August 14, 2003
    Inventors: James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
  • Publication number: 20030091505
    Abstract: The present invention provides compounds of Formula (I): 1
    Type: Application
    Filed: October 15, 2002
    Publication date: May 15, 2003
    Inventor: Jian-Min Fu
  • Publication number: 20030078254
    Abstract: Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease.
    Type: Application
    Filed: October 2, 2002
    Publication date: April 24, 2003
    Inventors: Stephen Evan Webber, Stacie S. Canan-Koch, Jayashree Tikhe, Lars Henrik Thoresen
  • Patent number: RE45288
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: December 9, 2014
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
  • Patent number: RE45325
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: January 6, 2015
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick