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)
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Patent number: 10669286Abstract: 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: GrantFiled: March 31, 2017Date of Patent: June 2, 2020Assignees: UCB Biopharma SRL, SanofiInventors: Michael Louis Robert Deligny, Jag Paul Heer
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Patent number: 9045487Abstract: 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: GrantFiled: May 8, 2014Date of Patent: June 2, 2015Assignee: PFIZER INC.Inventors: Patricia Ann Basford, Anthony Michael Campeta, Adam Gillmore, Matthew Cameron Jones, Eleftherios Kougoulos, Suman Luthra, Robert Walton
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Patent number: 8980879Abstract: 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: GrantFiled: March 11, 2014Date of Patent: March 17, 2015Assignee: AbbVie Inc.Inventors: Dachun Liu, John Pratt, Le Wang, Lisa A. Hasvold, Andrew Bogdan
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Publication number: 20150065703Abstract: 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: ApplicationFiled: August 22, 2014Publication date: March 5, 2015Applicant: Northwestern UniversityInventors: Karl A. Scheidt, Javier Izquierdo Ferrer
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Publication number: 20140275034Abstract: 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: ApplicationFiled: March 14, 2013Publication date: September 18, 2014Inventors: Kamlesh R. Chauhan, Bheema R. Paraselli
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Publication number: 20140256710Abstract: 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: ApplicationFiled: March 11, 2014Publication date: September 11, 2014Inventors: Dachun Liu, John Pratt, Le Wang, Lisa A. Hasvold, Andrew Bogdan
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Publication number: 20140243318Abstract: 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: ApplicationFiled: May 8, 2014Publication date: August 28, 2014Applicant: Pfizer Inc.Inventors: Patricia Ann Basford, Anthony Michael Campeta, Adam Gillmore, Matthew Cameron Jones, Eleftherios Kougoulos, Suman Luthra, Robert Walton
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Publication number: 20140228353Abstract: 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: ApplicationFiled: February 17, 2012Publication date: August 14, 2014Applicant: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvvajit Chakravarty
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Patent number: 8754072Abstract: 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: GrantFiled: February 10, 2011Date of Patent: June 17, 2014Assignee: Pfizer Inc.Inventors: Patricia Ann Basford, Anthony Michael Campeta, Adam Gillmore, Matthew Cameron Jones, Eleftherios Kougoulos, Suman Luthra, Robert Walton
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Patent number: 8710047Abstract: 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: GrantFiled: July 12, 2013Date of Patent: April 29, 2014Assignee: Albany Molecular Research, Inc.Inventors: David D. Manning, Christopher L. Cioffi
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Patent number: 8710046Abstract: 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: GrantFiled: June 30, 2010Date of Patent: April 29, 2014Assignee: Albany Molecular Research, Inc.Inventors: Peter R. Guzzo, David D. Manning, William Earley
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Patent number: 8691808Abstract: 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: GrantFiled: May 18, 2012Date of Patent: April 8, 2014Assignee: Influmedix, Inc.Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
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Publication number: 20130317007Abstract: 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: ApplicationFiled: April 11, 2013Publication date: November 28, 2013Applicant: Reata Pharmaceuticals, Inc.Inventors: Eric ANDERSON, Xin JIANG, Melean VISNICK
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Patent number: 8501729Abstract: 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: GrantFiled: February 14, 2012Date of Patent: August 6, 2013Assignee: Albany Molecular Research, Inc.Inventors: David D. Manning, Christopher Lawrence Cioffi
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Publication number: 20130144053Abstract: 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: ApplicationFiled: December 5, 2012Publication date: June 6, 2013Applicant: Mallinckrodt LLCInventor: Mallinckrodt LLC
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Patent number: 8440820Abstract: 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: GrantFiled: January 11, 2012Date of Patent: May 14, 2013Assignee: Reata Pharmaceuticals, Inc.Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
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Publication number: 20130053365Abstract: 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: ApplicationFiled: August 29, 2012Publication date: February 28, 2013Applicant: BioMarin Pharmaceutical, Inc.Inventors: Bing Wang, Daniel Chu
