The Ring Nitrogen Is Bonded Directly To Two Ring Carbons Of The Same Cyclo Which Carbons Are Members Of One Cyclo Only (i.e., Isoindoles Or Isoindolenines) Patents (Class 548/470)
  • Patent number: 10385018
    Abstract: There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: October 23, 2013
    Date of Patent: August 20, 2019
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
  • Publication number: 20150111890
    Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof,that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: April 19, 2013
    Publication date: April 23, 2015
    Inventors: Lisa A. Hasvold, Dachun Liu, Chang Hoon Park, John K. Pratt, George S. Sheppard, Le Wang
  • Patent number: 8916552
    Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxyg
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: December 23, 2014
    Assignee: Astex Therapeutics Limited
    Inventors: Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
  • Patent number: 8877944
    Abstract: There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating, diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: July 6, 2010
    Date of Patent: November 4, 2014
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Gianluca Mariano Enrico Papeo, Alina Anatolievna Busel, Alexander Khvat, Mikhail Yurievitch Krasavin, Barbara Forte, Fabio Zuccotto
  • Patent number: 8859784
    Abstract: The present disclosure provides substantially enantiomerically pure heterobicyclic compounds of the following structural formulas, wherein A, M, M?, and R5 are as described herein, and to biocatalytic processes for their preparation, and to the enzymes used in those processes.
    Type: Grant
    Filed: November 11, 2011
    Date of Patent: October 14, 2014
    Assignee: Codexis, Inc.
    Inventors: Jack Liang, James Lalonde, Jun Zhu, John M. Gruber, John D. Munger, Jr.
  • Patent number: 8809543
    Abstract: An N-phenyl-diphenylisoindole derivative having the following formula (1): wherein each of R1 and R2 represents a hydrogen atom, a substituted or an unsubstituted alkyl group, a substituted or an unsubstituted alkoxy group, a substituted or an unsubstituted phenyl group, or a substituted or an unsubstituted phenoxy group; R3 represents a hydrogen atom, a substituted or an unsubstituted alkyl group, a substituted or an unsubstituted alkoxy group, a substituted or an unsubstituted phenyl group, a substituted or an unsubstituted phenoxy group, or has the following formula (2): wherein each of R4 and R5 represents a substituted or an unsubstituted alkyl group, or a substituted or an unsubstituted phenyl group; 1 represents an integer of from 1 to 4; and each of m and n represents an integer of from 1 to 5.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: August 19, 2014
    Assignee: Ricoh Company, Ltd.
    Inventors: Ryota Arai, Tomoyuki Shimada
  • Patent number: 8765972
    Abstract: There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: July 6, 2010
    Date of Patent: July 1, 2014
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Gianluca Mariano Enrico Papeo, Alina Anatolievna Busel, Elena Casale, Alexander Khvat, Mikhail Yurievitch Krasavin, Paolo Orsini, Helena Posteri, Alessandra Scolaro
  • Patent number: 8716326
    Abstract: The present invention relates to an amide compound or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition comprising the same. The inventive amide compound facilitates bone formation and inhibits bone loss, and is therefore useful for preventing and treating bone disorders such as osteoporosis, osteodystrophy, bone fracture, periodontal disease, Paget's disease, bone metastasis, and rheumatoid arthritis.
    Type: Grant
    Filed: May 14, 2010
    Date of Patent: May 6, 2014
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jung Nyoung Heo, Bum Tae Kim, Hyuk Lee, Sung Youn Chang, Zang Hee Lee, Seong Hwan Kim, Hyun-Mo Ryoo
  • Patent number: 8716527
    Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2- substituted-p-quinone derivatives as disclosed herein.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: May 6, 2014
    Assignee: Edison Pharmaceuticals, Inc.
    Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christopher R. Cornell
  • Publication number: 20130331568
    Abstract: The invention provides compounds of formula I wherein n, A, R, R?, R?, R0, X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.
    Type: Application
    Filed: August 15, 2013
    Publication date: December 12, 2013
    Applicant: Novartis AG
    Inventors: Fabrizio Gasparini, Yves Auberson, Silvio Ofner, Terance W. Hart, Kaspar Zimmermann
  • Patent number: 8598078
    Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: December 3, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
  • Publication number: 20130295141
    Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.
    Type: Application
    Filed: July 8, 2013
    Publication date: November 7, 2013
    Inventors: Viswajanani J. SATTIGERI, Venkata P. PALLE, Manoj Kumar KHERA, Ranadheer REDDY, Manoj Kumar TIWARI, Ajay SONI, Abdul Rehman Abdul RAUF, Sony JOSEPH, Arpita MUSIB, Sunanda G. DASTIDAR, Punit Kumar SRIVASTAVA
  • Publication number: 20130281450
    Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula I.
    Type: Application
    Filed: March 12, 2013
    Publication date: October 24, 2013
    Inventors: John K. Pratt, Dachun Liu, Chang H. Park, George S. Sheppard, Lisa A. Hasvold, Le Wang
  • Patent number: 8541450
    Abstract: The invention relates to enantiomerically pure 3-(phthalimido)piperidines and processes for preparing enantiomerically pure 3-(phthalimido)piperidines.
    Type: Grant
    Filed: March 30, 2009
    Date of Patent: September 24, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Thorsten Pachur
  • Patent number: 8536221
    Abstract: The invention relates to novel amide derivatives that are PAMs of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: September 17, 2013
    Assignee: AbbVie Inc.
    Inventors: Kathleen H. Mortell, Diana L. Nersesian, Michael R. Schrimpf, Chih-Hung Lee, Murali Gopalakrishnan
  • Patent number: 8530469
    Abstract: The invention provides a combination comprising an Hsp90 inhibitor compound of the formula (VII): or tautomer or salt thereof and one or more therapeutic agents selected from topoisomerase I inhibitors; antimetabolites; tubulin targeting agents; DNA binder and topoisomerase II inhibitors; alkylating agents; monoclonal antibodies; anti-hormones; signal transduction inhibitors; proteasome inhibitors; DNA methyl transferases; cytokines; retinoids and HDAC or HAT modulators.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: September 10, 2013
    Assignee: Astex Therapeutics Ltd.
    Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford, Maria Grazia Carr, Robert Downham, Michael Alistair O'Brien, Theresa Rachel Phillips, Andrew James Woodhead
  • Patent number: 8481753
    Abstract: A method for manufacturing isoindolic compound, which can adopt a condition capable of being put to industrially practical use, which can produce stable isoindolic compound, and which can further produce the isoindolic compound with a high yield. The method for manufacturing isoindolic compound includes a thermal treatment step where a compound of which molecule includes a structure of pyrrole fused with bicyclo [2.2.2] octadiene skeleton, and includes a formula (I): is subjected to a supercritical carbon dioxide atmosphere. The thermal treatment step is preferably performed at a temperature of not less than 50° C. and not more than 300° C.
    Type: Grant
    Filed: December 24, 2008
    Date of Patent: July 9, 2013
    Assignee: Utsunomiya University
    Inventors: Satoshi Ito, Naotsugu Itoh, Takafumi Sato
  • Patent number: 8426609
    Abstract: A method for preparing a functionalized polymer, the method comprising the steps of preparing a reactive polymer and reacting the reactive polymer with an imide compound containing a protected amino group.
    Type: Grant
    Filed: February 22, 2011
    Date of Patent: April 23, 2013
    Assignee: Bridgestone Corporation
    Inventor: Steven Luo
  • Patent number: 8372988
    Abstract: The present invention relates to crystalline forms of [3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethylamine (“COMPOUND I”) useful in the treatment of RAGE mediated diseases.
    Type: Grant
    Filed: December 30, 2010
    Date of Patent: February 12, 2013
    Assignee: TransTech Pharma, Inc.
    Inventor: Anitha Hari
  • Patent number: 8314255
    Abstract: Preparation and use of phthalimide and/or sulphonamide derivatives with nitric oxide donor properties, having activities in increasing gamma-globin gene expression and anti-inflammatory and analgesic activities, effective in the treatment of hematologic diseases which require reducing the TNF-? levels and an exogenous source of nitric oxide, such as sickle-cell disease. The functionalized phthalimide derivatives are designed from the prototypes thalidomide and hydroxyurea.
    Type: Grant
    Filed: February 24, 2012
    Date of Patent: November 20, 2012
    Inventors: Jean Leandro Dos Santos, Chin Chung Man, Lidia Moreira Lima, Fernando Ferreira Costa, Carolina Lanaro
  • Publication number: 20120157690
    Abstract: Preparation and use of phthalimide and/or sulphonamide derivatives with nitric oxide donor properties, having activities in increasing gamma-globin gene expression and anti-inflammatory and analgesic activities, effective in the treatment of hematologic diseases which require reducing the TNF-? levels and an exogenous source of nitric oxide, such as sickle-cell disease. The functionalized phthalimide derivatives are designed from the prototypes thalidomide and hydroxyurea.
