Polycyclo Ring System Which Contains The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/211.04)
  • Patent number: 10881669
    Abstract: Disclosed are inhibitors of the plasmodial surface anion channel (PSAC) inhibitors and the use thereof in treating or preventing malaria in an animal such as a human, comprising administering an effective amount of an inhibitor or a combination of inhibitors. An example of such an inhibitor is a compound of formula I, or a pharmaceutically acceptable salt thereof, wherein R1 to R7 are as described herein.
    Type: Grant
    Filed: May 21, 2018
    Date of Patent: January 5, 2021
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Sanjay A. Desai, Ajay D. Pillai
  • Patent number: 10869865
    Abstract: The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula I: Q-Y—R1—R2??(I), wherein Q, Y, R1, and R2 are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula I in combination with any one or more compounds represented by formulas II, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions.
    Type: Grant
    Filed: March 5, 2019
    Date of Patent: December 22, 2020
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Serv
    Inventor: Sanjay A. Desai
  • Patent number: 10300049
    Abstract: Myeloid differentiating agents can be used in the treatment of myeloid proliferative disorders.
    Type: Grant
    Filed: September 12, 2016
    Date of Patent: May 28, 2019
    Assignee: CASE WESTERN RESERVE UNIVERSITY
    Inventor: David Wald
  • Patent number: 10239840
    Abstract: Compounds of Formula I are disclosed and methods of treating viral infections with compositions comprising such compounds.
    Type: Grant
    Filed: September 14, 2016
    Date of Patent: March 26, 2019
    Assignee: VIIV HEALTHCARE UK LIMITED
    Inventors: Brian Alvin Johns, Lita S. Suwandi, Emile Johann Velthuisen, Jason Gordon Weatherhead
  • Patent number: 9827244
    Abstract: The present invention relates to a compound having the general formula (V), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
    Type: Grant
    Filed: June 1, 2016
    Date of Patent: November 28, 2017
    Assignees: F. Hoffmann-La Roche AG, Savira pharmaceuticals GmbH, European Molecular Biology Laboratory
    Inventors: Tanja Schulz-Gasch, Robert Weikert, Werner Neidhart, Helmut Buschmann, Oliver Szolar, Andrea Wolkerstorfer, Norbert Handler, Franz-Ferdinand Roch, Stephen Cusack
  • Patent number: 9695192
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: February 24, 2015
    Date of Patent: July 4, 2017
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Patent number: 9439894
    Abstract: Myeloid differentiating agents can be used in the treatment of myeloid proliferative disorders.
    Type: Grant
    Filed: September 17, 2013
    Date of Patent: September 13, 2016
    Assignee: Case Western Reserve University
    Inventor: David Wald
  • Patent number: 9359351
    Abstract: The present invention relates to a compound having the general formula (V), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
    Type: Grant
    Filed: July 7, 2015
    Date of Patent: June 7, 2016
    Assignees: F. Hoffmann-La Roche AG, Savira pharmaceuticals GmbH, European Molecular Biology Laboratory
    Inventors: Tanja Schulz-Gasch, Robert Weikert, Werner Neidhart, Helmut Buschmann, Oliver Szolar, Andrea Wolkerstorfer, Norbert Handler, Franz-Ferdinand Roch, Stephen Cusack
  • Patent number: 9187483
    Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: November 17, 2015
    Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: Irini Akritopoulou-Zanze, Wilfried Braje, Stevan W. Djuric, Noel S. Wilson, Sean C. Turner, Albert W. Kruger, Ana-Lucia Relo, Shashank Shekhar, Dennie S. Welch, Hongyu Zhao, Jorge Gandarilla, Alan F. Gasiecki, Huanqiu Li, Christina M. Thompson, Min Zhang
  • Patent number: 9079901
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: July 14, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Tetsuya Kobayashi, Dmitry Koltun, Gregory Notte, Eric Parkhill, Jeff Zablocki
  • Patent number: 8999967
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C.
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: April 7, 2015
    Assignee: Presidio Pharmaceuticals, Inc.
    Inventors: Leping Li, Min Zhong
  • Patent number: 8962610
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: February 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Patent number: 8835421
    Abstract: The present invention provides a compounds of general formula (8), (11) and (14), useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepine hybrids of general formula (8), (11) and (14).
    Type: Grant
    Filed: October 31, 2008
    Date of Patent: September 16, 2014
    Assignee: Council of Scientific and Industrial Research
    Inventors: Ahmen Kamal, Pogula Praveen Kumar, Bobburi Naga Seshadri, Kokkonda Sreekanth
  • Publication number: 20140228353
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 14, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvvajit Chakravarty
  • Publication number: 20140206666
    Abstract: Pharmaceutical compositions of the invention comprise sulfamoylbenzamide derivative useful as pregenomic RNA encapsidation inhibitors, useful for the treatment of Hepatitis B virus (HBV) infection.
    Type: Application
    Filed: June 29, 2012
    Publication date: July 24, 2014
    Applicants: Philadelphia Helath & Education Corporation d/b/a Drexel University College of Medicine, Institute for Hepatitis and Virus Research
    Inventors: Ju-Tao Guo, Xiaodong Xu, Timothy M. Block
  • Patent number: 8779154
    Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: September 25, 2007
    Date of Patent: July 15, 2014
    Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen
  • Publication number: 20140193475
    Abstract: The present invention provides an implantable article comprising an amorphous terpolymer and a semi-crystalline polymer. The amorphous terpolymer can be admixed with the semi-crystalline polymer or form a block copolymer with the semi-crystalline polymer.
    Type: Application
    Filed: March 10, 2014
    Publication date: July 10, 2014
    Applicant: Abbott Cardiovascular Systems Inc.
    Inventors: Mikael Trollsas, Michael Ngo, Florencia Lim
  • Publication number: 20140113891
    Abstract: Methods for treating cancer using compounds that inhibit human DNA ligases. Methods for using compounds that inhibit human DNA ligases to provide insights into the reaction mechanisms of human DNA ligases, for example to identify the human DNA ligase involved in different DNA repair pathways. Screening methods for compounds that inhibit human DNA ligases.
    Type: Application
    Filed: April 17, 2013
    Publication date: April 24, 2014
    Inventors: Alan E. Tomkinson, Xi Chen, Barbara Dziegielewska, Alexander D. Mackerell, Shijun Zhong, Gerald M. Wilson
  • Patent number: 8697863
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: April 15, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Elfatih Elzein, Dmitry Koltun, Xiaofen Li, Jeff Zablocki, Chandrasekar Venkataramani
  • Publication number: 20140088082
    Abstract: Disclosed are inhibitors of the plasmodial surface anion channel (PSAC) inhibitors and the use thereof in treating or preventing malaria in an animal such as a human, comprising administering an effective amount of an inhibitor or a combination of inhibitors. An example of such an inhibitor is a compound of formula I, or a pharmaceutically acceptable salt thereof, wherein R1 to R7 are as described herein.
    Type: Application
    Filed: December 3, 2013
    Publication date: March 27, 2014
    Applicant: The U.S.A., as represented by the Secretary, Department of Health and Human Services.
    Inventors: Sanjay A. Desai, Ajay D. Pillai
  • Publication number: 20140079736
    Abstract: The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula (I): Q-Y—R1—R2 (I), wherein Q, Y, R1, and R2 are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula (I) in combination with any one or more compounds represented by formulas II, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions.
    Type: Application
    Filed: April 11, 2012
    Publication date: March 20, 2014
    Applicant: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventor: Sanjay A. Desai
  • Publication number: 20140045821
    Abstract: Compounds according to Formula (I), are potent inhibitors of protein kinase D (pan-PKD) activity. PKD controls key signaling cascades in cells, affecting cell proliferation, gene transcription, and protein trafficking. Accordingly, pharmaceutically acceptable compositions of the inventive compounds are candidate therapeutics for pathological conditions conditioned by changes in PKD activity.
    Type: Application
    Filed: December 8, 2011
    Publication date: February 13, 2014
    Inventors: Peter Wipf, Qiming Jan Wang
  • Patent number: 8618090
    Abstract: Disclosed are inhibitors of the plasmodial surface anion channel (PSAC) inhibitors and the use thereof in treating or preventing malaria in an animal such as a human, comprising administering an effective amount of an inhibitor or a combination of inhibitors. An example of such an inhibitor is a compound of formula I, Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R7 are as described herein.
    Type: Grant
    Filed: July 15, 2009
    Date of Patent: December 31, 2013
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Sanjay A. Desai, Ajay D. Pillai
  • Patent number: 8586732
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: November 19, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Publication number: 20130296304
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C.
    Type: Application
    Filed: September 28, 2011
    Publication date: November 7, 2013
    Applicant: PRESIDIO PHARMACEUTICALS, INC.
    Inventors: Leping Li, Min Zhong
  • Publication number: 20130252930
    Abstract: Provided herein are inhibitors of CYP11B, CYP17, and/or CYP21 enzymes of Formula (Z), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), or (XVII). Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.
    Type: Application
    Filed: December 16, 2011
    Publication date: September 26, 2013
    Applicant: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Daniel Chu, Bing Wang, Tao Ye
  • Publication number: 20130217673
    Abstract: Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of mixed monoamine reuptake inhibitor locally at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least thirty days. In some embodiments, the relief can be for at least at least fifty days, at least one hundred days, at least one hundred and twenty days, at least one hundred and thirty, at least one hundred fifty days or at least one hundred and eighty days.
    Type: Application
    Filed: February 22, 2012
    Publication date: August 22, 2013
    Applicant: Warsaw Orthopedic, Inc
    Inventor: Jared T. Wilsey
  • Publication number: 20130210804
    Abstract: The present invention is directed to tricyclic compounds which are positive allosteric modulators of metabotropic glutamate receptors, particularly the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: October 20, 2011
    Publication date: August 15, 2013
    Inventors: Neville J. Anthony, Robert P. Gomez, Jing Li, Swati P. Mercer, Anthony J. Roecker, Craig A. Stump, Theresa M. Williams
  • Publication number: 20130171158
    Abstract: A method of treating or preventing an abnormality of glucose metabolism in a subject, the method comprising administering an antagonist of Inhibitor of Differentiation 1 (Id1) to the subject.
    Type: Application
    Filed: June 29, 2011
    Publication date: July 4, 2013
    Applicant: GARVAN INSTITUTE OF MEDICAL RESEARCH
    Inventors: Mia Akerfeldt, Ross Laybutt
  • Patent number: 8460704
    Abstract: The invention relates to an extended release pharmaceutical composition comprising nevirapine.
    Type: Grant
    Filed: June 4, 2008
    Date of Patent: June 11, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Michael L. Cappola, Svetlana Sienkiewicz, Glenn Charles Snow, Feng-Jing Chen
  • Publication number: 20130012492
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: June 29, 2012
    Publication date: January 10, 2013
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Publication number: 20120040961
    Abstract: The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), polo kinase 1, 2, 3, or 4, Ack1, Ack2, AbI, DCAMKL1, ABL1, AbI mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS 1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, AxI, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.
    Type: Application
    Filed: January 6, 2010
    Publication date: February 16, 2012
    Applicant: DANA-FARBER CANCER INSTITUTE
    Inventors: Nathanael S. Gray, Xianming Deng, Nicholas Paul Kwiatkowski
  • Publication number: 20120040962
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C.
    Type: Application
    Filed: March 25, 2010
    Publication date: February 16, 2012
    Applicant: PRESIDIO PHARMACEUTICALS, INC.
    Inventors: Leping Li, Min Zhong
  • Patent number: 8034804
    Abstract: The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4)-alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: October 11, 2011
    Assignee: N.V. Organon
    Inventors: Simon James Anthony Grove, Julia Adam-Worrall, Mingqiang Zhang, Robert Gilfillan
  • Patent number: 7994160
    Abstract: Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds: In formula I indicates a single bond or a double bond; X is O, S or N—R5; R1, R2 are independently selected from the group consisting of H, NH2, NH—C1-C6-alkyl, OH, ?O, (i.e.
    Type: Grant
    Filed: July 12, 2006
    Date of Patent: August 9, 2011
    Assignee: Abbott GmbH & Co. KG
    Inventors: Sean C. Turner, Margaretha Bakker, Roland Grandel, Michael Vierling
  • Publication number: 20110160184
    Abstract: Compounds the following formula: wherein Z is as described in the specification, pharmaceutically acceptable salts thereof, compositions comprising the same, and methods of treating bipolar disorder, an anxiety disorder, a mood disorder or schizophrenia or other psychotic disorder with said compounds.
    Type: Application
    Filed: June 18, 2009
    Publication date: June 30, 2011
    Applicant: ASTRAZENECA AB
    Inventors: Dean Brown, Steven Wesolowski, Dan Widzowski, James R. Damewood, M. Edward Pierson, Jr., Michael Wood, Philip Edwards, James Hulsizer, Ashokkumar Bhikkappa Shenvi, James Campbell Muir
  • Publication number: 20110152246
    Abstract: The embodiments provide compounds of the general Formulae I, II, III, IV, or V as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
    Type: Application
    Filed: December 16, 2010
    Publication date: June 23, 2011
    Applicant: InterMune, Inc.
    Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
  • Publication number: 20110144086
    Abstract: Disclosed are inhibitors of the plasmodial surface anion channel (PSAC) inhibitors and the use thereof in treating or preventing malaria in an animal such as a human, comprising administering an effective amount of an inhibitor or a combination of inhibitors. An example of such an inhibitor is a compound of formula I, Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R7 are as described herein.
    Type: Application
    Filed: July 15, 2009
    Publication date: June 16, 2011
    Applicant: The United States of America, as represented by the Secretary, Dept of Health and Human Service
    Inventors: Sanjay A. Desai, Ajay D. Pillai
  • Publication number: 20110130382
    Abstract: The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2-a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X1, X2, X3, X4, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
    Type: Application
    Filed: October 21, 2010
    Publication date: June 2, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Ying Wang, Jason T. Brewer, Irini Akritopoulou-Zanze, Stevan W. Djuric, Frauke Pohlki, Wilfried Braje, Ana-Lucia Relo
  • Publication number: 20110086842
    Abstract: The present invention encompasses compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1 and R3 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 pharmaceutical composition having the above-mentioned properties.
    Type: Application
    Filed: December 20, 2010
    Publication date: April 14, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heinz STADTMUELLER, Harald ENGELHARDT, Martin STEEGMAIER, Anke BAUM, Ulrich GUERTLER, Andreas SCHOOP, Jens Juergen QUANT, Flavio SOLCA, Rudolf HAUPTMANN, Ulrich REISER, Stephan Karl ZAHN, Lars HERFURTH
  • Publication number: 20110046111
    Abstract: The present invention provides a compound of general formula 5, useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepine hybrids of general formula (5): wherein n=3, 4, 5, 6, 8 and wherein R1 and R2 is selected from the group consisting of R1?H, R2?H or R1?CH3O, R2=CH3O or R1?CH3O and R2?C2H5O.
    Type: Application
    Filed: October 31, 2008
    Publication date: February 24, 2011
    Inventors: Ahmed Kamal, Bandari Rajendra Prasad, Adla Malla Reddy
  • Publication number: 20110021499
    Abstract: Urethral suppositories containing a mixed-activity anti-cholinergic drug and methods of use for treatment of over-active bladder are provided. Buffering drugs to pH near their pKas can result in a desired proportion of uncharged drug and can enhance absorption of the agents into urethral tissues.
    Type: Application
    Filed: July 22, 2009
    Publication date: January 27, 2011
    Inventors: Amie Ellen Franklin, Dennis H. Giesing
  • Publication number: 20110015158
    Abstract: The presently disclosed subject matter is described to metalloenzyme inhibitors having metal binding moieties linked to a targeting moiety through a linking group or a direct bond, method of screening for metalloenzyme inhibitors, and methods for treating a metalloenzyme related disorder by administering a metalloenzyme inhibitor to a subject in need of treatment thereof.
    Type: Application
    Filed: December 3, 2008
    Publication date: January 20, 2011
    Applicant: Viamet Pharmaceuticals, Inc.
    Inventors: Robert J. Schotzinger, William J. Hoekstra
  • Patent number: 7842686
    Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.
    Type: Grant
    Filed: January 21, 2009
    Date of Patent: November 30, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Corey Don Anderson, Andreas P. Termin, Pramod Joshi, Sara S. Hadida Ruah, Daniele Bergeron, Sanghee Yoo, Jingrong Cao
  • Publication number: 20100204201
    Abstract: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: April 15, 2010
    Publication date: August 12, 2010
    Inventors: Joseph P. Vacca, Linda S. Payne, Richard C.A. Isaacs
  • Patent number: 7772224
    Abstract: The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: August 10, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Daniel V. Paone, Anthony W. Shaw
  • Publication number: 20100137281
    Abstract: The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like, which is useful for the prophylaxis or treatment s of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases, cerebral apoplexy and the like and/or metabolic diseases such as hyperlipidemia, obesity, diabetes and the like, central nervous disorders such as cerebral infarction and the like, mental diseases such as dementia, depression and the like, and the like. A compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: May 20, 2008
    Publication date: June 3, 2010
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Takanobu Kuroita, Hideyuki Igawa, Hiroki Sakamoto, Kouhei Asano, Minoru Sasaki
  • Publication number: 20100022509
    Abstract: The present invention utilizes three families of bacterial enzymes, which play a key role in mycothiol biosynthesis. The three families are bacterial cysteine:glucosaminyl inositol ligases (MshC) with catalytic ligase activity for ligation of glucosaminyl inositol and cysteine, bacterial acetyl-CoA:Cys-GlcN-Ins acetyltransferases (MshD) with catalytic activity for addition of an acetyl group to Cys-GlcN-Ins and bacterial MshA glycosyltransferase with catalytic activity for production of GlcNAc-Ins. The invention provides methods for using the mycothiol biosynthesis ligases, acetyltransferases or glycosyltransferases in drug screening assays to determine compounds that inhibit activity. The invention also provides inhibitors of the production or activity of the enzymes of mycothiol biosynthesis, and use of the inhibitors for treating microbial infection.
    Type: Application
    Filed: June 7, 2007
    Publication date: January 28, 2010
    Inventors: Robert C. Fahey, Gerald L. Newton, Philong V. Ta, Nancy Buchmeier
  • Publication number: 20090318412
    Abstract: The present invention provides a tricyclic heterocyclic compound having a serotonin 5-HT2C receptor activation action and the like. A 5-HT2C receptor activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.
    Type: Application
    Filed: July 10, 2007
    Publication date: December 24, 2009
    Inventors: Takahiro Matsumoto, Izumi Kamo, Izumi Nomura
  • Patent number: 7569561
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R6, X and Y are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, as well as the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: August 4, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heinz Stadtmueller, Anke Baum, Guido Boehmelt, Harald Engelhardt, Jens Juergen Quant, Flavio Solca, Martin Steegmaier, Stephan Karl Zahn