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Publication number: 20120295886Abstract: 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: ApplicationFiled: May 18, 2012Publication date: November 22, 2012Applicant: INFLUMEDIX, INC.Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
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Publication number: 20120270857Abstract: 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: ApplicationFiled: June 30, 2010Publication date: October 25, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. Guzzo, David D. Manning, William Earley
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Publication number: 20120271046Abstract: 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: ApplicationFiled: April 19, 2012Publication date: October 25, 2012Inventor: Christopher S. Jeffrey
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Publication number: 20120230951Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: March 8, 2012Publication date: September 13, 2012Inventors: Muzaffar Alam, Steven Joseph Berthel, John A. Brinkman, Ronald Charles Hawley, Hongju Li, Wylie Solang Palmer, Sherrie Pietranico-Cole, Ramakanth Sarabu, Mark Smith, Sung-Sau So, Lin Yi, Yansheng Zhai, Qiang Zhang, Shu-Hai Zhao
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Patent number: 8173802Abstract: 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: GrantFiled: October 10, 2007Date of Patent: May 8, 2012Assignee: Nippon Soda Co., Ltd.Inventors: Hirohito Oooka, Yasushi Shibata, Hiroki Inoue, Tsutomu Imagawa
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Patent number: 8124600Abstract: 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: GrantFiled: May 28, 2009Date of Patent: February 28, 2012Assignee: Albany Molecular Research, Inc.Inventors: David D. Manning, Christopher Lawrence Cioffi
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Publication number: 20110281845Abstract: The present disclosure relates to XIAP inhibitor compounds of the formula I.Type: ApplicationFiled: June 15, 2011Publication date: November 17, 2011Applicant: NOVARTIS AGInventors: Zhuoliang CHEN, Mark G. PALERMO, Sushil K. SHARMA, Troy SMITH, Christopher S. STRAUB, Run-Ming D. WANG, Yaping WANG, Leigh ZAWEL
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Patent number: 8008289Abstract: 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: GrantFiled: August 10, 2005Date of Patent: August 30, 2011Assignee: Cambridge Enterprise LimitedInventors: David J. Grainger, David John Fox
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Patent number: 8008288Abstract: 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: GrantFiled: August 10, 2005Date of Patent: August 30, 2011Assignee: Cambridge Enterprise LimitedInventors: David J. Grainger, David John Fox
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Patent number: 7947677Abstract: 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: GrantFiled: November 14, 2006Date of Patent: May 24, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Steven N. Gallicchio, C. Blair Zartman, Harold G. Selnick
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Patent number: 7915402Abstract: 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: GrantFiled: April 20, 2009Date of Patent: March 29, 2011Assignee: Reata Pharmaceuticals, Inc.Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
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Publication number: 20110053911Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.Type: ApplicationFiled: March 13, 2009Publication date: March 3, 2011Inventors: Raffaele Ingenito, Philip Jones, Laura Llauger Bufi, Jesus Maria Ontoria Ontoria, Rita Scarpelli
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Publication number: 20100093997Abstract: 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: ApplicationFiled: September 20, 2007Publication date: April 15, 2010Applicants: Pierre Fabre Medicament, COMMISSARIAT A L'ENERGIE ATOMIQUEInventors: Lionel Moisan, Sébastien Comesse, Emerson Giovanelli, Bernard Rousseau, Eric Doris, Paul Hellier
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Patent number: 7696192Abstract: 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: GrantFiled: September 6, 2005Date of Patent: April 13, 2010Assignee: 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
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Publication number: 20100056777Abstract: 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: ApplicationFiled: April 20, 2009Publication date: March 4, 2010Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
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Patent number: 7550588Abstract: Disclosed are novel homotropane compounds with CNS activity. These compounds can be used for alleviating symptoms of CNS disorders.Type: GrantFiled: March 12, 2007Date of Patent: June 23, 2009Assignee: The Research Foundation of State University of New YorkInventor: Huw M. L. Davies