    Type: Application
    Filed: February 24, 2012
    Publication date: June 21, 2012
    Applicants: UNIVERSIDADE ESTADUAL DE CAMPINAS - UNICAMP, UNIVERSIDADE ESTADUAL PAULISTA <<JULIO DE MESQUITA FILHO >> - UNESP, UNIVERSIDADE FEDERAL DO RIO DE JANEIRO - UFRJ
    Inventors: Jean Leandro DOS SANTOS, Chin CHUNG MAN, Lídia MOREIRA LIMA, Fernando FERREIRA COSTA, Carolina LANARO
  • Patent number: 8188139
    Abstract: The present invention relates to compounds of formula I wherein R1, R2, and are defined in the specification and to pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: April 13, 2009
    Date of Patent: May 29, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
  • Patent number: 8183279
    Abstract: Novel 1,3-dihydroisoindole derivatives of the formula (I), in which R1-R3 have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: July 28, 2008
    Date of Patent: May 22, 2012
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Hans Michael Eggenweiler, Christian Sirrenberg, Hans Peter Buchstaller
  • Patent number: 8158672
    Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.
    Type: Grant
    Filed: January 20, 2011
    Date of Patent: April 17, 2012
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man, Weihong Zhang
  • Publication number: 20120088790
    Abstract: The present invention relates to phenalkylamine derivatives of the formula (I) or (II) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: August 10, 2011
    Publication date: April 12, 2012
    Applicants: Abbott GmbH & Co. KG, Abbott Laboratories
    Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins, Wilfried Hornberger, Mario Mezler
  • Patent number: 8153679
    Abstract: The present invention relates to novel radiolabelled inhibitors of formula I for the Glycine 1 transporter (GlyT1), useful for the labelling and diagnostic imaging of the glycine 1 transporter functionality. wherein R1 is isopropoxy or 2,2,2-trifluoro-1-methyl-ethoxy; and R2 is a radiolabelled group CH3, wherein the radionuclide is 3H or 11C. The radiolabelled compounds of formula I may be used as PET (Positron Emission Tomography) radiotracer for the labelling and diagnostic molecular imaging of the glycine 1 transporter functionality.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: April 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniela Alberati, Edilio Maurizio Borroni, Thomas Hartung, Roger David Norcross, Emmanuel Pinard
  • Patent number: 8133914
    Abstract: The invention relates to novel compounds containing a carboxylic acid head group. The invention further provides compositions containing the novel compounds, a particulate solid and an organic medium or water.
    Type: Grant
    Filed: September 7, 2007
    Date of Patent: March 13, 2012
    Assignee: Lubrizol Limited
    Inventor: Dean Thetford
  • Patent number: 8101648
    Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydrogen; R2 is hydroxy or methoxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.
    Type: Grant
    Filed: April 13, 2006
    Date of Patent: January 24, 2012
    Assignee: Astex Therapeutics, Ltd.
    Inventors: Gianni Chessari, Miles Stuart Congreve, Eva Figueroa Navarro, Martyn Frederickson, Christopher Murray, Alison Jo-Anne Woolford, Maria Grazia Carr, Michael Alistair O'Brien, Andrew James Woodhead, Robert Downham, Theresa Rachel Phillips
  • Patent number: 8071787
    Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, X, Y, and Z are as defined herein. Also disclosed is a method for inhibiting actively of fibroblast activation protein or for treating cancer or inflammation conditions with such a compound.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: December 6, 2011
    Assignee: National Health Research Institutes
    Inventors: Weir-Tong Jiaang, Xin Chen
  • Patent number: 8026360
    Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, W, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: September 27, 2011
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Rajender Kamboj, Zaihui Zhang, Jianmin Fu, Vandna Raina, Serguei Sviridov, Vishnumurthy Kodumuru, Nagasree Chakka, Shifeng Lui, Shaoyi Sun, Duanjie Hou
  • Patent number: 8026269
    Abstract: The invention encompasses isoindoline compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.
    Type: Grant
    Filed: February 9, 2009
    Date of Patent: September 27, 2011
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man
  • Publication number: 20110224443
    Abstract: Process for preparation of fosamprenavir and its intermediate salts using novel phthalimide intermediates.
    Type: Application
    Filed: March 14, 2011
    Publication date: September 15, 2011
    Inventors: Venkata Naga Brahmeshwara Rao Mandava, Praveen Cherukupally, Ganesh Varanasi, Srinivas Areveli, Chandra Sekhar Vempati, Ramakrishna Reddy Narayana, Sreenadha Charyulu Kandala
  • Patent number: 8013171
    Abstract: To provide an axially asymmetric optically active biaryl ester compound that can easily produced without the step of optical resolution which was almost indispensable in conventional methods. There is provided a method for producing an axially asymmetric ester compound, comprising a cycloaddition of a compound having a triple bond with the use of a catalyst containing rhodium metal and an optically active bisphosphine.
    Type: Grant
    Filed: June 1, 2009
    Date of Patent: September 6, 2011
    Assignees: National University Corporation Tokyo University of Agriculture and Technology, Takasago International Corporation
    Inventor: Ken Tanaka
  • Patent number: 8012983
    Abstract: Novel [1.2.4]triazolo[1,5-a]pyrazine and imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, and others.
    Type: Grant
    Filed: May 6, 2009
    Date of Patent: September 6, 2011
    Assignee: Galapagos NV
    Inventors: Martin James Inglis Andrews, Mark Stuart Chambers, Hervé Van De Poël, Grégory Louis Joseph Bar
  • Publication number: 20110137024
    Abstract: Disclosed is a method for manufacturing isoindolic compound, which can adopt a condition capable of being put to industrially practical use, which can produce stable isoindolic compound, and which can further produce the isoindolic compound with a high yield. The method for manufacturing isoindolic compound comprises a thermal treatment step where a compound of which molecule includes a structure of pyrrole fused with bicyclo [2.2.2] octadiene skeleton is subjected to a supercritical carbon dioxide atmosphere. The thermal treatment step is preferably performed at a temperature of not less than 50° C. and not more than 300° C.
    Type: Application
    Filed: December 24, 2008
    Publication date: June 9, 2011
    Inventors: Satoshi Ito, Naotsugu Itoh, Takafumi Sato
  • Patent number: 7956185
    Abstract: Compounds of formula (I) where X1, C1, and D1 are defined herein, are inhibitors of polo-like kinases. The compounds of formula (I) are useful for treatment of diseases of cellular proliferation, such as, for example, cancer.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: June 7, 2011
    Assignee: Abbott Laboratories
    Inventors: Robert B. Diebold, Stevan W. Djuric, Vincent L. Giranda, Laura A. Hexamer, Nan-Horng Lin, Julie M. Miyashiro, Thomas D. Penning, Magdalena Przytulinska, Thomas J. Sowin, Gerard M. Sullivan, Zhi-Fu Tao, Yunsong Tong, Anil Vasudevan, Le Wang, Keith W. Woods, Zhiren Xia, Henry Q. Zhang
  • Publication number: 20110124679
    Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-substituted-p-quinone derivatives as disclosed herein.
    Type: Application
    Filed: March 4, 2009
    Publication date: May 26, 2011
    Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christpher R. Cornell
  • Patent number: 7943657
    Abstract: Imidoalkancarboxylic acids of formula: are described, wherein A, X and M are as defined in the application, said acids being in a crystalline form which in contact with water gives rise to crystals having sizes lower than 30 micron.
    Type: Grant
    Filed: February 29, 2008
    Date of Patent: May 17, 2011
    Assignee: Solvay Solexis S.p.A.
    Inventors: Ugo Piero Bianchi, Roberto Garaffa
  • Patent number: 7935777
    Abstract: Polycarbonate compositions are disclosed. The compositions comprise a polycarbonate polymer (A) having repeating units derived from 2-phenyl-3,3-bis(4-hydroxyphenyl)phthalimidine (PPPBP); a polycarbonate polymer (B) which is different from polymer (A); an impact modifier (C) which is different from polymer (A) and polymer (B); and talc filler (D). The resulting composition has an improved combination of properties, particularly heat resistance, low temperature impact performance, and viscosity.
    Type: Grant
    Filed: June 23, 2008
    Date of Patent: May 3, 2011
    Assignee: Sabic Innovative Plastics IP B.V.
    Inventors: Kees de Kraker, Andries Adriaan Volkers
  • Patent number: 7893102
    Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.
    Type: Grant
    Filed: January 30, 2009
    Date of Patent: February 22, 2011
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man, Weihong Zhang
  • Patent number: 7884219
    Abstract: The present invention relates to crystalline forms of [3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethylamine (“COMPOUND I”) useful in the treatment of RAGE mediated diseases.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: February 8, 2011
    Assignee: TransTech Pharma, Inc.
