1,2,3-triazoles (including Hydrogenated) Patents (Class 548/255)
Polycyclo heterocyclic ring system containing ring oxygen (Class 548/256)
Polycyclo ring system having the triazole ring as one of the cyclos (Class 548/257)
  • Purification Strategy for Direct Nucleophilic Procedures
    Publication number: 20110112293
    Abstract: The present invention provides novel and advantageous processes for preparing and purifying chemical compounds such as pharmaceuticals. The processes comprise a nucleophilic substitution reaction with a moiety X wherein the leaving group L of a substrate S in the reaction is covalently attached to a purification moiety M. This concept offers a convenient and lime-saving way to purity the desired product S-X from non-reacted precursors S-L-M and by-products L-M.
    Type: Application
    Filed: April 9, 2009
    Publication date: May 12, 2011
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: John Cyr, Ananth Srinivasan, Mathias Berndt, Keith Graham, Dae Yoon Chi, Byoung Se Lee, So Young Chu, Song-Yi Lim, Sang Ju Lee, Jin-Sook Ryu, Seung Jun Oh
  • INHIBITORS OF JANUS KINASES
    Publication number: 20110112081
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Application
    Filed: July 1, 2009
    Publication date: May 12, 2011
    Inventors: Kevin Wilson, Gabriela de Almeida, Andrew Haidle, Kaleen Konrad, Michelle Machacek, Ann Zabierek
  • Pyrrolopyrazine kinase inhibitors
    Patent number: 7939531
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R 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: February 20, 2009
    Date of Patent: May 10, 2011
    Assignee: Roche Palo Alto
    Inventors: Joe Timothy Bamberg, Mark Bartlett, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, Jaehyeon Park, David Bernard Smith, Michael Soth, Hanbiao Yang, Calvin Wesley Yee
  • UV-ABSORBERS FOR OPHTHALMIC LENS MATERIALS
    Publication number: 20110105765
    Abstract: 1,4-disubstituted-1,2,3-triazole UV absorbing monomers are disclosed. The UV absorbers are particularly suitable for use in intraocular lens materials.
    Type: Application
    Filed: January 11, 2011
    Publication date: May 5, 2011
    Applicant: Alcon, Inc.
    Inventor: Douglas C. Schlueter
  • Copper-catalysed ligation of azides and acetylenes
    Publication number: 20110105764
    Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting an organic azide and a terminal alkyne with a source of reactive Cu(I) ion for a time sufficient to form by cycloaddition a 1,4-disubstituted 1,2,3-triazole. The source of reactive Cu(I) ion can be, for example, a Cu(I) salt or copper metal. The process is preferably carried out in a solvent, such as an aqueous alcohol. Optionally, the process can be performed in a solvent that comprises a ligand for Cu(I) and an amine.
    Type: Application
    Filed: July 26, 2010
    Publication date: May 5, 2011
    Applicant: The Scripps Research Institute
    Inventors: K. Barry Sharpless, Valery Fokin, Vsevold A. Rostovtsev, Luke Green, Fahmi Himo
  • NEW HSL INHIBITORS USEFUL IN THE TREATMENT OF DIABETES
    Publication number: 20110092512
    Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof. The are useful as HSL inhibitors and may, for example, be used in treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, and obesity.
    Type: Application
    Filed: October 8, 2010
    Publication date: April 21, 2011
    Inventors: Jean Ackermann, Stephan Brugger, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch, Stanley Wertheimer
  • NOVEL IMAGING AGENTS FOR DETECTING NEUROLOGICAL DYSFUNCTION
    Publication number: 20110091382
    Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.
    Type: Application
    Filed: February 17, 2009
    Publication date: April 21, 2011
    Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Qianwa Liang, Brian A. Duclos, Wei Zhang, Peter J.H. Scott, Kai Chen, Zhiyong Gao, Tieming Zhao, Vani P. Mocharla, Dhanalakshmi Kasi, Gang Chen, Eric Wang, Anjana Sinha, Chunfang Xia, Henry Clifton Padgett, Farhad Karimi
  • Triazolone derivatives
    Patent number: 7928228
    Abstract: A Compound represented by the following general formula (1): wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen or salts thereof or hydrates of the foregoing.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: April 19, 2011
    Assignees: Eisai Co., Ltd., Eisai R&D Management Co., Ltd.
    Inventors: Richard Clark, Fumiyoshi Matsuura, Kazunobu Kira, Shinsuke Hirota, Hiroshi Azuma, Tadashi Nagakura, Tatsuo Horizoe, Kimiyo Tabata, Kazutomi Kusano, Takao Omae, Atsushi Inoue
  • NOVEL CURCUMIN DERIVATIVE
    Publication number: 20110082295
    Abstract: To develop a highly safe measure to treat Alzheimer's disease using a secretase-inhibiting substance, there is provided a compound represented by the following general formula (I) or a salt thereof: wherein A represents a phenyl group or the like, R1 represents a chlorine atom, a bromine atom, or a nitro group or the like, R2, R3, R4, and R5 each represent a hydrogen atom or the like, and L represents CH2—CH2 or CH?CH.
    Type: Application
    Filed: May 27, 2009
    Publication date: April 7, 2011
    Applicants: Tokyo Institute of Technology, Kyoto University
    Inventors: Hachiro Sugimoto, Takashi Takahashi, Ichiro Hijikuro, Michiaki Okuda
  • Therapeutic compounds
    Patent number: 7919488
    Abstract: The present invention provides compounds of formula (I), or pharmaceutically acceptable salts or solvates thereof, methods for their preparation, methods for their use, and pharmaceutical formulations comprising them.
    Type: Grant
    Filed: June 28, 2007
    Date of Patent: April 5, 2011
    Assignee: Pfizer Inc.
    Inventors: Simon Paul Planken, Scott Channing Sutton, Rongliang Chen
  • UV-absorbers for ophthalmic lens materials
    Patent number: 7909458
    Abstract: 1,4-disubstituted-1,2,3-triazole UV absorbing monomers are disclosed. The UV absorbers are particularly suitable for use in intraocular lens materials.
    Type: Grant
    Filed: April 29, 2008
    Date of Patent: March 22, 2011
    Assignee: Alcon, Inc.
    Inventor: Douglas C. Schlueter
  • POLYETHER POLYOL DENDRON CONJUGATES WITH EFFECTOR MOLECULES FOR BIOLOGICAL TARGETING
    Publication number: 20110065896
    Abstract: Subject of the present invention are polyether polyol dendron conjugates comprising a specific polyether polyol dendron moiety, at least one certain fluorescent effector molecule (E). Such polyether polyol dendron conjugates may be used for diagnostic and therapeutic purposes, whereby the optical properties of the at least one certain fluorescent effector molecule are enhanced due to the attachment to the polyether polyol dendron conjugate.
    Type: Application
    Filed: March 10, 2009
    Publication date: March 17, 2011
    Applicant: MIVENION GMBH
    Inventors: Kai Licha, Malte Bahner, Michael Schirner, Rainer Haag, Timm Heek, Monika Wyszogrodzka
  • HETEROCYCLIC COMPOUNDS AS FACTOR IXA INHIBITORS
    Publication number: 20110065682
    Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.
    Type: Application
    Filed: May 18, 2009
    Publication date: March 17, 2011
    Inventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu,, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick,, Liyuan Wang, Xiaobang Gao
  • DOUBLE-LABELLING AGENTS BASED ON VINYL SULPHONE
    Publication number: 20110065164
    Abstract: The invention relates to labelling agents containing a compound with two labelled molecules and a vinyl sulphone group. The invention also relates to the compounds, the method for obtaining these and the uses thereof in the marking of biomolecules and, more specifically, proteins.
    Type: Application
    Filed: February 19, 2009
    Publication date: March 17, 2011
    Applicant: Universidad De Granada
    Inventors: Francisco Santoyo Gonzalez, Fernando Hernández Mateo, Francisco Javier López Jaramillo, Julia Morales Sanfrutos, Rafael Salto Gonzáalez, Dolores Girón González
  • TRIAZOLE AMIDE DERIVATIVES FOR USE IN THERAPY
    Publication number: 20110065725
    Abstract: The invention relates to triazole amide derivatives of formula (I) for use in therapy, in particular for treating diseases and conditions mediated by antagonism of the mGluR5 receptor, in particular substance related disorders. The invention also relates to certain novel derivatives. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.
    Type: Application
    Filed: March 16, 2009
    Publication date: March 17, 2011
    Applicant: GLAXO GROUP LIMITED
    Inventors: Vincenzo Garzya, Stephen Paul Watson
  • Imidazoles and triazoles, their preparation, and their use as pharmaceutical compositions
    Patent number: 7906539
    Abstract: The present invention relates to imidazoles and triazoles of general formula wherein R1 to R4 and X are defined as in claims 1 to 8, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: March 15, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Leo Thomas, Mohammad Tadayyon
  • Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors
    Patent number: 7906556
    Abstract: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
    Type: Grant
    Filed: October 12, 2006
    Date of Patent: March 15, 2011
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: R. Jeffrey Neitz, Eric Tisdale, Barbara Jagodzinska, Anh Truong, Jay Tung
  • Novel compositions and processes for preparing 5-amino or substituted amino 1,2,3-triazoles and triazole orotate formulations
    Publication number: 20110060142
    Abstract: New polymorphs of 5-amino or substituted amino 1,2,3-triazole and substituted derivatives thereof, of orotates of the carboxyamidotriazoles, of formulations of the triazoles and orotic acid in the ratio of 1:1 to 1:4 (base:acid) and of safer processes of the preparation of the same are disclosed. The compounds are useful in the control and treatment of diseases including, but not limited to solid cancers, macular degeneration, retinopathy, chronic myeloid leukemia, AIDS and diseases which rely on aberrant signal transduction. The improved processes to prepare the orotate formulations use stable, efficient and safer starting azide intermediate materials in the synthesis of new polymorphs of carboxyamidotriazole.
    Type: Application
    Filed: September 3, 2010
    Publication date: March 10, 2011
    Inventor: Rashida A. Karmali
  • NEW CHEMICAL COMPOUNDS
    Publication number: 20110059938
    Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R2 to R4, L, Q and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: November 15, 2010
    Publication date: March 10, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Steffen STEURER, Peter ETTMAYER, Andreas MANTOULIDIS, Ioannis SAPOUNTZIS, Martin STEEGMAIER
  • NOVEL 1,2,3-TRIAZOLE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
    Publication number: 20110060017
    Abstract: This invention relates to novel 1,2,3-triazole derivatives, which are found to be modulators of the nicotinic acetyl-choline receptors. Due to their pharmacological profile, the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Application
    Filed: March 9, 2009
    Publication date: March 10, 2011
    Applicant: Neurosearch A/S
    Inventors: Antonio Nardi, Jeppe Kejser Christensen, Dan Peters
  • Hydroxamate-Based Inhibitors of Deacetylases
    Publication number: 20110060009
    Abstract: The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, R4, R5, ring A, and Z are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of use compounds of Formula I in treating pathologic conditions or disorders mediated wholly or in part by deacetylases.
    Type: Application
    Filed: August 27, 2010
    Publication date: March 10, 2011
    Inventors: Clinton A. BROOKS, Christine Hiu-Tung CHEN, Young Shin CHO, Lei JIANG, Gang LIU, Michael SHULTZ
  • Diaryl-substituted five-membered heterocycle derivative
    Patent number: 7902369
    Abstract: The present invention provides the compounds represented by formula (I): (I) or pharmaceutical salts thereof, wherein: X1 represents oxygen atoms and the like, X2 represents nitrogen atoms and the like, X3 represents nitrogen atoms and the like, X4 represents nitrogen atoms and the like, R1 represents formula (II-1): wherein X5 represents sulfur atoms and the like, A1 represents carbon atoms and the like, A2 represents nitrogen atoms and the like and A ring represents phenyl group and the like, having mGluR1 inhibiting effect, and being usefull for preventing or treating convulsion, acute pain, inflammatory pain, chronic pain, brain disorder such as cerebral infarction or transient ischemick attack, psychotic disorder such as schizophrenia, anxiety, drug dependence, Parkinson's disease, or gastrointestinal disorder.
    Type: Grant
    Filed: March 7, 2005
    Date of Patent: March 8, 2011
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Yukari Hirata, Satoru Ito, Hiroshi Kawamoto, Toshifumi Kimura, Yasushi Nagatomi, Hisashi Ohta, Akio Sato, Atsushi Satoh, Gentaroh Suzuki
  • Pyrrolopyrazine kinase inhibitors
    Patent number: 7902197
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R 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: February 20, 2009
    Date of Patent: March 8, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Todd Richard Elworthy, Robert Than Hendricks, Rama K. Kondru, Yan Lou, Timothy D. Owens, Michael Soth, Hanbiao Yang
  • DENDRIMERS WITH INTERIOR AND EXTERIOR FUNCTIONALITIES COMPRISING OF AZIDE OR ALKYNE GROUPS FOR POST-FUNCTIONALIZATION BY THE HUISGEN CLICK CYCLOADDITION
    Publication number: 20110052696
    Abstract: A dendritic structure includes a core and repeating units, wherein the repeating units comprise units of the type ABxCy, wherein x is 2, 3, or 4, wherein y is 1, 2, or 3, wherein C is selected from the group consisting of azides and alkynes, and wherein every repeating unit is bound to at least one other unit with at least one bond selected from the group consisting of the group consisting of an ester, an amide, a thioether, an ether, a urethane, an amine, and an imine. Advantages include that a “one-pot” growth of the dendritic structure is possible. It is possible to have more functional groups in a dendritic structure. It is possible to add different functional groups simultaneously both to an inner layer and to an outer layer in a dendritic structure.
    Type: Application
    Filed: May 6, 2009
    Publication date: March 3, 2011
    Applicant: POLYMER FACTORY SWEDEN AB
    Inventors: Anders Hult, Michael Malkoch, Per Antoni
  • CHEMICAL MOLECULES THAT INHIBIT THE SLICING MECHANISM FOR TREATING DISEASES RESULTING FROM SPLICING ANOMALIES
    Publication number: 20110053975
    Abstract: The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.
    Type: Application
    Filed: January 12, 2009
    Publication date: March 3, 2011
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS, INSTITUT CURIE, UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUES
    Inventors: Jamal Tazi, David Grierson, Florence Mahuteau-Betzer, Pierre Roux
  • Process for preparing five-membered heterocyclyl tetracycline compounds and methods of use thereof
    Patent number: 7897784
    Abstract: The present invention provides processes for preparing a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein A is a pyrrole, tetrazole or triazole ring.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: March 1, 2011
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
  • Inhibition and dispersion of bacterial biofilms with imidazole-triazole derivatives
    Patent number: 7897631
    Abstract: Disclosure is provided for imidazole-triazole derivative compounds such as those given in Formulas (I)-(VI) that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.
    Type: Grant
    Filed: April 20, 2009
    Date of Patent: March 1, 2011
    Assignee: North Carolina State University
    Inventors: Christian Melander, Steven A. Rogers, Robert W. Huigens, III, Catherine S. Reed
  • FUNGICIDAL SUBSTITUTED AZOLES
    Publication number: 20110045101
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein J is Q2 or R1; X is N, CR2 or CQ3; Y is N or CR3; Z is N or CR4; and Q1, Q2, Q3, R1 R2 and R3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: May 7, 2009
    Publication date: February 24, 2011
    Applicant: E.I. Du Pont De Nemours and Company
    Inventors: Thomas Paul Selby, James Francis Bereznak, John Joseph Bisaha, Amy X. Ding, Mary Ann Hanagan, Jeffrey Keith Long, Andrew Edmund Taggi, Vijayagopal Gopalsamuthiram
  • Novel Imaging Agents for Detecting Neurological Dysfunction
    Publication number: 20110046378
    Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease
    Type: Application
    Filed: February 17, 2009
    Publication date: February 24, 2011
    Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.
    Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Qianwa Liang, Brian A. Duclos, Wei Zhang, Peter J.H. Scott, Kai Chen, Zhiyong Gao, Tieming Zhao, Vani P. Mocharla, Dhanalakshmi Kasi, Gang Chen, Eric Wang, Anjana Sinha, Chunfang Xia, Henry Clifton Padgett, Farhad Karimi
  • CCR10 ANTAGONISTS
    Publication number: 20110039851
    Abstract: The invention relates to a compound of formula (I): or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.
    Type: Application
    Filed: October 14, 2008
    Publication date: February 17, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Kaka Dey, Donghong Amy Gao, Daniel R. Goldberg, Alexander Heim-Riether, John Edward Mangette, Ingo Andreas Mugge, Roger John Snow, Alan David Swinamer, Jiang-Ping Wu, Zhaoming Xiong, Yu Yang
  • Fused Phenyl Amido Heterocyclic Compounds
    Publication number: 20110039821
    Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).
    Type: Application
    Filed: October 27, 2010
    Publication date: February 17, 2011
    Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukui, Ru Zhou
  • CRYSTALLINE FORMS OF RUFINAMIDE
    Publication number: 20110034523
    Abstract: Disclosed is a crystalline form of rufinamide selected from: a substantially anhydrous and approximately monosolvated with trifluoroacetic acid crystalline form, hereinafter designated as Form ?, and a crystalline form, hereinafter designated as Form ?, characterised by an XRPD spectrum as shown in FIG. 3, wherein the most intense peaks fall at 4.5, 9.0, 13.5, 18.0, 18.8, 19.5, 20.6, 24.6, 25.7, 26.5, 27.4, 27.9, 28.7, 30.0 and 31.8±0.2° in 2?.
    Type: Application
    Filed: August 3, 2010
    Publication date: February 10, 2011
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Gabriele RAZZETTI, Chiara VLADISKOVIC, Pietro ALLEGRINI
  • Dimeric small molecule potentiators of apoptosis
    Patent number: 7884211
    Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: February 8, 2011
    Assignee: Board of Regents, The University of Texas System
    Inventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
  • INDAZOLE DERIVATIVES
    Publication number: 20110028447
    Abstract: This invention relates to compounds, pharmaceutical compositions and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) wherein R1, R2 and R3 are as defined in this specification.
    Type: Application
    Filed: February 26, 2009
    Publication date: February 3, 2011
    Inventors: Ingrid Price Buchler, Michael Joseph Hayes, Shridhar Gajanan Hegde, Susan Landis Hockerman, Darin Eugene Jones, Steven Wade Kortum, Joseph Gerace Rico, Ruth Elizabeth TenBrink, Kun Ken Wu
  • FULLERENE THERAPIES FOR INFLAMMATION
    Publication number: 20110028522
    Abstract: Described herein are methods for treating inflammatory disorders. The methods comprise administering to a subject in need thereof a therapeutically effective amount of a synthetically modified fullerene.
    Type: Application
    Filed: March 3, 2009
    Publication date: February 3, 2011
    Applicant: LUNA INNOVATIONS INCORPORATED
    Inventors: Christopher L. Kepley, Robert P. Lenk, Stephen R. Wilson, Zhiguo Zhou, Darren K. MacFarland
  • ANTI-CANCER COMPOUNDS, SYNTHESIS THEREOF, AND METHODS OF USING SAME
    Publication number: 20110021574
    Abstract: Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to anti-cancer compounds, synthesis thereof, and methods of using same. Disclosed herein are various heterocyclic compounds and methods of using the novel anti-cancer compounds to inhibit the growth of a cancer cell, for instance a leukemia, non-small cell lung, central nervous system (CNS), skin, ovarian, renal, prostate, breast, or colon cancer cell. Other embodiments include methods of treating cancer in a subject, such as using the disclosed heterocyclic anti-cancer agents.
    Type: Application
    Filed: March 3, 2009
    Publication date: January 27, 2011
    Applicant: University of Notre Dame du Lac
    Inventors: Marvin J. Miller, Garrett C. Morasaki, Jonathan Stefely
  • INSECTICIDAL ARYLPYRROLINES
    Publication number: 20110003690
    Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which having excellent insecticidal activity and which can thus be used as an insecticide is provided.
    Type: Application
    Filed: January 29, 2009
    Publication date: January 6, 2011
    Applicant: BAY CROPSCIENCE AG
    Inventors: Ulrich Goergens, Yasushi Yoneta, Tetsuya Murata, Jun Mihara, Kei Domon, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara
  • Nitro-Imidazole Hypoxia Imaging Agent
    Publication number: 20110002850
    Abstract: The present invention relates to novel radioactively labeled bioreducible tracers of Formula I useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linker with pharmacokinetics enhancing substituents, and a radioisotope. The preferred in vivo imaging modality is positron emission tomography.
    Type: Application
    Filed: July 15, 2010
    Publication date: January 6, 2011
    Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.
    Inventors: Thomas Lee Collier, Brian A. Duclos, Umesh B. Gangadharmath, Zhiyong Gao, Farhad Karimi, Dhanalakshmi Kasi, Hartmuth C. Kolb, Qianwa Liang, Henry Clifton Padgett, Joseph C. Walsh, Tieming Zhao
  • Kinase inhibitors
    Patent number: 7863310
    Abstract: The present invention provides kinase inhibitors of Formula I:
    Type: Grant
    Filed: January 21, 2005
    Date of Patent: January 4, 2011
    Assignee: Eli Lilly and Company
    Inventors: Rosanne Bonjouklian, Robert Dean Dally, Alfonso de Dios, Mirian Filadelfa del Prado Catalina, Carmen Dominguez-Fernandez, Carlos Jaramillo Aguado, Beatriz Lopez de Uralde-Garmendia, Timothy Alan Shepherd
  • Inhibitors of Jun N-Terminal Kinase
    Publication number: 20100331335
    Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
    Type: Application
    Filed: February 5, 2010
    Publication date: December 30, 2010
    Inventors: Hing L. Sham, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
  • AMINOTRIAZOLE DERIVATIVES AS ALX AGONISTS
    Publication number: 20100331378
    Abstract: The invention relates to aminotriazole derivatives of formula (I), wherein A, E, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Application
    Filed: December 17, 2008
    Publication date: December 30, 2010
    Applicant: Actelion
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • N-(2-(HETARYL)ARYL) ARYLSULFONAMIDES AND N-(2-(HETARYL)HETARYL ARYLSULFONAMIDES
    Publication number: 20100331302
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: July 8, 2010
    Publication date: December 30, 2010
    Applicant: Chemocentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Process for making cytokine inhibiting compounds containing 4- and 5-imidazolyl rings and the intermediates thereof
    Patent number: 7858804
    Abstract: Disclosed are processes for making compounds containing 4- and 5-imidazolyl rings, also disclosed are the intermediates useful in the processes disclosed herein.
    Type: Grant
    Filed: April 16, 2007
    Date of Patent: December 28, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Rogelio Perez Frutos, Dhileepkumar Krishnamurthy, Nitinchandra D. Patel, Sonia Rodriguez, Chris Hugh Senanayake
  • 4-CARBOXYBENZYLAMINO DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
    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
  • 1,2,3-TRIAZOLES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS
    Publication number: 20100324104
    Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein R1, R2, and R3 are defined herein.
    Type: Application
    Filed: February 11, 2009
    Publication date: December 23, 2010
    Inventor: James J. Li
  • HEPATITIS C VIRUS INHIBITORS
    Publication number: 20100316607
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: June 15, 2010
    Publication date: December 16, 2010
    Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
  • Compositions and methods for establishing and maintaining stem cells in an undifferentiated state
    Publication number: 20100317100
    Abstract: The present invention embraces compositions and methods for establishing and maintaining stem cells and inhibiting stem cell differentiation using a selective Protein Kinase C (PKC) inhibitor.
    Type: Application
    Filed: June 11, 2010
    Publication date: December 16, 2010
    Inventors: Soumen Paul, Debasree Dutta, Soma Ray, Jeffrey Aube, Frank John Schoenen
  • Development of Molecular Imaging Probes for Carbonic Anhydrase-IX Using Click Chemistry
    Publication number: 20100317842
    Abstract: The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.
    Type: Application
    Filed: August 25, 2010
    Publication date: December 16, 2010
    Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.
    Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Dhanalakshmi Kasi, Vani P. Mocharla, Bing Wang, Umesh B. Gangadharmath, Brian A. Duclos, Kai Chen, Wei Zhang, Gang Chen, Henry Clifton Padgett, Farhad Karimi, Peter J.H. Scott, Zhiyong Gao, Qianwa Liang, Thomas Lee Collier, Tieming Zhao, Chunfang Xia
  • Cyclohexanesulfonyl derivatives as GLYT1 inhibitors to treat schizophrenia
    Patent number: 7851638
    Abstract: The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3 is an alkyl, cycloalkyl, cycloalkylalkyl, amino or heterocyclyl group; R4 and R5 are hydrogen or alkyl or form a cycloalkyl ring; A is O or N; and m is zero or one; as inhibitors of GlyT1 and thus as useful for treating or preventing diseases such as schizophrenia; with the provision of pharmaceutical compositions, first and second medical uses and methods of treatment.
    Type: Grant
    Filed: October 1, 2009
    Date of Patent: December 14, 2010
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Richard Thomas Lewis, Elizabeth Mary Naylor, Leslie Joseph Street
  • 3-Substituted Propanamine Compounds
    Publication number: 20100311789
    Abstract: Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof are disclosed. Pharmaceutical compositions containing the subject compounds are also disclosed. The subject compounds are useful for the treatment of diseases of the central nervous system, such as depression, anxiety and pain disorders.
    Type: Application
    Filed: June 3, 2009
    Publication date: December 9, 2010
    Inventors: Chun-Eung Park, Kyung-Hyun Min, Yong-Je Shin, Yu-Jin Shin, Hae-Jeong Yoon, Won Kim, Eun-Ju Ryu, Coo-Min Chung, Hui-Ho Kim