Benzene Ring Containing Patents (Class 514/595)
  • Patent number: 10137123
    Abstract: Methods are provided of treating cardiac hypertrophy in a mammalian subject comprising administering to the subject an anti-hypertrophic effective amount of an ion channel TR-PV1 inhibitor. The methods include treatment of a symptom of cardiac hypertrophy in the subject comprises cardiac remodeling, cardiac fibrosis, apoptosis, hypertension, or heart failure.
    Type: Grant
    Filed: May 1, 2017
    Date of Patent: November 27, 2018
    Assignee: University of Hawaii
    Inventor: Alexander Stokes
  • Patent number: 9737496
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Grant
    Filed: September 8, 2016
    Date of Patent: August 22, 2017
    Assignee: ACUCELA INC.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Thomas L. Little, Jr., Anna Gall, Feng Hong
  • Patent number: 9670150
    Abstract: The present invention relates to (2-ureidoacetamido)alkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2.
    Type: Grant
    Filed: April 16, 2013
    Date of Patent: June 6, 2017
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Tien Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 9084786
    Abstract: Methods are provided of treating cardiac hypertrophy in a mammalian subject comprising administering to the subject an anti-hypertrophic effective amount of an ion channel TR-PV1 inhibitor. The methods include treatment of a symptom of cardiac hypertrophy in the subject comprises cardiac remodeling, cardiac fibrosis, apoptosis, hypertension, or heart failure.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: July 21, 2015
    Assignee: University of Hawaii
    Inventor: Alexander Stokes
  • Publication number: 20150132408
    Abstract: The present invention provides sorafenib analogs for use in a method of treating a disease mediated by p21, said method comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I. The present invention also provides methods of inhibiting p21 in a cell comprising contacting the cell with an effective amount of a compound of formula I.
    Type: Application
    Filed: June 20, 2013
    Publication date: May 14, 2015
    Inventors: Robert H. Weiss, Bruce D. Hammock, Hiromi Inoue, Sung Hee Hwang
  • Patent number: 9029401
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: May 12, 2015
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Publication number: 20150119396
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: April 30, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Publication number: 20150079177
    Abstract: The present invention provides combination therapy methods of treating proliferative diseases (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a second therapy which may include, for example, radiation, surgery, administration of chemotherapeutic agents, or combinations thereof. Also provided are methods of administering to an individual a drug taxane in a nanoparticle composition based on a metronomic dosing regime.
    Type: Application
    Filed: August 25, 2014
    Publication date: March 19, 2015
    Inventors: Neil P. DESAI, Patrick SOON-SHIONG, Tapas DE
  • Patent number: 8952031
    Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: March 5, 2012
    Date of Patent: February 10, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
  • Publication number: 20140322304
    Abstract: Anti-cancer compositions and methods are described herein. In particular, compositions including one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described. Methods for treatment of pathological conditions particularly cancer, in a subject using one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described herein.
    Type: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Inventors: Gavin P. Robertson, Raghavendra Gowda Chandagalu D., Subbarao V. Madhunapantula, Gajanan S. Inamdar, Omer F. Kuzu
  • Publication number: 20140288077
    Abstract: In one aspect, the invention relates to substituted 4-phenoxyphenol analogs, derivatives thereof, and related compounds, which are useful as inhibitors of proliferating cell nuclear antigen (PCNA); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating hyperproliferative disorders associated with PCNA using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: July 5, 2012
    Publication date: September 25, 2014
    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL
    Inventors: Naoaki Fujii, Marcelo Actis, Chandanamali Punchihewa, Michele Connelly, Sean Wu
  • Publication number: 20140256729
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: September 11, 2014
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Publication number: 20140171438
    Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.
    Type: Application
    Filed: December 9, 2013
    Publication date: June 19, 2014
    Applicant: CELLCEUTIX CORPORATION
    Inventors: Wenxi Pan, Haizhong Tang
  • Patent number: 8703822
    Abstract: The present invention relates to a method of removing undifferentiated stem cells and dedifferentiated stem cells from a sample of cells. The invention further relates to preventing dedifferentiation of differentiated cells. Both methods comprise of administering to said cells an effective amount of compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, n, p, Z and T are defined herein.
    Type: Grant
    Filed: June 11, 2010
    Date of Patent: April 22, 2014
    Assignee: Nanyang Polytechnic
    Inventors: Mark Richards, Chee Wee Phoon, Mun Kin Lee
  • Patent number: 8686042
    Abstract: The invention relates to urea derivatives of formula (I) as inhibitors of glycogen synthase kinase 3?, GSK-3, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which GSK-3 is involved, such as Alzheimer's disease or non-insulin dependent diabetes mellitus.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: April 1, 2014
    Assignee: Neuropharma, S.A.