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Publication number: 20090105219Abstract: 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: ApplicationFiled: November 14, 2006Publication date: April 23, 2009Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Steven N. Gallicchio, C. Blair Zartman, Harold G. Selnick
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Publication number: 20080214511Abstract: 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: ApplicationFiled: September 6, 2005Publication date: September 4, 2008Applicant: MERCK & CO., INC.Inventors: Ian M. Bell, Steven N. Gallicchiro, Craig A. Stump, Cory R. Theberge, Joseph P. Vacca, C. Blair Zartman, Xufang Zhang
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Publication number: 20080161283Abstract: 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: ApplicationFiled: August 10, 2005Publication date: July 3, 2008Applicant: CAMBRIDGE ENTERPRISE LIMITEDInventors: David J. Grainger, David John Fox
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Patent number: 7393953Abstract: 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: GrantFiled: March 31, 2003Date of Patent: July 1, 2008Assignee: Enzon, Inc.Inventors: Hong Zhao, Richard B. Greenwald
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Patent number: 7365196Abstract: 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: GrantFiled: March 15, 2001Date of Patent: April 29, 2008Assignees: 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
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Patent number: 7323562Abstract: 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: GrantFiled: September 21, 2005Date of Patent: January 29, 2008Assignees: Agouron Pharmaceuticals, Inc., Cancer Research Technology Ltd.Inventors: Chunrong Ma, Naresh Nayyar, Nebojsa Slobodan Stanković
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Patent number: 7268126Abstract: 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: GrantFiled: September 21, 2005Date of Patent: September 11, 2007Assignees: 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
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Patent number: 6977298Abstract: 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: GrantFiled: December 3, 2004Date of Patent: December 20, 2005Assignees: Agouron Pharmacetucals, Inc., Cancer Research Campaign Technology LimitedInventors: Stephen Evan Webber, Stacie S. Canan-Koch, Jayashree Tikhe, Lars Henrik Thoresen
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Patent number: 6958330Abstract: 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: GrantFiled: June 14, 2001Date of Patent: October 25, 2005Assignees: Elan Pharmaceuticals, Inc., Eli Lilly and CompanyInventors: James E. Audia, Thomas E. Mabry, Jeffrey A. Nissen, Stacey L. McDaniel, Warren J. Porter
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Publication number: 20040157826Abstract: The invention relates to novel heterocyclic compounds of general formula (I), and their salts with a base or an acid: 1Type: ApplicationFiled: December 4, 2003Publication date: August 12, 2004Applicant: AVENTIS PHARMA S.A.Inventors: Maxime Lampilas, Branislav Musicki, Michel Klich, David Alan Rowlands
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Patent number: 6630472Abstract: 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: GrantFiled: July 16, 1999Date of Patent: October 7, 2003Assignee: Pfizer IncInventors: Susumu Katoh, Hiroshi Kawakami, Hiroki Tada, Maria Angelica Linton, Vincent Kalish, John Howard Tatlock, Jesus Ernesto Villafranca
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Patent number: 6608175Abstract: 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: GrantFiled: November 16, 2001Date of Patent: August 19, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Publication number: 20030153550Abstract: 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: ApplicationFiled: October 7, 2002Publication date: August 14, 2003Inventors: James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
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Publication number: 20030091505Abstract: The present invention provides compounds of Formula (I): 1Type: ApplicationFiled: October 15, 2002Publication date: May 15, 2003Inventor: Jian-Min Fu
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Publication number: 20030078254Abstract: 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: ApplicationFiled: October 2, 2002Publication date: April 24, 2003Inventors: Stephen Evan Webber, Stacie S. Canan-Koch, Jayashree Tikhe, Lars Henrik Thoresen
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Patent number: RE45288Abstract: 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: GrantFiled: November 14, 2013Date of Patent: December 9, 2014Assignee: Reata Pharmaceuticals, Inc.Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
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Patent number: RE45325Abstract: 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: GrantFiled: November 14, 2013Date of Patent: January 6, 2015Assignee: Reata Pharmaceuticals, Inc.Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick