Unsaturated Carbocyclic Ring Attached Indirectly To The Six-membered Hetero Ring Through An Acyclic Hydrocarbon Chain Patents (Class 546/149)
  • Publication number: 20150133427
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: October 15, 2014
    Publication date: May 14, 2015
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
  • Patent number: 8957089
    Abstract: The present invention relates to tetrahydroisoquinoline of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are GlyT1 inhibitors.
    Type: Grant
    Filed: March 10, 2013
    Date of Patent: February 17, 2015
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Wilfried Braje, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles Hutchins
  • Publication number: 20140296286
    Abstract: Disclosed are compounds for the treatment of cancer. Compounds disclosed herein are particularly effective for the selective inhibition of glioma cells.
    Type: Application
    Filed: March 25, 2014
    Publication date: October 2, 2014
    Applicant: University of Tennessee Research Foundation
    Inventors: Duane D. Miller, Shivaputra Appanna Patil, Renukadevi Patil, Terreia Jones, Amira Ahmed, Likeselam Asres, Charles Ryan Yates, Eldon Geisert
  • Publication number: 20140249180
    Abstract: A tau aggregation inhibitor reduces tau aggregation in cells. The tau aggregation inhibitor can include a catechol structure-containing compound or a salt thereof, and the catechol structure-containing compound can be one of isoprenaline, dopamine, dobutamine, levodopa, levodopa/carbidopa, trimetoquinol, hexoprenaline, methyldopa, and droxidopa. One example of the catechol structure-containing compound is isoprenaline, which can be d-enantiomer of isoprenaline or d/l-racemic mixture of isoprenaline. Tauopathies to be prevented or treated by the inhibitor include AD, Down's syndrome, Pick's disease, corticobasal degeneration, and progressive supranuclear palsy.
    Type: Application
    Filed: October 3, 2012
    Publication date: September 4, 2014
    Applicants: National Center for Geriatrics and Gerontology, THE DOSHISHA
    Inventors: Akihiko Takashima, Yoshiyuki Soeda, Hiroyuki Nagata, Yasuo Ihara, Tomohiro Miyasaka, Hachiro Sugimoto
  • Publication number: 20140243524
    Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle opti
    Type: Application
    Filed: May 2, 2014
    Publication date: August 28, 2014
    Applicants: Albany Molecular Research, Inc., Bristol-Myers Squibb Company
    Inventors: Bruce F. Molino, Shuang Liu, Peter R. Guzzo, James P. Beck
  • Publication number: 20140228343
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: August 14, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
  • Patent number: 8785449
    Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: September 18, 2012
    Date of Patent: July 22, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
  • Publication number: 20140088069
    Abstract: An antibacterial composition is provided including a combination of a ?-lactam antibiotic that has a binding affinity for bacterial penicillin-binding protein 2; and a non-antibiotic compound which may be a thienopyridine or a non-thienopyridine compound. A method of treatment using the composition is also provided.
    Type: Application
    Filed: November 29, 2013
    Publication date: March 27, 2014
    Inventors: Eric D. Brown, Maya Farha, Alexander Leung, Gerry Wright, Kalinka Koteva, Ted Sewell, Linda Ejim
  • Patent number: 8680159
    Abstract: Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: March 25, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Melanie Reich, Stefan Schunk, Ruth Jostock, Jean De Vry, Christa Kneip, Tieno Germann, Michael Engels
  • Publication number: 20140039181
    Abstract: The invention relates to a method for producing a N-substituted amine compound by catalyzed alkylation. The method uses amine and alcohol or two kinds of amines as the reaction materials, employs composite metal oxides catalyst at a reaction temperature of 80-180° C. to catalyze the reaction for 6-36 hours, so as to produce the N-substituted amine compound. The reaction condition of the method of the invention is relatively moderate, using a catalyst made of cheap non-noble metals, which is non-caustic and easy to be separated and reused. The reaction does not need any medium and has relatively high conversion rate and selectivity.
    Type: Application
    Filed: December 28, 2012
    Publication date: February 6, 2014
    Applicant: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
    Inventor: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
  • Patent number: 8592451
    Abstract: The invention provides neuromuscular blockade agents of the non-depolarizing type with few if any circulatory effects. Compounds of the invention include bis(isoquinolylalkanol) diesters of fumaric, maleic, succinic, and acetylenedicarboxylic acids; compositions suitable for parenteral administration of these compounds as a surgical adjunct to anesthesia, and methods of preparation of the compounds. Compounds of the invention can produce neuromuscular blockade of short or intermediate duration, which for various compounds can be reversed by administration of a thiol compound such as L-cysteine, D-cysteine or glutathione. For various compounds of the invention, the neuromuscular blockade effect can be reversed quickly, efficiently, and without notable side-effects.
    Type: Grant
    Filed: March 17, 2010
    Date of Patent: November 26, 2013
    Assignee: Cornell University
    Inventor: John J. Savarese
  • Publication number: 20130310555
    Abstract: Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
    Type: Application
    Filed: May 17, 2013
    Publication date: November 21, 2013
    Applicant: Illinois Institute of Technology
    Inventor: Hyun-Soon Chong
  • Patent number: 8552028
    Abstract: A compound is provided.
    Type: Grant
    Filed: September 5, 2011
    Date of Patent: October 8, 2013
    Assignee: National Taiwan University
    Inventors: Ming-Jai Su, Ling-Wei Hsin
  • Publication number: 20130203749
    Abstract: The present invention relates to tetrahydroisoquinoline of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are GlyT1 inhibitors.
    Type: Application
    Filed: March 10, 2013
    Publication date: August 8, 2013
    Applicants: ABBVIE INC., ABBVIE DEUTSCHLAND GMBH & CO. KG
    Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Wilfried Braje, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles Hutchins
  • Publication number: 20130131018
    Abstract: The present invention relates generally to substituted isoquinolines and their use as tubulin polymerization inhibitors. In particular, the invention relates to substituted isoquinolines which possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.
    Type: Application
    Filed: June 1, 2011
    Publication date: May 23, 2013
    Applicant: Exonhit S.A.
    Inventors: Bertrand Leblond, Thierry Taverne, Eric Beausoleil, Cédric Chauvignac, Anne-Sophie Casagrande, Laurent Desire
  • Publication number: 20130123299
    Abstract: Small molecule compounds are provided for treating lupus as are methods of treating lupus using these compounds.
    Type: Application
    Filed: May 6, 2011
    Publication date: May 16, 2013
    Applicant: The Feinstein Institute for Medical Research
    Inventors: Yousef Al-Abed, Betty A. Diamond
  • Patent number: 8431705
    Abstract: The present invention provides an efficient process for the preparation of hexahydroisoquinolines from amides. In particular, the invention provides a good yielding, one-pot process for the synthesis of hexahydroisoquinolines.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: April 30, 2013
    Assignee: Mallinckrodt LLC
    Inventors: Christopher W. Grote, Frank W. Moser, Peter X. Wang, Gary L. Cantrell, David W. Berberich
  • Publication number: 20130059882
    Abstract: A compound is provided.
    Type: Application
    Filed: September 5, 2011
    Publication date: March 7, 2013
    Applicant: NATIONAL TAIWAN UNIVERSITY
    Inventors: MING-JAI SU, LING-WEI HSIN
  • Publication number: 20120323003
    Abstract: The disclosure relates to tetrahydroisoquinoline sulfonamide compounds of formula I: wherein R1, R2, n and B are as defined in the disclosure, their preparation and their use in therapies for the treatment of central nervous system diseases such as vigilance and sleep disorders, narcolepsy, Alzheimer's disease and other dementias, Parkinson's disease, attention disorders in hyperkinetic children, memory and learning disorders, epilepsy, schizophrenia, moderate cognitive disorders, depression, anxiety, sexual dysfunction, dizziness and travel sickness.
    Type: Application
    Filed: August 24, 2012
    Publication date: December 20, 2012
    Applicant: SANOFI
    Inventors: Juan Antonio DIAZ MARTIN, Maria Dolores JIMENEZ BARGUENO
  • Patent number: 8314238
    Abstract: The present invention relates to a process for the preparation of the compound of formula (7) which process comprises the hydrogenation of the compound of formula (4) using bis[chloro-1,5-cyclooctadiene-iridium], (S)-i-dicyclohexylphosphino-2-[(S)-?-(dimethylamino)-2-(dicyclohexylphosphino)benzyl]-ferrocene as a catalyst.
    Type: Grant
    Filed: December 23, 2008
    Date of Patent: November 20, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Erhard Bappert, Andreas Hendrikus Maria De Vries, Doris Domin, Matthias Helms, Christoph Imboden, Zarghun Nazir, Wolfgang Skranc, Felix Spindler, Michael Stanek, Wilhelm Tschebull, Gerardus Karel Maria Verzijl
  • Patent number: 8314107
    Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: April 22, 2009
    Date of Patent: November 20, 2012
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
  • Patent number: 8273766
    Abstract: The present invention relates a specific tetrahydroisoquinoline compound which is useful as a chemokine receptor type 3 (CCR3) antagonist, and a pharmaceutical composition comprising the same as an active ingredient. The tetrahydroisoquinoline compound of the present invention is useful for the treatment or prevention of a disease in which CCR3 participates.
    Type: Grant
    Filed: April 3, 2008
    Date of Patent: September 25, 2012
    Assignee: Kowa Company, Ltd.
    Inventors: Seiichi Sato, Junya Tagashira, Shunji Takemura, Yoshiharu Miyake, Tetsuya Ishikawa, Toshiharu Arai, Takahiro Ito, Takuya Hara
  • Patent number: 8273767
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: September 25, 2012
    Assignee: Abbott Laboratories
    Inventors: Robert J. Altenbach, Lawrence A. Black, Sou-Jen Chang, Marlon D. Cowart, Ramin Faghih, Gregory A. Gfesser, Yi-Yin Ku, Huaqing Liu, Kirill A. Lukin, Diana L. Nersesian, Yu-ming Pu, Padam N. Sharma, Youssef L. Bennani, Michael P. Curtis
  • Patent number: 8247560
    Abstract: The present invention relates to the compound of formula 7*acetate (see below), a process for its preparation, and its use
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: August 21, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Maria Andreas Hendrikus De Vries, Doris Domin, Matthias Helms, Christoph Imboden, Ralph Koberstein, Zarghun Nazir, Wolfgang Skranc, Michael Stanek, Wilhelm Tschebull, Maria Gerardus Karel Verzijl, Jurgen Stichler
  • Patent number: 8242277
    Abstract: The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate.
    Type: Grant
    Filed: December 10, 2007
    Date of Patent: August 14, 2012
    Assignee: Mallinckrodt LLC
    Inventors: Gary L. Cantrell, Dan P. Magparangalan, Frank W. Moser, Jian Bao, Christopher W. Grote, Peter X. Wang
  • Patent number: 8232400
    Abstract: The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl3 that is necessary to form the 3,4-dihydroisoquinoline.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: July 31, 2012
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Frank W. Moser, Christopher W. Grote, Gary L. Cantrell
  • Patent number: 8232399
    Abstract: A novel class of chiral ligands represented by a structure of Formula I: wherein R1, R2, R3, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy, C(O)R6, C(O)NHR6, Si(R6)3, benzyl and aryl; X is selected from the group consisting of OH, OR7, O-Prot and P(R7)2 where Prot represents a protecting group; and R6 and R7 are selected from the group consisting of hydrogen, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy, phenyl, and aryl is disclosed herein.
    Type: Grant
    Filed: March 2, 2007
    Date of Patent: July 31, 2012
    Inventors: Chao-Jun Li, Patricia MacLeod, Zhiping Li, Jianqing Feng
  • Patent number: 8227611
    Abstract: The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: July 24, 2012
    Assignee: Mallinckrodt LLC
    Inventors: Gary L. Cantrell, Dan P. Magparangalan, Frank W. Moser, Jian Bao, Christopher W. Grote, Peter X. Wang
  • Patent number: 8183378
    Abstract: Novel chemical agents are described herein. More a ligand of general Formula I: wherein R1, R2, R3 and R4, are independently selected from the group consisting of hydrogen, halogen, hydroxy, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C1-C10 alkoxy, C1-C10 alkylthio, C(O)R5, C(O)OR5, C(O)NHR5, Si(R5)3, benzyl and aryl; X is selected from the group consisting of Cl, Br, I, OR6, O-Prot, OPR6, P(R6)2, NHR6, N(R6)2, NHCSNHR6, NHCONHR6 and SR6; and R5 and R6 are independently selected from the group consisting of hydrogen, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy, phenyl, and aryl. These ligands are useful in asymmetric reactions as well as in asymmetric synthesis of molecules of biological interest.
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: May 22, 2012
    Inventors: Chao-Jun Li, Jianqing Feng
  • Patent number: 8163921
    Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: April 24, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ny Sin, Brian Lee Venables, Paul Michael Scola, Alan Xiangdong Wang
  • 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
  • Publication number: 20120059032
    Abstract: Disclosed are tetrahydroisoquinoline-derivative compounds effective for killing cancer cells, shrinking tumor size, and treating cancer.
    Type: Application
    Filed: March 7, 2011
    Publication date: March 8, 2012
    Applicant: University of Tennessee Research Foundation
    Inventors: Renukadevi Patil, Shivaputra A. Patil, Duane D. Miller, Charles Ryan Yates, Eldon E. Geisert
  • Patent number: 8115002
    Abstract: The present invention is directed to processes for the synthesis of morphinan-6-ones and salts, intermediates, and analogs thereof.
    Type: Grant
    Filed: September 6, 2007
    Date of Patent: February 14, 2012
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Frank W. Moser, Gary L. Cantrell, Christopher W. Grote
  • Publication number: 20110201816
    Abstract: The present inventors succeeded in isolating GWT1 (PfGWT1), which is one of the enzymes involved in GPI biosynthesis in the malaria parasite P. falciparum. In addition, the inventors revealed that degenerate mutant DNAs, with a lower AT content than the DNA encoding the PfGWT1 protein, can complement the phenotype of GWT1-deficient yeast. Based on the findings, the present invention provides the GWT1 protein of malaria parasites and the use of the protein in methods of screening for antimalarial drugs. The present invention also provides degenerate mutant DNAs encoding proteins involved in GPI biosynthesis, and which have a lower AT content than the original DNAs. The present invention also provides methods of screening for antimalarial drugs which use the degenerate mutant DNAs.
    Type: Application
    Filed: March 4, 2011
    Publication date: August 18, 2011
    Applicant: EISAI R&D MANAGEMENT CO., LTD
    Inventors: Katsura Hata, Kaoru Ogawa, Itaru Tsukada, Kazutaka Nakamoto, Koji Sagane, Keigo Tanaka, Kappei Tsukahara, Toshihiro Horii
  • Publication number: 20110195978
    Abstract: Described herein are compounds, and pharmaceutical compositions, methods, and uses thereof for treating Alzheimer's disease.
    Type: Application
    Filed: October 9, 2009
    Publication date: August 11, 2011
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventor: Arun K. Ghosh
  • Publication number: 20110136845
    Abstract: The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as methods for using the (+)-morphinans to treat pain. Also provided are pharmaceutical combination compositions comprising a (+)-morphinan and an opioid agonist/monoamine reuptake inhibitor, as well as methods for using the combination compositions to treat pain.
    Type: Application
    Filed: December 22, 2010
    Publication date: June 9, 2011
    Applicant: Mallinckrodt Inc.
    Inventors: Bobby N. Trawick, David W. Berberich, Christopher W. Grote
  • Patent number: 7906655
    Abstract: The present disclosure relates to 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: Grant
    Filed: August 5, 2009
    Date of Patent: March 15, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Makonen Belema, Andrew C. Good, Jason Goodrich, Ramesh Kakarla, Guo Li, Omar D. Lopez, Van N. Nguyen, Jayne Kapur, Yuping Qiu, Jeffrey Lee Romine, Denis R. St. Laurent, Michael Serrano-Wu, Lawrence B. Snyder, Fukang Yang
  • Patent number: 7902218
    Abstract: There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: March 8, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lorin A. Thompson, III, Kenneth M. Boy, Jianliang Shi, John E. Macor, Andrew C. Good, Lawrence R. Marcin
  • Publication number: 20100305325
    Abstract: The present invention relates to a process for the preparation of the compound of formula (7) which process comprises the hydrogenation of the compound of formula (4) using bis[chloro-1,5-cyclooctadiene-iridium], (S)-i-dicyclohexylphosphino-2-[(S)-?-(dimethylamino)-2-(dicyclohexylphosphino)benzyl]-ferrocene as a catalyst.
    Type: Application
    Filed: December 23, 2008
    Publication date: December 2, 2010
    Inventors: Erhard Bappert, Andreas Hendrikus Maria De Vries, Doris Domin, Matthias Helms, Christoph Imboden, Zarghun Nazir, Wolfgang Skranc, Felix Spindler, Michael Stanek, Wilhelm Tschebull, Gerardus Karel Maria Verzijl
  • Publication number: 20100298570
    Abstract: A process for the resolution of racemic tetrahydropapaverine with optically active arylpropionic acids is described.
    Type: Application
    Filed: February 25, 2009
    Publication date: November 25, 2010
    Applicant: RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.P.A.
    Inventors: Franca Segnalini, Angela Tuozzi, Angelo Gentile
  • Patent number: 7838677
    Abstract: The present invention is directed to processes for the synthesis of morphinans. In particular, a process for cyclizing a ?,?-bicyclic ketone compound to form a nordihydrothebainone product using the Grewe cyclization reaction is improved by forming a reaction mixture comprising a ?,?-bicyclic ketone compound, a cyclizing acid and a water scavenging cyclization additive. In one embodiment, the Grewe transformation occurs in the presence of an acid anhydride as the cyclization additive. Further, the present invention is directed to processes for converting ?,?-bicyclic ketone compounds (e.g., by-products of the Grewe cyclization reaction) to ?,?-bicyclic ketone compounds, wherein the ?,?-bicyclic ketone compounds may be recovered to further undergo Grewe cyclization and form the nordihydrothebainone product.
    Type: Grant
    Filed: February 23, 2006
    Date of Patent: November 23, 2010
    Assignee: Mallinckrodt Inc
    Inventors: Peter Xianqi Wang, Frank W. Moser, Gary L. Cantrell, Jian Bao
  • Patent number: 7834184
    Abstract: Novel opiate intermediate compositions and methods of synthesis that include changing the substitution pattern on the aromatic ring of the pre-Grewe intermediate are provided. The intermediates are morphinane derivatives of formula (10), wherein X is a F or Cl and R is selected from the group consisting of an H, alkyl, aryl, acyl, formyl, COR?, CONHR?, COOR, Bn(benzyl), alkyl(methyl), and sulfonamide SO2CH2COPh.
    Type: Grant
    Filed: October 21, 2005
    Date of Patent: November 16, 2010
    Assignee: Mallinckrodt Inc.
    Inventors: Peter Xianqi Wang, Frank W. Moser, Gary L. Cantrell, Daniel P. Magparangalan
  • Publication number: 20100273827
    Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
    Type: Application
    Filed: December 19, 2008
    Publication date: October 28, 2010
    Inventor: Jag Paul Heer
  • Publication number: 20100234417
    Abstract: A hetero-dimeric or hetero-oligomeric receptor, comprising at least one thyrotropin releasing hormone receptor subunit associated with at least one orexin receptor subunit.
    Type: Application
    Filed: November 9, 2007
    Publication date: September 16, 2010
    Applicant: DIMERIX BIOSCIENCE PTY LTD.
    Inventors: Kevin Donald George Pfleger, Ruth Marie Seeber, Heng See Boon, Karin Ann Eidne
  • Publication number: 20100222299
    Abstract: The present invention involves tetrahydroisoquinoline compounds and their use in the inhibition and/or prevention of tumor growth.
    Type: Application
    Filed: March 27, 2008
    Publication date: September 2, 2010
    Applicant: Sterix Limited
    Inventors: Fabrice Jourdan, Meriel Kimberley, Matthew Leese, Barry Victor Lloyd Potter, Atul Purohit, Michael John Reed
  • Publication number: 20100160289
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.
    Type: Application
    Filed: December 15, 2009
    Publication date: June 24, 2010
    Inventors: Mark J. Macielag, James J. McNally
  • Publication number: 20100144821
    Abstract: The invention is directed to compounds and methods for treating protein folder disorders. In certain embodiments the invention provides compounds and methods for treating neurodegenerative diseases such as Alzheimer's disease, tauopathy, cerebral amyloid angiopathy, Lewy body disease, dementia, Huntington's disease and prion-based spongiform encelopathy. The invention further provides compounds, methods and pharmaceutical compositions for inhibiting tau protein, A? protein or ?-synuclein protein aggregation.
    Type: Application
    Filed: November 19, 2007
    Publication date: June 10, 2010
    Applicant: Queen's University at Kingston
    Inventors: Michael D. Carter, Donald F. Weaver, Sheila Marie H. Jacobo, Erhu Lu, Fuye Gao
  • Publication number: 20100127618
    Abstract: There is provided an organic light-emitting device having an optical output with a high efficiency, a high luminance, and a long life.
    Type: Application
    Filed: May 16, 2008
    Publication date: May 27, 2010
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Hiroki Ohrui, Akihito Saitoh, Chika Negishi, Hironobu Iwawaki, Masanori Muratsubaki, Shinjiro Okada
  • Publication number: 20100120810
    Abstract: The present invention relates to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac GTPases (Rac1, Rac1b, Rac2 and/or Rac3).
    Type: Application
    Filed: July 11, 2008
    Publication date: May 13, 2010
    Inventors: Bertrand Leblond, Eric Beausoleil
  • Publication number: 20100120844
    Abstract: The present invention relates a specific tetrahydroisoquinoline compound which is useful as a chemokine receptor type 3 (CCR3) antagonist, and a pharmaceutical composition comprising the same as an active ingredient. The tetrahydroisoquinoline compound of the present invention is useful for the treatment or prevention of a disease in which CCR3 participates.
    Type: Application
    Filed: April 3, 2008
    Publication date: May 13, 2010
    Applicant: KOWA COMPANY, LTD.
    Inventors: Seiichi Sato, Junya Tagashira, Shunji Takemura, Yoshiharu Miyake, Tetsuya Ishikawa, Toshiharu Arai, Takahiro Ito, Takuya Hara