    Inventors: Ana Martinez Gil, Miguel Medina Padilla, Mercedes Alonso Cascon, Ana Fuertes Huerta, Maria Luisa Navarro Rico, Maria Jose Perez Puerto, Ana Castro Morera, Ester Martin Aparicio
  • Publication number: 20140088156
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Application
    Filed: February 14, 2012
    Publication date: March 27, 2014
    Applicant: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Patent number: 8673953
    Abstract: Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an ? adrenergic receptor agonist selected from selective ?1 adrenergic receptor agonist, selective ?2 adrenergic receptor agonist, non-selective ?1/?2 adrenergic receptor agonist, agents with ?2 adrenergic receptor agonist activity and combinations thereof, in a pharmaceutically acceptable carrier in order to treat and improve the cosmetic appearance of hemorrhagic (purpuric) lesions in the skin.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: March 18, 2014
    Assignee: Allergan, Inc.
    Inventors: Stuart D. Shanler, Andrew Ondo
  • Patent number: 8642657
    Abstract: 4-(methylsulfonylamino)phenyl analogues as potent vanilloid receptor antagonists and pharmaceutical compositions comprising the same. The compounds are useful as analgesics to prevent, alleviate or treat pain diseases or inflammatory disease including pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease, inflammatory disease and urgent urinary incontinence.
    Type: Grant
    Filed: July 2, 2004
    Date of Patent: February 4, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Jee Woo Lee, Young Ho Kim, Hee Kim, Hyun Kyung Choi, Hee Jin Ha
  • Patent number: 8642576
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: February 4, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Patent number: 8633228
    Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(?G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: January 21, 2014
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
  • Publication number: 20130345255
    Abstract: Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, prodrugs, or combinations thereof, wherein X1, L, Rx, Ry, Rz, R1, R2, A, m, n, p, q, and r are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Application
    Filed: June 20, 2013
    Publication date: December 26, 2013
    Inventors: Arthur Gomtsyan, Jerome Daanen, Michael E. Kort, Philip R. Kym, Eric A. Voight, Kevin R. Woller
  • Publication number: 20130231377
    Abstract: Disclosed are pactamycin analogs, pharmaceutical compositions including the analogs, and methods of using the analogs, such as to inhibit tumor growth or a pathogenic infection such as a bacterial or parasitic infection. The pactamycin analogs have a general formula where R1 is H, lower aliphatic, amide, acyl, or aminoacyl; R2 is —C(O)NR8R9 where R8 and R9 independently are hydrogen or lower aliphatic, or R1 and R2 together form a cyclic structure; R3 and R4 independently are hydrogen, hydroxyl, or lower aliphatic, or R2 and R3 together form a cyclic structure; R5 is hydrogen or acyl; R6 and R7 independently are hydrogen, hydroxyl, halogen, lower aliphatic, or amino.
    Type: Application
    Filed: August 2, 2011
    Publication date: September 5, 2013
    Applicants: Oregon State University
    Inventor: Taifo Mahmud
  • Publication number: 20130184279
    Abstract: Compounds of formula Ia and Ib wherein A, B, C, R1 and R14 are described herein.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 18, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130165479
    Abstract: The present application is directed to compounds that are TRPV1 antagonictc and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.
    Type: Application
    Filed: December 6, 2012
    Publication date: June 27, 2013
    Applicant: ABBVIE, INC.
    Inventor: AbbVie, Inc.
  • Publication number: 20130158036
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: November 1, 2012
    Publication date: June 20, 2013
    Applicant: PANMIRA PHARMACEUTICALS, LLC
    Inventor: PANMIRA PHARMACEUTICALS, LLC
  • Patent number: 8465725
    Abstract: A manufacturing process for the preparation of radiolabeled compounds of formula (I) includes reacting compounds of formula (II) with a source of radionuclide of a halogen in the presence of an oxidant under acidic condition, wherein: *I is 123I, 124I, 125I or 131I; R is lower alkyl, optionally substituted with one or more fluorine atoms; Q is C(O), O, NR?, S, S(O)2, C(O)2, (CH2)p; Y is C(O), O, NR?, S, S(O)2, C(O)2, (CH2)p; R? is H, C(O), S(O)2, C(O)2; Z is H, C1-C4 alkyl, benzyl, substituted benzyl or trialkylsilyl; m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4, 5 or 6; and p is 0, 1, 2, 3, 4, 5 or 6.
    Type: Grant
    Filed: June 15, 2010
    Date of Patent: June 18, 2013
    Assignee: Molecular Insight Pharmaceuticlas, Inc.
    Inventors: John W. Babich, Craig Zimmerman, Kevin P. Maresca
  • Publication number: 20130065963
    Abstract: The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.
    Type: Application
    Filed: July 17, 2012
    Publication date: March 14, 2013
    Applicant: Georgetown University
    Inventors: Alan P. Kozikowski, Anatoly Dritschilo, Mira Jung, Pavel A. Petukhov, Bin Chen
  • Publication number: 20130053392
    Abstract: A carbonic anhydrase IX (CA IX) inhibitor which comprises a compound of general formula: R—NH—CX—NH—(CH2)n—Ar-Q-SO2—NH2 or a pharmaceutically-acceptable salt, derivative or prodrug thereof; wherein n=0, 1 or 2; Q is O or NH; X is O or S; and R comprises an organic substituent group.
    Type: Application
    Filed: February 14, 2011
    Publication date: February 28, 2013
    Inventors: Peter Ebbesen, Claudlu T. Supuran, Andrea Scozzafava, Erik Olai Pettersen, Kaye Williams, Ludwig Dubois, Philippe Lambin
  • Publication number: 20130053412
    Abstract: The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R1, R2, R3, LO, W, AR1, n are as defined in claim 1.
    Type: Application
    Filed: October 15, 2010
    Publication date: February 28, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Joerg Kley, Bradford S. Hamilton, Juergen Mack, Norbert Redemann, Corinna Schoelch
  • Publication number: 20130023463
    Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Application
    Filed: April 19, 2012
    Publication date: January 24, 2013
    Applicant: ABBOTT LABORATORIES
    Inventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
  • Publication number: 20120328679
    Abstract: Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or bioavailability in a use environment.
    Type: Application
    Filed: September 7, 2012
    Publication date: December 27, 2012
    Inventors: William J. Curatolo, Scott M. Herbig, James A. S. Nightingale
  • Publication number: 20120322761
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Application
    Filed: August 29, 2012
    Publication date: December 20, 2012
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Publication number: 20120322805
    Abstract: A solid composition of a low-solubility drug and a concentration-enhancing polymer has a portion of the drug in a semi-ordered state.
    Type: Application
    Filed: August 23, 2012
    Publication date: December 20, 2012
    Applicant: BEND RESEARCH, INC.
    Inventors: Walter C. Babcock, William B. Caldwell, Marshall D. Crew, Dwayne T. Friesen, Ravi M. Shanker, Daniel T. Smithey
  • Publication number: 20120322877
    Abstract: The invention provides for novel (bis)urea and (bis)thiourea compounds which are inhibitors of lysine-specific demethylase 1 (LSD1). Such compounds may be used to treat disorders, including cancer.
    Type: Application
    Filed: August 18, 2010
    Publication date: December 20, 2012
    Inventors: Robert A. Casero, Patrick M. Woster
  • Patent number: 8329745
    Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules of the general formula: Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.
    Type: Grant
    Filed: September 6, 2011
    Date of Patent: December 11, 2012
    Assignee: Board of Regents, The University of Texas System
    Inventors: Patrcik G. Harran, Michael S. Brown, Joseph L. Goldstein, Jing Yang, Tong-Jin Zhao
  • Patent number: 8304403
    Abstract: Compounds of formula Ia and Ib and wherein A, B, C and R1 are described herein.
    Type: Grant
    Filed: June 10, 2010
    Date of Patent: November 6, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Patent number: 8247454
    Abstract: A liquid antibacterial soap comprising trichlorocarbanilide, wherein the composition includes, 0.1-5 wt. % trichlorocarbanilide, 0-40 wt. % water, 0.1-40 wt. % of a surfactant or mixture of surfactants, 10-60 wt. % of lower glycols to render the composition visually clear and stable, and 0.1-10 wt. % of a mixture of additional adjuvant ingredients.
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: August 21, 2012
    Assignee: The Dial Corporation
    Inventors: Timothy J. Taylor, Priscilla S. Fox
  • Patent number: 8222451
    Abstract: The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.
    Type: Grant
    Filed: October 25, 2010
    Date of Patent: July 17, 2012
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Anatoly Dritschilo, Mira Jung, Pavel A. Petukhov, Bin Chen
  • Publication number: 20120165360
    Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: March 5, 2012
    Publication date: June 28, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
  • Patent number: 8173841
    Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: May 8, 2012
    Assignee: Xention Limited
    Inventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
  • Publication number: 20120088837
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
    Type: Application
    Filed: December 8, 2011
    Publication date: April 12, 2012
    Inventors: Robert Greenhouse, Ralph New Harris, III, Saul Jaime-Figueroa, James M. Kress, David Bruce Repke, Russell Stephen Stabler
  • Patent number: 8153686
    Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: April 10, 2012
    Assignee: Theravance, Inc.
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
  • Publication number: 20120083532
    Abstract: The present invention relates to the use of a compound represented by the general formula (I), and pharmaceutically acceptable salts thereof, wherein: n is an integer from 2 to 5; p is an integer from 0 to 4; R1 is selected from the group consisting of a hydroxyl group, an alkoxy group, a thiol group, a thioether group, and an amino group, wherein at least two of R1 is a hydroxyl group, a thiol group or an amino group, with the proviso that wherein n is 2, R1 is not on the carbon-2 position and the carbon-5 position of the phenyl group; R2 and R3 are independently a methylene group or a nucleophile, with the proviso that at least one of R2 and R3 is a nucleophile group; Z is an oxygen (O) atom or sulfur (S) atom; T is hydrogen or an optionally substituted aliphatic group; in the manufacture of a medicament for treating a patient in need of cell therapy.
    Type: Application
    Filed: June 11, 2010
    Publication date: April 5, 2012
    Inventors: Mark Richards, Chee Wee Phoon, Mun Kin Lee
  • Patent number: 8114898
    Abstract: Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an ? adrenergic receptor agonist selected from selective ?1 adrenergic receptor agonist, selective ?2 adrenergic receptor agonist, non-selective ?1/?2 adrenergic receptor agonist, agents with ?2 adrenergic receptor agonist activity and combinations thereof, in a pharmaceutically acceptable carrier in order to treat and improve the cosmetic appearance of hemorrhagic (purpuric) lesions in the skin.
    Type: Grant
    Filed: November 17, 2008
    Date of Patent: February 14, 2012
    Assignee: Allergan, Inc.
    Inventors: Stuart D. Shanler, Andrew Ondo
  • Patent number: 8106221
    Abstract: The present invention is directed to aspartic protease inhibitors. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: January 31, 2012
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: John J. Baldwin, Salvacion Cacatian, David A. Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Alexey V. Ishchenko, Lanqi Jia, Gerard McGeehan, Robert D. Simpson, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Jing Yuan, Wei Zhao, Linghang Zhuang
  • Patent number: 8013015
    Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.
    Type: Grant
    Filed: October 1, 2009
    Date of Patent: September 6, 2011
    Assignee: Board of Regents, The University of Texas System
    Inventors: Patrcik G. Harran, Michael S. Brown, Joseph L. Goldstein, Jing Yang, Tong-Jin Zhao
  • Patent number: 7981923
    Abstract: Compounds of the formula I, II or III: or pharmaceutically acceptable salts thereof, wherein m, n, q, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formulas I-III.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: July 19, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Ralph New Harris, III, James M. Kress, David Bruce Repke, Russell Stephen Stabler
  • Publication number: 20110172174
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Application
    Filed: October 31, 2007
    Publication date: July 14, 2011
    Inventors: Niels H. Andersen, Jason Bowman, Alice Erwin, Eric Harwood, Toni Kline, Khisimuzi Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • Publication number: 20110152263
    Abstract: A composition for use in inhibiting the binding of a Norovirus to the histo-blood group antigen on the surface of epithelia. The composition contains a therapeutically effective amount of a binding-inhibiting compound selected from Compounds 1 through 15, and at least one diluent, carrier or excipient. The Compounds competitively bind a Norovirus that has the capability of binding with the histo-blood group antigens of secretor blood type, including A, B, AB, and O blood types. The compositions can be administered to a human prior to or after infection by a Norovirus, to prevent or ameliorate an infection.
    Type: Application
    Filed: November 15, 2007
    Publication date: June 23, 2011
    Inventor: Xi JIANG
  • Patent number: 7964642
    Abstract: The invention relates to compounds of formula (I), wherein R, R1, R2, X and n are as defined in the description, and their use for the preparation of pharmaceutical compositions for the treatment of inflammatory states.
    Type: Grant
    Filed: June 16, 2005
    Date of Patent: June 21, 2011
    Assignee: Pharmeste S.R.L.
    Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti