The Five-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/373)
  • Publication number: 20140005395
    Abstract: The present teachings provide a compound of Formula (I-B): wherein R1-R10 are as described herein; a pharmaceutically acceptable salt of the compound, a geometric isomer of the compound, or a pharmaceutically acceptable salt of the geometric isomer. Also described are methods of preparing the same, as well as methods for preparing vilazodone using the same.
    Type: Application
    Filed: July 1, 2013
    Publication date: January 2, 2014
    Inventor: Matthew Ronsheim
  • Patent number: 8604017
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: December 10, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Publication number: 20130324554
    Abstract: Disclosed herein is a stable amorphous form of vilazodone hydrochloride substantially free of crystalline forms, a process for the preparation, pharmaceutical compositions, and methods of treating thereof. Disclosed also herein are stable amorphous co-precipitates of vilazodone hydrochloride and a pharmaceutically acceptable excipient, methods for the preparation, pharmaceutical compositions, and method of treating thereof.
    Type: Application
    Filed: October 22, 2012
    Publication date: December 5, 2013
    Applicant: SYMED LABS LIMITED
    Inventors: Dodda MOHAN RAO, Aadepu JITHENDER
  • Patent number: 8598181
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: December 3, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
  • Patent number: 8598180
    Abstract: Compositions comprising tetrahydroindolone derivatives in which the tetrahydroindolone moiety is covalently linked to a substituted arylpiperazine moiety and methods for treating neurological and psychiatric conditions using such compositions are disclosed.
    Type: Grant
    Filed: August 6, 2010
    Date of Patent: December 3, 2013
    Assignee: Abraxis Bioscience, Inc.
    Inventors: David Reed Helton, David Brian Fick, Jason Paul Sharp, Ernest H. Pfadenhauer
  • Publication number: 20130296296
    Abstract: The present invention relates to compounds of formula (I), wherein R1 is heteroaryl or heterocyclyl, optionally substituted; R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocyclyl, C1-4alkylheterocyclyl, heterocyclyl-heteroaryl, aryl-heterocyclyl, carbocyclyl-heteroaryl, heterocyclyl-aryl, optionally substituted; R3 is hydrogen or C1-4alkyl, or R2 and R3 may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted; R4 is hydrogen, halogen, methyl or methoxy; to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders. The present invention further relates to new intermediates useful in the preparation thereof.
    Type: Application
    Filed: February 4, 2013
    Publication date: November 7, 2013
    Inventor: ASTRAZENECA AB
  • Publication number: 20130281451
    Abstract: A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.
    Type: Application
    Filed: April 3, 2013
    Publication date: October 24, 2013
    Applicant: ANNJI PHARMACEUTICAL CO., LTD.
    Inventors: Ji-Wang Chern, Ajit Dhananjay Jagtap, Hsiao-Chun Wang, Grace Shiahuy Chen
  • Publication number: 20130281430
    Abstract: The invention relates to new amino-indole-substituted imidazolyl-pyrimidines of formula 1 wherein R1, R2, R3, R4 and R5 are defined as in claim 1 and pharmaceutically acceptable salts thereof and the use of these compounds for the preparation of a medicament for treating a disease selected from asthma, COPD, rheumatoid arthritis, specific lymphomas and specific diseases of the nervous system.
    Type: Application
    Filed: April 17, 2013
    Publication date: October 24, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Georg DAHMANN, Horst DOLLINGER, Christian GNAMM, Dennis FIEGEN, Matthias HOFFMANN, Jasna KLICIC, David James LAMB, Andreas SCHNAPP
  • Publication number: 20130274260
    Abstract: This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic ?-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.
    Type: Application
    Filed: December 13, 2011
    Publication date: October 17, 2013
    Inventors: Gerard Griffioen, Tom Van Dooren, Verónica Rojas De La Parra, Sara Allasia, Arnaud Marchand, Amuri Kilonda, Patrick Chaltin
  • Publication number: 20130263390
    Abstract: The invention relates to 4-aminoindole derivatives of formula (I), and the addition salts thereof, mesomers thereof, isomers thereof and solvates thereof: and to their use for the oxidation dyeing of keratin fibres, and in particular of human keratin fibres such as the hair. The present invention makes it possible to achieve dark shades, natural shades and dark natural shades. The present invention also makes it possible to obtain powerful, chromatic, aesthetic, sparingly selective coloration of keratin fibres in varied shades, which is resistant to the various attacking factors to which the hair may be subjected. In particular, when the 4-aminoindole derivatives are combined with one or more heterocyclic oxidation bases, they make it possible to obtain a wide range of colours and coloration of keratin fibres that shows good chromaticity and good selectivity.
    Type: Application
    Filed: December 14, 2011
    Publication date: October 10, 2013
    Applicant: L'OREAL
    Inventors: Aziz Fadli, Fatima Makhlouf
  • Publication number: 20130259830
    Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed.
    Type: Application
    Filed: June 24, 2011
    Publication date: October 3, 2013
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Timothy Barden, Colleen Hudson, James Jia, Charles Kim, Regina Graul, Ara Mermerian, Joel Moore, Kevin Sprott, Yueh-tyng Chien
  • Publication number: 20130252969
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein one of R1 and R2 is H, and the other is selected from C1-8-alkyl, C3-6-cycloalkyl and C1-8-alkyl-C5-10-aryl; R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl, cyclohexyl and 1-methylcyclopentyl; R9 is selected from the following: wherein: R4 is selected from C1-8-alkyl and C3-8-cycloalkyl; G is selected from: CH, CMe and N; E is selected from: O, S, SO2, NH, NMe and N-oxide (N?O); J and R are independently selected from: CH, N and N-oxide (N?O); and R41 is selected from amino, methylamino, dimethylamino, isopropylamino, isopropyl(methyl)amino, cyclopropylamino, cyclopropyl(methyl)amino, cyclopentylamino, morpholino, piperidin-1-yl, piperidin-1-ylmethyl, morpholinomethyl, 4-methylpiperazin-1-yl, 4-(2-methoxyethyl)piperazin-1-yl, 1-morpholinoethyl, 1-(dimethylamino)ethyl, 1-(methylamino)ethyl, 4-fluoro-1-methylpyrrolidin-2-yl, 4,4-difluoropiperidin-
    Type: Application
    Filed: May 23, 2013
    Publication date: September 26, 2013
    Applicant: Amura Therapeutics Limited
    Inventors: Martin Quibell, John P. Watts
  • 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: 8524716
    Abstract: The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein R1; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
    Type: Grant
    Filed: December 23, 2008
    Date of Patent: September 3, 2013
    Assignee: Janssen R&D Ireland
    Inventors: Pierre Jean-Marie Bernard Raboisson, Lili Hu, Sandrine Marie Helene Vendeville, Origène Nyanguile, Abdellah Tahri
  • Publication number: 20130225818
    Abstract: The present invention relates, in a first aspect, to a process preparing vilazodone hydrochloride that comprises the reaction of 3-(4-chloro-1-hydroxy-butyl)-1H-indol-5-carbonitrile with 5-piperazin-1-yl-benzofuran-2-carboxylate methyl hydrochloride with the formation of a 1,4-piperazine, with subsequent dehydration, hydrogenation and treatment with ammonia, to obtain vilazodone in free base form that is then converted into the hydrochloride thereof.
    Type: Application
    Filed: April 2, 2013
    Publication date: August 29, 2013
    Applicant: ERREGIERRE S.P.A.
    Inventors: Massimo Ferrari, Daniele De Zani, Matteo Bonaldi
  • Patent number: 8518945
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X? and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: March 4, 2011
    Date of Patent: August 27, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert Than Hendricks, Johannes Hermann, Rama Kondru, Yan Lou, Stephen M. Lynch, Timothy D. Owens, Michael Soth
  • Publication number: 20130217650
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: November 15, 2012
    Publication date: August 22, 2013
    Applicant: Allergan, Inc.
    Inventor: Allergan, Inc.
  • Publication number: 20130217679
    Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
    Type: Application
    Filed: March 23, 2011
    Publication date: August 22, 2013
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, THE JOHNS HOPKINS UNIVERSITY
    Inventors: Donald J. Zack, Thomas Bannister, Tomas Vojkovsky, Zhiyong Yang, Cynthia Berlinicke
  • Publication number: 20130210834
    Abstract: Indirubin is the major active anti-tumor component of a traditional Chinese herbal medicine used for treatment of chronic myelogenous leukemia (CML). One aspect of the invention relates to a method of treating CML using at least one indirubin derivative compound or a pharmaceutical composition thereof. Indirubin derivatives (IRDs) potently inhibited Signal Transducer and Activator of Transcription 5 (Stat5) protein in CML cells. Compound IRD 810 inhibits Bcr-Abl/Stat5 or Src/Stat5 signaling in human KCL-22 CML and imatinib-resistant human KCL-22 CML cells expressing the T315I mutant Bcr-Abl. Previous studies indicate that SFKs cooperate with Bcr-Abl to activate downstream Stat5 signaling. Activation of Stat5 was strongly blocked by IRD 810 in CML cells. IRDs disclosed herein have been identified as potent inhibitors of Bcr-Abl/Stat5 or SFK/Stat5 signaling pathway.
    Type: Application
    Filed: February 4, 2013
    Publication date: August 15, 2013
    Applicant: CITY OF HOPE
    Inventor: CITY OF HOPE
  • Publication number: 20130210820
    Abstract: The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof.
    Type: Application
    Filed: January 30, 2013
    Publication date: August 15, 2013
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventor: ASTEX THERAPEUTICS LIMITED
  • Publication number: 20130203773
    Abstract: The present invention relates to a pharmaceutical dosage form delivering an immediate release profile containing the active substance 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate.
    Type: Application
    Filed: March 8, 2013
    Publication date: August 8, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Roman MESSERSCHMID, Peter LACH, Thorsten SOKOLIESS, Peter STOPFER, Dirk TROMMESHAUSER
  • Patent number: 8501780
    Abstract: The invention is directed to novel indazole carboxamide derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1 and Z are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Grant
    Filed: June 24, 2005
    Date of Patent: August 6, 2013
    Assignee: GlaxoSmithKline LLC
    Inventors: Jeffrey K. Kerns, Christine Edwards
  • Patent number: 8501745
    Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function in animals.
    Type: Grant
    Filed: September 1, 2010
    Date of Patent: August 6, 2013
    Assignee: Dart Neuroscience (Cayman) Ltd.
    Inventors: Terence P. Keenan, Alan P. Kaplan
  • Publication number: 20130190488
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Application
    Filed: December 12, 2012
    Publication date: July 25, 2013
    Applicant: Abbott Laboratories
    Inventor: Abbott Laboratories
  • Publication number: 20130172363
    Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
    Type: Application
    Filed: February 22, 2013
    Publication date: July 4, 2013
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventor: Galderma Research & Development
  • Publication number: 20130172365
    Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.
    Type: Application
    Filed: September 16, 2011
    Publication date: July 4, 2013
    Applicant: ADAMED SP. Z.O.O.
    Inventors: Marcin Kolaczkowski, Piotr Kowalski, Jolanta Jaskowska, Monika Marcinkowska, Katarzyna Mitka, Adam Bucki, Anna Wesolowska, Maciej Pawlowski
  • Patent number: 8470830
    Abstract: Compounds including 5-(Heterocyclyl)alkyl-N-(arylsulfonyl)indole, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them and a process for the preparation of these compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. These compounds are useful in the treatment of various disorders that are related to 5-HT6 receptor functions. Specifically, the compounds of this invention are also useful in the treatment of various CNS disorders, hematological disorders, eating disorders, diseases associated with pain, respiratory diseases, genito-urological disorders, cardiovascular diseases and cancer.
    Type: Grant
    Filed: July 26, 2007
    Date of Patent: June 25, 2013
    Assignee: Suven Life Sciences Limited
    Inventors: Venkata Satya Nirogi Ramakrishna, Rama Sastri Kambhampati, Jagadishbabu Konda, Prabhakar Kothmirkar, Venkateswarlu Jasti
  • Publication number: 20130158021
    Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.
    Type: Application
    Filed: October 26, 2012
    Publication date: June 20, 2013
    Applicant: Massachusetts Institute of Technology
    Inventor: Massachusetts Institute of Technology
  • Publication number: 20130158030
    Abstract: Provided are pyrrolyl substituted dihydroindol-2-one derivatives represented by formula (I), pharmaceutically acceptable salts or solvates of said derivatives, or solvates of said salts, which are effective tyrosine kinase inhibitors. Also provided are the preparation methods of the above compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in manufacturing drugs useful for the treatment or adjunctive treatment of tumors medicated by tyrosine kinases or proliferation or migration of tumor cells driven by tyrosine kinases in mammals (including human).