    Inventor: Anitha Hari
  • Patent number: 7879876
    Abstract: The present invention is related to sulfonamide derivatives of Formula (Ia) where the groups are as defined in the description, and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: February 1, 2011
    Assignee: Merck Serono SA
    Inventors: Patrick Gerber, Dominique Swinnen, Agnes Bombrun
  • Publication number: 20100324046
    Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: June 24, 2008
    Publication date: December 23, 2010
    Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
  • Patent number: 7847107
    Abstract: The present invention is to provide a novel method for producing (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid which is useful as a therapeutic agent for diabetes. The present invention relates to a method for producing (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid, which is characterized in that 2-benzylidene-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid is subjected to a catalytic reduction reaction in the presence of an asymmetric catalyst prepared from a pyrrolidinebisphosphine compound (I) represented by the following general formula (I): wherein, R1 represents a linear or branched alkyl group having 1-10 carbon atoms, cycloalkyl group, aralkyl group or aryl group which may respectively have a substituent; and R2 and R3 independently represent an optionally substituted aryl group. The * mark in the pyrrolidine ring shows that the carbon atom at that position has the S configuration, and a rhodium compound.
    Type: Grant
    Filed: December 26, 2006
    Date of Patent: December 7, 2010
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Yoshinori Matsumoto, Yuki Takeuchi, Hiroyuki Yamamoto
  • Publication number: 20100256114
    Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
    Type: Application
    Filed: June 17, 2010
    Publication date: October 7, 2010
    Applicant: INCYTE CORPORATION
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
  • Patent number: 7799806
    Abstract: This invention relates to compounds of the formula wherein A, R1 to R3 are as defined in the claims and G is benzoimidazole, quinoxaline, benzotriazole, dihydro-imidazo[4,5-c]pyridinone and dihydro-isoindolone group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5 such as diabetes mellitus.
    Type: Grant
    Filed: March 24, 2008
    Date of Patent: September 21, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Andreas D. Christ, Rainer E. Martin, Peter Mohr
  • Publication number: 20100179145
    Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxyg
    Type: Application
    Filed: October 12, 2007
    Publication date: July 15, 2010
    Inventors: Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
  • Publication number: 20100126378
    Abstract: A sulfonated derivative of an organic pigment moiety comprising a polyetheramine, and a metal or ammonium salt. The pigment is used for coloration of printing inks and coatings. For ink-jet systems there is excellent filterability, low viscosity, and stability thereof.
    Type: Application
    Filed: April 3, 2008
    Publication date: May 27, 2010
    Inventor: Stanislav Vilner
  • Patent number: 7678825
    Abstract: Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with an ?-(3,4-disubstituted phenyl)alkyl group and in the 4- and/or 5-position with a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNF? and phosphodiesterase. A typical embodiment is 2-[1-(3-ethoxy-4-methoxyphenyl)2-methylsulfonylethyl]4,5-diaminoisoindoline-1,3-dione.
    Type: Grant
    Filed: May 12, 2008
    Date of Patent: March 16, 2010
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, George W Muller
  • Publication number: 20100041866
    Abstract: A compound which can be attached to a solid support and used as a reagent for methods of solid phase synthesis has the following structure: (I) where Ri is selected from hydrogen and C1-C6 alkyl; R2 is selected from hydrogen, hydroxy, and C1-C6 alkoxy, or together R1 and R2 form a single bond; R3, R4, R5 and R6 are the same or different from each other and each represents hydrogen, C1-C6 alkyl, and halogen, or together R3 and R4 with R5 and R6 form an aromatic ring, further wherein the aromatic ring is substituted with one or more X; X is selected from halogen, nitro, amino, and aminocarbonyl; s is 0, 1, 2, or 3, t is 0, 1, 2, or 3, wherein s+t?1; R7 and R8 are the same or different from each other and each represents hydroxy, halogen, hydrogen, C1-C6 alkoxy, oxyacyl, or together R7 and R8 form a carbonyl; Y is selected from a methylene or substituted methylene, nucleoside, nucleotide, protected nucleoside, protected nucleotide, C1-C6 aryl, arylalkyl, heteroalkyl, heterocycle, and heteroaryl; n is 1, 2, 3, 4,
    Type: Application
    Filed: March 26, 2007
    Publication date: February 18, 2010
    Applicant: ARCHEMIX CORP.
    Inventors: Paul J. Hatala, Markus Kurz