    Type: Application
    Filed: March 31, 2011
    Publication date: June 20, 2013
    Applicant: QILU PHARMACEUTICAL CO., LTD
    Inventors: Jingyi Wang, Chuanwen Fan, Long Zhang, Boyan Xu, Shousheng Yan, Zongru Guo, Minghui Zhang, Dong Lin, Zhantao Zhang, Haojie Zhou
  • Publication number: 20130137674
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Application
    Filed: January 25, 2013
    Publication date: May 30, 2013
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Janssen Pharmaceutica, NV
  • Patent number: 8450484
    Abstract: The present invention relates to diazabicyclo[2.2.1]hept-2-yl analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: May 28, 2013
    Assignee: GlaxoSmithKline, LLC
    Inventors: Michael Jonathan Bury, Mui Cheung, Hilary Schenck Eidam, Ryan Michael Fox, Krista Goodman, Eric Steven Manas
  • Patent number: 8450361
    Abstract: Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS.
    Type: Grant
    Filed: August 4, 2011
    Date of Patent: May 28, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
  • Publication number: 20130131060
    Abstract: The present invention relates to a compound of formula (I) wherein R1, R2 and R3 are as defined in the description and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula I and of the salts thereof. The compounds of formula I are suitable for treating tumors.
    Type: Application
    Filed: December 10, 2010
    Publication date: May 23, 2013
    Applicant: Johannes Gutenberg-Universität Mainz
    Inventors: Gerd Dannhardt, Jan-Peter Kramb, Stanislav Plutizki
  • Publication number: 20130123259
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: December 20, 2012
    Publication date: May 16, 2013
    Applicant: Allergan, Inc.
    Inventor: Allergan, Inc.
  • Publication number: 20130123232
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Application
    Filed: December 18, 2012
    Publication date: May 16, 2013
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventor: JANSSEN PHARMACEUTICA NV
  • Patent number: 8435984
    Abstract: The present invention provides tertiary amine substituted peptides of Formula (I) useful as inhibitors of HCV replication. The variables R and R1-R12 in Formula I are described herein. The invention also includes methods for preparing such compounds. The present invention further includes pharmaceutical compositions containing tertiary amine substituted peptides and methods for using such compounds, including methods for using the compounds to treat hepatitis C infection.
    Type: Grant
    Filed: February 26, 2008
    Date of Patent: May 7, 2013
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Atul Agarwal, Xiangzhu Wang, Dawei Chen, Suoming Zhang, Avinash Phadke
  • Patent number: 8435977
    Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, W and are defined herein.
    Type: Grant
    Filed: April 22, 2010
    Date of Patent: May 7, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Chris Flores, Marina Nelen, Erica Nulton, Stephen Prouty, Matthew Todd, Sui-Po Zhang
  • Patent number: 8435983
    Abstract: A method for synthesizing anti-leukemic epothilone analogues includes rigidifying a region between the macrolactone ring and the aromatic side-chain. The anti-leukemic compositions are non-naturally occurring epothilone analogue that are rigidified between the macrolactone ring and the aromatic side-chain.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: May 7, 2013
    Assignee: The University of Toledo
    Inventors: Viranga Tillekeratne, Richard A. Hudson, Mamoun Alhamadsheh
  • Publication number: 20130102616
    Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.
    Type: Application
    Filed: October 23, 2012
    Publication date: April 25, 2013
    Applicant: Merck Patentgesellschaft
    Inventor: Merck Patentgesellschaft
  • Publication number: 20130102776
    Abstract: An anticancer agent comprising a compound represented by the formula (I) [R1 represents hydrogen atom, hydroxyl group, a C1-6 alkoxy group and the like; R2 and R3 represents hydrogen atom, a halogen atom, a C1-6 alkyl group and the like; R4 represents hydrogen atom, a C1-6 alkyl group, a C1-6 alkylsulfonyl group and the like; R5 represents hydrogen atom or a substituent; represents a single bond or a double bond; R6 and R7 represents hydrogen atom, a C1-6 alkyl group and the like; R8 represents hydrogen atom, a C1-6 alkyl group and the like; A represents —O—, —S—, or —CH2—; D represents —C? or —N?; X represents methylene group, —O—, or —CO—; Q represents —N? or —C(R8)?; and Y represents a heterocyclic group or amino group], which shows a superior inhibitory activity against pim-1 kinase.
    Type: Application
    Filed: April 28, 2011
    Publication date: April 25, 2013
    Applicants: RIKEN, THE UNIVERSITY OF TOKYO
    Inventors: Tetsuo Nagano, Takayoshi Okabe, Hirotatsu Kojima, Nae Saito, Hirofumi Nakano, Masanao Abe, Akiko Tanaka, Teruki Honma, Shigeyuki Yokoyama, Keiko Tsuganezawa, Hitomi Yuki
  • Publication number: 20130102615
    Abstract: A compound of Formula I, including pharmaceutically acceptable salts thereof: wherein A is selected from the group of:
    Type: Application
    Filed: April 11, 2012
    Publication date: April 25, 2013
    Inventors: Nicholas A. Meanwell, Tao Wang, Zhongxing Zhang, Lawrence G. Hamann, John F. Kadow
  • Patent number: 8420632
    Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: April 16, 2013
    Assignee: Galderma Research & Developlment
    Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marléne Schuppli
  • Publication number: 20130081213
    Abstract: The present invention relates to a cationic 6-aminoindoline of general formula (I), the addition salts thereof with an acid and the solvates thereof: the present invention is also directed towards a method for synthesizing this cationic 6-aminoindoline, the compositions, the uses, the hair dyeing methods and the devices using this cationic 6-aminoindoline.
    Type: Application
    Filed: March 2, 2011
    Publication date: April 4, 2013
    Inventor: Aziz Fadli
  • Publication number: 20130065882
    Abstract: This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A1 represents a nitrogen atom or C—R3d wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R1 represents H or a C1-8 alkyl group; R2 represents H, a halogen, a C1-8 alkoxy
    Type: Application
    Filed: October 3, 2012
    Publication date: March 14, 2013
    Inventors: Nobuo Machinaga, Shin Iimura, Yoshiyuki Yoneda, Jun Chiba, Fumihito Muro, Hideko Hoh, Atsushi Nakayama
  • Publication number: 20130064770
    Abstract: The present invention relates to radiodiagnostic compounds, methods of making those compounds, and methods of use thereof as imaging agents for preferably a HA serotonin 5-HT1A receptor for use in PET or SPECT, preferably PET. Compositions comprising an imaging-effective amount of radiolabeled compounds are also disclosed. The present invention also relates to non-radiolabeled compounds, methods of making those compounds, and methods of use thereof to treat various neurological and/or psychiatric disorders.
    Type: Application
    Filed: May 26, 2011
    Publication date: March 14, 2013
    Applicant: GE HEALTHCARE LIMITED
    Inventors: Ian Martin Newington, Duncan George Wynn, Robert James Domett Nairne, Benedicte Guilbert, Subrata Mandal, Jinto Jose, Sunderaraman Varadarajan, Chitralekha Rangaswamy, Helen Betts, Rebecca Davis
  • Publication number: 20130052138
    Abstract: The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.
    Type: Application
    Filed: March 27, 2012
    Publication date: February 28, 2013
    Applicant: Vanderbilt University
    Inventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
  • Patent number: 8383619
    Abstract: The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof; wherein either R1 is R1a and R2 is R2a; or R1 is R1b and R2 is R2b; provided that in each case at least one of R1 and R2 is other than hydrogen; R1a and R2a are the same or different and each is selected from hydrogen, C1-4 alkyl, C2-4 alkenyl and C2-4 alkynyl wherein the C1-4 alkyl is optionally substituted by C1-2 alkoxy; R1b and R2b are the same or different and are selected from hydrogen, C(O)NR4R5, C(O)R6 and C(O)OR6 where R6 is C1-4 alkyl, R4 and R5 are both C1-4 alkyl, or NR4R5 forms a 4 to 7 membered saturated heterocyclic ring optionally containing a second heteroatom ring member selected from O, N or S and oxidized forms of N and S, the heterocyclic ring being optionally substituted by one or two C1-4 alkyl groups and/or one or two oxo groups; and R3 is a group D: wherein the asterisk denotes the point of attachment to the isoindoline ring; but excluding acetic acid 5-acetoxy-4-isopro
    Type: Grant
    Filed: October 12, 2010
    Date of Patent: February 26, 2013
    Assignee: Astex Therapeutics Limited
    Inventors: Martyn Frederickson, Marian Williams
  • Publication number: 20130035329
    Abstract: Compounds and compositions comprising compounds useful in the treatment of cancer are described herein.
    Type: Application
    Filed: June 8, 2012
    Publication date: February 7, 2013
    Inventors: Jeffrey O. Saunders, Francesco G. Salituro
  • Patent number: 8367664
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: January 23, 2007
    Date of Patent: February 5, 2013
    Assignee: Allergan, Inc.
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
  • Patent number: 8367653
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: April 22, 2010
    Date of Patent: February 5, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark MacIelag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu